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Background: Supplementation of vitamin D2 or vitamin D3 is recommended for vitamin D deficiency. Weekly supplementation of 60,000 IU of vitamin D3 increases serum 25(OH) D to optimal values. Various marketed forms of vitamin D3 include tablets, capsule, granules and oral solution. The main objective of this study is to compare the relative bioavailability of vitamin D3 oral solution with vitamin D3 tablet and capsule.Methods: This is an open-label, randomized, single-dose, three-treatment study to compare the relative bioavailability of vitamin D3 oral solution with capsule and tablet. Subjects (n=70) were supplemented with single dose of one of these formulations and their blood sample were assessed for Cmax, AUC0-28d and Tmax.Results: The logarithmic transformed data of pharmacokinetic parameters were analyzed for 90% Confidence Intervals (CI) using ANOVA. The mean (90% CI) values of vitamin D3 oral solution against tablet for the ratio of Cmax and AUC0-28d were 113.00 (105.32-121.23) and 105.54 (97.95-113.72) respectively. The mean (90% CI) values of vitamin D3 oral solution against capsule for the ratio of Cmax and AUC0-28d were 115.02 (106.38 - 124.37) and 112.33 (104.44 - 120.81) respectively. These values were within the bioequivalence range of 80-125%.Conclusions: It is concluded that vitamin D3 Oral Solution formulated with nanotechnology is bioequivalent to vitamin D3 tablet and capsule. However, oral solution of vitamin D3 shows higher Cmax and AUC when compared to tablet and capsule formulations.
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Two novel Mannich base derivatives of silybin, SLB-DEA and DHSLB-PIP, were designed and synthesized. All the structures of new Mannich base derivatives of silybin were characterized by 1H NMR and HR-MS. Their protective action against CCl4-induced liver injury in mice were investigated. The changes of alanine aminotransferase (ALT), aspartate transaminase (AST), lactate dehydrogenase (LDH), total cholesterol (TC) and triglyceride (TG) were determined and the histopathological changes in liver tissues were examined. Pretreatment with a higher dosage of DHSLB-PIP (40 mg·kg-1) prevented CCl4-induced liver injury as indicated by the reduced levels of ALT, AST, LDH and TG. Meanwhile, liver histopathological improvement was observed in the model groups. The pharmacokinetics study in rats showed that the relative bioavailability of SLB-DEA and DHSLB-PIP were 172.5% and 259.8% compared with silybin. All the results suggest that SLB-DEA and DHSLB-PIP may protect liver against injury by CCl4 and the relative bioavailability was significantly increased, which is worth of further investigation for their druggability.
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Objective To investigate the pharmacokinetics and relative bioavailability of praziquantel injection in buffaloes in contrast to praziquantel tablet. Methods A single oral administration of praziquantel tablet at a dose of 20 mg/kg or intramus-cular administration of praziquantel injection at a dose of 10 mg/kg was performed in six healthy adult buffalos according to a two-period crossover design. The praziquantel concentration in plasma was determined by a high performance liquid chromatography (HPLC)method. The pharmacokinetic parameters were calculated by non-compartmental analysis. Results The main pharma-cokinetic parameters of praziquantel tablet were as follows:Tmax=(0.60±0.29)h,Cmax=(0.57±0.37)μg/ml,T1/2β=(0.70±0.42) h,AUC=(0.80±0.70)(μg/ml)·h. The main pharmacokinetic parameters of praziquantel injection were as follows:Tmax=(0.65± 0.49)h,Cmax=(3.82 ± 1.17)μg/ml,T1/2β=(1.00 ± 0.73)h,AUC=(1.61 ± 0.89)(μg/ml)·h. The relative bioavailability of pra-ziquantel injection was 402.5％in contrast to praziquantel tablet. Conclusion The praziquantel injection has pharmacokinetic characteristics of rapid absorption,high bioavailability and extensive distribution,and the clinical recommended dosage of pra-ziquantel injection is 10 mg/kg.
