[Studies on heart-protecting musk pH-dependent gradient-release pellets].

AIM: To prepare heart-protecting musk pH-dependent gradient-release pellets and investigate the drug release in vitro and in vivo. METHODS: The pH-dependent gradient-release pellet system was prepared by using HPMC, Eudragit L-30D-55 and Eudragit L100-Eudragit S100 (1:5) combinations as coater. The release of borneol and total ginsenoside from pH-dependent gradient-release pellets were determined according to the method of Pharmacopoeia of the People's Republic of China (2000) in the simulated gastrointestinal pH conditions. The gastrointestinal transit and disintegration of pellets was investigated by using gamma-scintigraphic trace in volunteers. The pharmacokinetics of borneol of heart-protecting musk pH-dependent gradient-release pellets was studied in 6 healthy volunteers by GC methods. RESULTS: The f2 value of release data of borneol and total ginsenoside of the heart-protecting musk pH-dependent gradient-release pellets was 79.6 in the simulated gastrointestinal pH conditions. The gamma-scintigraphic trace evaluation demonstrated that the pellets coated with HPMC, Eudragit L-30D-55 or Eudragit L100-Eudragit S100 (1:5) combinations can disintegrate in stomach, duodenum and jejunum or ileum. The gastrointestinal transit time of pellets was about 5 hours in fasted state and about 6 hours in fed state. The concentration-time curves of borneol of heart-protecting musk pills fit in two-compartment model. The pharmacokinetics data showed that borneol had a short time of absorption and elimination. The mean residence time (MRT) of borneol of heart-protecting musk pills was 2.61 hours. The plasma concentration of borneol of heart-protecting musk sustained-release capsule which consisted of three kinds of pellets coated with HPMC, Eudragit L-30D-55 or Eudragit L100-Eudragit S100 (1:5) combinations was steadier than those of heart-protecting musk pills, its Cmax was lower than and Tmax was near to those of heart-protecting musk pills, its MRT was 4.0 hours, and its relative bioavailability was 96%. CONCLUSION: The lipidsoluble borneol and watersoluble total ginsenoside of heart-protecting musk pH-dependent gradient-release pellets can release simultaneously while sustained-releasing in vitro. The heart-protecting musk pH-dependent gradient-release pellets had the characteristics of pH-dependent gradient-releasing and disintegration while transiting in gastrointestinal tract. A characteristic of gradient sustained-release was shown in the concentration-time curves of borneol of heart-protecting musk sustained-release capsule in volunteers.

[Experimental studies on antianimia effect of shengxuesu].

OBJECTIVE: Using animal anemia models to observe the antianemia effect of Shengxuesu, and to afford an experimental basis for preventing and treating anemia. METHOD: Rat model of iron deficiency induced by denutrition and mouse model of nemorrhagic anemia by blood lefting were established. Indices of hemoglobin(HB), red blood cell count(RBC), hematocrit(HCT), mean corpuscular hemoglobin count(MCHC), serum iron(SI), serum ferritin (SF) and total iron-binding capacity(TIBC) were monitored. RESULT: A dosage of Shengxuesu 0.5-2 g.kg-1 was given to the rat model of hypoferric anemia by gavage for 15 days, and to the mouse model of hemorrhagic anemia by gavage for 7 days. The result shows that HB, RBC, HCT, MCHC in blood and iron, ferroprotein in serum were elevated significantly; but total bounding iron in serum was decreased. Meanwhile, diet amount, diet consumption and general activity of the model rats were increased.

[Study on the preparation of venenum bufonis beta-cyclodextrin inclusion complexes].

OBJECTIVE: To study the preparation of Venenum Bufonis beta-cyclodextrin inclusion complexes. METHOD: An optimal condition was established by the uniform design. Under the optimal conditions the Venenum Bufonis beta-cyclodextrin inclusion complexes were prepared with 5 different methods. RESULT: The ball grinding method was superior to other four methods. The bufadienolide inclusion rate of Venenum Bufonis beta-cyclodextrin prepared with ball grinding method was 85.42%. CONCLUSION: Ball grinding method is the best method for the preparation of Venenum Bufonis beta-cyclodextrin inclusion complexes.