CN1077372A - Treat hypertensive nitrendipine chip and preparation method thereof - Google Patents
Treat hypertensive nitrendipine chip and preparation method thereof Download PDFInfo
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- CN1077372A CN1077372A CN 93110600 CN93110600A CN1077372A CN 1077372 A CN1077372 A CN 1077372A CN 93110600 CN93110600 CN 93110600 CN 93110600 A CN93110600 A CN 93110600A CN 1077372 A CN1077372 A CN 1077372A
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Abstract
The invention provides hypertensive transdermal nitrendipine adhesive patch of a kind of treatment and preparation method.Its basic structure is that the intermediate layer is the drug storehouse layer that contains nitrendipine and polyisobutylene macromolecule viscous material and solvent and penetrating agent, and one side is the macromolecule membrane backing layer, and another side covers with silicon paper.Preparation method dissolving colloid earlier becomes glue, and glue and medicated powder, penetrating agent, liquid paraffin are mixed into suspension, applies then.Compare with the nitrendipine oral tablet, the hypotensive effect gentleness is arranged, lasting, constant, long action time, the medication number of times is few, and is easy to use, and advantage such as have no side effect.
Description
The present invention relates to treat the external type nitrendipine chip of hypertensive Western medicine " nitrendipine ", particularly a kind of percutaneous dosing.
Nitrendipine (Nitrendipine Patch), chemical name: the 4-(3-nitrobenzophenone)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxyl 3-methyl 5-ethyl ester, molecular formula and molecular weight: C
18H
20N
2O
6=360.37, be the new drug that the eighties America and Europe is at first gone on the market, belong to calcium-channel antagonists, be applicable to various types of hypertension clinically, be specially adapted to hyperpietic with coronary heart disease.Mostly be oral tablet but at present the home and abroad produces, its shortcoming is that first pass effect is strong, and the half-life is short, and bioavailability is low.Report is arranged abroad to the dosage form beyond the tablet, also develop as injection, soft capsule etc.For the external type membranous patch of percutaneous dosing, produced the anginal nitro-dur of treatment etc. at present abroad, but the big very little medicine class of more options dosage is made paster, dosage is bigger, makes paster and remains in certain difficulty.
The present invention provides a kind of dosage bigger nitrendipine chip for overcoming above-mentioned deficiency.The basic structure of nitrendipine chip is three layers, and the centre is a drug storehouse layer, and one side is a backing layer, and another side is a cover layer.The composition of drug storehouse layer and proportioning are: nitrendipine 2-10%, polyisobutylene Oppanol B100 4.5-7.5%, polyisobutylene Oppanol B10 8-11%, liquid paraffin 3-7.5%, cyclohexane extraction (or heptane) 60-80%, azone 1-5%.Wherein: azone is a penetrating agent, and cyclohexane extraction (or heptane) is a solvent.Backing layer is a high molecular film material, and cover layer is a silicon paper, (or to the affinity of glue macromolecule membrane less than backing layer).Drug storehouse layer can resolve into the 3-5 layer, and the ingredient in every layer is identical, and content of dispersion is progressively successively decreased to cover layer by backing layer.The preparation method of nitrendipine chip is: take by weighing polyisobutylene Oppanol B100 in proportion, polyisobutylene Oppanol B10 and cyclohexane extraction, peptization is separated, again with nitrendipine medicated powder, azone and liquid paraffin are milled on mill, medicine is dispersed in the suspension, again with this suspension and above-mentioned glue mix homogeneously, make drug matrices, make cover layer with silicon paper (or to the affinity of glue macromolecule membrane), drug matrices evenly is coated with on it at the stand, in 60 ° of oven dry (or natural airing) less than backing layer, coated with backing layer, be cut into paster.Choose suitable paster area and every and contain the nitrendipine dose, can reach optimum efficiency.
