CN1436535A - Nisoldipine capsule composition - Google Patents
Nisoldipine capsule composition Download PDFInfo
- Publication number
- CN1436535A CN1436535A CN 02104211 CN02104211A CN1436535A CN 1436535 A CN1436535 A CN 1436535A CN 02104211 CN02104211 CN 02104211 CN 02104211 A CN02104211 A CN 02104211A CN 1436535 A CN1436535 A CN 1436535A
- Authority
- CN
- China
- Prior art keywords
- nisoldipine
- oral compositions
- liquid
- liquid oral
- surfactant
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- VKQFCGNPDRICFG-UHFFFAOYSA-N methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1C1=CC=CC=C1[N+]([O-])=O VKQFCGNPDRICFG-UHFFFAOYSA-N 0.000 title claims abstract description 32
- 229960000227 nisoldipine Drugs 0.000 title claims abstract description 32
- 239000007963 capsule composition Substances 0.000 title description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 44
- 239000007788 liquid Substances 0.000 claims abstract description 17
- 239000000203 mixture Substances 0.000 claims abstract description 17
- 239000007901 soft capsule Substances 0.000 claims abstract description 14
- 238000002360 preparation method Methods 0.000 claims abstract description 10
- 239000002904 solvent Substances 0.000 claims abstract description 9
- 239000004094 surface-active agent Substances 0.000 claims abstract description 8
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims description 9
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 claims description 9
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 206010020772 Hypertension Diseases 0.000 claims description 3
- 235000012424 soybean oil Nutrition 0.000 claims description 3
- 239000003549 soybean oil Substances 0.000 claims description 3
- 206010002383 Angina Pectoris Diseases 0.000 claims description 2
- 239000003921 oil Substances 0.000 claims 2
- 235000019198 oils Nutrition 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 239000002736 nonionic surfactant Substances 0.000 claims 1
- 235000015112 vegetable and seed oil Nutrition 0.000 claims 1
- 239000008158 vegetable oil Substances 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 abstract description 12
- 230000000694 effects Effects 0.000 abstract description 2
- 239000000470 constituent Substances 0.000 description 8
- 239000002775 capsule Substances 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000004064 cosurfactant Substances 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 description 2
- 229960001597 nifedipine Drugs 0.000 description 2
- YNGDWRXWKFWCJY-UHFFFAOYSA-N 1,4-Dihydropyridine Chemical compound C1C=CNC=C1 YNGDWRXWKFWCJY-UHFFFAOYSA-N 0.000 description 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920001214 Polysorbate 60 Polymers 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910001424 calcium ion Inorganic materials 0.000 description 1
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 230000000297 inotrophic effect Effects 0.000 description 1
- 230000037356 lipid metabolism Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000002107 myocardial effect Effects 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 230000036581 peripheral resistance Effects 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
- 229940113124 polysorbate 60 Drugs 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 230000005180 public health Effects 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000003087 receptor blocking agent Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention is liquid composition for soft capsule and is especially the liquid content for Nisoldipine soft capsule and the soft capsule preparation. The liquid content contains Nisoldipine as active component, glycerin as auxiliary surfactant, solvent and surfactant. In the preparation, Nisoldipine is dissolved in solvent for high biological utilization and fast effect.
Description
The present invention relates to contain the stable liquid capsule composition of the soft capsule that is suitable for preparing nisoldipine.More particularly, the present invention relates to a kind of liquid content that is suitable for being mixed with soft capsule, it contains nisoldipine is active component, and glycerol also relates to the soft capsule preparation that contains described solution shape content as cosurfactant, solvent composition and surfactant.
Nisoldipine is a second filial generation dihydropyridines calcium from antagonist, its chemical constitution and nifedipine are similar, to photaesthesia, picking up anti-agent with other dihydropyridine calcium ions compares, the effect of being characterized in is stronger, and biological half-life is longer, compares blood lipid metabolism and blood sugar level that nisoldipine can not influence the patient with the B-receptor blocking agent, compare with nifedipine, nisoldipine is because littler to the high selectivity thereby the negative inotropic action of blood vessel.It can reduce myocardial oxygen consumption and total peripheral resistance, also can increase the CC circulation, and coronary flow is increased.Nisoldipine is a German Bayer drugmaker initiative, and principal indication is hypertension and angina pectoris.China's Ministry of Public Health had been ratified nisoldipine raw material and tablet (specification: 5mg), produced by Shandong Province Pharmacy stock Co., Ltd of Xinhua and pharmaceutical factory of Shandong Province's industrial research institute thereof in 1998.The present invention is a nisoldipine capsule, does not see the report of the patent of relevant nisoldipine capsule and related preparations thereof so far as yet.
The present invention is a nisoldipine capsule, and wherein nisoldipine is dissolved in the solvent in the preparation, makes low dose of nisoldipine dispersed homogeneous degree better than tablet, and rapid-action, has overcome the lower shortcoming of conventional tablet bioavailability; Simultaneously, this product can provide the possibility of a kind of renewal, better dosage form selection for curing loyal both sides as a kind of novel form.
