Abstract
Understanding the properties, stability and transformations of the solid-state forms of an active pharmaceutical ingredient (API) in the development pipeline is of crucial importance for process-development, formulation development and FDA approval. Investigation of the polymorphism and polymorphic stability is a routine part of the preformulation studies. Vibrational spectroscopy allows the real-time in situ monitoring of phase transformations and probes intermolecular interactions between API molecules, between API and polymer in amorphous solid dispersions or between API and coformer in cocrystals or coamorphous systems and thus plays a major role in efforts to gain a predictive understanding of the relative stability of solid-state forms and formulations. Infrared (IR), near-infrared (NIR) and Raman spectroscopies, alone or in combination with other analytical methods, are important tools for studying transformations between different crystalline forms, between the crystalline and amorphous form, between hydrate and anhydrous form and for investigating solid-state cocrystal formation. The development of simple-to-use and cost-effective instruments on the one hand and recent technological advances such as access to the low-frequency Raman range down to 5 cm-1, on the other, have led to an exponential growth of the literature in the field. This review discusses the application of IR, NIR and Raman spectroscopies in the study of solid-state transformations with a focus on the literature published over the last eight years.
Keywords: IR spectroscopy, NIR spectroscopy, Raman spectroscopy, polymorphism, amorphous phase, hydrates, cocrystals, amorphous solid dispersions.
Current Pharmaceutical Design
Title:Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals
Volume: 22 Issue: 32
Author(s): Andrea Erxleben
Affiliation:
Keywords: IR spectroscopy, NIR spectroscopy, Raman spectroscopy, polymorphism, amorphous phase, hydrates, cocrystals, amorphous solid dispersions.
Abstract: Understanding the properties, stability and transformations of the solid-state forms of an active pharmaceutical ingredient (API) in the development pipeline is of crucial importance for process-development, formulation development and FDA approval. Investigation of the polymorphism and polymorphic stability is a routine part of the preformulation studies. Vibrational spectroscopy allows the real-time in situ monitoring of phase transformations and probes intermolecular interactions between API molecules, between API and polymer in amorphous solid dispersions or between API and coformer in cocrystals or coamorphous systems and thus plays a major role in efforts to gain a predictive understanding of the relative stability of solid-state forms and formulations. Infrared (IR), near-infrared (NIR) and Raman spectroscopies, alone or in combination with other analytical methods, are important tools for studying transformations between different crystalline forms, between the crystalline and amorphous form, between hydrate and anhydrous form and for investigating solid-state cocrystal formation. The development of simple-to-use and cost-effective instruments on the one hand and recent technological advances such as access to the low-frequency Raman range down to 5 cm-1, on the other, have led to an exponential growth of the literature in the field. This review discusses the application of IR, NIR and Raman spectroscopies in the study of solid-state transformations with a focus on the literature published over the last eight years.
Export Options
About this article
Cite this article as:
Erxleben Andrea, Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals, Current Pharmaceutical Design 2016; 22 (32) . https://dx.doi.org/10.2174/1381612822666160726110103
DOI https://dx.doi.org/10.2174/1381612822666160726110103 |
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
-
Ayahuasca-Assisted Therapy for Addiction: Results from a Preliminary Observational Study in Canada
Current Drug Abuse Reviews Serotonin 5-HT7 Receptor Antagonists
Current Medicinal Chemistry - Central Nervous System Agents Drug Metabolizing Enzymes in the Perinatal and Neonatal Period: Differences in the Expression and Activity
Current Drug Metabolism Nanoparticles in the Pharmaceutical Industry and the Use of Supercritical Fluid Technologies for Nanoparticle Production
Current Drug Delivery Recent Advances in Health Promoting Effect of Dietary Polyphenols
Current Nutrition & Food Science Different Factors Influence Recanalisation Rate After Coiling in Ruptured and Unruptured Intracranial Aneurysms
CNS & Neurological Disorders - Drug Targets Atypical Chest Pain in ACS: A Trap Especially for Women
Current Pharmaceutical Design The Influence of Host Factors on the Prognosis of Breast Cancer: Stroma and Immune Cell Components as Cancer Biomarkers
Current Cancer Drug Targets Specific Roles of NMDA Receptor Subunits in Mental Disorders
Current Molecular Medicine Phage Display as a Tool for Protease Ligand Discovery
Current Pharmaceutical Biotechnology Inhibition of Efflux of Quinolines as New Therapeutic Strategy in Malaria
Current Topics in Medicinal Chemistry Cerebrovascular Damage as a Cause for Alzheimers Disease
Current Neurovascular Research Application of Ligand SAR, Receptor Modeling and Receptor Mutagenesis to the Discovery and Development of a New class of 5-HT2A Ligands
Current Topics in Medicinal Chemistry Anabolic-androgenic Steroid use and Psychopathology in Athletes. A Systematic Review
Current Neuropharmacology Alzheimer's Disease: Related Targets, Synthesis of Available Drugs, Bioactive Compounds Under Development and Promising Results Obtained from Multi-target Approaches
Current Drug Targets PTML Modeling for Alzheimer’s Disease: Design and Prediction of Virtual Multi-Target Inhibitors of GSK3B, HDAC1, and HDAC6
Current Topics in Medicinal Chemistry Investigation of 5-HT<sub>2A</sub> gene expression in PBMCs of patients with allergic asthma
Inflammation & Allergy - Drug Targets (Discontinued) Mesenchymal Stem Cells for Multiple Sclerosis: Does Neural Differentiation Really Matter?
Current Stem Cell Research & Therapy In Transitional Space: A Whirlwind Tour of the DSM-5
Adolescent Psychiatry Co-Morbidity of APD and Reading Disabilities
Current Pediatric Reviews