Once daily nifedipine: the formulation dictates the pharmacokinetic characteristics and the therapeutic responses

Toal, Corey B.; Meredith, Peter A.; Elliott, Henry L.

doi:10.5414/cp201603

Cited by 12 publications

(11 citation statements)

References 55 publications

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“…The pharmacokinetics of NIF is highly influenced by its formulation. The first formulations of NIF were immediate-release (IR) soft gel capsules (SGC), followed by retarded action tablets and finally, extended-release osmotic pump tablets [2]. When the plasma concentration of NIF increases rapidly, e.g., by intravenous bolus injection or IR SGC, a rebound effect may occur, which is recognized by an increase in heart rate (29–38%) but little or no change in blood pressure [3,4,5,6].…”

Section: Introductionmentioning

confidence: 99%

Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate

Mantas

Mihranyan

2019

Pharmaceutics

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Nifedipine (NIF) is a 1,4-dihydropyridine-based calcium channel blocker with poor solubility, whose bioavailability is highly dependent on the type of formulation. Dry powder mixtures of 20% w/w NIF with microcrystalline cellulose (MCC) and its high surface area nanocellulose analogue, which is namely Cladophora (CLAD) cellulose, were produced by heating at the melting temperature of the drug for 1 h. Non-heated samples were used as a reference. The solid-state properties of the mixtures were characterized by scanning electron microscopy, differential scanning calorimetry and X-ray diffraction. The drug release was studied in biorelevant media, including simulated gastric fluid (SGF), fasted-state simulated intestinal fluid (FaSIF) and fed-state simulated intestinal fluid (FeSIF). An enhanced apparent solubility and faster dissolution rate of NIF were observed in the heated mixture of NIF with CLAD-H in all tested biorelevant media (i.e., SGF, FaSIF and FeSIF), which was due to NIF amorphization in the high surface area nanocellulose powder. Ordinary MCC, which is essentially non-porous, did not produce an enhancement of a similar magnitude. The results of the study suggest that dry powder formulation using high surface area nanocellulose is a facile new strategy for formulating calcium channel blocker drugs, which could potentially be a viable alternative to currently used soft gel liquid capsules.

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Section: Introductionmentioning

confidence: 99%

Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate

Mantas

Mihranyan

2019

Pharmaceutics

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“…When student's t-tests were used to analyze the two pharmacokinetic data, no significant differences in Cmax, MRT and AUC (0-24h) were found (P＞0.05). The relative oral bioavailability value from F1 in comparison with F2 was 97.12%, indicating bioequivalence that means the rate and extent of absorption of F1 prepared in this study do not show a significant difference from the rate and extent of absorption of the reference drug F2 when administered at the same drug dose under similar experimental conditions (Toal et al, 2012).…”

Section: In Vivo Pharmacokinetic Characterizationmentioning

confidence: 62%

Development and pharmacokinetic evaluation of once-daily sustained-released matrix capsules of nifedipine using solid dispersion technique

Zheng¹

2013

Afr. J. Pharm. Pharmacol.

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The purpose of this study was to develop once-daily sustained-release matrix capsules of nifedipine (F1) using the combination of solid dispersion and drug controlled release techniques. F1 were prepared by the wetting granules methods using hydroxypropyl methyl cellulose (HPMC) as hydrophilic retard drug release agent and ethylcellolulose (EC) ethanol solution based on the polyvinyl pyrrolidone / stearic acid solid dispersion. In vitro drug release kinetic model of F1 was fitted well with the zeroorder kinetic equation: Q=0.0736 t+0.0871 (R=0.993) in the range of 0-6 h, the first-order kinetic equation: Ln (1-Q) =-0.0934 t-0.1375 (R=0.999) in the range of 6-24 h, respectively. The relative bioavailability of F1 was studied in rabbits after oral administration using a commercial available controlled release tablet (F2) as a reference. The pharmacokinetic results showed no significant differences in Cmax, MRT and AUC (0-24h). The relative oral bioavailability value from F1 in comparison with F2 was 97.12 %. The results of both in vitro and in vivo studies indicated that once-daily sustainedrelease matrix capsules of NFD prepared by the optimized formulation exhibited excellent sustainedrelease effects and high relative oral bioavailability.

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“…In the class of dihydropyridine calcium channel blockers, amlodipine is a long‐acting compound because of its more than 50 hours of long half‐life time, and nifedipine gastrointestinal therapeutic system (GITS) uses a controlled‐release technique . Several previous studies compared the 24‐hour blood pressure–lowering effect of these two drugs, but produced inconsistent results .…”

Section: Introductionmentioning

confidence: 99%

A randomized controlled trial on the blood pressure–lowering effect of amlodipine and nifedipine‐GITS in sustained hypertension

Huang

Sheng

et al. 2019

J of Clinical Hypertension

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In a multicenter, randomized trial, we investigated whether the long half‐time dihydropyridine calcium channel blocker amlodipine was more efficacious than the gastrointestinal therapeutic system (GITS) formulation of nifedipine in lowering ambulatory blood pressure (BP) in sustained hypertension (clinic systolic/diastolic BP 140‐179/90‐109 mm Hg and 24‐hour systolic/diastolic BP ≥ 130/80 mm Hg). Eligible patients were randomly assigned to amlodipine 5‐10 mg/day or nifedipine‐GITS 30‐60 mg/day. Ambulatory BP monitoring was performed for 24 hours at baseline and 4‐week treatment and for 48 hours at 8‐week treatment with a dose of medication missed on the second day. After 8‐week treatment, BP was similarly reduced in the amlodipine (n = 257) and nifedipine‐GITS groups (n = 248) for both clinic and ambulatory (24‐hour systolic/diastolic BP 10.3/6.5 vs 10.9/6.3 mm Hg, P ≥ 0.24) measurements. However, after missing a dose of medication, ambulatory BP reductions were greater in the amlodipine than nifedipine‐GITS group, with a significant (P ≤ 0.04) between‐group difference in 24‐hour (–1.2 mm Hg) and daytime diastolic BP (–1.5 mm Hg). In conclusion, amlodipine and nifedipine‐GITS were efficacious in reducing 24‐hour BP. When a dose of medication was missed, amlodipine became more efficacious than nifedipine‐GITS.

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Once daily nifedipine: the formulation dictates the pharmacokinetic characteristics and the therapeutic responses

Cited by 12 publications

References 55 publications

Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate

Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate

Development and pharmacokinetic evaluation of once-daily sustained-released matrix capsules of nifedipine using solid dispersion technique

A randomized controlled trial on the blood pressure–lowering effect of amlodipine and nifedipine‐GITS in sustained hypertension

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