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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。
OBJECTIVE: To investigate the feasibility of preparing thermosensitive in situ gels for nasal use of poloxamer P407 (P407) using tetramethylpyrazine phosphate as a model drug. Methods: The gelling temperature (gelation temperature: T) of in situ gels of different formulations of ligustrazine phosphate was determined by agitation rotor method. The viscosity of P407 solution after adding different concentrations of excipients was determined by rotary viscometer under different temperatures Investigate the variation of viscosity with temperature. Results: The higher the concentration of P407 was, the lower the T was. The addition of excipients increased the concentration of T in P407 solution, while the prescription drug and isotonic regulator (0.9% NaCl) decreased the concentration of P407 in solution. When the temperature increases, the viscosity of P407 increases, while the addition of excipients will increase the temperature of the point of P407 viscosity mutation, the viscosity becomes smaller. Conclusion: By adjusting the concentration of P407 solution or adding a certain amount of adjuvant, the in situ gel of TMPP can be gelatinized at the nasal temperature (about 33 ℃), so as to increase the bioavailability and reduce the loss of dosage.