Current Issue : January-March Volume : 2013 Issue Number : 1 Articles : 17 Articles
Bioadhersive drug delivery systems have high gastric duration due to adherence with mucous membrane of biosubstrate therefore it''s used as controlled unleash and targeted drug delivery system. Bioadhesion is that the method by that a natural or an artificial polymer will adhere to a biological substrate and provides the action for extended length of time. Bioadhersive controlled-release devices will improve the effectiveness of a drug by maintaining the drug concentration between the effective and poisonous levels, inhibiting the dilution of the drug within the body fluids, and permitting targeting and localization of a drug at a specific site. In recent years several such bioadhersive drug delivery systems are developed for oral, buccal, nasal, rectal and vaginal routes for each general and native effects. This paper shows special attention on gi dose forms along with ideas, mechanism of mucoadhesion, factors affecting mucoadhesion, various polymers used, evaluation methods, recent advances and future aspects....
The purpose of dry suspension is permanent stable suspension prepared after reconstitution. The excipients should be kept as low as possible, especially the expensive ones & suspending agent because reconstituted suspension should be pourable one also....
The aim of the current investigation is to design oral once daily gastro retentive floating tablets of tolperisone hydrochloride, which release the drug for 24 hours and matches with marketed drug release profile of sustained release formulation. Tolperisone hydrochloride is unstable in intestinal pH 4 to 7, it breaks down into 2- methyl-1-(4-methylphenyl) propenone (4-MMPPO) and piperidine which is potential genotoxic impurity. In the present investigation efforts were made to develop the gastro retentive floating drug delivery system which releases the tolperisone hydrochloride in the stomach which is free from 4- MMPPO and also improve the bioavailability and half life of drug. Various release retarding polymers like HPMC K100M, ethyl cellulose, carbopol934P and effervescing agent like sodium bicarbonate and citric acid in combinations were tried and optimized to get the release profile for 24 hrs. Formulations were evaluated for in-vitro release profile of tolperisone hydrochloride. The in-vitro drug release of optimized formulation followed zero order. The in-vitro release also followed Higuchi kinetics and the drug release mechanism was found to be of anomalous or non-Fickian type. The high water uptake leading to higher swelling of the tablet supported the anomalous release mechanism of tolperisone hydrochloride. The similarity factor f2 and dissimilarity factor f1 were found to be 62.28 and 10.69, respectively for tolperisone hydrochloride release. One month of accelerated stability study reveals that the formulation is stable under the given conditions of stability studies....
Econazole nitrate topical spray is a novel dosage form formulated for the treatment of superficial fungal infections. Study was designed to formulate and evaluate the performance of econazole nitrate spray formulations by varying the concentrations of different constituents of the spray. Twelve formulations of econazole nitrate topical spray were prepared using 22 full factorial design, where components of formulation such as penetration enhancer (X1) and co-solvent (X2) were selected as independent variables and % drug release (Y1) and % drug retention in skin (Y2) were selected as dependent variables. All the formulations of spray were pressurized with LPG propellant and evaluated for delivery rate, delivery amount, pressure, minimum fill, flammability, density, pH, spray pattern, particle size, unit content per spray, spray angle, leakage test and ex vivo penetration studies. Effect of independent variables on dependent variables was investigated.Optimised formulation was finally compared for ex-vivo release and retention study with marketed preparation. Short-term stability study of optimized formulation demonstrated insignificant changes in performance characteristics....
Indapamide, a low-dose thiazide-type diuretic, is used for the treatment of essential hypertension. In this study, we developed an indapamide sustained release formulation using Methocel K15M CR and Methocel K100M LVCR, starch 1500, talc and magnesium stearate considering technical feasibility and performed a comparative study with the release pattern. The tablets showed sustained release curves at pH 6.8 phosphate buffer for up to 12 h. The granules showed satisfactory flow properties, compressibility index and drug content etc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulations F-6 and F-8 could extend the drug release up to 12 h. The data obtained from the dissolution profiles were compared in the light of different kinetics models and the regression coefficients were also compared. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport which was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion mechanism in all cases. This study explored the optimum concentration and effect of polymer(s) on Indapamide release pattern from the tablet matrix for 12 h period....
