CN106667903A - Fluoxetine tincture for treating leucoderma - Google Patents
Fluoxetine tincture for treating leucoderma Download PDFInfo
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- CN106667903A CN106667903A CN201710006871.8A CN201710006871A CN106667903A CN 106667903 A CN106667903 A CN 106667903A CN 201710006871 A CN201710006871 A CN 201710006871A CN 106667903 A CN106667903 A CN 106667903A
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- fluoxetine
- tincture
- vitiligo
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- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 title claims abstract description 14
- 229960002464 fluoxetine Drugs 0.000 title claims abstract description 14
- 229940098465 tincture Drugs 0.000 title claims abstract description 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 29
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 20
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 18
- 239000003814 drug Substances 0.000 claims abstract description 15
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 claims abstract description 9
- 229930003268 Vitamin C Natural products 0.000 claims abstract description 9
- 235000019154 vitamin C Nutrition 0.000 claims abstract description 9
- 239000011718 vitamin C Substances 0.000 claims abstract description 9
- GIYXAJPCNFJEHY-UHFFFAOYSA-N N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]-1-propanamine hydrochloride (1:1) Chemical compound Cl.C=1C=CC=CC=1C(CCNC)OC1=CC=C(C(F)(F)F)C=C1 GIYXAJPCNFJEHY-UHFFFAOYSA-N 0.000 claims abstract description 5
- 229960000389 fluoxetine hydrochloride Drugs 0.000 claims abstract description 5
- 238000004090 dissolution Methods 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 abstract description 15
- 235000011187 glycerol Nutrition 0.000 abstract description 7
- 238000002360 preparation method Methods 0.000 abstract description 5
- 210000002752 melanocyte Anatomy 0.000 abstract description 4
- 230000000694 effects Effects 0.000 abstract description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229960004756 ethanol Drugs 0.000 abstract 1
- 235000019441 ethanol Nutrition 0.000 abstract 1
- 229960005150 glycerol Drugs 0.000 abstract 1
- 229940079593 drug Drugs 0.000 description 8
- 239000000243 solution Substances 0.000 description 8
- 239000000203 mixture Substances 0.000 description 5
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 238000000034 method Methods 0.000 description 3
- 102000015617 Janus Kinases Human genes 0.000 description 2
- 108010024121 Janus Kinases Proteins 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000002547 new drug Substances 0.000 description 2
- 238000011084 recovery Methods 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 208000034493 Mucous membrane disease Diseases 0.000 description 1
- 229930003316 Vitamin D Natural products 0.000 description 1
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 description 1
- 230000001430 anti-depressive effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 229940046731 calcineurin inhibitors Drugs 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 238000002648 combination therapy Methods 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000035614 depigmentation Effects 0.000 description 1
- 238000007865 diluting Methods 0.000 description 1
- 230000003291 dopaminomimetic effect Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 238000002386 leaching Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 238000000554 physical therapy Methods 0.000 description 1
- 238000006479 redox reaction Methods 0.000 description 1
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 1
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 235000013619 trace mineral Nutrition 0.000 description 1
- 239000011573 trace mineral Substances 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 150000003710 vitamin D derivatives Chemical class 0.000 description 1
- 229940046008 vitamin d Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
本发明涉及一种用于治疗白癜风的酊剂及其制备方法。本发明氟西汀酊剂包含下列组分：盐酸氟西汀、乙醇、甘油、维生素C。本发明利用氟西汀的刺激黑素细胞产生的特性将氟西汀制备成酊剂药物，对一部分白癜风病症具有显著地疗效。且酊剂制备简单，成本低。具有极大的经济与社会意义。The invention relates to a tincture for treating vitiligo and a preparation method thereof. The fluoxetine tincture of the present invention comprises the following components: fluoxetine hydrochloride, ethanol, glycerin and vitamin C. The invention utilizes the property of fluoxetine to stimulate melanocytes to prepare fluoxetine into a tincture medicine, which has remarkable curative effect on some vitiligo diseases. Moreover, the preparation of the tincture is simple and the cost is low. It has great economic and social significance.
Description
技术领域technical field
本发明涉及医药生产技术领域，特别涉及一种治疗白癜风的氟西汀酊剂。The invention relates to the technical field of medicine production, in particular to a tincture of fluoxetine for treating vitiligo.
背景技术Background technique
白癜风是一种病因不明的后天性色素性皮肤黏膜疾病，最常见的原因是色素脱失，全球患病率为１％，我国的患病率为0.１％～２％。目前治疗白癜风的方法有：药物治疗、物理治疗、手术治疗以及联合疗法。其中治疗白癜风的药物有：皮质类固醇激素、钙调磷酸酶抑制剂、微量元素、维生素Ｄ、Janus激酶（JAK）抑制剂、调节细胞氧化还原反应的药物。目前申请专利的白癜风药物多为中药组方。例如申请号为CN201610713102.7专利《一种治疗白癜风的中药》，申请号为CN201410235188.8的专利《一种治疗白癜风的中药组合物》。Vitiligo is an acquired pigmented skin and mucous membrane disease of unknown etiology. The most common cause is depigmentation. The global prevalence rate is 1%, and the prevalence rate in my country is 0.1%-2%. The current treatment methods for vitiligo are: drug therapy, physical therapy, surgery and combination therapy. Among them, the drugs for the treatment of vitiligo include: corticosteroid hormones, calcineurin inhibitors, trace elements, vitamin D, Janus kinase (JAK) inhibitors, and drugs that regulate cellular redox reactions. Most of the currently patented vitiligo drugs are prescriptions of traditional Chinese medicine. For example, the patent application number is CN201610713102.7 "A Traditional Chinese Medicine for Treating Vitiligo", and the patent application number is CN201410235188.8 "A Chinese Medicine Composition for Treating Vitiligo".
