Singh P, Roberts M S
Department of Pharmacy, University of Queensland, Australia.
J Pharm Pharmacol. 1994 Dec;46(12):956-64. doi: 10.1111/j.2042-7158.1994.tb03250.x.
The local deep tissue penetration of bases such as diazepam, antipyrine, iodoantipyrine, haloperidol and steroids such as hydrocortisone, fluocinolone acetonide, testosterone and progesterone after dermal application as aqueous solutions was studied in a rat model. The extent of local, as distinct from systemic delivery, for each solute was assessed by comparing the tissue concentrations obtained below a treated site with those in contralateral tissues. Local direct penetration was evident for all solutes below the applied site, although depth of penetration varied between individual solutes. A physiological pharmacokinetic model was employed to estimate local tissue concentrations of various compounds after dermal application.
在大鼠模型中,研究了地西泮、安替比林、碘安替比林、氟哌啶醇等碱类以及氢化可的松、醋酸氟轻松、睾酮和孕酮等类固醇以水溶液形式经皮给药后在局部深层组织的渗透情况。通过比较处理部位下方获得的组织浓度与对侧组织中的浓度,评估了每种溶质的局部(与全身递送不同)递送程度。尽管不同溶质的渗透深度有所不同,但所有溶质在给药部位下方的局部直接渗透均很明显。采用生理药代动力学模型来估计经皮给药后各种化合物在局部组织中的浓度。