In-vitro and in-vivo correlation for two gliclazide extended-release tablets

Mandal, Uttam Kumar; Ray, Kamala Kanta; Gowda, Veeran; Ghosh, Animesh; Pal, Tapan Kumar

doi:10.1211/jpp.59.7.0009

Cited by 16 publications

(9 citation statements)

References 13 publications

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“…The highest R 2 using USP 1 and 2 was observed in HCl (pH 1.2) media at 100 rpm (R 2 =0.8906), which agrees with previous studies for GLZ with USP2. 5,28) All correlation coefficients obtained in our study using USP1 and USP2 were far below the recommended level according to FDA. 22) In addition to the observed blockage in the baskets (USP1) and the coning effect with the paddles (USP2) during the dissolution tests, the use of a single dissolution media most likely is not Table 2) A USP3 was used with 250 mL of media at 37°C, 30 dpm and 400 µm mesh.…”

Section: Resultsmentioning

confidence: 53%

“…MR gliclazide tablets has approximately 100% of bioavailability, linear pharmacokinetics and one compartment model, 3,28) see Fig. 1A.…”

Section: Resultsmentioning

confidence: 99%

“…20) Considering that the low solubility of GLZ can be the rate limiting step for its dissolution and absorption, a prediction of its in vivo behavior based on a dissolution test using biorelevant media should lead to a more relevant IVIVC. 17,27) The literature describes an IVIVC for GLZ-MR tablets using USP apparatus 2 28) and suggests the possible application of USP apparatus 3 to GLZ MR tablets. 29) Here, we have utilized a USP apparatus 3 to evaluate different dissolution parameters to develop a methodology for GLZ MR tablets and, based on IVIVC, we report a dissolution method that demonstrates high correlation with a potential use in further studies on GLZ formulations and quality control.…”

mentioning

confidence: 99%

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Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with in Vitro–in Vivo Correlation

et al. 2018

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Gliclazide (GLZ) is a second generation hypoglycemic drug used for the treatment of Type 2 diabetes mellitus. The low solubility of GLZ has been described as the rate limiting step for drug dissolution and absorption, thus a prediction of its in vivo behavior based on a discriminative dissolution test should lead to a relevant in vitro-in vivo correlation (IVIVC). The aim of this study was to develop a dissolution method for GLZ modified-release (MR) tablets using an United States Pharmacopeia (USP) apparatus 3 through its evaluation by an IVIVC analysis. Various dissolution parameters were evaluated to establish an in vitro method for GLZ tablets. The final dissolution conditions, referred to as method 3, utilized a 400 µm mesh and 30 dips per minute over a total period of 10 h that included 1h in HCl media (pH 1.2), 2h in acetate buffer solution (pH 4.5), 1 h in phosphate buffer solution (PBS; pH 5.8), 5h in PBS (pH 6.8) and finally 1h in PBS (pH 7.2). The calculated point-to-point IVIVC (R 2 0.9970) was significantly greater than other methods. The robustness of method 3 suggests it could be applied to pharmaceutical equivalence studies and for quality control analyses of GLZ.

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Section: Resultsmentioning

confidence: 53%

“…MR gliclazide tablets has approximately 100% of bioavailability, linear pharmacokinetics and one compartment model, 3,28) see Fig. 1A.…”

Section: Resultsmentioning

confidence: 99%

mentioning

confidence: 99%

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Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with in Vitro–in Vivo Correlation

et al. 2018

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“…9 Various IVIVC studies have been published for a number of formulations, including Busprion, propranolol, nevirapine, metoprolol and other drugs. [6][7][8][9][10][11][12][13][14][15][16][17] The concepts and methods used in establishing the IVIVC are reviewed elsewhere. 4,5 According to BCS classification naproxen sodium comes under class 2 drug and in addition naproxen is relatively having a short life suggest suitable applicant for modified release formulation.…”

Section: Introductionmentioning

confidence: 99%

Development, Internal and External Validation of Naproxen Sodium Sustained Release Formulation: an Level A In Vitro-In Vivo Correlation

