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A pharmaceutical formulation of palbociclib and a preparation method thereof
A pharmaceutical formulation of palbociclib and a preparation method thereof
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机译：palbociclib的药物制剂及其制备方法
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摘要
The present invention relates to a pharmaceutical composition of palbociclib in the form of an amorphous solid dispersion for use in the treatment of breast cancer, such as metastatic breast cancer. The amorphous solid dispersion comprising: palbociclib or a pharmaceutically acceptable salt thereof; an acidic auxiliary material comprising more than one pharmaceutically acceptable acid, at least one of which is an organic acid; and a hydrophilic high molecular weight material. The acidic auxiliary material may comprise one or more pharmaceutically acceptable inorganic acids as well as the at least one organic acid. The pharmaceutically acceptable organic acid may be tartaric acid, fumaric acid, succinic acid, citric acid, lactic acid, malic acid, an aliphatic sulfonic acid, or an aromatic sulfonic acid. The aliphatic sulfonic acid may be methanesulfonic acid, ethanesulfonic acid, or isethionic acid. The aromatic sulfonic acid may be benzenesulfonic acid or p-toluenesulfonic acid. The pharmaceutically acceptable inorganic acid may be hydrochloric acid, sulfuric acid, or phosphoric acid. The hydrophilic high-molecular weight material may be povidone K30, copovidone VA64 (PVP VA64), Soluplus, hydroxypropylmethylcellulose E5, hydroxypropylmethylcellulose acetate succinate, hydroxypropyl-β-cyclodextrin, or sulfobutyl ether-β-cyclodextrin. The mass ratio of the high molecular weight material to palbociclib may be from 0.1:1 to 10:1 and the mass ration of the acidic auxiliary material to palbociclib may be from 0.2:1 to 5:1. The dissolution rate of the palbociclib or pharmaceutically acceptable salt thereof in a solution of pH 6.0 may be greater than 60 % over a time period of 60 minutes, or greater that 50 % over a time period of 5 minutes. The amorphous solid dispersion may be stable for at least one week when stored at a temperature of 40 °C and humidity of about 75 %.
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