Development and in vitro Evalution of New Generation Superporous Hydrogel Beads (SPHBS) Containing Fluconazole

The preparation of superporous hydrogels based beads (SPHBs) with various concentrations of polymers such as guar gum,sodium alginate and hydroxy propyl cellulose combination. The superporous hydrogels beads containing carbonate salt, as a gas-forming agent, were prepared by dispersing carbonate salt in polymers solution and then extruding into either neutral or acidified solution of calcium chloride and citric acid. Acidity of gelation medium increased the pores in the structure of beads containing sodium bi carbonate. This is due to carbon dioxide generated from reaction of carbonate salts with citric acid. The effect of selected factors, such as polymer combination, per-centage of sodium bi carbonates, per-centage of citric acid and per-centage of calcium chloride. The characterization studies were performed by measurement of apparent density, porosity, swelling studies, mechanical strength studies, particle size, fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM) and differential scanning calorimetry (DSC). INTRODUCTION Fluconazole is a 1,2,4-triazole based drug that has established an exceptional therapeutic record for Candida infections, including oropharyngeal and esophageal candidiasis, vulvovaginal candidiasis, candidemia, and disseminated candidiasis. It is an antifungal agent of choice for the treatment of infections by Candida albicans and Cryptococcus neoformans due to its potent activity, excellent safety profile, and favorable pharmacokinetic characteristics. Hydrophilic polymers based hydrogels are cross-linked, with a network structure, which are able to absorb large amounts of water, and are water insoluble. For the pharmaceutical purpose they are distinctive carriers for controlled drug delivery, release control can be governed by both swelling and biodegrading properties. The swelling properties of hydrogels are mainly related to the elasticity of the network, the presence of hydrophilic functional groups in the polymer chains, the extent of cross-linking, and porosity of the polymer. The physical char-acteristics of hydrogels including their swelling ratio also depend on the balance between attractive and repulsive ionic interactions and solventmediated effects. due to their high water affinity and biocompatibility, hydrogels based on poly (acrylic acid) and its derivatives, chitosan, 12 alginate and collagen, have attracted the attention. However, these nonporous hydrogels swell slowly and exhibit low loading capacities, which restrict their use in effective drug delivery. A new generation of hydrogels, which swells and absorbs water very rapidly, has been developed. Examples of this new generation are superporous hydrogels (SPHs), which swell to equilibrium size in a short period of time.. Several important properties of SPHs, such as fast swelling, large swelling ratio, and surface slipperiness, make them an excellent candidate material to develop gastric retention devices. Due to poor mechanical strength of conventional SPHs (CSPHs), they are difficult to handle without breaking. The scope of the present study was to investigate the influence of some processing parameters on size and shape of alginate beads containing theophylline as a model drug, prepared by ionotropic gelation. MATERIAL AND METHODS Fluconazole gife sample obtained from Ranbaxy (M) Sdn Bhd (Sungai Petani,Malaysia).Guar gum, HPMC and calcium chloride purchesed from R&M Chemicals (Rssex.UK). Sodium Alginate were supplied from A.R Alatan Sains (K) Sdn Bhd (Malaysia). Sodium bi carbonate and citric acid from Bendosen Laboratory Chemicals. All other chemicals were used of AR grade . Preparation of internal phase The internal phase was prepared by homogination (table 1). Required quantity of polymers (guar gum, HPMC and sodium alginate) were added subsequently 50 ml of deionized water in a beaker, keep the mixer for swelling 24 hours followed by fluconazole and sodium bi carbonate added to the above mixers with glass rode with care. Preparation of external phase For the preparation of external phase (citric acid and calcium chloride) were added to the 50 ml of deionized water in a 100 ml beaker with continuous stirring. Preparation of drug-loaded SPHBS The drug-loaded superporous hydrogel beads were prepared by injection. The internal phase injected to the external phase with the help of 5 ml syringe (Needle size 0.50×25mm) the Jaraja Kumar et al /J. Pharm. Sci. & Res. Vol.5(12), 2013, 259 264