CN101669949A - Compound simvastatin nicolar sustained release capsule and preparation method thereof - Google Patents
Compound simvastatin nicolar sustained release capsule and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a compound simvastatin nicolar sustained release capsule and a preparation method thereof. The capsule contains 5-10 mg of simvastatin and 250 mg of nicolar and is prepared bythe following steps: preparing a blank core of a simvastatin fast-release micropill; preparing a coating solution of the simvastatin fast-release micropill; preparing the simvastatin fast-release micropill; preparing a core of a nicolar sustained release micropill; preparing a coating solution of the nicolar sustained release micropill; preparing the nicolar sustained release micropill; and preparing the compound simvastatin nicolar sustained release capsule. The nicolar is used as a sustained release component and the simvastatin is used as a fast-release component, thereby the invention is suitable for treating hypercholesterolemia and mixed dyslipidemia.
Description
Technical field
The present invention relates to a kind of compound simvastatin nicolar sustained release capsule and preparation method thereof.
Background technology
In recent years, along with people living condition's the improvement and the variation of dietary habit, the sickness rate of hypercholesterolemia and mixing dyslipidemia increases gradually.Hypercholesterolemia and mixing dyslipidemia are atherosclerotic main causes, and then cause the heart, cerebrovascular disease, comprise coronary heart disease, apoplexy, myocardial infarction etc., the serious harm human beings'health.At present, in various diseases, the M ﹠ M of the heart, cerebrovascular disease all occupies first.
In lipid composition, cholesterol and triglyceride are too high to be atherosclerosis and the main inducing that further causes the heart, cerebrovascular disease; High density lipoprotein is then just in time opposite, can and excrete cholesterol decomposition, therefore is called as " the arteriosclerosis factor ", " good cholesterol ", " the protection factor of coronary heart disease " etc.
Use wider blood lipid regulation medicine to have three kinds at present clinically: first kind, the HMG-CoA reductase inhibitor claims " his spit of fland " class again, based on cholesterol reducing; Second kind, fibric acid claims " Bei Te " class again, based on triglyceride reducing; The third, nicotinic acid and derivant thereof based on high density lipoprotein increasing, also have the effect of certain cholesterol reducing and triglyceride.These medicines all have good drug effect, but curative effect is single, can not satisfy patient's needs, and the compound preparation of therefore developing multiple curative effect is significant.
Nicotinic acid, chemical name are Nicotinicum Acidum, belong to vitamin B group, and chemical structural formula is as follows:
Nicotinic acid has the effect of tangible blood lipid regulation.The main mechanism of nicotinic acid blood lipid regulation is to suppress the formation of cAMP, cause the triglyceride enzymatic activity to reduce, the lipolysis in the fatty tissue slows down, the lowering of concentration of non-esterified fatty acid in the blood (NEFA), the synthetic VLDL of liver reduces, and IDL and LDL are also reduced.In addition, nicotinic acid can synthesize nitocinoylglycine with glycine under the effect of coenzyme A, utilize the coenzyme A synthetic cholesterol thereby hinder hepatocyte.Except triglyceride reducing and cholesterol, nicotinic acid is high density lipoprotein increasing significantly.Therefore, nicotinic acid is that a unique class can make the medicine of all lipid compositions towards the positive direction development and change, can have been reduced the sickness rate and the general mortality rate of the heart, cerebrovascular disease by the clinical research proof.
The common dose that nicotinic acid is used for blood lipid regulation is bigger, is 0.5-2 gram every day.But nicotinic acid has serious adverse effects under heavy dose, comprises erubescence, liver toxicity etc., makes that the toleration of nicotinic acid and drug compliance are poor, has limited the application of nicotinic acid greatly.And nicotinic acid is very fast the human body metabolism, about 45 minutes of half-life, need take medicine every day more than 3 times, and patient's compliance is relatively poor.
Therefore, in the present invention, nicotinic acid is designed to the slow release composition, make nicotinic acid in 12 hours slowly, continue, evenly discharge, the every day of each medication sooner or later once, good patient compliance; Simultaneously, the slow release process makes nicotinic acid two metabolic pathways in vivo obtain balance, thereby has reduced untoward reaction such as erubescence and liver toxicity.
