Percentage Friability Research Articles

DEVELOPMENT AND IN VITRO EVALUATION OF AN ORAL FLOATING TABLET OF METRONIDAZOLE

The present study was undertaken with an aim to develop and evaluate gastroretentive floating tablets of Metronidazole that are designed to retain in the stomach for a long time and have developed as a drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. The floating tablets of Metronidazole were made by direct compression method using polymer Carbopol 934 and sodium bicarbonate and citric acid as gas generating agent. The tablets were evaluated by pre and post compression parameters such as weight variation, thickness, friability, hardness, drug content, in- vitro buoyancy studies and in-vitro dissolution studies and results were within the limits. Hardness was found to be in the range of 7.6 ± 0.27 kg/ cm² to 7.9 ± 0.35 kg/cm², the percent friability was in the range of 0.48% to 0.52% w/w and the tablets showed 94% to 97% uniformity in drug content. The in-vitro dissolution studies were carried out in a USP type- II apparatus in 0.1N HCl. The formulations were able to within 2-7 minutes and showed buoyancy >12 hrs. The drug-polymer ratio, viscosity grades of Carbopol 934 and gas generating agents were found to influence the release of drug and floating characteristics from the prepared floating drug delivery system of Metronidazole. Kinetically, among the 4 assessed models the release pattern of Metronidazole from the tablets fitted best to Higuchi’s and zero order indicated that diffusion is the predominant mechanism controlling the drug release. Keywords: Metronidazole, Floating tablets, Carbopol 934, Gastroretentive, Dissolution

FORMULATION AND DESIGN OF EXTENDED RELEASE MATRIX TABLETS OF ZIDOVUDINE HYDROCHLORIDE: A STUDY ON EFFECT OF VARIOUS GRADES OF ETHOCEL AND HPMC

Objective: The current research was an attempt to formulate and design an extend release dosage form of zidovudine hydrochloride using various grades of ethyl cellulose (ethocel) such as ethocel 4CPS, ethocel 7 CPS and aqualon T10 Pharm EC with two grades of hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M).Methods: Pilot scale batches of nine formulations were prepared using kollidon and adopting wet granulation technique. Physiochemical properties of tablet and granules were examined prior compression to get tablet. Tablets were characterized as drug content, percentage weight variation, thickness, Hardness, percentage friability and in vitro drug release pattern and studied for 12 hour in USP Type-II apparatus using 900 ml Phosphate buffer at 37±0.5 °C. The dissolution release profile of drug in tablet was performed by various drug release kinetic modelling.Results: The result revealed formulation F8 containing ethocel 7CPS and aqualon T10 was able to delay the pure drug release for 12 h and followed Higuchi pattern. Whereas; formulations containing only ethocel 4CPS provided earlier drug release. Dissolution data of promising formulation were analysed with innovator formulation for similarity factor (f2), exhibited an acceptable value more than 50. FT-IR (fourier-transform infrared spectroscopy) and DSC (differential scanning calorimetry) study revealed no such incompatibility found between the pure drug and polymers but slight change in crystalinity were observed in XRD study (X-ray diffraction). SEM (scanning electron microscope) study revealed very rare intragranular pore and cavity.Conclusion: From that, it can be marked as viscosity and selection of ethocel have great importance in delay drug release.

Quality Assessment of Selected Vitamin C Tablets Sold at Bridge Head Market, Onitsha

Due to the importance of ascorbic acid in humans, qualitative and quantitative evaluation of ascorbic acid has gained a significant increase in several areas of analytical chemistry such as pharmaceutical analysis. Several analytical methods have been developed. Most of these methods are laborious and some require much reagents that may be either not readily available or are expensive. There is an influx of counterfeit drugs in the market and due to this, two questions come up; are we underdozed? Or overdozed? This is a research on the quality of selected brands of Vitamin C tablets. In this research work, five brands of Vitamin C tablets were purchased at Bridge head market, Onitsha and were analyzed for their percentage content of Ascorbic Acid (active pharmaceutical product), their average percentage friability, disintegration time and hardness using a UV/Vis spectrophotometer, friabilator, disintegration tester and hardness tester. The results showed that they all passed the hardness and disintegration time test. Samples 1, 3, 4, and 5 failed the test for the percentage content of Ascorbic acid; Sample 2 failed the friability test. Sample 2 has proven to have the highest quality and would be able to enact action faster since it has the highest quantity of Ascorbic acid that will be disintegrated at any time and this also means that it will be absorbed into the blood stream faster.

