Current Issue : July - September Volume : 2014 Issue Number : 3 Articles : 6 Articles
Duloxetine hydrochloride is an approved treatment option for fibromyalgia since 2004. But it has 2 hr lag time and low bioavailability. The objective of present work was to develop sublingual film of Duloxetine hydrochloride to provide quick relief in fibromyalgia. Film was prepared by solvent casting method using PVA as hydrophilic polymer and PEG-400 as plasticizer. Various batches were prepared with different concentrations of polymer and plasticizer. The formed films were evaluated for physical characteristics, thickness, weight, surface pH, disintegration time, tensile strength, folding endurance, drug content, in-vitro dissolution profile, ex-vivo permeation and stability. A thin and transparent film, formed by casting a solution containing 3% w/v polymer and 2.5% w/v plasticizer, showed disintegration time of about 437 seconds and higher in-vitro drug release (97.23 in 7 min). Ex-vivo permeation study of optimized batch exhibited that 92.16% drug was permeated in 8 minutes. The optimized batch showed good folding endurance and by tensile strength (332 gm/mm2). Accelerated stability study confirmed that batch was stable at ambient conditions of storage....
Prazosin, an antihypertensive drug undergoes hepatic metabolism so it has low bioavailability. Bioavailability of prazosin may be improved by buccal route. The objective of this work was to develop bioadhesive buccal tablets for the delivery of prazosin. Tablets were prepared by direct compression method. Screening of different bioadhesive polymers and penetration enhancers was done based on bioadhesion strength and ex-vivo diffusion. Optimization was done by 32 factorial Design. Different concentration of HPMC K4 and sodium deoxycholate were considered as independent variables. Bioadhesion strength, in- vitro release and ex-vivo release were considered as dependent variables. Optimized batch containing 40 mg HPMC K4 and 5 mg sodium deoxycholate was studied for weight variation, friability, content uniformity, surface pH, swelling index, bioadhesion strength and in-vitro and ex-vivo studies. Bioadhesion and ex-vivo studies were carried out using goat buccal mucosa. All the parameters of optimized batch were found to be in range. Surface pH was 6.91±0.01 which suggested that the formulation was non-irritant to the buccal environment. Swelling index was increased up to 73.31% at 9 h. Bioadhesion strength was found to be 27.44 g/cm2. % In-vitro drug release and Ex-vivo diffusion were found to be 92.28% and 66.49% at 12 h respectively. This result demonstrated that Prazosin tablets released drug in sustained manner....
Decitabine is a class II drug used in treatment of myeloid leukemia. Generally it is an unstable drug and requires\r\nstringent storage conditions. The objective of the study was to formulate a stable injectable dosage form containing decitabine\r\nand evaluating the injectable dosage form. For this purpose preformulation study of the drug was carried out using lactose,\r\nmannitol, dihydrogen potassium phosphate and other key excipients. Lyophilization technique was employed for the\r\nformulation of the injection, initially the drug was formulated as such with water for injection without any excipients and it was\r\nobserved that the cake characteristics of the lyophilized product were not good due to the less solute content, in order to\r\nincrease the bulk of the formulation the drug was formulated by using various excipients such as anhydrous lactose, lactose\r\nmonohydrate, mannitol. These lyophilized formulations were subjected to various evaluation parameters such as reconstitution\r\ntime, pH and percentage of water content, drug content and short term stability studies. It was observed that the selected\r\nformulation containing mannitol as bulking agent showed the promising results with 99.1 percentage of drug content even after\r\n3 months of stability studies passing all the vital evaluation parameters by maintaining integral cake appearance. From the\r\nresults it was concluded that the lyophilization technique proves to be an advantage for development of stable injectable dosage\r\nform and the identified formula F3 as the best for the treatment of myeloid leukemia....