Simvastatin, chemistry is called 2,2-acid dimethyl-8-[(4R, 6R)-and 6-2-[(1S, 2S, 6S, 8S, 8aR)-1,2,6,7,8, and 8a-hexahydro-8-hydroxy-2,6-dimethyl-1-naphthyl] ethyl tetrahydrochysene-4-hydroxyl-2H-pyran-2-one] ester, chemical structural formula is as follows:
Simvastatin is the HMG-CoA reductase inhibitor, can suppress the synthetic of endogenous cholesterol, significantly reduces plasma cholesterol concentration.Slight because simvastatin is evident in efficacy, untoward reaction is few, it has become one of the most frequently used blood lipid-lowering medicine in the whole world at present, is mainly used in the treatment hypercholesterolemia clinically.
In the present invention, with nicotinic acid as slow-released part, simvastatin is as immediate release section, can make each component bring into play synergism in vivo, comprehensive blood lipid regulation composition, thus bring into play drug effect to greatest extent, can reduce the toxic and side effects of medicine again, reduce blood drug level fluctuation in vivo, reduce patient's medicining times; And the design of micropill has greatly improved medicine and gastral contact area, makes bioavailability of medicament significantly improve; Be applicable to the treatment hypercholesterolemia and mix dyslipidemia.
Summary of the invention
The object of the present invention is to provide a kind of compound simvastatin nicolar sustained release capsule and preparation method thereof.
Compound simvastatin nicolar sustained release capsule of the present invention, every capsules contain 5mg or 10mg simvastatin and 250mg nicotinic acid.
Compound simvastatin nicolar sustained release capsule of the present invention is prepared by following steps:
(1) preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly.
(2) preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly.
(3) preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish about 5%, screening 16-30 order micropill, promptly.
(4) preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly.
(5) preparation of niacin sustained release micropill coating solution: get 100g Sulisi coating powder, add 1000ml water, mixing, promptly; Or get the strange NE30D of 417g You Te, 125g Pulvis Talci, and add 458ml water, mixing, promptly.
(6) preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, about weightening finish 5%-10%, screening 16-30 order micropill, promptly.
(7) preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 5mg or 10mg, nicotinic acid 250mg calculate loading amount and the ratio of two kinds of micropills in capsule according to every capsules.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
According to the compound simvastatin niacin sustained release tablet that the inventive method is made, wherein slow in 12 hours, lasting, the evenly release of nicotinic acid has the good slow release effect; Simvastatin was stripping more than 80% at 30 minutes, and good rapid release effect is arranged.Slow release composition nicotinic acid and rapid release composition simvastatin are formed compound preparation, can make each component bring into play synergism in vivo, comprehensively the blood lipid regulation composition, thereby bring into play drug effect to greatest extent, can reduce the toxic and side effects of medicine again, reduce blood drug level fluctuation in vivo, reduce patient's medicining times; And the design of micropill has greatly improved medicine and gastral contact area, makes bioavailability of medicament significantly improve; Be applicable to the treatment hypercholesterolemia and mix dyslipidemia.
The specific embodiment
Below describe several preferred implementation of the present invention, but be not in order to limit the present invention.
Embodiment 1:
The preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly.
The preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly.
The preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly.
The preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly.
The preparation of niacin sustained release micropill coating solution: get 100g Sulisi coating powder, add 1000ml water, mixing, promptly.
The preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly.
The preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 5mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
In the gained compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 5mg and nicotinic acid 250mg.
Embodiment 2:
The preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly.
The preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly.
The preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly.
The preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly.
The preparation of niacin sustained release micropill coating solution: get 100g Sulisi coating powder, add 1000ml water, mixing, promptly.
The preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly.
The preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 10mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
In the gained compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 10mg and nicotinic acid 250mg.
Embodiment 3:
The preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly.
The preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly.
The preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly.
The preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly.
The preparation of niacin sustained release micropill coating solution: get the strange NE30D of 417g You Te, 125g Pulvis Talci, add 458ml water, mixing, promptly.
The preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish 10%, screening 16-30 order micropill, promptly.
The preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 5mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
In the gained compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 5mg and nicotinic acid 250mg.
