马钱子-白芍配伍贴膏剂的制备与经皮渗透性质研究
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摘要
目的:制备马钱子-白芍配伍贴膏剂,研究不同浓度薄荷醇对马钱子-白芍配伍贴膏剂中马钱子生物碱(马钱子碱和士的宁)体外经皮渗透性的影响。方法:对马钱子-白芍配伍贴膏剂进行物理性质评价;采用Franz扩散池法,以离体小鼠皮肤为实验对象,HPLC测定透皮接受液中马钱子总碱的含量,并计算累积渗透量和透皮速率等渗透动力学参数,以氮酮为阳性对照,未加促透剂的贴膏剂为阴性对照,考察1%,3%,5%薄荷醇对马钱子生物碱(马钱子碱和士的宁)的促渗效果。结果:马钱子-白芍配伍贴膏剂的粘附力、赋型性符合要求,综合感官评分良好。1%,3%,5%薄荷醇对马钱子碱和士的宁的稳态渗透速率分别为5. 441,18. 105,14. 765μg·cm~(-2)·h~(-1)和15. 430,45. 243,30. 927μg·cm~(-2)·h~(-1)。3%,5%薄荷醇促透效果优于阳性对照3%氮酮,1%薄荷醇的促透效果与3%氮酮相当。不同浓度薄荷醇促透强弱顺序为3%薄荷醇> 5%薄荷醇> 1%薄荷醇。结论:马钱子-白芍配伍贴膏剂物理性质符合要求,薄荷醇能够促进马钱子-白芍配伍中马钱子生物碱(马钱子碱和士的宁)的体外透皮吸收。
Objective: To prepare hydrogel patch of Strychnos-Paeony compatibility,to study the effects of different concentrations of menthol in vitro percutaneous penetration of Strychnos alkaloids( strychnine and brucine) in Strychnos-Paeoniae Radix Alba compatibility Hydrogel patch. Method: Evaluation of physical properties of Strychnos-Paeony of compatibility Hydrogel patch. The excised abdominal skin of mice was used as the permeation model. Utilizing the modified Franz diffusion cell,the contents of brucine and strychnine in the receiving solution were determined by HPLC,and calculated the percutaneous rates and permeability coefficients.Azone was positive control,and no patch enhancers were negative control. The effects of 1%,3%,5% menthol on total alkaloids of Strychni Semen( brucine and strychnine) were investigated. Result: The adhesive force and shapeability of the Strychnos-Paeony of compatibility Hydrogel patch meet the requirements,and the comprehensive sensory score is good. The steady-state permeation rates of strychnine and brucine by 1%,3%,5% menthol were 5. 441,18. 105,14. 765 μg·cm~(-2)·h~(-1) and 15. 430,45. 243,30. 927 μg·cm~(-2)·h~(-1). 3 %,5 % menthol had better penetration than the positive control 3 % Azone and the effect of 1 % menthol was equivalent to 3 % Azone. The order of penetration enhancement of menthol with different concentrations was 3% Menthol > 5% Menthol > 1%Menthol. Conclusion: The physical properties of Strychnos-Paeony of compatibility Hydrogel patch meet the requirements,Menthol can promote the transdermal absorption of Strychnos alkaloids( strychnine and brucine) in Strychnos-Paeony of compatibility Hydrogel patch.
Objective: To prepare hydrogel patch of Strychnos-Paeony compatibility,to study the effects of different concentrations of menthol in vitro percutaneous penetration of Strychnos alkaloids( strychnine and brucine) in Strychnos-Paeoniae Radix Alba compatibility Hydrogel patch. Method: Evaluation of physical properties of Strychnos-Paeony of compatibility Hydrogel patch. The excised abdominal skin of mice was used as the permeation model. Utilizing the modified Franz diffusion cell,the contents of brucine and strychnine in the receiving solution were determined by HPLC,and calculated the percutaneous rates and permeability coefficients.Azone was positive control,and no patch enhancers were negative control. The effects of 1%,3%,5% menthol on total alkaloids of Strychni Semen( brucine and strychnine) were investigated. Result: The adhesive force and shapeability of the Strychnos-Paeony of compatibility Hydrogel patch meet the requirements,and the comprehensive sensory score is good. The steady-state permeation rates of strychnine and brucine by 1%,3%,5% menthol were 5. 441,18. 105,14. 765 μg·cm~(-2)·h~(-1) and 15. 430,45. 243,30. 927 μg·cm~(-2)·h~(-1). 3 %,5 % menthol had better penetration than the positive control 3 % Azone and the effect of 1 % menthol was equivalent to 3 % Azone. The order of penetration enhancement of menthol with different concentrations was 3% Menthol > 5% Menthol > 1%Menthol. Conclusion: The physical properties of Strychnos-Paeony of compatibility Hydrogel patch meet the requirements,Menthol can promote the transdermal absorption of Strychnos alkaloids( strychnine and brucine) in Strychnos-Paeony of compatibility Hydrogel patch.
