Current Issue : April-June Volume : 2013 Issue Number : 2 Articles : 23 Articles
Ketorolac Tromethamine (KT) is a non-steroidal agent with potent analgesic and moderate anti-inflammatory activity by inhibiting prostaglandin synthesis. The present work deals with the formulation and comparative evaluation of proniosomal and ethosomal gel of Ketorolac Tromethamine. The proniosomal gel was prepared by coacervation phase separation method by using different surfactants. The prepared proniosomal gel formulations were evaluated for vesicle size analysis, rate of spontaneity, entrapment efficiency, in-vitro release and in-vitro permeation study. The vesicle size of the proniosomes varied between 28.84 µm to 34.30 µm, rate of spontaneity between 2.0 mm3 × 1000 to 5.5 mm3 × 1000, % entrapment efficiency was in the range of 21.2% to 38.55%. In-vitro release profiles indicated that, increase in lipophilicity of surfactants decreases the release of Ketorolac Tromethamine. Among the various formulations studied, proniosomal gel with Tween 60 showed the highest % of drug release (80.35%) over a period of 12 hrs. The degree of in-vitro permeation across rat abdominal skin was found to be highest for the formulations P3 with 40.11% after 12 hours. Ethosomal gel formulations were prepared using varying concentrations of ethanol and lecithin. The prepared ethosomal gel formulations were evaluated for vesicle size analysis, entrapment efficiency, in-vitro release and in-vitro permeation study. Vesicle size of the ethosomes varied between 9.56 µm to 19.20 µm, % entrapment efficiency between 19.96% to 30.16%. Formulation E2 showed better in-vitro release profile with 45.46%. The degree of in-vitro permeation across rat abdominal skin was found to be highest for the formulations E1 which was 24.37% after 12 hours. Proniosomal gel formulations showed better entrapment efficiency, in-vitro release profile and permeation compared to ethosomal gel preparations....
Aim of present study was to evaluate the in-vitro drug release kinetic of 4 mg tablets containing non-micronized and micronized glimepiride by using micronization technology. Several tablet formulations were designed, optimized, developed and characterized. Best optimized tablet formulation was selected for further studies. Two batches of the tablets were prepared, one for non-micronized and other for micronized glimepiride 4 mg tablets. These tablets were subjected to evaluation for micromeritics, compatibility, physical properties viz. hardness, thickness, friability, weight variation, uniformity of content and dissolution studies. Total experiment was carried out quite methodically and scientifically. Micromeritics properties of powder blend of both non-micronized and micronized glimepiride 4 mg tablets for direct compression were found within permissible limits for successful compression. Also, it was found that the physical properties of non-micronized and micronized glimepiride 4 mg tablets such as hardness, thickness, friability, weight variation and content uniformity all were found within the Pharmacopoeial limit. No drug-excipients interaction was found and it was confirmed by infra-red spectroscopy which indicates the mutual compatibility. Finally, accelerated stability study was performed and results were compared between the two batches. Results of this studies revealed that, micronized tablet formulation of glimepiride 4 mg released much drug content i.e. 102.74 ± 5.13 % compared to non-micronized tablets which had released just 59.61 ± 8.64 %. Based on the above studies, it can be concluded that micronization of a poorly soluble drug such as glimepiride is an important technique to enhance the rate of dissolution....
Fast disintegrating tablets are now-a-days prominence novel drug delivery because of the faster action. By adding different super disintegrating in different concentration achievement of fast disintegrating is achieved. Diclofenac is a traditional nonsterodial anti-inflammatory agent. It is nonselective cyclooxygenase inhibitor. It inhibits prostaglandin synthesis. And its sodium salt increases its solubility and reduces its side effects. As widely useful in rheumatic arthritis as well as osteoarthritis as a pain relief and wound healing. Here different 9 batches with different disintegrating agent concentration are shown among them croscarmelose (4%) and sodium starch glycolate (3%) showing best result among them....