DESIGN AND EVALUATION OF CHRONOTHERAPEUTIC PULSATILE DRUG DELIVERY SYSTEM OF CILNIDIPINE

Objectives: Cilnidipine is the novel calcium antagonist accompanied with L-type and N-type calcium channel blocking function used for the treatment of hypertension. The aim of present work is formulate and evaluate a press coated pulsatile release tablets of Cilnidipine using an admixture of hydrophilic polymers in order to achieve a predetermined lag time for chronopharmacotherapy of Hypertension. Methods: The pulsatile drug release tablets were prepared by compression coating method. The tablets prepared were evaluated for different properties like bulk density, tapped density, angle of repose and Carr’s index), hardness, thickness, weight variation, friability, drug content uniformity and in vitro drug release study. Results: All formulations have shown good flow properties. The hardness of tablets ranged between 4.93±0.08 to 5.96±0.11 kg/cm2, percentage friability of tablets ranged between 0.68±0.21 to 0.82±0.06. Maximum drug release was found to be 94.39%. Conclusion: Study concludes that the prepared pulsatile drug delivery system can be considered as one of the promising formulation technique for delivery of Cilnidipine. Formulation of batch CPT1was found to be optimum. Peer Review History: Received 15 September 2017; Revised 28 October; Accepted 5 November, Available online 15 November 2017 Academic Editor: Ahmad Najib, Universitas Muslim Indonesia, Indonesia, ahmad.najib@umi.ac.id UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file: Reviewer's Comments: Average Peer review marks at initial stage: 4.5/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Dr. Viney Chawla, University Institute of Pharmaceutical Sciences, Baba Farid University of Health Sciences, Sadiq Road, Faridkot-Punjab 151203, drvineychawla@gmail.com Dr. Barkat Ali Khan, Kampala International University , Uganda, barki.gold@gmail.com

FORMULATION AND EVALUATION OF FUROSEMIDE LIQUISOLID COMPACT

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.

Torsemide Fast Dissolving Tablets: Development, Optimization Using Box-Bhenken Design and Response Surface Methodology, In Vitro Characterization, and Pharmacokinetic Assessment.

The present study planed to develop new fast dissolving tablets (FDTs) of torsemide. Solid dispersions (SDs) of torsemide and sorbitol (3:1) or polyvinylpyrrolidone (PVP) k25 were prepared. The prepared SDs were evaluated for in-vitro dissolution. Fourier transform infrared spectroscopy and differential scanning calorimetry for SDs revealed no drug/excipient interactions and transformation of torsemide to the amorphous form. Torsemide/sorbitol SD was selected for formulation of torsemide FDTs by direct compression method. Box-Bhenken factorial design was employed to design 15 formulations using croscarmellose sodium and crospovidone at different concentrations. The response surface methodology was used to analyze the effect of changing these concentrations (independent variables) on disintegration time (Y1), percentage friability (Y2), and amount torsemide released at 10min. The physical mixtures of torsemide and the used excipients were evaluated for angle of repose, Hausner's ratio, and Carr's index. The prepared FDTs tablets were evaluated for wetting and disintegration time, weight variation, drug content, percentage friability, thickness, hardness, and in vitro release. Based on the in-vitro results and factorial design characterization, F10 and F7 were selected for bioavailability studies following administration to Albino New Zealand rabbits. They showed significantly higher C max and (AUC0-12) and shorter T max than those obtained after administration of the corresponding ordinary commercial Torseretic ® tablets. Stability study was conducted for F10 that showed good stability upon storage at 30°C/75% RH and 40°C/75% RH for 3months.

