Formulation Optimization of Hydrodynamically Balanced Oral Controlled Release Bioadhesive Tablets of Tramadol Hydrochloride

Abstract

The directly compressible floating-bioadhesive tablets of tramadol were formulated using varying amounts Carbopol 971P (CP) and hydroxy-propylmethyl cellulose (HPMC), along with other requisite excipients. In vitro drug release profile, floatational characteristics and ex vivo bioadhesive strength using texture analyzer were determined, and systematically optimized using a 32 central composite design (CCD). The studies indicated successful formulation of gastroretentive compressed matrices with excellent controlled release, mucoadhesion and hydrodynamic balance. Comparison of the dissolution profiles of the optimized formulation, with optimal composition of CP:HPMC :: 80.0:125.0, with that of the marketed controlled release formulation other indicated analogy of drug release performance with each other. Validation of optimization study using eight confirmatory experimental runs indicated very high degree of prognostic ability of CCD with mean ± SEM of −0.06% ± 0.37. Further, the study successfully unravels the effect of the polymers on the selected response variables.

Formulation and Optimization of Gastric Bioadhesive Tablets of Diltiazem Hydrochloride using Central Composite Design

“…This is in agreement with earlier findings that a mixture of HPMC and Carbopol resulted in the reduction of polymer viscosity due to reduced hydration [11,18].…”

“…Based on phenomenological analysis, the type of release (i.e., whether Fickian, non-Fickian (anomalous) or zero order) was predicted [11]. t 60% value was calculated using Stineman interpolation option of the Graph 2.0 software (M/s Micromath Inc, St Louis, USA).…”

“…Linear correlation plots were constructed for the chosen eight optimized formulations. The residual graphs between predicted and observed responses were also constructed separately, and the percent bias (= prediction error) was calculated with respect to the observed responses [11].…”

“…Weight was slowly added on the right hand side pan until the tablet just got detached from the membrane surface. The peak detachment force was recorded as a measure of bioadhesive strength [11].…”

Design and evaluation of famotidine mucoadhesive nanoparticles for aspirin induced ulcer treatment

“…The combination of ionic polymer such as Na-CMC and nonionic polymer such as HPMCK4M is known to provide the formulation with desired mucoadhesive properties (B 3 ) (Singh et al 2010). …”