The studies described in this work were designed to evaluate a new sublingual tablet system using low doses of piroxicam. In this system, water-soluble carrier particles are covered with piroxicam and a bioadhesive material during dry mixing. The formulation was evaluated and compared to the influence of accelerated-aging conditions on the drug content and in vitro dissolution stability of piroxicam fast disintegrating mucoadhesive tablet. Dissolution efficiency (DE) was calculated from dissolution profiles that were performed according to the United State Pharmacopoeia monograph. This determination was performed at time zero, one and three months of storage; (40�°C/75% RH). Each formulation was compared with the reference at the specified times, in terms of DE and similarity factor f2. The in vitro drug release was studied in pH 7.2 Phosphate buffer using Franz diffusion cell. The model independent methods were used to estimate the kinetics of drug release. The criteria for selecting the most appropriate model were based on the goodness-of-fit test. Furthermore, experimentally, we assessed the in vitro transfer of the prepared piroxicam non aqueous emulsion for steady state flux and permeability coefficient through an artificial cellulose acetate membrane....
The purpose of this research work was to improve the solubility and dissolution rate of the telmisartan by using water soluble polymers like Hydroxypropyl methyl cellulose (HPMC E5 LV), Polyethylene glycol-4000 (PEG 4000) and Polyvinyl pyrrolidone (PVP K 30) at pH 7.5 (FDA recommended) using Solid dispersion technique. Solid dispersion of telmisartan were prepared using HPMC E5 LV, PEG 4000 and PVP K 30 polymers in ratios 1:1 to 1:4 (Drug :polymer). Saturation solubility, in-vitro dissolution, particle size distribution, FT-IR spectroscopy, PXRD, DSC and SEM studies were carried out. The results indicated that the formulation containing 1:4 ratio of drug: PVP-K30 showed the cumulative release of 98.42 % as compared to 9.36 % for the pure drug in pH 7.5 phosphate buffers and more than 100 times increases in solubility. X-ray diffraction, differential scanning calorimetry and Fourier transform infrared characterization indicated the solid dispersions exhibited change in crystalline nature. Solid dispersion of telmisartan has been successfully formulated avoiding the need for surfactant, basic amino acid, solubilising agents like alkali hydroxide uses during formulation, there by simplifying the techniques. It was concluded that PVP K 30 can be very well utilized as a carrier to improve the solubility and dissolution rate of poorly soluble drug telmisartan....
The main purpose of this present investigation is to develop de novo extended release system which can be easily administered by oral passage route and to compare with this with our controlled system (A4). In-vitro release data were obtained for each formulation using the dissolution apparatus (type I) at 50 rpm in 6.8 pH phosphate buffer. The extended release of drug from this formulation is superior and is able to maintain the release for almost 11 hours. An extended release rate developed using percent absorbed data and percent dissolved data from the formulation (A1, A2, A3 and A4). However HPMC proves a better and effective polymer and with increase in concentration by wet granulation technique the extendation of drug from HPMC matrixes also increases. This aspirin granule also exerts a good micromeritics property which is important for granules. Release kinetics of aspirin granules shows the zero order kinetics....
Ciprofloxacin is a fluoroquinolone antibacterial drug effective in the treatment of bacterial infections. Ciprofloxacin has a short biological half-life of 2-4 hrs; it has been given frequently to maintain effective plasma concentration, which leads to fluctuation in the plasma concentration and resulting in ineffective therapy. In order to maintain effective plasma drug concentration for prolonged period of time and to reduce several dose related side effects, controlled release formulations of Ciprofloxacin loaded with Ethyl cellulose and various grade of hydroxyl propyl methyl cellulose (HPMC) were formulated by the emulsion-solvent diffusion evaporation technique. The various batches of microspheres were characterized to percentage practical yield, particle size, percentage drug entrapment efficiency and in vitro drug release study. The percent drug entrapment of the prepared microspheres was found to be in the range of 62.43-87.21 % indicating the application of the present method for the preparation of microspheres with high content uniformity. In vitro studies showed that microspheres prepared from F5 batch showed best controlled release over a period of 8 hrs than others....
