Current Issue : July-September Volume : 2014 Issue Number : 3 Articles : 17 Articles
Medicated chewing gum is a novel drug delivery system containing masticatory gum base with pharmacologically active ingredient and intended to use for local treatment of mouth diseases or systemic absorption through oral mucosa. Motion sickness or kinetosis, also known as travel sickness, is a condition in which a disagreement exists between visually perceived movement and the vestibular systems sense of movement. Diphenhydramine HCl is anti-histaminic, anti-emetic drug used to treat the symptoms associated with motion sickness, nausea and vomiting, vertigo and insect bite. Taste masking of diphenhydramine HCl will be done by complexing with β-cyclodextrin. Medicated chewing gum formulations were prepared using health in gums as a gum base in different concentration using diphenhydramine HCl for the treatment of motion sickness by direct compression method. Pre-compression and post-compression characteristics were studied. In-vitro dissolution studies were carried out by using modified chewing gum dissolution apparatus. The selected formulation was subjected to stability studies and no significant variation was observed. Hence it could be concluded that medicated chewing gum containing diphenhydramine HCl can be successfully formulated for the treatment of motion sickness....
The objective of necessary work to develop fast dissolving tablet of Dimenhydrinate to give fast release of drug using different super disintegrants which would disintegrate tablet rapidly in oral cavity. Twelve batches of dimenhydrinate fast dissolving tablets were prepared by direct compression method using crospovidone, sodium starch glycollate, croscarmellosesodium and low substituted Hydroxypropyl cellulose as super disintegrants in different concentration in order to achieve faster disintegration of tablet. Crospovidone was the key ingredient which gives less disintegration time as well as fast drug release effect. Different nine formulations were prepared by varying the concentration of Crospovidone as a superdisintegrant and Microcrystalline cellulose. These formulations were evaluated for parameters like hardness, disintegration time, in-vitro drug release study, wetting time, water absorption ratio, drug content and drug excipient compatibility study. In this study, the release profile depends on the concentration of Crospovidone. A 32 factorial design was applied to check the effect of varying the concentration of Microcrystalline cellulose (X1) and Crospovidone (X2) on the dependent variable i.e. disintegration time (sec), wetting time (sec), % friability (%) and in-vitro drug release (%). Regression analysis and analysis of variance were performed for dependent variables. The results of the F-statistics were used to select the most appropriate model. Formulation F9 was considered optimum which contained Crospovidone (28 mg) and Microcrystalline cellulose (80 mg). The studies indicate that the formulation F9 was effective in providing less disintegration time as well as fast in-vitro drug release....
Quetiapine Fumarate (QF) is one of atypical antipsychotic drug used to control the schizophrenia and bipolar mania .Osmotically Controlled release tablet of Quetiapine Fumarate was performed for reducing dosing frequency and patient compliance. Elementary osmotic tablets of Quetiapine Fumarate were developed using Sodium chloride as a key ingredient which gives osmogent property which provides driving force inside the core tablet which leads to release of drug and Microcrystalline cellulose used as a release retardant material in the present work. Different formulations were prepared by varying the concentrations using 32 factorial design was applied to see the effect of variables Sodium chloride (X1) and MCC (X2) on the response percentage drug release as a dependent variable. These formulations were evaluated for Flow property, Hardness, Thickness, Friability, Drug content and In-vitro drug release. Tablets were coated with a semipermeable membrane using 5% w/v cellulose acetate(CA) in acetone and PEG 400(15%) used as Plasticizer. Coated Elementary osmotic tablets were drilled for delivery orifice using standard micro drill of diameter size 0.8mm .Drug release rate was increased as the increase in the concentration of sodium chloride and release rate decreased on increasing the concentration of MCC.Drug release rate was directly proportional to delivery orifice size .SEM Study carried out for detection of diameter size of delivery orifice. The FTIR studies demonstrate that there was no interaction between polymer and drug. The optimized formulation was stable for 3 months of accelerated stability study....