氟西汀是一种选择性的5-羟色胺重摄取抑制剂，由美国礼来公司研制，于20世纪90年代初上市，具有良好的抗抑郁效应，目前被当作一线药物广泛应用于临床。主要药理作用在于选择性地抑制中枢神经系统突触前释放的5－羟色胺的再摄取,又称为选择性的5-羟色胺重摄取抑制剂。而对其它受体，如α-肾上腺素能、β-肾上腺素能、5-羟色胺能、多巴胺能等，氟西汀则几乎没有结合力。最新发现氟西汀可以用于治疗白癜风。Fluoxetine is a selective serotonin reuptake inhibitor developed by Eli Lilly and Company of the United States and launched in the early 1990s. It has good antidepressant effects and is currently widely used in clinical practice as a first-line drug. The main pharmacological effect is to selectively inhibit the reuptake of 5-HT released in the central nervous system, also known as selective 5-HT reuptake inhibitor. For other receptors, such as α-adrenergic, β-adrenergic, 5-hydroxytryptaminergic, dopaminergic, etc., fluoxetine has almost no binding force. The latest discovery is that fluoxetine can be used to treat vitiligo.
酊剂，酊剂系指药物用规定浓度的乙醇浸出或溶解而制成的澄清液体制剂，亦可用流浸膏稀释制成，供内服或外用。白癜风外用药物中酊剂（酒精制剂）占有极大的比重，在完全静止期或者恢复期可以外用酊剂，以便刺激黑素细胞，使其功能恢复或者黑素细胞功能活跃。Tincture, tincture refers to a clear liquid preparation made by leaching or dissolving a drug with a specified concentration of ethanol, and it can also be made by diluting a liquid extract for internal or external use. Tinctures (alcohol preparations) account for a large proportion of Vitiligo topical medicines. Tinctures can be used externally during the complete quiescence or recovery period to stimulate melanocytes, restore their function or activate melanocytes.
目前白癜风的治疗仍较为困难，临床疗效由于个体的不同存在很大的差异，因此常规治疗无法满足所有患者的治疗，对于这些患者可尝试新的治疗方法。At present, the treatment of vitiligo is still relatively difficult, and the clinical efficacy varies greatly due to individual differences. Therefore, conventional treatment cannot satisfy the treatment of all patients. For these patients, new treatment methods can be tried.
发明内容Contents of the invention
本发明为了弥补现有技术的不足，提供了一种治疗白癜风的新药物。In order to make up for the deficiencies of the prior art, the invention provides a new drug for treating vitiligo.
本发明是通过如下技术方案实现的：The present invention is achieved through the following technical solutions:
本发明一种治疗白癜风的氟西汀酊剂，每1000ml药品中包含下列含量的组分：氟西汀50-100mg、75%乙醇400-750ml、甘油400-500ml、维生素C 0-200mg。The fluoxetine tincture for treating vitiligo of the present invention contains the following components in every 1000ml medicine: 50-100mg of fluoxetine, 400-750ml of 75% ethanol, 400-500ml of glycerin and 0-200mg of vitamin C.
其中优选每1000ml药品中包含下列含量的组分：氟西汀70-100mg、75%乙醇500-600ml、甘油400-500ml、维生素C 100-200mg。Among them, the following components are preferably included in every 1000ml of medicine: 70-100mg of fluoxetine, 500-600ml of 75% ethanol, 400-500ml of glycerin, and 100-200mg of vitamin C.
更优选每1000ml药品中包含下列含量的组分：氟西汀100mg、75%乙醇500ml、甘油500ml、维生素C 100mg。More preferably, every 1000ml of medicine contains the following components: 100mg of fluoxetine, 500ml of 75% ethanol, 500ml of glycerin, and 100mg of vitamin C.
其制备方法为：Its preparation method is:
(1)先将100mg维生素C溶于500ml75%的乙醇溶液；(1) Dissolve 100mg of vitamin C in 500ml of 75% ethanol solution;
(2) 称取100mg盐酸氟西汀，溶于步骤（1）中的所得的混合溶液中，搅拌使充分溶解；(2) Weigh 100 mg of fluoxetine hydrochloride, dissolve it in the mixed solution obtained in step (1), and stir to fully dissolve;
(3)量取500ml甘油，与步骤（2）所得溶液充分混合，得到澄清溶液。装于棕色瓶中。(3) Measure 500ml of glycerin and fully mix it with the solution obtained in step (2) to obtain a clear solution. Packed in a brown bottle.
