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药物在口腔黏膜中的渗透性研究 被引量:2

Drug permeability through buccal mucosa
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摘要 目的:研究药物的理化性质对口腔黏膜渗透性的影响。方法:选取苯甲酸和咖啡因及氢化可的松为模型药物,以离体猪颊黏膜作为动物模型,测定渗透系数。结果:苯甲酸和咖啡因及氢化可的松透过口腔黏膜的渗透系数分别为:(1.01×10-4±1.64×10-5)cm·s-1,(2.75×10-5±1.79×10-6)cm·s-1和(2.49×10-5±6.32×10-6)cm·s-1。结论:药物的口腔黏膜渗透性大于人皮渗透性。对于不同的药物,其增大倍数可能相差很大,苯甲酸和咖啡因及氢化可的松通过口腔黏膜的渗透系数分别是通过人皮的14倍和989倍及389倍。 Objective: To investigate the effects of physicochemical properties of drug on its permeability through buccal mucosa. Methods: Benzoic acid, caffeine and hydrocortisone were selected as model drugs and their permeability coefficients through isolated porcine buccal mucosa were determined. Results: The permeability coefficients of benzoic acid, caffeine and hydrocortisone through isolated porcine buccal mucosa were (1.01 × 10^-4± 1.64 × 10^-5)cm · s^-1, (2.75×10^-5±1.79×10^-6)cm · s^-1 and (2.49×10^-5±6.32×10^-6)cm · s^-1,which were 14,989 and 389 times as those through human skin,respectively. Conclusion: The permeability of drugs through buccal mucosa seems to be much better than that through human skin.
出处 《浙江大学学报(医学版)》 CAS CSCD 北大核心 2009年第2期181-185,共5页 Journal of Zhejiang University(Medical Sciences)
基金 浙江省科技计划项目(2005C30017) 杭州市属高校重点实验室科技创新项目(2006831H13)
关键词 苯甲酸 咖啡因 氢化可的松 口腔黏膜 渗透系数 Benzoic acid Caffeine Hydrocortisone Buccal mucosa Permeability coefficient
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参考文献22

  • 1SANDT J J,BURGSTEDEN J A,CAPE S,et al. In vitro predictions of skin absorption of caffeine,testosterone and benzoic acid: a multi centre comparison study [J]. Regul Toxicol Pharmacol, 2004,39 (3) : 272-281,
  • 2何毅,金克宁,汪晓军,葛新.反相高效液相色谱法同时测定复方苯甲酸酊中苯甲酸和水杨酸的含量[J].中国药房,2003,14(1):46-47. 被引量:8
  • 3张君倩,洪志玲,叶飞云.复方苯甲酸酊中苯甲酸和水杨酸含量的HPLC测定[J].中国医药工业杂志,2000,31(4):176-178. 被引量:11
  • 4MONTI D,GIANNELLI R,CHETONI P,et al. Comparison of the effect of ultrasound and of chemical enhancers on transdermal permeation of caffeine and morphine through hairless mouse skin in vitro [J]. Int J Pharm, 2001,229 (1-2) : 131 -137.
  • 5DINC E. A comparative study of the ratio spectra derivative spectrophotometry,Vierordt's method and high-performance liquid chromatography applied to the simultaneous analysis of caffeine and paracetamol in tablets [J]. J Pharm Biomed Anal, 1999,21 (4): 723- 730.
  • 6REFAI H, MuLLER-GOYMANN C C. The influence of dilution of topical semisolid preparations on hydrocortisone permeation through excised human stratum corneum[J]. Eur J Pharm Biopharm,2002,54(2):143-150.
  • 7EI-KATTAN A F, ASBILL CS, MICHNIAK B B. The effect of terpene enhancer lipophilieity on the percutaneous permeation of hydrocortisone formulated in HPMC gel systems[J].Int J Pharm, 2000,198 (2) : 179-189.
  • 8NICOLAZZO J A, REED B L,FINNIN B C. The effect of various in vitro conditions on the permeability characteristics of the buceal mucosa [J]. J Pharm Sci,2003,92(12).2399-2410.
  • 9DEWAR M J S,ZOEBISCH E G,HEALY E F, et al. AMI: A new general purpose quantum mechanical molecular model [J]. J Am Chem Soc, 1985,107 (13) : 3902-3909.
  • 10商志才,俞庆森,林瑞森.分子体积及表面积的Monte Carlo模拟计算[J].物理化学学报,1997,13(12):1097-1100. 被引量:16

