Statin oral self-microemulsifying release preparation and preparation method thereof

Abstract

The invention provides a statin oral self-microemulsifying release preparation and a preparation method thereof. The preparation comprises an effective amount of a statin self-microemulsifying concentrated solution and a medically acceptable carrier. The statin self-microemulsifying concentrated solution comprises, by weight, 1-10% of a calcium salt of (3R, 5S, 6E)-7-[6-fluoro-4,7-diphenylsulfo-quinolyl-3]yl-3,5-dihydroxy-6-heptenoic acid, 10-60% of an oil phase, 20-75% of an emulsifier, 2-45% of a co-emulsifier and 0-5% of an additive. The statin oral self-microemulsifying release preparation improves drug solubility, an oral administration absorption degree and a low cost and can be prepared by simple processes. The statin oral self-microemulsifying release preparation has a higher drug carrying amount and guarantees full dissolution of the statin drug. The statin drug is wrapped in a micro-emulsion and is protected so that drug stability in a human body is improved and a drug concentration in the liver as a targeting part is obviously improved without plasma drug concentration improvement.

Description

technical field [0001] The invention relates to a statin drug preparation and a preparation method thereof, in particular to (3R,5S,6E)-7-[6-fluoro-4,7-diphenylthio-quinolin-3]yl- Calcium 3,5-dihydroxy-6-heptenoate is an oral self-microemulsification drug release preparation and a preparation method thereof. Background technique [0002] Elevated plasma low-density lipoprotein cholesterol (LDL-C) concentration is one of the main causes of cardiovascular disease. 3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, namely statins, can inhibit the synthesis of mevalonate, a key substance in the rate-limiting step of cholesterol biosynthesis, and effectively reduce LDL -C concentration, thereby reducing the risk of cardiovascular disease. Due to the effectiveness and safety of statins, it has become the drug of choice for the treatment of hypercholesterolemia. Listed statins include lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, rosuvastati...

AI Technical Summary

Problems solved by technology

[0007] At present, the statin compound SMEDDS has problems such as low drug loading, incomplete dissolution after the formation of microemulsion, and drug precipitation. In addition, it does not increase the drug concentration in the blood circulation while increasing the drug concentration in the liver target site, so as to avoid side effects. It is also a statin. The key problems that need to be solved in the existence of compound SMEDDS

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