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OBJECTIVE: To investigate the pharmacokinetics and bioequivalence of hyaluronic acid-graft-poly(ethylene glycol)/α-cyclodextrin nanocapsules loaded with asparaginase (AHAPs) in SD rats. METHODS: Rats were randomly divided into two groups. After intravenous injecting AHAPs and free AN, the activity of AN in two groups was assayed at different time points. The pharmacokinetic parameters were calculated by software DAS2.1.1 and the bioequivalence of free AN and AHAPs was judged. RESULTS: AUC0-48 h of AHAPs and free AN were (132.26±1.59) and (46.38±1.98) U·h·mL-1. MRT0-48 h, of AHAPs and free AN were (3.64±0.04) and (1.76±5.99) h. The tmax of AHAPs and free AN were (0.75±0) and (0.08±0) h, respectively. The results showed that AUC0-48 h, MRT0-48 h and tmax of AHAPs increased to 2.85, 2.07 and 9.37 times, respectively, as compared with free AN. The 90% confidential intervals of AUC0-48 h, AUC0-∞ and ρmax of tested formulation were 77.0%-78.5%, 77.0%-78.5%, 94.4%-96.0%, respectively. The tmax checked by nonparametric method has significant difference (P<0.05) between AHAPs and free AN. CONCLUSION: AHAPs can improve the bioavailability and extend the action time of AN in rats. AHAPs and free AN were not bioequivalent. And AHAPs had better pharmacokinetics properties in rats.
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OBJECTIVE:To compare the bioequiavailability of two simvastatin preparations in human bodies.METHODS:A total of 18 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 40mg simvastatin orally disintegrating tablet(test) or simvastatin tablets(reference).The plasma concentrations of simvastatin were determined by LC-MS,and the pharmacokinetic parameters and bioavailability were calculated with 3p97 program.RESULTS:The pharmacokinetics of simvastatin test and reference preparations were fitted the one-compartment model.The main pharmacokinetic parameters of the two preparations were as following:Cmax:(6.73?5.22) vs.(7.08?5.41)ng?mL-1、tmax:(2.11?0.74)vs.(1.89?0.85)h,AUC0～12:(19.83?19.09)vs.(19.98?18.20)ng?h?mL-1,AUC0～∞:(22.18?20.09)vs.(22.41?21.07)ng?h?mL-1.The relative bioavailability of simvastatin orally disintegrating tabl-et as against simvastain tablet(reference) was (99.25?13.11)%.CONCLUSION:Simvastatin test and reference preparations were bioequivalent.
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OBJECTIVE:To study the bioequiavailability of both the domestic and the imported azithromycin tablets in healthy human body.METHODS:The serum concentrations in 12 healthy volunteers was determined by HPLC-UV after administration of a single oral dose of 500mg azithromycin tablets by a cross-over design.The compartment model was discriminated by F-test and AIC method and the pharmacokinetic parameters were calculated by DAS program.RESULTS:The optimal compartment model fitted to two-compartment model.The main pharmacokinetics parameters of the domestic azithromycin tablets vs.the imported ones were the following:Cmax was(437.4 670? 51.5 670),(442.9 670? 61.5 030)? g/L;t1/2? was(44.7 450? 13.1 750),(49.2 670? 15.1 740)h;tmax was(2.5 830? 0.5 150),(2.5 830? 0.5 150)h;AUC0～ 144 was(13.2 799? 2.9 827),(12.1 953? 2.9 140)(mg? h)/L.The relative bioavailability of the domestic azithromycin tablets was(101.7? 0.1)%.CONCLUSION:The domestic azithromycin tablets and the imported ones were bioequivalent.
