Enzymatic activity in the presence of surfactants commonly used in dissolution media, Part 1: Pepsin

MARIA L GUZMAN; ERIKA S STIPPLER; MARGARETH R MARQUES; MARIA E OLIVERA ME

Results in pharma sciences

Elsevier

Año: 2016

The United States Pharmacopeia (USP) General Chapters Dissolution 〈711〉 and Disintegration and Dissolutionof Dietary Supplements 〈2040〉 allows the use of enzymes in dissolution media when gelatincapsules do not conform to dissolution specifications due to cross linking. Possible interactions betweenenzymes and surfactants when used together in dissolution media could result in loss of the enzymaticactivity. Pepsin is an enzyme commonly used in dissolution media, and in this work, the activity ofpepsin was determined in the presence of different surfactants as usually found in case of dissolutiontests of certain gelatin capsule formulations.Pepsin enzymatic activity was determined according to the Ninth Edition of the Food Chemicals Codex(FCC) 9 method, in dissolution conditions: simulated gastric fluid, 37 °C and 50 rpm. Sodium dodecylsulfate (SDS), cetyltrimethyl ammonium bromide (CTAB), polysorbate 80 (Tween 80) and octoxynol 9(Triton X100) in concentrations above and below their critical micellar concentrations were selected.Results showed a significant reduction in the activity of pepsin at all the concentrations of SDS assayed.On the contrary, CTAB, Tween 80, and Triton X100 did not alter the enzymatic activity at of pepsin any ofthe concentration assayed.This data demonstrates a rational selection of the surfactant to be used when pepsin is required indissolution test