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OBJECTIVE:To study the pharmacokinetics behaviors and the bioavailability of aspirin phospholipid complex self-microemulsion in rats in vivo. METHODS:12 SD rats were randomly divided into aspirin suspension group(10 mg/kg)and as-pirin phospholipid complex self-microemulsion group (10 mg/kg),6 in each group. Rats were intragastrically administrated,and blood sample 0.6 mL was taken from jugular vein before administration and after 0.083,0.25,0.5,0.75,1.0,2.0,3.0,4.0,6.0, 8.0,12.0 h of administration. HPLC was used to determine the concentration of salicylic acid in rats'plasma. DAS 2.0 pharmacoki-netic software was adopted to calculate the pharmacokinetic parameters and relative bioavailability. RESULTS:The pharmacokinetic processes of both aspirin suspension and aspirin phospholipid complex self-microemulsion were in line with one-compartment mod-el. The salicylic acid of cmax of rats in aspirin suspension group and aspirin phospholipid complex self-microemulsion group were (1.904 ± 0.208),(6.457 ± 1.091) μg/mL;AUC0-12 h were (12.860 ± 1.327),(47.270 ± 12.860) μg/(h·mL);tmax were (2.167 ± 0.983),(0.917±0.540)h,respectively. Compared with aspirin suspension,salicylic acid of cmax and AUC0-12 h of aspirin phospholip-id complex self-microemulsion in rats in vivo were significantly increased (P<0.01),while tmax was significantly decreased (P<0.05);the relative bioavailability was 367.57%. CONCLUSIONS:Making aspirin into phospholipid complex self-microemulsion can improve the gastrointestinal absorption,with high relative bioavailability.
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Objetivo: Determinar la biodisponibilidad relativa de una formulación multifuente oral de sulfametoxazol de 200 mg/5 ml respecto a la formulación referente en Oryctolagus cuniculus L (conejos albinos). Material y métodos: Las muestras estudiadas consistieron en 25 frascos de suspensión de sulfametoxazol/ trimetoprima multifuente de 200 mg: 40 mg/5 ml asignado con la letra T1 para el lote 11070674; y como referente (R) 25 frascos de suspensión de Bactrim de 200 mg: 40 mg/5 ml, lote RJ0774. El protocolo consistió en administrar una dosis oral única de 100 mg/kg de sulfametoxazol de 200 mg/5 ml de cada una de las formulaciones a 12 conejos albinos, después de un ayuno de 12 horas, a través de un diseño abierto, en dos períodos cruzados (T/R), aleatorio y doble ciego, con un intervalo mayor de 5 tiempos de vida media entre cada administración, para determinar posteriormente las concentraciones plasmáticas del fármaco en períodos de tiempo predeterminados hasta las 12 horas por medio de un método espectrofotométrico colorimétrico de diazotación. Con los datos de las concentraciones plasmáticas se construyeron las curvas de biodisponibilidad y de ellas se determinaron el área bajo la curva (ABCo-12h, ABCo-∞), Cmáx y t máx. Resultados: Según análisis estadístico para bioequivalencia, se encontraron: ABCo-12h T1/ ABCo-12h R IC90% 0,873-1,021, ABC0-∞ T1/ ABC0-∞ R IC90% 0,868-1,032 y Cmáx T1/Cmáx R IC90% 0,866-1,045. Conclusiones: Los valores encontrados de sulfametoxazol multifuente están dentro del rango aceptable de bioequivalencia propuesto por la OMS y la FDA (0,80-1,25), demostrándose la bioequivalencia del multifuente T1 respecto al referente.
