Novel Use of Similarity Factorsf2andSdfor the Development of Diltiazem HCl Modified-Release Tablets Using a 32Factorial Design

Abstract. The aim of the present study was to enhance the dissolution rate of meloxicam (MLX), a practically water-insoluble drug by preparation of solid dispersion using a hydrophilic polymer, poloxamer 188 (PXM). The kneading technique was used to prepare solid dispersions. A 3 2 full factorial design approach was used for optimization wherein the drug, polymer ratio (X 1 ), and the kneading time (X 2 ) were selected as independent variables and the dissolution efficiency at 60 min (%DE 60 ) and yield percent were selected as the dependent variable. Multiple linear regression analysis revealed that for obtaining higher dissolution of MLX from PXM solid dispersions, a high level of X 1 and a high level of X 2 were suitable. The use of a factorial design approach helped in optimization of the preparation and formulation of solid dispersion. The optimized formula was characterized by solubility studies, angle of repose, and contact angle; Fourier transform infrared spectroscopy, differential scanning calorimetry, x-ray diffraction studies, and scanning electron microscopy demonstrated that enhanced dissolution of MLX from solid dispersion might be due to a decrease in the crystallinity of MLX and PXM. Analysis of dissolution data of optimized formula indicated the best fitting with KorsemeyerPeppas model and the drug release kinetics as Fickian diffusion. In conclusion, dissolution enhancement of MLX was obtained by preparing its solid dispersion with PXM using kneading technique.

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“…Similarity factor (f2) was calculated utilizing Moore and Flanner independent mathematical approach to compare the dissolution profile (18).…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

Kneading Technique for Preparation of Binary Solid Dispersion of Meloxicam with Poloxamer 188

et al. 2009

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“…A value of n = 0.5 indicates case I (Fickian) diffusion or square root of time kinetics, 0.5 G n G 1 anomalous (non-Fickian) diffusion, n = 1 Case-II transport and n 9 1 Super Case-II transport. 19 Model independent approaches (ie, dissolution efficiency [DE]) 20 and mean dissolution time (MDT) 21 were used to translate the profile differences into a single value.…”

Section: E2mentioning

confidence: 99%

Use of hydrophilic natural gums in formulation of sustained-release matrix tablets of tramadol hydrochloride

2006

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The objective of this work was to develop matrix sustainedrelease tablets of highly water-soluble tramadol HCl using natural gums (xanthan [X gum] and guar [G gum]) as costeffective, nontoxic, easily available, and suitable hydrophilic matrix systems compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose [HPMC]/carboxymethyl cellulose [CMC] with respect to in vitro drug release rate) and hydration rate of the polymers. Matrix tablets of tramadol (dose 100 mg) were produced by direct compression method. Different ratios of 100:0, 80:20, 60:40, 20:80, 0:100 of G gum (or X):HPMC, X gum:G gum, and triple mixture of these polymers (G gum, X gum, HPMC) were applied. After evaluation of physical characteristics of tablets, the dissolution test was performed in the phosphate buffer media (pH 7.4) up to 8 hours. Tablets with only X had the highest mean dissolution time (MDT), the least dissolution efficiency (DE 8 %), and released the drug following a zero-order model via swelling, diffusion, and erosion mechanisms. Guar gum alone could not efficiently control the drug release, while X and all combinations of natural gums with HPMC could retard tramadol HCl release. However, according to the similarity factor ( f 2 ), pure HPMC and H 8 G 2 were the most similar formulations to Topalgic-LP as the reference standard.

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“…Similarity (f2) and difference (f1) factors were also calculated by the following equations Gohel et al, 2002).…”

Section: Discussionmentioning

confidence: 99%

Formulation and in-vitro bioequivalence evaluation of verapamil hydrochloride matrix tablets with Calan R

et al. 2014

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The purpose of the current work was to formulate Verapamil Hydrochloride (VH) sustained release matrix tablets by using natural polymers and comparison with leading national brand Calan SR of Searle Pharmaceuticals. Tragacanth and pectin were used in various concentrations. Pre compression studies i.e. angle of repose, bulk density, tapped density, Carrs compressibility index and Hausners ratio were also performed and found within the Pharmacopoeial limits. Eight formulations (F1-F8) of (VH) were prepared by direct compression method. Post compression studies i.e. Thickness, Hardness, Diameter, Friability and Dissolution studies were conducted. Different kinetic models i.e. zero order, first order, Highuchi model and Korsmeyer Peppas were applied to study release patterns and similarity index was calculated. Dissolution studies were carried out in phosphate buffer of pH 6.8 showed that formulations (F4 and F8) formulated with higher polymers concentration showed comparatively better drug retardation. F5 was the most comparable with the reference product. Verapamil hydrochloride released was observed non-fickian as diffusion following Higuchi model.DOI: http://dx.doi.org/10.3329/icpj.v3i6.18761 International Current Pharmaceutical Journal, May 2014, 3(6): 286-290

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Novel Use of Similarity Factorsf₂andS_dfor the Development of Diltiazem HCl Modified-Release Tablets Using a 3²Factorial Design

Cited by 54 publications

References 19 publications

Kneading Technique for Preparation of Binary Solid Dispersion of Meloxicam with Poloxamer 188

Kneading Technique for Preparation of Binary Solid Dispersion of Meloxicam with Poloxamer 188

Use of hydrophilic natural gums in formulation of sustained-release matrix tablets of tramadol hydrochloride

Formulation and in-vitro bioequivalence evaluation of verapamil hydrochloride matrix tablets with Calan R

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