Current Issue : July - September Volume : 2015 Issue Number : 3 Articles : 8 Articles
Medicated chewing gums are solid, single-dose preparations that have to be chewed and not swallowed; chewing gums contain one or more active ingredients that are released by chewing. Drug absorbed directly, via the buccal membrane, avoids metabolism in the gastrointestinal tract and the first-pass effect of the liver. It might therefore be possible to administer a reduced dose in chewing gum compared to other oral delivery systems. In the present study six sets of coating formulations were prepared and studied. The coating solution was applied on uncoated chewing gum for six batches. Each coating on chewing gum was based on weight of uncoated chewing gum. This was applied in range of 40, 44, 48, 52, 56 and 60% with respect to weight of uncoated chewing gum. The dissolution curve for release of dichlorobenzyl alcohol and amylmetacresol for all six batches (AB1 to AB6) were compared. The drug release kinetics was calculated by dissolution curve. Formulation AB1 showed lowest drug release of 75.83% at the end of 30 minutes and formulation AB6 showed highest drug release of 91.72% at the end of 30 minutes. The formulation with lowest sensory determination was AB1 with acceptance of 40% and the formulation with highest sensory determination was AB6 with acceptance of 90%. As the concentration of the coating solution is increased in the coating formulation, the crunchiness was increased. It can be said that with varying the concentration of coating solution in the formulation, the crunchiness can be controlled....
The objective of the present study was to formulate a microemulsion system for ocular administration to improve the solubility and bioavailability due to efficient penetration of nano sized globules into the deep tissues of eye. Various formulations were prepared using different ratios of oils, surfactants and co-surfactants (S and CoS). Pseudo-ternary phase diagrams were constructed to evaluate the microemulsification existence area. The formulations were characterized by solubility of the drug in the vehicles, mean droplet size, zeta potential, drug content and in-vitro permeation study. The formulation was optimized using simplex lattice design and the optimal formulation consists of 12% Peceol, 14.66% Soluphor P, 29.34% Labrasol and 44% water (w/w), with a maximum solubility of Moxifloxacin up to ∼14.82 mg/ml. The mean droplet size of optimized microemulsion was 46.50 nm. The in-vitro permeation study result showed that percentage release of moxifloxacin from microemulsion vehicle was 93.72% in 1 hr. Our results indicated that the microemulsions could be used as an effective formulation for improvement in absorption, permeation and hence bioavailability and scale up flexibility....
The main aim of present research work was to formulate and evaluate chitosan based superporous hydrogel of simvastatin and to provide controlled release dosage form of by formulating gastric retention device. Simvastatin was chosen as good candidate for such system due to its narrow absorption window, low bioavailability and short half-life. SPHs were prepared by using chitosan and PVA (polymers), glyoxal (crosslinker), sodium bicarbonate (foaming agent), Span 80 (foam stabilizer). GAA and water were used to prepare chitosan and PVA solutions respectively. Direct addition method is used for drug loading. Suitable drug loading method was determined on the basis of drug content and in-vitro dissolution study. Optimized SPHs were evaluated for physical and mechanical properties like swelling ratio, geletion kinetics, density, viscosity, porosity, degradation kinetics, FT-IR spectroscopy, DSC. Direct addition method showed % drug release 95.31% with complete swelling of SPH. Results for optimized batch evaluation were found to be: The swelling ratio 3.70; after 90 min. at pH 1.2, gelation time; 29 sec., density; 0.41±0.003 g/cm3, viscosity; 210.1±4.75 cP, porosity; 89.77±4.83, degradation study; WRt of 0.037after 42 hr. Stability studies were carried out for 3 month as per ICH guidelines. There was no significant change in % drug release and other evaluation parameters. From above studies it can be concluded that the SPH of Simvastatin can be successfully formulated and evaluated....
Skin is the largest organ of the body which serves many functions. Because it is protective outermost layer of the body gets affected with environmental and microbial hazards. Some of the skin infections and disorders are difficult to treat and some reoccur because of insufficient treatment. Skin diseases of severe category can be treated by topical as well as systemic treatment using therapeutic agents. Any therapeutic agent given orally or by injection for the treatment of skin diseases will have more side effects than applied topically. This is the origin of this research. Salicylic acid and minocycline HCl are two drugs which are effective in the treatment of acne, dermatitis and fungal infections but failed to penetrate the skin effectively as both belong to BCS class III. Minocycline HCl is still under clinical trial for topical use. So this project was undertaken to design and develop better drug carrier system for these two drugs through skin. Liposomes are usually obvious answer but ethosomes may prove better, so the objectives decided for this study were: design, development and optimization of liposomal drug delivery for these two drugs; design, development and optimization of ethosomal drug delivery for these two drugs and compare liposomes and ethosomes with respect to % entrapment efficiency, vesicles size, skin penetration. During this research the liposomes and ethosomes were put into gel base and compared with marketed topical formulation (for salicylic acid). Since, there is no marketed formulation for minocycline HCl. 2% gel of minocycline HCl was prepared and compared with ethosomal and liposomal gel. In conclusion ethosomal drug delivery proved better than liposomal drug delivery with respect to skin penetration as well as % entrapment efficiency. Thin film hydration method proved better than other methods of liposomes and ethosomes preparation used....
