Current Issue : October - December Volume : 2012 Issue Number : 4 Articles : 10 Articles
Azithromycin is a macrolide antibiotic that has been used for more than a decade to treat urinary tract, bronchial tract, lungs and sinuses infections. The unique pharmacokinetics of Azithromycin-rapid absorption and extensive distribution in tissue allows for short 3-day (500 mg/day for 3 days) or 5-day (500 mg on day 1 followed by 250 mg on day 2-5) course of therapy. The aim of present work was to formulate sustained released azithromycin microsphere by varying drug polymer ratio with different solvents in emulsion solvent evaporation technique to reduce the problem related to drug like insoluble in water, bitter taste and gastrointestinal side-effects. Comparative evaluation of microspheres was done by determining bulk density, tapped density, Hausner ratio, angle of repose, particle size, drug loading, in-vitro dissolution study and kinetic study....
The present investigation was mainly focused on the development of controlled release pellets of verapamil HCl with ethyl cellulose and hydroxylpropyl methyl cellulose phthalate by employing fluid bed coating technique. Ethyl cellulose 7cps a high viscosity grade controlled release polymer was mainly used as coating agent for regulating the drug release from pellets. HPMCP, an enteric coating polymer was used in the present study to regulate the drug release at varied G.I pH conditions. An attempt was made to optimize the composition of these two polymers to achieve the controlled release of drugs from the pellets. HPMC E5 was used a film former in the present investigation. Croscaremellose sodium was used as disintegrant to create channels in the coating for drug release. Povidone was used as binder to achieve uniform drug layering in the present investigation. The drug release rate decreased as the concentration of ethyl cellulose polymer increased. It was observed that increase in the concentration of polymers ethyl cellulose and resulted in delay in the drug release. The increase in the HPMCP polymeric concentration in formulations showed initial delay in drug release....
Sodium alginate has been used for sustained delivery of several drugs since last few decades. In this work, an attempt has been made to formulate and characterize alginate beads along with additional blended polymers (Hydroxypropylmethylcellulose K100M, Hydroxypropylmethylcellulose E10 Premium, Eudragit L100 and Eudragit S100) in order to evaluate the effect of the added polymers on the drug release profile and other physicochemical characteristics of the alginate beads. Ofloxacin has been used as a model drug, which has a t1/2 of about 5-8 hours and is a broad spectrum antibiotic. The beads have been formulated by simple ionotropic gelation method and have been evaluated subsequently by various physicochemical characterization methods. The in-vitro drug release profile showed that there was an initial burst release for all the formulations with or without the additional polymers and thereafter sustained drug release for more than eight hours in phosphate buffer pH 7.2. Among the different additional polymers used, Hydroxypropylmethylcellulose K100M was found to affect the drug release significantly and gave the best release profile releasing about 62% drug in 8 hours....
Tamsulosin is an a1-adrenoceptor antagonist used for the treatment of lower urinary tract symptoms that are suggestive of benign prostatic hyperplasia. It is mostly used in modified-release (MR) formulations. This study was performed to assess the effect of food on the pharmacokinetics of two tamsulosine products in healthy subjects. A randomized single dose (0.4 mg capsules), two-way crossover study was performed in a fasting state or after a high-fat breakfast. Prior to the in vivo study, an in vitro comparative dissolution test was performed. Level A IVIVC was assesed to serve as a surrogate for in vivo bioavailability and to support biowaivers. The plasma samples drawn from the volunteers were analyzed utilizing a sensitive LC-MS-MS method and the bioequivalence between the two drug products was assessed by statistical analysis of the log transformed mean ratios of Cmax, AUC(0-t) and AUC(0-8). There were no serious or unexpected adverse events during the course of this study, with most events reported in comparable numbers of fed and fasted subjects. The bioequivalence of tamsulosine was similar with or without food, with 90% confidence intervals of 91% to 124.4 %, 86.7% to 123.6% and 84.2% to 124.7% for ln (Cmax), ln (AUC 0-48) and ln (AUC0-8), respectively. The fast state study showed a significant higher Cmax associated with insignificant shorter Tmax compared to the fed results (p<0.05). Level A IVIVC showed good point-to-point relationship in both fast and fed state for test and reference products with regression coefficient of 0.96 to 0.98 and 0.99, respectively....