The present work was planned with the objective of preparing naproxen solid dispersion in povidone (PVP K30) and hydroxyl propyl methyl cellulose (HPMC 3cps) with a view to design sustained release tablet formulation of naproxen. As naproxen is practically insoluble in water and aqueous fluids, its solid dispersion in povidone and hydroxyl propyl cellulose has markedly enhanced the dissolution rate of Naproxen. Solid Dispersions were prepared by solvent evaporation technique and were characterized for solid state properties by using differential scanning calorimetry (DSC), X-ray powder diffraction spectrometer (XRD) and FT-IR spectral studies. Solid dispersions were further evaluated for dissolution and stability studies. The aqueous solubility of naproxen was improved by the presence of both the polymers. Solid-state characterization indicated that naproxen was present as amorphous material in formulation with PVP K30 and HPMC 3cps due to efficient entrapment in polymer matrix. Sustained release tablets were formulated by employing naproxen solid dispersion with Methocel K4M and Methocel K15M as matrix polymers. Sustained release tablets prepared showed slow and controlled drug release over a period of 20 hrs. Drug release from these tablets followed first order kinetic. The ââ?¬Å?nââ?¬Â values obtained from peppas plots were within the range of 0.446 to 1.02, indicates the drug release by both dissolution and erosion...
Risperidone Orodispersible Tablets were prepared by three different methods. In the first formulatrion, cross povidone was used as superdisintegrant.In the second method cross povidone along with camphor was used in the preparation(Sublimation technology).In the last method evolution of carbon di oxide as disintegration mechanism was used.The prepared Risperidone Orodispersible tablets were evaluated for hardness, friability, weight variation, disintegration, wetting time, drug content and in vitro dissolution studies.The disintegration time of the Orodispersible were found to be be less than 30 seconds. Formulation prepared by using cross povidine (20mg) and Camphor (15mg) was selected as the best formulation (F6). The present study demonstrated potentials for rapid absorption, improved bioavailability, effective therapy and patient compliance....
The present study involves the preparation and evaluation of Chitosan based floating microspheres using Levetiracetam as model drug for prolongation of the gastric retention time. Levetiracetm is a BCS class-I drug hence it is absorbed rapidly from the stomach and having the half life of 6-7 Hrs. [1] so it is suitable candidate to formulate GRDDS. The microspheres were prepared by the simple emulsification phase separation technique using polymer Chitosan in fixed amount and varying the crosslinking agent Glutaraldehyde in varrient ratios. The shape and surface morphology of prepared microspheres were characterized by optical and scanning electron microscopy, respectively. The Percentage yield, Particle size distribution, Buoyancy percentage, Entrapment Efficiency and In vitro drug release studies were performed and drug release kinetics was evaluated. The prepared microspheres exhibited prolonged drug release (12h) and remained buoyant for > 8 h. The mean particle size increased and the drug release rate decreased at higher polymer concentration. In vitro studies demonstrated diffusion- controlled drug release from the microspheres....
The aim of the present study was to formulate and evaluate the pharmaceutical quality of a polyherbal capsule. Polyherbal formulation was prepared using seed powders of Azadirachta indica, Caesalpinia bonduc, Syzygium cumini, and Trigonella foenum-graecum in 1:1:2:2 ratio to obtain the best formulation; in order to increase the acceptability and adoptability of herbal medicine in the treatment of diabetic condition. To attain the purpose; identification of herbs used, pre-formulation and post formulation studies on polyherbal capsules were done. The quality of individual herbs was evaluated by observing particle size, pH, moisture content, ash values, extractive values. The flow capability of blended powder was calculated by angle of repose, bulk and tap density, Hausner ratio and Carr’s index, these properties helped to estimate the right size of capsule for the desired strength (500 mg). Preliminary phythochemical analysis of powders was also carried out to determine the presence of various phytoconstituents. The quality of polyherbal formulation was evaluated through its description, weight variation, disintegration time and stability studies that indicated light, temperature and humidity had no significant effects on the physiochemical properties of the formulated capsules. The conclusion of the study is that the herbal medicine can be used more conveniently and safely in various diseased conditions, if used in proper portion and combination....
