TW201828941A - Composition of nasal drops or nasal spray characterized by containing a local anesthetic agent and hydrocortisone acetate at low concentration, thereby facilitating the improvement of rhinitis - Google Patents
Composition of nasal drops or nasal spray characterized by containing a local anesthetic agent and hydrocortisone acetate at low concentration, thereby facilitating the improvement of rhinitis Download PDFInfo
- Publication number
- TW201828941A TW201828941A TW106103828A TW106103828A TW201828941A TW 201828941 A TW201828941 A TW 201828941A TW 106103828 A TW106103828 A TW 106103828A TW 106103828 A TW106103828 A TW 106103828A TW 201828941 A TW201828941 A TW 201828941A
- Authority
- TW
- Taiwan
- Prior art keywords
- nasal
- local anesthetic
- hydrocortisone acetate
- mucosa
- spray
- Prior art date
Links
- 239000007922 nasal spray Substances 0.000 title claims abstract description 63
- 229940097496 nasal spray Drugs 0.000 title claims abstract description 55
- 239000003589 local anesthetic agent Substances 0.000 title claims abstract description 38
- 229960001067 hydrocortisone acetate Drugs 0.000 title claims abstract description 37
- ALEXXDVDDISNDU-JZYPGELDSA-N cortisol 21-acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O ALEXXDVDDISNDU-JZYPGELDSA-N 0.000 title claims abstract description 36
- 239000000203 mixture Substances 0.000 title claims description 38
- 206010039083 rhinitis Diseases 0.000 title abstract description 25
- 239000007923 nasal drop Substances 0.000 title abstract 4
- 229940100662 nasal drops Drugs 0.000 title abstract 4
- 210000002850 nasal mucosa Anatomy 0.000 claims abstract description 50
- 230000000694 effects Effects 0.000 claims abstract description 23
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 239000003755 preservative agent Substances 0.000 claims abstract description 12
- 230000002335 preservative effect Effects 0.000 claims abstract description 10
- 239000004094 surface-active agent Substances 0.000 claims abstract description 8
- 239000002562 thickening agent Substances 0.000 claims abstract description 8
- 210000004556 brain Anatomy 0.000 claims description 24
- 210000003928 nasal cavity Anatomy 0.000 claims description 21
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 16
- 230000001028 anti-proliverative effect Effects 0.000 claims description 13
- 210000003097 mucus Anatomy 0.000 claims description 13
- 230000028327 secretion Effects 0.000 claims description 13
- 208000003251 Pruritus Diseases 0.000 claims description 12
- 206010041232 sneezing Diseases 0.000 claims description 8
- 239000000872 buffer Substances 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 230000000295 complement effect Effects 0.000 claims description 5
- 230000009545 invasion Effects 0.000 claims description 5
- 230000000259 anti-tumor effect Effects 0.000 claims description 4
- 229960004311 betamethasone valerate Drugs 0.000 claims description 3
- SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 claims description 3
- 210000004877 mucosa Anatomy 0.000 claims description 3
- 229960005205 prednisolone Drugs 0.000 claims description 3
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 claims description 3
- 230000001804 emulsifying effect Effects 0.000 claims 1
- 206010028735 Nasal congestion Diseases 0.000 abstract description 17
- 239000000546 pharmaceutical excipient Substances 0.000 abstract description 9
- 239000002904 solvent Substances 0.000 abstract description 9
- 239000003995 emulsifying agent Substances 0.000 abstract description 8
- 239000007921 spray Substances 0.000 abstract description 7
- 239000005526 vasoconstrictor agent Substances 0.000 abstract description 7
- 239000000243 solution Substances 0.000 abstract description 4
- 206010047139 Vasoconstriction Diseases 0.000 abstract description 3
- 230000025033 vasoconstriction Effects 0.000 abstract description 3
- 239000006172 buffering agent Substances 0.000 abstract description 2
- 210000004088 microvessel Anatomy 0.000 abstract description 2
- 239000006196 drop Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 description 17
- 210000001331 nose Anatomy 0.000 description 15
- 229940079593 drug Drugs 0.000 description 14
- 208000002874 Acne Vulgaris Diseases 0.000 description 11
- 206010000496 acne Diseases 0.000 description 11
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 8
- 208000030880 Nose disease Diseases 0.000 description 8
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 8
- 206010020751 Hypersensitivity Diseases 0.000 description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- 230000007815 allergy Effects 0.000 description 6
- 230000003266 anti-allergic effect Effects 0.000 description 6
- 238000006243 chemical reaction Methods 0.000 description 6
- 230000008961 swelling Effects 0.000 description 6
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 5
- 230000000845 anti-microbial effect Effects 0.000 description 5
- 230000002579 anti-swelling effect Effects 0.000 description 5
- 238000010586 diagram Methods 0.000 description 5
- 239000004615 ingredient Substances 0.000 description 5
- 229960004194 lidocaine Drugs 0.000 description 5
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 description 4
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 4
- 208000026344 Nasal disease Diseases 0.000 description 4
- 206010039085 Rhinitis allergic Diseases 0.000 description 4
- 230000000172 allergic effect Effects 0.000 description 4
- 201000010105 allergic rhinitis Diseases 0.000 description 4
- 208000010668 atopic eczema Diseases 0.000 description 4
- 229960000686 benzalkonium chloride Drugs 0.000 description 4
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 4
- 229960001747 cinchocaine Drugs 0.000 description 4
- PUFQVTATUTYEAL-UHFFFAOYSA-N cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 description 4
- 239000003246 corticosteroid Substances 0.000 description 4
- 229960000890 hydrocortisone Drugs 0.000 description 4
- 229960005016 naphazoline Drugs 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 230000011514 reflex Effects 0.000 description 4
- 230000000638 stimulation Effects 0.000 description 4
- 238000003860 storage Methods 0.000 description 4
- 238000009423 ventilation Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 3
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 3
- 230000001139 anti-pruritic effect Effects 0.000 description 3
- 230000002421 anti-septic effect Effects 0.000 description 3
- 229940046978 chlorpheniramine maleate Drugs 0.000 description 3
- 201000009151 chronic rhinitis Diseases 0.000 description 3
- 229960000520 diphenhydramine Drugs 0.000 description 3
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 3
- OCLXJTCGWSSVOE-UHFFFAOYSA-N ethanol etoh Chemical compound CCO.CCO OCLXJTCGWSSVOE-UHFFFAOYSA-N 0.000 description 3
- 238000010438 heat treatment Methods 0.000 description 3
- 239000011259 mixed solution Substances 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- 229940090248 4-hydroxybenzoic acid Drugs 0.000 description 2
- 206010024264 Lethargy Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 239000004909 Moisturizer Substances 0.000 description 2
- HUCJFAOMUPXHDK-UHFFFAOYSA-N Xylometazoline Chemical compound CC1=CC(C(C)(C)C)=CC(C)=C1CC1=NCCN1 HUCJFAOMUPXHDK-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 208000026935 allergic disease Diseases 0.000 description 2
- 239000002260 anti-inflammatory agent Substances 0.000 description 2
- 239000000739 antihistaminic agent Substances 0.000 description 2
