scholarly journals Pharmacokinetics study of Pioglitazone (30 mg) tablets in healthy volunteers

2015 ◽  
Vol 13 (2) ◽  
pp. 181-186 ◽  
Author(s):  
Sajal K Saha ◽  
AK Azad Chowdhury ◽  
Sitesh C Bachar
Keyword(s):  
High Performance ◽  
Reversed Phase ◽  
Pharmacokinetic Parameters ◽  
German Population ◽  
Polymorphic Variation ◽  
Healthy Male ◽  
Insulin Sensitizer ◽  
Bangladeshi Population ◽  
Randomized Protocol

Pioglitazone, an excellent insulin sensitizer, is used for the treatment of type 2 diabetes mellitus (T2DM). The present investigation demonstrated a single dose pharmacokinetic study of pioglitazone tablet in 24 healthy male volunteers in a randomized protocol. Blood samples were collected before and 0.5 to 24.0 h after a single oral dose of a 30 mg pioglitazone tablet. Plasma pioglitazone level was determined using a validated method of reversed phase binary high performance liquid chromatography (HPLC). The pharmacokinetic parameters determined were 1.117 ± 0.315 (?g/ml), 2.5 ± 0.735 (h), 9.014 ± 3.385 (?g.h/ml), 8.081 ± 3.407 (?g. h/ml), 1.315 ± 0.964 (h), 0.707 ± 1.636 (h-1), 0.078 ± 0.02 (h-1) and 8.884 ± 03.808 (h) for Cmax, Tmax, AUC0-?, AUC0-24, Ka, T1/2 (?), Kel, and T1/2(?), respectively. Variation of pioglitazone pharmacokinetic parameters in Bangladeshi population compared to Chinese, Thai and German population may indicate the polymorphic variation in the pioglitazone responsive metabolizing gene CYP3A4 and CYP2C19 in our population. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21896 Dhaka Univ. J. Pharm. Sci. 13(2): 181-186, 2014 (December)

Lack of Pharmacokinetic Interaction Between the Antimigraine Compound, Almotriptan, and Propranolol in Healthy Volunteers

Cephalalgia ◽  
2001 ◽  
Vol 21 (1) ◽  
pp. 61-65 ◽  
Author(s):  
JC Fleishaker ◽  
TA Sisson ◽  
BJ Carel ◽  
NE Azie
Keyword(s):  
High Performance ◽  
Treatment Effects ◽  
Vital Signs ◽  
Area Under The Curve ◽  
Pharmacokinetic Interaction ◽  
Concomitant Administration ◽  
Crossover Design ◽  
Pharmacokinetic Parameters ◽  
Percent Confidence Interval ◽  
Healthy Male

This study was designed to assess the pharmacokinetics of almotriptan, a 5-HT1B/1D agonist, when administered in the presence and absence of propranolol. Healthy male ( n = 10) and female ( n = 2) volunteers received (i) 80 mg propranolol twice daily for 7 days and 12.5 mg almotriptan on day 7, and (ii) 12.5 mg almotriptan on day 7, according to a two-way crossover design. Plasma and urinary almotriptan concentrations were measured by high performance liquid chromatography (HPLC) methods. Treatment effects on pharmacokinetic parameters were assessed by analysis of variance (anova). Statistically significant differences between treatments in area under the curve (AUC), clearance, and half-life were observed ( P < 0.03), but these differences were < 7%. Ninety percent confidence interval analysis of log-transformed pharmacokinetic parameters showed that the treatments were equivalent. Adverse events were mild to moderate in intensity, and no treatment effects on vital signs were observed. The results show that propranolol has no effect on the pharmacokinetics of almotriptan. Concomitant administration of the two drugs is well tolerated.

