温敏型原位凝胶的热力学及流变学性质研究

目的:以磷酸川芎嗪为模型药物,探讨运用泊洛沙姆P407(P407)制备鼻用温敏型原位凝胶的可行性。方法:采用搅拌转子法测定不同处方磷酸川芎嗪原位凝胶的胶凝温度(胶凝温度:T);在不同温度下,以旋转式黏度计测定加入不同浓度辅料后P407溶液的黏度,以考察黏度随温度的变化规律。结果:P407溶液浓度越高,T越低;辅料的加入可以使P407溶液T升高,而处方药物和等渗调节剂(0.9%NaCl)使P407溶液T降低。当温度升高时,P407黏度增大,而辅料的加入会使P407黏度突变点的温度升高,黏度变小。结论:通过调节P407溶液的浓度或加入一定量辅料的方法,可以使TMPP原位凝胶在鼻腔温度(33℃左右)下胶凝,从而达到增大生物利用度和减少给药流失的要求。

Thermodynamic and rheological properties of thermosensitive gels

OBJECTIVE By using tetramethylpyrazine phosphate(TMPP)as a model drug,to stady the feasibility of preparation of nasal thermosensitive gels of TMPP.METHODS The mixing rotor was used to determine the gelatin temperature(gelatin temperature:T) of different thermosensitive gels of TMPP.By the rotary viscometer,it was evaluated the viscosities of P407 solution under different temperatures.RESULTS The higher the concentration of P407,the lower the T of gel.Accessories could make T of P407 solution higher,however,TMPP and isotonic regulator(0.9% NaCl)induced the T of P407 gel decreased.When the temperature rose,the viscosity of P407 increased.And with the additions of accessories,the T of P407 increased,but the viscosity decreased.CONCLUSION By adjusting the concentration of P407 or adding a certain amount of accessories,thermosensitive gels of TMPP could be gelled at about 33 ℃,which will increase the bioavailability and reduce drug wastage.