不同皮肤组织对安替比林贴片经皮渗透的差异

目的：评价皮肤角质层和活性皮肤层对药物经皮渗透的差异。方法：选择安替比林（AT）为模型药物,采用Franz扩散池法,考察药物经完整皮肤和剥离角质层皮肤的体外透皮能力Kp,并比较吸收促进剂肉豆蔻酸异丙酯（IPM）共存时的促透能力大小。结果：AT经剥离角质层皮肤的Kp是经完整皮肤的3.24倍,加入IPM后AT的Kp分别提高到原来的3.68倍（经完整皮肤）和5.17倍（经剥离角质层皮肤）。结论：本实验为皮肤病态条件,如皮肤受伤或溃疡等时的药物经皮吸收规律研究提供一种新的方法。     

角质层与活性皮肤层对硝酸异山梨酯透皮吸收的影响

目的:评价皮肤角质层和真皮层对药物经皮吸收的影响。方法:以硝酸异山梨酯(ISDN)为模型药物,采用Franz吸收池法,考察药物单独或与吸收促进剂肉豆蔻酸异丙酯(IPM)合用时,经完整皮肤和角质层剥离皮肤的透皮能力。结果:IS-DN经剥离角质层皮肤的表观透皮系数的Kp是经完整皮肤的1.68倍,IPM能分布在活性皮肤层,并可明显增加ISDN在角质层或真皮层的分布量及经皮累积透皮吸收百分率。结论:本实验为研究皮肤病态条件下(如皮肤受伤或溃疡等),药物透皮吸收规律,提供了一种新的方法。     

氢醌经不同皮肤层的吸收差异

目的 :评价皮肤角质层和真皮层对药物经皮吸收的差异。方法 :选择氢醌 (HQ)为模型药物 ,采用Franz吸收池法 ,考察药物经完整皮肤和剥离角质层皮肤的体外透皮能力Kp ,并比较吸收促进剂肉豆蔻酸异丙酯(IPM)共存时的促透能力大小。结果 :HQ经剥离角质层皮肤的Kp 是经完整皮肤的3 29倍 ,加入IPM后HQ的Kp 分别提高到原来的4 95倍 (经完整皮肤 )和7 49倍 (经剥离角质层皮肤 )。结论 :本实验为皮肤病态条件 ,如皮肤受伤或溃疡等时的药物经皮吸收规律研究提供了一种新的方法。     

氟尿嘧啶经不同皮肤层吸收差异的评价

目的　评价皮肤角质层和真皮层对药物经皮吸收的差异。方法　选择氟尿嘧啶 (5 - FU)为模型药物 ,采用Franz扩散池法 ,考察药物经完整皮肤和剥离角质层皮肤的体外透皮能力 (Kp) ,并比较吸收促进剂肉豆蔻酸异丙酯 (IPM)共存时的促透能力大小。结果　 5 - FU经剥离角质层皮肤的 Kp是经完整皮肤的 2 .2倍 ,加入IPM后 5 - FU的 Kp分别提高到原来的 1 .6倍 (经完整皮肤 )和 2 .3倍 (经剥离角质层皮肤 )。结论　本实验为皮肤病态条件 ,如皮肤受伤或溃疡等时的药物经皮吸收规律研究提供一种新的方法。     

皮肤条件影响茶碱经皮吸收的观察

目的　考察不同皮肤组织对药物经皮吸收的影响。方法　选择茶碱 (TP)为模型药物 ,以体外Franz吸收池法 ,评价TP经完整皮肤和剥离角质层皮肤的体外透皮能力Kp ,以及吸收促进剂肉豆蔻酸异丙酯 (IPM)对Kp的影响。结果　TP经剥离角质层皮肤的Kp是经完整皮肤的 2 1倍 ,加入IPM后TP的Kp分别提高到原来的 8 9倍 (经完整皮肤 )和 15 1倍 (经剥离角质层皮肤 )。结论　IPM非常显著地增加TP经不同皮肤层的经皮吸收。本文也为皮肤病态条件 ,如皮肤受损或溃疡等时的药物经皮吸收规律研究提供一种新的方法     