The main aim of the study is to enhance the dissolution rate of efavirenz by solid dispersion (SD) method. Efavirenz is a BCS Class II drug having low solubility and high permeability. The technique employed was solvent evaporation method. Polyvinyl pyrrolidine (PVP - K30), urea, β-cyclodextrin (β-CD) were used as hydrophilic carriers (in the ratio of 1:1, 1:3, 1:5) and methanol used as common solvent. The in-vitro dissolution study of pure drug and solid dispersions (SDs) were performed by using USP Type 1 apparatus at temperature of 37±0.5°C, 75 RPM and 900 ml of distilled water with 2% sodium lauryl sulphate (SLS) as dissolution average. The pure drug showed very slow dissolution rate and the SD’s considerably enhanced the dissolution rate. The highest improvement in dissolution rate of efavirenz was observed in formulation F6 (drug: urea, 1:5). In-vitro drug release clearly showed significant increase in the dissolution rate of efavirenz. Physicochemical characterization of solid dispersions is done by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) suggests a reduction in drug crystallinity results in dissolution enhancement....
Drug delivery through nails (Transungual drug delivery) is considered to be highly propitious for treating nail disorders as systemic therapy is associated with severe systemic side effects like hepatic toxicity, gastric upset, hematological disorders, drug-drug interactions etc. However, the efficacy of topical therapy is limited due to minimal drug permeability through the nail plate, therefore, there is a need of a formulation which can easily penetrate the nail plate along with which provides safety, efficacy and compliance. The Current review focuses on the Anatomy of a human nail, Different type of nail disorders, Factors which affect drug permeation through the nail along with the different techniques which are available to improve drug permeation through nails and the latest trends which are available nowadays for transungual drug delivery. In this article nail lacquers, which past recently striked the formulation field along with some of the limitations of transungual drug delivery has been discussed in brief....
The aim of present work was to evaluate the effect of hydrophilic polymers and the effect of particle size on the release of Clozapine from matrix tablets. Hydrophilic polymerslike HPMC K 100 M, Guar gum and NaCMC were used as release retardant polymers and compressed the tablets using direct compression technology. The ratio of polymers used was 1:3, 1:4, 1:5 and 1:8. It was observed that the drug release decreased as the polymer ratio increased. The level of polymer ratio also had an effect on swelling index showing a linear relationship. At 1:8 (drug: polymer) ratio with HPMC K 100 M, tablets showed desirable release pattern, release up to 24 hr. It was found to release the drug in Zero order up to 24 hrs.For further study, 1:8 (drug: polymer) ratio was evaluated with particle sizes ranging from 250 micron to 106 microns on the release of drug. It was observed that as the particle size decreases, release also retards but follows zero order kinetics....
Topical preparations have been used for the localized effect at the site of application by virtue of drug penetration into the underlying layer of skin or mucous membrane. In spite of many advantages of gels a major limitation is in the delivery of hydrophobic drugs. So to overcome this limitation, an emulgel based approach is being used consideringan antifungal hydrophobic drug miconazole nitrate. The formulations of miconazole emulgels were prepared using liquid paraffin and cow ghee as oil phase in varied concentrations and evaluated for its suitability with the carbopol as the gel base. The emulgel formulations were white viscous creamy with a smooth and homogenous appearance. The pH values of all the formulations ranged between 6.5 to 7. The formulated emulgels exhibited shear thinning thixotropic properties when subjected to rheological studies. The formulation F3 with cow ghee as the oil base showed better spreadability when compared to all other formulations. The in-vitro drug permeation studies was carried out using egg membrane for all the emulgel formulations and compared with plain miconazole gel formulation. The studies reported excellent results for formulation F3 with 96.18% of drug release with flux of 1191.6 mcg/cm2/ min. when compared to gel formulation of 42.82% and 697.12 mcg/cm2/ min. at the end of 8 h....
The aim of present research work is to formulate and evaluate bilayer tablets of Salbutamol Sulphate with extended release. Salbutamol is a rapidly acting and rapidly eliminated bronchodilator agent. Salbutamol starts acting within 15-30 min or less after administration of tablet and its action lasts for 3 hrs. To provide extended release, polymers used are HPMC K100M, HPMC K4M, HPMC K15M and immediate release system is prepared by using different disintegrating agent like SSG, CMC, MCC by wet granulation method. 32 factorial design was chosen. Prepared batches evaluated for precompression parameters and process parameters like hardness, friability, morphology, drug content and in vitro drug release profile. Effect of polymers and disintegrants in two different layers affect in vitro drug release. It was found that the Salbutamol sulphate release rate increase with decrease amount of polymers and increase in amount of disintegrants. It can be concluded that Bilayer tablet is simple, cost effective and yields robust, stable tablets as a optimized formulation in research work....
