CN1203786A - Nicardipine hydrochloride slow release tablet and its preparing method - Google Patents
Nicardipine hydrochloride slow release tablet and its preparing method Download PDFInfo
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- CN1203786A CN1203786A CN 97112579 CN97112579A CN1203786A CN 1203786 A CN1203786 A CN 1203786A CN 97112579 CN97112579 CN 97112579 CN 97112579 A CN97112579 A CN 97112579A CN 1203786 A CN1203786 A CN 1203786A
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Abstract
The main ingredients of nicardipine hydrochloride slow release tablet as drug for curing angiocardiopathy and cerebrovascular disease are nicardipine hydrochloride, slow release skeletal substrate and adhesive. The slow release skeletal substrate is cellulose derivative and vinyl polymer. Said slow release material is low in cost, easily available, and can implement industrial large-scale production.
Description
The present invention relates to a kind of new drug formulation preparation for the treatment of the heart, cerebrovascular disease medicament preparation category, particularly a kind of nicardipine hydrochloride sustained-release tablet and process thereof.
Slow releasing tablet is a rising high tech novel form in recent years, uses the pharmacokinetics principle, makes with special adjuvant and technology.Medicine is arrived behind the gastrointestinal by slowly discharging in the dosage form for absorption, low " peak valley " phenomenon when high when therefore having avoided the common blood drug level of ordinary preparation.Thereby can not only stably keep the necessary blood drug level of treatment the long period, and its blood drug level is far away with the least concentration distance that toxic and side effects takes place, and has guaranteed the safety and effectiveness of medication, and easy to use.
Licardipine Hydrochloride (Nicardipine Hydrochlorid) chemical name is 2,6-dimethyl-4-(3-nitrobenzophenone)-1,4-dihydropyridine-3, the 5-dicarboxylic acids, 3-(β-(N-benzyl-N-methylamino)) ethyl ester-5-methyl ester hydrochloride, be that the eighties is widely used in clinical cardiovascular medicament both at home and abroad, in many calcium channel blockers, Licardipine Hydrochloride is many with its clinical use research, toxic and side effects is little, being widely used and being recorded by pharmacopeia, is as the various ischemic cerebrovascular of treatment, rheumatic heart disease, all kinds of angina pectoriss, one of myocardial infarction and hypertensive choice drug.But the weak point of Licardipine Hydrochloride is half-life short (1.5h), and patient need frequently take medicine (every day three times).Because the heart, cerebrovascular disease are burst easily, and " drug withdrawal knock-on " occur in some patient that can not take medicine on time, tend to serious harm patient's life security.In recent years Licardipine Hydrochloride is made slow releasing capsule abroad, only need sooner or later respectively to take medicine once, can make the patient obtain the ideal treatment blood drug level protection of 24h.But China does not still have the slow release formulation of this medicine.
The external synthesized polymer material that adopts is done slow releasing capsule, and this type of material resources is in short supply, cost an arm and a leg, and preparation piller coating and capsule form needs special installation, and technology difficulty is big, in China's suitability for industrialized production difficulty.
Purpose of the present invention is exactly under the prerequisite that guarantees the product slow releasing function, adopts domestic resourceful sustained-release matrix substrate, preferably is fit to the technology of national conditions, forms low-cost, large-tonnage industrial advantages, fills up domestic this blank.
The present invention realizes with following technical scheme:
Develop a kind of treatment heart, nicardipine hydrochloride sustained-release tablet and process thereof the pharmaceutical preparation category of cerebrovascular disease, that comprise formations such as principal agent, sustained-release matrix substrate and adjuvant, it is characterized in that its main component is principal agent, sustained-release matrix substrate and necessary adjuvant component, wherein:
1, principal agent is the treatment heart, cerebrovascular disease medicament Licardipine Hydrochloride,
2. sustained-release matrix substrate can be cellulose derivative and polyvinyl,
3. the necessary adjuvant component in the adjuvant is a binding agent,
Above-mentioned nicardipine hydrochloride sustained-release tablet and process thereof, described sustained-release matrix substrate can be cellulose derivative and polyvinyl, is meant that sustained-release matrix substrate can be from hydroxypropyl emthylcellulose with slow release characteristic, polyvinylpyrrolidone, ethyl cellulose, hydroxypropyl cellulose or by selecting its mixture of forming.
Above-mentioned nicardipine hydrochloride sustained-release tablet and process thereof, binding agent in the described necessary adjuvant component can be from hydroxypropyl emthylcellulose, polyvinylpyrrolidone, methylcellulose, ethyl cellulose, low-substituted hydroxypropyl cellulose, starch, sucrose, dextrin and lactose with adhesion characteristic or by selecting its one group of binding agent forming.
Above-mentioned nicardipine hydrochloride sustained-release tablet and process thereof, the ratio between described each main component is:
Principal agent: sustained-release matrix substrate=1: 0.2～4.
The process of slow releasing tablet of the present invention is the preparation method of conventional tablet.
Facts have proved that compare with background technology, the present invention has following advantage:
1. sustained-release matrix substrate is based on our country, aboundresources, inexpensive;
2. process of the present invention is the preparation method of conventional tablet, need not to increase extras and investment, the energy mass industrialized production;
3. the product drug effect is long, side effect is little;
Therefore the present invention has very big advantage and potentiality, has the very strong market competitiveness.