Objective: To determine the relative bioavailability of an oral formulation of multisource sulfamethoxazole 200 mg / 5 ml respect to the reference formulation Oryctolagus cuniculus L (albino rabbits). Material and methods: The samples studied consisted of 25 vials of suspension of sulfamethoxazole / trimethoprim multisource 200 mg: 40 mg / 5 ml T1 with the letter assigned to the batch 11070674; and as a reference (R) 25 flasks Bactrim suspension of 200 mg: 40 mg / 5 ml, RJ0774 batch. The protocol consisted of a single oral dose of 100 mg / kg of sulfamethoxazole 200 mg / 5 ml of each of the formulations to 12 albino rabbits after a 12 hour fasting, through an open design in two cross periods (T / R), randomized, double-blind study with a greater range of 5 half-lives between each administration, later to determine plasma concentrations of the drug in default until 12 hours by means of a spectrophotometric method periods of time colorimetric diazotization. With the data of plasma, bioavailability curves were constructed, including the area under the curve (ABCo-12h, ABCo-∞), Cmáx and t max were determined. Results: According to statistical analysis for bioequivalence, it was found: ABCo-12h T1/ ABCo-12h R CI 90% from 0.873 to 1.021, AUCo-∞ T1 / AUCo-∞ R 90% CI 0.868 to 1.032 and Cmax T1 / Cmax R CI 90% 0,866- 1,045. Conclusions: The values of multisource sulfamethoxazole found are within the acceptable range of bioequivalence proposed by WHO and the FDA (0.80-1.25), demonstrating the bioequivalence of multisource T1 respect to the reference.
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OBJECTIVE: To explore pharmacokinetics and relative bioavailability of penehyclidine hydrochloride in healthy subjects. METHODS: This study was an open, randomized and cross-over trial design. Twelve healthy subjects were randomized to receive pharmacokinetic analysis which were performed according to the order of ABC, BCA and CAB, and then pharmacokinetic trial of multiple dose was performed following penehyclidine hydrochloride. Twenty healthy subjects were selected to receive bioavailability study following an order of BD or DB. Blood and urine samples were collected at prescribed time and then investigated by LC-MS/MS. RESULTS: The 11 of 12 cases finished the pharmacokinetic trial. The lineare ranges of penehyclidine hydrochloride in plasma and urine were 0.1-8 ng·mL-1, 1-100 ng·mL-1, respectively and accuracy of the method was within 85%-115%. The concentration-time curve of penehyclidine hydrochloride was dose dependent within the ranges of 0.4-0.8 mg after oral administration. ρmax and AUC were significantly increased (P<0.01), Vd and CL were significantly decreased (P<0.01) following multiple dose. The relative bioavailability of penehyclidine hydrochloride was (72.44±21.03)%. The average cumulative excretion rate of penehyclidine hydrochloride with original form accounted for (4.98±1.10)% of the total administered dose. CONCLUSION: The characteristic of linear pharmacokinetics of penehyclidine hydrochloride is performed in healthy subjects after oral administration. Its excretion is mostly via non-urinary system or other metabolites.
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OBJECTIVE:To study relative bioavailability of dauricine self-microemulsifying drug delivery system (SMEDDS) in rats. METHODS:12 rats were randomly divided into dauricine SMEDDS group (20 mg/kg) and dauricine solution group (50 mg/kg),6 rats in each group. They were given relevant medicine intragastrically. Then,0.3 ml plasma was collected from orbital venous plexus before medication and 0.167,0.333,0.5,0.75,1,2,4,8,12,24,36 h after medication. The plasma concentration of da- uricine was determined by HPLC-MS/MS,and DAS 3.0 was used to calculate pharmacokinetic parameters and evaluate the relative bioavailability of dauricine with dauricine SMEDDS. RESULTS:The linear range of dauricine in plasma were 2.12-424 ng/ml (r=0.999 9);RSDs of intra-day and inter-day were all lower than 10%. Pharmacokinetic parameters of dauricine solution and dau-ricine SMEDDS were that cmax were(126.3±37.4)ng/ml and(179.6±51.5)ng/ml;t1/2 were(11.48±4.58)and(21.79±6.59)h;AUC0-t were (1 963.5±638.3)ng·h/ml and(2 535.8±739.5)ng·h/ml;AUC0-∞ were(2 256.3±703.5)ng·h/ml and(2 854.6± 768.7)ng·h/ml,respectively. The relative bioavailability of dauricine SMEDDS were 323% and 316% by calculating with AUC0-t and AUC0-∞,respectively. CONCLUSIONS:Intragastric administration of dauricine SMEDDS can improve relative bioavailability of dauricine significantly.