The aim of the present investigation was to develop oral dispersible films (ODFs) of Granisetran hydrochloride and to investigate the effect of the formulation variable plasticizer on the physic-chemical properties and on the dissolution profile of formulated ODFs. Hydroxypropyl methyl cellulose (HPMC- 50cps) was used as a film former and Poly ethylene glycol (PEG 4000), propylene glycol (PG), sorbitol, glycerin were used as plasticizers. The bioavailability of Granisetron HCl is only 65% indicating extensive first pass metabolism in liver which is an ideal feature for developing ODFs. Hence, the present investigation was undertaken with the objective of formulating ODFs of Granisetran HCl using different plasticizers (Glycerol, PEG, PG, Sorbitol) and to made it potentially useful for treatment of nausea and vomiting and to enhance the convenience and compliance of the elderly and pediatric patients. % drug release profile was found to alter with different plasticizers used and best release profile was observed in case of ODFs with glycerin as plasticizer with around 97% drug release in third minute....
Fast dissolving tablets have been improved the disintegration of tablets so ultimately increase the bioavailability of the drug. Tizanidine is a centrally acting α-2 adrenergic agonist. Here in present study fast dissolving tablets of Tizanidine HCl prepared by using superdisintegrating agents such as crospovidone, crosscarmellose, sodium starch glycolate. Crosscarmellose has less disintegration time as compared to other polymer due to its wicking type of mechanism and capillary action. Crospovidone has a higher disintegration time compared to other polymer. Combinations of polymer have better effects than single polymer. Formulation F9 which formulated by polymers Crosscarmellose and SSG were established to be the optimum formulation because of higher wetting ratio and less disintegration time....
In the present study, formulation of hard gelatin capsule containing granules of Losartan potassium, an antihypertensive drug was designed to achieve immediate release of drug from the dosage form, to increase therapeutic efficacy and to improve patient compliance. Advantages of hard gelatin capsule are rapid drug release possible, flexibility of formulation and sealed hard gelatin capsules are good barriers to atmospheric oxygen. The basic aim of this work is to produce immediate release action of drug from the hard gelatin capsule containing granules of Losartan potassium. Formulations were prepared using wet granulation method and then the formulations are filled into empty hard gelatin capsules for the dissolution studies. The prepared granules were evaluated for percentage yield, angle of repose, bulk density, tapped density, Hausner’s ratio and Carr’s index. The hard gelatin capsule containing granules of losartan potassium were also evaluated for disintegration time, drug content and in-vitro drug release. Stability study shows that there was no significant change in disintegration time, drug content and in-vitro drug release of the formulation. Thus, formulation was considered optimized formulation for immediate release of Losartan potassium....
Repaglinide (RPG) is a non-sulfonylurea oral hypoglycemic agent, mainly used in the management of type II diabetes mellitus. In this work a new attempt was made to enhance the solubility and dissolution rate of poorly soluble Repaglinide via complexation with β-cyclodextrins using various techniques and the feasability of employing Repaglinide inclusion complex in the design of mucoadhesive tablets using various mucoadhesive polymers for sustained release. The phase solubility studies indicated the formation of Repaglinide-β-cyclodextrin (1:1) inclusion complex with a stability constant of 293M-1. Mucoadhesive tablets formulated employing polymers gave slow, controlled and complete release spread over a period of 12 hrs. Drug release from the tablets followed first order kinetics upto 85-90% release and the release was diffusion controlled. The mechanism of drug release was by non Fickian diffusion. Tablets were evaluated for physical parameters, in-vitro dissolution studies, ex-vivo residence time, mucoadhesive strength and swelling index. The optimized inclusion complex and mucoadhesive tablet were evaluated by FTIR, SEM, DSC and XRD studies....
