Current Issue : July - September Volume : 2011 Issue Number : 3 Articles : 14 Articles
Tablet is the most popular dosage form among from all existing dosage form. but in some instances due to the large size of dosage forms, and in case of uncooperative, pediatric and dysphasia patients, it may create some problems, to overcome this problems, a new form of dosage form is developed, which is known as first dissolving tablet or mouth dissolving tablet. These tablets are the advanced dosage form which is dissolve with in few seconds after placing on the tongue. Fast dissolving tablets have gained considerable attention as a preferred alternative to conventional tablets and capsules due to better patient compliance. Today Melt in Mouth Tablets (MMT) are a proven & accepted technology for the systemic delivery of active pharmaceuticals ingredients....
Solid lipid nanoparticles (SLN) are a novel and innovative therapeutic delivery system. Clear advantages include the composition (physiological compounds), the effective production process (especially the possibility of large scale production), avoidance of organic solvents during the production process and the possibility of producing highly concentrated lipid dispersions. SLN are a characterization of the formulation requires several analytical methods and complex system due to the physical state of the lipid. There are a large number of methods available to characterize nanoparticles. Some approaches, such as DLS for size, or nuclear magnetic resonance (NMR) for diffusivity, are unique to the analysis of nanoparticles compared to that of more macroscopic species. Other techniques, such as differential scanning calorimetry (DSC) or X-ray diffraction, are not significantly affected by the sub micrometer particle size. Rather, in these cases, it is the interpretation of the results in the context of the problem at hand that renders the corresponding method relevant....
The buccal region offers an attractive route for systemic drug delivery. Perindopril is an ACE inhibitor widely used as an antihypertensive agent shows less oral bioavailability as it undergoes first pass metabolism. Perindopril patches were prepared using HPMCK4M, Chitosan, HPMCP, PVP and PVA. FTIR and DSC studies revealed that there was no interaction between perindopril and polymers. Gas phase chromatography was carried to estimate the residual Methanol, acetic acid and dichloromethane. The patches were evaluated for their thickness, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH. The tensile strength was higher for formulations containing HPMCP and HPMCK4M. In vitro release studies were conducted for perindopril loaded patches in 6.6 pH phosphate buffer solution. Patches containing chitosan and HPMCK4M exhibited greater release than other formulations containing HPMCP, PVP, PVA and HPMCK4M. Patches exhibited drug release in the range of 66.93 to 98.9% in 8 hrs. Data of in vitro release from patches were fit to different equations and kinetic models to explain release profiles. Many of the buccoadhesive systems followed zero-order release kinetics. Buccoadhesive patches of perindopril can be developed as potential controlled release formulations for the treatment of hypertension....
The purpose of this research was to mask the bitter taste of Rizatriptan benzoate (RB) and to formulate an oral disintegrating tablet (ODT) of the taste-masked drug. Taste masking was done by mass extrusion with Eudragit EPO, in different ratios. The drug: polymer ratio was optimized based on bitterness score and RB –polymer interaction. Taste masking was evaluated by checking the in vitro release of RB in simulated salivary fluid (SSF) of pH 6.8 and by sensory evaluation in human volunteers. For formulation of rapid- disintegrating tablets of RB, the batch that depicted optimum release of RB in SSF was considered. ODTs of Rizatriptan Benzoate were prepared by using superdisintegrants namely, sodium starch glycolate, and crospovidone and croscarmellose sodium using the direct compression method. The tablets were evaluated for hardness, friability, wetting time, in vitro disintegration time. The optimum formulation was selected and the tablets were evaluated for thickness, drug content, content uniformity, and mouth feel, in vivo disintegration time, in vitro drug release at pH 1.2 and 6.8 and stability study. Eudragit EPO was able to mask the bitter taste of Rizatriptan benzoate effectively in 1:1 ratio by mass extrusion method. FTIR and DSC data revealed absence of RB-polymer interaction. ODTs containing crospovidone (5% w/w) depicted minimum disintegration time. Taste evaluation of ODT in human volunteers revealed considerable taste masking. Thus, results conclusively demonstrated successful taste masking and formulation of ODT of Rizatriptan benzoate by a rapid, simple and cost effective mass extrusion method....
In the present study maize starch, tapioca starch, potato starch and soluble starch were used as a disintegrating agent and an antiadherent in Isoniazid as well as Diclofenac sodium tablets at concentration of 2, 4, 6% w/w. Properties of the granules prepared from various starches were evaluated for Moisture content, Bulk density, Tapped density, Carr’s index and Hausner’s ratio. The tablets were evaluated for thickness, weight variation, hardness, friability, disintegration time and dissolution profiles. The granules formulated using Maize starch showed the least Carr’s index, Hausner’s ratio, moisture content values. The results obtained indicate that among the granules prepared from all the starches in relation to their flowability, the granules prepared from maize starch possess the best flow property. Also, the disintegrants maize starch, tapioca starch, potato starch showed comparable results in Isoniazid as well as Diclofenac sodium tablets....
