Development and Validation of a Dissolution Test for 6 mg Deflazacort Tablets

Abstract

The aim of this study was to develop and validate a dissolution test for the quality control of deflazacort (DEF) tablets, a drug mainly used for the prevention of organ transplantation rejection, labeled as containing 6 mg of active pharmaceutical ingredient (API), using an RP-HPLC method. After testing sink conditions and stability at 37°C, DEF was found to be unstable, and decomposed as a function of the dissolution media. However, in water the decomposition was not significant enough to interfere with the determination of dissolution for DEF. The best conditions to carry out the dissolution test were paddle at 50 rpm, with 500 mL of deaerated water at 37°C. Under these conditions, the in vitro release profiles of 6 mg DEF tablets produced by two different laboratories, representing all approved products in the national market, shown to be dissimilar. A correlation between disintegration and in vitro dissolution was found for the two investigated formulations. The developed dissolution test was adequate for its purpose and can be applied for the quality control of 6 mg DEF tablets.

Response Surface Optimization of Ultra-Elastic Nanovesicles Loaded with Deflazacort Tailored for Transdermal Delivery: Accentuated Bioavailability and Anti-Inflammatory Efficacy

“…5,6 Unfortunately, problems such as poor solubility, erratic absorption and many drug dosing are encountered with oral DFZ. 7 Additionally, gastrointestinal symptoms are the most frequently reported adverse events in DFZ recipient. 8,9 DFZ belongs to biopharmaceutics classification system (BCS) class II with an oral bioavailability of about 68% and short elimination half-life (t 1/2 ) from 1.9 to 2.3 h. 2 Different strategies have been developed with a focus on enhancing solubility, dissolution rate, and bioavailability of class II drugs.…”

Sensitive Determination of Deflazacort by Comparative Nano-Voltammetric and Ion Selective Potentiometric Analysis in Pharmaceuticals and Biologicals

“…Apparatus.--Metrohm computrace voltammetric analyzer model 797 VA with Software Version 1.0 (Metrohm, Switzerland) for voltammetric analysis equipped with three-electrodes: a working electrode, Ag/ AgCl (3 M KCl) electrode as reference electrode and a platinum electrode as auxiliary electrode. Nano-gold electrode NGE Streptavidin Gold, with nanoparticles of spherical shape and average radius (15)(16)(17)(18)(19)(20) nm as working electrode which was purchased from Spherotech, (Chicago, USA). -The structural phase characterization of Tetrakis was analyzed and investigated using energy dispersive X-ray analysis with a Joel JSM6360 high-resolution scanning electron microscope.…”

“…5 Some of the well known side effects of such drugs are bone loss, glucose intolerance or Cushing's syndrome. 6 Literature survey reveals that spectrophotometric methods have been reported for the determination of DZC in bulk and tablets [7][8][9][10][11][12] and high performance liquid chromatographic assay methods have been reported for the determination of DZC in different formulations, [12][13][14][15][16] stability indicating UPLC method. 17 Various analytical techniques like HPLC and LC-MS are used for the quantization of DZC and its metabolites in human biological fluid have been reported.…”

“…18,19 The determination of DZC dissolution studies by HPLC was reported. 16 Estimation of DZC in tablet was reported by HPTLC method. 20 Literature survey revealed no methods were found based on the electrochemical redox properties of DZC.…”

Comparative dissolution and polymorphism study of clopidogrel bisulfate tablets available in Argentine

“…Consequently, drug resistance and treatment failure are commonly reported in emerging markets, such as in Asian and African countries (Reddy et al, 2014). The Americas and Argentine do not escape this problem since many multisource products were found to be in-vitro inequivalent to the innovator ones (Kassuha et al, 2009;Löbenberg et al, 2012;Simionato et al, 2018;Sperandeo and Kassuha, 2009), and at least in the case of some drugs [Biopharmaceutical Classification System (BCS) Class II, highly permeable and poorly soluble], significant differences in the dissolution profiles will result in differences in bioavailability since dissolution is the rate-determining step of the absorption process (Ruiz et al, 2012).…”