引文
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[14]Williams AC,Barry BW. Penetration enhancers[J]. Adv Drug Deliv,2012,64(Supplement):128-137.
[15]冯鑫.挥发油促透作用适用性研究进展[J].中成药,2013,35(1):157-161+164.
[16]王晖,黄钊,梁庆,等.促透剂薄荷醇对大鼠皮肤角质层超微结构的影响[J].广东药学院学报,2012,28(3):303-306.
[17]Vashisth I,Ahad A,Aqil M,etal. Investigating the potential of essential oils as penetration enhancer for transdermal losartan delivery:effectiveness and mechanism of action[J]. Asian J Pharm Sci,2014,9(5):260-267.
[2]赵引利,何燕宁,杨宇杰,等.马钱子及其制剂药动学研究进展[J].中草药,2015,46(11):1 710-1 714.
[3]陈丽华,陈家乐,朱卫丰,等.马钱子总碱-白芍总苷配伍凝胶剂的制备及其经皮吸收性能的考察[J].中国药学杂志,2016,51(22):1 953-1 957.
[4]刘烨.马钱子配伍白芍减毒增效作用的研究[D].济南:山东中医药大学,2011.
[5]吴璐,罗永明,梁秉文,等.制川乌-白芍配伍对芍药苷经皮吸收的影响[J].中国实验方剂学杂志,2015,21(13):1-4.
[6]张贵华,马云淑,黄金娥,等. 3种挥发油对马钱子总碱透皮贴片体外经皮渗透的影响[J].中草药,2012,43(11):2 158-2 163.
[7]Olivella M S,Lhez L,Pappano N B,etal. Effects of dimethylformamide and L-menthol permeation enhancers on transdermal delivery of quercetin[J]. Pharm Dev Technol,2007,12(5):481-484.
[8]兰颐,王景雁,陶野,等.薄荷油与薄荷醇促进中药成分经皮吸收的对比研究[J].中国中药杂志,2016,41(8):1 516-1 522.
[9]吴珍珍,胡杰,胡克菲,等.马钱子总碱囊泡凝胶的体外透皮扩散和抗炎作用[J].中国实验方剂学杂志,2011,17(13):1-4.
[10]温思菁,陈家乐,陈丽华,等.马钱子总碱脂质体凝胶的制备及其体外透皮作用[J].中国医院药学杂志,2017,37(1):36-39.
[11]郑俊民.经皮给药新剂型[M].北京:人民卫生出版社,2006:35-42.
[12]Gary PM,Simon CW,Sun Y,etal. Mathematical modellingof percutaneous absorption[J]. Curr Opin Colloid InterfaceS,2012,17(3):166-172.
[13]杨春光,张令君,李湘玲,等.不同透皮促进剂对马钱子碱体外透皮吸收的影响[J].中南药学,2014,12(9):882-884.
[14]Williams AC,Barry BW. Penetration enhancers[J]. Adv Drug Deliv,2012,64(Supplement):128-137.
[15]冯鑫.挥发油促透作用适用性研究进展[J].中成药,2013,35(1):157-161+164.
[16]王晖,黄钊,梁庆,等.促透剂薄荷醇对大鼠皮肤角质层超微结构的影响[J].广东药学院学报,2012,28(3):303-306.
[17]Vashisth I,Ahad A,Aqil M,etal. Investigating the potential of essential oils as penetration enhancer for transdermal losartan delivery:effectiveness and mechanism of action[J]. Asian J Pharm Sci,2014,9(5):260-267.