CN1043731C - Nitrendipine adhesive plaster for treating hypertension - Google Patents
Nitrendipine adhesive plaster for treating hypertension Download PDFInfo
- Publication number
- CN1043731C CN1043731C CN93110600A CN93110600A CN1043731C CN 1043731 C CN1043731 C CN 1043731C CN 93110600 A CN93110600 A CN 93110600A CN 93110600 A CN93110600 A CN 93110600A CN 1043731 C CN1043731 C CN 1043731C
- Authority
- CN
- China
- Prior art keywords
- nitrendipine
- layer
- drug
- azone
- coated
- 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.)
- Expired - Fee Related
Links
- PVHUJELLJLJGLN-INIZCTEOSA-N (S)-nitrendipine Chemical compound CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)[C@@H]1C1=CC=CC([N+]([O-])=O)=C1 PVHUJELLJLJGLN-INIZCTEOSA-N 0.000 title claims abstract description 34
- 229960005425 nitrendipine Drugs 0.000 title claims abstract description 34
- 206010020772 Hypertension Diseases 0.000 title abstract description 5
- 239000000853 adhesive Substances 0.000 title abstract 2
- 230000001070 adhesive effect Effects 0.000 title abstract 2
- 239000011505 plaster Substances 0.000 title 1
- 239000003814 drug Substances 0.000 claims abstract description 34
- 229940079593 drug Drugs 0.000 claims abstract description 24
- 229920002367 Polyisobutene Polymers 0.000 claims abstract description 19
- 239000000725 suspension Substances 0.000 claims abstract description 15
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical compound [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims abstract description 10
- 229940057995 liquid paraffin Drugs 0.000 claims abstract description 10
- 229910052710 silicon Inorganic materials 0.000 claims abstract description 10
- 239000010703 silicon Substances 0.000 claims abstract description 10
- 238000002360 preparation method Methods 0.000 claims abstract description 6
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 5
- 230000000149 penetrating effect Effects 0.000 claims abstract description 5
- 239000002904 solvent Substances 0.000 claims abstract description 4
- 229920005987 OPPANOL® Polymers 0.000 claims description 13
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 claims description 11
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims description 11
- 238000000605 extraction Methods 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 8
- 238000001035 drying Methods 0.000 claims description 6
- 229920002521 macromolecule Polymers 0.000 claims description 5
- 239000012528 membrane Substances 0.000 claims description 4
- 238000005303 weighing Methods 0.000 claims description 3
- 230000003247 decreasing effect Effects 0.000 claims description 2
- 239000006185 dispersion Substances 0.000 claims description 2
- 239000004615 ingredient Substances 0.000 claims description 2
- 238000001935 peptisation Methods 0.000 claims description 2
- 229920002402 Oppanol® B 100 Polymers 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 1
- 235000010603 pastilles Nutrition 0.000 claims 1
- 239000011345 viscous material Substances 0.000 claims 1
- 239000003292 glue Substances 0.000 abstract description 9
- 239000000463 material Substances 0.000 abstract description 7
- 239000000843 powder Substances 0.000 abstract description 7
- 239000007935 oral tablet Substances 0.000 abstract description 3
- 230000002045 lasting effect Effects 0.000 abstract description 2
- 231100000957 no side effect Toxicity 0.000 abstract description 2
- 230000036772 blood pressure Effects 0.000 abstract 1
- 239000000084 colloidal system Substances 0.000 abstract 1
- 229920000642 polymer Polymers 0.000 abstract 1
- 229920006254 polymer film Polymers 0.000 abstract 1
- 239000002120 nanofilm Substances 0.000 description 6
- 239000004698 Polyethylene Substances 0.000 description 5
- 239000012530 fluid Substances 0.000 description 5
- 238000010030 laminating Methods 0.000 description 5
- -1 polyethylene Polymers 0.000 description 5
- 229920000573 polyethylene Polymers 0.000 description 5
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 4
- 230000001631 hypertensive effect Effects 0.000 description 2
- 229940096978 oral tablet Drugs 0.000 description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- IZEKFCXSFNUWAM-UHFFFAOYSA-N dipyridamole Chemical compound C=12N=C(N(CCO)CCO)N=C(N3CCCCC3)C2=NC(N(CCO)CCO)=NC=1N1CCCCC1 IZEKFCXSFNUWAM-UHFFFAOYSA-N 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000010579 first pass effect Methods 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 229940072981 nitro-dur Drugs 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 238000012795 verification Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention provides a transdermal administration type nitrendipine patch for treating hypertension and a preparation method thereof. The nitrendipine patch has the basic structure that a middle layer is a drug storage layer which comprises nitrendipine, polyisobutylene polymer adhesive material, solvent and a penetrating agent, wherein one surface of the middle layer is a polymer film back lining layer, and the other surface is covered by silicon paper. The preparation method comprises the steps that colloid is first dissolved into glue solution which is mixed with medicinal powder, the penetrating agent and liquid paraffin into suspension, and then the suspension is coated. Compared with nitrendipine oral tablets, the nitrendipine patch has the advantages of mild, lasting and constant action in lowering blood pressure, long acting time, fewer times of medication, convenient use, no side effect, etc.
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: 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%, and polyisobutylene Oppanol 8100 4.5-7.5%, polyisobutylene Oppanol 810 8-11%, liquid paraffin 3-7.5%, cyclohexane extraction (or heptane 160-80%, 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 8100 in proportion, polyisobutylene Oppanol 810 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, with this suspension and above-mentioned glue mix homogeneously, make drug matrices again, make cover layer with silicon paper (or to the affinity of glue macromolecule membrane) less than backing layer, drug matrices evenly is coated with on it at the stand, in 60 ° of oven dry (or natural airing),, be cut into paster coated with backing layer, choose suitable paster area and every and contain the nitrendipine dose, can reach optimum efficiency.
Embodiment 1: with polyisobutylene Oppanol 8100 75g, polyisobutylene 0ppanol 810110g 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 68 ° 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 8100 68g, polyisobutylene Oppanol 810103g 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 14138cm 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 0ppanol 8100 60g, polyisobutylene Oppanol 81096g 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 8100 53g, polyisobutylene Oppanol 81087g mixes, and 758ml is dissolved as Colloidal fluid with it with cyclohexane extraction; After again nitrendipine medicated powder 80g being crossed 138 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 48mg.
Embodiment 5: with polyisobutylene 0ppanol 8100 45g, polyisobutylene Oppanol 81080g 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 68 ° 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%, cyclohexane extraction 60-80%, azone 1-5%, wherein: cyclohexane extraction is a solvent, 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 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 CN1077372A (en) | 1993-10-20 |
| CN1043731C true 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) |
Families Citing this family (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 |
| CN101933915B (en) * | 2010-09-03 | 2012-07-04 | 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0359625A1 (en) * | 1988-09-07 | 1990-03-21 | Laboratoires D'hygiene Et De Dietetique | Self-adhesive device for transdermal administration of an active agent |
| 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
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0359625A1 (en) * | 1988-09-07 | 1990-03-21 | Laboratoires D'hygiene Et De Dietetique | Self-adhesive device for transdermal administration of an active agent |
| DE4223360C1 (en) * | 1992-07-16 | 1993-04-08 | Lts Lohmann Therapie-Systeme Gmbh & Co Kg, 5450 Neuwied, De |
Non-Patent Citations (1)
| Title |
|---|
| 安徽医学，16(4) 1995.4.1 梁虎青等，尼群地平贴片治疗高血压临床疗效观察 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1077372A (en) | 1993-10-20 |
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| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C19 | Lapse of patent right due to non-payment of the annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |