CN102342917A - Slow release oral solid preparation with Nilvadipine as active component - Google Patents
Slow release oral solid preparation with Nilvadipine as active component Download PDFInfo
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- CN102342917A CN102342917A CN2010102468658A CN201010246865A CN102342917A CN 102342917 A CN102342917 A CN 102342917A CN 2010102468658 A CN2010102468658 A CN 2010102468658A CN 201010246865 A CN201010246865 A CN 201010246865A CN 102342917 A CN102342917 A CN 102342917A
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- nilvadipine
- release
- oral solid
- solid preparation
- release oral
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Abstract
The invention relates to a slow release oral solid preparation with Nilvadipine and its salts as active components. The slow release oral solid preparation is prepared with Nilvadipine and pharmaceutically acceptable accessories by a preparation technology. The slow release oral solid preparation involved in the invention comprises but is not limited to tablets, capsules, particles and slow release pellets. The preparation provided in the invention has the advantages of stable and controllable quality, controllability, safety and effectiveness.
Description
Technical field
The present invention relates to a kind of is the release oral solid preparation of main component with the nilvadipine.It is the solid preparation of processing through preparation technique with nilvadipine and acceptable accessories.Release oral solid preparation steady quality of the present invention, controlled, safe and effective.Belong to medical technical field.
Background technology
Hypertension be a kind of with body circulation systolic arterial pressure (SBP) and (or) diastolic pressure (DBP) raises be the clinical syndrome of characteristic, it is one of present the most common clinical, most important cardiovascular disease.Along with improving constantly of people's living standard, hypertensive prevalence is also increasing year by year, and China generally investigates preventing and controlling since nineteen fifty-nine to hypertension, and the hypertensive prevalence of being grown up at that time is 5.1%; During to 1979-1980 hypertension sampling survey for the second time, adult's hypertension prevalence (comprising borderline hypertension) has been increased to 7.73%; 1990-1991 time national hypertension census result for the third time shows that the hypertension prevalence is having phenomenal growth during the decade again, estimates that the whole nation had 6,000 ten thousand hyperpietics at least at that time.According to another updated statistics, at present the hypertensive prevalence of China has risen to 11.68%, and target organ damages such as the heart of hypertension secondary, brain, kidney especially have a strong impact on patient's life-span and quality of life, have become the disease of serious threat human health and life.
Nilvadipine is a dihydropyridine type calcium antagonists class antihypertensive.Its calcium antagonism and stronger 10 times than nitre benzene heavy stone used as an anchor with film specificity combination, the long 2-3 of acting duration are doubly.The effect characteristics are strong to the effect comparison action of the heart of blood vessel; Other tremulous pulse of dilating effect comparison to vertebral artery and hat tremulous pulse is strong; Can obviously improve because of hypertension with the vein extensibility low, thereby reduce preload; The effect that also has antianginal and arteriosclerosis.
Summary of the invention
For improving patient compliance, it is the release oral solid preparation of main component that the present invention provides a kind of nilvadipine.This release oral solid preparation is that main component and acceptable accessories are processed through preparation technique with the nilvadipine, includes but not limited to tablet, capsule, granule and slow-release pill.
The consumption of the nilvadipine in this each prescription of release oral solid preparation is per unit dosage 0.5-8mg.Comprise following constituent: nilvadipine, composite materials, sustained-release matrix material, rate of release regulator, lubricant.
Described composite materials can form complex with nilvadipine, and this complex can be by rapid aquation, and this material is a polyox-yethylene-polyoxypropylene block copolymer, i.e. poloxamer, preferably poloxamer-188.The ratio of itself and nilvadipine is preferably 5: 1.
Described rate of release adjustment agent for the soluble small molecular material, includes but not limited to lactose, mannitol, sucrose, glucose, fructose, xylitol, sorbitol and electrolyte.
Described composite materials, a kind of solvent environment of when forming complex with nilvadipine, still needing is about to nilvadipine and this composite materials and is dissolved in this solvent jointly; This solvent is the lower aliphatic alcohols of the straight or branched of 1-7 carbon atom, like methanol, and ethanol; Normal propyl alcohol, n-butyl alcohol.
Described sustained-release matrix material stops drug crystallization and controls medicine thereby can form the low viscosity clear gel after the imbibition, and this material includes but not limited to hyprolose, hypromellose.Preferred hydroxypropyl emthylcellulose.Hydroxypropyl emthylcellulose through adding different proportion is the speed of control drug release effectively.
The described nilvadipine release oral of this patent solid preparation can be used for treating various hypertension.
The specific embodiment:
Following case study on implementation is used to explain the present invention, but is not limited thereto.
Embodiment 1 nilvadipine slow releasing tablet
Process 100000 nilvadipine slow releasing tablet with following materials of weight proportions.
Prescription:
Preparation technology:
1. nilvadipine is pulverized, crossed 80 mesh sieves, subsequent use.
