首页|加味寿胎贴脐片释药动力学与药效学研究

加味寿胎贴脐片释药动力学与药效学研究

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本研究旨在通过体外透皮试验考察加味寿胎贴脐片的透皮效果,以大鼠先兆性流产模型的流产率、脏器指数、胚胎个数和血清激素水平为评价指标,进一步确定其疗效,以期为临床治疗先兆性流产提供疗效显著且使用方便的新制剂。试验采用Franz扩散池法进行体外透皮试验,考察贴脐片中金丝桃苷、槲皮素、大黄素和川续断皂苷Ⅵ的透皮吸收情况,以评价经皮渗透效果。建立大鼠先兆性流产模型,动物随机分为4组,即空白组、空白贴脐片对照组(只含辅料,不含药)、阳性组及加味寿胎贴脐片组,以流产率、脏器指数、胚胎个数、雌二醇(E2)、孕酮(P)、人绒毛膜促性腺激素(β-HCG)、前列腺素(PGF-2α)水平考察加味寿胎贴脐片对模型动物先兆性流产的影响。结果表明,加味寿胎贴脐片中4种指标成分24h累计透过量为142。68μg/cm2、3。44 μg/cm2、3。78 μg/cm2、718。77 μg/cm2,累计透过速率分别为 0。049 7 μg/(cm2·h)、0。048 5 μg/(cm2·h)、0。054 4 μg/(cm2·h)、0。045 μg/(cm2·h)。4 种指标成分的透过率规律均符合一级动力学方程。金丝桃苷透过百分率为23。9%、槲皮素透过百分率为17。6%、大黄素透过百分率为27。7%、川续断皂苷Ⅵ透过百分率为27。1%。药效学试验结果显示,与空白贴脐片对照组相比,各给药组大鼠血清中E2、P、β-HCG的含量均有上调,PGF-2α的含量均有下调,贴脐片组在治疗先兆流产的作用上疗效显著,保胎效果更优。加味寿胎贴脐片具有体外经皮渗透的特性,对大鼠先兆性流产的治疗具有一定的改善作用,说明该制剂具有一定的临床开发价值。
Study on Release Kinetics and Pharmacodynamics of Jiawei Shoutai Tieqiu Tablets
Based on the development of a new formulation,this study investigated the transdermal effect of Jiawei Shoutai Umbilical patch through in vitro percutaneous experiments.The rat abortion rate,organ index,embryo count,and serum hormone levels were used as evalu-ation parameters to further determine its therapeutic effect.The aim was to provide a significantly effective and convenient new formulation for the clinical treatment of threatened miscarriage.The Franz diffusion cell method was used for in vitro percutaneous experiments.The per-cutaneous absorption of hyperin,quercetin,emodin,asperosaponinⅥ in the Umbilical patch was investigated to evaluate the transdermal penetration effect.A rat model of threatened miscarriage was established,and the animals were randomly divided into four groups:blank group,model group,positive control group,and Jiawei Shoutai Umbilical patch group.The effects of Jiawei Shoutai Sticking Umbilical Tablet on threatened miscarriage in the model animals were evaluated based on abortion rate,organ index,embryo count,and serum levels of E2,P,β-HCG,and PGF-2α.The cumulative amounts of percutaneous absorption of hyperin,quercetin,emodin,asperosaponinⅥ in 24 hours were 142.68 μg/cm2、3.44 μg/cm2、3.78 μg/cm2、718.77 μg/cm2,respectively,and the cumulative permeation rates were 0.049 7 μg/(cm2·h)、0.048 5 μg/(cm2·h)、0.054 4 μg/(cm2·h)、0.045 9 μg/(cm2·h),respectively.The cumulative transdermal penetration percentage Rn was 23.9%,17.6%,27.7%and 27.1%respectively.Pharmacodynamics experimental results showed that compared to the model group,the serum levels of E2,P,β-HCG were upregulated,and the PGF-2α levels were downregulated in the treatment groups.Jiawei Shouta Sticking Um-bilical Tablet group demonstrated significant efficacy in the treatment of threatened miscarriage,with better fetal preservation effects.Jiawei Shouta Sticking Umbilical Tablet exhibits transdermal characteristics in vitro.Jiawei Shouta Sticking Umbilical Tablet has a certain thera-peutic effect on threatened miscarriage in rats.This preliminary study suggests that the formulation has certain clinical development value.

threatened abortionJiawei Shoutai sticking umbilical tabletpercutaneous penetrationpharmacodynamics

张琪、刘婧、杨雪、李伟男、关枫、王艳宏

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黑龙江中医药大学,黑龙江 哈尔滨 150040

北药基础与应用研究教育部重点实验室,黑龙江 哈尔滨 150040

先兆流产 加味寿胎贴脐片 经皮渗透 药效学

国家自然科学基金项目

82074025

2024

特产研究
中国农业科学院特产研究所,中国农学会特产学会

特产研究

CSTPCD
影响因子:0.331
ISSN:1001-4721
年,卷(期):2024.46(5)