HPMC

ABSTRACTThe aim of the present study is to design and develop sustained release pellets formulations for Amlodipine besylate. Amlodipine is an oral antihypertensive agent, commonly used as calcium channel blocker for treating high blood pressure. It is frequently used to treat heart diseases like angina pectoris. The dose of Amlodipine in case of hypertension or angina initially 5 mg daily later adjusted to 10 mg daily by oral route. Amlodipine has a maximum solubility in acidic pH. Amlodipine has a high bioavailability ranging from 60 to 80 % and slow rate of elimination. Amlodipine besylate at different drug to polymer ratios were prepared by extrusion and spheronization technique. The influence of the proportion of the polymer on the release rate of the drug from the pellets was studied. The in-vitro release studies of pellets were carried out in 0.1N HCl for 12 hours. The studies indicated that the drug release can be modulated by varying the concentration of the polymer. Pellets were prepared and evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. Formulation was optimized on the basis of acceptable pellet properties and in-vitro drug release. The resulting formulation produced robust pellets with acceptable drug content and low friability. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer- Peppas, First-order and Zero-order to evaluate the kinetics and mechanism of the drug release.Keywords: Sustained release, Ethyl cellulose, HPMC, Pellets, Amlodipine besylate  

ABSTRACTThe present study deals with the formulation of fast dissolving films of vildagliptin that is used for the treatment of Diabetes. The concept of fast dissolving drug delivery emerging from the desire to provide better patient compliance and avoid first pass metabolism. In the present research work, various trials were carried out using film forming agents such as HPMC, Maltodextrine, Polyethylene alcohol, to prepare an ideal film. Solvent casting method was used for the preparation of films. The prepared films were evaluated for weight uniformity, drug content, film thickness, folding endurance. The in vitro dissolution studies were carried out using ph-6.8 phosphate buffer. This approach increase therapeutic efficiency of pharmaceutical actives by avoiding hepatic first pass metabolism, deliver drug molecule in control manner, enhance absorption and improves patient compliance Keywords: Fast dissolving buccal film, Vildagliptin, HPMC, Maltodextrine, poly-ethylene oxide, tween 80,  aspartame Glycerin Solvent casting method, In vitro drug release, Ex-vivo drug diffusion studies,

Darifenacin is a muscarinic M3 selective receptor antagonist, which is intended for symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may occur in patients with overactive bladder syndrome. Darifenacin extended release tablets were developed to overcome the inconvenience of multiple dosing per day that is necessary with the immediate release formulation. There is therefore a need of administrating darifenacin in an oral dosage form once or twice daily in the form of extended release tablets  provide therapeutically effective plasma concentrations of darifenacin for the treatment of overactive bladder in humans. Therefore the present investigation concerned with the development of once-a-day darifenacin hydrobromide extended release tablets to extend the duration of action up to 24 hrs by controlling the dissolution rate using different viscosity grades of HPMC.

In present work calcium alginate (CA) microbeads encapsulated clonidine hydrochloride was prepared by ionotropic external gelation method in which calcium chloride used as cross-linking agent. Clonidine hydrochloride is a sympatholytic centrally acting α2 adrenergic agonist and imidazoline receptor agonist used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, migraine, and menopausal flushing but it have very short half life which required some new approach which help to retain it in the body for longer period of time. Calcium alginate microbeads represent a useful tool for oral sustained/ controlled drug delivery. The prepared alginate beads were studied for percent loading efficiency, average particles size, shape and surface morphology, Differential Scanning calorimeter (DSC) and drug release behavior. Chitosan and HPMC incorporated in addition to overcome rapid drug release at higher pH due to its high porosity. Prepared optimized alginate microbeads formulation found to be 356.22±8.1nm average in size, 86.46±2.6% entrapment efficiency. DSC and FT-IR confirm no interaction with the polymers used in the formulation. High concentration of polymer and CaCl2 increase the drug loading efficiency while high concentration of CaCl2  also retard the release of clonidine hydrochloride from the beads. The shape and surface morphology was determined by scanning electron microscopy (SEM) and found the beads in smooth and spherical in shape. In-vitro release study showed that microbeads release 97.85 % drug in 7 hr which was pH dependent and also due to swelling and surface erosion. Microbead release the drug which follow Higuchi matrix diffusion release kinetic. Finally it is concluded that alginate, HPMC and chitosan in combination can be used to prepare microbead to encapsulate clonidine hydrochloride in higher amount. Biodegradable and non toxic nature of polymer make the prepared microbeads suitable for oral administration. 

In the present investigation, an attempt has been made to increase therapeutics efficacy, reduce frequency of administration and improve patient compliance by developing sustained release gastro retentive floating tablets of Captopril using hydrocolloids like hydroxy propyl methylcellulose and Carbopol 934P by effervescent technique using direct compression method. In tablets formulations sodium bicarbonate and citric acid using gas generating agent and HPMC different grade was used to retard the drug release for 24 hrs in stomach. The prepared Gas powered tablets were subjected to post-compressional parameters. Drug compatibility with excipients was checked by DSC and FTIR studies. The stability study conducted 3 months as per the ICH guidelines. In all the formulations, hardness test indicated good mechanical strength, friability is less than 1% indicated that tablets had a good mechanical resistance. The results were revealed that as concentration of HPMC increases there is increase in floating time but release of the drug from all the formulation shows the slow release of Drug, as the concentration of sodium bicarbonate increases there is quick release of drug from all the formulation but the floating time decreases as the concentration of sodium bicarbonate increases so the optimum concentration of HPMC and Sodium bicarbonate is essential in order to achieve good result with respect to both drug release as well as floating time and floating lag time. It has been concluded that Formulation F1 and F4are the excellent formulation as they shows excellent drug release for 24 hrs with minimum floating lag time and more total floating time.