Pharmaceutical Diluents and Their Unwanted Effects: A Review

Abstract

Diluents are chemically inactive excipients, mostly used to make up the required bulk of solid dosage form and used up to 80% in a formulation. Various studies reported that diluents used in the solid dosage forms shows unwanted effects in body on long term and some time in short duration therapy. So, it is necessary to study the unwanted effects of diluents by researchers and production chemists before preparation of a pharmaceutical formulation to reduce the unwanted actions. Present review provides toxicological data of commonly used pharmaceutical diluents and summarizes the unwanted effects of pharmaceutical diluents on public health.

<p>Safety and Biopharmaceutical Challenges of Excipients in Off-Label Pediatric Formulations</p>

“…So, it is necessary to categorize the safety of diluents before preparing a pharmaceutical formulation to reduce the adverse effects. 66 Lactose and mannitol are the most frequently reported toxic fillers in pediatric off-label formulations.…”

“…In some cases, hypersensitivity and anaphylactic reactions are reported after intravenous infusion of 10% or 20% (w/v) solutions containing mannitol. 66 Direct action of mannitol on mast cells is responsible for the anaphylactic reactions. Its absorption is not more than 20% when taken orally.…”

“…It is also sometimes used in injectable solutions of small molecules for the purpose of solubility enhancement due to its ability to form micelle. 66 However, the polysorbate content in pediatric therapeutic formulations has been less clearly regulated or defined with regard to safety. Parenteral administration of more than 50.6 g polysorbate 80 and 3.37 g polysorbate 20 in biotherapeutics have been linked to hypersensitivity and other toxicity-related effects such as thrombocytopenia, cholestasis, ascites, hypotension, renal dysfunction, hepatomegaly, and severe metabolic acidosis which may lead to death.…”