CN101468009A - Method for preparing manidipine sustained release tablets and use thereof - Google Patents
Method for preparing manidipine sustained release tablets and use thereof Download PDFInfo
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- CN101468009A CN101468009A CNA2007103084422A CN200710308442A CN101468009A CN 101468009 A CN101468009 A CN 101468009A CN A2007103084422 A CNA2007103084422 A CN A2007103084422A CN 200710308442 A CN200710308442 A CN 200710308442A CN 101468009 A CN101468009 A CN 101468009A
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- manidipine
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Abstract
The invention belongs to the novel technical field of medicament and specifically relates to a preparation method of manidipine sustained release tablets and use thereof. The tablets are used for treating high blood pressure. The novel dosage form is characterized in that the products are sustained release tablets. Each tablet contains manidipine 10mg-100mg, preferably 20mg-60mg. The objective of the invention is to provide sustained release tablets having good stability, high quality and obvious curative effect, and taking manidipine as a main medicament, and preparation method thereof. The inventive Chinese traditional medicine is slowly released so as to maintain relatively stable blood concentration and longer action time, and has advantages of reducing side effect, more convenient administration etc.
Description
Technical field
The invention belongs to the medicine new technical field, a kind of novel form that relates to Manidipine, be used for the treatment of pharmaceutical preparation with the overactive bladder of urge incontinence, urgent micturition, frequent micturition symptom and preparation method thereof, a kind of preparation method of manidipine sustained release tablets and application thereof specifically.
Background technology
Hypertension is one of modal cardiovascular disease in the world today.Recent statistics result according to health ministry announcement on October 12nd, 2004 shows that China 18 years old and above resident's hypertension prevalence are 18.8%, estimate national number of patients more than 1.6 hundred million.Compared with 1991, prevalence rises 31%, and number of patients increases about more than 7,000 ten thousand people.The rural area prevalence rises rapidly, and the town and country gap is not obvious.Big city, small and medium-sized cities, one to four class rural area hypertension prevalence are followed successively by 20.4%, 18.8%, 21.0%, 19.0%, 20.2% and 12.6%.In the huge hyperpietic group of China's quantity, the hypertension awareness is 30.2% in addition, and treatment rate is 24.7%, and control rate only is 6.1%; With 26.6%, 12.2% compare with 2.9% and to increase in 1991, but still be in relatively poor level.Hypertension is the important risk factor that causes apoplexy, coronary heart disease and renal failure, and in clinical trial, antihypertensive therapy on average can reduce by 35-40% apoplexy and take place, 20-25% myocardial infarction and surpass 50% heart failure.This shows that research antihypertensive agent market potential is very huge.
" 2000 market forces: antihypertensive drug " prediction: by 2007, global antihypertensive drug market value will be above 52,000,000,000 dollars, and calcium-channel antagonists will be positioned at 10 leading product ranks.
Calcium-channel antagonists is by the selective exclusion voltage dependent channel, and lax vascular smooth muscle brings high blood pressure down.First generation calcium-channel antagonists is fugitive chemical compound, easily causes turn back chamber speed and sympathetic activity; As nifedipine; Second filial generation calcium-channel antagonists is the chemical compound that plasma half-life prolongs, as amlodipine; Third generation calcium-channel antagonists is the height lipophilic compound, and very strong membrane-binding slowly is discharged into calcium channel, and onset slowly and lastingly.
Manidipine is a kind of lipophilic, and third generation bihydropyridine type calcium-channel antagonists has high selectivity to vascular smooth muscle, therefore can induce peripheral vasodilation significantly, and the heart inhibitory action is very slight.In addition, Manidipine can the appreciable impact noradrenaline levels, shows that it can not influence sympathetic nervous system.Effect engenders but lasting behind this drug administration, can only take once every day.Manidipine can be exported and the input tremulous pulse by the diastole kidney, and kidney is had certain benefit, and also uncorrelated to effect and its antihypertensive function of kidney.Every day, an oral Manidipine was to light effective and toleration is good to the moderate hypertension patient.It should be noted that in a large-scale double blinding clinical trial patient of Manidipine group generation ankle edema will significantly be less than the amlodipine group.Manidipine also is suitable for the hypertensive patient that complication is arranged, for example type 2 diabetes mellitus and renal function injury.Manidipine can improve insulin sensitivity and not influence metabolic function.In brief, Manidipine can be used as the line medication use that constitutional gently arrives moderate hypertension.
CV-4093 is by the exploitation listing of Japan military field medicine Co., Ltd., back Chiesi company adds and carries out market development jointly, mainly be conceived to the European market, at present in nearly ten Eurasian national registration listings such as Japan, France, Italy, Greece, Spain, Korea S, external specification has 5,10,20mg, and price is roughly equal to 10 yuan/sheet of RMB (10mg).Listing does not at home have import yet.
