Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems
Active pharmaceutical ingredients (API) with unfavorable physicochemical properties and stability present a significant challenge during their processing into final dosage forms. Cocrystallization of such APIs with suitable coformers is an efficient approach to mitigate the solubility and stability...
| Main Authors: | , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-04-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/15/4/1161 |
| _version_ | 1827744049372594176 |
|---|---|
| author | Maan Singh Harsh Barua Vaskuri G. S. Sainaga Jyothi Madhukiran R. Dhondale Amritha G. Nambiar Ashish K. Agrawal Pradeep Kumar Nalini R. Shastri Dinesh Kumar |
| author_facet | Maan Singh Harsh Barua Vaskuri G. S. Sainaga Jyothi Madhukiran R. Dhondale Amritha G. Nambiar Ashish K. Agrawal Pradeep Kumar Nalini R. Shastri Dinesh Kumar |
| author_sort | Maan Singh |
| collection | DOAJ |
| description | Active pharmaceutical ingredients (API) with unfavorable physicochemical properties and stability present a significant challenge during their processing into final dosage forms. Cocrystallization of such APIs with suitable coformers is an efficient approach to mitigate the solubility and stability concerns. A considerable number of cocrystal-based products are currently being marketed and show an upward trend. However, to improve the API properties by cocrystallization, coformer selection plays a paramount role. Selection of suitable coformers not only improves the drug’s physicochemical properties but also improves the therapeutic effectiveness and reduces side effects. Numerous coformers have been used till date to prepare pharmaceutically acceptable cocrystals. The carboxylic acid-based coformers, such as fumaric acid, oxalic acid, succinic acid, and citric acid, are the most commonly used coformers in the currently marketed cocrystal-based products. Carboxylic acid-based coformers are capable of forming the hydrogen bond and contain smaller carbon chain with the APIs. This review summarizes the role of coformers in improving the physicochemical and pharmaceutical properties of APIs, and deeply explains the utility of afore-mentioned coformers in API cocrystal formation. The review concludes with a brief discussion on the patentability and regulatory issues related to pharmaceutical cocrystals. |
| first_indexed | 2024-03-11T04:38:23Z |
| format | Article |
| id | doaj.art-9325202b99af427681c110541af1c536 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T04:38:23Z |
| publishDate | 2023-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-9325202b99af427681c110541af1c5362023-11-17T20:53:35ZengMDPI AGPharmaceutics1999-49232023-04-01154116110.3390/pharmaceutics15041161Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API ProblemsMaan Singh0Harsh Barua1Vaskuri G. S. Sainaga Jyothi2Madhukiran R. Dhondale3Amritha G. Nambiar4Ashish K. Agrawal5Pradeep Kumar6Nalini R. Shastri7Dinesh Kumar8Pharmaceutical Solid State Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, IndiaSolid State Pharmaceutical Cluster (SSPC), Science Foundation Ireland Research Centre for Pharmaceuticals, Bernal Institute, Department of Chemical Sciences, University of Limerick, V94T9PX Limerick, IrelandDepartment of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad 500037, IndiaPharmaceutical Solid State Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, IndiaPharmaceutical Solid State Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, IndiaPharmaceutical Solid State Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, IndiaWits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South AfricaSolid State Pharmaceutical Research, Hyderabad 500037, IndiaPharmaceutical Solid State Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, IndiaActive pharmaceutical ingredients (API) with unfavorable physicochemical properties and stability present a significant challenge during their processing into final dosage forms. Cocrystallization of such APIs with suitable coformers is an efficient approach to mitigate the solubility and stability concerns. A considerable number of cocrystal-based products are currently being marketed and show an upward trend. However, to improve the API properties by cocrystallization, coformer selection plays a paramount role. Selection of suitable coformers not only improves the drug’s physicochemical properties but also improves the therapeutic effectiveness and reduces side effects. Numerous coformers have been used till date to prepare pharmaceutically acceptable cocrystals. The carboxylic acid-based coformers, such as fumaric acid, oxalic acid, succinic acid, and citric acid, are the most commonly used coformers in the currently marketed cocrystal-based products. Carboxylic acid-based coformers are capable of forming the hydrogen bond and contain smaller carbon chain with the APIs. This review summarizes the role of coformers in improving the physicochemical and pharmaceutical properties of APIs, and deeply explains the utility of afore-mentioned coformers in API cocrystal formation. The review concludes with a brief discussion on the patentability and regulatory issues related to pharmaceutical cocrystals.https://www.mdpi.com/1999-4923/15/4/1161coformercocrystalsolubilitystabilityfumaric acidoxalic acid |
| spellingShingle | Maan Singh Harsh Barua Vaskuri G. S. Sainaga Jyothi Madhukiran R. Dhondale Amritha G. Nambiar Ashish K. Agrawal Pradeep Kumar Nalini R. Shastri Dinesh Kumar Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems Pharmaceutics coformer cocrystal solubility stability fumaric acid oxalic acid |
| title | Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems |
| title_full | Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems |
| title_fullStr | Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems |
| title_full_unstemmed | Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems |
| title_short | Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems |
| title_sort | cocrystals by design a rational coformer selection approach for tackling the api problems |
| topic | coformer cocrystal solubility stability fumaric acid oxalic acid |
| url | https://www.mdpi.com/1999-4923/15/4/1161 |
| work_keys_str_mv | AT maansingh cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT harshbarua cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT vaskurigssainagajyothi cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT madhukiranrdhondale cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT amrithagnambiar cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT ashishkagrawal cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT pradeepkumar cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT nalinirshastri cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems AT dineshkumar cocrystalsbydesignarationalcoformerselectionapproachfortacklingtheapiproblems |