Speaker
Description
Since the past several decades, poor water solubility of existing and new drugs in the pipeline has remained a challenging issue for the pharmaceutical industry. These compounds have high therapeutic potential but are difficult to formulate as oral dosage forms due to their poor aqueous solubility. The use of conventional approaches such as solubilizing agents, salt formation, complexing agents, etc. have previously been successfully used to improve the solubility of several compounds. However, these approaches have inadequate applications due to their limited effectiveness of solubility enhancement, approved concentration of excipients, and various side effects associated with the excipients and cosolvents used in these approaches. Amorphous solid dispersions (ASD) have been one of the successful approach in enhancing the rate and extent of dissolution in drug product development process. These are the molecular mixtures of poor water soluble drugs with hydrophilic carriers, responsible for modulate drug release profile, and characterized by the reduction of drug particle size to a molecular level solubilizing or co-dissolving the drug in the soluble carriers. ASD can accelerate a project by improving dissolution rate and solubility, offering dose escalation flexibility and excipient acceptance for toxicology studies, as well as providing adequate preclinical and clinical exposure. This review summarizes methodologies of preparation, polymer selection and characterization of ASDs with brief insights on recent advances in the dissolution and supersaturation of these amorphous formulations.
Keywords: Amorphous solid dispersion, polymer selection, preparation, stability and characterization.