The object of the present invention is to provide a kind of nisoldipine novel formulation, said preparation is guaranteeing under the suitable prerequisite of principal agent dosage, by selecting adjuvant and formulation method for use, nisoldipine is made solution to be wrapped in and to make soft capsule in the rubber, help oral, the absorption of medicine, reach high bioavailability.Simultaneously, also be clinical a kind of renewal, the better dosage form selection of providing.
Be described more specifically the present invention by the following example.But these embodiment should not be construed as the restriction to any aspect of the present invention.
Embodiment 1
The PEG400 (60 ℃ of water temperatures) in water-bath that takes by weighing 180g is heated, add the 5.0g nisoldipine, constantly stir and make medicine dissolution, add 6.3g glycerol again, stir, add the 95.7g PEG400 at last, stir to put and be chilled to room temperature, make the pale yellow solution that contains principal agent 17.4mg among every 1g, after measuring content, medicinal liquid is incorporated in the machine of preparation soft capsule, regulates this machine and make the medicinal liquid that injects 0.287g in each soft capsule, preparation contains the soft capsule of nisoldipine pale yellow solution in gelatin shell.
Embodiment 2
Preparing the soft capsule with following composition according to same steps as among the embodiment 1, is the consumption difference as the glycerol of cosurfactant.2-A constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 4.3
PEG400 275.7
Amount to 285mg2-B constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 10.3
PEG400 275.7
Amount to 291mg
Embodiment 3
Prepare soft capsule according to embodiment 1 identical step, just increase the composition of surfactant with following composition.3-A constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 6.3
Tween 80 10
PEG400 275.7
Amount to 297mg3-B constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 4.3
Polysorbate60 10
PEG400 275.7
Amount to 297mg embodiment 4
Same steps as preparation according to embodiment 1 has following soft capsule, just the composition of solvent and its changes of contents.4-A constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 4.3
PEG400 220.7
Amount to 230mg4-B constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 4.3
PEG400 350.7
Amount to 360mg4-C constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 8.0
Soybean oil 250
Amount to 262mg4-D constituent content (mg/ grain)
Nisoldipine 5.0
Glycerol 6.0
Soybean oil 300
Amount to 310mg
Claims (9)
1. be used for that constitutional is light, the oral liquid composition of moderate hypertension and angina pectoris and the treatment of coronary heart disease complicated hypertension, comprise the glycerol of principal agent nisoldipine and capacity, an amount of solvent and surfactant etc. and be fit to oral liquid to form.
2. the liquid oral compositions of claim 1, it also comprises pharmaceutic adjuvant or excipient.
3. the liquid oral compositions of claim 1, wherein said solvent is oil and polyethylene glycols.
4. the liquid oral compositions of claim 3, wherein said oil is soybean oil or more refined vegetable oil.
5. the liquid oral compositions of claim 3, wherein said polyethylene glycols is a PEG400.
6. the liquid oral compositions of claim 1, wherein said surfactant is a nonionic surfactant.
7. the liquid oral compositions of claim 1, the ratio of wherein said nisoldipine, described glycerol, described solvent and described surfactant is 1: 1～4: 50～100: 0.5～3 (weight).
8. the liquid oral compositions of claim 7, the ratio of wherein said nisoldipine, described glycerol, described solvent and described surfactant is 1: 1.2～3: 50～80: 0.8～2 (weight).
9. the liquid oral compositions of claim 1, it is made into soft capsule preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02104211 CN1261097C (en) | 2002-02-09 | 2002-02-09 | Nisoldipine capsule composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02104211 CN1261097C (en) | 2002-02-09 | 2002-02-09 | Nisoldipine capsule composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1436535A true CN1436535A (en) | 2003-08-20 |
| CN1261097C CN1261097C (en) | 2006-06-28 |
Family
ID=27627961
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02104211 Expired - Fee Related CN1261097C (en) | 2002-02-09 | 2002-02-09 | Nisoldipine capsule composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1261097C (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1771949B (en) * | 2005-11-06 | 2011-04-20 | 沈阳药科大学 | Soft nimodipine capsule and its preparation |
| WO2012171364A1 (en) * | 2011-06-13 | 2012-12-20 | 浙江爱生药业有限公司 | Oil-soluble pharmaceutical composition |
| CN106511294A (en) * | 2016-12-09 | 2017-03-22 | 汤臣倍健股份有限公司 | Soft capsule and preparation method thereof |
-
2002
- 2002-02-09 CN CN 02104211 patent/CN1261097C/en not_active Expired - Fee Related
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1771949B (en) * | 2005-11-06 | 2011-04-20 | 沈阳药科大学 | Soft nimodipine capsule and its preparation |
| WO2012171364A1 (en) * | 2011-06-13 | 2012-12-20 | 浙江爱生药业有限公司 | Oil-soluble pharmaceutical composition |
| CN106511294A (en) * | 2016-12-09 | 2017-03-22 | 汤臣倍健股份有限公司 | Soft capsule and preparation method thereof |
| CN106511294B (en) * | 2016-12-09 | 2019-05-07 | 汤臣倍健股份有限公司 | A kind of soft capsule and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1261097C (en) | 2006-06-28 |
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