The objective of present work was to develop oral Fast dissolving film of Montelukast sodium which was indicated for the prophylaxis and chronic treatment of asthma. Which offers a solution for those patients having difficulty in swallowing tablets/capsules and allowing fast reproducible drug dissolution in oral cavity thus by passing first pass metabolism, to enhance the convenience and compliance by the elderly and pediatric patients. Montelukast oral fast dissolving oral thin films were prepared by solvent casting method with using different film-forming agents like pullulan gum, Sodium CMC, PEG 400, glycerol as a plasticizer and mannitol as filler and sweetener. Oral films were evaluated for weight variation, thickness, folding endurance, drug content, disintegration time, and invitro dissolution studies. Montelukast oral films based on evaluation studies pullulan gum showed optimum performance against other formulations. The prepared films were clear, transparent, and had a smooth surface. It was concluded that the fast dissolving oral thin films of montelukast can be made by solvent casting technique with enhanced dissolution rate, better patient compliance and effective therapy....
The purpose of this research was to formulation and evaluation of oral disintegrating tablets of haloperidol - hydroxypropyl β-cyclodextrin (HPβCD) complex. Haloperidol is used for treatment of severe nausea and emesis in post-operative and palliative care for radiation therapy and chemotherapy, also in acute delirium, anxiety, depression, hyperactivity, psychosis, schizophrenia. Phase solubility study indicated formation of 1:1 molar ratio of inclusion complex system of haloperidol with HPβCD. Complexes were prepared by freeze drying method. Complex may improve solubility, reduce irritation, protect from light and mask the taste of haloperidol. Prepared complexes were evaluated for DSC, FTIR, drug content and in-vitro release study. Oral disintegrating tablets (ODTs) were developed from haloperidol inclusion complex containing superdisintegrants by direct compression method. Different formulations were prepared by varying the concentration of sodium starch glycolate (SSG) and micro crystalline cellulose (MCC) PH102. The directly compressible powder was evaluated for precompression parameters. Prepared tablets were evaluated for postcompression parameters. Dissolution studies were performed in SSF pH 6.8 and 0.1 N HCl (pH 1.2). The optimized batch was compared with the control (C1, C2) and marketed formulation, also charged for stability study as per ICH guidelines. In 32 full factorial design, Quadratic model was suggested, contour and 3D Graph was generated. By using Overlay plot, batch was optimized. F9 batch prepared with 5% SSG and 70% MCC PH102 decrease disintegration time and Wetting time i.e. (8±1) sec and 12±1.52 sec respectively....
Candesartan cilexetil is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. The drug is having low solubility in biological fluids which results in poor bioavailability after oral administration. Hence present study was carried to enhance dissolution properties of candesartan cilexetil. Solid dispersions of candesartan cilexetil were prepared by using PEG-4000 and PEG-6000 as water soluble carries at various proportions 1:1, 1:2, 1:3. The kneading and solvent evaporation methods were used to prepare solid dispersions. The prepared dispersions were made into tablets by direct compression method. The release profile was studied in phosphate buffer pH 6.5 containing 0.35% polysorbate 20. It was found that the dissolution rate of tablets containing solid dispersions were higher than those of intact drug. The degree of dissolution rate enhancement depended on the nature and amount of the carrier i.e., the higher the amount of the carrier used, the higher dissolution rate was obtained. Among the prepared batches formulation F4 gave highest dissolution. The increase in the dissolution rate of the drug may be due to increase in wettability, hydrophilic nature of the carrier and also possibility due to reduction in drug crystallinity. Formulation F4 was subjected to stability studies. The formulation was found to be stable for 45days at 40℃ with insignificant change in drug release pattern....
The purpose of this study was to develop and optimize oral delayed release formulation for Omeprazole. The drug loaded pellets were prepared by spaying Omeprazole suspension on the sugar spheres. These drug loaded pellets were coated with acid resistant polymer Hydroxypropylmethyl cellulose phalate-HP55 in a Wurster coater, to different polymer levels. The in vitro dissolution studies were conducted in 0.1N HCl for 2 hrs., followed by phosphate buffer pH 6.8, for 45 mins., with USP dissolution tester (type II).Enteric coated pellets with polymer load of 6.98 and 8.073% failed to provide required acid resistance to the pellets, but very insignificant amount of drug was leached from the coated pellets in the acid phase with polymer load 9.301 and 10.093%, whereas almost whole amount of drug was released in the buffer phase. The results generated showed the optimal % coating formulation with HPMC phthalate HP55 which is important in designing delayed release pellets dosage form, with acceptable dissolution profile....
