Solid dispersion of tamoxifen citrate, method for preparing same and application thereof

Abstract

The invention discloses a solid dispersion of tamoxifen citrate. The solid dispersion of tamoxifen citrate consists of tamoxifen citrate, polyethylene glycol-6,000 and a flow aid, wherein the weight ratio of the tamoxifen citrate to the polyethylene glycol-6,000 is 1:4.5-12.5; and the flow aid is micropowder silica gel or talcpowder, and the dosage of the flow aid is 0.5 to 3 percent based on the total weight of the tamoxifen citrate and the polyethylene glycol-6,000. The solid dispersion of tamoxifen citrate can be made into orally taken solid preparations with high bioavailability and good absorbability, such as common tablets, dispersible tables, sustained release tablets and capsules, can be conveniently prepared, and the dissolution of the tamoxifen citrate can stably reach over 90 percent; and the preparation method has the advantages of low cost, easy operation, no special requirement on equipment, suitability for mass production and the like, and establishes a good relationship between the disintegration, dispersion and release speed and the medical dissolution of the solid dispersion of tamoxifen citrate.

Description

technical field The present invention relates to a kind of tamoxifen citrate solid dispersion and its preparation method and application, specifically, relate to a kind of tamoxifen citrate that can improve the dissolution rate of oral solid preparation of tamoxifen citrate The xifen solid dispersion and its preparation method and application belong to the technical field of pharmaceutical preparations. Background technique Tamoxifen Citrate, chemical name: (Z)-N,N-dimethyl-2-[4-(1,2-diphenyl-1-butenyl)phenoxy Base] - ethylamine citrate, the molecular formula is: C 26 h 29 NO·C 6 h 8 o 7 . The product is white or off-white crystalline powder, odorless; easily soluble in glacial acetic acid, soluble in methanol, slightly soluble in ethanol and acetone, very slightly soluble in chloroform, almost insoluble in water; melting point is 142~148℃, melting and decomposing at the same time. Tamoxifen is a non-steroidal anti-estrogen drug. Its structure is similar to estrogen....

AI Technical Summary

Problems solved by technology

The object of the present invention is to provide a kind of tamoxifen citrate solid dispersion and preparation method thereof and its application in the preparation of tamoxifen citrate oral solid preparations, to overcome the defects in the prior art, Solve the unreasonable relationship between the dissolution rate of tamoxifen citrate oral solid preparation and the disintegration and dispersion release of the preparation, and improve drug absorption and bioavailability