Polymeric delivery systems based on nanoparticles have emerged as a promising approach for peroral insulin delivery. The aim of the present study was to investigate the release of insulin nanoparticulate systems and ex vivo studies. The nanoparticles were prepared by the ion gelation method. Particle size distribution, zeta potential, and polydispersity index of the nanoparticles were determined. It was found that the nanoparticles carried positive charges and showed a size distribution in the range of 170ââ?¬â??200?nm. The electrostatic interactions between the positively charged group of chitosan and negatively charged groups of Arabic gum play an important role in the association efficiency of insulin in nanoparticles. In vitro insulin release studies showed an initial burst followed by a slow release of insulin. The mucoadhesion of the nanosystem was evaluated using excised rat jejunum. Ex vivo studies have shown a significant increase in absorption of insulin in the presence of chitosan nanoparticles in comparison with free insulin....
Many drugs exhibit absorption windows in particular portion of gastrointestinal tract which can limit the bioavailability of orally administered compounds and can be a major obstacle to the development of controlled release formulations for such regional specific drugs. Various approaches to increase the residence of drug formulations at or above the absorption window to enhance the bioavailability of such drugs are presented in this review. A good understanding of gastrointestinal transit in humans and the effect of factors such as food can be helpful in the design of rational drug delivery systems that will have clinical advantage. Different approaches presently being explored includes (i) Modification of intestinal transit time (ii) bioadhesive microspheres that have a slow intestinal transit; and (iii) the gastroretentive dosage system, which is further divided into several approaches like floating , swelling, expanding and magnetic systems. These approaches are promisingly found to improve bioavailability of different narrow absorption window drugs compared to conventional dosage forms....
A multiparticulate dosage form taken at night (bedtime) that delivers drug prior to and during “morning surge” activities will prove useful to treat circadian disorder hypertension. The purpose of the study was to develop pulsatile release multiparticulate dosage form. Carvedilol is a non-selective β-adrenergic blocking agent with α adrenergic blocking activity, used for the treatment of hypertension. In this study, the drug loaded nonpareil seeds were coated with a pH-sensitive Acrycoat L100 and Acrycoat S100 polymers to obtain two population of pellets to achieve drug release with a specific lag time and the effect of weight gain of polymer on lag time was investigated. The formulated pellets were characterized for friability, SEM studies, in vitro dissolution studies and micromeritic properties. The pellets were spherical in shape with smooth texture. The drug loaded pellets coated with Acrycoat L100, with 5% weight gain and the drug loaded pellets coated with Acrycoat S100, with 7.5% weight gain was found to be optimum with desired lag time. The release of the drug after a lag time consistent with requirement for chronotherapeutics was achieved with developed formulation....
In this study microcrystalline cellulose, coded MCC-MA was obtained from the processed stem of Momordica augustisepala. This extraction was effected by a two stage sodium hydroxide delignification process followed by a beaching process using laboratory prepared sodium hypochlorite. The product was examined for its physicochemical properties, flow characteristics and swelling parameters in comparison with Avicel, after which it was used as a disintegrant at various concentrations for the production of paracetamol tablets. The tablets were subsequently subjected to tablet quality testing procedure. The extraction yield of alpha cellulose from the sponge was approximately 56% and that of MCC-MA from the alpha cellulose approximately 77%. Results obtained from physicochemical tests showed a true density of 2.0lg/ml and a moisture content of 6.87%. The hydration and moisture sorption capacities were 3.24 and 13% respectively. The flow indices (angle of repose-37.25o, Carr’s index- 12.26%, Hausner’s index-1.14) showed that MCC-MA had good flow properties. Tablets produced with MCC-MA showed reasonable resistance to abrasion, excellent disintegration and tablet weight uniformity conforming to specified standards in the British and United State pharmacopoeia. Generally there was no significant difference (P>0.05) in the friability and disintegration time of tablets produced with Avicel and MCC-MA. However, there was significant difference (P<0.05) in the hardness and dissolution profile of tablets produced with both Avicel and MCC-MA. Tablets made with MCC-MA were less friable but have higher dissolution rate than those produced with Avicel....
“Respirocytes” are artificial red blood cells that can supplement or replace the function of much of the human body's normal respiratory system. Molecular manufacturing promises precise control of matter at the atomic and molecular level, allowing the construction of micron scale machines comprised of nanometer scale components. Medical nanomachines will be among the earliest applications. The artificial red blood cell or "respirocyte" proposed here is a bloodborne spherical 1 micron diamondoid 1000 atm pressure vessel with active pumping powered by endogenous serum glucose, able to deliver 236 times more oxygen to the tissues per unit volume than natural red cells and to manage carbonic acidity. An onboard nanocomputer and numerous chemical and pressure sensors enable complex device behaviors remotely reprogrammable by the physician via externally applied acoustic signals. Primary applications will include transfusable blood substitution, partial treatment for anemia, perinatal/neonatal and lung disorders, enhancement of cardiovascular/neurovascular procedures, tumor therapies and diagnostics, prevention of asphyxia, artificial breathing, and a variety of sports, veterinary, battlefield and other uses. Respirocytes could be designed to capture nitrogen molecules during dives. The present article aims to reveal its impact on nanorobotic human science pharmaceuticals....
