Approaches for Establishing Clinically Relevant Dissolution Specifications for Immediate Release Solid Oral Dosage Forms

Hermans, Andre; Abend, Andreas; Kesisoglou, Filippos; Flanagan, Talia; Cohen, Michael J.; Diaz, Dorys Argelia; Mao, Yun; Zhang, Limin; Webster, Gregory K.; Lin, Yiqing; Hahn, David A.; Coutant, Carrie A.; Grady, Haiyan

doi:10.1208/s12248-017-0117-1

Cited by 52 publications

(54 citation statements)

References 19 publications

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“…Various approaches for the development and application of clinically relevant dissolution specifications (CRS) for IR oral solid dosage forms of non‐narrow therapeutic window drugs have been described (Hermans et al, ). The CRS data can be used as important research and quality control tool for the optimization of formulations, setting specifications for final product quality and serve as a substitute for BA/BE studies on supporting product and process modifications during SUPAC.…”

Section: In Vitro Dissolutionmentioning

confidence: 99%

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

Jacob

Nair

2018

Drug Development Research

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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.

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Section: In Vitro Dissolutionmentioning

confidence: 99%

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

Jacob

Nair

2018

Drug Development Research

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“…IQ Consortium member companies have compiled our thoughts on this topic in a publication which may serve as a base for such discussion. 52…”

Section: Establish Clinical Relevance For Dissolution Methodsmentioning

confidence: 99%

“…For BCS 1 and 3 compounds, a Q of 80% dissolved in 15 min (BCS3) and 30 min (BCS1) in 500 mL 0.01 N HCl with gentle agitation should be considered clinically relevant without actual in vivo data. 52 For BCS 2 and 4 compounds, establishing clinical relevance of the dissolution method would require linking in vitro dissolution data with in vivo PK data which may be a challenge due to the constraints mentioned previously.…”

Section: Clinically Relevant Dissolution: Linking In Vitro Dissolutiomentioning

confidence: 99%

Industry's View on Using Quality Control, Biorelevant, and Clinically Relevant Dissolution Tests for Pharmaceutical Development, Registration, and Commercialization

Grady

Elder²,

Webster

et al. 2018

Journal of Pharmaceutical Sciences

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This article intends to summarize the current views of the IQ Consortium Dissolution Working Group, which comprises various industry companies, on the roles of dissolution testing throughout pharmaceutical product development, registration, commercialization, and beyond. Over the past 3 decades, dissolution testing has evolved from a routine and straightforward test as a component of end-product release into a comprehensive set of tools that the developer can deploy at various stages of the product life cycle. The definitions of commonly used dissolution approaches, how they relate to one another and how they may be applied in modern drug development, and life cycle management is described in this article. Specifically, this article discusses the purpose, advantages, and limitations of quality control, biorelevant, and clinically relevant dissolution methods.

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“…Much scientific research has also been devoted to this topic, with the exploration of new methods to fabricate high-performance formulations (e.g. electrospinning, 3D printing, and combinations with traditional pharmaceutical strategies) [43][44][45][46].…”

Section: Introductionmentioning

confidence: 99%

Immediate release of helicid from nanoparticles produced by modified coaxial electrospraying

Zheng

Yang

et al. 2019

Applied Surface Science

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In this paper, a modified coaxial electrospraying process was explored for the generation of novel nanoscale composite materials. A solution comprising 5% (w/v) of the model drug helicid and 10% (w/v) polyvinylpyrrolidone (PVP) K10 in a mixture of N,N-dimethylacetamide and ethanol (4:6, v:v) was employed as the shell working liquid.This could not be processed into a solid product when processed by single-fluid electrospraying. However, when undertaking co-axial electrospraying with a core shellac solution (40% w/v in ethanol) solid particles were obtained. An extremely thin nanocoating layer of drug-polymer composite with an estimated thickness of 7 nm was deposited on a shellac core. X-ray diffraction and infrared spectroscopy demonstrated that the drug was converted into an amorphous nanocomposite with the PVP in the shell layer, losing its original crystalline state. In vitro dissolution tests revealed that all the helicid loading could be released within one minute, suggesting the particles have potential applications to deliver very rapid therapeutic effects. Mechanisms are proposed underlying the formation and functional performance of the materials.

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Approaches for Establishing Clinically Relevant Dissolution Specifications for Immediate Release Solid Oral Dosage Forms

Cited by 52 publications

References 19 publications

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

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

Industry's View on Using Quality Control, Biorelevant, and Clinically Relevant Dissolution Tests for Pharmaceutical Development, Registration, and Commercialization

Immediate release of helicid from nanoparticles produced by modified coaxial electrospraying

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