The Aim of the present investigation was to design and evaluate sustained release drug delivery system for Venlafaxine Hydrochloride with reduced frequency of drug administration, reduced side effects and improved patient compliance. Matrix tablets of Venlafaxine Hydrochloride were prepared using combination of various Hydrophobic and Hydrophilic polymers like Eudragit RS 100, EC 45 CPS, HPC EXF & HXF and HPMC K100M. All the precompressional parameter was found to be within the standard limit. No drug excipient incompatibility was seen. Venlafaxine Hydrochloride is an Antidepressant of the serotonin-nor epinephrine reuptake inhibitor (SNRI) After oral administration, Venlafaxine is completely absorbed from the gastrointestinal tract and undergoes extensive first pass metabolism and having low bioavailability (45%) with biological half life of 5hrs. Venlafaxine hydrochloride suitable candidate for developing matrix tablets. The matrix tablets of Venlafaxine hydrochloride were prepared by wet granulation method. The prepared tablets were evaluated for thickness, weight variation, friability, hardness and in vitro release of drug. All the physical characteristics of the fabricated tablets were found to within the acceptable limits. Among the formulations studied, first 5 formulations drug release was very fast and 90% of the drug was released in first 12 hrs only. Further batches were prepared and F9 containing HPMC K100M showed sustained release up to 24hrs and releases 99.31% of drug. Formulations containing HPC EXF, HPC HXF, Eudragit RS100 and EC 45 CPS could not efficiently retard the drug release up to 24hrs. The similarity factor (F2 value) of formulation F-9 was 77.38 and dissimilarity factor (F1 value) was 3.48. Successful development of the formulation fulfils the objective of the study. Hence formulation F9 was selected as the optimized formulation....
The study was undertaken with an aim to formulate and evaluate immediate release pellets of atorvastatin calcium by drug layering method in to order reduce dosing frequency and improve patient compliance. This is due to the fact that atorvastatin calcium which is rapidly absorbed after administration. Preformulation studies like physicochemical properties, solubility of the drug and excipient compatibility study were studied. Formulated Pellets were evaluated for pellet size, hardness, bulk density, tapped density, compressibility index, Hausner’s ratio, drug content, In-vitro dissolution, differential scanning calorimetry (DSC) analysis and release kinetics. In-vitro dissolutions were performed for all the prepared formulations. Dissolution profile of F4 (100.2 ± 0.30 %) was matched perfectly with the innovator formulation (100.31 ± 0.43). Release kinetics indicates that all the formulations follows non- fickian diffusion mechanism. After exposing to short term stability conditions the formulation was analyzed for various evaluation parameters. Results concluded that F4 was found to be best formulation out of all six formulations. It can be concluded that the immediate release tablet was beneficial for delivering the drug which needs faster release to achieve the immediate action....
The aim of the present investigation is to formulation development and evaluation of pulsatile drug delivery system for Anti-Asthmatic drug of Montelukast sodium. Sodium CMC generally used for super disintegrator, it increased the lag time of pulsatile drug delivery system with decreasing the amount of quantity and increased the amount of quantity of Carbopol 971P was generally used for swelling agent, Eudragit RS PO is an enteric polymer and the pH of that 7.4. The formulations were evaluated for Drug content, in-vitro dissolution study, Disintegration time and lag time. The developed formulations of pulsatile drug delivery system which give the better lag time. From these formulation the optimize formulation F3 provide lag time of rupture of PRTs is 6:10 hr and release drug after rupture of outer coat. So we can conclude that the Formulation F3 give better lag time of rupture....
Objective of the present review is to focus recent advancements in gastroretentive drug delivery system (GRDDS) technology and its implications in pharmaceutical formulation development. With upcoming new drug molecules, majority pose challenge in the field due to their lack of solubility and permeability. The way out is either to design new molecules or to opt for a novel approaches for such molecules. Design and development of GRDDS has emerged as a leading tool in the field of site specific drug delivery system. Gastro-retention is of potential benefit for drugs bearing poor solubility and display availability through absorption window. The main aim of present review is to discuss rationale for developing GRDDS and to discuss different advancements in technologies used for design and development of gastroretentive dosage forms....
