Composition of mifepristone semi-solid skeleton preparation

Abstract

The composition consists of: mifepristone 0.5-5 wt%, surfactant with HLB greater than 12 1-50 wt%, and semi-solid sleleton carrier 45-98.5 wt%. The composition has good leaching performance, powerful early pregnancy resisting effect, rat Ed50 as high as 17 times that of the marketed tablet and dog's biological utilization as high as 5 times that of the marketed tablet. Central double-blind clinical research shows that the present invention has threefold clinical effect as the marketed tablet. The mifepristone capsule of the present invention has the advantages of small dosage, less negative effect and high biological utilization.

Description

Technical field [0001] The invention relates to a mifepristone preparation. Background technique [0002] Mifepristone, its English name is mifepristone, and its chemical name is 11β-[4-(N,N-dimethylamino)phenyl]-17β-hydroxy-17α-(1propynyl)estrogen-4 , 9-dien-3-one 1,3, its structural formula is as follows: [0003] The molecular formula is C 29 H 35 NO 2 , The molecular weight is 429.61. [0004] Chinese patent 86102502 discloses mifepristone and its preparation method. Mifepristone is a receptor-level anti-progesterone antagonist, which has the effects of terminating early pregnancy, anti-implantation, inducing menstruation and promoting cervical ripening. It has been widely used clinically to prevent early pregnancy and emergency contraception, and has a good effect. New indications for treatment of uterine fibroids, endometriosis, breast cancer, depression, etc. are also under development and research. [0005] As a relatively novel endometrial progesterone receptor antagoni...

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved in the present invention is to disclose a semi-solid matrix preparation (Semi Solid Mairix) of mifepristone, that is, a substance with a waxy melting point is added to the medicinal liquid, which can be melted at high temperature and solid at room temperature. , compared with traditional powder particles, it can avoid the flying of drug powder (especially for hormones and anticancer drugs); the filling volume is uniform, and the dosage of the main drug is accurate; the drug or liquid is dispersed in the excipient and air and moisture It is isolated, so it is more stable; proper adjustment of the prescription can obtain the desired high bioavailability, in order to make the pharmacologically active substance mifepristone better absorbed in the body, achieve good curative effect and reduce adverse reactions at a lower dose