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Objective: To determine the potential drug-drug interactions between anti-malarial candidate 97/78 and anti-tubercular drug rifabutin in-vivo in rats followed by in-vitro investigation of the underlying mechanisms of drug interaction. Methods: Single oral dose study was conducted in male and female rats at 40 mg/kg and 70 mg/kg for 97/78 and rifabutin respectively. Results: It was reported that rifabutin co-administration altered pharmacokinetics of 97/63 (active metabolite of 97/78). A significant decrease was reported in the systemic exposure of 97/63 by a factor of 3-4. The AUC0-last values were (4.03 ± 0.60) and (5.44 ± 1.15) μg h mL-1 upon 97/78 administration alone, while the values were decreased to (1.13 ± 0.10) and (1.23 ± 1.13) μg h mL-1 upon rifabutin co-administration in male and female rats respectively. Statistically significant differences were also reported in Cmax and Tmax values upon rifabutin co-administration. In-vitro drug metabolism study in rat liver microsomes has shown that the metabolism of 97/63 was increased by 10%-12% upon rifabutin co-incubation. The extent of plasma protein binding of 97/63 was found to be decreased from 54%-55% to 6%-8% upon rifabutin addition. Conclusions: It was concluded that rifabutin co-administration altered PK parameters of 97/63 in SD rats. However, no intersex influences were reported in the interaction pattern. The results obtained in the in-vivo study were well correlated with the in-vitro findings and can further be applied to explore other aspects of potential drug interactions between these two drugs.
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OBJECTIVE@#To determine the potential drug-drug interactions between anti-malarial candidate 97/78 and anti-tubercular drug rifabutin in-vivo in rats followed by in-vitro investigation of the underlying mechanisms of drug interaction.@*METHODS@#Single oral dose study was conducted in male and female rats at 40 mg/kg and 70 mg/kg for 97/78 and rifabutin respectively.@*RESULTS@#It was reported that rifabutin co-administration altered pharmacokinetics of 97/63 (active metabolite of 97/78). A significant decrease was reported in the systemic exposure of 97/63 by a factor of 3-4. The AUC0-last values were (4.03 ± 0.60) and (5.44 ± 1.15) μg h mL(-1) upon 97/78 administration alone, while the values were decreased to (1.13 ± 0.10) and (1.23 ± 1.13) μg h mL(-1) upon rifabutin co-administration in male and female rats respectively. Statistically significant differences were also reported in Cmax and Tmax values upon rifabutin co-administration. In-vitro drug metabolism study in rat liver microsomes has shown that the metabolism of 97/63 was increased by 10%-12% upon rifabutin co-incubation. The extent of plasma protein binding of 97/63 was found to be decreased from 54%-55% to 6%-8% upon rifabutin addition.@*CONCLUSIONS@#It was concluded that rifabutin co-administration altered PK parameters of 97/63 in SD rats. However, no intersex influences were reported in the interaction pattern. The results obtained in the in-vivo study were well correlated with the in-vitro findings and can further be applied to explore other aspects of potential drug interactions between these two drugs.
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OBJECTIVE: To investigate the enhancing effect of borneol on the absorption of chlorogenic acid (CGA) with two different biological models and to evaluate the correlation of these two models. METHODS: The in situ rat perfusion model was used to investigate the enhancing effect of borneol on the absorption of CGA. The in vivo pharmacokinetics study was carried out to evaluate the correlation of the two-compartment open model. RESULTS: With the in situ rat perfusion model, the absorption rate constant (Ka) of CGA was 0.083 4 h-1, which was up to 1.58-fold higher by borneol. The results of in vivo pharmacokinetics study in rats suggested that 0.04% borneol could increase the relative bioavailability by 116.02% and maximum plasma concentration increased slightly. The consistent result of these two different absorption models was provided (r=0.941). CONCLUSION: Borneol could promote the oral absorption of CGA.
