Zafar Saqib, Ali Asgar, Aqil Mohammed, Ahad Abdul
Abbott Vascular, New Friend's Colony Okhla, New Delhi - 110 025, India.
J Pharm Bioallied Sci. 2010 Oct;2(4):321-4. doi: 10.4103/0975-7406.72132.
The objective of this study is to investigate the feasibility of transdermal drug delivery of Labetalol Hydrochloride (LHCl) and to study the effect of different penetration enhancers on the skin permeability of LHCl.
The permeability experiments were conducted using a horizontal glass diffusion cell with a diffusional area of 2.37 cm-(2) on albino rat skin. The effect of various penetration enhancers namely turpentine oil, dimethyl formamide (DMF), menthol, dimethyl sulfoxide, pine oil, and 2-pyrollidone, and the effect of the concentration of drug and enhancer in the donor phase on the skin permeability of LHCl was studied.
The apparent partition coefficient of the drug was found to be 6.95, suggesting it to be a lipophilic drug. The preliminary skin permeation studies revealed that the permeation of LHCL through albino rat skin was moderate (K(p) = 6.490 × 10(-2) cm hr(-1)) from isotonic phosphate buffer of pH 7.4. An appreciable increase in the LHCl permeability coefficient was observed on using a co-solvent (ethanol 95%) with the penetration enhancers in the donor phase. DMSO (10% v/v) was found to be the most effective enhancer for Labetalol hydrochloride (Enhancement Factor = 1.165). An increase in the concentration of drug and enhancer in the donor cell accentuated the permeability coefficient of LHCl.
It was concluded that LHCl could be delivered via the dermal route with the use of 10% DMSO as the penetration enhancer.
本研究的目的是探讨盐酸拉贝洛尔（LHCl）经皮给药的可行性，并研究不同渗透促进剂对LHCl皮肤渗透性的影响。
使用扩散面积为2.37 cm²的水平玻璃扩散池对白化大鼠皮肤进行渗透性实验。研究了各种渗透促进剂，即松节油、二甲基甲酰胺（DMF）、薄荷醇、二甲基亚砜、松油和2-吡咯烷酮，以及供体相中药物和促进剂浓度对LHCl皮肤渗透性的影响。
发现该药物的表观分配系数为6.95，表明它是一种亲脂性药物。初步的皮肤渗透研究表明，LHCL从pH 7.4的等渗磷酸盐缓冲液中透过白化大鼠皮肤的渗透率适中（K(p)=6.490×10⁻² cm/hr）。在供体相中使用共溶剂（95%乙醇）与渗透促进剂时，观察到LHCl渗透系数有明显增加。发现二甲基亚砜（10% v/v）是盐酸拉贝洛尔最有效的促进剂（增强因子=1.165）。供体细胞中药物和促进剂浓度的增加加剧了LHCl的渗透系数。
得出的结论是，使用10%二甲基亚砜作为渗透促进剂时，LHCl可以通过皮肤途径给药。