本发明的有益效果是：本发明为白癜风的治疗提供了新药物及新剂型。适用于完全静止期或者恢复期，可以刺激黑素细胞，使其恢复功能，效果显著。The beneficial effects of the invention are: the invention provides a new drug and a new dosage form for the treatment of vitiligo. It is suitable for complete quiescence or recovery period, it can stimulate melanocytes to restore their functions, and the effect is remarkable.
具体实施方式detailed description
实施例1：Example 1:
称取100mg维生素C，将维生素C加入到500ml 75%的乙醇溶液中，慢慢加入，边加边搅拌，直至完全溶解；称取100mg盐酸氟西汀，加入含维生素C的乙醇溶液中，搅拌5分钟；量取500ml甘油，与上述溶液混合，振荡混匀，装入棕色瓶中密封保存。Weigh 100mg of vitamin C, add vitamin C to 500ml of 75% ethanol solution, add slowly, stir while adding, until completely dissolved; weigh 100mg of fluoxetine hydrochloride, add to the ethanol solution containing vitamin C, stir 5 minutes; measure 500ml of glycerin, mix with the above solution, oscillate and mix well, put it into a brown bottle and seal it for storage.
实施例2：Example 2:
称取100mg盐酸氟西汀固体，将其加入到500ml75%的乙醇溶液中，边加边搅拌，使其完全溶解，再加入500ml甘油，振荡混合，装入棕色瓶中密封保存。Weigh 100mg of fluoxetine hydrochloride solid, add it to 500ml of 75% ethanol solution, stir while adding to make it completely dissolved, then add 500ml of glycerin, shake and mix, put it into a brown bottle and seal it for storage.
Claims (6)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710006871.8A CN106667903A (en) | 2017-01-05 | 2017-01-05 | Fluoxetine tincture for treating leucoderma |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710006871.8A CN106667903A (en) | 2017-01-05 | 2017-01-05 | Fluoxetine tincture for treating leucoderma |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106667903A true CN106667903A (en) | 2017-05-17 |
Family
ID=58849961
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710006871.8A Pending CN106667903A (en) | 2017-01-05 | 2017-01-05 | Fluoxetine tincture for treating leucoderma |
Country Status (1)
| Country | Link |
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| CN (1) | CN106667903A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107375428A (en) * | 2017-07-20 | 2017-11-24 | 山东润泽制药有限公司 | Ointment for treating vitiligo with fluoxetine combined with traditional Chinese medicine components and preparation method thereof |
| CN108969512A (en) * | 2017-06-05 | 2018-12-11 | 南京睿鹰润泽生物医药科技有限公司 | A pharmaceutical composition of R-fluoxetine or racemic fluoxetine salt type and its application |
| WO2020238570A1 (en) * | 2019-05-28 | 2020-12-03 | 南京睿鹰润泽生物医药科技有限公司 | Composition containing fluoxetine and vitamin d 3 or its derivatives, and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102429894A (en) * | 2011-12-07 | 2012-05-02 | 中国药科大学 | Application of fluoxetine to treatment of depigmentation disease |
| CN103381204A (en) * | 2012-05-06 | 2013-11-06 | 田荣侠 | Leucoderma medicament and preparation method thereof |
-
2017
- 2017-01-05 CN CN201710006871.8A patent/CN106667903A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102429894A (en) * | 2011-12-07 | 2012-05-02 | 中国药科大学 | Application of fluoxetine to treatment of depigmentation disease |
| CN103381204A (en) * | 2012-05-06 | 2013-11-06 | 田荣侠 | Leucoderma medicament and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 南京医学院，南京医学院第一附属医院: "《临床药物手册》", 30 October 1986, 上海科学技术出版 * |
| 李圣惠: "积雪草等３种挥发油对盐酸氟西汀体外经皮渗透性的影响", 《南京中医药大学学报》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108969512A (en) * | 2017-06-05 | 2018-12-11 | 南京睿鹰润泽生物医药科技有限公司 | A pharmaceutical composition of R-fluoxetine or racemic fluoxetine salt type and its application |
| CN107375428A (en) * | 2017-07-20 | 2017-11-24 | 山东润泽制药有限公司 | Ointment for treating vitiligo with fluoxetine combined with traditional Chinese medicine components and preparation method thereof |
| WO2020238570A1 (en) * | 2019-05-28 | 2020-12-03 | 南京睿鹰润泽生物医药科技有限公司 | Composition containing fluoxetine and vitamin d 3 or its derivatives, and application thereof |
| JP2022534264A (en) * | 2019-05-28 | 2022-07-28 | ナンジン ルーイン ルンゼ バイオファーマシューティカル テクノロジー カンパニー インコーポレイテッド | COMPOSITION CONTAINING FLUOXETINE AND VITAMIN D3 OR DERIVATIVE THEREOF AND USE THEREOF |
| JP7413619B2 (en) | 2019-05-28 | 2024-01-16 | ナンジン ルーイン ルンゼ バイオファーマシューティカル テクノロジー カンパニー インコーポレイテッド | Composition containing fluoxetine and vitamin D3 or its derivatives and uses thereof |
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Application publication date: 20170517 |