Fenofibrate Composition

Abstract

The invention relates to a novel fenofibrate composition, in particular to a fenofibrate composition. The composition comprises i) an effective dose of fenofibrate, ii) oil, iii) polyvinyl pyrrolidone (PVP) and iv) a solid auxiliary material, and the composition is in a solid form. The invention also relates to a preparation method for the composition, a medicinal preparation containing the composition and application of the composition to the preparation of medicaments for treating and / or preventing diseases or symptoms which are related to dyslipidemia. The composition has advantages in aspects of the use of surfactants, production manipulation, storage stability, the convenience of administration, thermodynamic stability and the like.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to a novel fenofibrate composition, a method for preparing the composition, and pharmaceutical preparations containing the fenofibrate composition, such as hard capsules. Background technique [0002] Many drugs have the disadvantage of low solubility and insufficient dissolution in aqueous media, resulting in low bioavailability in organisms after oral administration. Thus, the required therapeutic dose must be increased to overcome this disadvantage. This is especially true for many active ingredients for lowering blood lipids, such as those belonging to fibrates. [0003] Fenofibrate, English name: fenofibrate, chemical name: 2-methyl-2-[4-(4-chlorobenzoyl)phenoxy]propionate isopropyl ester, molecular formula C 20 h 21 ClO 4 , Molecular weight: 360.84. The structural formula is as follows: [0004] [0005] Fenofibrate is a white or off-white crystallin...

AI Technical Summary

Problems solved by technology

Although the method disclosed in the above-mentioned EP-A-0330532 teaches to obtain a preparation with high bioavailability, the surfactants used therein will cause problems such as gastrointestinal irritation

[0008] Gao Xuefeng et al. (Chinese Journal of Pharmacy, 2007, Vol.5, No.6, p.288) disclosed a liquid fenofibrate preparation called self-emulsification, which consists of fenofibrate, ethyl oleate , Tween 80, PEG 400 (3.5:35:55:10, w / w), however, the literature further pointed out that "nonionic surfactants have low toxicity and good oral safety, but long-term use can stimulate the gastrointestinal mucosa It may cause changes in mucosal permeability and chronic toxicity to the system, and the alcohol used as a co-emulsifier also has certain irritating and pharmacological activities”

Chinese patent application 200810167197.2 discloses a liquid fenofibrate preparation called self-microemulsion, which consists of fenofibrate, MCT, oleic acid, EL-35, 1,2-propanediol (5:20:20: 40:20, w / w), also use a large amount of surfactant, there are also gastrointestinal irritation and toxicity problems

In addition, it should be noted that the self-emulsifying and self-microemulsifying preparations prepared in the above documents are all liquid preparations, and are not as good as solid preparations in terms of preparation, storage, administration, and inherent thermodynamic instability of liquid preparations.

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