Chemical structural formula:
Molecular formula: C
35H
38N
4O
6
Molecular weight: 610.70
This product has following characteristics:
This product is a slow releasing tablet, the release medicine of non-constant speed slowly in the release medium of regulation.
Summary of the invention
The object of the invention be to provide a kind of good stability, quality height, evident in efficacy, untoward reaction is little is slow releasing tablet of making of principal agent and preparation method thereof with the Manidipine, uses manidipine sustained release tablets that this method the makes release medicine of non-constant speed slowly in the release medium of regulation.
Manidipine sustained release tablets is including but not limited to following adjuvant: one or more mixing wherein such as No. 3, acrylic resin, microcrystalline Cellulose, lactose, starch, magnesium stearate, Pulvis Talci, hydroxypropyl emthylcellulose series, Polyethylene Glycol series, dextrin, mannitol, methylcellulose, ethyl cellulose.
This invention is that every contained Manidipine is 10mg～100mg, preferred 20mg～60mg.
A kind of slow releasing tablet that contains Manidipine of the present invention is made up of following component, but is not limited to these components:
40 parts of Manidipines
20 parts of No. 3, acrylic resins
Hydroxypropyl emthylcellulose K
4M20 parts
90 parts of microcrystalline Cellulose
50 parts of lactose
80 parts of PEG6000
2%pvp ethanol liquid is an amount of
Magnesium stearate is an amount of
The prescription of coating solution
5 parts of hydroxypropyl emthylcelluloses
PEG400 part
1.5 parts of Pulvis Talci
Distilled water 30ml
80% ethanol liquid adds to 100ml
A kind of slow releasing tablet that contains Manidipine of the present invention is achieved through the following technical solutions:
Manidipine is crossed 120 mesh sieves, take by weighing the Manidipine of prescription proportional quantities, No. 3, acrylic resin, microcrystalline Cellulose, HPMC K
4M, lactose, PEG6000 mix homogeneously, with 2%PVP ethanol liquid system soft material.18 mesh sieves are granulated, 70～80 degree oven dry, and 18 mesh sieve granulate add stearic magnesium, mixing, tabletting, coating, promptly.
A kind of slow releasing tablet that contains Manidipine that the present invention obtains has that method is simple, good stability, characteristics that quality is high.
Embodiment 1: 1000 of specifications
Prescription:
Manidipine 40g
No. 3 20g of acrylic resin
Hydroxypropyl emthylcellulose K
4M20g
Microcrystalline Cellulose 90g
Lactose 50g
PEG6000 80g
2%pvp ethanol liquid is an amount of
Magnesium stearate is an amount of
The prescription of coating solution
Hydroxypropyl emthylcellulose 5g
PEG400 g
Pulvis Talci 1.5g
Distilled water 30ml
80% ethanol liquid adds to 100ml
Method for making:
Manidipine is crossed 120 mesh sieves, take by weighing the Manidipine of prescription proportional quantities, No. 3, acrylic resin, microcrystalline Cellulose, HPMC K
4M, lactose, PEG6000 mix homogeneously, with 2%PVP ethanol liquid system soft material.18 mesh sieves are granulated, 70～80 degree oven dry, and 18 mesh sieve granulate add stearic magnesium, mixing, tabletting, coating, promptly.
Embodiment 2: 10000 of specifications
Prescription:
Manidipine 400g
No. 3 200g of acrylic resin
Hydroxypropyl emthylcellulose K
4M200g
Microcrystalline Cellulose 900g
Lactose 500g
PEG6000 800g
2%pvp ethanol liquid is an amount of
Magnesium stearate is an amount of
The prescription of coating solution
Hydroxypropyl emthylcellulose 50g
Macrogol 4000 g
Pulvis Talci 15g
Distilled water 300ml
80% ethanol liquid adds to 1000ml
Method for making:
Manidipine is crossed 120 mesh sieves, take by weighing the Manidipine of prescription proportional quantities, No. 3, acrylic resin, microcrystalline Cellulose, HPMC K
4M, lactose, PEG6000 mix homogeneously, with 2%PVP ethanol liquid system soft material.18 mesh sieves are granulated, 70～80 degree oven dry, and 18 mesh sieve granulate add stearic magnesium, mixing, tabletting, coating, promptly.
Claims (9)
1. the preparation method of manidipine sustained release tablets and application thereof is characterized in that this slow releasing tablet is is the tablet that principal agent is made with the Manidipine.
2. according to the preparation method and the application thereof of the described manidipine sustained release tablets of claim 1, it is characterized in that the contained Manidipine of this slow releasing tablet is 10mg～100mg, preferred 20mg～60mg.