The aim of present work is to develop floating osmotic tablet (FOT) for controlled release of losartan potassium that deliver drug at zero order over prolong period. The objective of investigation was to formulate a FOT for controlled release of losartan potassium which is useful for treatment of the hypertension by maintaining the plasma drug concentration above the minimum effective concentration. Tablet formulation was carried out by wet granulation technique and before that preformulation study of the drug was carried out. Various factor affect on drug release of losartan potassium from FOT, among them concentration of polymer, osmotic agent and sodium bicarbonate were selected as the independent variable for optimization of the formulation by box-behnken design. From in vitro dissolution and buoyancy study T50, Q12 and floating lag time were selected as the dependent variable (Y). By the help of DE® 9.0.1.0 software the optimized batch was found out. SEM study of the optimized batch was performed which showed the orifice size was around 500 μm. Release kinetic model were applied to the optimized batch which showed the formulation follow zero order drug release with anomalous transfer because R2 of zero order plot was 0.989 and n of korsmeyer peppas model was 0.862 which was less than 1. Stability study of optimized batch was performed at 40°C/ 75% RH up to 1 month and there was no stability problem reported....
Selegiline have poor brain uptake due to its poor aqueous solubility, so the study aimed to develop its microemulsion formulation to enhance the solubility and to accomplish the intranasal delivery of the drug to brain. Selegiline microemulsion (SME) was prepared using 1% labrafil M 1944 CS as oil, 25% tween 80 as surfactant and 25% transcutol P as co-surfactant by titration method. Pseudo ternary phase diagram was constructed to determine the microemulsion existing zone. Optimized microemulsion was characterized for their % transmittance, globule size, zeta potential and viscocity. Mucoadhesive microemulsion containing Selegiline (SMME) was prepared using chitosan in different concentrations. Nasal ciliotoxicity studies were carried out for SME and ME 3 using sheep nasal mucosa. Developed formulations were subjected for stability study as per the ICH guidelines for one month. Drug release from the formulations was carried out through excised sheep nasal mucosa using modified franz diffusion cell. The optimized SME was transparent with mean globule size 54.57 nm and zeta potential +21mV and PDI of 0.180. Stability study revealed that SME and ME3 were stable for 1 months. Microscope investigation revealed no marked damage on the sheep nasal mucosa after nasal application of SME and ME 3 for 1hr. Ex-vivo release study was performed of the optimized batch for 8 hrs. Transmission electron microscopy was performed and the image showed spherical globule with size of 72.85 nm. Based on the results, ME3 and SME were stable and can target the drug to brain through intranasal route and thus can play as an alternative for conventional dosage form....
Quinapril is the drug, in the series of angiotensin converting enzyme (ACE) inhibitors used in cardiac ailments. Since\r\nquinapril has a short half-life, consecutive doses have to be administered. Formulating quinapril as a controlled release dosage\r\nform can minimize this disadvantage. In the present study a total of 14 formulations were studied and characterized on basis of\r\nbuoyancy and lag time. Among all the formulations F14 showed lag time of 0 minutes and remained floating for >24 hrs. Thus\r\nthe formulation F14 was further investigated for formulation of quinapril floating tablets using suitable design. The effect of\r\nindependent variables on quality determinant parameters in a formulation was studied using 22 factorial design. The drug: total\r\npolymer ratio was considered as factor A and carbopol: ethyl cellulose ratio was considered as factor B. Diffusion coefficient and\r\ntime required for 50% of drug release was considered as the response variable. The regression statistics and ANOVA for\r\nresponse variable diffusion coefficient were calculated. From the ANOVA it is observed that the ââ?¬Ë?Fââ?¬â?¢ value is greater than\r\nââ?¬Ë?significance Fââ?¬â?¢ value indicating the model significantly predicts the effect of considered factors. From the regression statistics\r\npolynomial equation was derived. By utilizing the polynomial equations obtained the optimized formulation and their\r\ndesirability were calculated. The formulation with maximum desirability was chosen as the optimized formula....
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