The main objective of formulating the dosage form is to develop a multi-unit dosage form which is basically targeted for gastro retention. This will improve the gastric residence time, which also increases the bioavailability of famotidine. It was reported that this drug absorbed only in stomach and has about 45% absolute bioavailability and undergoes degradation in colon, floating dosage form helps in better absorption of drug by releasing the drug before it reaches the site of absorption and prevents the degradation of famotidine in colon. In the present study, an attempt was made to prepare oil entrapped floating beads of famotidine prepared by inotropic gelation method using Sodium alginate, Pectin, HPMC K4M with Calcium Chloride as curing agent and various concentration of mineral oil as a floating agent. In the preliminary trials, beads were prepared without oil and various parameters were optimized such as concentration of polymer, height and size of needle, speed and time of curing agent. It was concluded that the beads with the 30% of oil ratio showed oil leakage. Beads were unable to formulate if pectin or HPMC K4M were used alone, and of irregular shape when pectin and HPMC were used. Uniform beads were formulated only with sodium alginate alone or together with pectin and HPMC K4M....
Microparticles were now widely prepared to increase solubility, dissolution enhancement, to improve flow property of powders etc. The present investigation was aimed to prepare microparticles of fenofibrate, poorly water soluble drug, using spray drying technique. Fenofibrate, lipid lowing agent, was selected as model drug. Microparticles of fenofibrate were prepared by incorporating poloxamer 407 as solubilizing agent. Box-Behnken experimental design was used to prepare and optimize factors affecting during development of microparticles using spray drying technique. Atomizing air pressure (X1), feed rate (X2) and polymer: drug ratio (X3) was selected as independent variables, while microparticle size (µm) and T90% (min) was selected as response to the independent variable. Optimization of formulation of microparticles was done by multiple linear regression analysis. Design Expert 8.0.2 demo version was used to generate polynomial and second order equation for optimization. Optimized batch of microparticles was evaluated for physical characterization using DSC, XRD, FTIR, and SEM. Atomizing air pressure and polymer: drug ratio was affected microparticle properties. Microparticle size was decreased as the level of atomizing air pressure was changed from lower to higher. T90% was decreased as change in value of polymer: drug ratio and atomizing air pressure. At higher atomizing air pressure microparticles size was decreased, hence, increased wetting of microparticles and dissolution of fenofibrate....
Cold cream is o/w type of emulsion. The preparation & Evaluation parameters both are influenced by method of preparation. In laboratory scale Tituration technique by means of mortar & pastel is employed for preparation of cold cream.Vigrous Tituration of emulsion by means of pastel in mortar is also affect the formulation that only vigorous Tituration can give emulsion i.e. cream otherwise both phases of oil & liquid are separated out, however cream preparation is irrespective of content, that may affect emulsion preparation but mostly Tituration technique have great influence on cream preparation....
Today the world is really facing a huge problem of poorly water soluble drugs. Many methods are there for increasing the solubility, but nanotechnology is one of the most prominent and latest technologies. It deals with the nanoparticles (having high surface area) which are useful for increasing the solubility of poor water soluble drugs. Nanoparticles hold tremendous potential as an effective drug delivery system. This article discussed nanotechnology, its advantages, disadvantages, limitatations and developments for drug delivery. To overcome the problems of drug delivery of hydrophobic compounds, nanotechnology has gained interest in recent years. Important advances are being made in improving the bioavailability of hydrophobic compounds, so that promising candidate drugs need no longer be abandoned or have their development stalled by sub-optimal formulation. In addition to more conventional methods, tackling this problem has become one of the main applications of nanotechnology in drug delivery. This is also the most advanced approach commercially, as formulation scientists increasingly turn to a range of nanotechnology-based solutions to improve drug solubility and bioavailability. This paper highlights the properties of nanoparticles used in targeted drug delivery of poorly water soluble drug arteether. Nanoparticles exploit biological pathways to achieve payload delivery to various cellular and intracellular targets. Different nanodispersion systems such as micelles, nanoemulsions and nanosuspensions along with advantages and disadvantages are discussed here. Various nanoformulations represent promising means for delivering many bioactive agents, including peptide and protein drugs. The importance of these methods grew with the advancement in the understanding pharmacology of hydrophobic drugs as well as the ability to mass-produce these compounds. The polymers used here are non-toxic, non- immunogenic, non-antigenic, and highly soluble in water and FDA approved. In this article, we introduce the different strategies that have been developed with the use of different polymers such as polyethylene glycol (PEG) in delivery of hydrophobic compounds....