Embodiment 4:
The preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly.
The preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly.
The preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly.
The preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly.
The preparation of niacin sustained release micropill coating solution: get the strange NE30D of 417g You Te, 125g Pulvis Talci, add 458ml water, mixing, promptly.
The preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish 10%, screening 16-30 order micropill, promptly.
The preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 10mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
In the gained compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 10mg and nicotinic acid 250mg.
Facts have proved, compound simvastatin nicolar sustained release capsule of the present invention, wherein nicotinic acid has the good slow release effect; Simvastatin has good rapid release effect.
In order further to investigate niacin sustained release effect of the present invention,, carry out following research according to two appendix XD of Chinese Pharmacopoeia version in 2005 drug release determination method, first method:
Getting this product, is dissolution medium with pure water 900ml, adopts the basket method of changeing, and rotating speed is that per minute 100 changes, operation in accordance with the law, and it is an amount of to get solution in the 1st, 2,4,6,8,12 hour, filters, and subsequent filtrate is as need testing solution.It is an amount of that other gets this product, grinds, and precision takes by weighing the fine powder that is equivalent to average loading amount, adds pure water, ultrasonic, makes the abundant stripping of nicotinic acid, filters, and gets subsequent filtrate solution in contrast.Press the quality standard operation.The nicotinic acid release result of embodiment sample is as shown in table 1:
The nicotinic acid release result of table 1 embodiment sample
| Time (hour) | ??1 | ??2 | ??4 | ??6 | ??8 | ??12 |
| Embodiment 1 | ??22.04％ | ??36.25％ | ??54.65％ | ??75.96％ | ??84.24％ | ??93.50％ |
| Embodiment 2 | ??22.98％ | ??37.33％ | ??55.72％ | ??76.48％ | ??85.98％ | ??94.99％ |
| Embodiment 3 | ??23.86％ | ??38.07％ | ??56.87％ | ??78.66％ | ??88.41％ | ??97.25％ |
| Embodiment 4 | ??23.51％ | ??37.94％ | ??56.15％ | ??77.38％ | ??87.28％ | ??96.80％ |
By table 1 as seen, slow in 12 hours, lasting, the evenly release of nicotinic acid has the good slow release effect.
In order further to investigate simvastatin rapid release effect of the present invention,, carry out following research according to two appendix XC of Chinese Pharmacopoeia version in 2005 dissolution method, first method:
Get this product, (get sodium lauryl sulphate 5g with the phosphate buffer that contains 0.5% sodium lauryl sulphate, sodium dihydrogen phosphate 1.2g is dissolved in the 1000ml water, regulates pH to 7.0 with sodium hydroxide solution) 900ml is dissolution medium, adopt the basket method of changeing, rotating speed is that per minute 100 changes, operation in accordance with the law, and it is an amount of to get solution in the 15th, 30,45 minute, filter, subsequent filtrate is as need testing solution.It is an amount of that other gets this product, grinds, and precision takes by weighing the fine powder that is equivalent to average loading amount, adds methanol, ultrasonic, makes the abundant stripping of simvastatin, filters, and gets subsequent filtrate solution in contrast.Press the quality standard operation.The simvastatin dissolution result of embodiment sample is as shown in table 2:
The simvastatin dissolution result of table 2 embodiment sample
| Time (minute) | ??15 | ??30 | ??45 |
| Embodiment 1 | ??77.19％ | ??90.55％ | ??93.25％ |
| Embodiment 2 | ??75.90％ | ??87.70％ | ??91.92％ |
| Embodiment 3 | ??78.58％ | ??91.63％ | ??94.87％ |
| Embodiment 4 | ??76.12％ | ??89.71％ | ??92.24％ |
By table 2 as seen, simvastatin was stripping more than 80% at 30 minutes, and good rapid release effect is arranged.
Experimental result shows, simvastatin niacin sustained release tablet of the present invention can make each component bring into play synergism in vivo, comprehensive blood lipid regulation composition, thus bring into play drug effect to greatest extent, can reduce the toxic and side effects of medicine again, reduce blood drug level fluctuation in vivo, reduce patient's medicining times; And the design of micropill has greatly improved medicine and gastral contact area, makes bioavailability of medicament significantly improve; Be applicable to the treatment hypercholesterolemia and mix dyslipidemia.
