Current Issue : July-September Volume : 2015 Issue Number : 3 Articles : 10 Articles
Oral route of administration is most common and preferred method of delivery due to its convenience and ease of ingestion. BCS class II drugs are poorly water soluble drug with low aqueous solubility and high permeability, such drugs exhibit dissolution rate limited absorption resulting in poor bioavailability of drug when deliver through oral route. Solid dispersion is very efficient technique to increase the bioavailability and dissolution rate of poorly soluble drug. This article reviews background of solid dispersion, classification, advantages, disadvantages, selection of solvents and carriers. It also reviews characterization and method of preparation of solid dispersion....
The objective of present study was to design and evaluate immediate release tablets of digoxin. There are various tablet formulations of digoxin available in the market. The purpose of the research is, to prepare digoxin immediate release tablet with low cost excipients as compared to marketed formulation and also to explore hydro-alcoholic wet granulation technique. In order to obtain the best product, nine different formulations were developed by using different filler, disintegrants and lubricants. The immediate release tablets were evaluated for weight variation, thickness, hardness, friability, disintegration time, content uniformity and in-vitro drug release. The in-vitro drug release was found to be faster in all formulations except F008 and F009 as compared to that of the reference product. The different physical properties and in-vitro release profile showed F008 and F009 as the best formulations comparable with the reference product and that F009 reproducible batch of F008....
The objective of the current study was to develop and optimize oral disintegrating tablets of rosiglitazone maleate which is an effective drug in the treatment of type II diabetes mellitus. Rosiglitazone maleate containing tablets were prepared by direct compression method using different ingredients such as croscarmellose sodium, crospovidone, potato starch, sodium saccharine, lactose, talc and magnesium stearate. The tablets were evaluated for physical properties including hardness, weight variation, thickness, friability, drug content, in-vitro disintegration time and in-vitro dissolution study. The hardness, weight variation, thickness, friability and drug content of tablets were found to be acceptable according to pharmacopoeial limits. An optimized tablet formulation i.e. F12 was found, which provided short in-vitro disintegration time of 10.14 sec. From the above results, it indicated that the amount of superdisintegrant i.e. crospovidone and croscarmellose sodium was significantly affected the dependent variables like in-vitro disintegration time. The best in-vitro drug release was found to be in F12 98.67% during the end of 60 min....
The present study was planned to design an immediate release film coated tablet of atorvastatin calcium, which is used in cardiovascular diseases (CVD). CVD are the most prevalent cause of death and disability in both developed as well as developing countries. Atorvastatin calcium is BCS class II drug having low solubility and high permeability, it has less acid stability and produces lactone impurity in acidic media. Formulation of atorvastatin calcium immediate release tablet is planned to enhance acid stability and water solubility. Immediate release tablet of atorvastatin calcium was formulated by using different formulation approaches such as direct compression and wet granulation method by using rapid mix granulator. The excipients used in designed formulation are less in cost as compared to the marketed formulation. Drug is highly susceptible to moisture and at low pH environments; the objective of our study is to protect atorvastatin calcium from moisture and low pH environment. Film coating was applied to protect formulation from moisture by using OPADRY® white which contained hypermellose, polyethylene glycol, TiO2 and talc. Calcium carbonate was used in the designed formulation which acts as a stabilizer by neutralizing acidic pH environment hence it increases the acid stability of the formulation. Batch F6 formulation was found to be the best formulation which was prepared by the wet granulation method and it contains surfactant polysorbate 80 which has shown significant improvement in percent cumulative drug release. The batches F7 to F10 were formulated by using same formula and procedure used for batch F6 to check reproducibility of the formulation. The result obtained for batch F7 to F10 formula are found equivalent to batch F6 formula, which proves reproducibility of the formulation....
Fabrication of zolmitriptan nasal gel was aimed to get better absorption and patient compliance. Nasal route of administration would also thwart the pre systemic metabolism thus mounting the bioavailability of the drugs. In the present study various formulations were prepared by using gellan gum as gelling agent and mixture of HPMC K 100 and carbopol 940 as controlled or sustained release polymer. Zolmitriptan, 4S-4-({3-[2-(dimethylamino) ethyl]-1H-indol-5-yl} methyl)-1, 3-oxazolidin -2- one, is a second –generation triptan prescribed for patients with migraine attack. All the formulations were investigated for various parameters like pH, viscosity, drug content, gel strength, mucoadhesive strength and release of active pharmaceutical excipient. At least amount of polymer mislay their integrity and at highest concentration stiff gel were formed. At optimized concentration of gelling agent and PVP K25 showed in-situ gelling with all parameter in range. In-vitro release data exposed that the optimized formulation showed controlled and sustained release pattern....
