Current Perspectives on Pain upon Injection of Drugs

Abstract

A limitation in the administration of parenteral products is the pain caused upon injection. Injection site pain has been predominately associated with intravenous, intramuscular, and subcutaneous administration. It becomes important for the formulation scientist to have a basic understanding of the physiology underlying the pain process, as well as the pharmaceutical factors associated with injection site pain. Initially, this review will provide the reader with a primer on the mediation of pain in the periphery and a compilation of those drugs that have been associated with pain on injection. In addition, this review will present important considerations and general formulation approaches or methods that have been used to overcome pain on injection. Finally, a brief overview of the various experimental systems used to investigate injection site pain is discussed.

Composition Optimization and Stability Testing of a Parenteral Antifungal Solution based on a Ternary Solvent System

“…Therefore, a dilution plot of solute concentration as a function of the composition of the excipients is a straight line that passes from the initial composition to the origin (33). Three such dilution lines (represented by dashed lines), originating from different initial concentrations of miconazole (10,20, and 30 mg/mL), are illustrated in Figs. 5 and 6.…”

“…In the case of liquid formulations comprising one or more active ingredients which show poor water solubility, solubility enhancers are often used to ensure the therapeutically effective dose of the compounds (3)(4)(5)(6)(7)(8)(9). The effect of such excipients on the pharmacokinetics of the drugs and their impact on the blood have been widely studied (10)(11)(12)(13) and although the toxicity of a formulation can by no means be explained solely by the concentration of the applied excipients, it is widely accepted that the lower the level of an excipient in a formulation, the less likely it is to induce toxicity. An inappropriate amount or composition of solvents can cause hemolysis, precipitation of the drug, phlebitis, and pain (14)(15)(16)(17).…”

A Practical Approach to the use of Nanoparticles for Vaccine Delivery

“…For the administration of a parenteral product, the osmolarity needs to be in the range of 280-330 mOsm/L. 44 We did not test higher sugar concentrations because they would exceed this osmolarity limit. The literature reports examining sugars for resuspension also contain surfactants with the nanoparticles and thus cannot be directly compared to our results.…”

“…For the administration of a parenteral product, the osmolarity should be in the range of 280-330 mOsm/L to reduce pain upon injection. 44 This limits the total concentration of sugars that can be used as excipients for a vaccine formulation. The ideal is a single vial formulation that can be reconstituted and used without further dilution which otherwise would be a burden for a practical vaccine formulation.…”

Evaluation of sodium diclofenac release using natural rubber latex as carrier

“…When drugs are injected intravenously only one part in ten thousand reaches its final target, in appropriate concentrations to cause the expected therapeutic effect 5,6 . This proportion is due to many anatomical, chemical and biological obstacles verified between the local administration of the drug and the target organ or tissue.…”