The present study as designed to formulate and develop 12 prototype gastro retentive mucoadhesive tablets formulations using alfuzosin HCl as a model drug. Alfuzosin HCl belongs to a series of drugs called alpha blockers used in the treatment of benign prostrate hyperplasia. Based on the preformulation studies 12 optimized formulations were prepared by direct compression using a swelling agent viz: carbopol 934P and controlled release polymers such as HPMCK15M, HPMCK4M, sodium carboxyl methyl cellulose and sodium alginate in different concentration. A dissolution method and an analytical procedure by UV spectrophotometry were developed and validated for evaluation of the dissolution behavior of designed tablet dosage form. The method was validated according to international conference on harmonization (ICH) guidelines which include accuracy, precision, specificity, linearity and analytical range. The tablets were also evaluated for other quality parameters like in-vitro diffusion study and in-vitro bioadhesion strength. The data obtained from dissolution studies was fitted in 5 models viz: zero order, first order, higuchi matrix, peppas and erosion plot. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation and therefore followed non-fickian or anomalous release approaching zero order kinetics. The cumulative percentage drug release data revealed that formulations and were highly effective in retarding drug release up to 15 hrs respectively as compared to marketed preparation releasing the drug at the end of 10th hr itself....
The aim of the present work was improvement of ocular bioavailability of Loteprednol Etabonate, a novel drug, by prolonging its residence time in precorneal area. One of the method is to achieve this by formulation of the solid lipid nanoparticles and then dispersing it into an in-situ gelling system. The Solid Lipid Nanoparticle was prepared by Hot Homogenisation Method. Drug/Excipient interaction was determined by DSC study. The Particle size and Zeta potential of solid lipid nanoparticles was measured with other evaluating parameter. Simantaneously in-situ gel was also prepared and dispersed these Solid lipid nanoparticles into in-situ gelling system. In vitro drug diffusion study was carried out from the nanosuspension using Franz diffusion cell apparatus. The release data were subjected to different models in order to evaluate their release kinetics and mechanisms. The drug diffusion was found 89% in 24 hrs. The present study conclude that it is possible to prepare solid lipid nanoparticle of Loteprednol Etabonate (LE) with desired criteria which increases the dissolution of drug and improves drug absorption and hence improve drug effect....
The purpose of the present study was to investigate the mixed hydrotrophic solid dispersions of Rifampicin (RIF) with hydrotrophic agents like sodium benzoate & citric acid. Mixed hydrotrophic solid dispersions were prepared by using solvent evaporation and hydrotrophy method. The prepared solid dispersions were subjected to particle size analysis, solubility analysis, in vitro dissolution, Fourier Infra Red Spectroscopy, Differential Scanning Calorimetry , X-ray diffraction etc. It was observed that dissolution rate of RIF enhanced to a great extent by solid dispersion technique using sodium benzoate and citric acid as hydrotrophic agents....
Orodispersible tablets are novel oral drug-delivery system as they have improved patient compliance and for those patients having difficulty in swallowing tablet. They have a medicinal substance which rapidly disintegrates within second when placed on tongue. Metoclopramide hydrochloride tablet is prepared by using superdisintegrants crospovidone and croscarmellose sodium by direct compression technique. The hardness of all the formulations was found in the range of 6.51�±0.21 kg/cm2. The friability of formulation F1-F6 was found to be in the range of 0.20-0.15 which was within the IP limit i.e below 1%. The drug content of all the formulation was found in the range of 98.85-99.25 % which was whithin acceptable limit. The In-vitro disintegration time of all formulation was found in the range of 18-12 sec. Wetting time which is the important parameter for understanding the capacity of disintegrants to swell in presence of little amount of water were found to be in the range of 23-20 sec. All the formulations releases the drug within 5-10 minutes....
Co-processed excipients with microcrystalline cellulose and mannitol in different ratios were fabricated by different methods and its influence on blend fluidity, friability of the tablet and dissolution characteristics of chloroquine phosphate from direct compressible tablets was studied. The flow properties of the blends were determined by carr’s index and hausner’s ratio. The co-processed excipient contained higher proportion of microcrystalline cellulose imparted low flowability and the blends containing high proportion of mannitol failed to meet friability criteria. Optimized co-processed formulation containing microcrystalline cellulose and mannitol in the ratio 9:1 was found to be more acceptable to formulate chloroquine phosphate tablets. The co-processed excipients were prepared by using granulation technique. The preformulation parameters like flow property and the performance parameters were dependent on the proportion of components present in the co-processing excipient. The co-processed excipient prepared with granulation technique imparted the desired qualities to the tablet....
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