Ranitidine HCl matrix floating tablets were formulated to release 90% of drug in stomach within 12 h. Hence, release of the drug could be sustained within narrow absorption site. Moreover, the dosage form was found to be floating within a fraction of second independent of the pH of media ensuring a robust formulation.
Over the last three decades, various approaches have been pursued to increase the retention of an oral dosage form in the stomach, including floating drug delivery systems (FDDS), swelling and expanding systems, bioadhesive systems, modified shape systems, high-density systems and other delayed gastric emptying devices (1). FDDS are widely explored for gastroretention purposes and have a bulk density lower than gastric fluids and thus remain buoyant in the stomach without affecting the gastric emptying rate for a prolonged period of time. While the system is floating on gastric contents, the drug is released slowly at a desired rate from the system (1, 2).Sodium alginate (SA) is a widely used natural polymer in various drug delivery systems. It exhibits favourable biological properties such as non-toxicity, biocompatibility, biodegradability and ulcer healing traits. Moreover, gelation of dilute solutions of SA occurs on addition of di-and trivalent metal ions by a co-operative process involving consecutive G-residues in the a-L-guluronic acid blocks of the alginate chain in a manner described by the 'egg-box' model (3). The procedure by which gelation is achieved is similar to the previously reported in situ gelling formulations of sodium alginate (4, 5).H 2 -antagonists or proton pump inhibitors are clinically used in treating chronic conditions like peptic ulcer and reflux oesophagitis. H 2 -antagonists competitively inhibit his- In the present work, a gastroretentive in situ gelling liquid formulation for controlled delivery of ranitidine was formulated using sodium alginate (low, medium and high viscosity grades), calcium carbonate (source of cations) and ranitidine. Prepared formulations were evaluated for viscosity, buoyancy lag time and buoyancy duration, drug content and in vitro drug release. Formulation variables such as concentration of sodium alginate, calcium carbonate and drug significantly affected the formulation viscosity, floating behavior and in vitro drug release. Analysis of the release pattern showed that the drug release from in situ gel followed a diffusion mechanism.
Abstract. In the present investigation, hydrogenated cottonseed oil (HCSO) was evaluated as a sustained release matrix for a freely soluble drug, tramadol. Hydrophobic matrix tablets of tramadol, was evaluated by compression of physical mixture of drug and wax, dispersion of drug in HCSO by hot fusion or solubilisation techniques. The method of preparation of tablet had a significant effect on drug release with higher release observed from direct compression matrices and slower release from matrix prepared by dispersion (hot-fused matrices). Influence of addition of hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose, polyethylene glycol 4000 and surfactants like sodium lauryl sulphate and polysorbate 20 to HCSO matrix on drug release was investigated. The added excipients exhibited a propensity to enhance drug release from the HCSO matrix. NaCMC was effective at a lower ratio (<10% w/w) and when incorporated at higher level made HCSO matrix to erode and disintegrate in a short period.
A rapid and sensitive RP-HPLC method with UV detection (262 nm) for routine analysis of adefovir dipivoxil in bulk and in pharmaceutical formulation was developed. Chromatography was performed with mobile phase containing a mixture of acetonitrile and phosphate buffer (50:50, v/v) with flow rate 1.0 mL min-l. In the range of 5.0-100 µg/mL, the linearity of adefovir dipivoxil shows a correlation co-efficient of 0.9999. The proposed method was validated by determining sensitivity accuracy, precision, robustness stability, specificity, selectivity and system suitability parameters.
Aim of the work: The present study was aimed to investigate matrix-forming property of gum olibanum for sustained-release tablets of tramadol, a freely water-soluble drug. The possible synergistic effect of gum olibanum with hydroxypropyl methylcellulose (HPMC) and xanthan gum, and widely used pharmaceutical excipients on tablet properties was investigated. Methods: Matrix tablets were prepared containing polymers, either alone or in combinations, by wet granulation. Tablets were evaluated for their physico-mechanical properties, drug release and hydration properties. Results: Tablets swelling increased till ~3-4 h this was followed by a decline phase. Drug release from the matrix tablets was dependent on the concentration of gum olibanum. Formulation with drug: gum olibanum in 1:2 released 94.37±2.37% drug in 6 h. The drug release data was analyzed by model dependent and model independent equations. Combination of gum olibanum with HPMC or xanthan gum matrices significantly (p<0.05) modulated drug release, which was reflected by the mean dissolution times (MDTs). Incorporation of lactose induced faster drug release compared to dicalcium phosphate and microcrystalline cellulose. Drug release largely followed first-order kinetics and non-Fickian type of diffusion.
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