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OBJECTIVE: To study the endosomatic pharmacokinetics and bioequiavailability of kushenin tablets in health adults. METHODS: The blood concentrations of the blood samples taken from 22 healthy volunteers were determined by HPLC-MS after a single oral 0.3g kushenin (either tablet or capsule) dose and pretreatment with the internal standard (cimetidine) with m/z 265 (kushenin) taken as the detection ions and m/z 253 as the internal standard. RESULTS: The main pharmacokinetic parameters of the tablet and capsule of kushenin were as follows: t1/2 stood at (2.30?1.09)h and (1.90?0.58) h, respectively; tmax stood at (1.86?0.74)h and (1.68?0.55) h, respectively; Cmax stood at (525.09?208.94)ng/ml and (530.32?202.04) ng/ml, respectively; AUC0～11 stood at(2 048.5?749.4)(ng?h)/ml and (2 042.0?743.0)(ng?h)/ml, respectively;AUC0～∞ stood at(2 163.2?783.1)(ng?h)/ml and (2 136.4?792.1)(ng?h)/ml, respectively. The relative bioavailability of the kushenin tablet stood at (101.06?9.41) %. CONCLUSION:The tablet and capsule of kushenin were bioequiva_lent.
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0.05) . CONCLUSION: Ampicillin and probenecid capsules are of bioe-quiavailability.
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OBJECTIVE:To establish Bayesian statistics data processing method for the evaluation of bioequiavailability.METHODS:The procedures of the posterior probability calculation were simplified by means of the Excel-programmed double crossover designed Bayesian statistics analytical table for bioequiavailability.RESULTS:This method can be used as variance analysis and data processing of Bayesian statistics evalustion.CONCLUSION:The results are accurate and the application is convenient in this method.
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OBJECTIVE:To study the bioavailability of the domestic and the imported zolmitriptan tablets in human body.METHODS:The plasma concentration of zolmitriptan in24healthy male volunteers were determined by HPLC-FI after o?rally administered with single dose of5mg zolmitriptan tablets by randomized crossover way,the pharmacokinetics parameters and the relative bioavailability of which were calculated.RESULTS:The plasma concentration-time curves of the oral zolmitriptan tablets fitted one-compartment open model of linear dynamics,the main parameters of domestic tablets and im?ported tablets were described as follows,C max (8.273?3.379)ng/ml and(7.756?2.623)ng/ml,t max (2.341?1.169)h and(2.644?1.121)h,AUC 0～t (47.95?15.75)(ng?h)/ml and(46.27?13.71)(ng?h)/ml,the relative bioavailability of do?mestic zolmitriptan tablets and the imported tablets was(106.72?32.03)%.CONCLUSION:The domestic and the imported zomitriptan tablets is bioequivalent.
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OBJECTIVE:To study the bioequivalences of both domestic nevirapine capsules and imported nevirapine tablets.METHODS:24healthy male volunteers were administered orally with single dose of either the domestic nevirapine trial capsules or the imported nevirapine reference tablets by randomized crossover way,the blood concentration of nevirapine was determined by HPLC,and the pharmacokinetics parameters and the relative bioavailability of whom were calculated.RE?SULTS:The C max of the trial preparation and the reference preparation were(2.516?0.446)?g/ml and(2.798?0.394)?g/ml,respectively t max were(7.5?10.7)and(3.6?2.1)h,t 1/2 were(51.4?25.3)h and(46.4?9.8)h;AUC 0～168 were(160.540?38.007)(?g?n)/ml and(167.459?30.629)(?g?n)/ml;AUC 0～∞ were(180.064?51.005)(?g?n)/ml and(183.052?36.828)(?g?n)/ml;The relative bioavailability of the trial preparation was(98.368?22.99)%.CONCLUSION:The results shows that the trial preparation and the reference preparation of nevirapine were bioequivalent.
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OBJECTIVE:To study the bioequiavailability of domestic roxithromycin tablets and imported ones.METH?ODS:20male healthy volunteers took single dose of150mg roxithromycin tablet orally in a random crossover design,blood concentrations were determined by LC-MS.RESULTS:The main pharmacokinetic parameters of domestic and imported tablets were determined respectively as follows,AUC 0～72 were(72.81?23.85)(mg?n)/L and(72.63?20.86)(mg?h)/L,AUC 0～∞ were(74.41?24.45)(mg?h)/L and(74.42?24.45)(mg?h)/L,C max were(6.46?1.51)mg/L and(6.58?1.55)mg/L,t max were(1.9?0.5)h and(1.8?0.5)h,t 1/2 were(13.56?1.35)h and(14.18?1.50)h,the relative bioavailability of the homemade tablet to imported one was(99.8?11.2)%.CONCLUSIONS:Domestic and imported roxithromycin are bioequivalent.