- 206010003119 arrhythmia Diseases 0.000 description 2
- 230000006793 arrhythmia Effects 0.000 description 2
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 2
- 229940081733 cetearyl alcohol Drugs 0.000 description 2
- 230000002650 habitual effect Effects 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 229940057995 liquid paraffin Drugs 0.000 description 2
- 229960005015 local anesthetics Drugs 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 230000001333 moisturizer Effects 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 239000012188 paraffin wax Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 206010020880 Hypertrophy Diseases 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 241000283955 Ochotonidae Species 0.000 description 1
- 241000282405 Pongo abelii Species 0.000 description 1
- 208000036071 Rhinorrhea Diseases 0.000 description 1
- 206010039101 Rhinorrhoea Diseases 0.000 description 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 230000003409 anti-rejection Effects 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 239000003908 antipruritic agent Substances 0.000 description 1
- 229960005274 benzocaine Drugs 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- WCOATMADISNSBV-UHFFFAOYSA-K diacetyloxyalumanyl acetate Chemical compound [Al+3].CC([O-])=O.CC([O-])=O.CC([O-])=O WCOATMADISNSBV-UHFFFAOYSA-K 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 238000003255 drug test Methods 0.000 description 1
- 230000002910 effect on acne Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 208000014617 hemorrhoid Diseases 0.000 description 1
- 230000001969 hypertrophic effect Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 230000001151 other effect Effects 0.000 description 1
- 229960001528 oxymetazoline Drugs 0.000 description 1
- WYWIFABBXFUGLM-UHFFFAOYSA-N oxymetazoline Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C)=C1CC1=NCCN1 WYWIFABBXFUGLM-UHFFFAOYSA-N 0.000 description 1
- 229960001802 phenylephrine Drugs 0.000 description 1
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical compound CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- OJTDGPLHRSZIAV-UHFFFAOYSA-N propane-1,2-diol Chemical compound CC(O)CO.CC(O)CO OJTDGPLHRSZIAV-UHFFFAOYSA-N 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 238000002435 rhinoplasty Methods 0.000 description 1
- -1 steroid Hydrocortisone Acetate Chemical class 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000002522 swelling effect Effects 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 229960002372 tetracaine Drugs 0.000 description 1
- GKCBAIGFKIBETG-UHFFFAOYSA-N tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000032258 transport Effects 0.000 description 1
- 210000001944 turbinate Anatomy 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
- 210000002268 wool Anatomy 0.000 description 1
- 229960000833 xylometazoline Drugs 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
本發明是以局部麻醉劑及Hydrocortisone Acetate為主,利用極低濃度局部麻醉劑配合極低濃度Hydrocortisone Acetate視需要再加入防腐劑、緩衝劑、乳化劑、親水性增稠劑、界面活性劑、純水等賦形劑等一至數種組合製成一種點鼻劑或噴鼻劑組合物,當噴入或點入或塗摩於鼻黏膜時,極低濃度之Hydrocortisone Acetate為短效期的皮質類固醇性質溫和為最安全最佳之消炎消腫藥劑,它具有抗炎、抗過敏、抗增生、止癢、減少滲出等作用[參考:http://www.baike.com/wiki/%E9%86%8B%E9%85%B8%E6%B0%A2%E5%8C%96%E5%8F%AF%E7%9A%84%E6%9D%BE%E8%BD%AF%E8%86%8F+(HYDROCORTISONE+ACETATE+OINTMENT)(參考資料:附件一)及衛署藥輸字第121XX號藥物仿單說明書等(參考資料:附件二)]能對鼻黏膜進行消炎消腫作用,與現有的點鼻劑或噴鼻劑所含血管收縮劑及抗阻織胺不同的是因它具有抗增生作用使鼻黏膜不至於變厚而影響鼻道通氣,且它具有止癢作用減少打噴嚏的發生,因它具有減少滲出可讓分泌物黏液減少,而極低濃度之局部麻醉劑暫時阻斷鼻黏膜將異物侵入之訊息傳至腦部,因此腦部也暫停鼻黏膜繼續加強分泌之命令,兩者相輔相成,使鼻腔中鼻黏液減少,因此得以讓空氣通過鼻腔,讓發炎之鼻黏膜得以休息復原,因此兩者相乘效果激增,極有助於鼻病之治療。 The invention is based on a local anesthetic and Hydrocortisone Acetate, and uses a very low concentration of local anesthetic with a very low concentration of Hydrocortisone Acetate. If necessary, preservatives, buffers, emulsifiers, hydrophilic thickeners, surfactants, pure water, etc. are added. One to several combinations of excipients, etc., to form a nasal or nasal spray composition, when injected or spotted or coated on the nasal mucosa, a very low concentration of Hydrocortisone Acetate is a short-lived corticosteroid with mild properties. It is the safest and best anti-inflammatory swelling agent, it has anti-inflammatory, anti-allergic, anti-proliferation, anti-itch, reduce exudation and other effects [Reference: http://www.baike.com/wiki/%E9%86%8B %E9%85%B8%E6%B0%A2%E5%8C%96%E5%8F%AF%E7%9A%84%E6%9D%BE%E8%BD%AF%E8%86%8F+(HYDROCORTISONE +ACETATE+OINTMENT) (Reference: Annex 1) and the Department of Medicine's Drugs No. 121XX, such as drug copying instructions (Reference: Annex 2)] can anti-inflammatory and swelling effects on nasal mucosa, and existing nasal spray Or the nasal vasoconstrictor and anti-resistance of the nasal spray are different because of its anti-proliferative effect, so that the nasal mucosa does not become thicker. Ventilation, and it has an antipruritic effect to reduce the occurrence of sneezing, because it has reduced oozing to reduce secretion mucus, and a very low concentration of local anesthetic temporarily blocks the nasal mucosa to transmit foreign body intrusion message to the brain, so The brain also suspends the nasal mucosa to continue to strengthen the secretion of the command, the two complement each other, so that the nasal mucus in the nasal cavity is reduced, so that the air can pass through the nasal cavity, so that the inflamed nasal mucosa can rest and rest, so the synergy between the two is greatly increased, very helpful Treatment of nasal diseases.
傳統治療鼻炎之點鼻劑或噴鼻劑大都含血管收縮劑,諸如Oxymetazoline Hcl、Xylometazoline、Naphazoline Hcl、Phenylephrine Hcl等(參考資料附件三:藥證查詢網蒐索:噴鼻或點鼻http://www.fda.gov.tw/MLMS/H0001D.aspx?Type=Lic&LicId=01005125)是利用鼻粘膜血管收縮的作用,達到暫時去鼻塞的效果,因此例如鼻塞,剛噴時固然很快鼻子就通了,但隨著藥效逐漸退去,微血管又再次膨脹,鼻塞又來了,且越噴有效期間就越短,鼻黏膜也變肥厚,最後變成習慣性,甚至就失效了,甚至變成難以醫治之藥物性鼻炎、肥厚性鼻炎、慢性鼻炎,。傳統治療鼻炎之點鼻劑或噴鼻劑也有含抗組織胺諸如Diphenhydramine、Chlorpheniramine Maleate一般而言容易造成嗜睡,引起心律不整,造成危險,以上所述之組成物無論是血管縮收劑或抗組織胺其消炎消腫能力亦遠不及Hydrocortisone Acetate,也沒有Hydrocortisone Acetate具有抗增生作用使鼻黏膜不至於變厚而不至影響鼻道通氣,以及沒有Hydrocortisone Acetate具有止癢作用可減少打噴嚏的發生之作用。 Most of the traditional rhinitis or nasal sprays for the treatment of rhinitis contain vasoconstrictors, such as Oxymetazoline Hcl, Xylometazoline, Naphazoline Hcl, Phenylephrine Hcl, etc. (Refer to Appendix 3: Drug Search Network Search: Nasal or Point Nose http:// www.fda.gov.tw/MLMS/H0001D.aspx?Type=Lic&LicId=01005125 ) is the use of nasal vasoconstriction to achieve a temporary nasal congestion effect, so for example, nasal congestion, just after the spray, the nose will soon pass However, as the drug effect gradually recedes, the microvessels expand again, the nasal congestion comes again, and the shorter the effective period of the spray, the more the nasal mucosa becomes hypertrophy, and finally becomes habitual, even invalid, and even becomes a drug that is difficult to treat. Rhinitis, hypertrophic rhinitis, chronic rhinitis. The traditional rhinitis or nasal spray for treating rhinitis also contains antihistamines such as Diphenhydramine and Chlorpheniramine Maleate, which are generally prone to lethargy, causing arrhythmia and causing danger. The composition described above is either a vasoconstrictor or an anti-tissue. The anti-inflammatory and anti-tumor ability of amines is far less than that of Hydrocortisone Acetate, and there is no anti-proliferative effect of Hydrocortisone Acetate so that the nasal mucosa does not thicken and not affect nasal ventilation, and there is no anti-itch effect of Hydrocortisone Acetate to reduce the occurrence of sneezing. effect.