FORMULATION AND EVALUATION OF NICORANDIL FLOATING PULSATILE PELLETS FOR CHRONOTHERAPEUTIC DRUG DELIVERY

The objective of the work was to develop nicorandil floating pulsatile pellets by pan coating technique where drug loaded pellets were coated with pH dependent polymer Eudragit S100 for chronotherapy of angina pectoris, an underlying cause of heart attack. These pellets were evaluated for micromeritics properties, particle size, percent entrapment efficiency, percent friability, in vitro floating ability, drug release and kinetics of pellets. The optimized batch exhibited good entrapment efficiency and flow properties, optimum friability and good floating property and released the drug at right time when symptoms are at peak level in early hours by maintaining required lag phase during floating in acidic medium for 5 hours, followed by burst release in simulated intestinal fluid (pH 7.4 phosphate buffer). It followed first order kinetics. Scanning Electronic Microscopy analysis of optimized batch revealed that the pellets were spherical in shape with smooth surface.

DESIGN AND DEVELOPMENT OF TASTE MASKED ORAL DISINTEGRATING TABLET OF ONDANSETRON HYDROCHLORIDE

Ondansetron HCl is effective in the treatment of nausea and vomiting caused in such condition it is difficult to administer drug with a glass of water; hence it is beneficial to administer such drugs as orodispersible. Thus in the present study an attempt has been made to mask the taste of Ondansetron HCl and to formulate orodispersible with good mouth feel so as to prepare a “patients friendly dosage form.”. The tablets prepared by sublimation method. The prepared tablets were evaluated for various pharmaceutical characteristics such as hardness, % friability, weight variation, drug content all the results were within the IP. Limit. The tablets prepared possess a weight variation in the range 99 to 101 mg which is below ± 7.5%, hardness of 2.7 to 3.0 kg/cm2, percentage friability of 0.42 to 0.73%. The wetting time of Ondansetron HCl fast dissolving tablets was found to be in the range of 44 to 81 sec. The prepared formulations shows water absorption ratio in the range of 72 to 85%. The percentage drugs content of the tablets were found to be between 98.24 to 101.20% of Ondansetron HCl. In-vitro disintegration time the formulations OHS4 and OHS8 were found to be promising and showed a 28 sec and 32 sec respectively. Based on the in-vitro disintegration time and dissolution studies formulations OHS4 and OHS8 were found to be promising and showed a disintegration time of 28 sec and 32 sec respectively. Formulation OHS4 containing camphor showed highest drug release 99% within 8 min. Formulation OHS8 showed highest drug release 90% within 8 min. From FTIR and DSC study results reveals that there is no interaction between drug and any other formulation excipients. In case of stability study there is decrease in disintegration time, wetting time was observed. The results concluded that fast dissolving tablets of Ondansetron HCl showing enhanced dissolution will lead to improved bioavailability and effective therapy. This drug resin complex was compressed in tablets by adding diluents to see its mouth feel properties and bitter taste is masked.

Development of a multi-layered vaginal tablet containing dapivirine, levonorgestrel and acyclovir for use as a multipurpose prevention technology

Multipurpose prevention technologies (MPTs) are preferably single dosage forms designed to simultaneously address multiple sexual and reproductive health needs, such as unintended pregnancy, HIV infection and other sexually transmitted infections (STIs). This manuscript describes the development of a range of multi-layered vaginal tablets, with both immediate and sustained release layers capable of delivering the antiretroviral drug dapivirine, the contraceptive hormone levonorgestrel, and the anti-herpes simplex virus drug acyclovir at independent release rates from a single dosage form. Depending on the design of the tablet in relation to the type (immediate or sustained release) or number of layers, the dose of each drug could be individually controlled. For example one tablet design was able to provide immediate release of all three drugs, while another tablet design was able to provide immediate release of both acyclovir and levonorgestrel, while providing sustained release of Dapivirine for up to 8h. A third tablet design was able to provide immediate release of both acyclovir and levonorgestrel, a large initial burst of Dapivirine, followed by sustained release of Dapivirine for up to 8h. All of the tablets passed the test for friability with a percent friability of less than 1%. The hardness of all tablet designs was between 115 and 153N, while their drug content met the European Pharmacopeia 2.9.40 Uniformity of Dosage units acceptance value at levels 1 and 2. Finally, the accelerated stability of all three actives was significantly enhanced in comparison with a mixed drug control.

