Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Nifedipine

Gajendran, Jayachandar; Krämer, Johannes; Shah, Vinod P.; Langguth, Peter; Polli, James E.; Mehta, Mehul; Groot, D.W.; Cristofoletti, Rodrigo; Abrahamsson, Bertil; Dressman, Jennifer B.

doi:10.1002/jps.24560

Cited by 32 publications

(27 citation statements)

References 45 publications

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“…Nifedipine was chosen to represent BCS class II. A Biowaiver monograph of nifedipine has recently been published by Gajendran et al . Because of low solubility and high permeability, absorption of a BCS class II drug is often limited by dissolution of the drug particles, which in turn can lead to slower absorption than for a BCS class I compound .…”

Section: Methodsmentioning

confidence: 99%

“…[7] Nifedipine was chosen to represent BCS class II. A Biowaiver monograph of nifedipine has recently been published by Gajendran et al [8] Because of low solubility and high permeability, absorption of a BCS class II drug is often limited by dissolution of the drug particles, which in turn can lead to slower absorption than for a BCS class I compound. [17] The example chosen, nifedipine, can be administered in an oily solution housed in a soft gelatine capsule to circumvent dissolution-based limitations to absorption.…”

Section: Absorption Modelsmentioning

confidence: 99%

See 1 more Smart Citation

Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models

Hansmann

Darwich

Margolskee

et al. 2016

Journal of Pharmacy and Pharmacology

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Section: Methodsmentioning

confidence: 99%

Section: Absorption Modelsmentioning

confidence: 99%

Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models

Hansmann

Darwich

Margolskee

et al. 2016

Journal of Pharmacy and Pharmacology

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“…The bioavailability of nifedipine IR ranges from 42% to 56% due to its wide and variable pre‐systemic and first‐pass metabolism. In addition, food intake can affect the time required for nifedipine IR to reach its maximum concentration in plasma . In the osmotic push–pull system formulation, drug absorption is not affected by food intake or gastrointestinal pH value .…”

Section: Discussionmentioning

confidence: 99%

Comparison of the efficacy of the immediate‐release and osmotic push–pull system formulations of nifedipine for tocolysis

İnan

Sayın

Dolgun

et al. 2019

J of Obstet and Gynaecol

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Aim: To compare the immediate-release (IR) and osmotic push-pull system formulations of nifedipine used for tocolysis in prolonging pregnancy, neonatal outcomes and maternal-fetal adverse effects. Methods: We evaluated 140 pregnant women who received the IR (n = 72) and osmotic push-pull system (n = 68) formulations of nifedipine for tocolysis due to threatened preterm labor between 24 0/7 and 33 6/7 weeks of gestation. Groups were compared in terms of efficacy of tocolysis in prolonging pregnancy for more than 48 h, 7 days and up to 37 weeks of gestation, total number of days gained for prolonging pregnancy, delivery weeks, maternal-fetal adverse effects and neonatal outcomes including ventilation support, need for intubation or surfactant, intraventricular hemorrhage, respiratory distress syndrome, necrotizing enterocolitis, admission to neonatal intensive care unit, neonatal death, Apgar scores at the 1st and 5th minutes.Results: There was no significant difference between the two groups in prolonging pregnancy for more than 48 h or 7 days, total number of days gained after tocolysis initiation, delivery weeks, the number of births at 34 0/7 -36 6/7 weeks or after 37 weeks of gestation (P > 0.05). Maternal-fetal adverse effects and neonatal outcomes were similar in both groups (P > 0.05). Conclusion: The efficacy of IR and osmotic push-pull system formulations of nifedipine have similar effects in terms of tocolysis and neonatal outcomes, adverse effects. Osmotic push-pull system formulation of nifedipine may be an alternative medication in tocolytic therapy due to its ease of use and the absence of loading dose necessity.

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“…3 It undergoes extensive presystemic metabolism and exhibits highly variable pharmacokinetics. 4 Nifedipine is available as immediate-release (IR) tablet and soft gelatin capsule (SGC) formulations and as extended-release tablets. In some countries, SGCs are the only solid oral IR nifedipine formulations available.…”

Section: Introductionmentioning

confidence: 99%

“…Despite the drug being presented to GI fluids in the solubilized form, the bioavailability of nifedipine from SGCs ranges from 31% to 81%. 4 In a study on 14 pregnant women, dosecorrected C max ranged from 41 to 397 mg/mL with the IR SGC. 5 The aims of our present in vitro study are to try and understand the reasons behind this variability and how it can be minimized.…”

Section: Introductionmentioning

confidence: 99%

A Simulated Stomach Duodenum Model Predicting the Effect of Fluid Volume and Prandial Gastric Flow Patterns on Nifedipine Pharmacokinetics From Cosolvent-Based Capsules

Honigford

Aburub

Fadda

2019

Journal of Pharmaceutical Sciences

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Nifedipine is a Biopharmaceutics Classification System class II drug displaying large variability in absorption even when administered as immediate-release soft gelatin capsules of a cosolvent formulation. This in vitro study sought to understand the reasons behind variability in nifedipine absorption, how it can be minimized, and if it can be predicted using in vitro models. A dynamic in vitro simulated stomach duodenum model was used to explore drug concentration-time profiles of nifedipine soft gelatin capsules under conditions simulating how patients take their medicines. Specifically, the effect of prandial gastric emptying patterns and fluid volume administration (250 mL vs. 50 mL water) were investigated. Significant supersaturation of nifedipine was observed. While administration of large and small water volumes gave rise to a similar C and area under the curve (AUC), the coefficient of variation in AUC was 4.8% and 49%, respectively, which can be attributed to differences in precipitation kinetics. Fasting and fed gastric emptying patterns also gave rise to a similar AUC; however, C was significantly lower in the fed state. These trends are consistent with previously published in vivo results in healthy volunteers. The simulated stomach duodenum provides a good discriminative screening tool for predicting trends in drug concentration profiles of Biopharmaceutics Classification System class II drugs.

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Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Nifedipine

Cited by 32 publications

References 45 publications

Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models

Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models

Comparison of the efficacy of the immediate‐release and osmotic push–pull system formulations of nifedipine for tocolysis

A Simulated Stomach Duodenum Model Predicting the Effect of Fluid Volume and Prandial Gastric Flow Patterns on Nifedipine Pharmacokinetics From Cosolvent-Based Capsules

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