Percentage Friability Research Articles

Design and Characterization of Mangiferin Sustained-Release Tablets

Background: Mangiferin is a natural bioactive compound used for various pharmacological activities like antidiabetic, anticancer, and anti-inflammatory. Objective: The development of unique sustained-release matrix tablets of mangiferin is the purpose of the work that is being presented here. Method: In this study, an effort is made to formulate mangiferin sustained-release matrix tablets by combining the sustained-release polymers HPMC K100M, Kollidone@SR, Keltone LVCR. Mangiferin matrix tablets have been synthesized by wet granulation utilizing the lactose works as the diluent. Systems were developed with different polymer percentages. Results: Refine the design based on observed differences in weight, hardness, thickness, percent friability, percent drug content, and in-vitro drug release. In-vitro release trials conducted by utilizing a USP type II device utilizing a 6.8 pH phosphate buffer as the separation medium revealed that the most successful F2 formulation, which included 20% polymer, was capable of supporting the mangiferin release for a time of 12 hours period. This sample showed the greatest coefficient (R) value in the Hixson-Crowell model, and release kinetics studies showed that this sample exhibited an erosion process and followed zero-order kinetics. Conclusion: We can conclude that Kollidone@Sr can be used to prepare sustained-release mangiferin.

Evaluation of Orally Disintegrating Tablet Formulations in The Treatment of Oral Mucositis

Aim: Orally disintegrating tablets (ODT) are widely used dosage forms with high patient compliance, which preferred in the treatment of many diseases currently. In this study we aimed to develop an orally disintegrating tablet formulation can be preferred in the treatment of oral mucositis, which often occurs after chemotherapy during cancer treatment.
 Methods: Lidocaine hydrochloride, which is a local anesthetic substance, was used as active pharmaceutical ingredient to obtain ODT formulation for the treatment of oral mucositis. ODTs were prepared by direct compression technique and crospovidone was used as super-dispersant
 Results: The method developed for lidocaine determination was validated. Characterization of powder mixtures conducted; angle repose was found to be as 25.78°±0.810, flow time was 4.18±0.772 s, compressibility index was 9.591±0.774% and Hausner’s ratio was calculated as 1.106±0.014. The uniformity of weight and content for the ODT formulation was 493.705±3.583 g, 78.89+2.546 mg, respectively. The tablets had a diameter of 12.031 ±0.015 mm while thickness was 4.420 ±0.021 mm. The hardness was calulated as 28.7±1.123 N, while percent friability value was 0.76%. Disintegration time of the tablets were 31.55±0.354 sec., and approximately 90% of the prepared formulation dissolved in around 20 minutes according to dissolution testing.
 Conclusions: The prepared formulation was evaluated through powder and tablet controls, it was found to comply with the limits specified in the European Pharmacopoeia. The developed ODT formulation for the treatment of oral mucositis, is planned to be evaluated through in vivo tests to complete the assessment of the formulation.

OPTIMIZATION AND CHARACTERIZATION OF MELOXICAM ORODISPERSIBLE TABLETS USING MIXED HYDROTROPY FOR ENHANCED WATER SOLUBILITY

Introduction: In order to attain rapid discharge in saliva and enhanced absorption, drug was incorporated in a fast-dissolving dosage form (ODTs) as a solid dispersion. In this present work ODTs of Meloxicam were prepared by sublimation techniques where different subliming agents were used with super disintegrant. Materials and Methods: Hydrotropic solid dispersions were prepared using different ratios (1:2, 1:4 and 1:6) of drug and hydrotropic blends (Niacinamide, Anhy. Sodium citrate, Sodium Salicylate and Sodium benzoate). Best hydrotropic solid dispersion was selected to prepare ODTs comprising of croscarmellose sodium and camphor in different concentration along with other pharmaceutical excipients. From the primary trial batches, T3 was selected for optimization experimental designs due to lowest disintegration time and highest in vitro drug release. Secondary batches (F1-F9) were prepared by using 32 full factorial design with different concentration of croscarmellose sodium (12, 14 and 16 mg) and camphor (8, 10 and 12 mg) as two independent variables while disintegration time and percent friability were considered as two dependent response variables. These formulations were subjected to study of various post compression evaluation parameters like hardness, thickness, friability, weight variation, disintegration time (25-117 sec) and in-vitro drug release (99.09%).
 Result and Discussion: Equilibrium solubility studies were reported that by utilizing hydrotropy, the solubility of Meloxicam got enhanced from 20.5 to 140.96 times as compared to its aqueous solubility. The desirability fraction was used to optimize the response variables for specific targets, i.e., minimum disintegration time and maximum dissolution, and the responses obtained were consistent for experimental values.

