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目的制备溴吡斯的明脂质体,考察其体外释药性质及各肠段的吸收情况。方法采用逆向蒸发法制备溴吡斯的明脂质体,测定其包封率,考察脂质体体外释放情况;运用大鼠离体外翻肠囊模型,采用RP-HPLC法测定肠囊液中溴吡斯的明浓度,考察脂质体肠道吸收行为。结果脂质体包封率为(51.81±2.15)%,72 h累积释放率(95.08±4.02)%;脂质体能显著增加溴吡斯的明在十二指肠、空肠、回肠和结肠段的吸收(P<0.05);溴吡斯的明溶液和脂质体在各肠段表观渗透系数分别为(1.41±0.73)×10-5、(2.21±0.62)×10-5、(2.13±0.27)×10-5、(1.30±0.79)×10-5 cm/s和(1.53±0.38)×10-5、(2.67±0.55)×10-5、(2.39±0.42)×10-5、(2.59±0.70)×10-5 cm/s,其中两者结肠段表观渗透系数值差异有统计学意义(P<0.05)。结论脂质体在体外介质中具有一定缓释作用。通过增加渗透性有望提高溴吡斯的明在体内生物利用度。
OBJECTIVE To prepare the liposomes of Radix Bupleuri and study its in vitro drug release properties and the absorption of each segment. Methods Liposomes were prepared by reverse evaporation method. The entrapment efficiency of the liposomes was determined and the release of liposomes in vitro was investigated. The eversion capsule model was used in vitro and the content of bromine Mice’s concentration, the study of liposome intestinal absorption behavior. Results The encapsulation efficiency of liposomes was (51.81 ± 2.15)%, and the cumulative release rate was (95.08 ± 4.02)% after 72 h. (1.41 ± 0.73) × 10-5, (2.21 ± 0.62) × 10-5, (2.13 ± 0.62) × 10-5, respectively) (P <0.05) 0.27) × 10-5, (1.30 ± 0.79) × 10-5 cm / s and (1.53 ± 0.38) × 10-5, (2.67 ± 0.55) × 10-5, (2.39 ± 0.42) × 10-5, (2.59 ± 0.70) × 10-5 cm / s, respectively. There was significant difference between the two groups in the apparent permeability coefficient (P <0.05). Conclusion Liposomes have some sustained release in vitro. It is expected to increase the in vivo bioavailability of triptolide by increasing permeability.