傳統點鼻劑及噴鼻劑只是治標不治本,只能暫時緩解鼻塞而無法從其病因做根本治療。從其說明書均註明:不可長期使用或連續使用10日後,應停甩2~3日再繼續使用或使用避免超過一個星期可略知其一二,因此很可能越用越沒效,而且一停藥就鼻塞。傳統治療鼻炎之點鼻劑及噴鼻劑並未完全對症下藥,因此鼻病患者眾多,常為鼻子過敏、鼻塞、打噴嚏所苦。(參考資料:附件四,鼻炎不易醫治或說無法根治有關網頁請在雅虎奇摩直接搜尋網 頁:鼻子過敏字樣可查到許多網站)。 Traditional nasal sprays and nasal sprays are only a temporary solution, and can only temporarily relieve nasal congestion and cannot be fundamentally treated from their causes. It is stated from the instructions that it can not be used for a long time or after 10 days of continuous use. It should be stopped for 2~3 days before continuing to use or use it for more than one week to know one or two. Therefore, it is likely that the more effective it is, the more effective it will be. The medicine is stuffy. Traditional nose and nasal spray for the treatment of rhinitis are not completely correct, so many patients with nasal diseases are often suffering from nasal allergies, nasal congestion, and sneezing. (Reference: Annex IV, rhinitis is not easy to cure or can not cure the relevant webpages. Please search the website directly at Yahoo!) Page: Nose allergies can be found on many websites).
根據統計,台灣約有四百萬人飽受鼻炎困擾(參考資料附件五:資料來源:雅虎奇摩直接搜尋:台灣約有四百萬人飽受過敏性鼻炎困擾 字樣);傳統治療鼻炎之點鼻劑或噴鼻劑治療鼻炎之藥物並未全對症下藥„理論上本發明是以局部麻醉劑配合Hydrocortisone Acetate為主,視需要再加入防腐劑、緩衝劑、乳化劑、親水性增稠劑、界面活性劑、純水等賦形劑等一至數種組合製成一種點鼻液或噴鼻液組合物來治療鼻炎。 According to statistics, about 4 million people in Taiwan suffer from rhinitis (see Annex 5: Source: Yahoo! Chimo direct search: about 4 million people suffering from allergic rhinitis in Taiwan); traditional treatment of rhinitis The agent or nasal spray for treating rhinitis is not completely symptomatic. In theory, the present invention is mainly based on a local anesthetic with Hydrocortisone Acetate, and if necessary, a preservative, a buffer, an emulsifier, a hydrophilic thickener, and a surfactant are added. One to several combinations of excipients such as pure water are used to make a nasal or nasal spray composition for treating rhinitis.
下列論點至今全世界尚未有人提出,現由本人首先提出:人體是一部複雜之機器許多構造及反應至今未全為人類所了解,單就鼻腔黏膜與腦部而言,當異物侵入鼻黏膜時,我們感覺會癢,會打噴嚏,會流鼻涕,因此再再證明鼻黏膜與腦部之間必存在著刺激與反射之關係。 The following arguments have not yet been proposed in the world. I now propose that the human body is a complex machine. Many structures and reactions have not been fully understood by humans. In the case of nasal mucosa and the brain, when foreign bodies invade the nasal mucosa. We feel itchy, sneezing, and runny nose, so we must prove that there is a relationship between stimulation and reflex between the nasal mucosa and the brain.
以鼻子過敏時鼻塞為例,當鼻塞時由於鼻腔兩側較易互相接觸,鼻黏膜極可能誤將異物侵入鼻黏膜訊息傳至腦部,腦部於是命令鼻黏膜加強分泌鼻黏液以排除異物,此一分泌之結果,使鼻腔兩側接觸面積更大,造成鼻黏膜更大之誤判異物侵入,又將異物侵入之訊息傳至腦部,腦部復命令鼻黏膜加強分泌鼻黏液,如此交互作用反覆糾纏是造成鼻子過敏、鼻塞、打噴嚏不易醫好的原因。 For example, when the nose is allergic to nasal congestion, when the nasal congestion is easy to contact each other on both sides of the nasal cavity, the nasal mucosa may mistakenly invade the nasal mucosa to the brain, and the brain then commands the nasal mucosa to strengthen the secretion of nasal mucus to exclude foreign bodies. As a result of this secretion, the contact area on both sides of the nasal cavity is larger, causing the nasal mucosa to be more intrusive into the foreign body, and transmitting the message of foreign body invasion to the brain. The brain repeatedly commands the nasal mucosa to strengthen the secretion of nasal mucus, so that interaction Repeated entanglement is the cause of nasal allergies, nasal congestion, and sneezing.
本發明是以局部麻醉劑及Hydrocortisone Acetate為主,利用極低濃度局部麻醉劑配合極低濃度Hydrocortisone Acetate視需要再加入防腐劑、緩衝劑、乳化劑、親水性增稠劑、界面活性劑、純水等賦形劑等一至數種組合製成一種點鼻液或噴鼻液組合物,當噴入鼻黏膜時,局部麻醉劑暫時阻斷鼻黏膜將異物侵入之訊息傳至腦部,因此腦部也暫停鼻黏膜繼續加強分泌之命令,使鼻腔中鼻黏液減少,得以讓空氣通過鼻腔,讓發炎之鼻黏膜得以休息復原。 The invention is based on a local anesthetic and Hydrocortisone Acetate, and uses a very low concentration of local anesthetic with a very low concentration of Hydrocortisone Acetate. If necessary, preservatives, buffers, emulsifiers, hydrophilic thickeners, surfactants, pure water, etc. are added. One to several combinations of excipients and the like are used to form a nasal or nasal spray composition. When sprayed into the nasal mucosa, the local anesthetic temporarily blocks the nasal mucosa and transmits the message of foreign body invasion to the brain, so the brain is also suspended. The nasal mucosa continues to strengthen the secretion command, which reduces the nasal mucus in the nasal cavity, allowing the air to pass through the nasal cavity, allowing the inflamed nasal mucosa to rest and recover.
