少腹逐瘀凝胶贴膏剂基质处方优化及体外透皮特性研究
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摘要
目的通过Plackett-Burman联用Box-Behnken响应面法优化少腹逐瘀凝胶贴膏剂基质处方并对其体外透皮特性进行研究。方法在预实验基础上,采用Plackett-Burman设计联用Box-Behnken响应面法,以外观性状、初黏力、持黏力和剥离强度为综合指标优化最优处方,采用改良Franz扩散池法,以阿魏酸、芍药苷、异鼠李素-3-O-新橙皮苷、香蒲新苷为评价指标,考察不同用量氮酮促渗剂对凝胶贴膏体外透皮渗透量的影响。结果凝胶贴膏最优处方为Viscomate~(TM) NP-700-酒石酸-高岭土(2.42∶0.16∶0.96),3%氮酮对指标成分促渗效果良好,阿魏酸、芍药苷、异鼠李素-3-O-新橙皮苷、香蒲新苷体外透皮速率依次为6.889 4、1.917 4、0.842 0、0.893 7μg/(cm~2·h)。结论制备的少腹逐瘀凝胶贴膏膏体均匀,敷贴无残留,具有较好的释药性和透皮性,透皮行为符合零级动力学方程。
Objective To optimize the matrix formulation for Shaofu Zhuyu Cataplasm(SZC) by Plackett-Burman design combined with Box-Behnken response surface method and study its transdermal permeation properties in vitro. Methods In this paper, the appearance description, initial bonding strength, endurance bonding strength, and peel strength were taken as indexes. Based on the result of a single factor experiment, the formula for the SZC was optimized by Plackett-Burman combined with Box-Behnken method. Franz diffusing cells method was chosen to investigate the tansdermal infiltration capacity of SZC with different dosage penetration enhancers of azone in vitro, taking ferulic acid, paeoniflorin, isorhamnetin-3-O-neohesperidin, and typhaneoside as index components. Results NP-700, tartaric acid and kaolin had significant effects on the properties of SZC. The optimal ratio of the prescription was as follows: NP-700-tartaric acid-kaolin(2.42∶0.16∶0.96). The promoting effect of 3% concentration for index component was better, and the transdermal rates of ferulic acid, paeoniflorin, isorhamnetin-3-O-neohesperidin, and typhaneoside were 6.889 4, 1.917 4, 0.852 0, and 0.893 7 μg/(cm~2·h), respectively. Conclusion The SZC was uniform, without residual behavior in application. And it had a good release and transdermal properties, and transdermal actions were consistent with zero-order kinetics.
Objective To optimize the matrix formulation for Shaofu Zhuyu Cataplasm(SZC) by Plackett-Burman design combined with Box-Behnken response surface method and study its transdermal permeation properties in vitro. Methods In this paper, the appearance description, initial bonding strength, endurance bonding strength, and peel strength were taken as indexes. Based on the result of a single factor experiment, the formula for the SZC was optimized by Plackett-Burman combined with Box-Behnken method. Franz diffusing cells method was chosen to investigate the tansdermal infiltration capacity of SZC with different dosage penetration enhancers of azone in vitro, taking ferulic acid, paeoniflorin, isorhamnetin-3-O-neohesperidin, and typhaneoside as index components. Results NP-700, tartaric acid and kaolin had significant effects on the properties of SZC. The optimal ratio of the prescription was as follows: NP-700-tartaric acid-kaolin(2.42∶0.16∶0.96). The promoting effect of 3% concentration for index component was better, and the transdermal rates of ferulic acid, paeoniflorin, isorhamnetin-3-O-neohesperidin, and typhaneoside were 6.889 4, 1.917 4, 0.852 0, and 0.893 7 μg/(cm~2·h), respectively. Conclusion The SZC was uniform, without residual behavior in application. And it had a good release and transdermal properties, and transdermal actions were consistent with zero-order kinetics.
引文
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[2]周鹿安,陆政日,刘姝娆,等.少腹逐瘀汤治疗寒凝血瘀型原发性痛经的Meta分析[J].药物评价研究,2016,39(5):858-864.
[3]韦悦,贺吉香.凝胶膏剂的研究进展[J].中医药导报,2017,23(11):57-59.
[4]郑立红,李淑莉.中药凝胶膏剂研究进展[J].中国中医药信息杂志,2017,24(4):134-136.
[5]刘帝灵,朱莉,林吉,等.仁术微乳凝胶膏剂的制备[J].中成药,2016,38(12):2570-2574.
[6]黄晓晨,宿树兰,钱大玮,等.不同促渗剂对少腹逐瘀方外用贴剂中效应成分群体外透皮吸收的影响[J].中草药,2014,45(21):3074-3080.
[7]宋立华,杜茂波,刘淑芝.Plackett-Burman联用Box-Behnken响应面法优化凝胶膏剂基质研究[J].中成药,2015,37(12):2623-2627.
[8]李智,于金英,蒋瑶,等.Box-Behnken优化痹痛宁凝胶膏剂基质处方研究[J].天然产物研究与开发,2015,27(2):226-231.
[9]权亮,赵永峰,陈志敏,等.基于信息熵赋值法的正交联用Box-Behnken设计-响应面法优化黄丝郁金醋炙工艺研究[J].中草药,2018,49(8):1823-1828.
[10]严倩茹.痹痛宁凝胶膏剂的药学研究[D].成都:成都中医药大学,2013.
[11]朱力阳.丁桂凝胶膏剂的制备工艺及主要药效学研究[D].成都:成都中医药大学,2015.
[12]杨秀梅.祛斑凝胶膏剂的药学研究[D].成都:成都中医药大学,2015.
[13]吴俊洪.痛经舒凝胶膏剂的研制[D].广州:广州中医药大学,2014.
[14]胡晓.复方积雪草苷凝胶膏剂的研究[D].武汉:湖北中医药大学,2013.
[15]刘秀洁.双氯芬酸钠巴布剂的研制及体内外透皮动力学研究[D].上海:华东理工大学,2012.
[16]黄秋洁,叶勇,魏涌标,等.战骨提取物中柚皮素透皮吸收促进剂的筛选[J].中草药,2017,48(16):3366-3369.
[17]银杉杉,汪艳秋,周国良,等.不同促渗剂对三威跌打风湿贴中柚皮苷体外透皮吸收的影响[J].中国实验方剂学杂志,2016,22(7):15-18.
[18]温亚,韩彬,戴王强,等.薄荷醇对芍药苷透皮吸收作用的影响[J].湖南中医杂志,2014,30(5):128-130.
[19]史亚军,吴品江,魏萍.Plackett-Burman设计与星点设计-效应面法优化山楂总黄酮磷脂复合物制备工艺[J].中药材,2010,33(3):437-441.
[20]涂颖秋,朱孟夏,刘会,等.优化药物制剂工艺的多种数据处理方法的研究进展[J].中国药学杂志,2013,48(16):1333-1337.