In Vitro Dissolution Kinetics of Amlodipine Tablets Marketed in Russia Under Biowaiver Conditions

Шохин, И. Е.; Ramenskaya, G. V.; Василенко, Г. Ф.; Малашенко, Е. А.

doi:10.14227/dt170310p20

Cited by 16 publications

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“…However, the greatest IDR values were obtained when 0.1 M HCl was used as a dissolution medium, even causing the compressed material to loosen, regardless of the compaction pressure used (as observed in assays E3, E6 and E9). This behavior is due to the basic property of amlodipine besylate (pKa=8.7), indicating that it is much more soluble in an acidic medium (Shoin et al, 2010;van Zwieten, 1994).…”

Section: Resultsmentioning

confidence: 99%

The effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate of amlodipine besylate, using the rotating disk method

Giorgetti¹,

Issa²,

Ferraz³

2014

Braz. J. Pharm. Sci.

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The aim of this study was to evaluate the effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate (IDR) of the antihypertensive drug amlodipine besylate, using the rotating disk method. Accordingly, a fractional factorial design (3 3-1 ) was used, employing dissolution media (water, phosphate buffer pH 6.8 and HCl 0.1 M), rotation speed (50, 75 and 100 rpm), and compaction pressure (1000, 1500 and 2000 psi) as independent variables. The assays were randomized and statistically compared using the Statistica ® 11 software program. Significance testing (ANOVA) indicated that the dissolution medium had a considerable impact on the IDR of amlodipine besylate. Analysis of the linear and quadratic components of the variables led to the proposition of a mathematical model that describes the IDR as a function of the parameters studied. Conversely, the levels of compaction pressure and rotation speed employed during experimental planning were less relevant, especially when the assay was conducted in the HCl 0.1 M medium.Uniterms: Amlodipine besylate/intrinsic dissolution. Biopharmaceutical classification system. Drugs/ experimental design. Antihypertensive drugs/Amlodipine besylate.A finalidade do presente trabalho foi avaliar o efeito do meio de dissolução, velocidade de rotação e pressão de compactação na velocidade de dissolução intrínseca (VDI) do fármaco anti-hipertensivo besilato de anlodipino, usando o método do disco rotativo. Dessa forma, foi utilizado um planejamento experimental do tipo fatorial facionado (3 3-1 ) utilizando como variáveis independentes o meio de dissolução (água, HCl 0,1M e tampão fosfato pH 6,8), velocidade de rotação (50, 75 e 100 rpm) e pressão de compactação do fármaco (1000, 1500 e 2000 psi). Os ensaios foram randomizados e comparados estatisticamente pelo software Statistica ® 11. A análise de variância (ANOVA) indicou que o meio de dissolução exerce considerável impacto na VDI do besilato de anlodipino. A análise das variáveis em seus componentes lineares e quadráticos permitiu a proposição de um modelo matemático que descreve a VDI em função dos parâmetros estudados. Por outro lado, os níveis de pressão de compactação e velocidade de rotação empregados exercem efeito menos relevantes, especialmente quando o ensaio é conduzido em HCl 0,1 M. Unitermos:Besilato de anlodipino/dissolução intrínseca. Sistema de classificação biofarmacêutica. Fármacos/delineamento experimental. Fármacos/anti-hipertensivos/ Besilato de anlodipino.

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Section: Resultsmentioning

confidence: 99%

The effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate of amlodipine besylate, using the rotating disk method

Giorgetti¹,

Issa²,

Ferraz³

2014

Braz. J. Pharm. Sci.

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“…With regard to amlodipine, different studies have been performed to determine the release of amlodipine Besylate tablets using various dissolution conditions, and results are discordant. Thus, Shohin et al [13] evaluated the dissolution characteristics of the reference product and one product marketed in Russia, using 500 mL of USP buffer solutions at pH 1.2, 4.5 and 6.8 and apparatus 2 at 75 rpm. They found that the products dissolved very rapidly at pH 1.2 and 4.5, while at pH 6.8 they behaved as rapidly dissolving products and dissolution profiles were comparable.…”

