Use of IVIVC to Optimize Generic Development

Cardot, J; Garrait, G.; Beyssac, Eric

doi:10.14227/dt220215p44

Cited by 11 publications

(4 citation statements)

References 10 publications

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“…For class II drugs an IVIVC is expected if in vitro dissolution rate is like in vivo dissolution rate, unless dose is very high [26]. Some authors have been discussed the use of IVIVC to optimize the development of generic drug formulations [27,28].…”

Section: Prediction Of Smz and Tmp Plasma Levelsmentioning

confidence: 99%

Prediction of Sulfamethoxazole and Trimethoprim Plasma Levels From Tablets and Dissolution Media of Physiological Relevance

RIOS-RODRIGUEZ,

REYES-RAMIREZ,

RUIZ-SEGURA

et al. 2024

Int J App Pharm

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Objective: To estimate plasma concentrations-time profiles of Sulfamethoxazole (SMZ) and Trimethoprim (TMP) from fixed-dose combination formulations through in vitro data of dissolution media of physiological relevance and a convolution model. Methods: Dissolution profiles of SMZ/TMP tablets (400/80 mg) were obtained with USP paddle apparatus at 100 rpm and 900 ml of 0.1 N HCl, pH 4.5 acetate buffer, and pH 6.8 phosphate buffer. The reference drug product and two generic formulations were tested. Drugs were quantified by a derivative method. Dissolution profiles were compared with model-dependent and independent methods. SMZ/TMP plasma levels were simulated with dissolution data and published in vivo information. Percent of prediction error (PE) for peak plasma concentration (Cmax) and area under the curve from zero time to infinity (AUC0-inf) at each condition were calculated. Results: In all used conditions, similar dissolution profiles were found excepting for TMP at pH 1.2 (f2<50). The in vitro release performance for reference and generic formulations was explained by the Weibull function only for SMZ at pH 6.8 and TMP at pH 4.5. Values of PE>19% for both generic formulations were found with TMP at pH 1.2. Conclusion: Significant differences in TMP dissolution profiles of generic formulations at pH 1.2 reflect the subsequent differences found in predicted Cmax and AUC0-inf.

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Section: Prediction Of Smz and Tmp Plasma Levelsmentioning

confidence: 99%

Prediction of Sulfamethoxazole and Trimethoprim Plasma Levels From Tablets and Dissolution Media of Physiological Relevance

RIOS-RODRIGUEZ,

REYES-RAMIREZ,

RUIZ-SEGURA

et al. 2024

Int J App Pharm

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“…Bioavailability and bioequivalence (BE) are often used in generic drug evaluation, new dosage form development, quality control, and manufacturing changes. Since clinical trials are costly, time-consuming, and risky, Food and Drug Administration (FDA) and other counterparties have been working to establish reliable in vitro–in vivo correlation (IVIVC) evaluation methods to guide or even replace clinical trials. − The prescription and preparation processes determine the formulation structure, which further affects drug release and bioavailability. The correlation between the in vitro structure of the formulation and drug release has been studied by several researchers.…”

Section: Evaluation Of Structure-oriented Ddssmentioning

confidence: 99%

Advances in Structure Pharmaceutics from Discovery to Evaluation and Design

Xue

et al. 2023

Mol. Pharmaceutics

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Drug delivery systems (DDSs) play an important role in delivering active pharmaceutical ingredients (APIs) to targeted sites with a predesigned release pattern. The chemical and biological properties of APIs and excipients have been extensively studied for their contribution to DDS quality and effectiveness; however, the structural characteristics of DDSs have not been adequately explored. Structure pharmaceutics involves the study of the structure of DDSs, especially the three-dimensional (3D) structures, and its interaction with the physiological and pathological structure of organisms, possibly influencing their release kinetics and targeting abilities. A systematic overview of the structures of a variety of dosage forms, such as tablets, granules, pellets, microspheres, powders, and nanoparticles, is presented. Moreover, the influence of structures on the release and targeting capability of DDSs has also been discussed, especially the in vitro and in vivo release correlation and the structure-based organ- and tumor-targeting capabilities of particles with different structures. Additionally, an in-depth discussion is provided regarding the application of structural strategies in the DDSs design and evaluation. Furthermore, some of the most frequently used characterization techniques in structure pharmaceutics are briefly described along with their potential future applications.

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“…Couple of other publications compared bioequivalence guidelines similarities among various regulatory agencies. In another related area, in vitro in vivo correlation (IVIVC), even though couple of articles addressed importance of IVIVC in generic drug development, no comparison of guidelines was found (Cardot et al, 2015;Kaur et al, 2015). In the area of in silico PBPK modeling and simulations, both EMA and USFDA have come up with recent guidelines in 2018 and 2020, respectively.…”

Section: Introductionmentioning

confidence: 99%

In vitro and In silico biopharmaceutic regulatory guidelines for generic bioequivalence for oral products: Comparison among various regulatory agencies

Kollipara

Ahmed

Bhattiprolu

et al. 2021

Biopharm & Drug Disp

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Generic drug development is a complex process that involves development of formulation similar to reference product. Because of the complexity associated with generic drug development, many regulatory agencies have come up with various guidelines. Out of many guidelines, the biopharmaceutics classification system that was introduced in 1995 based on aqueous solubility and permeability helped many pharmaceutical scientists across the globe to utilize the tool for formulation development, waiver of in vivo studies. Later on in vitro guidelines based on dissolution and in vitro in vivo correlation were introduced by many regulatory agencies with an intent to reduce number of in vivo human testing thereby facilitating shorter development time and faster approvals and launch. Most recently, understanding the importance in silico approaches such as physiologically based pharmacokinetic modelling, regulatory agencies such as United States Food and Drug Administration (USFDA) and European Middle East and Africa (EMA) came up with modelling guidance documents. Even though consensus exists between guidance documents from various regulatory agencies, still there are many minor to major differences exists between these guidance documents that needs to be considered while submitting a generic drug application. This review aims to compare all the in vitro and in silico guidance documents from major regulatory agencies with emphasis on latest trends and technologies combined with regulatory acceptability with an intention to harmonize regulations. Guidance documents from major regulatory agencies such as USFDA, EMA, World Health Organization, International Council for Harmonization and other emerging markets were compared. Similarities &differences among these guidance documents are critically reviewed to provide the reader a detailed overview of these guidance documents at one place.

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Use of IVIVC to Optimize Generic Development

Cited by 11 publications

References 10 publications

Prediction of Sulfamethoxazole and Trimethoprim Plasma Levels From Tablets and Dissolution Media of Physiological Relevance

Prediction of Sulfamethoxazole and Trimethoprim Plasma Levels From Tablets and Dissolution Media of Physiological Relevance

Advances in Structure Pharmaceutics from Discovery to Evaluation and Design

In vitro and In silico biopharmaceutic regulatory guidelines for generic bioequivalence for oral products: Comparison among various regulatory agencies

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