3. according to the preparation method and the application thereof of the described manidipine sustained release tablets of claim 1, it is characterized in that this slow releasing tablet release medicine of non-constant speed slowly in the release medium of regulation.
4. according to the preparation method and the application thereof of the described manidipine sustained release tablets of claim 1, it is characterized in that this slow releasing tablet is to be used for the treatment of hypertension.
5. according to the preparation method and the application thereof of the described manidipine sustained release tablets of claim 1, it is characterized in that including but not limited to following component:
40 parts of Manidipines
20 parts of No. 3, acrylic resins
Hydroxypropyl emthylcellulose K
4M20 parts
90 parts of microcrystalline Cellulose
50 parts of lactose
80 parts of PEG6000
2%pvp ethanol liquid is an amount of
Magnesium stearate is an amount of
The prescription of coating solution
5 parts of hydroxypropyl emthylcelluloses
PEG400 part
1.5 parts of Pulvis Talci
Distilled water 30ml
80% ethanol liquid adds to 100ml
6. according to the preparation method and the application thereof of the described manidipine sustained release tablets of claim 5, it is characterized in that including but not limited to following adjuvant: one or more mixing wherein such as No. 3, acrylic resin, microcrystalline Cellulose, lactose, starch, magnesium stearate, Pulvis Talci, hydroxypropyl emthylcellulose series, Polyethylene Glycol series, dextrin, mannitol, methylcellulose, ethyl cellulose.
7. according to the preparation method and the application thereof of the described manidipine sustained release tablets of claim 5, it is characterized in that described solvent is distilled water, 80% ethanol liquid, but be not limited to these solvents.
8. the preparation method of manidipine sustained release tablets according to claim 5 and application thereof, one of prescription that it is characterized in that this slow releasing tablet is:
Manidipine 40g
No. 3 20g of acrylic resin
Hydroxypropyl emthylcellulose K
4M20g
Microcrystalline Cellulose 90g
Lactose 50g
PEG6000 80g
2%pvp ethanol liquid is an amount of
Magnesium stearate is an amount of
The prescription of coating solution
Hydroxypropyl emthylcellulose 5g
PEG400 g
Pulvis Talci 1.5g
Distilled water 30ml
80% ethanol liquid adds to 100ml
9. the preparation method of the preparation method of manidipine sustained release tablets according to claim 8 and application thereof is characterized in that including but not limited to following steps:
Preparation technology: Manidipine is crossed 120 mesh sieves, take by weighing the Manidipine of prescription proportional quantities, No. 3, acrylic resin, microcrystalline Cellulose, HPMC K
4M, lactose, PEG6000 mix homogeneously, with 2%pvp ethanol liquid system soft material.18 mesh sieves are granulated, 70～80 degree oven dry, and 18 mesh sieve granulate add stearic magnesium, mixing, tabletting, coating, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007103084422A CN101468009A (en) | 2007-12-29 | 2007-12-29 | Method for preparing manidipine sustained release tablets and use thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007103084422A CN101468009A (en) | 2007-12-29 | 2007-12-29 | Method for preparing manidipine sustained release tablets and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101468009A true CN101468009A (en) | 2009-07-01 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2007103084422A Pending CN101468009A (en) | 2007-12-29 | 2007-12-29 | Method for preparing manidipine sustained release tablets and use thereof |
Country Status (1)
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| CN (1) | CN101468009A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102415998A (en) * | 2010-09-28 | 2012-04-18 | 扬子江药业集团北京海燕药业有限公司 | Manidipine hydrochloride solid dispersion and preparation method thereof |
| CN102988325A (en) * | 2012-10-08 | 2013-03-27 | 李正梅 | Preparation method of manidipine sustained release tablet |
| CN103120651A (en) * | 2011-11-21 | 2013-05-29 | 四川海思科制药有限公司 | Manidipine tablet |
-
2007
- 2007-12-29 CN CNA2007103084422A patent/CN101468009A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102415998A (en) * | 2010-09-28 | 2012-04-18 | 扬子江药业集团北京海燕药业有限公司 | Manidipine hydrochloride solid dispersion and preparation method thereof |
| CN103120651A (en) * | 2011-11-21 | 2013-05-29 | 四川海思科制药有限公司 | Manidipine tablet |
| CN103120651B (en) * | 2011-11-21 | 2014-11-05 | 四川海思科制药有限公司 | Manidipine tablet |
| CN102988325A (en) * | 2012-10-08 | 2013-03-27 | 李正梅 | Preparation method of manidipine sustained release tablet |
| CN102988325B (en) * | 2012-10-08 | 2014-04-02 | 广西南宁科冠医药科技开发有限公司 | Preparation method of manidipine sustained release tablet |
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Open date: 20090701 |