Preparation method of atorvastatin calcium capsule

A technology of atorvastatin calcium and capsules, which can be used in capsule delivery, metabolic diseases, active ingredients of heterocyclic compounds, etc., can solve problems such as unsatisfactory dissolution and bioavailability

Inactive Publication Date: 2012-01-11
HENAN TOPFOND PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, whether it is a commercially available tablet or capsule preparation, there are generally unsatisfactory problems in terms of dissolution and bioavailability.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The preparation method of 1000 atorvastatin calcium capsules:

[0022] Heat 10g of atorvastatin calcium raw material and 90g of PEG6000 together to 60°C to be in a molten state, quickly cool the mixture on a metal plate in an ice-water bath, dry it at a low temperature below 60°C for 24 hours, take out the solid dry matter, Pass through an 80-mesh sieve, try to keep a certain particle size, then add 50g of lactose, 49g of microcrystalline cellulose, and 1g of magnesium stearate, mix for 15 minutes, and fill the mixture of the prepared granules and powder into No. 2 capsules.

[0023] In order to verify that the present invention improves drug dissolution rate and bioavailability, we also cite two other preparation methods of capsules and compare them with existing tablets in the market.

Embodiment 4

[0030] Embodiment 4: effect comparative test

[0031] The atorvastatin calcium capsules prepared in Example 1 of the present invention, the atorvastatin calcium capsules prepared in Comparative Examples 2 and 3 and the commercially available tablets have been carried out in vitro dissolution rate and in vivo bioavailability comparative tests, the results are as follows :

[0032] 1. Dissolution comparative test:

[0033] Get 6 tablets of this product, according to dissolution assay (Chinese Pharmacopoeia 2005 edition two appendix X C the second method), the instrument that uses is the RCZ-8B drug dissolution apparatus that Tianjin University Radio Factory produces, and the second method device is made of stirring paddle and The dissolution vessel is composed of a dissolution vessel, and the deviation between the paddle shaft and the vertical axis of the dissolution vessel at any point shall not be greater than 2mm; the instrument is generally equipped with 6 sets of measuri...

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Abstract

The invention provides a preparation method of an atorvastatin calcium capsule preparation, and the method comprises the following steps: uniformly mixing amorphous atorvastatin calcium with a water-soluble solid dispersion carrier; heating to melt the solid dispersion carrier, and cooling and curing after the amorphous atorvastatin calcium is uniformly dispersed in the molten dispersion carrier; drying the obtained mixture at a low temperature to obtain mixture particles; and then mixing the obtained particles with other medicinal auxiliary materials, and filling into capsules. By utilizing the preparation method provided by the invention, the dispersion degree of the atorvastatin calcium raw material is improved, the granularity of the medicament is reduced, and the specific surface area is increased, so that the dissolution rate is improved.

Description

technical field [0001] The invention relates to a preparation for treating primary hypercholesterolemia and a preparation method thereof, in particular to an atorvastatin calcium capsule preparation for treating primary hypercholesterolemia and its preparation method. Background technique [0002] The chemical name of atorvastatin calcium is: [R-(R,R)]-2-(4-fluorophenyl)-β,β-dihydroxy-5-(1-methylethyl)-3- Phenyl-4-[(aniline)carbonyl]-1hydro-pyrrole-1-calcium heptanoate trihydrate is a selective and competitive 3-hydroxy-3-methylglutaryl-CoA (HMG -C 0 A) Reductase inhibitor, the lipid-lowering effect is higher than other HMG-C 0 A reductase inhibitor. Patients with primary hypercholesterolemia, including those with familial hypercholesterolemia (heterozygous type) or mixed hyperlipidemia (equivalent to Fredrickson types IIa and IIb), if treated with diet and other nonpharmacologic treatments If the curative effect is not satisfactory, the application of this product can ...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/40A61K47/34A61P3/06
Inventor 毛新付李富志吕兰亭宋喜芳王晓峰焦国华窦建华刘黎静邵曙光朱义彬王颖慧陈运来郑杰邱银霞唐世宏曹济宁
Owner HENAN TOPFOND PHARMA
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