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用肠溶性辅料将Nap制成孔道型骨架结构的缓释胶囊,与市售片进行溶出度比较;用HPLC测定健康受试者1次和多次服用本胶囊和片剂后的血药浓度,计算胶囊剂的生物利用度.结果:Nap缓释胶囊具有缓释作用,缓释胶囊1次给药后3～24h血药浓度在40～80μg/ml的有效浓度范围内,多次给药缓释胶囊能较快达到稳态,峰谷浓度波动小,与普通片生物利用度相当,具有生物等效性;体内吸收与体外溶出度有显著相关性.提示Nap能动释胶囊是一种1d眼药1次能够维持有效治疗浓度的新的缓释制剂.
Enteric-coated adjuvant was used to make the sustained-release capsules with pore-type framework structure. The dissolution rate of Nap was compared with that of the commercially available tablets. The plasma concentrations of the capsules and tablets were measured by HPLC once and several times. The bioavailability of capsules was calculated.RESULTS: Nap sustained-release capsules had a sustained-release effect, and the drug concentrations of 40 ~ 80μg / ml 3 ~ Release capsules can reach steady state faster, peak-valley concentration fluctuation is small, with the bioavailability of ordinary tablets is equivalent, with bioequivalence; in vivo absorption and dissolution in vitro have a significant correlation.It is suggested Nap active capsule is a kind of 1d eye A new sustained-release formulation capable of maintaining a therapeutically effective concentration once a day.