Can Biorelevant Media be Simplified by using SLS and Tween 80 to Replace Bile Compounds?~!2009-10-23~!2010-01-04~!2010-04-29~!

Abstract

Abstract:In the scientific literature, the use of a surfactant is recommended for both designing quality control tests for water insoluble or sparingly water soluble drugs and for predicting the bioavailability of drugs from various types of formulations. Since the number of poorly soluble drugs is increasing, the selection of adequate dissolution test for these becomes more and more important. The aim of the present study was to develop predictive and discriminatory test methods based on surfactants that are recommended in the literature. Particular respect was given to the use of sodium lauryl sulfate and Tween 80, the two most commonly used surfactants for this purpose. Tamoxifen was used as a model drug. Dissolution experiments were performed using various concentrations of the two surfactants in buffer media typically used to prepare biorelevant test media. Results were then compared with those deriving from the same test formulations in biorelevant and simplified "biorelevant" media. Results from this study indicate that the concentration of surfactant has a huge impact on both the rate and extent of drug release from the formulation and also on the discriminatory power of the test. However, they also indicate that a well designed and validated test medium containing SLS or Tween 80 can be useful in terms of establishing a discriminatory test medium that possibly could also be used to assure batch to batch bioequivalence. Therefore, the approach described in the present paper might be very helpful for developing predictive and discriminatory methods in early formulation development for poorly soluble drugs and which could also be adopted for QC.

Computational Prediction of Drug Solubility in Fasted Simulated and Aspirated Human Intestinal Fluid

“…Alternatives to HIF for dissolution testing and solubility measurements became available when Dressman and colleagues introduced fasted state simulated intestinal fluid (FaSSIF) in 1998 [ 11 ]. Other biorelevant dissolution media (BDM) have been developed since then, some to closer mimic the intestinal milieu [ 12 , 13 ] and others for ease of preparation or lower expense [ 14 , 15 ]. Nonetheless the use of FaSSIF continues to be widespread and a large number of compounds and formulations have been evaluated in them.…”

Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool

“…These dissolution conditions were able to order in vitro dissolution profiles in the same rank order as the in vivo ones and the f 2 values gave the same conclusion as the bioequivalence study. According to Taupitz and Klein, dissolution media modified with synthetic surfactants can be discriminatory to evaluate dissolution differences between formulations of drugs with low solubility, being the amount of surfactant a critical aspect to obtain predictive conditions [36].…”

Assessment of physical and dissolution characteristics of various itraconazole capsule formulations: a comparative analysis

“…Dissolution test of itraconazole capsule was performed using a United States Pharmacopeia type II (Paddle) apparatus (Labindia Analytical Instruments), at 37°C0.5°C, 100 rpm in simulated gastric fluid (SGF, 900 ml, pH 1.2) without enzyme, acetate buffer (pH 4.5+0.5% sodium lauryl sulfate [SLS], 900 ml), and phosphate buffer (pH 6.8+0.5% SLS, 900 ml). 25,26 One itraconazole capsule was added to each of the 6 dissolution vessels and 10 ml aliquots were withdrawn at 15, 30, 45, and 60 minutes. All aliquots were filtered through 0.45 µm nylon membrane and analyzed using high-performance liquid chromatography (HPLC).…”