2. get 40 ℃ of heating of 95% ethanol, add poloxamer 188, stir, make dissolving fully, add the nilvadipine powder, stir, make dissolving fully.Get orange-yellow transparent viscous solution.
3. get HPMC 6cps, HPMC 15cps joins in the above-mentioned solution, stirs, and makes mix homogeneously.
4. get lactose and join in the above-mentioned suspension, stir, make mix homogeneously.
5. with the above-mentioned thickness suspension that obtains, in the tray, vacuum decompression is dry, makes moisture less than 1%.
6. above-mentioned gained dried material is pulverized, crossed 40 mesh sieves, add magnesium stearate as lubricant, mix homogeneously.Tabletting.
5. prepare 6% Opadry ordinary coating agent aqueous dispersion suspension;
6. get the plain sheet of above-mentioned gained, pour coating pan into and carry out coating, about 30 ℃ of hot blast temperature, the relative label weightening finish of coating powder: 3.0-5.0%.
Embodiment 2 nilvadipine slow releasing capsule
Process 100000 nilvadipine slow releasing capsule with following materials of weight proportions, every is 150mg.
Prescription:
Preparation technology:
1. nilvadipine is pulverized, crossed 80 mesh sieves, subsequent use.
2. get 40 ℃ of heating of 95% ethanol, add poloxamer 188, stir, make dissolving fully, add the nilvadipine powder, stir, make dissolving fully.Get orange-yellow transparent viscous solution.
3. get HPMC 6cps, HPMC 15cps joins in the above-mentioned solution, stirs, and makes mix homogeneously.
4. get lactose and join in the above-mentioned suspension, stir, make mix homogeneously.
5. with the above-mentioned thickness suspension that obtains, in the tray, vacuum decompression is dry, makes moisture less than 1%.
6. above-mentioned gained dried material is pulverized, crossed 40 mesh sieves, add microcrystalline Cellulose, magnesium stearate is as lubricant, mix homogeneously.Encapsulated, every 150mg.
Claims (8)
- The present invention for a kind of be the slow release release oral solid preparation of active component with the nilvadipine; This release oral solid preparation is that main component and acceptable accessories are processed through preparation technique with the nilvadipine, comprises tablet, capsule, granule and slow-release pill.
- 2. nilvadipine release oral solid preparation as claimed in claim 1 is characterized in that, the consumption of the nilvadipine in this each prescription of release oral solid preparation is per unit dosage 0.5-8mg.
- 3. nilvadipine release oral solid preparation as claimed in claim 1 is characterized in that said preparation comprises following constituent: nilvadipine, composite materials, sustained-release matrix material, rate of release regulator, lubricant.
- 4. composite materials as claimed in claim 3; It is characterized in that this material can form complex with nilvadipine; This complex can be by rapid aquation; This material is a polyox-yethylene-polyoxypropylene block copolymer; It is poloxamer; Preferred poloxamer-188, the ratio of itself and nilvadipine is preferably 5: 1.
- 5. rate of release as claimed in claim 3 is adjusted, and it is characterized in that this material is the soluble small molecular material, comprises lactose, mannitol, sucrose, glucose, fructose, xylitol, sorbitol and electrolyte.
- 6. composite materials as claimed in claim 3; It is characterized in that a kind of solvent environment of still needing when this material can form complex with nilvadipine; Be about to nilvadipine and this composite materials and be dissolved in this solvent jointly; This solvent is the lower aliphatic alcohols of the straight or branched of 1-7 carbon atom; Like methanol; Ethanol, normal propyl alcohol, n-butyl alcohol.
- 7. sustained-release matrix material as claimed in claim 3, thus it is characterized in that can stoping drug crystallization and control medicine by formation low viscosity clear gel after this material imbibition, and this material includes but not limited to hyprolose, hypromellose.Preferred hydroxypropyl emthylcellulose.Hydroxypropyl emthylcellulose through adding different proportion is the speed of control drug release effectively.
- 8. nilvadipine release oral solid preparation as claimed in claim 1 can be used for treating various hypertension.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010102468658A CN102342917A (en) | 2010-08-06 | 2010-08-06 | Slow release oral solid preparation with Nilvadipine as active component |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010102468658A CN102342917A (en) | 2010-08-06 | 2010-08-06 | Slow release oral solid preparation with Nilvadipine as active component |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102342917A true CN102342917A (en) | 2012-02-08 |
Family
ID=45542247
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010102468658A Pending CN102342917A (en) | 2010-08-06 | 2010-08-06 | Slow release oral solid preparation with Nilvadipine as active component |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102342917A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5160734A (en) * | 1987-11-25 | 1992-11-03 | American Cyanamid Company | Sustained release delivery system for substituted dihydropyridine calcium channel blockers |
-
2010
- 2010-08-06 CN CN2010102468658A patent/CN102342917A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5160734A (en) * | 1987-11-25 | 1992-11-03 | American Cyanamid Company | Sustained release delivery system for substituted dihydropyridine calcium channel blockers |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20120208 |