而極低量之類固醇Hydrocortisone Acetate為短效期的皮質類固醇性質溫和為最安全最佳之消炎消腫藥劑,它具有抗炎、抗過敏、抗增生、止癢、減少滲出等作用能對鼻黏膜進行消炎消腫作用,因它具有抗增生作用使鼻黏膜不至於變厚而影響鼻道通氣,且它具有止癢作用減少打噴嚏的發生,因它具有減少滲出作用可讓分泌物黏液減少,兩者相輔相成,效果激增,極有助於鼻病之治療。 The very low amount of steroid Hydrocortisone Acetate is the shortest-acting corticosteroid. It is the safest and best anti-inflammatory and anti-inflammatory agent. It has anti-inflammatory, anti-allergic, anti-proliferative, anti-itching, and anti-exudation effects on the nasal mucosa. It has anti-inflammatory and anti-tumor effect, because it has anti-proliferative effect, so that the nasal mucosa does not become thicker and affects nasal ventilating, and it has anti-itching effect to reduce the occurrence of sneezing, because it has the effect of reducing exudation, which can reduce secretion mucus. The two complement each other and the effect is greatly increased, which is very helpful for the treatment of nasal diseases.
本人三十多年以前也是嚴重過敏性鼻炎患者,看遍中西醫師耳鼻喉科都無效,用過市售噴鼻藥,點鼻藥數種,連續多年,不但病症沒減輕,反而越用越重,變成藥物性鼻炎,也就是慢性鼻炎,深感鼻病之痛苦,在求助無門之下,三十多年以前無意間發現某些痔瘡藥膏對鼻塞鼻過敏有極大的治療效果,經長期研究學理確定是因含極低濃度局部麻醉劑及極低濃度Hydrocortisone Acetate組合物共同發揮效果是真正極有助於鼻炎之改善之因素。 I have been suffering from severe allergic rhinitis more than 30 years ago. I have seen all the doctors in the Department of Otorhinolaryngology are ineffective. I have used commercially available nasal sprays and several kinds of nasal medicines. For many years, not only the symptoms have not been alleviated, but the more heavier the more It becomes drug-induced rhinitis, which is chronic rhinitis, and it is deeply painful. In the absence of help, more than 30 years ago, some acne ointments were inadvertently found to have a great therapeutic effect on nasal allergies. It is determined by the combination of a very low concentration of local anesthetic and a very low concentration of Hydrocortisone Acetate composition that is truly a contributing factor to the improvement of rhinitis.
有感於人體器官與器官有刺激與反射之關係,同理鼻黏膜與腦部之間也自然也有刺激與反射之關係,因此當鼻塞時由於鼻腔兩側較易互相接觸,鼻黏膜誤判異物侵入訊息傳至腦部,於是腦部命令鼻黏膜加強分泌鼻黏液,造成鼻腔兩側更互相接觸,如此鼻黏膜與腦部刺激與反射交替作用是造成鼻塞鼻過敏之重要原因,若鼻黏膜不再將誤判異物侵入訊息一段時間內不再傳至腦部,腦部也暫時不再命令鼻黏膜加強分泌鼻黏液,鼻黏膜自然有一段時間得以休息,因此如以含極低濃度局部麻醉劑及極低濃度Hydrocortisone Acetate的的藥品經適當溶劑稀釋極低之比例安全量噴入或點入或塗摩於鼻黏膜時鼻中,效果應遠大於傳統之點鼻劑或噴鼻劑,本人此一鼻黏膜與腦部之間有刺激與反射關係之推論應是言之有理,且利用極低濃度局部麻醉劑配合極低濃度但有極優質消炎且抗增生抗癢能力之Hydrocortisone Acetate製成一種點鼻劑或噴鼻劑組合物治療鼻炎,理論上應是正確可行的,實際上本人三十年前無意間發現其效果也比任何市售之點鼻劑或噴鼻劑有效,且查遍藥證資料噴鼻劑82種及點鼻劑19種共101種至今為止從未有以局部麻醉劑配合Hydrocortisone Acetate治療鼻炎鼻塞鼻過敏之點鼻劑或噴鼻劑者(參考資料:藥證查詢網http://www.fda.gov.tw/MLMS/H0001D.aspx?Type=Lic&LicId=01005125蒐索:噴鼻或點鼻字樣),查遍專利檔案亦無此項資料。 It is related to the relationship between stimulation and reflex in human organs and organs. Naturally, there is also a relationship between stimulation and reflex between the nasal mucosa and the brain. Therefore, when the nasal congestion is easy to contact with each other on both sides of the nasal cavity, the nasal mucosa misjudges foreign matter intrusion. The message is transmitted to the brain, so the brain commands the nasal mucosa to strengthen the secretion of nasal mucus, causing the nasal cavity to contact each other more. Therefore, the alternation of nasal mucosa and brain stimulation and reflex is an important cause of nasal congestion and nasal allergy. If the nasal mucosa is no longer The misinformation of the foreign body intrusion message will not be transmitted to the brain for a period of time, and the brain will no longer order the nasal mucosa to strengthen the secretion of nasal mucus. The nasal mucosa naturally has a rest for a period of time, so if it contains a very low concentration of local anesthetic and very low The concentration of Hydrocortisone Acetate is diluted by a suitable solvent to a very low proportion of safely sprayed or applied to the nose of the nasal mucosa. The effect should be much greater than the traditional nasal spray or nasal spray. I have a nasal mucosa. The inference between the stimulus and the reflection between the brain and the brain should be justified, and the use of very low concentrations of local anesthetics with very low concentrations but very good quality The anti-proliferative and anti-itch ability of Hydrocortisone Acetate is a nasal or nasal spray composition for the treatment of rhinitis. In theory, it should be correct and feasible. In fact, I accidentally discovered that the effect was better than any commercial one 30 years ago. It is effective for nasal spray or nasal spray, and it has a total of 102 kinds of nasal sprays and a total of 101 kinds of nasal sprays. There have never been a local anesthetic with Hydrocortisone Acetate for rhinitis nasal allergic rhinitis. Or nasal spray (Reference: Drugs Enquiry Network http://www.fda.gov.tw/MLMS/H0001D.aspx?Type=Lic&LicId=01005125 Search: Nasal or Nose), search for patent files There is also no such information.
經查某藥證含有Naphazoline Hcl,Diphenhydramine,及經查某藥證含有Naphazoline Hcl,Chlorpheniramine Maleate,而Naphazoline Hcl它只對血管收縮有效,沒有抗過敏作用,也沒有抗增生及止癢作用,因此仿單大都註明:不可 長期使用或連續使用7至10日後,應停用2~3日再繼續使用。而遠不如Hydrocortisone Acetate抗炎、抗過敏、抗增生、止癢、減少滲出等作用。而抗組織胺Diphenhydramine及Chlorpheniramine Maleate一般而言消炎消腫能力極弱且對鼻黏膜也沒有抗增生及止癢作用,且容易造成嗜睡,引起心律不整,造成危險,故其消炎消腫能力遠不及Hydrocortisone Acetate。 After checking a drug certificate containing Naphazoline Hcl, Diphenhydramine, and a drug test containing Naphazoline Hcl, Chlorpheniramine Maleate, and Naphazoline Hcl it is only effective for vasoconstriction, no anti-allergic effect, no anti-proliferation and anti-itch effect, so imitation All of them are indicated: they cannot be used for a long time or after 7 to 10 days of continuous use, they should be suspended for 2~3 days before continuing to use. It is far less effective than Hydrocortisone Acetate in anti-inflammatory, anti-allergic, anti-proliferative, anti-itching, and reduced exudation. Anti-histamine Diphenhydramine and Chlorpheniramine Maleate generally have very weak anti-inflammatory and anti-tumor properties, and have no anti-proliferative and anti-itching effects on the nasal mucosa, and are prone to lethargy, causing arrhythmia and causing danger, so the anti-inflammatory and swelling ability is far less than that. Hydrocortisone Acetate.