Influence of pressurized carbon dioxide on ketoprofen-incorporated hot-melt extruded low molecular weight hydroxypropylcellulose

Objectives: The aim of the current research project was to investigate the effect of pressurized carbon dioxide (P-CO2) on the physico-mechanical properties of ketoprofen (KTP)-incorporated hydroxypropylcellulose (HPC) (Klucel™ ELF, EF, and LF) produced using hot-melt extrusion (HME) techniques and to assess the plasticization effect of P-CO2 on the various polymers tested.Methods: The physico-mechanical properties of extrudates with and without injection of P-CO2 were examined and compared with extrudates with the addition of 5% liquid plasticizer of propylene glycol (PG). The extrudates were milled and compressed into tablets. Tablet characteristics of the extrudates with and without injection of P-CO2 were evaluated.Results and conclusion: P-CO2 acted as a plasticizer for tested polymers, which allowed for the reduction in extrusion processing temperature. The microscopic morphology of the extrudates was changed to a foam-like structure due to the expansion of the CO2 at the extrusion die. The foamy extrudates demonstrated enhanced KTP release compared with the extrudates processed without P-CO2 due to the increase of porosity and surface area of those extrudates. Furthermore, the hardness of the tablets prepared by foamy extrudates was increased and the percent friability was decreased. Thus, the good binding properties and compressibility of the extrudates were positively influenced by utilizing P-CO2 processing.

Formulation optimization of mouth dissolving tablets of Meloxicam using mixed hydrotropic solublization technique

The objective of the present study was to develop mouth dissolving tablets of meloxicam in order to achieve rapid release in saliva which may result in enhanced absorption and thereby improved bioavailability. Six batches of mixed hydrotropic solid dispersions and physical mixtures were prepared using different ratios (1:2, 1:4 and 1:6) of hydrotropic blends (urea, Nicotinamide & sodium citrate). The best batch was selected to prepare mouth dissolving tablets comprising solid dispersion of Meloxicam in six preliminary batches using croscarmellose sodium & crospovidone as superdisintegrants and camphor as subliming agent in different ratios along with other excipients. Secondary batches were prepared based on 32 factorial design with amount of superdisintegrant (crospovidone) and camphor (subliming agent) as two independent formulation variables. Two dependent response variables considered were disintegration time and percentage friability. All the batches of mouth dissolving tablets were evaluated for pre-compre sion parameters and post-compression parametes. The results of accelerated stability studies revealed no physical and chemical changes in the tablets during three months.

FORMULATION DEVELOPMENT AND EVALUATION OF SR MATRIX TABLETS OF PEFLOXACIN

The basic objective in dosage form design is to optimize the delivery of medication to achieve the control of therapeutic eff ect in the fa ce of uncertain fluctuation in the system in which drug release takes place. This is usually concerned with the maximum drug availability by attempting to attain a maximum rate and extent of drug absorption, however ; control of drug action through formulat ion also implies controlling the bioavailability to reduce drug absorption rates. So in the present study, an attempt has been made to formulate sustained release matrix tablets of Pefloxacin. Tablets were prepared using a direct compression method employi ng natural sustain ed release polymer such as Xanthum gum in different concentrations . The tablets were evaluated for physical characteristic like hardness, weight variation, friability and drug content. In - vitro release of drug was performed in phosphate b uffer pH 6.8 for fourteen hours, percent friability 0.22 % and disintegration time 2.20 h. All the physical characters of the fabricated tablet were within the acceptable limits . The data obtained from in vitro dissolution studies were fitted in different models viz. Zero order, first order, Higuchi and Korsmeyer - Peppas equation. It was also observed that the highest correlation was for Korsmeyer - Peppas profile (R 2 = 0 . 9938). A value of n for all matrices studied here was ranged between 0.4339 to 0.4840; indicating an anomalous behavior corresponding to swelling, diffusion and erosion mechanism .

