Abstract
Solid-state mechanochemical grinding is important for promoting cocrystal formation, particularly in the design of new solids in the pharmaceutical industry. Pharmaceutical cocrystals are defined as crystalline materials comprising an active pharmaceutical ingredient (API) and one or more appropriate coformers in a definite stoichiometric ratio, formed via non-covalent interactions. Recently, both the US FDA (2013) and the EU EMA (2015) provided a Guidance for Industry and a Reflection Paper, respectively, emphasizing that cocrystals are a new type of substance with potential applications in the pharmaceutical industry. This paper contains a brief and systematic overview of pharmaceutical cocrystals prepared by four grinding processes: neat grinding, solvent-assisted grinding, thermal stress after neat grinding, and polymer-assisted grinding. The paper also highlights some examples of pharmaceutical cocrystals prepared by the above grinding approaches, and discusses the stability of cocrystals prepared by mechanical grinding. Also, an overview of cocrystals that are commercially available or undergoing clinical trials is given. A novel methodology for real-time and in situ monitoring of mechanochemical grinding reactions using various analytical techniques is addressed and can be expected to be applied in the near future.
Keywords: Pharmaceutical cocrystal, mechanochemistry, stability, neat grinding, solvent-assisted grinding, thermal stress after grinding, polymer-assisted grinding.
Current Pharmaceutical Design
Title:Mechanochemical Approaches to Pharmaceutical Cocrystal Formation and Stability Analysis
Volume: 22 Issue: 32
Author(s): Shan-Yang Lin
Affiliation:
Keywords: Pharmaceutical cocrystal, mechanochemistry, stability, neat grinding, solvent-assisted grinding, thermal stress after grinding, polymer-assisted grinding.
Abstract: Solid-state mechanochemical grinding is important for promoting cocrystal formation, particularly in the design of new solids in the pharmaceutical industry. Pharmaceutical cocrystals are defined as crystalline materials comprising an active pharmaceutical ingredient (API) and one or more appropriate coformers in a definite stoichiometric ratio, formed via non-covalent interactions. Recently, both the US FDA (2013) and the EU EMA (2015) provided a Guidance for Industry and a Reflection Paper, respectively, emphasizing that cocrystals are a new type of substance with potential applications in the pharmaceutical industry. This paper contains a brief and systematic overview of pharmaceutical cocrystals prepared by four grinding processes: neat grinding, solvent-assisted grinding, thermal stress after neat grinding, and polymer-assisted grinding. The paper also highlights some examples of pharmaceutical cocrystals prepared by the above grinding approaches, and discusses the stability of cocrystals prepared by mechanical grinding. Also, an overview of cocrystals that are commercially available or undergoing clinical trials is given. A novel methodology for real-time and in situ monitoring of mechanochemical grinding reactions using various analytical techniques is addressed and can be expected to be applied in the near future.
Export Options
About this article
Cite this article as:
Lin Shan-Yang, Mechanochemical Approaches to Pharmaceutical Cocrystal Formation and Stability Analysis, Current Pharmaceutical Design 2016; 22 (32) . https://dx.doi.org/10.2174/1381612822666160726111253
DOI https://dx.doi.org/10.2174/1381612822666160726111253 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
SGLT-2 Inhibitors and Cardiovascular Risk in Diabetes Mellitus: A Comprehensive and Critical Review of the Literature
Current Pharmaceutical Design Early Intervention in Psychosis: Rationale, Results and Implications for Treatment of Adolescents at Risk
Adolescent Psychiatry The Fetal Cardiac Function
Current Cardiology Reviews Lost in Translation: What is Limiting Cardiomyoplasty and Can Tissue Engineering Help?
Current Stem Cell Research & Therapy Mineralocorticoid Receptor Antagonism and Cardiac Remodeling in Ischemic Heart Failure
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Role of Infrared Spectroscopy in Medicinal Plants Research in Pakistan
Current Bioactive Compounds Pleural Fluid Analysis for Evaluating Pleural Effusions
Current Respiratory Medicine Reviews By Discontinuing Beta-Blockers Before an Exercise Test, We may Precipitate a Rebound Phenomenon
Current Vascular Pharmacology p38 MAP Kinase Mediated Proteoglycan Synthesis as a Target for the Prevention of Atherosclerosis
Cardiovascular & Hematological Disorders-Drug Targets Store-Dependent Ca2+ Entry in Endothelial Progenitor Cells As a Perspective Tool to Enhance Cell-Based Therapy and Adverse Tumour Vascularization
Current Medicinal Chemistry DNA Repair in Premature Aging Disorders and Neurodegeneration
Current Aging Science Epidemiology of Hypertension and Diabetes Mellitus in Latin America
Current Hypertension Reviews Sulfonamides and Sulfonylated Derivatives as Anticancer Agents
Current Cancer Drug Targets Diagnostic Tools, Biomarkers, and Treatments in Diabetic polyneuropathy and Cardiovascular Autonomic Neuropathy
Current Diabetes Reviews Leishmania Heat Shock Proteins as Effectors of Immune Evasion and Virulence
Current Immunology Reviews (Discontinued) The Diagnosis of Drug-Induced Liver Disease
Current Clinical Pharmacology Resuscitation of the Newborn in the Delivery Room
Current Pediatric Reviews Voltage-Gated Sodium Channels: Mutations, Channelopathies and Targets
Current Medicinal Chemistry G Protein-Coupled Receptor Kinase 2 - a Feedback Regulator of Gq Pathway Signalling
Current Drug Targets - Immune, Endocrine & Metabolic Disorders GRK2 Inhibition in Heart Failure: Something Old, Something New
Current Pharmaceutical Design