Claims (4)
1. a compound simvastatin nicolar sustained release capsule is characterized in that, in the described compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 5mg and nicotinic acid 250mg; Described compound simvastatin nicolar sustained release capsule is prepared by following steps:
(1) preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly;
(2) preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly;
(3) preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly;
(4) preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly;
(5) preparation of niacin sustained release micropill coating solution: get 100g Sulisi coating powder, add 1000ml water, mixing, promptly;
(6) preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly;
(7) preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 5mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
2. a compound simvastatin nicolar sustained release capsule is characterized in that, in the described compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 10mg and nicotinic acid 250mg; Described compound simvastatin nicolar sustained release capsule is prepared by following steps:
(1) preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly;
(2) preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly;
(3) preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly;
(4) preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly;
(5) preparation of niacin sustained release micropill coating solution: get 100g Sulisi coating powder, add 1000ml water, mixing, promptly;
(6) preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish 5%, screening 16-30 order micropill, promptly;
(7) preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 10mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
3. a compound simvastatin nicolar sustained release capsule is characterized in that, in the described compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 5mg and nicotinic acid 250mg; Described compound simvastatin nicolar sustained release capsule is prepared by following steps:
(1) preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly;
(2) preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly;
(3) preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish about 5%, screening 16-30 order micropill, promptly;
(4) preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly;
(5) preparation of niacin sustained release micropill coating solution: get the strange NE30D of 417g You Te, 125g Pulvis Talci, add 458ml water, mixing, promptly;
(6) preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish about 10%, screening 16-30 order micropill, promptly;
(7) preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 5mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
4. a compound simvastatin nicolar sustained release capsule is characterized in that, in the described compound simvastatin nicolar sustained release capsule, every capsules contains simvastatin 10mg and nicotinic acid 250mg; Described compound simvastatin nicolar sustained release capsule is prepared by following steps:
(1) preparation of simvastatin fast release micropill celphere: get microcrystalline Cellulose 100g, add suitable quantity of water and make soft material, use is extruded spheronizator and is made celphere, after the drying, and screening 18-30 order micropill, promptly.
(2) preparation of simvastatin fast release micropill coating solution: get hypromellose 60g, Polyethylene Glycol 6g, simvastatin 36g, be dissolved in 1000ml 80% alcoholic solution, promptly.
(3) preparation of simvastatin fast release micropill: get simvastatin fast release micropill celphere 50g, place fluid bed, spray into simvastatin fast release micropill coating solution, weightening finish about 5%, screening 16-30 order micropill, promptly.
(4) preparation of niacin sustained release fine pellet core: get microcrystalline Cellulose 50g, nicotinic acid 50g adds suitable quantity of water and makes soft material, and use is extruded spheronizator and made the ball core that contains nicotinic acid, after the drying, and screening 18-30 order micropill, promptly.
(5) preparation of niacin sustained release micropill coating solution: get the strange NE30D of 417g You Te, 125g Pulvis Talci, add 458ml water, mixing, promptly.
(6) preparation of niacin sustained release micropill: get niacin sustained release fine pellet core 50g, place fluid bed, spray into niacin sustained release micropill coating solution, weightening finish about 10%, screening 16-30 order micropill, promptly.
(7) preparation of compound simvastatin nicolar sustained release capsule: measure the content of simvastatin and nicotinic acid in simvastatin fast release micropill and the niacin sustained release micropill respectively, contain simvastatin 10mg, nicotinic acid 250mg according to every capsules and calculate loading amount and the ratio of two kinds of micropills in capsule.Take by weighing two kinds of micropills in proportion respectively, put in the mixer, mix homogeneously will mix micropill by the loading amount of calculating and incapsulate, promptly.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103432103A (en) * | 2013-09-11 | 2013-12-11 | 中国药科大学 | Compound nicotinic acid sustained-release capsules and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103432103A (en) * | 2013-09-11 | 2013-12-11 | 中国药科大学 | Compound nicotinic acid sustained-release capsules and preparation method thereof |
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