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Objective:To determine the potential drug-drug interactions between anti-malarial candidate 97/78 and anti-tubercular drug rifabutin in-vivo in rats followed byin-vitro investigation of the underlying mechanisms of drug interaction.Methods: Single oral dose study was conducted in male and female rats at 40 mg/kg and 70 mg/kg for 97/78 and rifabutin respectively. Results:It was reported that rifabutin co-administration altered pharmacokinetics of 97/63 (active metabolite of 97/78). A significant decrease was reported in the systemic exposure of 97/63 by a factor of 3-4. The AUC0-last values were (4.03 ± 0.60) and (5.44 ± 1.15) μg?h?mL-1 upon 97/78 administration alone, while the values were decreased to (1.13 ± 0.10) and (1.23 ± 1.13) μg?h?mL-1 upon rifabutin co-administration in male and female rats respectively. Statistically significant differences were also reported in Cmaxand Tmax values upon rifabutin co-administration.In-vitro drug metabolism study in rat liver microsomes has shown that the metabolism of 97/63 was increased by 10%-12% upon rifabutin co-incubation. The extent of plasma protein binding of 97/63 was found to be decreased from 54%-55% to 6%-8% upon rifabutin addition.Conclusions:It was concluded that rifabutin co-administration altered PK parameters of 97/63 in SD rats. However, no intersex influences were reported in the interaction pattern. The results obtained in the in-vivo study were well correlated with thein-vitro findings and can further be applied to explore other aspects of potential drug interactions between these two drugs.
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Se evaluó el desempeño productivo, la composición corporal y la biodisponibilidad relativa de selenio en tilapia nilótica (Oreochromis niloticus) suplementada con selenio dietario. Una dieta basal fue suplementada con selenio en forma de selenito de sodio o seleno-levadura en niveles crecientes de suplementación (0.00, 0.10, 0.20, 0.40, 0.80 y 1.60 mg/kg de dieta). Un total de 336 individuos de tilapia nilótica, con un peso inicial de 13.41±0.12 g, fueron distribuidos de forma aleatoria en 48 acuarios de vidrio (80 l, 4 réplicas, 7 peces por acuario). No se detectó selenio en el agua de abastecimiento. Los peces fueron alimentados hasta saciedad aparente 3 veces al día por un período de 9 semanas. El desempeño productivo de la tilapia nilótica no se vio afectado (P>0.05) por la suplementación con selenio dietario. El selenio corporal se incrementó de forma lineal (P<0.05) con la suplementación de selenio orgánico e inorgánico. La composición corporal de selenio fue menor (P<0.05) en los peces suplementados con selenito de sodio (1.67±0.14 mg/kg) en comparación con la seleno-levadura (1.95±0.21 mg/kg). A partir de la relación entre pendientes se estimó que la biodisponibilidad relativa de la seleno-levadura para la composición de selenio corporal fue de 155.72±0,10%, con relación al selenito de sodio (fijada en 100%). De acuerdo con los resultados, la concentración basal de selenio dietario (0.21 mg/kg) no limitó el desempeño productivo de tilapia nilótica. La suplementación con selenio orgánico (seleno-levadura) e inorgánico (selenito de sodio) entre 0.10 y 1.60 mg/kg no afectó el desempeño productivo de la tilapia nilótica.
The aim of this study was to evaluate the productive performance, whole body selenium retention and relative selenium bioavailability in Nile tilapia (Oreochromis niloticus). A practical basal diet was supplemented with either sodium selenite or seleno-yeast at tilapia fish (n=336) with an initial weight of 13.41±0.12 g were randomly distributed into forty-eight glass aquaria (80 l, 4 replicates, 7 fish per aquarium). There was no detectable selenium in supply water. Fish were fed the experimental diets to apparent satiation three times daily for nine weeks. Selenium supplementation did not affect the productive performance of Nile tilapia (P>0.05). Total whole body selenium increase linearly in response to dietary selenium supplementation (P<0.05). Fish fed sodium selenite had lower (P<0.05) whole body selenium (1.67±0.14 mg/kg) compared to fish fed seleno-yeast (1.95±0.21 mg/kg). Based on the slope-ratio assay for whole body selenium, the relative bioavailability of seleno-yeast was 155.72%±0.10 compared to sodium selenite (set at 100%). According to results the basal selenium content in expegraded selenium levels (0.0, 0.10, 0.20, 0.40, 0.80 and 1.60 mg/kg). Reversed Nile rimental diets (0.21 mg/kg) did not limit the productive performance of Nile tilapia. Supplementation of inorganic and organic selenium (0.10-1.60 mg/kg) did not affect the productive performance of Nile tilapia.
