Current Issue : January - March Volume : 2013 Issue Number : 1 Articles : 12 Articles
The purpose of this study was to formulate an Orodispersible tablet of Itopride Hydrochloride by direct compression method. It’s unpleasant taste and hence taste masked by ion exchange resin method which rapid onset of action, increased bioavailability and dual mode action of antiemetic and prokinetics. The tablets were made by direct compression method using Kyron T-314, Sodium starch glycolate, Crosscarmellose sodium and crosspovidone as superdisintegrant conc. 0.5%, 1.0% and 1.5% respectively and taste masking using ion exchange resin method kyron T-114 used as a taste masking ratio 1:1 to 1:4 and also by solid dispersion method. Characterization of DRC in which drug content, In vivo taste evaluation, In vitro drug release, drug- polymer interaction study and drug resin complex formation and also evaluations of the formulations were conducted including weight variation, hardness, disintegration time, friability and in-vitro dissolution. The DSC study showed complete disappearance of the Itopride peak confirming complex formation by ion exchange resin method. FTIR study revealed no interaction between drug and polymer. DRC drug: kyron T-114 (1:3) was optimized and the results show that the presence of a superdisintegrant kyron T 314 [0.5%] gives good result. DT 13 sec., drug content of 99.7 % & 98.83±0.9 % drug release within 10 min. and as compared with the conventional tablet (23.43±1.3%). Short term stability study of optimized formulation showed that formulation was stable. Orodispersible tablets of Itopride Hydrochloride with acceptable disintegration time, rapid drug release and good hardness and taste masked....
Nebivolol hydrochloride is a selective β1-receptor antagonist with antihypertensive properties having plasma half life of 10 h and 12 % oral bioavailability. In the present work transdermal matrix patches of Nebivolol hydrochloride were prepared to improve its therapeutic efficacy and to avoid its extensive hepatic first pass metabolism of the drug. Nine formulations using 32 full factorial design (composed of Hydroxypropyl methyl cellulose K15M and Eudragit RL100 at a ratios of 1: 1) containing 15% w/w triethyl citrate as plasticizer were prepared. HPMC K15M and Eudragit RL100 were taken as independent variables. Folding endurance, % moisture content, tensile strength, in vitro drug release and flux were taken as dependent variables. Compatibility between drug and polymer was accessed by Fourier transform infrared spectroscopy (FTIR). The prepared TDDSs were evaluated for physicochemical parameters and in vitro skin permeation. F7 formulation exhibit maximum drug release of 99.53% for 24 h due to its higher amount of hydrophobic polymer concentration. Formulation F5 was optimized on the basis of results of dependent variables. The short term accelerated stability study was carried out for the optimized formulation and results revealed that all dependent variables and other parameters were within acceptable limits. Skin irritation study on albino rats have not shown any sign of erythema or edema. Result of high f2 value showed similarity between in vitro drug release profile of reference and test formulation of before and after stability period. Thus, the prepared matrix transdermal film may prove to be a potential candidate to provide sustained drug release for 24 h....
Conventional tablet formulation has acquired the 50 to 60 % market stake. But with this tablet having acceptance problem in the patients suffering from dysphagia, Parkinson’s disease, mycosystis or vomiting, geriatric and pediatric patient because unwilling to take solid preparations due to fear of choking. From the patient point of view Fast dissolving film offers ease of administration and improved compliance. Research and development in the oral drug delivery system has led to transition of dosage forms from simple conventional tablets/capsules to modified release tablets/capsules followed by oral disintegrating tablet (ODT). Further development leads to formulation of wafer of which oral fast dissolving film (FDF) are most preferred. Since, review forms basis for research, current article exhaustively covers formulation aspects of FDF including natural and synthetic polymers as film formers. It also focuses on formulation methods like Solvent casting, hot melt extrusion, roller compaction etc. and technologies like FOAM BURST, SOLULEAVES, WAFER TAB etc. that have made products like Zofran, Listerine, Gas- X etc. popular in public domain. An important aspect of FDF is making new business opportunities available for the same drug. In the post GATT era, where patents of many high selling drugs are expiring, a lot of new opportunities can be created by incorporating the drug in a novel dosage forms....
Paclitaxel is an anticancer drug used in ovarian cancer, breast cancer and small cell lung carcinoma. The objective of the present investigation was to develop liposomal formulation of Paclitaxel. Dipalmitoylphosphatidylcholine (DPPC), Dipalmitoylphosphatidylglycerol (DPPG) and cholesterol were used to prepare Paclitaxel liposomes. Thin film hydration method was adopted for preparing Paclitaxel liposomes. FTIR study revealed no any interaction between drug and excipients and they were found to be compatible with each other. Drug content and percentage drug entrapment were selected for optimization of liposomal formulations of Paclitaxel. Maximum percentage drug entrapment was found to be 67.08%. Optimized Batch (F5) was characterized for various parameters such as drug content, percentage drug entrapment, particle size, zeta potential, Transmission electron microscopy and photo microscopic study. Optimized batch showed particle size 237.3nm and negative zeta potential -37.9 mV. In vitro drug release study of optimized formulation (F5) showed 41.12% of drug release after 48 h. It was found to be zero-order release. Formulation was stable at 2-8 oC after one month stability study. The result of optimized batch (F5) indicated that sustained release formulation of Paclitaxel could be formulated....