Determination of Fenofibric Acid in Rat Plasma and its Application to a Comparative Pharmacokinetic Study of JW322 and Fenofibrate

Drug Research ◽  
2017 ◽  
Vol 67 (09) ◽  
pp. 534-538
Author(s):  
Tae Kim
Keyword(s):  
High Performance ◽  
Internal Standard ◽  
Relative Bioavailability ◽  
Rat Plasma ◽  
Reversed Phase ◽  
Pharmacokinetic Parameters ◽  
Fenofibric Acid ◽  
Ultraviolet Detector ◽  
Quantitation Limit

AbstractIn this study, a sensitive and reliable method for the quantitation of fenofibric acid in rat plasma was developed and validated using high performance liquid chromatography (HPLC). The plasma samples were prepared by deproteinization, and sildenafil was used as an internal standard. Chromatographic separation was achieved using a reversed-phase (C18) column. The mobile phase, 0.02 M ammonium acetate buffer:acetonitrile (35:65, v/v), was run at a flow rate of 1.0 mL/min, and the column eluent was monitored using an ultraviolet detector at 280 nm at room temperature. The retention times of sildenafil (an internal standard), and fenofibric acid were approximately 5.9 and 7.7 min, respectively. The quantitation limit of fenofibric acid in rat plasma was 0.03 μg/mL. Pharmacokinetic parameters of fenofibric acid was evaluated after oral (at doses of 20 mg/kg) administration of JW322 and fenofibrate in rats. After oral administration (20 mg/kg) of JW322, relative bioavailability was approximately 272.8% compared to fenofibrate.

scholarly journals Comparative Bioequivalence Studies of doxysam and doxycycline (Pfizer) by reversed phase HPLC.

2010 ◽  
Vol 7 (1) ◽  
pp. 601-606
Author(s):  
Baghdad Science Journal
Keyword(s):  
Single Dose ◽  
High Performance ◽  
Body Height ◽  
Reversed Phase ◽  
Healthy Male ◽  
Reference Drug ◽  
Crossover Studies ◽  
Significant Difference ◽  
The Mean ◽  
Sampling Times

Isocratic high performance liquid chromatography on reversed phase a (150x 4.6 mm I.D), 5 ?m ?-Bondapak RP-8 column (with acidic mobile phase allow the separation of doxcycycline hydrochloride with low detection limit of 0.2 µg/ml detected by UV set at 226 nm. The method was validated for Doxycycline between 0.156- to 5 µg/ml. The concentration of doxycycline was assessed in two single dose randomized crossover studies with intervals of one week between two period. In sera of 20 adults healthy male volunteers with average age of (42 + 10) year, body weight 48-85 kg, body height of (160-185cm) after a single dose of doxycycline hydrochoride 100 mg in form of capsules were orally administrated for both formulations. The blood samples (2ml) were drawn concomitantly from 0.5 – 24 hours. µg The pharmacokinetics parameter were obtained from the mean serum concentration measured at various sampling times for both formulations. The maximum peak concentration (Cmax) of doxycycline reference drug from Pfizer In serum was (3.1 +0.094 µg /ml) attained in 2 hrs. While the maximum concentration (Cmax) of test drug doxysam (2.8 +0.098 µg /ml) attained in about 2 hrs, both drug have long elimination time with half time of approximately (13 hrs.) Both test and reference drug were show no significant difference in pharmacokinetics parameters, so they were considered to be bioequivalent.

scholarly journals Analytical Methods for Simultaneous Estimation of SGLT2 Inhibitor and DPP-4 Inhibitor in their Combination for Treatment of Type 2 Diabetes Mellitus

2020 ◽  
Vol 10 (1) ◽  
pp. 1799-1815
Keyword(s):  
Type 2 Diabetes ◽  
High Performance ◽  
Sglt2 Inhibitor ◽  
Simultaneous Equation ◽  
Reversed Phase ◽  
Fixed Dose ◽  
Simultaneous Estimation ◽  
Rp Hplc ◽  
Relative Standard

