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Medicine for improving bioavailability of atorvastatin

A technology of atorvastatin and availability, which is applied in the directions of drug combination, pharmaceutical formulation, plant raw material, etc., to achieve the effect of improving bioavailability, increasing curative effect and reducing clinical dosage

Active Publication Date: 2013-01-09
SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, drug metabolism experiments show that the absolute bioavailability of 10mg ATV after oral administration is only 14%.

Method used

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  • Medicine for improving bioavailability of atorvastatin
  • Medicine for improving bioavailability of atorvastatin
  • Medicine for improving bioavailability of atorvastatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation of water decoction - preclinical animal studies and clinical human studies

[0038] Get medicinal material and prepare water decoction by above-mentioned weight ratio:

[0039] Get medicinal material by following weight ratio:

[0040] Atractylodes 12%, Polygonum cuspidatum 16%, Magnolia officinalis 12%, Alisma 12%, Prunella vulgaris 40%, Licorice 8%

[0041] Soak all the medicines in 12 times the amount of water for 1 hour and then extract, decoct for 60 minutes for the first time, add 8 times the amount of water for the second time, decoct for 60 minutes, combine the decoctions, filter, and concentrate the filtrate under reduced pressure. spare.

Embodiment 2

[0042] Embodiment 2 prepares granules

[0043] Get medicinal material by following weight ratio:

[0044] Atractylodes 12%, Polygonum cuspidatum 16%, Magnolia officinalis 12%, Alisma 12%, Prunella vulgaris 40%, Licorice 8%,

[0045] Soak all the medicines in 12 times the amount of water for 1 hour and then extract, decoct for 60 minutes for the first time, add 8 times the amount of water for the second time, decoct for 60 minutes, combine the decoctions, filter, and concentrate the filtrate under reduced pressure. spare. Add ethanol under stirring to make the alcohol content reach 50%, leave it for 48 hours, filter, concentrate the filtrate until it has no alcohol smell, recover ethanol, and concentrate to obtain an extract; take 50% of the extract and spray dry it to obtain an extract powder; dry, Whole grains; bag the prepared grains.

Embodiment 3

[0046] Example 3 Test of Inhibiting Liver Drug Enzyme 3A4 in Vitro

[0047] The HMG-CoA inhibitor atorvastatin is metabolized by hepatic CYP450 drug-metabolizing enzyme 3A4 (CYP3A4) after oral administration. Evaluate the traditional Chinese medicine compound medicine of the present invention to avoid the metabolic failure of atorvastatin by inhibiting CYP3A4:

[0048] 1 . In vitro system: Mixed human liver microsomes were provided by Reid Disease Research (Shanghai) Co., Ltd. The use of human liver tissue complies with the principles stipulated in the Declaration of Helsinki and the International Ethical Guidelines for Human Biomedical Research. It is obtained from the discarded whole liver or liver lobe due to the failure of the recipient for transplantation for some reasons. The liver donor information includes informed consent and serological tests, and the donors are negative for HBV, HCV, HIV virus and venereal pathogens. Prepared by differential centrifugation [3] A...

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Abstract

The invention belongs to the field of a traditional Chinese medicine, and relates to a medicine for improving the bioavailability of atorvastatin as a HMG-CoA (beta-hydroxy-beta-methylglutaryl coenzyme A) inhibitor. The medicine screens, evaluates and optimizes a traditional Chinese medicine compound formula for treating hyperlipidaemia and coronary disease with the symptoms of spleen deficiency and damp obstruction, endogenous phlegm retention, stagnation of qi activity and edema and tumescence and the like, and the compound medicine for improving the bioavailability of atorvastatin is prepared from the traditional Chinese medicinal materials such as rhizoma atractylodis, polygonum cuspidatum, cortex magnoliae officinalis, rhizoma alismatis, spica prunellae and liquorice; the medicine improves the bioavailability of the HMG-CoA inhibitor atorvastatin through the metabolic interaction, and avoids the defects of the HMG-CoA inhibitor atorvastatin, and the efficacy of the medicine is improved due to the fact that the bioavailability of the atorvastatin is improved, and the medicine is safe and effective, and good in stability.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine, relates to a medicine for treating hyperlipidemia, in particular to a traditional Chinese medicine compound medicine for improving the bioavailability of an HMG-CoA inhibitor (atorvastatin). Background technique [0002] Studies have shown that statins block cholesterol biosynthesis by competitively inhibiting trihydroxytrimethylglutaryl coenzyme A (HMG-CoA) reductase, thereby reducing atherosclerotic low-density lipoprotein-cholesterol (LDL -C) Effect of content. In addition, this type of drug also has the effects of improving endothelial function, antiplatelet, antithrombotic, anti-inflammatory, and promoting the release of nitric oxide from coronary endothelium, so it can prevent plaque rupture, bleeding, and thrombus formation, stabilize plaque, and reduce coronary artery disease. The role of pulse events. A large amount of evidence-based medical evidence shows that active lipid-...

Claims

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Application Information

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IPC IPC(8): A61K36/884A61P3/06A61K31/40
Inventor 王肖龙王英杰沈智杰胡卓汉王白杨毛玉昌
Owner SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M
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