因此本發明理論上功效遠大於現有市售之點鼻劑或噴鼻劑,本發明也經本人在無意間發現其效果極良好,因此才提出專利申請,才有廠商願意花錢花時間更近一步去申請人體臨床試驗,待通過人體臨床試驗後再由藥廠生產才能安全地服務廣大之鼻炎患者。 Therefore, the theoretical effect of the present invention is far greater than that of the currently available nasal spray or nasal spray. The present invention has also been inadvertently found to have an excellent effect, so that a patent application is filed, and only manufacturers are willing to spend money to spend more time. One step to the applicant's clinical trial, after passing the human clinical trial and then by the pharmaceutical factory to safely serve the majority of rhinitis patients.
本發明提供藉由點鼻器或噴霧器或塗摩經由病人鼻道給予本發明一種點鼻劑或噴鼻劑組合物,是最直接最有效使用最少藥劑最無副作用的方式。 The present invention provides a nasal spray or nasal spray composition of the present invention by means of a nose or spray or by application through the patient's nasal passages, which is the most direct and effective way to use the least amount of the agent with no side effects.
一般的有關醫藥發明首先要做動物試驗,以猩猩或其他動物如鼠兔要來測定鼻塞鼻過敏有無改善是不可能的事,本實驗以人體肛門之痔瘡來做為引證試驗,因為剛它周邊之黏膜極似鼻腔中之黏膜,因此如同一般的醫藥發明申請案在未做人體臨床實驗前只能旁徵引證上述本發明試用於腫大的痔瘡(第1圖)在數小時內即產生強大的消腫作用(第2圖)極易於觀察(且本發明是痔瘡藥的一種新用途,故使用於痔瘡也是合法使用),而鼻過敏鼻塞主因乃如第3 圖所示因鼻甲腫大阻塞鼻道造成,而消腫後如第4圖,極類似於痔瘡,故可推論該痔瘡藥極有助於鼻過敏鼻塞之治療。 In general, the relevant medical inventions should first be tested in animals. It is impossible to determine whether nasal congestion or nasal allergy is improved by using orangutans or other animals such as pikas. This experiment uses human anal acne as a citation test because it is just around it. The mucosa is very similar to the mucosa in the nasal cavity, so as the general medical invention application can only be used for side-by-side examination before the human clinical trials. The above-mentioned invention for the treatment of swollen acne (Fig. 1) produces strong in a few hours. The swelling effect (Fig. 2) is extremely easy to observe (and the present invention is a new use of acne medicine, so it is also legally used for acne), and the main cause of nasal allergic nasal congestion is as shown in Fig. 3 due to swelling of the nose. Blocking the nasal passages, and after swelling, as shown in Figure 4, is very similar to hemorrhoids, so it can be inferred that the acne medicine is very helpful for the treatment of nasal allergic nasal congestion.
本發明含極低濃度局部麻醉劑配合極低濃度Hydrocortisone Acetate製成一種點鼻劑或噴鼻劑組合物與傳統點鼻劑或噴鼻劑之比較:三十多年以前本人也是嚴重過敏性鼻炎患者,自患有鼻病多年看遍中西醫師耳鼻喉科都無效,用過市售噴鼻藥,點鼻藥數種,連續數年,不但病症沒減輕,反而越用越重,變成藥物性鼻炎,也就是慢性鼻炎,深感鼻病之痛苦,在求助無門之下,無意間發現某些痔瘡塗摩軟膏對治療鼻過敏鼻塞有極大功效,經長期研究主要其因含局部麻醉劑及含Hydrocortisone Acetate的組合物共同發揮效果極有助於鼻炎之改善。 The present invention contains a very low concentration of local anesthetic with a very low concentration of Hydrocortisone Acetate to make a nasal or nasal spray composition compared with traditional nasal or nasal spray: more than 30 years ago, I was also a patient with severe allergic rhinitis Since the nose disease has been seen for many years, both Chinese and Western doctors have been ineffective in otolaryngology. They have used commercially available nasal sprays and several kinds of nasal medicines. For several consecutive years, not only the symptoms have not been alleviated, but the more they use, the more they become drug-induced rhinitis. , that is, chronic rhinitis, the pain of deep nose disease, in the absence of help, unintentionally found that some acne coated ointment has great effect on the treatment of nasal allergic nasal congestion, after long-term research mainly because it contains local anesthetic and contains Hydrocortisone The combination of Acetate's composition contributes greatly to the improvement of rhinitis.
傳統之點鼻劑或噴鼻劑(第5圖,第6圖);傳統之噴鼻劑大都是含血管收縮劑,使用後約10分鐘後感到舒服,但有效時間剛用之初約5至6小時,每日需點4至5次(第2圖),隨著用久了,有效時間越來越短只有1至2小時,每日使用次數增加至10餘次,如連續使用5至7日後最後就失效了(第6圖)。 Traditional nasal spray or nasal spray (Fig. 5, Fig. 6); traditional nasal sprays are mostly vasoconstrictors, which are comfortable after about 10 minutes of use, but the effective time is just about 5 at the beginning. 6 hours, 4 to 5 times a day (Figure 2), with the use of a long time, the effective time is shorter and shorter only 1 to 2 hours, the number of daily use increased to more than 10 times, such as continuous use of 5 to After 7 days, it finally failed (Figure 6).
本發明含極低濃度局部麻醉劑配合Hydrocortisone Acetate之一種點鼻劑或噴鼻劑組合物(第7圖);本發明極低濃度局部麻醉劑配合極低濃度 Hydrocortisone Acetate之一種點鼻劑或噴鼻劑組合物,理論上當它噴在鼻黏膜時利用局部麻醉劑暫時阻斷異物侵入之訊息由鼻黏膜傳達至腦部,因此腦部也暫停命令鼻黏膜大量分泌黏液,而極低量之Hydrocortisone Acetate為短效期的皮質類固醇性質溫和為最安全最佳之消炎消腫藥劑,它具有抗炎、抗過敏、抗增生、止癢、減少滲出等作用能對鼻黏膜進行消炎消腫作用,因它具有抗增生作用使鼻黏膜不至於變厚而影響鼻道通氣,且它具有止癢作用可減少打噴嚏的發生,因它具有減少滲出可讓分泌物黏液減少,兩者相輔相成,因此極有助於鼻病之治療,因此它應是治本之道。第7圖為本人在三十年前無意間所發現如使用本發明點入鼻中後之鼻通暢度與時間關係示意圖。 The present invention contains a very low concentration of local anesthetic agent combined with Hydrocortisone Acetate as a nasal spray or nasal spray composition (Fig. 7); a very low concentration local anesthetic of the present invention is combined with a very low concentration of Hydrocortisone Acetate, a nasal spray or nasal spray The composition, in theory, when it is sprayed on the nasal mucosa, the local anesthetic is used to temporarily block the invasion of foreign bodies. The message is transmitted from the nasal mucosa to the brain. Therefore, the brain also suspends the command of the nasal mucosa to secrete a large amount of mucus, while the extremely low amount of Hydrocortisone Acetate is short. The mild corticosteroid is the safest and best anti-inflammatory and anti-tumor agent. It has anti-inflammatory, anti-allergic, anti-proliferative, antipruritic and anti-exudation effects. It can inhibit the inflammation and swelling of the nasal mucosa. The proliferative effect makes the nasal mucosa not thicken and affects the nasal passage ventilation, and it has an antipruritic effect to reduce the occurrence of sneezing, because it has reduced leakage and can reduce the secretion mucus, which complement each other, thus greatly contributing to the nose. The treatment of the disease, so it should be the cure. Figure 7 is a schematic diagram showing the relationship between nasal patency and time after inadvertently found in the nose 30 years ago, using the present invention.
