星点的设计―效应面法优化苍艾油包合物―鼻用温敏原位凝胶制备工艺.docVIP

星点的设计―效应面法优化苍艾油包合物―鼻用温敏原位凝胶制备工艺 　　摘要：目的 采用星点设计-效应面法优化苍艾油包合物-鼻用温敏原位凝胶的制备工艺。方法 以泊洛沙姆407、泊洛沙姆188用量为考察因素，胶凝温度为评价指标，采用二次多项式模型描述评价指标与2个因素之间的数学关系，以此确定优化处方，并加以验证。结果 根据二次多项式模型，发现2个考察因素与评价指标之间存在可信的定量关系，其中泊洛沙姆407、泊洛沙姆188的最佳用量分别为19.37%、2.73%。结论 采用星点设计-效应面法得到了基于二次多项式的苍艾油包合物-鼻用温敏原位凝胶处方最优模型，处方工艺稳定可行，实现了该原位凝胶的处方优化。 　　关键词：苍艾挥发油；包合物；鼻用温敏原位凝胶；星点设计-效应面法 　　DOI：10.3969/j.issn.1005-5304.2016.11.021 　　中图分类号：R283.5 文献标识码：A 文章编号：1005-5304（2016）11-0086-04 　　Abstract： Objective To optimize the preparation technology of Cangai volatile oil dextrin inclusion compound/ in situ nasal thermosensitive gel by the central composite design-response surface method. Methods In the design， the investigation factors were the amounts of poloxamer 407 and poloxamer 188， and the evaluation index was the gel temperature. Quadratic models were used to evaluate the mathematic relation between the evaluation index and two investigation indexes to identify the optimum prescription， and then the optimum prescription was verified. Results According to the quadratic models， it was found that there was reliable quantitative relation between the evaluation index and two investigation indexes， among which the optimum dosage was 19.37% for poloxamer 407 and 2.73% for poloxamer 188. Conclusion The optimum model of Cangai volatile oil dextrin inclusion compound/ nasal thermosensitive gel can be obtained from central composite design-response surface method based on quadratic models. This method is reliable and feasible， which can realize the prescription optimization of the in situ gel. 　　Key words： Cangai volatile oil； dextrin inclusion compound； in situ nasal thermosensitive gel； central composite design-response surface method 　　苍艾挥发油系以熊磊教授预防上呼吸道感染的临床效验方为基础，选用含挥发油成分较多、气味清香、抗菌谱广、抗菌能力强并有一定增强免疫作用的中药组方[1]。临床采用鼻腔吸入给药方式，主要用于肺气虚证的治疗。根据挥发油的性质及给药方式的特点，本试验先将其制备成羟丙基-β-环糊精包合物，以降低其挥发性，减小刺激性、提高溶解度及稳定性。此外，综合归纳影响鼻腔吸收的因素，为保证其在鼻腔吸收完全，将包合物进一步制备成鼻温敏凝胶（在鼻腔内成为半固体状态），即能以溶液状态给药后，在鼻腔发生相转变而形成凝胶[2]，增强了与鼻黏膜的亲和力，减少药物流失，延长药物的滞留时间，增加药物吸收，提高了生