Preparation of aminophylline patches and their pharmacokinetics in rabbits after navel adminstration / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare aminophylline patches and study the pharmacokinetic characteristics in rabbits after application on navel. METHODS: Aminophylline patches were prepared by hot-envelop method. Modified Franz diffusion cells were employed to screen permeation enhancers with excised rat abdomen skins as diffusion barrier. The concentration of aminophylline in rabbit plasma was determined by HPLC after aminophylline solution was irrigated intragastrically and the aminophylline patches were applied on notum and navel, respectively. Pharmacokinetic parameters were calculated and the pharmacokinetic profiles were characterized by comparing the above three groups with statistical analysis. RESULTS: Based on the excised rat skin permeation test, 3% menthol-propanediol (1 1) mixture was the optimal permeation enhancer with a steady state permeation rate of (9.08 ± 0.21) μg · cm-2 · h-1. The main pharmacokinetic parameters of, notum application group and navel application group were as follows ρmax were (13.42 ± 1.10), (4.53 ± 0.39) and (5.77 ± 0.44) μg · mL-1 and tmax(1.83 ± 0.29), (5.67 ± 0.58) and (4.33 ± 0.58) h, AUC0→t, (47.65 ± 3.46), (31.65 ± 4.11) and (39.97 ± 3.14) μg · h · mL-1, t1/2 (1. 90 ± 0.30), (2.45 ± 0.07) and (1.90 ± 0.06) h, Ka(2.01 ± 0.55), (0.33 ± 0.02) and (0.55 ± 0.04) h-1, tlag were (0.19 ± 0.04), (0.59 ± 0.03) and (0.32 ± 0.19) h, respectively. The relative bioavailabilities of aminophylline after notum and navel application were (67.41 ± 19.11)% and (84.81 ± 18.03)% respectively compared with intragastrical irrigation group. CONCLUSION: The preparation process of aminophylline patches with desirable skin permeation property is practicable. Aminophylline patches are able to realize sustained-drug release and have higher bioavailability after navel application compared with notum application.