本發明以實施例一為例,兩邊鼻孔如各點入下列實施例一溶液最多各0.5毫升,兩邊鼻孔共1毫升,合算其藥劑量Lidocain最多約0.3mg,Hydrocortisone Acetate最多約0.02mg,比起其他皮膚或痔瘡塗摩用量約只為其十分之一,因此它應是安全無疑的,它開始作用時間約一小時鼻部就會感到輕鬆舒服,但有效時間卻長達一至至數日,效果驚人,甚至就好了,因此沒有習慣性之問題。 In the first embodiment of the present invention, the nostrils on both sides are as long as 0.5 ml each of the following examples, and 1 ml of the nostrils on both sides, the total amount of Lidocain is about 0.3 mg, and the Hydrocortisone Acetate is about 0.02 mg. Other skin or acne application is about one-tenth of the amount, so it should be safe. It will feel relaxed and comfortable for about one hour, but it will last for one to several days. The effect is amazing, even better, so there is no habitual problem.
本發明是以局部麻醉劑及Hydrocortisone Acetate為主,利用極低濃度局部麻醉劑及極低濃度Hydrocortisone Acetate溶於適當之溶劑中視需要再加入防腐劑、緩衝劑、乳化劑、親水性增稠劑、界面活性劑、純水等賦形劑等一至數種組合製成一種點鼻劑噴鼻劑組合物,當噴入鼻黏膜時,極低濃度之Hydrocortisone Acetate為短效期的皮質類固醇性質溫和為最安全最佳之消炎消腫藥劑,能對鼻黏膜進行消炎消腫,並有抗過敏、抗增生、止癢作用,而極 低濃度之局部麻醉劑暫時阻斷鼻黏膜將異物侵入之訊息傳至腦部,因此腦部也暫停鼻黏膜繼續加強分泌之命令,兩者相輔相成,使鼻腔中鼻黏液減少,因此得以讓空氣通過鼻腔,讓發炎之鼻黏膜得以休息復原,兩者相乘效果激增,極有助於鼻病之治療。 The invention is based on a local anesthetic and Hydrocortisone Acetate, and is dissolved in a suitable solvent by using a very low concentration of local anesthetic and a very low concentration of Hydrocortisone Acetate. If necessary, a preservative, a buffer, an emulsifier, a hydrophilic thickener, and an interfacial activity are added. One or several combinations of excipients, pure water and the like are used to form a nasal spray nasal spray composition. When sprayed into the nasal mucosa, the extremely low concentration of Hydrocortisone Acetate is the safest of short-acting corticosteroids. The best anti-inflammatory and swelling agent can anti-inflammatory and swelling of the nasal mucosa, and has anti-allergic, anti-proliferative and anti-itching effects, while a very low concentration of local anesthetic temporarily blocks the nasal mucosa and transmits the message of foreign body invasion to the brain. Therefore, the brain also suspends the nasal mucosa to continue to strengthen the secretion of the command, the two complement each other, so that the nasal mucus in the nasal cavity is reduced, so that the air can pass through the nasal cavity, allowing the inflamed nasal mucosa to rest and rest, the synergy between the two is greatly increased, very Help with the treatment of nasal diseases.
局部麻醉劑種類眾多,常用者有利多卡因Lidocain,Prilocaine,Cinchocaine,Procaine,Dibucaine,CinchocaineHyddrochloride,Tetracaine Hcl,Benzocaine等,而Hydrocortisone Acetate為溫和的糖皮質激素具有很強的抗發炎、抗排斥、消腫、抗增生、止癢的作用,另可替代Hydrocortisone Acetate使用而也未見於藥證資料之點鼻劑或噴鼻劑之組成分中者與局部麻醉劑一起使用者尚有Prednisolone,Betamethasone Valerate。 There are many types of local anesthetics, such as Lidocain, Pilocaine, Cinchocaine, Procaine, Dibucaine, Cinchocaine Hyddrochloride, Tetracaine Hcl, Benzocaine, etc., while Hydrocortisone Acetate is a mild glucocorticoid with strong anti-inflammatory, anti-rejection and swelling. Anti-proliferative, anti-itching effect, another alternative to Hydrocortisone Acetate, but also not found in the drug information of the nose or nasal spray component with the local anesthetic users also have Prednisolone, Betamethasone Valerate.
本發明以局部麻醉劑利多卡因Lidocain及Hydrocortisone Acetate等溶解後視需要再加入防腐劑、緩衝劑、乳化劑、親水性增稠劑、界面活性劑、純水等賦形劑等一至數種組合製成一種點鼻劑或噴鼻劑組合物為實施例,只是最佳實施例的代表,並非侷限本發明之領域。 The invention is prepared by adding a preservative, a buffering agent, an emulsifier, a hydrophilic thickener, a surfactant, a pure water and the like to the local anesthetic agent Lidocain and Hydrocortisone Acetate. Forming a nasal or nasal spray composition is an example and is merely representative of the preferred embodiment and is not intended to limit the scope of the invention.
本發明進一步可以加入具有可相容性收斂劑Aluminium acetate或Zinc Oxide為收斂劑可消除腫脹及發炎,並具有殺菌作用。可以加入具有可相容性抗微生物防腐劑例如P-Hydroxybenzoic acid(對羥基苯甲酸)或Propylene Glycol(丙烯乙二醇)等作為溶劑、保濕劑亦有助防腐作用,可以加入Cetearyl Alcohol棕櫚醇作界面活性劑、乳化劑、親水性稠化劑,乙二胺 四乙酸二鈉,作為礦物質螯合劑,並可協同防腐作用。可加純水稀釋溶劑及其他醫葯具可相容性之藥劑及緩衝劑。 The invention can further be added with a compatible astringent Aluminium acetate or Zinc Oxide as an astringent to eliminate swelling and inflammation, and has a bactericidal effect. It can be added with a compatible antimicrobial preservative such as P-Hydroxybenzoic acid (P-hydroxybenzoic acid) or Propylene Glycol (propylene glycol) as a solvent, moisturizer and antiseptic effect. It can be added to Cetearyl Alcohol palmitol. Surfactant, emulsifier, hydrophilic thickener, disodium edetate, as a mineral chelating agent, and synergistic antiseptic effect. It can be diluted with pure water to dilute solvents and other pharmaceutical compatibility and buffers.