The Ropinirole Hydrochloride is a non-ergoline dopamine agonist with high relative specificity and full intrinsic activity at the D2 and D3 dopamine receptor subtypes. This action in humans correlates with treatment for Parkinson’s disease due to stimulation of postsynaptic dopamine D2-type receptors. Ropinirole Hydrochloride after oral administration shows a lesser bioavailability up to 55% and biological half life of 4 to 6 hours. So, present investigation deals with formulation and evaluation of buccal tablet of Ropinirole Hydrochloride. Ropinirole Hydrochloride buccal tablets were prepared by wet granulation method using Polycarbophil and HPMC K15M as mucoadhesive polymers. A 32 full factorial design was applied to investigate the combined effect of concentration of Polycarbophil (X1) and concentration of HPMC K15M (X2). Results of the multiple regression analysis revealed that the independent variables significantly affected the dependent variables (Q7(%), Mucoadhesive strength (gm) and Swelling index). An optimized formulation F6 was found to have good mucoadhesive strength 6.805 ± 0.12 gm, swelling index 106.00 ± 0.03 after 8 hr; mucoadhesive residence time was found to be more than 8 hr and cumulative percentage drug release 98.44 ± 1.47 within 8 hr. Release kinetic model studies indicated that optimized batch followed diffusive mechanism with Zero order release kinetics....
Cefuroxime Axetil (CFA) is one of the most widely prescribed third generation cephalosporin comes in BCS classification as ClassII drug (i.e. High permeability and Low solubility) which has a wide range usage in various diseases. The half life and the bioavailability is poor. These parameters encouraged developing a gastroretentive floating microspheres delivery system for Cefuroxime Axetil. In this study we prepare floating microspheres by emulsion diffusion technique using Eudragit S100 and HPMC with Glycerin Monostereate as wall reinforcing agent and evaluate for compability, morphological and dissolution studies the study also concluded that the microsphere with good entrapping capacity and morphology can be prepared with improving the half life, bioavailability and dissolution rate....
Sustained release microspheres offer advantages like limiting fluctuation within therapeutic range, reducing side effects and improving patient compliance. These also enhance therapeutic efficacy as well as bioavailability of the drug. In the present work ethyl cellulose was used as polymer for formulation of microspheres of antipsychotic agent paliperidone. Emulsion solvent diffusion technique was employed for preparing microspheres by using liquid paraffin as a continuous phase. The prepared microspheres were evaluated for production yield, particle size, drug content, encapsulation efficiency, surface morphology and in vitro drug release. Dissolution study revealed drug release from the microspheres was affected by drug-polymer ratio....
Suppositories are spherical shaped solid dosage form of medicament meant for insertion into body cavities other than mouth. They are generally intended for use in the rectum, vagina, and to lesser extent, the urethra. Metronidazole is the FDA-approved drug for clinical use for the treatment of vaginal infections either alone or in combination with other antibiotics. Metronidazole is absorbed rapidly following oral administration producing peak plasma concentration within 1-2 hours with100% bioavailability. Elimination half life is 6-7 hours and is usually administered in a dose of 200-500 mg in order to maintain effective concentration throughout the day. So the present work involves use of suppositories which has no first pass effect. This will ensure minimum fluctuations in the plasma drug concentration and reduced dosing frequency which will result into improved patient compliance. The objective of the work is to Formulate and evaluate the Metronidazole containing cocoa butter suppositories, to study the effect of different surfactants and different concentration of individual surfactants on the drug release behavior. To perform stability studies as per ICH guidelines. The study has shown that different physical properties and release rates depends up on the formulation contents Tween 80, SLS and Span 20 at various levels are used for formulation studies. From the results it was conclude that Twee 80 has shown a considerable increase in disintegration and dissolution behavior and Sodium lauryl sulphate 2% has shown a good sustaining property for a period of 12 hours....
The cellulose was modified by using 2-fluoro benzoylchloride by base catalyzed reaction. Modification of cellulose was confirmed by IR studies. The hybrid biodegradable composite films were developed by film casting method using modified cellulose with Poly (vinyl alcohol) and Poly (lactic acid) in different compositions. Obtained films showed better biodegradability, barrier properties and higher mechanical properties. It was observed that, these properties increases as the percentage of modified cellulose increases. This indicates the importance of modified cellulose as a reinforcing agent. After analyzing these properties of film composites, we came to conclusion that these biocomposites can be used for membrane and packaging applications....
Pioglitazone is a class II BCS drug having poor water solubility, slow dissolution rate and hence it may have negative impact on its bioavailability. Sub therapeutic plasma drug level of this drug is observed due to poor water solubility and thus it may lead to therapeutic failure. In order to improve its solubility and thus dissolution rate cyclodextrin complexation technique was followed. Binary system of pioglitazone with β-CD and HP β-CD were prepared separately by kneading method and evaluated for various parameters. The IR spectra confirmed the formation of a complex in between drug and cyclodextrin. The complexes prepared with the molar ratio 1:2 (drug: complexing agent) offered better dissolution rare. Mouth dissolving tablets were prepared with such complexes by employing wet granulation technique .The tablets were subjected to various quality control tests .The tablets containing the superdisintegrating agent crosspovidone and Pioglitazone-HPβCD complex showed immediate disintegration and fast rate of drug release....
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