Inclusion compound containing celecoxib and preparation method thereof

Abstract

The invention relates to an inclusion compound containing celecoxib and a preparation method thereof. The inclusion compound containing celecoxib comprises celecoxib and an inclusion material, wherein the inclusion material is preferable one or two of beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin; the weight ratio of the inclusion material to the celecoxib is (0.5-10):1. The preparation method comprises the following steps: respectively dissolving the inclusion material and the celecoxib in water and an organic solvent; slowly dropwise adding the saturated aqueous solution of the inclusion material into the organic solution containing the celecoxib; continuously stirring to form a white suspension; preparing the inclusion compound containing the celecoxib by adopting a vacuum drying or freeze-drying mode. The inclusion compound can be crushed to be prepared into various solid preparations. According to the inclusion compound containing celecoxib, the problem of extremely poor dissolubility of celecoxib in water can be solved, a high-bioavailability solid preparation with stable property can be prepared by adopting a simple and practical process, and the problem that a celecoxib raw material medicine is difficult to crush can be solved.

Description

technical field [0001] The invention relates to a celecoxib inclusion compound, a method for preparing the inclusion compound and a solid preparation containing the inclusion compound. Background technique [0002] Celecoxib is a coxib non-steroidal anti-inflammatory drug. It is a new generation of compounds with a unique mechanism of action, that is, it specifically inhibits cyclooxygenase-2. It is mainly used clinically for the treatment of osteoarthritis and rheumatoid arthritis. Treatment and adjuvant treatment of familial adenomatous polyps, this variety was approved for marketing in the United States in 1998. In September 2000, the State Food and Drug Administration approved the import sub-packaging of celecoxib of Pfizer Pharmaceuticals Co., Ltd. and put it on the market in China. So far, celecoxib has been approved for marketing in dozens of countries (regions). [0003] Celecoxib is a white to off-white crystalline powder, easily soluble in methanol, ethanol, acet...

AI Technical Summary

Problems solved by technology

[0003] Celecoxib is a white to off-white crystalline powder, easily soluble in methanol, ethanol, acetone and dimethyl sulfoxide, and almost insoluble in water, so oral absorption is poor. In order to improve its bioavailability, the patent number is 99802185.7 The patent literature reports that the D90 of celecoxib particles is less than 200um, preferably less than 100um in D90, more preferably less than 45um in D90, and most preferably less than 25um in D90 and made into preparations according to conventional methods to achieve effective bioavailability. Lecoxib raw material has low bulk density, and it is easy to bond into agglomerates during the pulverization process of raw materials, so micronization is relatively difficult, and the D90 is less than 35um after repeated jet pulverization, so industrial production is relatively difficult, so the present invention considers adopting a Inclusion technology to increase the solubility of celecoxib, thereby improving the bioavailability of various preparations, and can also solve the problem that celecoxib is easy to adsorb and difficult to crush

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