以下述成分製成一種點鼻劑或噴鼻劑組合物 Making a nasal spray or nasal spray composition with the following ingredients
此溶液以下述方法製備 This solution was prepared as follows
於適宜的反應容器內.先加賦型劑:Paraffinum Liquidum液態石蠟適量(約7-10%),Cetearyl Alcohol棕櫚醇適量(約5-9%)作為界面活性劑、乳化劑、,親水性稠化劑,Propylene Glycol丙烯乙二醇適量(約9-15%)作為溶劑、保 濕劑亦有助防腐作用,利用隔水加熱至攝氏50度後加入Lidocaine混合至少5分鐘使變成極低濃度局部麻醉劑,然後繼續加Hydrocortisone Acetate攪拌混合再5分鐘,混合均勻後,再加入Purified Water(約85-90%)攪拌混合均勻成為懸浮液點鼻劑,再加微量之抗微生物防腐劑Benzalkonium Chloride適量(0.001-0.02%))混合均勻,以進一部提高醫藥組合物的儲存性。 In a suitable reaction vessel, first add excipient: Paraffinum Liquidum liquid paraffin amount (about 7-10%), Cetearyl Alcohol palmitol (about 5-9%) as a surfactant, emulsifier, hydrophilic thick Properizer, Propylene Glycol propylene glycol (about 9-15%) as a solvent, moisturizer also helps antiseptic effect, use water to heat to 50 degrees Celsius, add Lidocaine mixed for at least 5 minutes to become a very low concentration of local anesthetic Then continue to add Hydrocortistis Acetate and mix for 5 minutes, mix well, then add Purified Water (about 85-90%) and mix and mix to form a suspension nose, plus a small amount of antimicrobial preservative Benzalkonium Chloride amount (0.001 -0.02%)) Mix evenly to further improve the storage of the pharmaceutical composition.
以下述成分製成一種點鼻劑或噴鼻劑組合物 Making a nasal spray or nasal spray composition with the following ingredients
於適宜的反應容器內.先加入賦型劑約百分之99的溶劑(水),加溫至攝氏50 度後加入Lidocaine(局部麻醉劑)適量(約0.3%)及Hydrocortisone Acetate適量(0.02%)混合至少5分鐘使變成極低濃度局部麻醉劑然後繼續加入攪拌混合至少5分鐘,混合均勻後冷卻後,再用過濾設備過濾設備過濾後再加微量之抗微生物防腐劑(Benzalkonium Chloride適量(0.001-0.02%),Ethanol乙醇適量(0.2-0.5%),L-Menthol(L-Menthol左旋薄荷、)混合均勻,以進一部提高醫藥組合物的儲存性,此混合溶液作為噴鼻劑用。 In a suitable reaction vessel, first add about 99% of the solvent (water) of the excipient. After heating to 50 degrees Celsius, add Lidocaine (local anesthetic) to the right amount (about 0.3%) and Hydrocortisone Acetate (0.02%). Mix for at least 5 minutes to become a very low concentration of local anesthetic and then continue to add stirring and mixing for at least 5 minutes, mix evenly and then cool, then filter with filtration equipment and then add a trace amount of antimicrobial preservative (Benzalkonium Chloride amount (0.001-0.02 %), Ethanol ethanol (0.2-0.5%), L-Menthol (L-Menthol L-Menthol), evenly mixed to further improve the storage of the pharmaceutical composition, the mixed solution as a nasal spray.
以下述成分製成一種點鼻劑或噴鼻劑組合物 Making a nasal spray or nasal spray composition with the following ingredients
於適宜的反應容器內.先加入賦型劑約百分之98的溶劑(水),加溫至攝氏50 度後加入Lidocaine混合至少5分鐘使變成極低濃度局部麻醉劑然後繼續加入Prednisolone攪拌混合至少5分鐘,混合均勻後冷卻後,再用過濾設備過濾後再加微量之抗微生物防腐劑(Benzalkonium Chloride適量(0.001-0.02%),Ethanol乙醇適量(0.2-0.5%),L-Menthol(左旋薄荷)混合均勻,以進一部提高醫藥組合物的儲存性。,此混合溶液作為噴鼻劑用。 In a suitable reaction vessel, first add about 98% of the solvent (water) of the excipient, warm to 50 degrees Celsius, add Lidocaine for at least 5 minutes to become a very low concentration of local anesthetic and then continue to add Prednisolone to mix and mix at least 5 minutes, mix evenly and then cool, then filter with filter equipment and then add a trace amount of antimicrobial preservative (Benzalkonium Chloride amount (0.001-0.02%), Ethanol ethanol amount (0.2-0.5%), L-Menthol (L-Menthol The mixture is uniformly mixed to further improve the storage property of the pharmaceutical composition. The mixed solution is used as a nasal spray.
以下述成分及比例製成一種點鼻劑或鼻腔塗抹劑組合物 Making a nasal spray or nasal spread composition with the following ingredients and ratios
此點鼻劑係以下列方法製備,供直接塗摩或點入於鼻腔中 於適宜的反應容器內.先加賦型劑liquid paraffin適量(約60-90%),white soft Paraffin白凡士林適量(約10-20%),Wool fat羊毛脂適量(約10-20%),利用隔水加熱至攝氏50-70度後加入Cinchocaine,攪拌混合至少5分鐘,使變成極低濃度之局部麻醉劑,然後繼續加入Hydrocortisone Acetate,混合至少5分鐘,混合均勻後冷卻後,再用過濾設備過濾後冷卻。 This nasal preparation is prepared by the following method for direct application or in the nasal cavity in a suitable reaction container. Firstly, the amount of the liquid paraffin is added (about 60-90%), white soft Paraffin white Vaseline ( About 10-20%), Wool fat lanolin amount (about 10-20%), use Caspochine after heating to 50-70 degrees Celsius, stir and mix for at least 5 minutes, so that it becomes a very low concentration of local anesthetic, then Continue to add Hydrocortisone Acetate, mix for at least 5 minutes, mix well and cool, then filter with filter and cool.
以下述成分製成一種點鼻劑或噴鼻劑組合物 Making a nasal spray or nasal spray composition with the following ingredients
此溶液以下述方法製備 This solution was prepared as follows
於適宜的反應容器內.先加入賦型劑約百分之99的溶劑(水),加溫至攝氏50 度後加入Lidocaine(局部麻醉劑)適量(約0.3%)及Betamethasone Valerate適量(0.006%)混合至少5分鐘使變成極低濃度局部麻醉劑然後繼續加入攪拌混合至少5分鐘,混合均勻後冷卻後,再用過濾設備過濾後再加微量之抗微生物防腐劑(Benzalkonium Chloride適量(0.001-0.02%),Ethanol乙醇適量(0.2-0.5%),L-Menthol(L-Menthol左旋薄荷適量(0.001-0.02%),混合均勻,以進一部提高醫藥組合物的儲存性,此混合溶液作為噴鼻劑用。 In a suitable reaction vessel, first add about 99% of the solvent (water) of the excipient. After heating to 50 degrees Celsius, add Lidocaine (local anesthetic) to the right amount (about 0.3%) and Betamethasone Valerate (0.006%). Mix for at least 5 minutes to become a very low concentration of local anesthetic and then continue to add stirring and mixing for at least 5 minutes, mix well and then cool, then filter with filter equipment and then add a trace amount of antimicrobial preservative (Benzalkonium Chloride amount (0.001-0.02%) Ethanol Ethanol (0.2-0.5%), L-Menthol (L-Menthol L-Menthol) (0.001-0.02%), evenly mixed to further improve the storage of the pharmaceutical composition, the mixed solution as a nasal spray .
第1圖為痔瘡發病時腫脹照片(引證)。 Figure 1 is a photo of swelling in the onset of acne (cited).
第2圖為痔瘡經塗摩本發明消腫照片[藥證衛署藥輸字第223XX號之合法使用於痔瘡(參考資料:附件六),內含局部麻醉劑Cinchocaine及Hydrocortisone,此外其他品牌內含局部麻醉劑lidocaine及Hydrocortisone,作用於痔瘡效果亦同](引證)。 Figure 2 is a photo of the swelling of the acne by the invention. The drug is used in the acne (Reference: Annex 6), which contains the local anesthetic Cinchocaine and Hydrocortisone, among other brands. The local anesthetic lidocaine and Hydrocortisone have the same effect on acne] (cited).