The present invention is further elaborated below in conjunction with drawings and Examples:
Fig. 1 is Licardipine Hydrochloride sheet (20mg) stripping curve of conventional formulation;
Fig. 2 is product nicardipine hydrochloride sustained-release tablet of the present invention (20mg) release profiles; Vertical coordinate is stripping (release) degree, and unit is %, and abscissa is the time, and unit is hour.
1000 of [embodiment one] preparation nicardipine hydrochloride sustained-release tablets,
Its prescription is:
Licardipine Hydrochloride 20.0g
Hydroxypropyl emthylcellulose 10.0g
Lactose 20.0g
Dextrin 50.0g
PVP solution is an amount of
Magnesium stearate 0.5%
Preparation technology: be the preparation technology of conventional tablet.Other adjuvant such as diluent, lubricant etc. with principal agent, sustained-release matrix substrate and necessary adjuvant component and convention amount through pulverizing, mixing, granulation, tabletting, packing, make the slow releasing tablet that meets the pharmaceutical production code requirement.
Detect other inspection item under the tablet item of its drug content, uniformity of dosage units, release and national regulation, all conformance with standard regulation through drug inspection department.
Following implementation column technological operation, result and quality situation are all with embodiment one.
1000 of [embodiment two] preparation nicardipine hydrochloride sustained-release tablets,
Its prescription is:
Licardipine Hydrochloride 20.0g
Hydroxypropyl emthylcellulose 20.0g
Lactose 20.0g
Dextrin 40.0g
PVP solution is an amount of
Magnesium stearate 0.5%
1000 of [embodiment three] preparation nicardipine hydrochloride sustained-release tablets,
Its prescription is:
Licardipine Hydrochloride 20.0g
Hydroxypropyl emthylcellulose 25.0g
Ethyl cellulose 5.0g
Lactose 20.0g
Dextrin 30.0g
Ethyl cellulose solution is an amount of
Magnesium stearate 0.5%
1000 of [embodiment four] preparation nicardipine hydrochloride sustained-release tablets,
Its prescription is:
Licardipine Hydrochloride 20.0g
Hydroxypropyl emthylcellulose 5.0g
PVP 15．0g
Ethyl cellulose 20.0g
Lactose 20.0g
Dextrin 20.0g
Ethyl cellulose solution is an amount of
Magnesium stearate 0.5%[embodiment five] prepare 1000 of nicardipine hydrochloride sustained-release tablets, its prescription is:
Licardipine Hydrochloride 20.0g
Hydroxypropyl emthylcellulose 10.0g
Low-substituted hydroxypropyl cellulose 60.0g
Starch 10.0g
Ethyl cellulose solution is an amount of
Magnesium stearate 1%
Claims (4)
1. treat the heart, cerebrovascular disease medicament preparation category for one kind, comprise nicardipine hydrochloride sustained-release tablet and process thereof that principal agent, sustained-release matrix substrate and adjuvant etc. constitute, it is characterized in that its main component is principal agent, sustained-release matrix substrate and necessary adjuvant component, wherein:
1.1. principal agent is the treatment heart, cerebrovascular disease medicament Licardipine Hydrochloride,
1.2. sustained-release matrix substrate can be cellulose derivative and polyvinyl,
1.3. the necessary adjuvant component in the adjuvant is a binding agent,
2. according to described nicardipine hydrochloride sustained-release tablet of claim 1 and process thereof, the described sustained-release matrix substrate of its qualifying part can be cellulose derivative and polyvinyl, is meant that sustained-release matrix substrate can be from hydroxypropyl emthylcellulose with slow release characteristic, polyvinylpyrrolidone, ethyl cellulose, hydroxypropyl cellulose or by selecting its mixture of forming.
3. according to described nicardipine hydrochloride sustained-release tablet of claim 1 and process thereof, its qualifying part is that the binding agent in the described necessary adjuvant component can be from hydroxypropyl emthylcellulose, polyvinylpyrrolidone, methylcellulose, ethyl cellulose, low-substituted hydroxypropyl cellulose, starch, sucrose, dextrin and lactose with adhesion characteristic or by selecting its one group of binding agent forming.
4. according to described nicardipine hydrochloride sustained-release tablet of claim 1 and process thereof, its qualifying part is that the ratio between described each main component is:
Principal agent: sustained-release matrix substrate=1: 0.2～4.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 97112579 CN1203786A (en) | 1997-06-27 | 1997-06-27 | Nicardipine hydrochloride slow release tablet and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 97112579 CN1203786A (en) | 1997-06-27 | 1997-06-27 | Nicardipine hydrochloride slow release tablet and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1203786A true CN1203786A (en) | 1999-01-06 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 97112579 Pending CN1203786A (en) | 1997-06-27 | 1997-06-27 | Nicardipine hydrochloride slow release tablet and its preparing method |
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| CN (1) | CN1203786A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102908327A (en) * | 2011-08-05 | 2013-02-06 | 江苏恒瑞医药股份有限公司 | Sustained release preparation for ivabradine or medicinal salt thereof |
-
1997
- 1997-06-27 CN CN 97112579 patent/CN1203786A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102908327A (en) * | 2011-08-05 | 2013-02-06 | 江苏恒瑞医药股份有限公司 | Sustained release preparation for ivabradine or medicinal salt thereof |
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