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花椒挥发油微乳凝胶的制备及其对不同油水分配系数药物的体外释放研究 被引量:6

Microemulsion gel containing essential oil from Zanthoxylum bungeanum Maxim.:preparation,stability and in vitro release of model drugs with different oil-water partition coefficients
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摘要 目的制备花椒挥发油微乳凝胶,探究微乳凝胶中花椒挥发油的稳定性及不同油水分配系数(log P)药物的体外释放行为。方法首先以凝胶基质的外观、成型性、黏稠度为评价指标,筛选凝胶基质种类及用量,以花椒挥发油为油相的微乳制备为花椒挥发油微乳凝胶,并通过GC指纹图谱相似度评价花椒挥发油在微乳凝胶中的稳定性。然后,采用改良Franz扩散池法考察花椒挥发油微乳凝胶中不同log P值药物的体外释放行为。结果优选得到的凝胶基质及用量为1%的卡波姆940,基于此制备的微乳凝胶中花椒挥发油稳定性较好,模型药蛇床子素、川芎嗪、阿魏酸、葛根素及京尼平苷的24 h累积释放率分别为(1.28±0.16)%、(85.90±4.57)%、(43.82±5.34)%、(46.87±5.26)%、(88.60±5.46)%。结论微乳凝胶能增强花椒挥发油在制剂中的稳定性,且对亲水性及小分子亲脂性成分释放能力强,可作为花椒挥发油在今后临床应用的优良剂型,为富含挥发油的中药外用制剂开发和临床应用提供指导。 Objective To prepare microemulsion gel containing essential oil from Zanthoxylum bungeanum Maxim.(Z.bungeanum oil)and explore its stability and the in vitro release behaviors with different oilwater partition coefficients(log P).Methods According to the type and amount of gel matrix selected by the appearance,moldability and viscosity,a microemulsion gel entrapping Z.bungeanum oil was prepared.The stability of Z.bungeanum oil in the preparation was evaluated by the similarity of gas chromatography fingerprints obtained at intervals.A series of components with different log P values were selected as model drugs.The in vitro release behaviors of the model drugs in microemulsion gel were further examined with the improved Franz diffusion cell method.Results The optimal gel matrix and dosage was 1%carbomer 940.According to the stability test and in vitro release experiments,Z.bungeanum oil was stable in the optimal microemulsion gel.The Q24%of osthole,tetramethylpyrazine,ferulic acid,puerarin and geniposide was(1.28±0.16)%,(85.90±4.57)%,(43.82±5.34)%,(46.87±5.26)%and(88.60±5.46)%,respectively.Conclusion Microemulsion gel can enhance the stability of Z.bungeanum oil in the preparation,and has strong release to hydrophilic and small-molecular lipophilic components.Microemulsion gel can be used as an excellent dosage form for future clinical application of Z.bungeanum oil,providing guidance for the development and clinical application of essential oil-enrichment traditional Chinese medicine external preparations.
作者 刘欣妍 徐铃燕 刘鑫 王永洁 赵颖 兰海 吴清 LIU Xin-yan;XU Ling-yan;LIU Xin;WANG Yong-jie;ZHAO Ying;LAN Hai;WU Qing(School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 102488)
出处 《中南药学》 CAS 2020年第2期189-193,共5页 Central South Pharmacy
基金 国家自然科学基金资助项目(No.81473365)。
关键词 花椒挥发油 微乳凝胶 稳定性 油水分配系数 体外释放 essential oil from Zanthoxylum bungeanum Maxim. microemulsion gel stability oil-water partition coefficient in vitro release
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