Formulation and evaluation of sustained release venlafaxine tablets using hydrophilic-hydrophobic polymer combinations by melt granulation

The current research aims to formulate Venlafaxine Sustained Release (VHL-SR) tablets using hydrophilic-hydrophobic polymers combination blends by melt granulation technique which highlights the novelty. The polymers selected for the present study have matrix forming properties. Results of FTIR studies have shown that there were no interactions between the polymers used and the drug VHL. Various formulations of VHL- SR tablets (F1-F16) using different combinations of hydrophilic and hydrophobic polymers viz. Carbopol 71G, HPMC K15M, PEO, sodium CMC, Eudragit RS100 and precirol were formulated. Prior preformulation studies carried out on powder blend showed good flow properties. Routine quality evaluations of the VHL-SR tablets showed the diameter of the tablets of all formulations were found to be 9.0±0.0 mm and thickness ranged between 2.08±0.08 to 2.25±0.14 mm, hardness 4.08±0.20 - 5.50±0.31 kg/cm2 , percentage friability 0.24±0.03 - 0.45±0.01%, weight variation from 0-1.15%, drug content uniformity from 98.17±0.68 to 101.89±0.73%, all within Pharmacoepial limits. Results of in-vitro drug release study indicated that the formulation containing Carbopol 71G (50 mg), Xanthan gum (75 mg) and MCC (50 mg) extended the release of the VHL. Formulation F15 was the optimized one which gave satisfactory release (95.2%) for 16 hr and with a similarity factor (f2) 68.46, the release kinetics best explained by the Korsmeyer-peppas and Higuchi diffusion models. The “N” values between 0.5-1.0 in all the formulations exhibiting a non-Fickian release behavior controlled by a combination of diffusion and chain relaxation mechanism. The formulation showed appreciable stability under accelerated conditions after 2 m.

Formulation and in vitro evaluation of fast dissolving tablets of metoprolol tartrate

The demand for fast dissolving tablets has been growing during the last decade, especially for elderly and children who have swallowing difficulties. In the present work, fast dissolving tablets of metoprolol tartrate, were prepared using sodium starch glycolate, sodium croscarmellose and crospovidone as superdisintegrants, by the direct compression method. The tablets prepared were evaluated for various parameters including weight variation, hardness, friability, in vitro dispersion time, drug-polymer interaction, drug content water absorption ratio, wetting time, in vitro drug release, FTIR and DSC studies. The tablets prepared by the direct compression method had a weight variation in the range of 145 mg to 152 mg, which is below ± 7.5%, a hardness of 3.6 kg/cm² to 4.5 kg/cm², percentage friability of 0.46% to 0.73%, in vitro dispersion time of 18 s to 125 s, drug content uniformity of between 98.12% and 100.03%, a water absorption ratio of 67% to 87%, wetting time of 32 sec. to 64 sec., and an in vitro drug release of 53.92% - 98.82% within 15 min. The IR spectral analysis and DSC study showed no drug interaction with formulation additives of the tablet, and the formulations indicated no significant changes in hardness, friability, drug content or in vitro drug release. Fast dissolving tablets of metoprolol tartrate have enhanced dissolution and will lead to improved bioavailability and more effective therapy.

