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目的:研制盐酸文拉法辛(venlafaxine hydrochloride,VH)缓释片,并评价其家犬药动学特性及生物利用度。方法:以Kollidon SR为基本骨架材料制备缓释片芯,用Kollicoat SR 30D包衣混悬液包衣,采用单因素考察法优化VH缓释片。以RP-HPLC测定VH血药浓度,对6只家犬进行药动学和生物利用度初步研究。结果:VH缓释片优化处方中片芯骨架材料为Kollidon SR 80%,以Kollicoat SR 30D包衣混悬液包衣增重为1%时,具有良好的缓释特征;单剂量口服自制VH缓释片与市售VH缓释胶囊的AUC0～36 h分别为(1 107.25±202.85)和(1 172.54±276.05)ng.h.mL-1;Tmax为(7.2±0.8)和(6.7±0.8)h;Cmax为(106.57±19.40)和(102.00±34.00)ng.mL-1;缓释片的相对生物利用度为(96.04±13.20)%。结论:盐酸文拉法辛缓释片具有缓释特征,同市售缓释胶囊生物等效。
OBJECTIVE: To develop sustained-release tablets of venlafaxine hydrochloride (VH) and evaluate its pharmacokinetics and bioavailability in dogs. Methods: Kollidon SR was used as the basic framework material to prepare sustained-release core. The coating was coated with Kollicoat SR 30D and the VH sustained-release tablets were optimized by single factor method. The plasma concentration of VH was determined by RP-HPLC. The pharmacokinetics and bioavailability of 6 domestic dogs were studied. Results: The optimized formulation of VH sustained-release tablet was Kollidon SR 80%, and sustained-release characteristics were obtained when Kollicoat SR 30D coating suspension weight gain was 1%. A single dose of oral self-made VH The AUC0 ~ 36 h of the release tablets and the commercially available VH sustained release capsules were (1 107.25 ± 202.85) and (172.24 ± 276.05) ng.h.mL-1, respectively; the Tmax was (7.2 ± 0.8) and (6.7 ± 0.8) h; Cmax was (106.57 ± 19.40) and (102.00 ± 34.00) ng.mL-1 respectively; The relative bioavailability of the sustained-release tablets was (96.04 ± 13.20)%. CONCLUSION: Venlafaxine hydrochloride sustained-release tablets have sustained-release characteristics and are bioequivalent to commercially available sustained-release capsules.