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OBJECTIVE：To stud y the pharmacok inetics of PELGE-crebanine nanopartic les （PELGE-Cre-NPs） in rabbits. METHODS：Totally 6 rabbits were collected ，and injected with PELGE-Cre-NPs （3.5 mg/kg）via ear vein. 1 mL of blood samples were collected at 5，15，30，60，90，120，150，180，240，300 min after administration from the ear vein. After the plasma were isolated and Cre were extracted with ethyl acetate ，HPLC method was adopted to determine the plasma concentration of Cre by using verapamil hydrochloride as internal standard. The plasma concentration-time curve was drawed and pharmacokinetic parameters were calculated by using DAS 2.0 software. Chromatographic conditions such as the chromatographic column was Agilent ZORBAX Extend-C 18；the mobile phase consisted of methanol- 0.01％ triethylamine solution （75 ∶ 25，V/V）；the flow rate was 1 mL/min；the detection wavelength was 280 nm；the column temperature was 30 ℃；the injection volume was 20 μL. RESULTS：The linear range of Cre were 45.0-3 600 µg/L（R2＝0.999 9）. RSDs of inter-day and intra-day precision and stability tests were all lower than 5％（n＝6 or n＝12）；the accuracies were （97.44±2.41）％-（98.45±3.87）％（n＝6）. PELGE-Cre-NPs was in a two-compartment model in rabbits. Main pharmacokinetic parameters included that t1/2 was（109.357±33.917）min；CL was（0.016±0.001）L/（min·kg）；MRT was （76.733±7.502）min；cmax was（3 699.458±287.713）μg/L. CONCLUSIONS：The half-life period of PELGE-Cre-NPs in rabbits is longer than that of Cre injection；its retention time in the body is prolonged ，and sustained-release effect is obvious.
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Objective To optimize the preparation technology ofCangai volatile oil dextrin inclusion compound/ in situ nasal thermosensitive gel by the central composite design-response surface method.Methods In the design, the investigation factors were the amounts of poloxamer 407 and poloxamer 188, and the evaluation index was the gel temperature. Quadratic models were used to evaluate the mathematic relation between the evaluation index and two investigation indexes to identify the optimum prescription, and then the optimum prescription was verified. Results According to the quadratic models, it was found that there was reliable quantitative relation between the evaluation index and two investigation indexes, among which the optimum dosage was 19.37% for poloxamer 407 and 2.73% for poloxamer 188.Conclusion The optimum model ofCangai volatile oil dextrin inclusion compound/ nasal thermosensitive gel can be obtained from central composite design-response surface method based on quadratic models. This method is reliable and feasible, which can realize the prescription optimization of the in situ gel.
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Aim To investigate the effect of isocorydine on arrhythmia in rats induced by myocardial ischemia/reperfusion injury. Methods SD rats were randomly divided into 6 groups: sham group, myocardial ische-mia/reperfusion group, verapamil group and isoc-orydine group of 2. 5 , 5 , 10 mg · kg-1 , each group having 16 rats. Left anterior descending ( LAD ) was tied up to establish the injury model of myocardial is-chemia. ECG was recorded for analysis. The ischemic and infarction area was measured and indexes of SOD, MDA, GSH-Px in the myocardial were determined. Re-sults Isocorydine could significantly reduce the inci-dence of arrhythmia induced by ischemic/reperfusion, including VT, VF;and reduce ischemic and infarction area. Further study demonstrated that isocorydine could increase myocardial SOD and GSH-Px, but de-crease myocardial MDA. Conclusion Isocorydine has a protective effect on the myocardial ischemia/reperfu-sion injury, which might be related to its anti-oxidative function.