Effect of monoglycerides on the percutaneous absorption of papaverine hydrochloride.

Drug design and delivery Pub Date : 1990-06-01
M Okumura, Y Nakamori, Y Yoshida, H Niwa, K Sugibayashi, Y Morimoto
{"title":"Effect of monoglycerides on the percutaneous absorption of papaverine hydrochloride.","authors":"M Okumura,&nbsp;Y Nakamori,&nbsp;Y Yoshida,&nbsp;H Niwa,&nbsp;K Sugibayashi,&nbsp;Y Morimoto","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>The skin permeation enhancement of papaverine hydrochloride by free fatty acids (C3-C12), monoglycerides (side chains C5-C12) and caprylic acid (C8) esters was evaluated using the excised hairless rat skin. Enhancement was marked in the case of glyceryl monocaprylate; the cumulative amount of papaverine that permeated through skin over 28 hours from an aqueous suspension was 29.7 mg/cm2 with, and 26.9 micrograms/cm2 without glyceryl monocaprylate. The mechanism of enhancement was studied by measuring the effect the enhancers had on the diffusion and partition parameters of papaverine. Free fatty acids mainly affected the drug's diffusion, and monoglycerides mainly affected the drug's partition. For monoglyceride enhancers, a good linear relationship between the flux of papaverine and the amount of enhancer in skin was established. n-Octanol-water partition coefficients (log Pcal) of the enhancers were selected as indicators of their physicochemical properties, and related to their penetration-enhancing abilities. A parabolic relationship was found between the log of the flux of papaverine and log Pcal, for all types of enhancers. The relationship may be a good indicator in predicting enhancing effects.</p>","PeriodicalId":11271,"journal":{"name":"Drug design and delivery","volume":"6 2","pages":"137-48"},"PeriodicalIF":0.0000,"publicationDate":"1990-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug design and delivery","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

Abstract

The skin permeation enhancement of papaverine hydrochloride by free fatty acids (C3-C12), monoglycerides (side chains C5-C12) and caprylic acid (C8) esters was evaluated using the excised hairless rat skin. Enhancement was marked in the case of glyceryl monocaprylate; the cumulative amount of papaverine that permeated through skin over 28 hours from an aqueous suspension was 29.7 mg/cm2 with, and 26.9 micrograms/cm2 without glyceryl monocaprylate. The mechanism of enhancement was studied by measuring the effect the enhancers had on the diffusion and partition parameters of papaverine. Free fatty acids mainly affected the drug's diffusion, and monoglycerides mainly affected the drug's partition. For monoglyceride enhancers, a good linear relationship between the flux of papaverine and the amount of enhancer in skin was established. n-Octanol-water partition coefficients (log Pcal) of the enhancers were selected as indicators of their physicochemical properties, and related to their penetration-enhancing abilities. A parabolic relationship was found between the log of the flux of papaverine and log Pcal, for all types of enhancers. The relationship may be a good indicator in predicting enhancing effects.

分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
单甘油酯对盐酸罂粟碱经皮吸收的影响。
采用切除的无毛大鼠皮肤,评价了游离脂肪酸(C3-C12)、单甘油酯(侧链C5-C12)和辛酸(C8)酯对盐酸罂粟碱的皮肤渗透增强作用。单癸酸甘油酯有明显的增强作用;在水溶液悬浮液中,28小时内通过皮肤的罂粟碱累积量为:含单癸酸甘油酯时为29.7 mg/cm2,不含单癸酸甘油酯时为26.9 mg/cm2。通过测定增强剂对罂粟碱扩散和分配参数的影响,研究增强机理。游离脂肪酸主要影响药物的扩散,单甘油酯主要影响药物的分配。对于单甘酯增强剂,罂粟碱的通量与皮肤中增强剂的量之间建立了良好的线性关系。选择增强剂的正辛醇-水分配系数(log Pcal)作为其物理化学性质的指标,并与增强剂的渗透能力有关。对于所有类型的增强剂,罂粟碱通量的对数与对数cal之间存在抛物线关系。这种关系可能是预测增强效果的一个很好的指标。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 去求助
来源期刊
自引率
0.00%
发文量
0
期刊最新文献
In-silico drug design: An approach which revolutionarised the drug discovery process Insoluble drug delivery technologies: review of health benefits and business potentials Microscopy characterisation of micro- and nanosystems for pharmaceutical use Synthesis and anticonvulsant activity of 3-(3'-trifluoromethylphenoxy)-pyridines and -dihydropyridines. Synthesis of the diastereomers of 5-(2,2-dichlorocyclopropyl)- and 5-(2-chlorocyclopropyl)-2'-deoxyuridine, and the antiviral and cytotoxic activity of these and bromo analogues.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1