Double-layer sustained-release nifedipine tablet and preparation method thereof

A bilayer, nifedipine technology, applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, pill delivery, etc., can solve the problems of short half-life, large fluctuation of blood drug concentration, peak-to-valley phenomenon, etc.

Active Publication Date: 2011-07-06
COSCI MED TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Due to the short half-life of nifedipine oral capsules (T 1 / 2 =2-4h), the patient takes frequent medications, the blood drug concentration fluctuates greatly, and peak-valley phenomenon occurs, causing adverse reactions caused by reflex sympathetic excitement, such as headache, flushing, rapid heart rate, etc.

Method used

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  • Double-layer sustained-release nifedipine tablet and preparation method thereof
  • Double-layer sustained-release nifedipine tablet and preparation method thereof
  • Double-layer sustained-release nifedipine tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] prescription:

[0048] Immediate release layer:

Nifedipine

3.0g

[0049] Crospovidone XL

4.5g

Microcrystalline Cellulose 101

16.5g

Lactose Granulac200

30.0g

Povidone K30

4.5g

Micropowder silica gel

1.0g

Magnesium stearate

0.3g

water

Appropriate amount

Slow release layer:

Nifedipine

7.0g

Hypromellose 100LV

18.0g

Microcrystalline Cellulose 101

49.0g

Povidone K30

7.0g

Micropowder silica gel

2.0g

Magnesium stearate

0.7g

water

Appropriate amount

production

1000 pieces

[0050] Preparation:

[0051] (1) Material preparation: Nifedipine (Tianjin Zhongan Pharmaceutical Co., Ltd.) was micronized to a particle size range of 10-20 μm, and each component was weighed according to the prescription amount.

[0052] (2) Preparation of immediate-release granu...

Embodiment 2-8

[0070] prescription:

[0071]

[0072]

[0073] Preparation method: with embodiment 1, obtain the nifedipine double-layer sustained-release tablet of the present invention in the same manner as embodiment 1. Among them, mannitol was used from French Roquette Company, starch was used from Shenyang Yian Pharmaceutical Excipients Co., Ltd., sodium alginate was used from Yantai Xingfu Seaweed Industry Co., Ltd., and hydroxypropyl cellulose was used from Japan Soda Co., Ltd. Products, calcium hydrogen phosphate use the product of JRS in Germany, and pregelatinized starch use the product of Shanghai Colorcon Coating Technology Co., Ltd.

[0074] In order to investigate the in vitro release effect of the present invention, according to the release assay ("Chinese Pharmacopoeia" edition in 2005 two appendix X D first method), adopt the second method device of dissolution assay (operation in dark place), with hydrochloric acid solution (9 → 1000) 1000ml is the release medium, th...

Embodiment 9

[0079] Three batches of samples (batch numbers 090810, 090811, and 090812, each batch of 10,000 pieces) were amplified by the prescription process of Example 1, and the data of the three batches of amplified experiments are summarized in Table 2. in:

[0080] The release measurement method is the same as above.

[0081] Content determination method Avoid light operation. Take 20 tablets of this product, accurately weigh, grind finely, accurately weigh an appropriate amount (approximately equivalent to 30mg of nifedipine), put it in a mortar, add 2ml of chloroform, grind it, and quantitatively transfer it to a 100ml measuring bottle with absolute ethanol. , dilute to the mark with absolute ethanol, shake well, filter, discard the initial filtrate, accurately measure 5ml of the subsequent filtrate, put it in a 50ml measuring bottle, add absolute ethanol and release to the mark, shake well, and measure the UV-visible spectrophotometry Method (two appendix IV A of Chinese Pharma...

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Abstract

The invention relates to a double-layer sustained-release nifedipine tablet and a preparation method thereof, and the double-layer sustained-release nifedipine tablet is characterized by consisting of an immediate-release layer and a slow-release layer, wherein the nifedipine-containing proportion of the immediate-release layer and the slow-release layer, by weight, is 1:1 to 1:15. The invention belongs to medicine preparation technical field. The purpose of the invention is to provide a double-layer sustained-release nifedipine tablet capable of good patient compliance, little side-effect, fast acting and enduringly keeping stable effective plasma concentration. In addition, an another purpose of the invention is to provide a preparation method for double-layer sustained-release nifedipine tablet, and the method has the advantages of good reappearance of the preparation technology, high production efficiency, and is suitable for industrialized mass production and has good release homogeneity of the prepared double-layer sustained-release nifedipine tablet.

Description

technical field [0001] The invention relates to a nifedipine double-layer sustained-release tablet and a preparation method thereof, which is characterized in that the sustained-release tablet is composed of an immediate-release layer and a sustained-release layer, wherein the immediate-release layer and the sustained-release layer contain nifedipine The specific gravity is 1:1-1:15. It belongs to the technical field of pharmaceutical preparations. Background technique [0002] Nifedipine is a dihydropyridine calcium channel blocker, which can selectively inhibit the transmembrane transport of calcium ions into cardiomyocytes and smooth muscle cells, and inhibit the release of calcium ions from cells without changing the plasma calcium ion concentration, Thereby blocking the muscle contraction-coupling effect, causing smooth muscle relaxation and blood vessel expansion, so as to achieve the purpose of treating diseases. [0003] Nifedipine oral capsule was first approved f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K31/4422A61P9/12G01N21/33
Inventor 蒋海松王锦刚
Owner COSCI MED TECH CO LTD
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