Polymorphism is the phenomena where drug exists in more than one crystalline form. Though polymorphs are chemically identical, they exhibit different physicochemical properties like melting point, solubility, dissolution profile etc. which further affect the biological properties of drugs. The purpose of this work was to study the effect of solvents of different polarity and processing conditions on crystallization and physicochemical properties of Aceclofenac. The crystals were prepared from solvents of different polarity and processing conditions. The melting point, solubility, dissolution, Fourier Transform Infra-Red Spectroscopy, Differential Scanning Calorimetry, X-Ray Diffraction and Scanning Electron Microscopy studies were carried out to check for polymorphism in drug. Dissolution kinetics was also studied to compare the dissolution profiles of drug and its crystals. The result indicate that the crystal obtained from different solvents and processing conditions exhibited different physicochemical properties. Though FT-IR and XRD gave an indication of difference in the spectra, but DSC proved absence of any polymorphic behavior in the crystals of aceclofenac. It was concluded that the crystals with different properties can be obtained by changing solvent polarity and processing conditions....
The objective of present investigation was to evaluate the flow, mechanical ,compression and release properties of diclofenac sodium tablets formulated by using binders namely starch ,gelatin ,acacia, polyvinyl pyrrolidone. Granule properties were evaluated using Carr's index and Hausner’s ratio. Based on the Carr's index values the flow properties of binders can be ranked as gelatin>acacia>polyvinyl pyrrolidone>Starch. Granule friability and compressibility properties were determined from %Friability and kawakita parameters. The mechanical properties of the tablets were assessed by using crushing strength, while the drug release properties of the tablets were determined by using Disintegration and dissolution parameters. Based on the dissolution rate, the order of performance of binders was Polyvinyl pyrrolidone>Starch>>Gelatin>Acacia. The flow, compression and dissolution characteristics depend on the binder used. Among all, the granule formulated with polyvinyl pyrrolidone exhibits maximum drug release and satisfies in-vitro quality control requirements....
Solubility and dissolution are the rate limiting factors to achieve their desired concentration in systemic circulation for pharmacological response especially poorly water soluble drugs. About 40% of drugs discovered as noble compound can’t reach higher stage being poorly water soluble. Effectiveness of the drug can be severely insufficient by poor aqueous solubility and some drugs also show side effects due to their poor solubility. For formulation scientist, problem of solubility is a major challenge. For pharmaceutical product development several methods for poorly water soluble drugs are available to circumvent these. These methods are preferred on the basis of certain aspects such as properties of drug under consideration, nature of excipients to be selected, and nature of intended dosage form. Solid dispersion, micronization, salt formation, are some of the vital approaches routinely employed to enhance the solubility of poorly soluble drugs but each approach has some limitation and advantages. Novel techniques like nano-suspension, Supercritical processing, cryogenic technology may allow greater opportunities in the delivery of poorly soluble drugs. The solubility behavior of drugs remains one of the most challenging aspects in formulation development. There are several methods are available for solubility and dissolution enhancement of poorly water soluble drugs. Various methods of solubility and dissolution enhancement for poorly water soluble drugs confer in this review....
The main goal of this study was to develop a stable formulation of antibiotic drug Azithromycin as an immediate-release tablet. The task of developing immediate release tablet is accomplished by using a suitable diluents and super-disintegrant. Faster disintegration of the tablet administrated orally minimizes absorption time and improves its bioavailability in less time. Microcrystalline cellulose PH 102 was used as diluents. Povidone was used as the binder. Crosscarmellose sodium and pre gelatinized starch was added as a disintegrating agent. Talc and magnesium stearate was used as the lubricant. The prepared granules were compressed into a compression machine. To evaluate the formulated tablets as per requirements of standards. The tablets thus formulated showed satisfactory physical parameters. Evaluation Parameters Like weight variation, hardness of the tablet, friability, thickness, disintegration test, drug content uniformity and in vitro release studies were performed. To optimize the trial batch by 32 full factorial design study and determined the best batch by in vitro release studies are showed that optimization formulation (OF7) was 101.62% respectively. The optimized formulation is further selected and compared with the release profile of the innovator product. The results suggest the feasibility of developing immediate tablets consisting of Azithromycin for the convenience of patients with respiratory infections, gonorrhoea, community-acquired pneumonia, pelvic inflammatory disease, paediatric otitis media and pharyngitis and Mycobacterium avium complex (MAC) in patients with advanced HIV disease....
