Preparation and quality evaluation of mesalazine thermosensitive gel for rectal use
Objective To prepare a mesalazine thermosensitive gel(MZ-Gel)with sustained release for rectal administration.Methods The dosage of Porloxam 407 and Porloxam 188 was optimised with star point design-response surface methodology using gelling temperature as the evaluation index.The in vitro drug release behavior was further determined by Franz diffusion cell method to obtain the optimal formula and evaluate its quality.Results The optimal formula of MZ-Gel was P407 22.56％,and P188 3.34％,with gelling temperature at(32.8±0.3)℃.The in vitro drug release of MZ-Gel was in accordance with the first-order kinetic characteristics,with sustained release.The average value of the gelation time was 38.3 s,the average value of pH was 4.07,and the coefficient of expansion was 4.81％,with a water-holding capacity of 99.78％.The infrared ray(IR)characterization showed that the addition of mesalazine did not destroy its thermosensitivegel structure.Conclusion This preparation method is simple and stable,and has good in vitro drug release characteristics.
mesalazinethermosensitive gelstar point design-response surface methodologyFranz diffusion cell methodin vitro drug release
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