Considerations for the development of in vitro dissolution tests to reduce or replace preclinical oral absorption studies

Grignard, Elise; Taylor, Robert W.; McAllister, Mark; Box, Karl; Fotaki, Nikoletta

doi:10.1016/j.ejps.2016.12.004

Cited by 24 publications

(9 citation statements)

References 59 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…[37][38][39][40] Dose concentrations (1 mg/mL in the stomach and 0.5 mg/mL in the intestine) were chosen based on average gastric and intestinal volumes in dogs and an estimate of the rate-determining steps to absorption in the intestinal compartment. 37,41,42 The SGF portion of the SGF/SIF dissolution test represented a nonsink condition for all SDDs, whereas the SIF portion of the test represented near-sink conditions, with a potential for up to 40% of the saturation solubility reached for HPMCAS-M and PVP K30 SDDs and 100% saturation solubility reached for the PVP VA64 SDD (based on data from the solventshift UV assay, Table 2). Sink conditions in the SIF portion of the dissolution test are consistent with the estimation of dissolutionrate-limited performance of these SDDs in the upper small intestine of fasted dogs according to the Fraction Absorbed Classification System.…”

Section: Selection Of Dissolution Methodology and Parametersmentioning

confidence: 99%

Mechanistic Study of Belinostat Oral Absorption From Spray-Dried Dispersions

Stewart¹,

Yates

Mudie³

et al. 2019

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Section: Selection Of Dissolution Methodology and Parametersmentioning

confidence: 99%

Mechanistic Study of Belinostat Oral Absorption From Spray-Dried Dispersions

Stewart¹,

Yates

Mudie³

et al. 2019

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…The first step to characterise the dissolution and solubility behaviour of a drug is reliable and appropriate in vitro models . The selection of the media is a crucial step, and bio‐relevant media simulating the human's gastrointestinal conditions is a useful tool to get a first impression of the dissolution properties of a drug .…”

Section: Role Of In Vitro and In Silico Models For Predicting The Suimentioning

confidence: 99%

The pig as a preclinical model for predicting oral bioavailability and in vivo performance of pharmaceutical oral dosage forms: a PEARRL review

Henze

Koehl

O’Shea

et al. 2018

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

Objectives In pharmaceutical drug development, preclinical tests in animal models are essential to demonstrate whether the new drug is orally bioavailable and to gain a first insight into in vivo pharmacokinetic parameters that can subsequently be used to predict human values. Despite significant advances in the development of bio-predictive in vitro models and increasing ethical expectations for reducing the number of animals used for research purposes, there is still a need for appropriately selected pre-clinical in vivo testing to provide guidance on the decision to progress to testing in humans. The selection of the appropriate animal models is essential both to maximise the learning that can be obtained from such experiments and to avoid unnecessary testing in a range of species. Key findings The present review, provides an insight into the suitability of the pig model for predicting oral bioavailability in humans, by comparing the conditions in the GIT. It also contains a comparison between the bioavailability of compounds dosed to both humans and pigs, to provide an insight into the relative correlation and examples on why a lack of correlation may be observed. Summary While there is a general trend towards predicting human bioavailability from pig data, there is considerable variability in the data set, most likely reflecting species specific differences in individual drug metabolism. Nonetheless, the correlation between pigs vs. humans was comparable to that reported for dogs vs. humans. The presented data demonstrate the suitability of the pig as a preclinical model to predict bioavailability in human.

show abstract

“…Dissolution testing is a critical tool both during new drug development and for quality control testing of commercial formulations during production [4][5][6]. From an analytical chemistry point of view, dissolution testing produces a large amount of samples, particularly when time based dissolution profiles have to be created.…”

Section: Introductionmentioning

confidence: 99%

Development and Validation of an Automated Zone Fluidics-Based Sensor for In Vitro Dissolution Studies of Captopril Using Total Error Concept

Karakosta¹,

Tzanavaras

Zacharis

2021

Molecules

View full text Add to dashboard Cite

In the present research, a zone fluidics-based automated sensor for the analysis of captopril in in vitro dissolution samples is reported. Captopril is reacted under flow conditions with Ni(II) (10 mmol L−1) in alkaline medium (0.15 % v/v NH3) to form a stable derivate, which is monitored spectrophotometrically at 340 nm. The chemical and instrumental parameters were carefully investigated and optimized. The validation of the developed method was performed in the range of 5 to 120% of the expected maximum concentration using the accuracy profiles as a graphical decision-making tool. The β-expectation tolerance intervals did not exceed the acceptance criteria of ±10%, which means that 95% of future results will be encompassed in the defined bias limits. The variation of the relative bias ranged between −2.3% and 3.5% and the RSD values for repeatability and intermediate precision were lower than 2.3% in all cases. The limit of detection (LOD), and the lower and the upper limit of quantification (LLOQ, ULOQ) were satisfactory and found to be 1%, 5% and 120% (corresponding to 0.6, 2.78 and 66.67 μg mL−1 in dissolution medium). The developed method was successfully applied for the analysis of captopril in dissolution tests of two commercially available batches.

show abstract

Considerations for the development of in vitro dissolution tests to reduce or replace preclinical oral absorption studies

Cited by 24 publications

References 59 publications

Mechanistic Study of Belinostat Oral Absorption From Spray-Dried Dispersions

Mechanistic Study of Belinostat Oral Absorption From Spray-Dried Dispersions

The pig as a preclinical model for predicting oral bioavailability and in vivo performance of pharmaceutical oral dosage forms: a PEARRL review

Development and Validation of an Automated Zone Fluidics-Based Sensor for In Vitro Dissolution Studies of Captopril Using Total Error Concept

Contact Info

Product

Resources

About