盐酸奥昔布宁醇脂质体凝胶家兔体内药动学研究

Pharmacokinetics in Rabbits of Oxybutynin Hydrochloride Ethosomal Gel

目的以自制盐酸奥昔布宁(OXB)凝胶为对照,测定盐酸奥昔布宁醇脂质体凝胶经皮给药后家兔体内主要药动学参数。方法家兔分别经皮给药盐酸奥昔布宁醇脂质体凝胶及普通凝胶后,采用高效液相色谱-质谱联用法(HPLC-MS)分析血药浓度,并用DAS2.1.1软件计算主要药动学参数。结果给药剂量为20 mg的盐酸奥昔布宁醇脂质体凝胶与50 mg盐酸奥昔布宁凝胶的AUC0→48分别为597.63、518.40 ng·h·mL-1,ρmax分别27.91、29.81 ng·mL-1,tmax分别为6.67、4.67 h。盐酸奥昔布宁醇脂质体凝胶对盐酸奥昔布宁普通凝胶的相对生物利用度为288.4%。结论研究表明,盐酸奥昔布宁醇脂质体凝胶减少了给药剂量,并显著性地提高了生物利用度。

OBJECTIVE In vivo study on the oxybutynin hydrochloride （ OXB ） ethosomal gel in rabbits was carried out to obtain pharmacokinetic parameters in comparison to contrast gel. METHODS After transdermal administration in rabbits of the OXB ethoso- real gel and contrast gel respectively, OXB in the plasma was determined by HPLC-MS, the pharmacokinetic parameters were calculat- ed with DAS 2. 1.1. RESULTS Dose of OXB for 20 mg in the ethosomal gel and for 50 mg in contrast gel transdermal delivery, the AUC0→48 of ethosomal gel and contrast gel were 597.63,518.40 ng . h . mL-1, ρmax were 27. 91, 29. 81 ng . mL-1,and tmax were 6. 67, 4. 67 h respectively. A relative bioavailability of OXB ethosomal gel was 288.4% compared with contrast gel. CONCLUSION In vivo experiments indicate that the OXB ethosomal gel not only reduce the drug dosage, but also show good bioavailability in rabbits.