月桂氮酮对皮肤促透作用的研究近况

月桂氮　酮（Ａｚｏｎｅ）系一种新型皮肤渗透促进剂,具有促进渗透作用强,有效浓度低,性质稳定,毒性小,无臭等特点,在透皮吸收制剂中广泛应用,对提高制剂质量和局部治疗效果有较重要意义。现将其皮肤促透作用的研究近况综述如下：１酮基布洛芬凝胶 以离体小白鼠皮肤为渗透模型进行的Ａｚｏｎｅ对酮基布洛芬凝胶透皮吸收影响的实验结果表明［１］,３～５％的 Ａｚｏｎｅ对酮基布洛芬凝胶有非常明显的促渗透作用,在实验后６～８ｈ,即可使酮基布洛芬凝胶透皮释放率达到５０％以上,且３％、４％和５％三浓度间无明显的统计学差异（Ｐ…     

促进剂预处理皮肤对环吡酮胺经皮渗透的影响

目的：考察透皮促进剂对环吡酮胺经皮渗透的影响,方法：用透皮促进剂预处理离体小鼠皮肤,以改良的Franz扩散装置进行体外渗透实验,结果：环吡酮胺经皮渗透符合零级动力学过程,几种透皮促进剂的促渗作用大小依次为月桂氮zhuo酮－丙二醇（1：1）＞二甲基亚砜＞月桂氮zhuo＞水溶性月桂氮zhuo酮＞N－甲基吡咯烷酮＞薄荷油,结论：体外实验证明,透皮促进剂可增加环吡酮胺的透皮吸收。     

盐酸丁螺环酮透皮促渗剂选择及其透皮机制的研究

目的研究透皮促渗剂对盐酸丁螺环酮体外经皮渗透的影响以及盐酸丁螺环酮的透皮机制。方法采用改良Franz扩散池,比较不同促渗剂种类、浓度、配比对盐酸丁螺环酮的促渗效果,同时通过改变扩散池的介质pH及皮肤的状态,研究药物的透皮机制。结果采用3%氮酮为透皮促渗剂时药物透过量最大。盐酸丁螺环酮随着分子型浓度的升高透过量也随之增加,皮肤去除角质层后,药物的透过量显著大于完整皮肤,而完整皮肤的贮库效应大于去角质皮肤。结论药物透皮以3%氮酮为透皮促进剂促渗效果最佳。盐酸丁螺环酮主要是以分子型透过皮肤,药物的透皮屏障与贮库效应发生的主要部位是皮肤的角质层。     

曲安奈德经皮渗透特性研究

目的评价曲安奈德经皮渗透的特性。方法采用Franz扩散池法,考察药物经完整皮肤和去角质层皮肤的体外透皮能力,并采用了胶带剥离、皮肤萃取法分别获取了皮肤角质层、去角质层皮肤样本,用HPLC法测定了样本中的药物含量,考察曲安奈德在皮肤不同层的分布情况。结果曲安奈德的24 h透过量去角质层皮肤约为完整皮肤的1.6倍;8 h透皮实验,高、中、低3个浓度角质层中药物含量基本相同,真皮层则存在浓度依赖现象。结论角质层是曲安奈德的透皮吸收重要屏障,但角质层对药物的储留有饱和现象,临床上应用时需特别关注。     

派瑞松乳膏中3种药物透皮特性的研究

目的:评价派瑞松乳膏中曲安奈德(TACA)、苯甲酸(BEN)、硝酸益康唑(ECN)3种药物的透皮特性.方法:采用Franz扩散池法,考察药物经完整皮肤和去角质层皮肤的体外透皮能力,并采用了胶带剥离、皮肤萃取法分别获取了皮肤角质层、去角质层皮肤样本,用HPLC法测定了样本中的药物含量.结果:经过24 h透皮吸收,TACA和BEN的去角质层皮肤渗透量分别为完整皮肤的1.5和1.3倍,ECN的渗透量基本为零.8h透皮实验,TACA高、中、低3个浓度角质层中药物含量基本相同,真皮层则存在浓度依赖现象;ECN在皮肤各层和接受室均检测不到;BEN在角质层和真皮层中的分布与TACA相似,但透过量比TACA大.结论:角质层是皮肤渗透的重要屏障,派瑞松乳膏应用于皮肤溃疡、受损或者婴幼儿皮肤仍需谨慎.     

