Qilu Pharmaceutical Co., Ltd.

Chinese Academy of Sciences

Qingmin Yang

Jingyi Wang

Long Zhang

Jianrong Zhu

Zongru Guo

Yong Gan

Minghui Zhang

Chuanwen Fan

Chunliu Zhu

Shousheng Yan

Xiaoqing Zheng

Li Gan

Xinxin Zhang

Zhongru Guo

Ying Li

Shaobo Yang

A paliperidone double-layered osmotic pump controlled release tablet and the preparation method thereof are disclosed. The double-layered osmotic pump controlled release tablet comprises a rigid membrane, a push layer, a drug layer, an isolation layer and an aesthetic coating, wherein the rigid membrane contains a semi-permeable polymer, a porogen and/or a plasticizer and has one or more drug release orifices on one end, the push layer comprises an expanding material, an osmotic agent, a binder, a colorant and a lubricant, the drug layer contains a pharmaceutically active ingredient, a hydrophilic polymer, an osmotic agent, a colorant, a lubricant and an antistatic agent, the isolation layer is located between the inner surface of the rigid membrane and the push layer, and contains a hydrophilic polymer. The paliperidone double-layered osmotic pump controlled release tablet shows an increasing drug release rate at early stage and keeps a constant drug release rate at later stage.

Paliperidone double-layered osmotic pump controlled release tablet and preparation method thereof

The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors. 

4-(substituted anilino)-quinazoline derivatives useful as tyrosine kinase inhibitors

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Jinan, China

Qingmin Yang