A Review on IVIVC in The Development of Oral Drug Formulation: Data Obtained from Past Two Decades

Sirisha, S.

doi:10.5958/0975-4377.2020.00034.8

Cited by 5 publications

(3 citation statements)

References 0 publications

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“…An information summary of the treatment groups composing the clinical studies is reported in Table 2. For the PK analysis, serum progesterone was measured at 0.5, 1, 2, 3, 4, 6,8,12,18,24,36,48,72,96,120,144,168,216,264,312,380, and 408 h post-dosing. Serum progesterone levels were measured using an IMMUNLITE 2000 automated system (Siemens Medical solutions Diagnostics), based on a solid-phase-competitive chemiluminescent immunoassay assay.…”

Section: In Vitro Release Datamentioning

confidence: 99%

“…This guideline, in agreement with most of the older literature, presented the so-called deconvolution- and convolution-based methods as the standard IVIVC technique [ 4 , 5 ], although the development of alternative approaches was encouraged. Since then, the establishment and application of IVIVC have increased and various alternatives to the conventional IVIVC approaches have been introduced [ 2 , 6 , 7 , 8 ]. In few but extremely relevant examples, the IVIVC was developed using nonlinear mixed-effect models [ 9 ] or physiologically based pharmacokinetic (PBPK) models [ 10 , 11 , 12 ], in the latter cases frequently implemented in closed software such as GastroPlus TM .…”

Section: Introductionmentioning

confidence: 99%

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In Vitro–In Vivo Correlation (IVIVC) Population Modeling for the In Silico Bioequivalence of a Long-Acting Release Formulation of Progesterone

Tosca

Rocchetti

Pérez³

et al. 2021

Pharmaceutics

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Health authorities carefully evaluate any change in the batch manufacturing process of a drug before and after regulatory approval. In the absence of an adequate in vitro–in vivo correlation (Level A IVIVC), an in vivo bioequivalence (BE) study is frequently required, increasing the cost and time of drug development. This study focused on developing a Level A IVIVC for progesterone vaginal rings (PVRs), a dosage form designed for the continuous delivery in vivo. The pharmacokinetics (PK) of four batches of rings charged with 125, 375, 750 and 1500 mg of progesterone and characterized by different in vitro release rates were evaluated in two clinical studies. In vivo serum concentrations and in vitro release profiles were used to develop a population IVIVC progesterone ring (P-ring) model through a direct differential-equation-based method and a nonlinear-mixed-effect approach. The in vivo release, was predicted from the in vitro profile through a nonlinear relationship. was used as the input of a compartmental PK model describing the in vivo serum concentration dynamics of progesterone. The proposed IVIVC P-ring model was able to correctly predict the in vivo concentration–time profiles of progesterone starting from the in vitro PVR release profiles. Its internal and external predictability was carefully evaluated considering the FDA acceptance criteria for IVIVC assessment of extended-release oral drugs. Obtained results justified the use of the in vitro release testing in lieu of clinical studies for the BE assessment of any new PVRs batches. Finally, the possible use of the developed population IVIVC model as a simulator of virtual BE trials was explored through a case study.

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Section: In Vitro Release Datamentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

In Vitro–In Vivo Correlation (IVIVC) Population Modeling for the In Silico Bioequivalence of a Long-Acting Release Formulation of Progesterone

Tosca

Rocchetti

Pérez³

et al. 2021

Pharmaceutics

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“…The latest article in the field of IVIVC applicability was published in 2020 that summarizes the data obtained from past decade. As a part of this study, many literature examples were identified in the domain of IVIVC indicating the significant research that has been put into this field, however it is also important to translate this research knowledge into industrial or practical knowledge (Sirisha, 2020). In this context, understanding the regulatory requirement for IVIVC becomes paramount importance.…”

Section: Ivivc Guidelines Comparisonmentioning

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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Improve Bioequivalence predictions with PAMPA Dissolution using Etoricoxib and five other Drug Formulations

Chou,

Lai,

Chou

et al. 2023

RJPDFT

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In the generic drug formulation development, pilot bioequivalence (BE) study with a small group of subjects is the current practice for oral formulation prediction. However, due to the difficulty in differentiating the variation between subject and drug formulation with the current BE practice，a new instrument called PAMPA Dissolution is proposed to eliminate the subjects variation and to enhance the correlation between in vitro to in vivo absorption in BE study. PAMPA Dissolution simultaneously measures drug dissolution (Cb) and permeation (Pe), following the validated oral drug absorption equation F (drug absorbed) = Cb*Pe*Area. The use of biorelevant media further allows this device to mimic in vivo conditions closely. Formulations of 60 mg etoricoxib tablets were studied to verify system reproducibility and BE prediction to demonstrate the potential of PAMPA Dissolution in generic drug development. The BE predictions between generic and brand etoricoxib tablets (test/reference) from this system produced a Cmax value of 99.0% and AUC value of 99.1%, indicating that PAMPA Dissolution predictions conform with bioequivalence results. Other oral formulations of valsartan/hydrochlorothiazide, ezetimibe, telmisartan, and amlodipine were also tested for their permeation (Pe) by PAMPA Dissolution. Results of drug permeation compared to the literature values indicates that the PAMPA Dissolution is reliable and precise in formulation development.

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A Review on IVIVC in The Development of Oral Drug Formulation: Data Obtained from Past Two Decades

Cited by 5 publications

References 0 publications

In Vitro–In Vivo Correlation (IVIVC) Population Modeling for the In Silico Bioequivalence of a Long-Acting Release Formulation of Progesterone

In Vitro–In Vivo Correlation (IVIVC) Population Modeling for the In Silico Bioequivalence of a Long-Acting Release Formulation of Progesterone

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

Improve Bioequivalence predictions with PAMPA Dissolution using Etoricoxib and five other Drug Formulations

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