An updated overview with simple and practical approach for developing in vitro–in vivo correlation

Abstract

Preclinical Research & Development An in vitro-in vivo correlation (IVIVC) is as a predictive mathematical model that demonstrates a key role in the development, advancement, evaluation and optimization of extended release, modified release and immediate release pharmaceutical formulations. A validated IVIVC model can serve as a surrogate for bioequivalence studies and subsequently save time, effort and expenditure during pharmaceutical product development. This review discusses about different levels of correlations, general approaches to develop an IVIVC by mathematical modelling, validation, data analysis and various applications. In the current setting, the dearth of success associated with IVIVC is due to complexity of underlying scientific principles as well as the practice of fitting/matching in vivo plasma level-time data with in vitro dissolution profile. Hence, a simple, straightforward practical means to predict plasma drug levels by convolution technique and percentage drug absorbed computed from in vitro dissolution profile based on deconvolution method are illustrated. The bioavailability/bioequivalence assessment and evaluation are frequently validated by the pharmacokinetic parameters such as maximum concentration, time to reach maximum concentration, and area under the curve. The implementation of a quality by design manufacturing based on in vivo bioavailability and clinically relevant dissolution specification are recommended because corresponding design safe space will guarantee that all batches from relevant products are met with sufficient quality and bioperformance. Recently, United States Food and Drug Administration and European Medicines Agency have proposed that in silico/physiologically based pharmacokinetic modelling can be used in decision making during preclinical experiments as well as to recognize the dissolution profiles that can forecast and ensure the desired clinical performance.

In Vivo Predictive Dissolution (IPD) for Carbamazepine Formulations: Additional Evidence Regarding a Biopredictive Dissolution Medium

“…In accordance with these characteristics, its dissolution process is not affected by the transit to one intestinal segment to the next, and the dissolved amounts are absorbed at a similar rate in the different intestinal segments. In consequence, the challenges for the classical two-step IVIVC approach are minimal as long as the in vitro dissolution method reflects the in vivo dissolution process [37]. In this work, similar predictive performance was achieved with both mathematical approaches.…”

Experimental design, formulation and in vivo evaluation of a novel topical in situ gel system to treat ocular infections

“…Comparison of in vitro release between MH7 and commercial eye drops of moxifloxacin was accomplished by applying direct modelindependent mathematical method, the similarity factor (F 2 ). The calculated similarity factor value between MH7 and commercial eye drops was 16.94, proving that the both batches are dissimilar in terms of in vitro drug release profile according to the literature [41].…”

Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation

“…In vitro drug release studies are important to learn about the liberation of therapeutic actives from the film to the buccal mucosa and subsequent permeation through this biological membrane. The correlation among in vitro release data and in vivo absorption is also demonstrated [ 33 , 48 ]. Further, it is a well-known fact that drug delivery from a formulation is primarily dictated by the properties of the drugs and polymers [ 49 ].…”