Formulation Development of Oral Mucoadhesive Tablets of Losartan Potassium using Mucilage Isolated from Diospyros melonoxylon Roxb Seeds


 Diospyros melonoxylon Roxb is a small tree with rather slender stem and smooth grey bark belonging to family Ebenaceae found widely in Chhattisgarh. The present investigation reports the isolation of mucilage from Diospyros melonoxylon seeds as per AOAC guideline and evaluating it as mucoadhesive agent. Physiochemical characteristics of mucilage, such as appearance, solubility, swelling index, microbial count, loss on drying, viscosity, hydration capacity, flow property, hausner ratio and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, using Losartan Potassium as model drug. Granules were prepared by wet granulation process using polyvinylpirroli-done as binding agent. Mucilage was used in four different concentrations i.e. 20, 40 and 60 % w/w. The prepared granules were evaluated for micrometrics property. The tablet were prepared and evaluated for weight variation, thickness diameter, hardness, percent friability, in vitro dissolution and degree of swelling. The property of bioadhesive strength of isolated mucilage was compared with Guar Gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. The tablets had good physiochemical properties, and drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.2063N, 0.3837N, 0.5175N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study of effect of intensity of agitation at different rpm (50 and 150) and electrolyte (NaCl and CaCl2), and formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months all formulation showed stability with respect to release pattern.

Oral disintegration tablets of stavudine for HIV management: A new technological approach

Stavudine oral disintegration tablets were formulated to minimize the bitter taste and to reduce the first-pass hepatic metabolism. The various precompression parameters like the angle of repose, bulk density, compressibility index and Hausner's ratio were determined for the powder blend. In this study, 14 formulations of stavudine oral disintegration tablet were prepared by direct compression method. The tablets were evaluated for weight variation, percentage friability, disintegration time, hardness, wetting time and water absorption ratio. The in vitro dissolution study results of the batch S1 (stavudine+crospovidone+sodium starch glycollate) are encouraging as highest dissolution rate (99.2% in 100 min) and lowest time of disintegration (56 s) was achieved. The in vivo drug release studies were carried out in rabbits and the relative bioavailability of formulation S1 was found to be 2.83 times greater than that of conventional tablets.

Development and Characterization of Mouth Dissolving Tablet of Zolmitriptan

ObjectiveTo formulate and Characterize Mouth Dissolving Tablet of Zolmitriptan to produce the intended benefits. MethodsTablets were prepared using a direct compression method employing superdisintegrants such as Kyron T-314, Crospovidone, Croscarmellose Sodium, and Sodium Starch Glycolate. Tablets of Zolmitriptan prepared using Kyron T-314 exhibited the least friability and disintegration time 35 seconds. To decrease the disintegration time further, a sublimation technique was used along with the superdisintegrants for the preparation of Mouth Dissolving Tablet (MDTs). The addition of camphor as a subliming agent lowered the disintegration time 10 seconds further, but the percent friability was increased. A 32 full factorial design was employed to study the joint influence of the amount of superdisintegrant (Kyron T-314) and the amount of sublimating agent (Camphor) on the percent of friability and the disintegration time. ResultsThe results of multiple linear regression analysis revealed that an effective MDT of Zolmitriptan requires higher percentages of Kyron T-314 and camphor should be used. The approach using the optimization technique helped to produce a detailed understanding effect of formulation parameters. An optimized formulation was found to have good hardness, wetting time, disintegration time. Release kinetic model study indicated that all the formulations follow zero order kinetics. It also indicated that batch F1, F2, F5 and F8 releases the drug at constant rate as well as fast rate as per the Weibull model which was also confirmed by Hixson-Crowell model. Stability studies indicated that there are no significant changes in hardness, Percentage friability, drug content and in-vitro disintegration time and cumulative percentage drug release. ConclusionsThus, it was concluded that by adopting a systematic formulation approach, Zolmitriptan Mouth dissolving tablet could be formulated using superdisintegrants in combination with a vacuum-drying technique for improved therapeutic efficacy.