Section: Discussionmentioning

confidence: 99%

“…With regard to its permeability, Caron et al [12] found that neutral amlodipine shows high permeability while cationic amlodipine does not permeate. In vivo studies have shown that although bioavailability is low (60 -65 %), its permeability could be considered high due to metabolite excretion in urine (90 -95 %) [13]. Moreover, the WHO guidance assigned amlodipine to BCS class 1 [4]; therefore, it has been considered as a candidate for a biowaiver through dissolution testing.…”

Section: Introductionmentioning

confidence: 99%

Comparative <i>in vitro</i> dissolution and <i>in vivo</i> bioavailability of commercial amlodipine tablets

Jung-Cook¹,

Mayet-Cruz²,

Girard-Cuesy³

2018

Trop. J. Pharm Res

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Purpose: To evaluate the in vivo and in vitro behavior of amlodipine immediate release products. Methods: Three Mexican amlodipine products and the innovator (Norvasc®) were evaluated. Three bioequivalence studies were performed in 24 healthy male and female volunteers each. Plasma concentrations were determined using a liquid chromatographic method coupled with tandem mass spectrometry (LC/MS/MS). Dissolution profiles were evaluated using USP type apparatus 2 at 75 rpm and 500 mL of HCl 0.1N, pH 4.5 and pH 6.8. Also, the dissolution behavior of different lots of the innovator product was evaluated using apparatus 1 or 2 and 900 mL of buffer pH 6.8. Results: All the generic products under study were bioequivalent to the innovator. In vitro data showed that although at pH 1.2 and 4.5, the products met the specifications for very rapidly dissolving products but at pH 6.8, neither the innovator nor the test products complied with the criteria for rapidly dissolving products. When the study was performed at pH 6.8 in 900 mL of medium, the innovator showed a rapid dissolution behavior. Conclusion: The results show that the use of WHO conditions (900 mL of media, apparatus 2 at 75 rpm) are more adequate to predict the in vivo behavior of the amlodipine products.

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“…Both evaluated drugs were "rapidly dissolving" [ Table 1] because the active pharmaceutical ingredient release at time point 30 min was >85%. [21][22][23][24][25] Table 1.…”

Section: If Both the Test And The Reference Dosage Forms Are Verymentioning

confidence: 99%

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Logoyda¹

2019

AJP

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Introduction: Biowaiver procedure, nowadays, is a trend of Modern Biopharmaceuticals. The biowaiver approach based on Biopharmaceutical Classification System BCS is intended to replace bioequivalence in vivo studies. Bisoprolol is a medicine most commonly used for heart diseases, the beta blocker family of medications, and is of the β 1-selective type. The Aim of the Study: The aim was to study the dissolution kinetics of bisoprolol tablets to assess their equivalence under conditions in vitro according to the biowaiver. Methods: The study of dissolution kinetics of drugs in the form of bisoprolol tablets has been carried out in accordance with the requirements of the "biowaiver" procedure, the recommendations of the SPhU, and the WHO requirements to assess the possibility of replacing the pharmacokinetic studies in vivo by tests in vitro. Results and Discussion: The possibility to use the recommendations of the "biowaiver" procedure for the registration of generics bisoprolol tablets has been found. The studies conducted have shown that bisoprolol can be referred to Class І of the BCS, i.e., substances with a high biopharmaceutical solubility and a high penetration rate. It will allow conducting comparative studies in vitro to confirm the equivalence of drugs. Conclusions: The evaluated bisoprolol drugs fulfill biowaiver criteria for drugs containing BCS Class I active pharmaceutical ingredients. Both drugs are "rapidly dissolving," both meet the criteria of dissolution profile similarity, f 2 (i.e., the dissolution profile of the test product is similar to that of the reference product in pH 1.2, 4.5, and 6.8 buffers using the paddle method at 75 rpm), and both are considered to be in vitro equivalent without in vivo evaluation.

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In Vitro Dissolution Kinetics of Amlodipine Tablets Marketed in Russia Under Biowaiver Conditions

Cited by 16 publications

References 0 publications

The effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate of amlodipine besylate, using the rotating disk method

The effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate of amlodipine besylate, using the rotating disk method

Comparative <i>in vitro</i> dissolution and <i>in vivo</i> bioavailability of commercial amlodipine tablets

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