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目的:研制美沙拉嗪羟丙基β-环糊精(HP-β-CD)包合物温敏型液体栓,并对其体外性质进行考察。方法:以泊洛沙姆407和泊洛沙姆188为温敏材料,负载美沙拉嗪HP-β-CD包合物,制备美沙拉嗪HP-β-CD包合物温敏型液体栓;比较美沙拉嗪HP-β-CD包合物温敏型液体栓和美沙拉嗪液体栓的黏度、胶凝强度、生物黏附性、体外凝胶溶蚀及药物释放等。结果:与MSZ液体栓相比,美沙拉嗪HP-β-CD包合物的加入不影响液体栓的胶凝温度,能使液体栓的黏度、胶凝强度及生物粘附性显著增加。凝胶溶蚀不受包合物的影响,而药物释放率得到显著提高,且药物释放与凝胶溶蚀呈现良好的线性关系。结论:美沙拉嗪HP-β-CD包合物温敏型液体栓具有较理想的胶凝温度,以及良好的粘性、胶凝强度及生物粘附性,且体外释药速度较MSZ液体栓快。
OBJECTIVE: To develop a thermosensitive liquid suppository of mesalazine hydroxypropyl β-cyclodextrin (HP-β-CD) inclusion complex and its in vitro properties. METHODS: Poloxamer 407 and poloxamer 188 were used as thermosensitive materials and loaded mesalazine HP-β-CD inclusion complex to prepare mesalazine HP-β-CD inclusion temperature-sensitive liquid suppository. Mesalazine HP-β-CD inclusion temperature-sensitive liquid suppository and mesalamine liquid suppository viscosity, gel strength, bioadhesion, in vitro gel dissolution and drug release. Results: Compared with MSZ liquid suppository, the inclusion of mesalazine HP-β-CD did not affect the gelatinization temperature of liquid suppository, and significantly increased the viscosity, gel strength and bioadhesion of liquid suppository. Gel dissolution is not affected by the inclusion compound, but the drug release rate is significantly increased, and the drug release and gel dissolution showed a good linear relationship. Conclusion: Mesalazine HP-β-CD inclusion thermosensitive liquid suppository has an ideal gelation temperature, good viscidity, gelling strength and bioadhesion, and release rate in vitro is faster than that of MSZ liquid plug .