Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Acetylsalicylic Acid

Dressman, Jennifer B.; Nair, Anita; Abrahamsson, Bertil; Barends, D. M.; Groot, D.W.; Kopp, Sabine; Langguth, Peter; Polli, James E.; Shah, Vinod P.; Zimmer, Markus

doi:10.1002/jps.23212

Cited by 52 publications

(36 citation statements)

References 21 publications

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“…The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

“…This literature review found that phosphate buffer solutions, in the range of pH 5.8-8.0, were employed in 32.6% of cases as medium for the shake-flask method (15 of 46 studies) (8,11,19,31,32,37,(41)(42)(43)45,46,48,51,57,58) and in 40.0% as dissolution medium (8 of 20 studies) (10,11,22,24,(51)(52)(53)56). Acetate buffer was used less frequently, in 4 of 46 studies (8.7%) (41,42,45,49) as medium for the shake-flask method and in 2 of 20 studies (10.0%) as dissolution medium (52,56).…”

Section: Buffer Solutionsmentioning

confidence: 99%

“…Acetate buffer was used less frequently, in 4 of 46 studies (8.7%) (41,42,45,49) as medium for the shake-flask method and in 2 of 20 studies (10.0%) as dissolution medium (52,56). Phosphate and acetate buffer solutions, which were claimed to have similar osmolality and ionic strength as the physiological fluids, were the most employed buffer solutions to determine solubility (27.3% for the phosphate buffer and 9.1% for the acetate buffer).…”

Section: Buffer Solutionsmentioning

confidence: 99%

“…In the last decade, biorelevant media have been extensively used to determine drug solubility and as dissolution media, especially for BCS class II compounds (14 studies or 25.0%) (8,9,13,22,27,33,35,42,44,45,47,51,54,55) as well as for BCS class I (4 studies or 7.1%) (33,34,49,51), class III (2 or 3.6%) (33,51), and class IV (2 or 3.6%) (33,51). As mentioned, biorelevant media contain generally components which are likely present in the human GI tract such as bile salts and lecithin aiming to mimic the physiological conditions in specific segments of the GI tract; thus, in these media, pH, osmolality, and surface tension are adapted to physiological values (75).…”

Section: Biorelevant Mediamentioning

confidence: 99%

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Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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“…The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

Section: Buffer Solutionsmentioning

confidence: 99%

Section: Buffer Solutionsmentioning

confidence: 99%

Section: Biorelevant Mediamentioning

confidence: 99%

See 2 more Smart Citations

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

View full text Add to dashboard Cite

show abstract

“…Class I (High Permeability, High Solubility) 1,2 Biowaivers are considered as the waivers of clinical bioequivalence studies . Bioequivalence studies are as vital concern in drug development process, which are required for small changes in drug products that develop during drug 3 development to ensure that the dosage forms prove to be safe and effective .…”

Section: Biopharmaceutics Classification System (Bcs)mentioning

confidence: 99%

Biowaivers-An updated Review

Abilash¹,

Chandramouli²

2017

Journal of Pharmaceutical Research

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PURPOSE:A Biowaiver has been regarded as an official approval of the waiver for conducting a bioequivalence study in the context of an application for drug approval process. Bioequivalence is an important parameter in the process of drug development that is needed to be performed when there is a change in the formulation of dosage form. Approach:The approach of biowaivers is necessary to waive a complete and systemic Bioequalence study, which as a fast track approach to boost the drug development process. Findings:This review mainly discusses about the criteria for Biowaivers, requirements for a BCS based biowaiver study, conditions to grant the BCS based biowaiver, Applications, limitations, supporting data for Biowaivers.Conclusion: BCS biowaiver studies in preparing a submission for worldwide filing to satisfy US, European, and emerging market regulators. It is hoped that the availability of BCS Class I and Class III biowaivers in multiple jurisdictions will encourage more sponsors to request waivers of in vivo bioavailability/bioequivalence testing using the BCS approach.

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Application of data mining approach to identify drug subclasses based on solubility and permeability

Gatarić¹,

Parojčić

2019

Biopharm & Drug Disp

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Solubility and permeability are recognized as key parameters governing drug intestinal absorption and represent the basis for biopharmaceutics drug classification. The Biopharmaceutics Classification System (BCS) is widely accepted and adopted by regulatory agencies. However, currently established low/high permeability and solubility boundaries are the subject of the ongoing scientific discussion. The aim of the present study was to apply data mining analysis on the selected drugs data set in order to develop a human permeability predictive model based on selected molecular descriptors, and to perform data clustering and classification to identify drug subclasses with respect to dose/solubility ratio (D/S) and effective permeability (Peff). The Peff values predicted for 30 model drugs for which experimental human permeability data are not available were in good agreement with the reported fraction of drug absorbed. The results of clustering and classification analysis indicate the predominant influence of Peff over D/S. Two Peff cut‐off values (1 × 10−4 and 2.7 × 10−4 cm/s) have been identified indicating the existence of an intermediate group of drugs with moderate permeability. Advanced computational analysis employed in the present study enabled the recognition of complex relationships and patterns within physicochemical and biopharmaceutical properties associated with drug bioperformance.

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Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Acetylsalicylic Acid

Cited by 52 publications

References 21 publications

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Biowaivers-An updated Review

Application of data mining approach to identify drug subclasses based on solubility and permeability

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