The Saxagliptin Hydrochloride (SAXA) and Dapagliflozin (DAPA) Fixed-Dose Combination has recently been approved for the treatment of Mellitus type 2 diabetes. In order to simultaneously estimate SAXA and DAPA is a bulk product and its formulation, the study aimed at developing a simple, fast, sensitive, and validated UV-Spectrophotometric and reversed-phase high-performance liquid chromatography (RP-HPLC) methods. Simultaneous equation UV method was performed on Shimadzu UV-1800 Spectrophotometer based on measurement of SAXA and DAPA absorption in methanol at 210 nm and 224 nm, respectively, over 6-22 μg / mL and 12-44 μg / mL linear ranges. RP-HPLC method was designed using an HPLC system-equipped PDA detector. The method has been validated for SAXA and DAPA for a range of 8 to 22 μg / ml and from 16 to 44 μg / mL. In compliance with ICH guideline Q2(R1), the optimal approach is successfully validated. The results showed that the method was accurate (98.22–100.28 percent w / w and 99.48–100.15 percent w / w SAXA and DAPA, respectively) and precise (percentage of relative standard deviation < 2.0). Developed methods follow ICH Q2 (R1) criteria and sufficient to apply regulatory versatility for submission.

scholarly journals STEADY-STATE PHARMACOKINETICS OF METFORMIN IN OBESE PATIENTS WITH TYPE 2 DIABETES MELLITUS: A PRELIMINARY STUDY

2016 ◽  
Vol 10 (1) ◽  
pp. 294
Author(s):  
Vitarani Dwi Ananda Ningrum ◽  
Zullies Ikawati ◽  
Ahmad Hamim Sadewa ◽  
M. Robikhul Ikhsan ◽  
S. Saepudin
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Steady State ◽  
High Performance ◽  
Peak Level ◽  
Reversed Phase ◽  
Chromatography Method ◽  
The Impact

ABSTRACTObjective: This study aimed to determine the metformin plasma steady-state concentration (PSSC) either trough and peak level in Type 2 diabetesmellitus patients with obesity and the impact of SLC22A1 gene organic cation transporter 1 (OCT) rs628031 A>G on PSSC of metformin.Methods: Validated reversed-phase high-performance liquid chromatography method with ultraviolet detector was used to determine the metforminPSSC, as well as genotype variation was performed using the restriction fragment length polymorphisms-polymerase chain reaction method.Results: A total of 13 patients were recruited from five Primary Health Centers in Yogyakarta Province of Indonesia. The results showed that themeans of their trough and peak PSSC were 0.285±0.192 and 1.175±0.814 µg/ml, respectively. Only 10 patients (77%) had peak PSSC within theplasma therapeutic level (PTL) of metformin, and 14-fold variability was observed for the peak PSSC. None of the patients achieved the PTL ofmetformin with regard to their trough PSSC. The PSSC of metformin was independent of the OCT1 genotype in rs628031 (A>G) 408M/V SLC22A1.Conclusion: This study found a huge variability in the trough concentration of metformin (>100-fold) and 14-fold for the peak PSSC, and no impactof a variant of rs628013 SLC22A1 OCT1 on metformin PSSC was revealed.Keywords: Metformin, Steady-state pharmacokinetics, Obesity, Type 2 diabetes mellitus.

scholarly journals Effects of Borneol on Pharmacokinetics and Tissue Distribution of Notoginsenoside R1 and Ginsenosides Rg1 and Re inPanax notoginsengin Rabbits

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Shixiang Wang ◽  
Weijin Zang ◽  
Xinfeng Zhao ◽  
Weiyi Feng ◽  
Ming Zhao ◽  
...  
Keyword(s):  
High Performance ◽  
Ion Trap ◽  
Panax Notoginseng ◽  
Underlying Mechanism ◽  
Reversed Phase ◽  
Pharmacokinetic Parameters ◽  
Ion Trap Mass Spectrometry ◽  
Rabbit Plasma ◽  
Apparent Permeability ◽  
Efflux Ratio

