Current Issue : October - December Volume : 2015 Issue Number : 4 Articles : 9 Articles
Exploration of sintering concept in the pharmaceutical science is relatively recent. The objective of this study was to investigate the release characteristic of matrix tablet consisting of a hydrophobic polymer and aceclofenac for sustain release formulation using different sintering techniques. Aceclofenac is a NSAID is an ideal candidate for designing sustaining drug formulation due to its frequent dosing and short biological half-life (4 hr). The aceclofenac tablet was prepared by using different polymers by direct compression method. The sintering of tablet was done by using different techniques like thermal sintering and microwave sintering. The sintered tablets were tested for weight variation, content uniformity, hardness, friability and in-vitro dissolution study. The sintered tablets showed more strength than unsintered tablet and sintered tablet show less drug release than the unsintered tablet. It can be concluded that as sintering time and temperature increases drug retardation also increases....
Every medicinal product is a combination of drug substance and various excipients which are indispensible components comprising the greater proportion of dosage unit. Therefore, the knowledge of the composition, function and behavior of excipients is important for the successful design, development and manufacturing of pharmaceutical dosage form. In present work the effect of four different diluents namely starch, microcrystalline cellulose, mannitol and calcium sulphate dihydrate on the release of theophylline from an immediate release tablet has been studied. The physicochemical properties such as hardness, thickness, friability, uniformity of weight and the drug content of the formulated tablets and in- vitro drug dissolution study were evaluated....
The present study aims at the formulation and evaluation of orodispersible tablets (ODTs) containing tadalafil self emulsifying system (SEDDS) loaded on Neusilin® US2 carrier. The study included the investigation of different binders and disintegrants to promote the formation of a tablet with fast disintegration and suitable hardness. The ODT tablet of choice was compared to hard gelatin capsule and market product. Direct compression method was adopted. Seven different binders were evaluated to determine the one obtaining the highest hardness. Afterwards, four different disintegrants were investigated at 5% addition. The tadalafil SEDDS was loaded on Neusilin® US2 at a ratio of (3:1) SEDDS liquid to carrier. The solidified SEDDS was then mixed geometrically with different binders. The binder of choice was further tested with 5% different disintegrants. ODTs were evaluated for thickness and weight variation, hardness, friability, disintegration and wetting test and in vitro drug release studies. The optimized ODT in-vitro release was compared to hard gelatin capsule containing solidified SEDDS and market tablet. The best ODT was prepared using microcrystalline cellulose (MCC) type 102 as a binder and croscarmellose sodium (Ac-Di-Sol) as a superdisintegrant. The disintegration time, thickness and weight variation of the tablet met the compendial limits. Hardness, friability and wetting time were acceptable. The in-vitro release of the ODT of choice was significantly faster than the capsule and the market tablet. MCC type 102 and Ac-Di-Sol were suitable excipients for the formulation of ODT containing solidified tadalafil SEDDS....
The objective of present study was to formulate and evaluate sustained release tablets of Eperisone hydrochloride. The matrix tablets containing eperisone hydrochloride 75 mg were formulated using release retarding polymers such as hydroxy propyl methyl cellulose (HPMC K4M), xanthan gum in combination with other standard excipients. The formulated tablets obtained by the direct compression method and were evaluated for physical characteristics viz, hardness, thickness, friability, percentage weight variation. The results of all the evaluation parameters were in the limits. Further, tablets were evaluated for in-vitro release characteristics for 12 hrs. Batches B1, B2 and B3 showed release 80.21%, 79.58% and 78.41% at 12th hr respectively. While, batch B4, B5 and B6 showed release 76.45%, 76.22% and 73.25% at 12th hr respectively. Release kinetics of all the batches was evaluated. The formulations B1, B2, B3, B4, B5 were followed Korsmeyer–peppas model, whereas B6 formulation showed zero order kinetics. The stability studies of the optimised formulation were performed as per ICH guidelines and were found to be stable. The designed eperisone hydrochloride sustained release matrix tablets have potential for sustained action of eperisone hydrochloride....
The aim of the present work was to formulate and evaluate an oral time controlled drug delivery system of doxofylline, based on chronotherapeutic approach for the treatment of nocturnal asthma. In this study, compression coated time release tablets of doxofylline were prepared by compression coating the core tablet using polymers HPMC K4M with EC in various proportions using RSM. The basic idea behind the dosage form development was to investigate effect of coating design on lag time and drug release from directly compressed time-controlled release tablet. The RSM was applied for optimization of the formulation. A 32 full factorial design was used in the present study. The amount of release retarding polymer HPMC K4M (X1) and amount of erodible polymer EC (X2) were selected as independent variables and the % CDR (drug release), lag time and hardness were considered as the dependant variables. The in-vitro drug release profile of the formulations was performed in 0.1 N HCl and pH 7.4 phosphate buffer. The desired lag time of 5 h was obtained for selected formulations and burst release was obtained after the lag time, which was consistent with the demands of chronotherapeutic drug delivery. The results were analyzed with the design expert software and predicted formulation ratios were obtained. Studies were carried out on the prepared optimized formulation to verify the theoretical prediction. The results were found to be within the range. The optimized batch gave a lag time of 5 hr and drug release of 98.9%. Using RSM, with few runs, effective chronomodulated drug delivery of doxofylline can be achieved....