The conventional dissolution test, particularly the USP apparatus I and II, remains an important tool in the field of the pharmaceutical product development. For accurate dissolution characterization, sink conditions, where saturation solubility of a drug in the dissolution medium is at least three times more than the drug concentration, are significant. These conditions can be difficult to maintain with formulations containing poorly soluble active pharmaceutical ingredients. This research summarizes the role of the excipients to enhance dissolution of racecadotril and facilitate the achievement of sink. The dissolution model utilizes various media (0.1N HCl, Acetate buffer pH 4.5 and Phosphate buffer pH 6.8) with surfactant to improve the dissolution limitation of racecadotril. Crucially, the acetate buffer pH 4.5 with 0.75% SLS does allowed sink conditions to be maintained and hence the experiment will yield complete dissolution....
The present study involves formulation development and optimization of oral taste masked Mouth Dissolving Films (MDFs) of Bisoprolol Hemifumarate(BH). MDF is novel dosage forms that improve disintegration and dissolve within the oral cavity in seconds. BH (Ã?Ÿ-blocker) belongs to BCS class-I, a drug of choice for hypertensive patients.\r\nBH is bitter tasting drug. Various taste masking techniques were utilized to formulate MDF with acceptable taste. For this purpose, various sweetening agents like sucralose, mannitol, sucrose, sorbitol, aspartame and menthol were tried but, taste masking was not successfully achieved. Thus Ã?Ÿââ?¬â??cyclodextrin (Ã?Ÿ-CD) was used to mask bitter taste by complexation with drug. Various molar ratio of BH to Ã?Ÿ-CD was tried, complete taste masking of BH were achieved using 1:0.25 molar ratio of BH:Ã?Ÿââ?¬â??CD.\r\nPolymers like Hydroxypropyl methylcellulose (HPMC) and Polyethylene oxide were used in developing MDF of BH using solvent casting method. The effect of amount of polymer and amount of plasticizer (propylene glycol) was studied. MDFs were evaluated for organoleptic properties, thickness, mechanical properties like tensile strength and folding endurance, in vitro disintegration and in vitro dissolution studies. \r\nBatch F-19 containing HPMC (5cps) at 4%w/v concentration and PG at ratio (0.4:1) as plasticizer showed acceptable thickness (600Ã?µm), tensile strength (46.386 N/cm2), folding endurance was 30 and in vitro disintegration time (32 sec). Complete drug was released within 20 minutes using simulated saliva as a medium. The study indicated that developed film formulation will be highly effective in improving onset of action thus, useful to hypertensive patient....
Pegylated Solid dispersion of diclofenac was prepared to achieve improved bioavailability. Currently only 8% of new drug candidates have both high solubility and permeability. More than 60% of potential drug products suffer from poor water solubility. This frequently results in potentially important products not reaching the market or not achieving their full potential. Experience with solid dispersions over the last 20-30 years indicates that this is a very fruitful approach to improving the release rate and oral bioavailability of poorly water soluble drugs. So this article highlights technology various approaches for the preparation of solid dispersion, technology involved, detail description of poorly water soluble drugs & carriers. The purpose of this study is to fabricate the polyethylene glycol matrix tablet by mold technique. Diclofenac and hydroxyl propyl methyl cellulose were used as model drug and polymer, respectively, in PEG matrix system. Scanning electron microscope photomicrograph indicated the drug diffusion outward through the porous network of this developed matrix tablet into the dissolution fluid. Both the enhancement of drug dissolution and the prolongation of the drug release could be achieved for aqueous insoluble drug such as, Diclofenac by using polyethylene glycol-hydroxy propyl methylcellulose matrix system prepared with melting and mold technique....
Compared to single-unit dosage forms, oral multi particulate drug-delivery systems (e.g. pellets, granules) offer biopharmaceutical advantages in terms of a more even and predictable distribution and transportation in the gastrointestinal tract. Today pelletization technology represents an efficient pathway for manufacture of drug delivery system. There is different pelletization and granulation techniques available to prepare drug loaded spherical particles or granules. Extrusion-spheronization seems to be the most promising process for the optimum delivery of many potent drugs having high systemic toxicity. It also offers immense pharmaceutical applicability due to the benefits of high loading capacity of active ingredient(s), narrow size distribution, and cost-effectiveness. On application of a specific coat, these systems can also aid in site-specific delivery, thereby enhancing the bioavailability of many drugs. In this review article we mainly focus on the process of Extrusion-spheronization and machine (friction plate pattern, speed, retention time, charge volume) product (excipients, API level, moisture, binders, and lubricants) parameters. Here we also discussed about Holt Melt Extrusion (HME) process, parameters and it�s applications in the pharmaceutical industry....
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