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      Recent Advances in Pharmaceutical Cocrystals: From Bench to Market

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          Abstract

          The pharmacokinetics profile of active pharmaceutical ingredients (APIs) in the solid pharmaceutical dosage forms is largely dependent on the solid-state characteristics of the chemicals to understand the physicochemical properties by particle size, size distribution, surface area, solubility, stability, porosity, thermal properties, etc. The formation of salts, solvates, and polymorphs are the conventional strategies for altering the solid characteristics of pharmaceutical compounds, but they have their own limitations. Cocrystallization approach was established as an alternative method for tuning the solubility, permeability, and processability of APIs by introducing another compatible molecule/s into the crystal structure without affecting its therapeutic efficacy to successfully develop the formulation with the desired pharmacokinetic profile. In the present review, we have grossly focused on cocrystallization, particularly at different stages of development, from design to production. Furthermore, we have also discussed regulatory guidelines for pharmaceutical industries and challenges associated with the design, development and production of pharmaceutical cocrystals with commercially available cocrystal-based products.

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          Polymorphs, Salts, and Cocrystals: What’s in a Name?

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            Solubility Advantage of Amorphous Drugs and Pharmaceutical Cocrystals

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              Pharmaceutical Particle Engineering via Spray Drying

              This review covers recent developments in the area of particle engineering via spray drying. The last decade has seen a shift from empirical formulation efforts to an engineering approach based on a better understanding of particle formation in the spray drying process. Microparticles with nanoscale substructures can now be designed and their functionality has contributed significantly to stability and efficacy of the particulate dosage form. The review provides concepts and a theoretical framework for particle design calculations. It reviews experimental research into parameters that influence particle formation. A classification based on dimensionless numbers is presented that can be used to estimate how excipient properties in combination with process parameters influence the morphology of the engineered particles. A wide range of pharmaceutical application examples—low density particles, composite particles, microencapsulation, and glass stabilization—is discussed, with specific emphasis on the underlying particle formation mechanisms and design concepts.
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                Author and article information

                Contributors
                Journal
                Front Pharmacol
                Front Pharmacol
                Front. Pharmacol.
                Frontiers in Pharmacology
                Frontiers Media S.A.
                1663-9812
                11 November 2021
                2021
                : 12
                : 780582
                Affiliations
                [ 1 ]Department of Industrial and Engineering Chemistry, Institute of Chemical Technology-Indian Oil Bhubaneswar Campus, Bhubaneswar, India
                [ 2 ]School of Pharmacy, Faculty of Health and Medical Sciences, Taylor’s University, Subang Jaya, Malaysia
                [ 3 ]Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia
                [ 4 ]Center of Excellence for Drug Research & Pharmaceutical Industries, King Abdulaziz University, Jeddah, Saudi Arabia
                [ 5 ]Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India
                Author notes

                Edited by: Kaisar Raza, Central University of Rajasthan, India

                Reviewed by: Mayank Joshi, Indian Institute of Science Education and Research Mohali, India

                Ranjeet Bapat, International Medical University, Malaysia

                Farrukh Zeeshan, International Medical University, Malaysia

                *Correspondence: Prashant Kesharwani, prashantdops@ 123456gmail.com ; Rambabu Dandela, r.dandela@ 123456iocb.ictmumbai.edu.in

                This article was submitted to Drugs Outcomes Research and Policies, a section of the journal Frontiers in Pharmacology

                Article
                780582
                10.3389/fphar.2021.780582
                8632238
                34858194
                e679abd3-f14c-458d-818f-4dc5ea989d5b
                Copyright © 2021 Kumar Bandaru, Rout, Kenguva, Gorain, Alhakamy, Kesharwani and Dandela.

                This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

                History
                : 21 September 2021
                : 11 October 2021
                Categories
                Pharmacology
                Review

                Pharmacology & Pharmaceutical medicine
                solid dosage forms,pharmaceutical cocrystals,solubility,permeability,cocrystallization,formulation,regulatory guidelines,particle size

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