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLET OF LEVOCETIRIZINE DIHYDROCHLORIDE AND MONTELUKAST SODIUM

Introduction: Fast disintegrating tablets (FDTs) have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Objective: The aim of the present study was to formulate fast-dissolving tablets of Levocetirizine dihydrochloride (LEV) and Montelukastsodium (MON) by direct compression method. Material And Methods: An attempt was made to mask the bitter taste of Levocetirizine by preparing an ion exchange resin complex by a batch method using Kyron T-104. The tablets were prepared using mannitol, microcrystalline cellulose as diluents, and croscarmellose sodium and crospovidone as super disintegrants. Parameters like a drug: resin ratio, pH & swelling time were successfully optimized to prepare the drug resin complex. The fast-dissolving tablets were characterized for various pre and post-compression parameters along with disintegration time, content uniformity, wetting time, in-vitro drug release, in vivo taste evaluation, and compatibility studies. Result and Discussion: The tablets prepared by direct compression method possess a hardness of 3.4 to 3.6 Kg/cm², percentage friability of 0.65 to 0.80, in vitro disintegration time of 29.82 to 51.7 seconds, and wetting time of 20.4 to 46.8 seconds. The formulation (F4)containing crospovidone and croscarmellose sodium in 2:4 ratios showed better disintegration time and more than 99% drug release within 6 minutes. Comparative taste evaluation proves the palatability of formulated tablets. Results of stability studies were also found in acceptable limits. Conclusion: The prepared orodispersible tablets disintegrate within seconds without the need for water and enhance absorption; thismay lead to increased bioavailability of LEV as well as MON.

Formulation and Evaluation of Controlled Release Theophylline Tablets using Grewia spp Gum as Binder

The major reason for development of new drug delivery system is based largely on promoting therapeutic outcome and minimizing toxic effect of a drug by increasing the amount and persistence of a drug in target cells areas, while reducing exposure of the drug to non-target cells. In this study, Grewia spp gum obtained from Grewia spp pods was extracted and used as binder and release retardant in the formulation of controlled release theophylline tablets. A total of six (6) batches of the tablets were produced with carried concentrations of the test gum by wet granulation technique. To produce the tablets, various granules were formulated via wet granulation and characterized by measuring flow and packing properties. Granules with adequate flow properties were compressed to tablets. Tablets so formed were evaluated for hardness, percentage friability, weight variability and drug release profiles. The percentage yield was 18.64% and the pH of the test gum was 6.15. The angle of repose, bulk density, tapped density and Carr’s index of the formulated granules ranged from 22.48±0.00 to 24.90±0.00˚, 0.53±0.03 to 0.67±0.00g/ml, 0.67±0.02 to 0.82±0.00g/ml and 18.29±0.00 to 22.06±0.26% respectively. Resultant tablets hardness values of 3.69±0.45 to 13.39±0.65kgF and friability percentage of 0.40± 0.00 to 2.56%±0.01% were also obtained. The formulated theophylline granules showed good flow properties and compressibility. Thus, the study revealed that the test gum has comparable binding effect to Eudragit RS 100 at a ratio of 2:1. We recommend further studies to rule out any interaction of Grewia spp gum with theophylline in controlled release theophylline tablets.

Quality Assessment of Ascorbic Acid Tablet Formulations and Comparative Analysis with Edible Fruits

Background: Ascorbic acid is a vitamin, soluble in water and essential for human health. It plays vital role in collagen production, iron absorption, wound healing, osteogenesis, and scurvy treatment. Objective: The study aimed to evaluate the physicochemical features of ascorbic acid oral tablet formulations and compare the amount found in natural sources to that found in commercial brands. Method: The study used six brands of ascorbic acid tablets. The drugs were analyzed using the iodometric titration employing the oxidation-reduction reaction of ascorbic acid and iodine as well as assessing uniformity of weight, hardness, dissolution, friability and disintegration. Results: The fruits were obtained from the fruit market. All the brands of Vitamin C tablets used were within their shelf-lives, standard British pharmacopeia range. Brand E had the highest weight (910.26 mg) and more variation (<2.98 ± 4.23), brand C had the highest percentage friability (0.924%), while D showed lower degree of hardness (0.065%) compared to other brands. Brand D had the highest percentage of drug release (102.973%). Brand F disintegrated at about 21:06 minutes. From the ten samples purchased, none had 100% ascorbic acid though brand B had almost 100% (99.5 mg). Brand E had the least concentration (89.5 mg). Conclusion: The results shows that all the tablets had appreciable percent of ascorbic acid. Strawberries had higher percentage of ascorbic acid among the fruits, followed by orange, papaya, pineapple, mango, kiwi and lemon, respectively.

