发明名称 Crystal entecavir, crystal entecavir formulation and methods for the preparation thereof
摘要 The present invention relates to a pharmaceutical composition for treating hepatitis B virus infection comprising crystalline entecavir as the pharmaceutically active ingredient and one or more pharmaceutically acceptable excipients. The tablet and capsule of the pharmaceutical composition have improved stability compared to that of amorphous entecavir under the conditions of light, high temperature and high humidity.
申请公布号 US9408849(B2) 申请公布日期 2016.08.09
申请号 US201414246029 申请日期 2014.04.04
申请人 Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical Factory 发明人 Yi Deping;Tian Zhike;Ye Weidong
分类号 A61K31/522;A61K9/20;A61K9/48;C07D473/18 主分类号 A61K31/522
代理机构 McNeely Hare & War, LLP 代理人 Hare William D.;McNeely Hare & War, LLP
主权项 1. A pharmaceutical composition for treating hepatitis B virus infection, comprising the crystal entecavir as the active ingredient and one or more pharmaceutically acceptable excipients, wherein: the crystal entecavir has the x-ray diffraction pattern of FIG. 1 and is present at an amount of from 0.001 mg to 25 mg; and the one or more pharmaceutically acceptable excipients comprise one or more of diluents, adhesives, glidants and disintegrants, wherein the diluents comprise one or more compounds selected from lactose, starch, sucrose, glucose, mannitol, xylitol, maltitol, dextrin, calcium sulfate and calcium phosphate, wherein the diluent is present at an amount of from 50% to 90% by weight of the total composition; the adhesives comprise one or more compounds selected from hydroxypropylmethylcellulose, alginic acid, sodium alginate, carbomer, poloxamer, and gelatin, wherein the adhesive is present in an amount of from 2% to 18% by weight of the total composition; the glidants comprise one or more compounds selected from silica, stearic acid, sodium stearate, calcium stearate, sodium lauryl sulfate, sucrose fatty acid ester, and talcum powder, wherein the glidant is present in an amount of from 0.1% to 5% by weight of the total composition; and the disintegrants comprising one or more compounds selected from hydroxypropyl cellulose, croscarmellose sodium, and crospovidone, the disintegrant is present in an amount of from 1% to 5% by weight of the total composition.
地址 Huancheng Donglu CN