Fabrication of Triple-Layer Matrix Tablets of Venlafaxine Hydrochloride Using Xanthan Gum

Abstract

Abstract. The objective of present investigation was to develop venlafaxine hydrochloride-layered tablets for obtaining sustained drug release. The tablets containing venlafaxine hydrochloride 150 mg were prepared by wet granulation technique using xanthan gum in the middle layer and barrier layers. The granules and tablets were characterized. The in vitro drug dissolution study was conducted in distilled water. The tablets containing two lower strengths were also developed using the same percentage composition of the middle layer. Kinetics of drug release was studied. The optimized batches were tested for water uptake study. Radar diagrams are provided to compare the performance of formulated tablets with the reference products, Effexor XR capsules. The granules ready for compression exhibited good flow and compressibility when xanthan gum was used in the intragranular and extragranular fractions. Monolayer tablets failed to give the release pattern similar to that of the reference product. The drug release was best explained by Weibull model. A unified Weibull equation was evolved to express drug release from the formulated tablets. Lactose facilitated drug release from barrier layers. Substantial water uptake and gelling of xanthan gum appears to be responsible for sustained drug release. The present study underlines the importance of formulation factors in achieving same drug release pattern from three strengths of venlafaxine hydrochloride tablets.

Optimization and In vivo Pharmacokinetic Study of a Novel Controlled Release Venlafaxine Hydrochloride Three-Layer Tablet

“…It is a white crystalline solid freely soluble in water (534 mg/ml) (2). The recommended dose of VenHCl is 75 to 450 mg/day (3). The steady-state half lives of venlafaxine and its active metabolite, o-desmethylvenlafaxine, are 5 and 11 h, respectively, necessitating the administration, two or three times daily so as to maintain adequate plasma levels of the drug (4).…”

“…VenHCl is currently available as an extended release capsule, containing VenHCl equivalent to venlafaxine 75 mg in the form of coated pellets for a once daily administration under the brand name of Effexor®XR. The major disadvantages of coating methods are their low productivity, long processing time, high cost, and variation between and within batches (3).…”

Formulation and Evaluation of Zolpidem Tartrate Layered Tablets by Melt Granulation Technique for Treatment of Insomnia

“…Formulations ZT8 and ZT9 were layered top and bottom using a hydrophilic polymer. Initially, the core tablet was slightly precompressed and was layered top and bottom with HPMC K4M [9][10][11]. Tablets were prepared with different diluents and channeling agents (HPMC K100 and lactose monohydrate at concentrations of 2.5%, 5%, and 10%) ( Table 3).…”

Comparative In Vitro Dissolution Testing of Hydrophilic Controlled-Release Venlafaxine Matrix Tablets and Effexor XR Using QbD

“…Various patents (6)(7)(8) also disclose extended-release (once-a-day) venlafexine formulations to be composed of spheroids of Ven HCl coated with either ethyl cellulose or a combination of ethyl cellulose and hydroxypropyl methylcellulose (HPMC). This multi-unit particulate system (MUPS) is extremely expensive and time-consuming to produce on the shop floor due to multiple coating stages, long coating times, capsule filling after testing, and evaluation of pellets at completion of each stage (9). In the present work, a simple hydrophilic matrix-based tablet formulation was developed using a 33 full-factorial design with a target dissolution profile similar to that of Effexor XR capsules.…”