The specific aim of this work was to prepare mucoadhesive patches containing tetracycline hydrochloride and carvacrol in an attempt to develop a novel oral drug delivery system for the treatment of mouth infections. The bilayered patches were prepared using ethyl cellulose as a backing layer and carbopol 934 as a matrix mucoadhesive layer. Patches were prepared with different loading amounts of tetracycline hydrochloride and carvacrol. The antimicrobial activity was assessed for the prepared patches using the disc-diffusion method against the yeast Candida albicans and five bacterial strains, including Pseudomonas aeruginosa, Escherichia coli, Bacillus cereus, Staphylococcus aureus, and Bacillus bronchispti. In this work, we highlighted the possibility of occurrence of a synergistic action between carvacrol and tetracycline. The best formulation was selected based on microbiological tests, drug release, ex-vivo mucoadhesive performance, and swelling index. Physical characteristics of the selected formulations were determined. These included pH, patch thickness, weight uniformity, content uniformity, folding endurance, and patch stability....
Coating is a process involving the application of coating material to the moving bed of core material. Coating is done to confer benefits from the dosage form in respect of its appearance and its function. With the improved technologies and innovations there is occurring a increase in competition to produce a better dosage form and the coating process is one of the field which is being used as a tool to produce a better dosage form according to the requirements but there is an inherent opposition to changes expressed by pharmaceutical manufacturers towards accepting major changes in the processing technologies which is leading to the advancements and modifications in the conventional coating process . There has been seen modification of the different processing parameters like spray pattern, spray time, type of coating material, drying methods, etc which led to development of dry coating, compression coating, magnetic coating, etc with reduced air pollution, high time and energy consumption and expensive operation cost as encountered by liquid coating. Thus, the change tends to be gradual in spite of drastic, means it is “Evolutionary rather than Revolutionary”. So as a result, there has been seen many modifications in the tableting and coating process to meet the required specifications according to the needs....
The objective of the present research work was to develop “once daily” extended release granules of aceclofenac by wet granulation using HPMC as a hydrophilic polymer and to check the effect of humidity on granules prepared by using different concentrations of polymer. HPMC K100M and K15M were used to check the release of drug, of which one trial showed optimum release of drug i.e. for 24 hours and were stable under accelerated conditions of temperature since there were no significant changes in drug content and physical parameters....
Matrix tablets were prepared by direct compression using blends of xanthan gum (XG) and guar gum (GG). Diethylcarbamazine (DEC) was used as model drug. Sufficient quantities of materials were weighed to make provision for up to 1080 tablets for 27 batches (40 tablets per batch at a target weight of 500mg each. The individual polymers (Guar gum and Xanthan gum ) were included in the formulation in various proportions (10% to 40 % w/w) while their combinations were employed in the ratio of 30%w/w.Drug release studies were conducted under conditions mimicking mouth-to-colon transit. The dissolution medium consisted of 500 ml 0.1 mol/l HCl kept for 2h, replaced by 500 ml phosphate buffer, pH 7.4 for 3 h, kept at 37±0.5 oC and stirred at 100 rpm, using USP dissolution apparatus 1.Samples were withdrawn at the end of the specified periods (1h,2h,4h,5h,8h,10h,12h,and16h),filtered and assayed spectrophotometrically for diethylcarbamazine, at 250 nm in 0.1 mol/l HCl and 320 nm in pH 7.4 buffer. In order to investigate the release kinetics the dissolution data were fitted into different kinetic models namely zero order, first order and Higuchi models. Korsemeyer et al model was used to determine the mechanism of release. To assess the susceptibility of the prepared DEC delivery systems to the enzymatic action of colonic bacteria, drug release studies were continued in PBS pH 6.8 in the absence (control) and presence of rat caecal contents since these are known to have similar contents to those of human colon. The release study was continued for up to 24h. Samples were withdrawn at different times (6, 8, 10, 12, 16 and 24 h), and assayed spectrophotometrically for DEC at 270 nm. The same volume of fresh dissolution medium was added to restore the initial volume of the dissolution medium after each sample withdrawal. The tablets from various batches exhibited good mechanical properties in terms of hardness, friability, diameter and thickness. Based on in vitro studies, optimum release was observed with formulations containing xanthan gum alone ( 30% w/w and 40% w/w) and in combination (formulation containing xanthan gum 22.5%:guar gum 7.5%, Xanthan 22.5%:). XG 30 % followed first order kinetics via fickian mechanism, while XG 40 % released the drug by zero order kinetics via non-fickian mechanism. The formulations with polymer combinations release the drug fitted best to higuchi kinetics via fickian mechanism. .Presence of xanthan gum in combination with guar gum in the tablets retarded the initial release of drugs from the tablets due to high swelling, which made them more vulnerable to digestion by the microbial enzymes in the colon. Significant difference was observed between drug release in dissolution medium with and without rat cecal contents for al the batches of diethylcarbamazine tablets (P<0.05)....
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