制川乌凝胶膏剂基质处方优化及体外释放研究
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篇名: 制川乌凝胶膏剂基质处方优化及体外释放研究
TITLE:
摘要: 目的: 优化制川乌凝胶膏剂基质处方工艺并考察其体外释放特性。方法:以初黏力、剥离强度、感官评价的综合评分为评价指标,采用星点设计-响应面法优化制川乌凝胶膏剂基质中聚丙烯酸钠(NP700)、甘羟铝、酒石酸、聚乙烯吡咯烷酮K90(PVP K90)的比例。采用改良的Franz扩散池法,以制川乌中6种酯型生物碱[苯甲酰新乌头原碱(BM)、苯甲酰乌头原碱(BA)、苯甲酰次乌头原碱(BH)、新乌头碱(MT)、次乌头碱(HT)、乌头碱(AT)]的累积释放量为评价指标,进行制川乌凝胶贴膏剂的体外释放试验。结果:优化的基质处方为NP700-甘羟铝-酒石酸-PVP K90(1.72 ∶ 0.10 ∶ 0.02 ∶ 1.65,m/m/m/m);验证试验中BM、BA、BH、MT、HT、AT 6种酯型生物碱的含量分别为52.77、28.52、28.78、8.81、8.75、8.21 μg/g,综合评分为118.67±1.33(RSD=4.62%,n=3)。BM的体外释放行为符合Higuchi方程,其余5种生物碱体外释放行为符合零级动力学方程,BM、BA、BH、MT、HT、AT 12 h累积释放量分别为12.04、2.95、3.55、2.64、2.48、1.97  μg/cm2。结论:优化基质处方所制备的制川乌凝胶膏剂外观、黏着力及体外释放效果良好。本研究可为制川乌的新剂型开发提供依据。
ABSTRACT: OBJECTIVE: To optimize formulation matrix of processed Aconitum carmichaelii hydrogel patch, and to investigate its in vitro drug release. METHODS: The ratio of NP700, dihydroxyaluminum aminoacetate, tartaric acid and PVP K90 in processed A. carmichaelii hydrogel patch matrix was optimized by central composite design-response surface method (CCD-RSM) with initial adhesion, peel strength and sensory evaluation as evaluation indexes. The modified Franz diffusion cell method was used for in vitro drug release test processed A. carmichaelii hydrogel patch using accumulative release amount of six ester type alkaloids benzene [benzoyl mesaconine (BM), benzoyl aconitum (BA), benzoylhy paconine (BH), mesaconitine (MT), hypaconitine (HT) and aconitine (AT)] as evaluation indexes. RESULTS: The optimal matrix formulation was NP700-dihydroxyaluminum aminoacetate-tartaric acid- PVP K90 (1.72 ∶ 0.10 ∶ 0.02 ∶ 1.65, m/m/m/m). In validation test, the contents of six ester type alkaloids were 52.77, 28.52, 28.78, 8.81, 8.75, 8.21 μg/g(RSD<5%,n=3), comprehensive score was 118.67±1.33 (RSD=4.62%, n=3). The release behavior of BM in vitro conformed to the Higuchi equation. The release behaviors of other 5 alkaloids were consistent with the Higuchi equation. 12 h accumulative release amounts of BM, BA, BH, MT, HT and AT were 12.04, 2.95, 3.55, 2.64, 2.48, 1.97 μg/cm2, respectively. CONCLUSIONS: The processed A. carmichaelii hydrogel patch prepared by matrix prescription is good in appearance, adhesion and in vitro release. The research can provide a basis for the development of new dosage form of processed A. carmichaelii.
期刊: 2018年第29卷第1期
作者: 吴璐,吴维刚,江亭,王希霖,杨华生
AUTHORS: WU Lu,WU Weigang,JIANG Ting,WANG Xilin,YANG Huasheng
关键字: 制川乌;凝胶膏剂;基质处方优化;星点设计;体外释放;酯型生物碱
KEYWORDS: Processed Aconitum carmichaelii; Hydrogel patch; Matrix formulation optimization; Central composite design; In vitro drug release; Ester type alkaloids
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