芍药苷醇质体凝胶剂体外释放及透皮特性研究

摘要

目的:优化芍药苷醇质体凝胶剂处方并对其体外释放、透皮特性进行研究.方法:以均匀度、性状等为质控指标,对芍药苷醇质体凝胶剂中羧甲基纤维素钠、丙三醇、醇质体的用量进行优化;分别采用透析袋法、Franz扩散池法研究芍药苷醇质体凝胶剂的体外释放及经皮渗透性;利用HPLC测定接收液中芍药苷的浓度.结果:当羧甲基纤维素钠、丙三醇及醇质体的用量分别为1.82％,27.3％及36.4 mL· 100 9-1时,所得到的醇质体凝胶剂质量最优;醇质体凝胶剂中芍药苷的累积释放率为(49.73±1.79)％;芍药苷的累积透过量是(361.67±69.98) μg· cm-2,14 h透过率为(19.40±3.75)％.结论:凝胶基质对芍药苷的释放有一定的阻碍,但醇质体凝胶载药体系能够明显加快芍药苷的经皮渗透速率、提高其药效,对其安全、高效新型载药体系的研究与开发具有重要意义.%Objective:This study aimed to optimize the prescription of paeoniflorin ethosomal gel and study its release and permeation behavior.Methods:Uniformity,character,stability and pH value were taken as indexes of the quality evaluate to optimize the dosage of carboxymethylcellulose sodium(CMC-Na),glycerol and ethosome in the preparation prescription;Bag filter method and improved Franz diffusing cells were used to estimate the in vitro release and dermal permeability of ethosomal gel.High performance liquid chromatography (HPLC) was applied to detect the concentration of paeoniflorin in transdermal receiving solutions and the curve of paeoniflorin cumulative permeation and release amount versus time was plotted.Results:The optimal formulation gained from experiments was composed of 1.82％ CMC-Na,27.3％ glycerol and 36.4 mL· 100 g-1 ethosome;The release of paeoniflorin from ethosomal gel fitted first grade equation,which was a multiple process of diffusion,dissolution and corrosion,and accumulative releasing ratio within 14 h was (49.73 ± 1.79)％;Percutaneous accumulative penetration amount and rate of paeoniflorin were respectively (361.67 ± 69.98) μg· cm-2 and (19.40 ± 3.75)％.Conclusion:Gel material hinder slightly the release of paeoniflorin but the permeation rate and efficacy of paeoniflorin were improved significantly carried by ethosomal gel system,which had an important significance for the further research and development of effective,safe and novel delivery drug system.