Embodiment 1: with polyisobutylene Oppanol B100 75g, polyisobutylene Oppanol B10 110g mixes, and 600ml is dissolved as Colloidal fluid with it with cyclohexane extraction; After again nitrendipine medicated powder 20g being crossed 130 mesh sieves, arise from the mill with azone 10g and liquid paraffin 30g one and to mill, medicine is dispersed in the suspension; With this suspension and above-mentioned glue mix homogeneously, make drug matrices.Drug matrices evenly is coated on the silicon paper at the stand, can be in 60 ° of oven dry 10 minutes, but also one night of natural drying then coated with high molecular film material, as polyethylene film, is made 6280cm altogether
2Three laminating sheets, the garden shape paster 2000 that can be cut into r=1cm at last pastes, and every contains nitrendipine 10mg.
Embodiment 2: with polyisobutylene Oppanol B100 68g, polyisobutylene Oppanol B10 103g mixes, and 650ml is dissolved as Colloidal fluid with it with cyclohexane extraction; After again nitrendipine medicated powder 40g being crossed 130 mesh sieves, arise from the mill with azone 20g and liquid paraffin 41g one and to mill, medicine is dispersed in the suspension; With this suspension and above-mentioned glue mix homogeneously, make drug matrices.Drug matrices evenly is coated on the silicon paper at the stand, can be in 60 ° of oven dry 10 minutes, but also one night of natural drying then coated with high molecular film material, as polyethylene film, is made 14130cm altogether
2Three laminating sheets, the garden shape paster 2000 that can be cut into r=1.5cm at last pastes, and every contains nitrendipine 20mg.
Embodiment 3: with polyisobutylene Oppanol B100 60g, polyisobutylene Oppanol B10 96g mixes, and 700ml is dissolved as Colloidal fluid with it with cyclohexane extraction; After again nitrendipine medicated powder 60g being crossed 130 mesh sieves, arise from the mill with azone 30g and liquid paraffin 52g one and to mill, medicine is dispersed in the suspension; With this suspension and above-mentioned glue mix homogeneously, make drug matrices.Drug matrices evenly is coated on the silicon paper at the stand, can be in 60 ° of oven dry 10 minutes, but also one night of natural drying then coated with high molecular film material, as polyethylene film, is made 18000cm altogether
2Three laminating sheets can be cut into 3 * 3cm at last
2Square patch 2000 paste, every contains nitrendipine 30mg.
Embodiment 4: with polyisobutylene Oppanol B100 53g, polyisobutylene Oppanol B10 87g mixes, and 750ml is dissolved as Colloidal fluid with it with cyclohexane extraction; After again nitrendipine medicated powder 80g being crossed 130 mesh sieves, arise from the mill with azone 40g and liquid paraffin 62g one and to mill, medicine is dispersed in the suspension; With this suspension and above-mentioned glue mix homogeneously, make drug matrices.Drug matrices evenly is coated on the silicon paper at the stand, can be in 60 ° of oven dry 10 minutes, but also one night of natural drying then coated with high molecular film material, as polyethylene film, is made 32000cm altogether
2Three laminating sheets can be cut into 4 * 4cm at last
2Square patch 2000 paste, every contains nitrendipine 40mg.
Embodiment 5: with polyisobutylene Oppanol B100 45g, polyisobutylene Oppanol B10 80g mixes, and 800ml is dissolved as Colloidal fluid with it with cyclohexane extraction; After again nitrendipine medicated powder 100g being crossed 130 mesh sieves, arise from the mill with azone 50g and liquid paraffin 75g one and to mill, medicine is dispersed in the suspension; With this suspension and above-mentioned glue mix homogeneously, make drug matrices.Drug matrices evenly is coated on the silicon paper at the stand, can be in 60 ° of oven dry 10 minutes, but also one night of natural drying then coated with high molecular film material, as polyethylene film, is made 48000cm altogether
2Three laminating sheets can be cut into 4 * 6cm at last
2Rectangle paster 2000 paste, every contains nitrendipine 50mg.
The nitrendipine chip that the present invention makes is through 223 routine clinical verifications, has identical effect with oral tablet, and the hypotensive effect gentleness, lasting, constant, long action time, the medication number of times is few, changes paster, and only need tear cover layer during use off and be affixed on chest in three days, conveniently have no side effect, the patient welcomes more.
