30. July 2018
Injection site reactions (ISRs) and other adverse side-effects are commonly observed during therapy with biologics. These hypersensitivity related side-effects can vary from simple rash to life-threatening anaphylactic reaction, and may be linked to the immunogenicity of the drug including formation of antidrug antibodies. Reactions can also occur as a consequence of excipients in the product. We report the case of a patient who developed erythematous ISRs to both commercial PCSK9i formulations...
19. April 2018
Excipients are materials added along with therapeutic agents; and incompatibility between excipients and therapeutic agents affect the final outcome of the product. Aspirin is an ester and is prone to hydrolysis. This study focus on the effect of magnesium stearate as an excipient on stability of aspirin in granules. For that an accelerated degradation study was done on aspirin-magnesium stearate containing granules. For that, aspirin containing granules were sequentially mixed with increasing...
16. March 2018
Pharmaceutical drug products contain various excipients in combination with the active pharmaceutical ingredient (API), and those excipients have the potential to have as impurities reactive oxygen species that can react directly with the API and lead to oxidative degradation. Such degradation can impact long-term stability of the drug product, reduce drug product purity, limit shelf life, and increase time to market.
13. March 2018
Twenty years ago, a number of eminent pharmaceutical scientists collaborated on an article describing a rational approach to developing stable lyophilized protein formulations (Carpenter, Pikal, Chang, & Randolph, 1997). Since that time, no corresponding document for rational development of liquid formulations of proteins has appeared.
16. September 2017
The choice of excipients constitutes a major part of preformulation and formulation studies during the preparation of pharmaceutical dosage forms. The physical, mechanical, and chemical propertiesofexcipients affect various formulation parameters, such as disintegration, dissolution, and shelf life, and significantly influence the final product. Therefore, several studies have been performedtoevaluate the effect of drug-excipient interactions on the overall formulation. This article reviews the...
09. August 2016
Abstract This work aimed at developing enalapril maleate granules in order to improve its stability in solid dosage form. Granules were prepared by hot melt granulation using a fluidized bed apparatus. Gelucire 50/13®, polyethylene glycol 6000 e Poloxamer 407® were studied and compared as binders in 2 × 2 factorial designs where the proportions of enalapril maleate, binders and spray dried lactose were varied. The granulation process resulted in high yields and granule sizes that...
08. June 2016
The objective of this work was to improve the dissolution rate of candesartan cilexitil, a poorly water soluble prodrug and to reduce its premature degradation in the intestinal lumen. Binary and ternary solid dispersions (SD) of the drug with Pluronic F68, Polyvinyl pyrrolidone (PVP), Hydroxypropyl Methylcellulose (HPMC) and Tween 80 were prepared using the solvent evaporation method. The dissolution rate of the drug was monitored and the prepared SD systems were characterized using thermal...
16. February 2016
Polyvinyl alcohol has received little attention as a matrix polymer in amorphous solid dispersions (ASDs) due to its thermal and rheological limitations in extrusion processing and limited organic solubility in spray drying applications. Additionally, in extrusion processing, the high temperatures required to process often exclude thermally labile APIs. The purpose of this study was to evaluate the feasibility of processing polyvinyl alcohol amorphous solid dispersions utilizing the model...
05. February 2016
Reactions between active drug substances and excipients are of interest in the drug formulation process should be checked for the interactions during the storage conditions. Some excipients react with certain chemical groups in drug substances which will form new impurities in the finished product formulations. In the present paper transesterification reaction of methylphenidate with glycerin to form different structural isomeric products was described. These impurities identified in forced...
29. January 2016
The objective of the current research article is to provide a comprehensive review of excipients impact on the stability of the drug product and their implications during the product development. Recent developments in the understanding of the degradation pathways further impact methodologies used in the pharmaceutical industry for potential stability assessment. The formation of drug excipient adducts was very common based on the sensitive chemical moieties in the drugs and the excipients. The...