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OBJECTIVE: To prepare rhein-loaded polylactic acid nanoparticles, and investigate their physicochemical properties, release behavior in vitro and pharmacokinetics in vivo in rats. METHODS: Rhein-loaded polylactic acid nanoparticles were prepared by a modified spontaneous emulsificationsolvent diffusion method with PLA as the carrier. The morphology of rhein-loaded polylactic acid nanoparticles was observed by transmission electron microscope. Mean particle size and Zeta potential were estimated by laser particle size analyzer. Entrapment efficiency and drug loading were investigated by ultracentrifugation. Drug release behavior in vitro was studied by dialysis. Using rhein aqueous suspension as control, the pharmacokinetic behavior of rhein-loaded polylactic acid nanoparticles after oral administration in rats were studied. RESULTS: The shape of rhein-loaded polylactic acid nanoparticles was spherical. The mean particle size, Zeta potential, entrapment efficiency and drug loading were (134.37 ± 3.61) nm, (-18.41 ± 0.07) mV, (60.37 ± 1.52)% and (1.32 ± 0.09)%, respectively. The profiles of release were fitted well by Higuchi equation. Results of pharmacokinetic study showed that the ρmax of rhein suspension and rhein-loaded polylactic acid nanoparticles were (5.788 ±0.15) and (11.607 ± 0.56) mg · L-1, tmax were (0.193 ±0.01) and (1.102 ±0.13) h, AUC0→t were(8.077 ±2.98) and (34.583 ±3.93) mg · h · L-1, t1/2β were (3.319 ±0.23) and (21.721 ± 6.13) h, respectively. CONCLUSION: Polylactic acid nanoparticles can effectively improve the pharmacokinetic behaviour and oral bioavailability of rhein. Copyright 2012 by the Chinese Pharmaceutical Association.
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OBJECTIVE: To develop an HPLC method for simultaneously determining the contents of naringin and neohespiridin in rat plasma, and to investigate the pharmacokinetics and relative bioavailability of self-microemulsifying pellets of daidai flavones in rats. METHODS: The rats were divided into two groups randomly. They were administered orally suspension of daidai flavones effective parts and its self-microemulsifying pellets, which both contained 120 mg · kg-1 of flavonoids. Blood samples were collected at 0.083, 0.167, 0.333, 0.5, 0.667, 1, 2, 4, 6, 8, 10, 12 and 24 h and the concentrations of naringin and neohesperidin in rat plasma were simultaneously determined by HPLC. The pharmacokinetic parameters were calculated by DAS 3.0 pharmacokinetic program. RESULTS: The pharmacokintic parameters of naringin in the self-microemulsifying pellets of daidai flavones and the suspension were as follows: AUC0-24 (17.710 ± 6.588) and( 9.139 ± 1.982) mg · h · L-1, ρmax (4.816 ± 1.329) and (1.572 ± 0.324) mg · L-1, tmax (0.611 ± 0.086) and (1.575 ± 0.324)h, and t1/2 (13.078 ± 6.382) and (11.678 ± 6.919)h, respectively. And the pharmacokintic parameters of neohesperidin were as follow: AUC0-24 (18.094 ± 4.892) and (10.961 ± 2.276)mg · h · L-1, ρmax (5.657 ± 1.391) and (2.096 ± 0.512) mg · L-1, tmax(0.583 ± 0.091) and (0.806 ± 0.222) h, and t1/2 (14.606 ± 7.562) and (10.985 ± 6.963)h, respectively. The relative bioavailabilities of naringin and neohesperidin in the self-microemulsifying pellets of daidai flavones were 193.78% and 165.08%, respectively. CONCLUSION: The bioavailability of daidai flavones is increased by making them into self-microemulsifying pellets, and the biopharmaceutical property of the flavones is improved.