Claims (4)
1, a kind of percutaneous dosing paster that contains the Western medicine nitrendipine is characterized in that basic structure is three layers, and middle for containing the drug storehouse layer of medicine, macromolecule viscous material, solvent and penetrating agent, drug storehouse layer is formed proportioning and is:
Nitrendipine 2-10%, polyisobutylene Oppanol B100 4.5-7.5%, polyisobutylene Oppanol B10 8-11%, liquid paraffin 3-7.5%, thiacyclohexane (or heptane) 60-80%, azone 1-5%.Wherein: thiacyclohexane (or heptane) is a solvent, and azone is a penetrating agent, and drug storehouse layer simultaneously is the macromolecule membrane backing layer, and another side is a silicon paper cover layer.
2, nitrendipine chip according to claim 1, drug storehouse layer also can be decomposed into the 3-5 layer, and the ingredient in every layer is identical, and content of dispersion is progressively successively decreased to cover layer by backing layer.
3, a kind of preparation method of nitrendipine chip according to claim 1 is characterized in that:
A takes by weighing polyisobutylene Oppanol B100, polyisobutylene Oppanol B10 and cyclohexane extraction (or heptane) in proportion, and peptization is separated;
B takes by weighing nitrendipine, azone and liquid paraffin, and they are milled on mill, makes the uniform suspension of pastille;
C, with b, result and a, the result mix, make drug matrices;
D makes cover layer with silicon paper, and drug matrices evenly is coated with on it at the stand, and oven dry again coated with the macromolecule membrane backing layer, is cut into the appropriate size paster then.
4, according to the described nitrendipine chip preparation method of claim 3, it is characterized in that among the 3d oven dry be under 60 ℃ of conditions heating 10 minutes or one night of natural drying.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN93110600A CN1043731C (en) | 1993-03-05 | 1993-03-05 | Nitrendipine adhesive plaster for treating hypertension |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN93110600A CN1043731C (en) | 1993-03-05 | 1993-03-05 | Nitrendipine adhesive plaster for treating hypertension |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1077372A true CN1077372A (en) | 1993-10-20 |
| CN1043731C CN1043731C (en) | 1999-06-23 |
Family
ID=4988448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN93110600A Expired - Fee Related CN1043731C (en) | 1993-03-05 | 1993-03-05 | Nitrendipine adhesive plaster for treating hypertension |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1043731C (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101933915A (en) * | 2010-09-03 | 2011-01-05 | 蚌埠丰原涂山制药有限公司 | Trans-dermal drug administration type Cilnidipine paster for treating hypertension and preparation method thereof |
| CN101703494B (en) * | 2009-11-27 | 2012-03-14 | 蚌埠丰原涂山制药有限公司 | Transdermal nitrendipine adhesive patch and preparation method thereof |
| CN108392424A (en) * | 2018-05-14 | 2018-08-14 | 山西鑫煜制药有限公司 | It is a kind of that micro constitutent is made to mix uniform method and application in pharmacy procedure |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2635979B1 (en) * | 1988-09-07 | 1992-05-29 | Lhd Lab Hygiene Dietetique | SELF-ADHESIVE DEVICE FOR ADMINISTERING AN ACTIVE PRINCIPLE BY PERCUTANEOUS ROUTE |
| DE4223360C1 (en) * | 1992-07-16 | 1993-04-08 | Lts Lohmann Therapie-Systeme Gmbh & Co Kg, 5450 Neuwied, De |
-
1993
- 1993-03-05 CN CN93110600A patent/CN1043731C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101703494B (en) * | 2009-11-27 | 2012-03-14 | 蚌埠丰原涂山制药有限公司 | Transdermal nitrendipine adhesive patch and preparation method thereof |
| CN101933915A (en) * | 2010-09-03 | 2011-01-05 | 蚌埠丰原涂山制药有限公司 | Trans-dermal drug administration type Cilnidipine paster for treating hypertension and preparation method thereof |
| CN108392424A (en) * | 2018-05-14 | 2018-08-14 | 山西鑫煜制药有限公司 | It is a kind of that micro constitutent is made to mix uniform method and application in pharmacy procedure |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1043731C (en) | 1999-06-23 |
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