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

Abstract

Aim: The aim of this study was to develop an in-vitro-in-vivo correlation (IVIVC) for two ibuprofen (IF) and extended release (ER) formulations and to compare their plasma concentrations. Materials and Methods: In vitro release rate data were obtained for each formulation using the USP apparatus 2, paddle stirrer at 100 rpm in pH 6.8 phosphate buffer. In vitro samples were analyzed using high performance liquid chromatography (HPLC) with ultraviolet detection, and in vivo samples were analyzed using a HPLC assay an additional model dependent approaches for different types of release rate of IF was prepared for evaluating the external predictability. Results and Discussion: A Higuchi model optimally fits the in vitro data. The similarity factor (f 2) was used to analyze the dissolution data. In vivo plasma concentrations and pharmacokinetic parameters in New Zealand rabbits were obtained after administering oral, Poly-β-hydroxybutyrate, and hydroxypropyl methylcellulose base ER formulations. A linear correlation model was developed using percent absorbed data and percent dissolved data from the two formulations. Conclusion: Linear regression analyses of the mean percentage of dose absorbed versus the mean in vitro release resulted in a significant correlation (r 2 >0.95) for the two formulations.

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

“…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.…”

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

“…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.…”

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

“…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.…”

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

“…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.…”