The purpose of this study is to investigate the effects of Borneol on the pharmacokinetics of notoginsenoside R1 (NGR1) and the ginsenosides Rg1 (GRg1) and Re (GRe) inPanax notoginseng. Reversed phase high-performance liquid chromatography coupled with electrospray ion trap mass spectrometry was employed to determine the concentrations of the three compounds in rabbit plasma. In comparison with rabbits administratedPanax notoginsengextract alone, animals simultaneously takingPanax notoginsengextract and Borneol exhibited significant differences in pharmacokinetic parameters of NGR1, GRg1, and GRe, such as increasing their bioavailability. Quantities of NGR1, GRg1, and GRe in rabbit tissues were also increased after combining administration of Borneol. In addition, the apparent permeability coefficients (Papp) of NGR1, GRg1, and GRe were raised by Borneol significantly in Caco-2 cells. However, no significant changes were observed in the efflux ratio (Er) of NGR1, GRg1 and GRe. These data indicate that Borneol has the properties of enhancing the intestinal absorption, increasing the distribution, and inhibiting the metabolism of NGR1, GRg1, and GRe. The underlying mechanism might be attributed to the loosening of the intercellular tight junction.

scholarly journals Pharmacokinetics of diltiazem hydrochloride delay-onset sustained-release pellet capsules in healthy volunteers

2013 ◽  
Vol 49 (1) ◽  
pp. 29-38 ◽  
Author(s):  
Xi-Qing Yan ◽  
Zhi-Gang Chen ◽  
Rong-Liang Wang ◽  
Jun Yang ◽  
Fang Ai ◽  
...  
Keyword(s):  
Controlled Release ◽  
Oral Dose ◽  
Sustained Release ◽  
Healthy Volunteers ◽  
Single Oral Dose ◽  
High Performance ◽  
Reversed Phase ◽  
Pharmacokinetic Parameters ◽  
Diltiazem Hydrochloride ◽  
New Formulation

The pharmacokinetics (PK) of ordinary tablets and sustained release capsules of diltiazem hydrochloride in human clinical trials had been studied. The PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules, a new dosage form, has not been reported, although it is very important to clinical use. In this paper, we investigated the PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules and the food influence in Chinese healthy volunteers. The PK parameters indicated that the diltiazem hydrochloride delay-onset sustained-release pellet capsules appeared marked characteristics of delayed and controlled release. An opened-label, randomized and parallel clinical trial was conducted in 36 Chinese healthy volunteers with single oral dose (90 mg, 180 mg or 270 mg) and a multiple oral dose (90 mg d-1×6 d) administration. The effect of food on the PK of one single oral dose (360 mg) was investigated in 24 healthy Chinese volunteers. Plasma diltiazem concentration was determined by reversed-phase high-performance liquid chromatography (RP-HPLC) and the main pharmacokinetic parameters were analyzed by PKSolver (Ver 2.0). All clinical studies were conducted in the Clinical Pharmacological Center (No. JDX1999064) of Xiangya Hospital Affiliated Central South University, China. The PK parameters suggested that the new formulation had marked characteristics of delayed and controlled release of diltiazem, and food intake did not alter significantly diltiazem pharmacokinetic parameters.

scholarly journals Pharmacokinetic parameters of Amoxicillin in Bangladeshi volunteers: a preliminary evaluation

2014 ◽  
Vol 26 (1-2) ◽  
pp. 1-9
Author(s):  
Reefat Zaman Chowdhury ◽  
Md. Saiful Islam ◽  
Md. Sayedur Rahman
Keyword(s):  
Healthy Volunteers ◽  
High Performance ◽  
Oral Route ◽  
Absolute Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Intravenous Route ◽  
Population Pharmacokinetic ◽  
Preliminary Evaluation ◽  
The Difference ◽  
Bangladeshi Population

