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吡罗昔康-苯甲酸共晶的制备与体外释放研究
吡罗昔康-苯甲酸共晶的制备与体外释放研究
张跃勇,田佳鑫,吕 琳,兰亚茹,张 雷,郭永学

沈阳药科大学制药工程学院,沈阳 110016
Preparation and in vitro release of piroxicam-benzoic acid cocrystal
(School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China)

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起始页:91

摘要:[摘要] 目的:本实验采用共晶技术制备难溶性药物吡罗昔康的共晶物,以期提高难溶性药物的溶解度和溶出度。方法:采用混合溶剂结晶法制备了吡罗昔康共晶,采用差示扫描量热分析(DSC)、高效液相色谱(HPLC)及X射线粉末衍射(XRPD)对制备得到的产品进行表征,并对共晶物的粒径、稳定性和体外释放等性质进行了考察。结果:吡罗昔康与苯甲酸之间形成了共晶物。形成的共晶物粒径分布均匀、晶体性质稳定。同时提高了吡罗昔康的溶解度并改善其体外释放性质。结论:共晶技术在提高难溶性药物溶解度和溶出度方面具有广阔的应用前景。

关键词:[关键词] 吡罗昔康;药物共晶;混合溶剂结晶;溶解度;体外释放

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Abstract:[Abstract] Objective:This experiment adopted the eutectic technology for preparation of insoluble drug piroxicam eutectic materials, in order to improve the solubility of insoluble drugs and dissolution. Methods:Piroxicam cocrystal with benzoic acid was prepared by cooling crystallization method to improve the solubility and bioavailability of piroxicam drug. The cocrystal was characterized by high performance liquid chromatography, differential scanning calorimetric(DSC)and X-ray powder diffraction(XRPD). Meanwhile, the solubilities and dissolution properties of piroxicam and cocrystal were determined by digital tachometer temperature water bath oscillator and intelligent dissolution apparatus. Results: The cocrystal formation of piroxicam with benzoic acid has been prepared successfully, and displayed higher solubility and better release in vitro than piroxicam. Conclusion:The cocrystal technology has broad application prospects in improving solubility and dissolution of poorly soluble drugs.

Key words:[Key words] proxicam;drug cocrystal;mixed solvent crystallization;solubility;release in vitro

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