目的研究一种全新合成的抗抑郁药物AJS的自微乳化制剂(AJS-SMEDDS)的理化性质和体外释药行为。方法考察AJS-SMEDDS制剂的黏度、zeta电位和粒度,研究其流变学性质及电学性质;采用总体液平衡反向透析法测定其体外释药性能;并考察了其稳定...目的研究一种全新合成的抗抑郁药物AJS的自微乳化制剂(AJS-SMEDDS)的理化性质和体外释药行为。方法考察AJS-SMEDDS制剂的黏度、zeta电位和粒度,研究其流变学性质及电学性质;采用总体液平衡反向透析法测定其体外释药性能;并考察了其稳定性。结果 AJS-SMEDDS制剂为塑性流体,在分散介质中所形成的乳滴zeta电位为-2.76 m V,粒径为(26.08±1.68)nm,制剂质量稳定,低温不影响其性能。结论 AJSSMEDDS制剂质量稳定,适合工业生产。展开更多
Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying drug delivery system(SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of H...Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying drug delivery system(SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion(SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve(AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension(P <0.01).The absorption rate constant(K_a) and the apparent permeability coefficient(P_(app)) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of K_a and P_(app) of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration(C_(max)) of the blocking model were significantly lower than those of the control model(P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%,respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.展开更多
目的筛选葛根素自微乳的处方。方法通过药物溶解度实验和伪三元相图的绘制,以粒径大小和分布为指标,筛选油相、乳化剂、助乳化剂的处方配比。测定葛根素自微乳释药系统的溶出度。结果确定的葛根素自微乳处方比例为葛根素∶油酸聚乙醇甘...目的筛选葛根素自微乳的处方。方法通过药物溶解度实验和伪三元相图的绘制,以粒径大小和分布为指标,筛选油相、乳化剂、助乳化剂的处方配比。测定葛根素自微乳释药系统的溶出度。结果确定的葛根素自微乳处方比例为葛根素∶油酸聚乙醇甘油酯(labrafil M 1944CS)∶聚氧乙烯氢化蓖麻油(RH-40)∶聚乙二醇400(PEG 400)=9.1%∶36.4%∶36.4%∶18.1%。结论通过研究确定了最优化的葛根素自微乳处方,微乳粒径分布均匀。展开更多
目的:对大蒜素自微乳肠溶软胶囊、肠溶液体硬胶囊进行体外评价。方法:对该2制剂进行自微乳化效率、粒径、形态等理化性质的考察和含量的测定,比较2制剂与市售制剂在不同释放条件下的释放度。结果:自微乳化效率<1 m in,2制剂经分散后...目的:对大蒜素自微乳肠溶软胶囊、肠溶液体硬胶囊进行体外评价。方法:对该2制剂进行自微乳化效率、粒径、形态等理化性质的考察和含量的测定,比较2制剂与市售制剂在不同释放条件下的释放度。结果:自微乳化效率<1 m in,2制剂经分散后可得到平均粒径均在(30±2)nm、呈高斯分布的球形微乳,2制剂释放度分别为80.8%和81.5%,明显高于市售制剂。结论:自微乳肠溶制剂显著提高了大蒜素的体外溶出。展开更多
文摘目的研究一种全新合成的抗抑郁药物AJS的自微乳化制剂(AJS-SMEDDS)的理化性质和体外释药行为。方法考察AJS-SMEDDS制剂的黏度、zeta电位和粒度,研究其流变学性质及电学性质;采用总体液平衡反向透析法测定其体外释药性能;并考察了其稳定性。结果 AJS-SMEDDS制剂为塑性流体,在分散介质中所形成的乳滴zeta电位为-2.76 m V,粒径为(26.08±1.68)nm,制剂质量稳定,低温不影响其性能。结论 AJSSMEDDS制剂质量稳定,适合工业生产。
基金supported by the National Natural Science Foundation of China(Grant Nos.8127410081573615)+2 种基金Natural Science Foundation of Anhui Province of China(Grant No.1408085QH189)Key Project for the Excellent Higher Education of Anhui Province of China(Grant No.2013SQRL019ZD)Research Project for the Science and Technology of Bozhou city of China(Grant No.BK2015005)
文摘Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying drug delivery system(SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion(SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve(AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension(P <0.01).The absorption rate constant(K_a) and the apparent permeability coefficient(P_(app)) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of K_a and P_(app) of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration(C_(max)) of the blocking model were significantly lower than those of the control model(P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%,respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.
文摘目的筛选葛根素自微乳的处方。方法通过药物溶解度实验和伪三元相图的绘制,以粒径大小和分布为指标,筛选油相、乳化剂、助乳化剂的处方配比。测定葛根素自微乳释药系统的溶出度。结果确定的葛根素自微乳处方比例为葛根素∶油酸聚乙醇甘油酯(labrafil M 1944CS)∶聚氧乙烯氢化蓖麻油(RH-40)∶聚乙二醇400(PEG 400)=9.1%∶36.4%∶36.4%∶18.1%。结论通过研究确定了最优化的葛根素自微乳处方,微乳粒径分布均匀。
文摘目的:对大蒜素自微乳肠溶软胶囊、肠溶液体硬胶囊进行体外评价。方法:对该2制剂进行自微乳化效率、粒径、形态等理化性质的考察和含量的测定,比较2制剂与市售制剂在不同释放条件下的释放度。结果:自微乳化效率<1 m in,2制剂经分散后可得到平均粒径均在(30±2)nm、呈高斯分布的球形微乳,2制剂释放度分别为80.8%和81.5%,明显高于市售制剂。结论:自微乳肠溶制剂显著提高了大蒜素的体外溶出。