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OBJECTIVE:To study the bioequivalence of 2 kinds of Losartan potassium tablets in healthy volunteers. METHODS: A single oral dose of test tablet 100 mg and reference tablet 100 mg were given to 20 healthy volunteers in randomized crossover study. The plasma concentrations of losartan and its metabolite EXP3174 were determined by LC-MS. The pharmacokinetic parameters were calculated and bioequivalence of 2 kinds of tablets was evaluated. RESULTS: Main pharmacokinetic parameters of Losartan of test tablets vs. reference tablets were as follows: Cmax(534.230?238.642) ng?mL-1 vs.(520.020?226.800) ng?mL-1; tmax(1.401?0.946)h vs.(1.334?0.750)h; AUC0～36(871.177?232.315) ng?h?mL-1 vs. (773.030?252.209) ng?h?mL-1; pharmacokinetic parameters of metabolite EXP3174 of test tablets vs. reference tablets were as follows: Cmax (1 294.000?387.815) ng?mL-1 vs.(1 140.900?317.615)ng?mL-1;tmax(2.667?1.144)h vs.(2.734?1.162)h;AUC0～36(6 267.905?1 350.300)ng?h?mL-1 vs.(5 719.411?1 127.725) ng?h?mL-1; AUC0～∞(6 316.605?1 343.048)ng?h?mL-1 vs. (5 755.335?1 138.358) ng?h?mL-1. The relative bioavailability of test tablet was (116.6?24.3)%. CONCLUSION: 2 kinds of Losartan potassium tablets are bioequivalent.
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OBJECTIVE:To study the pharmacokinetics and the bioequivalence of cefdinir dispersible tablets in healthy volunteers.METHODS:Microbiological assay method was used to determine the plasma concentration at different time in 20 healthy volunteers after oral administration of single dose of 400mg of cefdinir dispersible tablets(test preparation) and cefdinir capsule(reference preparation) by cross-over way.RESUTLS:The concentration-time curves of test preparation and reference preparation of cefdinir fitted one compartment open model.The pharmacokinetic parameters of the test preparation vs.the reference preparation were as follows:tmax(3.48?0.53)h vs.(3.60?0.48)h,Cmax(2.10?0.32)mg?L-1 vs.(2.15?0.26)mg?L-1.t1/2ke(2.41?0.39)h vs.(2.33?0.41)h,AUC0～12(9.51?1.65)mg?h?L-1 vs.(10.05?1.72)mg?h?L-1,AUC0～∞(10.43?1.62)mg?h?L-1 vs.(11.01?1.81)mg?h?L-1,respectively.The relative bioavailability of cefdinir dispersible tablet as against its reference preparation was(96.03?14.89)%.CONCLUSION:The two preparations of cefdinir were proved to be bioequivalent.
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OBJECTIVE:To evaluate the relative bioavailability of2kinds of preparations of cefaclor capsules.METH?ODS:The subjects'blood concentrations were determined by HPLC at different time after administered randomly crossover with single oral dose of cefaclor testing preparation or reference preparation.The actual values of C max and T max were adopted;AUC was calculated by trapezoid planimetry;the bioequiavailability of the2preparations were evaluated by two-sides and one-side t-test.RESULTS:The AUC 0～4 of the testing preparation and reference preparation were respectively(13.44?3.06)(?g?h)/ml and(14.19?3.28)(?g?h)/ml;their respective AUC 0～∞ were(13.80?3.08)(?g?h)/ml and(14.62?3.33)(?g?h)/ml;their respective C max were(11.65?2.39)?g/ml and(12.37?2.41)?g/ml;their respective t max were(0.57?0.24)h and(0.66?0.19)h.The relative bioavailability of testing preparation was(95.62?13.51)%.CON?CLUSION:The2preparations are bioequivalent.