In vitro evaluation of Moringa oleifera gum for colon- specific drug delivery

Background:Moringa gum obtained from stem of the plant Moringa oleifera Lam. belonging to family Moringaceae. Number of naturally occurring polysaccharides obtained from plant (guar gum, inulin), animal (chitosan, chondrotin sulphate), algal (alginates) or microbial (dextran) origin.Objective:The present study was evaluated Moringa oleifera gum as a carrier for colon specific drug delivery using in vitro drug release studies.Materials and Methods:Six formulations of curcumin were prepared using varying concentration of Moringa oleifera gum containing 50 mg curcumin by wet granulation method. Tablets were subjected for evaluation by studying the parameter like hardness, friability, drug content uniformity and in vitro drug release study. Hardness was found to be in the range of 5.5 to 7.3 kg/cm2, the percentage friability was in the range of 0.60 to 0.89%, and tablet showed 98.99% to 99.89% of the labeled amount of curcumin indicating uniformity in drug content.Results and Discussion:In vitro drug release study was performed using simulated stomach, intestinal and colonic fluid. The susceptibility of Moringa gum to colonic bacteria was also assessed using drug release study with rat caecal contents. 30% Moringa gum containing formulation (F-3) was shown better drug released that is 90.46%, at the end of 24 h of dissolution study in the presence of rat caecal contents in comparison to 40% Moringa gum containing formulation (F-4) that was 78.03%.Conclusion:The results illustrate the usefulness of Moringa olefera gum as a potential carrier for colon-specific drug delivery.

PREPARATION AND EVALUATION OF COPROCESSED SUPERDISINTEGRANT IN THE DESIGN OF PROCHLORPERAZINE MALEATE FAST DISSOLVING TABLETS

The demand for fast dissolving tablet (FDT) has been growing during the last decade especially for elderly, children and patients who have swallowing difficulties. This dosage form is placed in the mouth, allowed to disperse or dissolve in the saliva, and then swallowed without the need of water. The problem of certain FDT is their low resistance and high friability. FDT having alone superdisintegrant have slow disintegration and high friability. The purpose of this study was to prepare and evaluate the coprocessed superdisintegrant in promoting tablet disintegration and having low friability. Attempt was made to develop FDT of Prochlorperazine Maleate with the help of coprocessed superdisintegrant. The tablets were evaluated for its percentage friability, disintegration time, wetting time, and hardness. In the investigation, a 32 full factorial design was used to investigate the combined influence of two formulation variables: amount of sodium starch glycolate and crospovidone. The results of multiple linear regression analysis revealed that for obtaining a hard and rapidly disintegrating dosage form. A checkpoint batch was also prepared to prove the validity of the evolved mathematical model. The concentration was optimized at which FDT disintegrate within 30 seconds and having friability 0.60%. A response surface plot is also presented to graphically represent the effect of the independent variables on the disintegration time and percentage friability. Optimized FDT should be prepared using an optimum concentration of sodium starch glycolate and crospovidone. Short-term stability studies indicated that there are no significant changes in drug content and in vitro disintegration time. The optimized tablet was found to be stable and shelf life is predicted more than two years.

Utilization of Superdisintegrants in the Design, Evaluation and Optimization of Orodispersible Tablets containing Simvastatin-Cyclodextrin Inclusion Complexes

A B S T R A C T Simvastatin is a BCS class II drug, having low aqueous solubility [1.45μg/ml] and therefore low oral bioavailability [5%]. In present study attempt has been made to prepare orodispers in cyclodextrin complexes. For enhancing solubility of drug, inclusion complexes of drug were prepared using hydroxy propyl β-cyclodextrin. The inclusion coplexes prepared by solvent evaporation method exhibited highest enhancement in solubility (520μg/ml) and also showed fastest dissolution profile (99.30% of drug release in 120 min) in comparison of pure drug and other formulations. These copmlexes were characterized by solubility study, differential scanning calorimetry, and X-ray diffractometry. So, this complex was worked further for formulation of simvastatin orodispersible tablets. To aid in faster disintegration of tablets, superdisintegrants in 2 different proportions were used and their effect on 2 2 disintegration was studied. The formulation was optimized using 3 factorial design. In 3 factorial design, amount of superdisintegrant (X1) and amount of effervescing agent (X2) were selected as independent variables. The time of disintegration (Y1) and percentage of friability (Y2) were selected as dependent variables. The data clearly indicated that the disintegration time and percentage friability values strongly depend on the selected independent variables. Hence, use of hydroxyl propyl β-cyclodextrin and addition of superdisitigrants is useful technique in enhancement of dissolution rate of simvastatin. ible tablets of simvastat