The present study was designed to get preliminary idea about the pharmacokinetic behavior of the Bangladeshi population through estimating plasma amoxicillin concentration by High-Performance Liquid Chromatography (HPLC) with ultraviolet detection. In this study, Bangladeshi healthy volunteers were divided in two groups, 8 Bangladeshi Bangalee and 7 Bangladeshi Tribal male healthy volunteers. Both the groups received 500 mg of amoxicillin in oral route and blood samples were collected at 0, 30, 60, 120, 180, 360 and 480 minutes after drug administration. After 1 week of washout period, same volunteers of two groups received 500 mg of amoxicillin in intravenous route. In case of oral route, the Cmax, AUC0–8h, Tmax and T1/2 values for Bangladeshi Bangalee and Tribal healthy volunteers were 6.78 ± 1.20 & 9.10 ± 1.34 ìg/mL, 1290.13 ± 158.39 & 1766.06 ± 188.37 ìg min/mL, 82.50 ± 32.05 & 102.86 ± 29.28 min and 96.05 ± 3.80 & 88.15 ± 5.33 min respectively. The difference in Cmax, AUC0–8h and T1/2 values between these two groups of volunteers was significant (p<0.01, p<0.001 and p<0.01 respectively). However, the difference in Tmax was not significant (p>0.05). In case of intravenous route, the C30 min and AUC0–8h values for Bangladeshi Bangalee and Tribal healthy volunteers were 17.88 ± 1.14 & 18.58 ± 0.71 ìg/mL, 2297.96 ± 222.49 & 2376.41 ± 149.99 ìg min/mL respectively and the difference was not significant (p>0.05). The T1/2 for Bangladeshi Bangalee and Tribal healthy volunteers were 97.50 ± 3.33 & 94.40 ± 2.33 min respectively and the difference was significant (p<0.05). The Mean Percent Absolute Bioavailability in Bangladeshi Bangalee and Tribal healthy volunteers was 56.76 ± 5.39 and 74.17 ± 3.90 respectively and the difference was highly significant (p<0.001). The study concluded that the pharmacokinetic parameters of amoxicillin significantly varied among Bangladeshi Bangalee and Bangladeshi Tribal healthy volunteers indicating necessity of further study on population pharmacokinetic to formulate tailor-made drug therapy in these groups of people. http://dx.doi.org/10.3329/bjpp.v26i1-2.19958 Bangladesh J Physiol Pharmacol 2010; 26(1&2) : 1-9

scholarly journals Development and Validation of Bioanalytical HPLC Method For Estimation of Telmisartan In Rat Plasma: Application To Pharmacokinetic Studies

2013 ◽  
Vol 11 (2) ◽  
pp. 121-127 ◽  
Author(s):  
Jaydeep M Patel ◽  
Anjali P Dhingani ◽  
Kevin C Garala ◽  
Mihir K Raval ◽  
Navin R Sheth
Keyword(s):  
High Performance ◽  
Limit Of Detection ◽  
High Performance Liquid Chromatographic ◽  
Rat Plasma ◽  
Reversed Phase ◽  
Hplc Method ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Limit Of Quantification ◽  
Liquid Chromatographic

A simple, specific, sensitive and rapid reversed phase high performance liquid chromatographic (HPLC) method has been developed and validated for the determination of telmisartan in small volumes of rat plasma. Biological sample preparation involving simple extraction with organic solvent, followed by dilution with mobile phase was adopted to eliminate any chromatographic solvent effects. The method was proven to be linear over a plasma concentration range of 10 to 1000 ng/mL with a mean correlation coefficient of 0.9942. The limit of detection and the limit of quantification of the newly developed method were determined to be 1 ng/mL and 10 ng/mL, respectively. The method was successfully applied to assess pharmacokinetic parameters of telmisartan in Wister rats following a single oral dose (1.8 mg/kg, b.w.). The developed method was established as a rapid analytical tool in a pharmacokinetic study as it required short retention time, high precision, sensitivity and small volumes of plasma for analysis. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14562 Dhaka Univ. J. Pharm. Sci. 11(2): 121-127, 2012 (December)

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