二级参考文献41

  • 1傅旭春,孙群.β受体阻断剂的小肠吸收速率与分子结构的相关性[J].浙江大学学报(医学版),2005,34(2):177-180. 被引量:3
  • 2傅旭春,詹淑玉.从极性原子净电荷预测药物在人体小肠中的吸收[J].浙江大学学报(医学版),2006,35(2):199-203. 被引量:2
  • 3潘学田主编.中国医院制剂规范 :第 2版[M].北京 : 中国医药科技出版社,1995.77.
  • 4朱本仁,蒙特卡罗方法引论,1987年
  • 5顾学裘,药物制剂注解,1983年,1019页
  • 6YEE S.In vitro permeability across Caco-2 cells (colo-nic) can predict in vivo (small instinal) absorption in man--fact or myth [J].Pharm Res,1997,14(6):763-766.
  • 7ARTURSSON P,KARLSSON J.Correlation between oral drug absorption in humans and apparent drug per-meability coefficients in human intestinal epithelial (Caco-2) cells[J].Biochem Biophys Res Commun,1991,175:880-885.
  • 8ARTURSSON P, PALM K, LUTHMAN K. Caco-2 monolayers in experimental and theoretical predictions of drug transport [J].Adv Drug Deliv Res,1996,22:67-84.
  • 9TAYLOR D C,POWNALL R,Burke W.The absorption ofβ-adrenoreceptor antagonists in rat in-situ small intestine:the effect of lipophilicity [J].J Pharm Pharmaco,1985,37:280-283.
  • 10LIPISKI C A,LOMBARDO F,Dominy B W,et al.Experimental and computational approaches to eastimate solubility and permeability in drug discovery and deve-lopment settings [J].Adv Drug Deliv Res,1997,23:3-25.

共引文献34

同被引文献36

  • 1田卫群,罗勇,高秋华,黄开勋,徐辉碧.磷酸盐缓冲介质促进胰岛素透口腔黏膜渗透作用机制研究[J].中国药理学通报,2003,19(12):1354-1358. 被引量:3
  • 2CAMPISI G,PADERNI C,SACCONE R,et al.Human buccal mucosa as an innovative site of drug delivery[J].Curr Pharm Des,2010,16(6):641-652.
  • 3SUFHAKAR Y,KUOTSU K,BANDYOPADHYAY AK.Buccal bioadhesive drug delivery-A promising option for orally less effi-cient drug[J].J Control Release,2006,114(1):15-40.
  • 4KULKARNI U,MAHALINGAM R,PATHER SI,et al.Porcine buccal mucosa as an in vitro model:relative contribution of epi-thelium and connective tissue as permeability barriers[J].J Pharm Sci,2009,98(2):471-483.
  • 5LIU C,XU HN,LI XL.In vitro permeation of tetramethylpyrazine across porcine buccal mucosa[J].Acta Pharmacol Sin,2002,23(9):792-796.
  • 6NICOLAZZO JA,REED BL,FINNIN BC.Buccal penetration enhancers-How do they really work?[J].J Control Release,2005,105(1-2):1-15.
  • 7KOKATE A,LI X,JASTI B.Effect of Drug lipophilicity and i-onization on permeability across the buccal mucosa:a technical note[J].AAPS PharmSciTech,2008,9(2):501-504.
  • 8KOKATE A,LI X,WILLIAMS PJ,et al.In silico prediction ofdrug permeability across buccal mucosa[J].Pharm Res,2009,26(5):1130-1139.
  • 9DE CARO V,GIANDALIA G,SIRAQUSA MG,et al.Evalua-tion of galantamine transbuccal absorption by reconstituted human oral epithelium and porcine tissue as buccal mucosa models:part I[J].Eur J Pharm Biopharm,2008,70(3):869-873.
  • 10NICOLAZZO JA,REED BL,FINNIN BC.Enhancing the buccal mucosal uptake and retention of triamcinolone acetonide[J].J Control Release,2005,105(3):240-248.

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