Bioequivalence study of two formulations of enalapril, at a single oral dose of 20 mg (tablets): A randomized, two-way, open-label, crossover study in healthy volunteers

Portolés, Antonio; Terleira, Ana; Almeida, Susana; García-Arenillas, Mar; Caturla, Mari-Cruz; Filipe, A. P.; Vargas, Emilio

doi:10.1016/s0011-393x(04)90003-3

Cited by 17 publications

(14 citation statements)

References 5 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Inrecenty ears,the useo fg enericdrugshasincreased duetotheireffectiveness and the increasing variety of drugst hataren owavailable asgenericformulations. However,theiru sei nclinicalpracticedependsnotonly on theiressentialsimilarity (in formulation and composition,a sdetermined byr egulatory agencies),b ut also on theirbioequivalencewiththeirr eferencecounterparts.Therefore,studyof the comparativebioavailability of test and referencef ormulationsisimportantfor appropriateassessmentbyt he scientificc ommunity [17].…”

Section: Discussionmentioning

confidence: 99%

Relative bioavailability and pharmacokinetic study of two trimetazidine modified release formulations in healthy Bangladeshi male volunteers

Chowdhury

Ullah

Iqbal

et al. 2011

Arzneimittelforschung

View full text Add to dashboard Cite

Trimetazidine (CAS 5011-34-7) is an effective and well-tolerated antianginal drug that possesses protective properties against ischemia-induced heart injury. The relative bioavailability and pharmacokinetic characteristics of two modified release formulations of 35 mg trimetazidine, one as the test product (Metacard MR) and one as the reference product, were compared in healthy Bangladeshi male volunteers. The randomized, two-way crossover study was conducted in 24 healthy male volunteers after administration of a single 35 mg dose of each modified release formulation after 12-h overnight fasting, with a washout period of two weeks. Blood samples were collected at various time intervals following oral administration and analyzed for trimetazidine concentrations using a validated HPLC method. The pharmacokinetic parameters were determined by a non-compartmental method. After administering a single dose of 35 mg of each trimetazidine formulation, the obtained mean (SD) values for the test and reference products were 104.78 (29.3) and 98.57 (28.7) ng/ml for Cmax; 4.00 (1.1) and 3.54 (1.32) h for tmax; 423.81 (173.9) and 410.01 (195.87) ng ? h/ml for AUC0?12; and 472.51 (195.2) and 462.78 (225.13) ng ? h/ml for AUCo?? respectively. The mean t1/2 was found 3.69 (1.1) h and 3.45 (0.72) h for test and reference products respectively. From paired t-test, no significant differences were observed (p > 0.05) for any pharmacokinetic parameters. The 90% confidence intervals of the test/reference mean ratios of the In-transformed AUC0?12, AUC0?? and Cmax mean values were 106.19% (97.16%?116.06%), 104.74% (95.04%?115.42%) and 106.30% (95.23%?118.66%), respectively. The two formulations demonstrated similar bioavailability with respect to both the rate and extent of trimetazidine absorption.

show abstract

Section: Discussionmentioning

confidence: 99%

Relative bioavailability and pharmacokinetic study of two trimetazidine modified release formulations in healthy Bangladeshi male volunteers

Chowdhury

Ullah

Iqbal

et al. 2011

Arzneimittelforschung

View full text Add to dashboard Cite

show abstract

“…These LOQs were validated in terms of relative standard deviation (RSD) and RE < 20% and signals at least 10 times higher than the blank's response. The working ranges were defined considering the LOQ, the normal therapeutic dosage and the time needed to achieve the maximum plasmatic levels [7,[10][11][12][13][14][20][21][22][23][24].…”

Section: Validationmentioning

confidence: 99%

LC–MS/MS method for the determination of several drugs used in combined cardiovascular therapy in human plasma

González

Iriarte

Rico

et al. 2010

Journal of Chromatography B

View full text Add to dashboard Cite

“…Ìàêñèìàëüíàÿ êîíöåíòðàöèÿ ýíàëàïðèëà â êðîâè äîñòèãàåòñÿ ÷åðåç 1 ÷, ýíàëàïðèëàòà -÷åðåç 3 -4 ÷. Ìàêñèìàëüíàÿ êîí-öåíòðàöèè ýíàëàïðèëà è ýíàëàïðèëàòà â ïëàçìå êðîâè ÷åëîâåêà ñîñòàâëÿåò 90,5 è 47,5 íã/ìë, ïåðèîä ïîëóâû-âåäåíèÿ -1,35 è 6,71 ÷, ñîîòâåòñòâåííî [14]. Ïðè ïðà-âèëüíî ïîäîáðàííîì ðåaeèìå äîçèðîâàíèÿ êîíöåíòðà-öèÿ ýíàëàïðèëàòà â ïëàçìå êðîâè äîëaeíà îñòàâàòüñÿ â ðàìêàõ òåðàïåâòè÷åñêîãî äèàïàçîíà, à êëèíè÷åñêèé ýôôåêò ñîõðàíÿåòñÿ äî 24 ÷ ïîñëå ïðè¸ìà ïðåïàðàòà.…”

Section: ââåäåíèåunclassified

Определение Эналаприла И Его Активного Метаболита Эналаприлата В Плазме Крови Методом Вэжх-Мс/Мс При Персонализации Фармакотерапии Больных Артериальной Гипертензией

Родина¹,

Мельников²,

Sokolov³

et al. 2015

Эксп. и клин. фармакол.

View full text Add to dashboard Cite

Разработана селективная, чувствительная и воспроизводимая методика количественного определения эналаприла и его активного метаболита эналаприлата в плазме крови человека методом обращенно-фазовой высокоэффективной жидкостной хроматографии с тандемным масс-спектрометрическим детектированием (ВЭЖХ-МС/МС). Применён метод ионизации DUIS: одновременное использование электрораспыления (ESI) и химической ионизации при атмосферном давлении (APCI). Детектирование осуществляли в режиме положительной ионизации путём мониторинга множественных реакций (MRM). Пробоподготовку плазмы крови проводили путём осаждения белков ацетонитрилом. Расчёты при количественном определении проводили методом внешнего стандарта. Калибровочная кривая носила линейный характер в диапазоне концентраций 5 – 100 нг/мл для обоих исследуемых веществ. Разработанный метод может быть использован для подбора дозы эналаприла при терапевтическом лекарственном мониторинге.

show abstract

Bioequivalence study of two formulations of enalapril, at a single oral dose of 20 mg (tablets): A randomized, two-way, open-label, crossover study in healthy volunteers

Abstract: Background: Enalapril maleate is the monoethyl ester prodrug of enalapril-

Cited by 17 publications

References 5 publications

Relative bioavailability and pharmacokinetic study of two trimetazidine modified release formulations in healthy Bangladeshi male volunteers

Relative bioavailability and pharmacokinetic study of two trimetazidine modified release formulations in healthy Bangladeshi male volunteers

LC–MS/MS method for the determination of several drugs used in combined cardiovascular therapy in human plasma

Contact Info

Product

Resources

About