第3圖為左鼻腔因鼻甲腫大阻塞鼻道造成鼻塞示意圖(以左鼻腔為例)。 Figure 3 is a schematic diagram of nasal congestion caused by obstruction of the nasal passages in the nasal cavity of the left nasal cavity (taking the left nasal cavity as an example).
第4圖 左鼻腔因本發明可使鼻甲腫大消除鼻道變大通氣順暢示意圖(以左鼻腔為例)。 Fig. 4 The left nasal cavity can make the nasal turbinate enlargement by eliminating the smoothness of the nasal passages and the ventilation according to the present invention (taking the left nasal cavity as an example).
第5圖為傳統含血管收縮劑之點鼻劑或噴鼻劑剛開始點入鼻腔中後藥效使鼻通暢度與時間關係示意圖。(73.02.01-73.12.31本人三十年前為嚴重之鼻病患者,經醫生藥師指示下使用點鼻劑或噴鼻劑之經驗紀錄)。 Figure 5 is a schematic diagram showing the relationship between nasal patency and time after the traditional rhinoplasty or nasal spray containing vasoconstrictor has just begun to be placed in the nasal cavity. (73.02.01-73.12.31 I was a severe nasal disease patient 30 years ago, using the experience of using a nose spray or nasal spray under the direction of a doctor pharmacist).
第6圖為傳統含血管收縮劑之點鼻劑或噴鼻劑連續數日點入鼻腔中約5至7日後藥效使鼻通暢度與時間關示意圖。(73.02.01-73.12.31本人三十年前為嚴重之鼻病患者,經醫生藥師指示下使用點鼻劑或噴鼻劑之經驗紀錄)。 Fig. 6 is a schematic diagram showing the effect of the nasal fluency and time after the traditional nasal injection or nasal spray containing vasoconstrictor for several days into the nasal cavity for about 5 to 7 days. (73.02.01-73.12.31 I was a severe nasal disease patient 30 years ago, using the experience of using a nose spray or nasal spray under the direction of a doctor pharmacist).
第7圖為本發明含極低濃度局部麻醉劑配合極低濃度Hydrocortisone Acetate之一種點鼻劑或噴鼻劑組合物如噴入或點入或塗摩於鼻黏膜時鼻腔中後藥效使鼻通暢度與時間關係示意圖。(73.02.01-73.12.31)。 Figure 7 is a nasal or nasal spray composition containing a very low concentration of a local anesthetic with a very low concentration of Hydrocortisone Acetate, such as sprayed or applied or coated on the nasal mucosa, the nasal effect is smooth Schematic diagram of degree versus time. (73.02.01-73.12.31).
附註:1,醫療法中華民國七十五年十一月二十四日公佈.2,本發明符合藥事法施行細則第5條之規定:藥事法第二十條第一款所稱未經核准,擅自製造者,不包括非販賣之研究、試製之藥品。 Notes: 1. The Medical Law was promulgated on November 24, 1975. 2. The present invention complies with the provisions of Article 5 of the Regulations on the Implementation of the Pharmaceutical Affairs Law: Approved, unauthorized manufacturers, do not include non-trafficking research, trial production of drugs.
Claims (2)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TW106103828A TW201828941A (en) | 2017-02-06 | 2017-02-06 | Composition of nasal drops or nasal spray characterized by containing a local anesthetic agent and hydrocortisone acetate at low concentration, thereby facilitating the improvement of rhinitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TW106103828A TW201828941A (en) | 2017-02-06 | 2017-02-06 | Composition of nasal drops or nasal spray characterized by containing a local anesthetic agent and hydrocortisone acetate at low concentration, thereby facilitating the improvement of rhinitis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201828941A true TW201828941A (en) | 2018-08-16 |
Family
ID=63960264
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW106103828A TW201828941A (en) | 2017-02-06 | 2017-02-06 | Composition of nasal drops or nasal spray characterized by containing a local anesthetic agent and hydrocortisone acetate at low concentration, thereby facilitating the improvement of rhinitis |
Country Status (1)
| Country | Link |
|---|---|
| TW (1) | TW201828941A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025144994A1 (en) * | 2023-12-29 | 2025-07-03 | Regents Of The University Of Minnesota | Compositions and methods for intranasal delivery of hydrocortisone |
-
2017
- 2017-02-06 TW TW106103828A patent/TW201828941A/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025144994A1 (en) * | 2023-12-29 | 2025-07-03 | Regents Of The University Of Minnesota | Compositions and methods for intranasal delivery of hydrocortisone |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TW201016209A (en) | Intranasal compositions, dosage forms and methods of treatments | |
| JP2008521815A (en) | Capsinoid gel preparation and use thereof | |
| CN105142625A (en) | Neosaxitoxin combination formulations for prolonged local anesthesia | |
| US20060211665A1 (en) | Reduction of postoperative pain medication | |
| JPH0269413A (en) | Treatment of allergic rhinitis | |
| Fischer et al. | Efficacy and tolerability of ambroxol hydrochloride lozenges in sore throat | |
| KULLY | The use and abuse of nasal vasoconstrictor medications | |
| Schutz et al. | Local anaesthetic properties of ambroxol hydrochloride lozenges in view of sore throat | |
| Lieberman et al. | Two-week comparison study of olopatadine hydrochloride nasal spray 0.6% versus azelastine hydrochloride nasal spray 0.1% in patients with vasomotor rhinitis | |
| KR101800851B1 (en) | Local anesthesia pain-relieving time-delay angent | |
| JP6770091B2 (en) | Compositions and Methods for Treating Sinous Mucosal Diseases with Nicotinic Acetylcholine Receptor Agonists | |
| WO2010015253A1 (en) | Pharmaceutical composition for nasal application | |
| JP2022540702A (en) | Pharmaceutical and/or pharmaceutical composition for intravesical instillation, manufacture and use thereof | |
| CN108366991B (en) | Synergistic compounds of pyrrolidone carboxylic acid and/or its salts and hyaluronic acid and/or its salts for the treatment and/or prevention of mucous membrane drying and irritation, and related pharmaceutical formulations | |
| TW201828941A (en) | Composition of nasal drops or nasal spray characterized by containing a local anesthetic agent and hydrocortisone acetate at low concentration, thereby facilitating the improvement of rhinitis | |
| CN112770765B (en) | Composition for prophylaxis and/or treatment of urogenital mucosa | |
| Graf et al. | Efficacy and safety of intranasal xylometazoline and ipratropium in patients with common cold | |
| Mogahed et al. | The effect of adding two different doses of magnesium sulphate as adjuvant to ropivacaine in peribulbar block for cataract surgery | |
| Mehmood et al. | Efficacy and safety of a new mometasone furoate nasal spray formulation in patients with acute rhinosinusitis: A randomized clinical trial | |
| JP2006008540A (en) | Cold remedy | |
| CN111840226A (en) | A kind of medicine for treating allergic rhinitis and preparation method thereof | |
| US20150374644A1 (en) | Therapeutic Composition for the Treatment of Perianal Disorders | |
| US10583081B1 (en) | Apparatus and formulation for treating mouth ulcers | |
| CN100384435C (en) | A kind of saline medicinal solution and application device for treating nasal diseases | |
| Brem et al. | Intranasal application of buffered tripelennamine (pyribenzamine) solution in allergic rhinitis A preliminary report |