不同渗透促进剂对复方盐酸多塞平乳膏体外经皮的促渗作用研究

目的研究不同浓度油酸和氮酮及其复合物对复方盐酸多塞平乳膏透皮吸收的影响,提高乳膏中两种主要有效成分盐酸多塞平和醋酸曲安奈德的渗透效果.方法选用1%氮酮(aonze,AZ)、2%AZ、1%油酸(oleic acid,OA)、2%OA、1%OA-AZ 5种渗透吸收促进剂,采用离体小鼠皮为皮肤模型,在Franz扩散池上进行促渗实验.结果 5种渗透吸收促进剂对复方盐酸多塞平乳膏中盐酸多塞平促渗能力为2%AZ＞1%OA-AZ＞2%OA＞1%AZ＞1%OA;对醋酸曲安奈德促渗能力为2%AZ＞1%OA-AZ＞1%AZ＞2%OA＞1%OA.结论在所选的5种渗透促进剂中,选用2%AZ渗透促进剂对复方盐酸多塞平乳膏体外经皮促渗作用最显著,油酸、氮酮联合应用有协同作用,比单用氮酮或油酸促渗能力强.     

Age-related changes in skin permeability of hydrophilic and lipophilic compounds in rats

The effect of age on intact and stripped skin permeability of lipophilic (ketoprofen and isosorbide dinitrate) and hydrophilic permeants (deuterium oxide and diclofenac sodium) was investigated using STD: Wistar male rats aged 5 to 180 days. The permeability of permeants through intact skin increased with increasing lipophilicity of the permeants at each age, indicating that the permselective property of rat skin is revealed even at 5-days-old. The permeability coefficients through intact skin decreased with increasing age, and the extent of these decreases was higher for lipophilic permeants than that for hydrophilic permeants. On the other hand, the stripped skin permeability of permeants was almost the same at each age, and with aging each permeability coefficient through stripped skin decreased up to 21 days, dramatically during 21-90 days and then gradually again to 180 days. The thickness of the stratum corneum and stripped skin increased according to age with faster growth during 21-90 days. The reciprocal of the mean thickness of stratum corneum and stripped skin correlated well with intact skin and stripped skin permeability (r > 0.9), respectively. These results clarified that the permselectivity of rat skin against lipophilicity of permeant exists at the latest from 5 days after birth. In addition, it is speculated that the thickness of skin is a large factor in the decrease of its permeability with age.     

Enhanced transdermal delivery of triprolidine from the ethylene-vinyl acetate matrix.

Triprolidine-containing matrix was fabricated with ethylene-vinyl acetate (EVA) copolymer to control the release of the drug. The permeation rate of triprolidine in the stripped skin was greatly larger than that in the whole skin. Thus it showed that the stratum corneum acts as a barrier of skin permeation. The effect of penetration enhancer and stripping of skin on the permeation of triprolidine through the excised mouse skin was studied. Penetrating enhancers showed increased flux probably due to the enhancing effect on the skin barrier, the stratum corneum. Among enhancers used such as glycols, fatty acids and non-ionic surfactants, polyoxyethylene-2-oleyl ether showed the best enhancement. The permeability of triprolidine was markedly increased with stripping of the mouse skin to remove the stratum corneum that acts as a barrier of skin permeation. For the controlling transdermal delivery of triprolidine, the application of EVA membrane containing permeation enhancer could be useful in the development of transdermal drug delivery system.     

Improvement of Transdermal Delivery of Tetragastrin by Lipophilic Modification with Fatty Acids

The in-vitro permeability of chemically modified tetragastrin with fatty acids through the rat skin was studied. The permeability of these compounds through intact skin and stripped skin of rat was determined with a Franz-type diffusion cell. The permeation of tetragastrin across the intact skin was improved by chemical modification with acetic acid and butyric acid. However, tetragastrin and caproyl-tetragastrin did not permeate across the intact skin up to the end of experiment. The permeation of tetragastrin across the stripped skin was improved by chemical modification, the skin flux of these acyl derivatives being in the order: acetyl > butyroyl > caproyl. The stability of tetragastrin in skin homogenate was also significantly improved by chemical modification with fatty acids. These results suggest that chemical modification of tetragastrin with fatty acids increases its lipophilicity, which makes it permeable across the stratum corneum. Moreover, the chemical modification reduced the degradation of tetragastrin in the viable skin, resulting an increase in permeation of tetragastrin across the skin.