A multiple-unit-type oral floating dosage form of loratadine was developed to prolong gastric residence time, target peptic ulcer and increase drug bioavailability. The purpose of present research work was to prepare calcium alginate beads containing water-soluble drug loratadine. A multiple-unit-type oral floating dosage form of loratadine was developed to prolong gastric residence time, target peptic ulcer and increase drug bioavailability. The floating bead formulations were prepared by dispersing loratadine together with calcium carbonate into a mixture of sodium alginate and hydroxypropyl methylcellulose solution and then dripping the dispersion into a solution of calcium chloride. Calcium alginate beads were formed, as alginate undergoes ionotropic gelation by calcium ions and carbon dioxide develops from the reaction of carbonate salts with acid. The evolving gas permeated through the alginate matrix, leaving gas bubbles or pores, which provided the beads buoyancy. The prepared beads were evaluated for percent drug loading, drug entrapment efficiency, buoyancy and in-vitro release. The formulations were optimized for different weight ratios of gas-forming agent and sodium alginate....
The aim of the present study was to develop a gastroretentive drug delivery system of lamivudine, an antiretroviral drug. The tablets of the active pharmaceuticals agent lamivudine were prepared by direct compression technique using HPMC K15M as a polymer with additional standard excipients. The assortment of sodium bicarbonate and citric acid was used as gas generating agent. Prelude studies established that the, tablets remained buoyant for over 15 hr in the dissolution medium. 32 factorial designs were used to thoroughly optimize the drug release profile. The amount of retardant material HPMC K15M (X1) and gas generating agent (X2) were chosen as independent variables. The time requisite for drug release t50% (Y1) was selected as dependent variable. The statistical analysis of the drug release data was done by multiple regression analysis using software microsoft excel and statplus 2008. Analysis of variance was performed using biostatplus to evaluate contribution of factors. The response surface plots were generated using table curve 3D V4. The resultant polynomial equations for t50% were demonstrated by two check point formulations, which expressed that factor X1 and X2 appreciably affects the studied dependent variable. The non fickian diffusion release transport was inveterate as the release mechanism for the optimized formulation. The predicated values approved well with the experimental values and the consequences demonstrated practicability of the model in the development of gastroretentive drug delivery system....
In all over the world, High levels of cholesterol or hypercholesterolemia are an important risk factor for coronary heart disease. The pivotal motif of the present research was to formulate the two drug in bilayer tablet in the form of immediate release and sustained release layer for better patient compliance. Immediate release layer was formulated by using the excipients like microcrystalline cellulose, crosscarmellose sodium (Ac-di-sol), sodium starch gycolate (Explotab) and sustained release layer was formulated using polymers and gum like HPMC E15, HPMC K100M - CR, xanthan gum. The disintegration and dissolution study of the entire bilayer tablet was studied. Kinetic studies of optimized Immediate release layer (IR3) and sustained release layer (SR10) showed good linearity with regression coefficient of 0.9855 (Higuchi model) and 0.9899 (Zero order), respectively. The above results reveal that optimized immediate release layer of ezetimibe (IR3) and sustained release layer of simvastatin (SR10) might be suitable for the treatment of hypercholesterolemia by sequential release of two drugs in a bilayer tablets....
The strain was procured from National chemical laboratory, Pune. The fermentation conditions were studied: fermentation period 4 d, pH 6.0 and temperature 28°C. Under these conditions, this strain produced 15.23 g/l of pullulan. The parent strain was mutated by ultraviolet irradiation and the fermentation conditions were studied with the mutants. Isolated polymer was characterized by fourier transform infra-red (FTIR) and antimicrobial activity was also studied. Drug release behavior of the polymer was evaluated from the prepared microsphere using donepezil HCl. Microspheres were characterized by FTIR, differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), Zeta potential, particle size and entrapment efficiency. The strain exposed under UV light of 25 minutes produced 22.06 g/l. FTIR spectrum is similar to that of standard pullulan. Isolated polymer of pullulan showed negative antimicrobial activity. Prepared microspheres showed almost similar drug release behavior to that of standard polymer. FTIR and DSC studies revealed that there is no interaction between polymer and drug. Prepared microspheres had particle size of 535.9 nm, zeta potential of −7.44 mV, entrapment efficiency 88.64% and cumulative drug release of 95.78% in 24 h....
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