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Objective To study the pharmacokinetics and bioequiavailability of Glipizide in healthy volunteers. Methods The plasma levels of Glipizide were determined at 30 min,1,2,3,4,5,6,8,10,12,14 h by HPLC after single-dose oral cross administration of 10 mg Glipizide tablets of two brands in 18 healthy male volunteers aged 23 to 25 years old,with the interval of one week. Results Glipizide tablets of the two brands were as follows,Tmax: (2.39?0.50),(2.33?0.49) h; Cmax: (675.3?151.7),(647.1?166.7)g/L; AUC_ 0-t : (3 565.4? 733.4) ,(3 304.8?588.4) ?g?h -1 ?L -1 . Conclusion The two preparations were bioequivalent.
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0.05)in healthy volunteers.
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0.05).The relative bioavailability of experimental preparation vs.reference preparation was(93.80?12.24)%.CONCLUSION:Telmisartan capsule has the same bioe-quiavailability with telmisartan tablet.
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0.05).The bioequivalence of test tablets was (105.7?13.9)%.CONCLUSION:The results of statistics analysis show that the test and reference tablets were bioequivalent.
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OBJECTIVE:To study the bioequiavailability of two sertraline hydrochloride formulations in healthy volunteers.METHODS:A randomized, crossover study of 22 healthy volunteers receiving single oral dose of 50mg sertraline hydrochloride solution(test preparation) or sertraline hydrochloride tablets(comparator preparation) was conducted and the blood concentrations determined by LC/MS/MS.RESULTS: The pharmacokinetic parameters for the test sertraline and the comparator sertraline were as follows:t1/2 were (27.3?5.2)h and (26.3?3.0)h,respectively;Cmax were(9.56?2.49)?g?L-1 and(9.43?2.91)?g?L-1,respectively;tmax were(5.18?1.47)h and(6.00?1.07)h,respectively;AUC0～108 were(329?112)?g?h?L-1 and (297?111)?g?h?L-1,respectively;AUC0～∞ were(354?127)?g?h?L-1 and (316?122)?g?h?L-1,respectively.There were no significant differences in main pharmacokinetics parameters between the 2 preparations,except in tmax from analysis of variance and one-side & two-sides t tests.The relative bioavailability of the test sertraline was(115.5?26.7)%.CONCLUSION:These two sertraline hydrochloride formulations are bioequivalent.
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OBJECTIVE:To evaluate the human body pharmacokinetics and bioequiavailability of two kinds of oral single dose of hydrochloric itraconazole capsules.METHODS:A randomized,crossover study of20healthy volunteers receiving sin-gle oral dose of200mg itraconazole was conducted with in vivo blood concentrations determined by HPLC-fluorescence de-tection.RESULTS:The pharmacokinetic parameters for the testing itraconazole and the reference itraconazole were as fol-lows,t 1/2 were(29.3?5.62)h and(29.3?5.81)h,respectively;C max were(81.4?60.0)?g/L and(77.8?45.2)?g/L,respec-tively;t max were(3.9?0.70)h and(4.2?0.70)h,respectively;AUC 0～72 were(1199.4?649.6)(?g?h)/L and(1174.3?701.9)(?g?h)/L,respectively;AUC 0～∞ were(1414.0?815.2)(?g?h)/L and(1386.1?735.8)(?g?h)/L,respectively.there were no significant differences in main pharmacokinetics parameters between2preparations,except in t max from analysis of variance and one-side&two-sides t-tests.The relative bioavailability of trial itraconazole capsule was(105.3?23.4)%.CONCLUSION:These two kinds of itraconazole capsules are bioequivalent.