Ziprasidone Hydrochloride is one of the drugs of choice for the Psychosis. It has a half life of 8 h. The present investigation is concerned with the development of the fast dissolving tablets. Fast dissolving tablets of Ziprasidone hydrochloride were prepared by sublimation method. Ziprasidone hydrochloride showed maximum absorption at wavelength 317 nm in phosphate buffer pH 7.4. Various formulations were developed by using different concentration of superdisintegrant and camphor. The prepared batches were evaluated for pharmacotechnical parameter like hardness, friability, weight variation, in vitro disintegration time, wetting time, water absorption ratio, in vitro drug release studies, and stability studies. Drug-polymer compatibility studies by FTIR gave conformation about drug purity and showed no interaction between drug and selected polymers. All the formulations exhibited in vitro disintegration time below 57 seconds. From among all the developed formulations Z9 containing Cropovidone-6mg, Camphor-15mg showed minimum time to disintegrate (37 sec.) and almost complete release of drug within 30 minutes. The best formulations were found to be stable during stability studies done for one month. Thus, best formulations satisfied physico-chemical parameters, friability, wetting time, in vitro disintegration time and in vitro drug release profile requirements for fast dissolving tablets. Tablets of Ziprasidone HCl prepared with Crospovidone and Camphor were found to be acceptable in vitro disintegration time, water uptake, friability and in vitro drug release. Finally it was concluded that FDT of Ziprasidone Hydrochloride can be successfully formulated by sublimation methods....
The present work was aimed at formulating a solid dosage form system (tablets) for Trimetazidine dihydrochloride (TDH) using the principles of osmosis which will bring down its dosing frequency to once a day and at the same time produce a zero-order release system. A monolayer osmotic tablet was formulated by coating the core tablet (containing 60 mg of drug and osmogen) with a semi permeable membrane to permit the penetration of water and drilling an orifice which would permit the release of drug after development of suitable osmotic pressure. For formulating a monolayer osmotic tablet, initially core and coating feasibility trials were carried out to select the best formulation for optimization study. Optimization study of HPMC K4M, Carbopol 71G, Osmogen (Mannitol and sodium chloride) and coating composition was done by varying the proportion of each in various formulations (MT1 to MT20) and analysing the release profile kinetics. Comparison of the release profiles of each formulations was made with the theoretically calculated target release profile using the f1 (Difference Factor) and f2 (Similarity factor). Formulation MT20 was selected as the final optimized formulation for monolayer osmotic drug delivery system. It showed an almost perfect zero order release (r2 = 0.995) and almost 100 % release after 24 hours....
The aim of the current study was to design controlled porosity osmotic pump tablets of Rabeprazole sodium. The porous osmotic pump contains pore forming water-insoluble additive (Synthetic Hydrotalcite) in the coating membrane which after coming in contact with water is removed from membrane, resulting in an in situ formation of micro porous structure. The dosage regimen of Rabeprazole sodium is a 50-mg tablet once in a day. The plasma half-life ranges from 1 to 2 hours. Hence, Rabeprazole sodium was chosen with an aim to develop a controlled release system for 5 hours. The effect of different formulation variables, namely, ratio of drug to osmogent, membrane weight gain and level of pore former on the in vitro release was studied using 23 factorial designs. Ethyl cellulose was used as the semi permeable membrane. The effects of pH and agitation on drug release were also studied. Drug excipients compatibility was studied by FT-IR. The optimized formulation was subjected to stability study for one month period. It was found that drug release rate increased with the amount of osmogent because of increased water uptake, and hence, increased the driving force for drug release. Drug release was inversely proportional to membrane weight gain, however, directly related to the level of pore former in the membrane. Optimized formulation was found to deliver above 98% of drug (Rabeprazole sodium) at a zero order rate for 5 hours....
Irinotecan hydrochloride trihydrate is a drug of choice in the treatment of colon cancer. The purpose of this study was to investigate the anticancer activity of anticancer drug irinotecan hydrochloride trihydrate in maltodextrin based proniosomes towards human Colon cancer cell lines (SW-620). MTT (3-(4, 5-Dimethyl thiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay was used for quantitative measurements for the anticancer cell activity. Proniosomes of Irinotecan hydrochloride trihydrate were prepared by slurry method using different surfactants. The formulations were then characterized with respect to vesicle size. The size of the vesicles was in the range of 3.18±1.65 to 4.16±2.68 µm respectively. The findings of this study inferred that formulation PN5 showed better cytotoxicity effect with IC 50 value of 38 µg....