Narayanasamy¹,

Shabaraya²

2017

tjps

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Amaç: Bu çalışmanın amacı, naproksen sodyumun sürekli salım tableti için in vitro-in vivo korelasyon (IVIVC) geliştirmek, doğrulamak ve zamana bağlı plazma konsantrasyonlarını derhal salınan tabletle karşılaştırmaktır. Gereç ve Yöntemler: İn vitro salım hızı verileri, pH 7.4 fosfat tampon içinde 50 dev/dakikada, USP Apparatus II, palet karıştırıcısı kullanılarak her bir tablet için elde edilmiştir. Naproksen sodium 375 mg sürekli salım ve 500 mg derhal salım tabletleri 6 sağlıklı kişiye uygulanarak dört yönlü bir çaprazlama çalışması gerçekleştirilmiştir. Yirmi dört saat boyunca toplanan kan örnekleri valide edilmiş sıvı kromatografisi tandem-kütle spektrometresi yöntemi kullanılarak tayin edilmiştir. Bulgular: Hesaplanan ve 50-100 arasında bulunan değerler benzerlik faktörlerini göstermektedir. C max ve AUC ortalama değerlerine yakın bulunmuştur. Tahmin edilen ve gözlemlenen biyoyararlanım değerlendirmesi yapıldı ve Gıda İlaç İdaresi yönetmeliklerine göre % tahmin hataları (PE) hesaplandı; iç tahmin ile IVIVC'nin oluşturulması için C max 'ın ortalama mutlak %PE'si ve formülasyonun bireysel formülasyonun AUC'si %15'in altında bulundu, naproksen sodyumun IVIVC modelleri geçerlidir. Dış validasyon sırasında, naproksen sodyumun sürekli salım tableti için öngörülen eğri, derhal salım tableti ile aynı bulunması geçerli olduğunu göstermektedir. Sonuç: Bu IVIVC, in vivo biyoyararlanım araştırması için vekil olarak hizmet edebilir ve biyolojik yönlendiricileri destekler, çözünme yöntemlerini ve spesifikasyon ayarlarını destekler ve onaylar, ölçek büyütme ve onay sonrası değişiklikler sırasında kalite kontrolünde yardımcı olur. Yer değişikliği, proses değişiklikleri ve farklı emisyon oranlarına sahip naproksen sodyum ürünlerinin emme performansını tahmin etmek için kullanılabilir. Anahtar kelimeler: IVIVC, naproksen sodyum, sürekli salım, çözünme, in vivo biyoyararlanım çalışması, iç ve dış öngörülebilirlik Objectives:The aim of the present study was to develop and validate an in vitro-in vivo correlation (IVIVC) for naproxen sodium-sustained release tablets and to compare their plasma concentrations over time with the immediate-release tablets. Materials and Methods:In vitro release rate data were obtained for each tablet by using the USP Apparatus II, paddle stirrer at 50 rpm in pH 7.4 phosphate buffer. A four-way crossover study was conducted in 6 healthy subjects by administering naproxen sodium sustained release 375 mg and 500 mg of immediate release tablets. Series of blood samples were collected over 24 hours and estimated by using the validated liquid chromatography tandem-mass spectrometry method. Results: The similarity factor was calculated and it was found that values between, 50 and 100 indicates similarity of the profiles. Assessment of predicted and observed bioavailability was performed and prediction errors (PE) % calculated, as per the Food Drug Administration guidelines, the average absolute PE% of C max and AUC of individual formulation was found below 15% for establishment of IVIVC, based on ...

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“…6 Numerous investigations have been undertaken to develop In vitro in vivo correlation models, a level A correlation utilize the complete time course of in vitro dissolution and in vivo input and recognized model of choice for achieve biowaivers or setting of dissolution specifications. [7][8][9][10][11][12][13][14][15][16] However, level B and C models may be used in the initial stages of formulation development to inspect level A In vitro in vivo correlation models shall be used. 6 The present work aim was to develop and establish the internal and external predictability of level A In vitro in vivo correlation models for the three Metoclopramide sustained release and one immediate release formulation were evaluated.…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of Internal and External Predictability of Metoclopramide Hydrochloride Modified Release Formulations: An Establishment of Level A In vitro and In vivo Correlation

Narayanasamy¹,

Shabaraya²

2017

IJPER

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The objective of this study was to develop an in vitro-in vivo correlation (IVIVC) model for hydrophilic matrix sustained-release (SR) Metoclopramide formulations. The in vitro release characteristics of the drug were determined using USP apparatus II at 50 rpm, pH 6.8. In vivo plasma concentrations and pharmacokinetic parameters in healthy human subjects were obtained after administering oral dose, developed SR formulations and marketed immediate-release (IR) products. The similarity factor f2 was used to compare the dissolution data. The IVIVC model was developed using pooled fraction dissolved and fraction absorbed of developed SR formulations i.e. fast, medium and slow release and marketed immediate-release (IR) products. An in vitro-in vivo correlation (IVIVC) was established for sustained release tablet by deconvolution using data from an immediate-release treatment as the characteristic response. To assess the correlation between in vitro dissolution uniqueness and in vivo absorption performance of Metoclopramide sustained release (SR) and immediate release (IR) tablet in human subjects. The established IVIVC was evaluated internally by predicting data used to develop and externally by predicting data not originally included in developing the IVIVC model. The observed low prediction errors for Cmax and AUC demonstrated that the Metoclopramide IVIVC model was valid.

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In-vitro and in-vivo correlation for two gliclazide extended-release tablets

Cited by 16 publications

References 13 publications

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Development, Internal and External Validation of Naproxen Sodium Sustained Release Formulation: an Level A <i>In Vitro-In Vivo</i> Correlation

Development and Evaluation of Internal and External Predictability of Metoclopramide Hydrochloride Modified Release Formulations: An Establishment of Level A In vitro and In vivo Correlation

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