Gliclazide is a novel antidiabetic drug of 2nd generation in sulfonylurea group which is classified under BCS Class II. It is characterized by low solubility in gastric fluid, low dissolution rate and inter-individual variability in bioavailability. The objective of this study was to design solid dispersions (SD) of Gliclazide with a hydrophilic carrier viz., Kollidon VA 64 by hot melt extrusion method in an attempt to enhance the aqueous solubility and therapeutic efficacy of the drug. The absorption rate of gliclazide was increased from upper part to lower part of GIT and from jejunum to descending colon which has pH-dependent solubility, drug with complexing agent to increase the solubility of gliclazide and pH-independent release patterns were assigned.Solid dispersions were prepared by using Kollidon VA 64 as carriers, in different drug-to-carrier ratios (1:1, 1:2, 1:3, 1:4) by hot melt extrusion . These formulations were subjected to solubility, dissolution study and were characterized for solid state properties by differential scanning calorimetry (DSC). The optimized solid dispersion (1:4) was characterized for solid state properties by powder X-ray powder diffraction (PXRD) and Fourier Transform Infrared (FTIR) spectral studies. Solid-state characterization revealed the conversion of Gliclazide from crystalline to amorphous form in the formulation (1:4) with Kollidon VA 64. The aqueous solubility and dissolution rate of Gliclazide in solid dispersion was greatly improved when compared to pure form. Solid dispersions also showed efficient wetability and dispersability than pure drug....
Glibenclamide an oral anti-hyperglycaemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). The poor water solubility and poor micromeritic properties of Glibenclamide lead to low dissolution rate and poor flow during tabletting. The aim of present study was to enhance solubility, dissolution rate and improvement of micromeritic properties of the poorly soluble drug. The parameters optimized were type, amount, and method of addition of bridging agent The spherical agglomerate/crystals of Glibenclamide was prepared by solvent change method in the presence of hydrophilic polymer in different concentration. The solvent system used was acetone, water and dichloromethane as good solvent, anti-solvent and bridging liquid respectively. Spherical agglomerates were subjected for determination of percent drug content and particle size analysis. The agglomerates were also characterized by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), X-Ray Powder Diffraction (XRD) and Scanning Electron Microscopy (SEM) analysis. The FTIR and DSC study showed no interaction between drug and polymer. XRD studies showed a slight decrease in crystallinity in agglomerates. Spherical agglomerates showed improvement in solubility, dissolution rate and micromeritic properties in comparison to that of the pure drug. The SEM also showed that the agglomerate possess a good spherical shape....
Recent developments in the technology have presented viable dosage alternatives from oral route for pediatrics, geriatric, bedridden, nauseous or noncompliant patients. Fast dissolving films offer fast, accurate dosing in a safe, efficacious format that is convenient and portable, without the need for water or measuring devices. Fast dissolving films are typically the size of a postage stamp and disintegrate on a patient''s tongue in a matter of seconds for the rapid release of one or more APIs. The present research involves the formulation development of oral films of Famotidine by solvent casting method employing superdisintegrants like sodium starch glycolate, crosscarmellose sodium and crospovidone at different concentration levels. it was concluded that crospovidone (6%) could be used as a super disintegrant and HPMC E5 as a hydrophilic polymer in the formulation of fast dissolving oral films when compared to croscaramellose sodium and sodiumstarch glycolate in the formulations prepared by solvent casting method ....
Poor solubility of new drugs and their related low oral bioavailability and general delivery problems are becoming a major challenge. Nanosuspensions are a “universal” type of formulation for these molecules and are reviewed in this paper regarding their methods of preparation and the recent advancements in the various top down and bottom up approaches. This review has been performed with particular emphasis on the advancement in the different techniques of preparation of nanosuspensions and the drugs under investigation. Special focus has also been made in the use of stabilizer and advancement in the scale up techniques....
Loading....