The blood-brain barrier (BBB) limits the distribution of systemically administered therapeutics to the central nervous system (CNS), posing a significant challenge to drug development efforts to treat neurological and psychiatric diseases and disorders. A growing body of evidence demonstrates that intranasal administration of a broad spectrum of therapeutics results in significant delivery to the cerebrospinal fluid (CSF), brain and spinal cord in animals and in humans. While the exact mechanisms underlying intranasal delivery to the CNS are not understood, olfactory and trigeminal nerves, which connect the nasal cavity and the CNS, clearly play an important role in direct delivery to the CNS. In addition, pathways involving the vasculature, cerebrospinal fluid and lymphatic system have also been implicated in the transport of molecules from the nasal cavity to the CNS. Combination of these pathways into the CNS is likely followed after intranasal administration and may be heavily dependent on the specific properties of the therapeutic as well as the composition of the nasal formulation. In the last decade, research efforts have focused on improving delivery efficiency and drug targeting to the CNS with the intranasal method by using a variety of formulations strategies including solution, nanoparticle, microspheres microemulsion and nanoemulsion....
Poly (d, l) lactide (PLA) based nanoparticulate carriers attracted pharmaceutical formulator for delivery of bioactive agents owing to its biocompatibility, biodegradability and outstanding controlled release characteristics. The objective of this study was the preparation, physico-chemical characterization and statistical optimization of size controlled PLA nanoparticles by modified nanoprecipitation technique. Preliminary experiments suggested that particle size as well as process yield of PLA nanoparticles were affected by number of formulation as well as process parameters. But it was difficult to identify critical quality attributes which significantly affect particle size and process yield amongst the large number of variables. Hence in current research attempts have been made to identify critical quality attributes by exploration of statistical screening design i.e. 27-4 fractional factorial design. Concentration of stabilizer i.e. tween 20 and type of external phase emerged as critical formulation parameters from the screening experiments. Hence, in further investigation a 32 full factorial design was used to investigate the combined influence of concentration of tween 20 (X1) and type of external phase (X2) on particle size (Y1) and process yield (Y2). The nanoparticles were also evaluated for particle size distribution and zeta potential. Statistically significant model were evolved to predict entrapment efficiency and particle size. The effect of factor X1, X2 and X12 were found to be statistically significant in nature. Response variables i.e. particle size and process yield were simultaneously optimized using desirability function using Design Expert software. This process allowed selection of most suitable level of factors to achieve desired level of particle size and process yield. The results of multiple linear regression analysis revealed that for obtaining desirable particle size (less than 150 nm) and process yield (more than 80 %), the nanoparticles should be prepared using 0.3 % w/v of tween 20 and water : ethanol (75: 25) as a external phase. In conclusion, results of the present study demonstrated that PLA nanoparticles with expected particle size and process yield can be obtained by adopting the concept of quality by design....
Till the date development of dosage form that improves bioavailability of drug with poor aqueous solubility is challenging task. Poor bioavailability problem associated with hydrophobic drug can be resolved by developing self-emulsifying drug delivery system (SEDDS). However most of self-emulsifying drug delivery system developed or published is either typical liquid dosage form or solid dosage form which presents some problems. As liquid dosage form shares some disadvantages, development of perfect solid self-emulsifying tablet dosage form is desirable. This review focuses on recent works published on different methods for development of solid self-emulsifying drug delivery system....
The present work was aimed for development and evaluation of monolithic polymeric patch for transdermal delivery of ondansetron hydrochloride at therapeutic level and prediction of in vivo performance in human from the ex vivo data across porcine ear epidermis. The monolithic matrix patch containing ondansetron hydrochloride was prepared by solvent evaporation technique using ethylcellulose (EC) and poyvinylpyrolidone (PVP) in varying proportins. The prepared patch was subjected to various physicochemical evaluations with respect to drug content, moisture content, moisture uptake, thickness and folding endurance. The ex vivo permeation of ondansetron was investigated across porcine ear epidermis using Keshary-Chien glass diffusion cell. The films were uniform with respect to drug content, thickness and with low moisture content and moisture uptake capacity. The DSC analyses confirmed the stability of ondansetron in the polymeric film. The SEM and XRD analyses confirmed that the drug was uniformly distributed in amorphous state. The permeation of ondansetron seemed to follow zero order kinetic by diffusion mechanism. The patch formulation having polymeric composition of EC:PVP at 1:1 with 15% w/w of lemon oil as permeation enhancer produced desired transdermal target flux of ondansetron hydrochloride at 179.93 µg/cm2/h. An area of 3 cm2 of patch would be required to deliver ondansetron at 26.2 ng/ml in human by transdermal route....
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