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OBJECTIVE:To study the pharmacokinetics and bioequivalence of both domestic ranitidine hydrochloride capsules and imported ranitidine hydrochloride tablets.METHODS:20healthy volunteers were randomized into groups,whose plasma concentrations of ranitidine were determined at different time after single oral dose of300mg ranitidine hydrochloride capsule or ranitidine hydrochloride tablets300mg by own control by a RP-HPLC method,the pharmacokinetic parameters were computed and which were experienced variance analysis and two-way t-tests and one-way t-tests.RESULTS:The respective pharmacokinetic parameters of ranitidine hydrochloride tablets and ranitidine hydrochloride capsuless were as fol?lows,the C max were(1247.1?547.5)?g/L and(1294.8?613.2)?g/L;t max were(2.98?0.73)h and(2.73?0.80)h;t 1/2 were(3.17?0.36)h and(3.33?0.42)h;AUC 0～t were(5805.9?1403.5)(?g?h)/L and(5941.2?1526.3)(?g?h)/L;AUC 0～∞ were(6163.8?1456.4)(?g?h)/L and(6351.8?1652.7)(?g?h)/L;The relative bioavailability of the ranitidine hydrochloride capsules to ranitidine hydrochloride tablets was(104.3?24.3)%.CONCLUSION:Ranitidine hydrochloride capsules and the ranitidine hydrochloride tablets were bioequivalent.
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AIM:To study the pharmacokinetics and relative bioavailability of citalopra hydrobromide in human plasma.METHODS:The citalopra hydrobromide concentrations in plasma were determined by HPLC-UV.The column was Lichrospher ODS(5 ?m,250 mm?4.6 mm).The mobile phase was acetonitrile-0.1 mol/L KH2PO4 buffer-triethylamine(35:65:0.3,v/v/v).The flow rate was 1 mL/min.The detection wavelength was 240 nm.The test and reference formulations of citalopra were given to 18 healthy male volunteers.RESULTS:The calibration curve was linear within the range of 2-128 ?g/L,r=0.9992.The minimum detection limit was 1 ?g/L.The recovery was 80%-88%,the RSDs of inter-day and intra-day were not more than 15%.After a single oral dose of 20 mg citalopra hydrobromide was given,the main pharmacokinetic parameters tmax were(4.6?1.0),(4.4?1.4) and(4.0?1.4) h;Cmax were(70?19),(71?17) and(66?21) ?g/L;and t1/2 were(37?9),(37?6) and(36?6) h respectively.CONCLUSION:No significant difference exists among the pharmacokinetic parameters of the three formulations.They are bioequivalent.
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AIM: To study the relative bioavailability of clavulanic acid/amoxicillin dispersive tablets. METHODS: A single oral administration of 125 mg clavulanic acid and 500 mg amoxicillin of dispersive tablet and Anqi tablet to 18 healthy male volunteers in a randomized cross-over study. The plasma concentration of clavulanic acid and amoxicillin simultaneous were determined with HPLC. RESULTS: The pharmacokinetic parameters of dispersive tablet and Anqi tablet for clavulanic acid were: Tmax (0.89± 0.25) h and (1.01±0.30) h; Cmax (1.92±0.64) mg·L-1 and (1.49±0.65) mg·L-1; AUC0→∞ (4.347±1.542) mg·h·L-1 and (3.395±1.468) mg·h·L-1, the pharmacokinetic parameters for amoxycillin were: Tmax (1.15±0.41) h and (1.34±0.40) h; Cmax (5.81±1.40) mg·L-1 and (4.60±1.37) mg·L-1; AUC0→∞ (13.472±3.114) mg·h·L-1 and (11.937±2.735) mg·h·L-1. The clavulanic acid Tmax of clavulanic acid/amoxicillin dispersive tablet was significantly shorter, clavulanic acid and amoxicillin Cmax, AUC0→∞ of clavulanic acid/amoxicillin dispersive tablet were significantly greater than the control Anqi tablet respectively, while there was no significant difference between amoxicillin Tmax of two tablets. CONCLUSION: The bioavailability of clavulanic acid/amoxicillin dispersive tablet is superior to Anqi tablet.