The objective of the present investigation is to formulate multiparticulate gastroretentive dosage form of Nizatidine, a H2-receptor antagonist widely prescribed in gastric ulcers, duodenal ulcers. The short biological half-life (1 -2 hours), maximum absorption in initial part of small intestine, colonic metabolism of Nizatidine favors, development of gastro retentive floating dosage form. The present study involves preparation and evaluation of floating microspheres prepared by solvent evaporation and spray drying method using polymers HPMC and EC with Nizatidine as model drug for prolongation of gastric residence time. The drug-excipient compatible studies performed using FTIR and DSC and study revealed that there is no drug-excipient interaction. The central composite design was employed to evaluate contribution of HPMC: EC and SET: SDT technique on entrapment efficiency and percentage of drug release of floating microspheres. The prepared multiparticulate system were evaluated for various physicochemical parameters such as flow properties, in-vitro buoyancy (floating lag time, total floating time), swelling studies, drug content and in-vitro drug release. The shape and surface morphology of prepared microspheres were characterized by optical and scanning electron microscopy, respectively Size of the microparticle ranged from 5-20 μm expressing that microparticle are spherical and non-aggregated. As the mean particle size increased, the drug release rate decreased at higher polymer concentration. In this study it was found that spray drying was effective method to produce floating microparticles successfully without use of solvents like dichloromethane, which is a class II solvent or aromatic solvents like ethyl acetate. Microparticles were evaluated for buoyancy and drug release study using paddle type dissolution apparatus using pH 1.2 buffer as dissolution medium. The in vitro drug release pattern of Nizatidine floating microspheres was fitted to different kinetic models which showed highest regression for zero order kinetics with non fickian diffusion mechanism and prepared microspheres exhibited prolonged drug release (8 h) and remained buoyant for >10 h....
Nanoemulsions have received great attention for various applications including, dermal and transdermal drug delivery due to higher storage stability, ease of preparation, lower preparation cost, thermodynamic stability, permeation enhancement activity of their components and a high solubilizing capacity for various drugs over conventional topical formulation vehicles. So the aim of this study was to develop a nanoemulsion for transdermal delivery of lacidipine, as an antihypertensive drug, so as to avoid extensive first pass metabolism. Nanoemulsions containing 1% lacidipine were prepared using capryolTM 90 as oil, cremophor RH 40/ transcutolTM HP in the ratio of 3:1 as surfactant and co-surfactant respectively and assessed for visual inspection, pH measurements and droplet size analysis. In vitro permeation of lacidipine from nanoemulsion formulae through semi-permeable membranes was carried out and compared to lacidipine suspension. In all tested formulae, the permeation of lacidipine was at a higher rate than that from the suspension. N4 showed the highest permeation where 90.52±1.22% of lacidipine was permeated within 24 h....
The present study was to develop solid nanodispersed tablet formulation containing 4 mg of glimepiride for the treatment of Type II diabetes mellitus. Solid nanodispersions of glimepiride (GMP) were prepared using two different ratios of two different carriers and by adopting two different techniques. Solid nanodispersed tablets of glimepiride were prepared by compression of the prepared solid nanodispersions using direct compression method. The differential scanning calorimetry (DSC) analysis and Fourier transform infra-red (FTIR) analysis was conducted for the thermal behavior and surface structure characterization, respectively. The prepared solid nanodispersion and solid nanodispersed tablet were evaluated in terms of pre-compression and post-compression parameters, respectively. The DSC and FTIR studies revealed that there was no interaction between GMP and all the excipients. The resulted values of pre-compression evaluated parameters revealed that the prepared solid nanodispersions powder blends showed poor to excellent flow properties and with drug content ranged from 97.2±0.4% to 99.40.2%, with particle size ranged from 111.2±1.7 nm to 282.5±2.6 nm and with zeta potential ranged from -9.34±38.6 mV to -63.4±12.8 mV. The results of TEM analysis of formula (F6) showed spherically-shaped particles with particle size ranged from 650 nm to 850 nm. The resulted spectra of PXRD analysis of formula (F6) showed much reduced crystallinity of the homogenized form on comparison with pure GMP powder and with un-homogenized form of the same formula. The aqueous phase solubility study showed that, the increase in aqueous solubility was in the range of 2.4 folds for formula (F4) to 7.7 folds for formula (F6). The in-vitro dissolution studies of the prepared solid nanodispersions showed that, formulae F2 and F6 were released the highest quantity of drug. One way ANOVA for the percent of drug released from the prepared GMP-nanodispersion formulae (F1-F8) after 60 and 120 minutes showed significant differences between the percent of drug released from different GMP-nanodispersion formulae, (P<0.05). The disintegration time of the prepared nanodispersed tablets ranged from 140±18 seconds to 235 ±12 seconds. The drug content was be in the ranged of 99.9±0.2% for F8 to 96.9±0.7% for F4 and the weight variation indicated that, none of the tablets deviated from the average weight by more than ±1.5%....
The objective of the present research work was to optimize the preparation of ritonavir loaded albumin nanoparticles by modified desolvation technique using response surface methodology. A box-behnken design with 3 factors and 3 levels were used in the study. The albumin concentration, pH and rate of ethanol were selected as independent variables, loading capacity; entrapment efficiency and release of drug were chosen as response variables. The optimized formulation of RV was composed of 9.5% BSA, pH at 7.4 and 1.4 ml/ min of ethanol rate. The optimized formulation showed mean particle size of 163.1 nm, zeta potential of -23.9 mV, loading efficiency 31.23%, entrapment efficiency 76.80% and release of drug at 12 h 58.23%. In-vitro experiments showed a burst release at the initial stage and followed by prolonged release of RV from the nanoparticles up to 24 h....
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