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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 To determine the pharmacokinetic parameters of oxybutynin hydrochloride (OXB) gel in rabbits after transdermal administration of oxybutynin hydrochloride liposome gel. Methods Rabbits were respectively administered with oxybutynin hydrochloride liposome gel and normal gel, and the plasma concentration of the drug was analyzed by HPLC-MS with DAS2.1.1 software The main pharmacokinetic parameters. Results The AUC0 → 48 values of oxybutynin hydrochloride liposome gel and oxycodone hydrochloride 50 mg were 597.63 and 518.40 ng · h · mL-1, respectively, and the values of ρmax were 27.91, 29.81 ng · mL-1, tmax was 6.67 and 4.67 h respectively. The relative bioavailability of oxybutynin HCl liposome gel to the conventional oxybutynin gel was 288.4%. Conclusions Studies have shown that oxybutynin HCl liposome gel reduces the dosage administered and significantly improves bioavailability.