The main aim of the present study was to formulate, evaluate the extended release matrix tablets of tramadol HCl and to match the in-vitro drug release profile with the drug release criterion of the drug according to USP 37 NF 32. Extended release tablets were prepared by non-aqueous wet granulation method using HPMC K100 M, HPMC K15 M, HPMC K100 M LVP, HPMC K15 M CR, carbopol 971 NF and carbopol 71G as release retardants. The powder blend was evaluated for pre-compressional parameters like angle of repose, tapped density, bulk density, carrs index and Hausner’s ratio. Then the tablets were evaluated for post-compressional parameters viz weight variation, hardness, thickness, friability and in-vitro drug release pattern. Among all formulations F7 showed best drug release pattern which matched with drug release criterion of the drug. The drug kinetic modeling was established for zero order, first order, Higuchi and Korsemeyer peppas. The drug release mechanism confirmed that it followed first order release kinetics. From Highuchi kinetics it was concluded that most of the formulations diffusion was major release mechanism. From korsemeyer peppas, mechanism of drug release was diffusion coupled dissolution followed by erosion....
The main objective of the present work was to develop extended release matrix tablets of ranolazine, to reduce the frequency of administration and to improve the patient compliance; a once daily extended release formulation of ranolazine is desirable. Ranolazine is an anti-anginal drug used to treat chronic stable angina in adults. The main drawback with normal conventional dosage form is that the solubility of ranolazine is relatively high at the lower pH (4.5 and below) and also has short plasma half-life of 7 hrs. Ranolazine comes under class II of biopharmaceutical classification system. The ranolazine 500 mg extended release matrix tablets were prepared by wet granulation method using different polymers. Pre-formulation studies were done initially and the results were found to be within the limits. All the mentioned batches were prepared and granules were evaluated for pre-compression parameters such as loss on drying, bulk density, tapped density, hasuner’s ratio and compressibility index. Tablets were evaluated for weight variation, thickness, hardness and friability, were found to be within limits. The in-vitro release of ranolazine extended release tablets was studied in 900 ml of 0.1 N HCl as dissolution medium using a USP dissolution paddle assembly at 50 rpm and 37±0.5°C for 24 hrs. Final selection of formulation (F8) exhibited in-vitro drug release that matched with marketed product (Rancad 500 mg). The (F8) formulation shown best results of 99.26% drug release in 24 hrs....
Fast dissolving films have been played an important role in the current pharmaceutical research. They have convenience and ease of use over other dosage forms such as orally disintegrating tablets and immediate release tablets. In the present research, rapidly dissolving films of flunarizine dihydrochloride were developed using low viscosity grades of HPMCE50LV, CMC as film forming polymers. HPMCE50LV, CMC is a water soluble synthetic polymer which was used as film former. The films of flunarizine dihydrochloride were prepared by solvent casting method using ethanol as solvents. The prepared films were evaluated for drug content, weight variation, thickness, pH and in-vitro disintegration time. Flunarizine dihydrochloride is a hypertensive drug; taste masking was achieved by use of sweeteners, flavors’ and sodium saccharin. The in-vitro dissolution time of the optimized formulation was carried 30, 60, 90, 120, 150, 180 sec respectively. The prepared films exhibited good integrity and thickness. In-vitro dissolution studies were performed as per the FDA dissolution guidelines for about 3 minutes, the optimum formulation released complete drug within 2.5 minutes. Dissolution was done for all prepared formulation among all formulation F -7 formulations which are having HPMC E 50 LV and SLS in-vitro drug release 98.6 % in 3 seconds FTIR studies showed no drug polymer interaction....
The objective of the present study was to design and develop microemulsion based gel formulation of imidazole substitute for enhancing its solubility and permeability. Topical permeability of bifonazole is very low. For this purpose, initially, solubility and permeability of bifonazole was determined in various vehicles. Dissimilar formulations of bifonazole in microemulsion base using isopropyl myristate as oil phase, Acrysol K150 as surfactant and plurol oleique as co-surfactant after preliminary screening of excipients. Carbopol 971 as gelling agent. Isopropyl myristate was chosen as oil phase due to its good solublizing capacity. Microemulsion existence region was specified using the pseudo-ternary phase diagrams for preparing dissimilar formulations. The system was optimized by ternary phase diagram. The equipped formulations were characterized for drug content, % transmittance, visual assessment, particle size, zeta potential and compare in-vitro diffusion study of prepared microemulsion based gel with marketed formulation, Skin irritation study. The optimized batch contains mean particle size of 28.57nm and zeta potential (ζ) -8.25mV and viscosity study and spreadability also in-vitro permeation study. In-vitro diffusion study of optimized formulation MEB2 carried out which gives satisfactory release. Therefore by formulating into microemulsion based gel the solubility of bifonazole was found to be significantly improved....
A gas chromatographic method has been developed for the determination of propionic acid in pramipexole hydrochloride drug substance. The method was optimised based on the basis of peak shape of propionic acid. The method was validated as per ICH guideline in terms of LOD, LOQ prediction, precision, accuracy, method precision, repeatability and specificity. The LOD and LOQ values were found to be 21 and 64 µg/g and linearity range was found to be 0.99875 and hence three commercial batches was analysed and propionic acid was not found in all three batches....
Loading....