ABSTRACT
OBJECTIVE: To study the in vitro dissolution and permeation process of montelukast sodium chewable tablets, and establish the in vivo-in vitro correlation models to predict the bioequivalence of the generic preparations. METHODS:The Macro Flux drug dissolution absorption test system was used, and the satiety intestinal simulated liquid ( pH 5. 0) was used as the medium to compare the penetration of the reference preparation and test preparation. The rate, release and absorption process of the drug were examined by the quality parameters, and the bioavailability of the test preparation was predicted, thereby predicting whether the preparation was bioequivalent. RESULTS: In the satiety small intestine simulating solution, the permeation rate, ρmax and AUC0-t of the test preparation and the reference preparation were basically the same. The bioavailability was approximately 97% of the reference formulation. CONCLUSION: It is preliminarily predicted that the test preparation of montelukast sodium chewable tablets is bioequivalent with the reference preparation.
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Objective: To investigate the effect of borneol on puerarin through in vitro blood-brain barrier (BBB) model and to discuss the main pathway of borneol to promote the opening of BBB. Methods: MTT assay was conducted to investigate the toxic effects of borneol and puerarin with different concentration on the cells and to screen the concentration of tested drug. In vitro model of BBB was used to observe the effect of borneol on the opening of tight junction and the effect of borneol on puerarin through BBB. Results: The experimental drug concentration of borneol and puerarin was both 50 μmol/L by MTT experiment. There was no significant change in transepithelial electrical resistance (TEER) before administration and 24 h after administration, and the permeation rate of puerarin group and borneol + puerarin group were (59.96 ± 5.90)% and (106.80 ± 2.73)%, respectively, with significant difference between two groups. Conclusion: Borneol combined with puerarin can promote its permeation rate to a certain extent, but its mechanism needs to be further explored by cell-related tight junction proteins level and adenosine receptor signaling pathway.
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OBJECTIVE:To study the percutaneous permeability of Hydrocortisone cream with different substrates in diabetic model rats. METHODS:The Hydrocortisone O/W(oil/water)cream,water-soluble cream and oil-soluble cream were respectively prepared. Wistar rats were randomly divided into normal control group and model group. Model group was given streptozotocin(40 mg/kg)to reproduce diabetic model. Franz diffusion cell percutaneous test and HPLC were used to detect the percutaneous permea-bility rates of Hydrocortisone O/W cream,water-soluble cream and oil-soluble cream in rats of 2 groups. RESULTS:Compared with normal control group,the percutaneous permeability rates of Hydrocortisone O/W cream and water-soluble cream were obvi-ously increased,with significant difference(P0.05). CONCLUSIONS:Hydrocortisone O/W cream and water-soluble cream are easier to go through the skin of diabetic model rats,and Hydrocortisone oil-soluble cream is hard.
ABSTRACT
OBJECTIVE:To investigate the permeability of lomefloxacin through blood-pancreatic barrier in rats.METHO-DS:Lomefloxacin(20mg/kg body weight) was injected through caudal vein.At the given time points,the samples were collected.The concentrations of lomefloxacin in the serum,pancreatic tissue and liver tissue were measured by HPLC.RESULTS:The concentration-time profiles of lomefloxacin could be described as two-compartment model in rats.The peak concentrations in serum,pancreatic tissue and liver tissue were 65.550?g/ml,48.801?g/g and 84.121?g/g at 5 min post-injection respectively.Then the concentrations decreased quickly in all of them.Concentrations in pancreatic tissue were higher than those in serum at 10 min and even at 480 min post-injection.The permeation ratio (PR) through blood-pancreatic barrier was 0.744 at 5 min and rose to 3.817 at 480min.CONCLUSION:After intravenous injection,lomefloxacin can permeate blood-pancreatic barrier satisfactory,therefore it is worthy of being recommended for prevention and treatment of pancreatic infections.