Comparative Analysis of In vitro Quality Parameters of Different Brands of Marketed Ciprofloxacin Tablets Available in Bangladesh

Aim: Ciprofloxacin is a broad‑spectrum antibiotic under the group of drugs called fluoroquinolones. It is extensively being manufactured and marketed drug by many national and multinational pharmaceutical companies. The purpose of this study was to compare the quality of different brands of ciprofloxacin 500mg tablets available in Bangladesh using quality characteristics such as weight variation, hardness, thickness, friability, disintegration time, and dissolution profile.
 Methodology: The tablets' overall quality criteria, such as weight variation, hardness, thickness, diameter, friability, disintegration time, and dissolving profile, were evaluated using established protocols. An electric analytical balance was employed to measure weight variation. An automated hardness tester was used to determine the hardness, thickness, and diameter. A friabilator was used to determine the degree of friability. A disintegration equipment and a dissolution tester were used to examine the disintegration time and dissolution profile, respectively.
 Results: In this study, all the values were compared with the standards. All brands had been passed for the weight variation test, because no tablets surpass the ± 5 % weight variation. The weight variation range was from 714.57±4.08 mg (brand C) to 837.92±7.49 mg (brand E). In hardness testing procedure, all brands of ciprofloxacin 500mg tablets were within the specified limit. The average hardness of the items ranges from 11.11±1.44 kgF to 19.26±2.20 kgF respectively. The five brand's percentage friability was less than 1%, indicating that they met the requirements. The lowest friability (0.015 %) was found in Brand E, while the highest friability (0.032 %) was found in Brand B. Within 10 minutes, the entire trademark had disintegrated, indicating that they had met the requirements. Brand E had the quickest disintegration time (5.35±0.49 minutes), while brand B had the slowest (9.12±0.88 minutes).All brands had a dissolution rate of 83.56% for A, 95.84% for B, 91.15% for C, 84.46% for D and 88.97% for E, all those were within 60 minutes in dissolution testing. The five brands' assay was within the specified limit, indicating that they met the requirements
 Conclusion: In conclusion, the present study of evaluating quality control parameters revealed that all of the leading brands of this tablet comply the quality control parameters as per pharmacopoeial specifications. Further work is recommended on bioequivalence of these tablets.

Design of Experiment Approach to Assess the Effect of Formulation Variables on Extrusion and Spheronization of Telmisartan and Cilostazol Loaded Pellets and its Pharmacokinetic Study

Background: Solubility is an important parameter that affects the availability of drug in systemic circulation. Drugs having poor solubility belonging to BCS class II eventually result in lower dissolution and bioavailability. Hence, improvement of solubility is a challenging task. Hence the present work focuses on using solid dispersion and inclusion complex approach for both telmisartan and cilostazol belonging to BCS Class II drugs. Objective: The present study was carried out to improve apparent solubility of telmisartan and cilostazol (BCS-Class II drugs) and optimization as pellets along with its pharmacokinetic study. Methods: Phase solubility study was carried out to screen the excipients such as, PVPK30, PVA, HPMC E5 and β-CD. Solvent evaporation method was adopted to prepare the solid dispersions and inclusion complex of both drugs. Pellets were optimized by extrusion spheronization method using 32 factorial design and characterized by morphology, drug content, DSC, FTIR, XRD, SEM, in- -vitro studies and drug content study. Results: Phase solubility study showed improved apparent solubility of telmisartan with HPMC E5 (1:3) by solid dispersion and cilostazol with β-CD (1:3) using inclusion complexation method. Drug characterization did not reveal any incompatibility. Formulation was optimized on the basis of acceptable pellet properties, including acceptable spherical shape and micromeritics properties. The percent friability of all batches was found to be less than 1%. The optimized pellets of both drugs prepared with micro crystalline cellulose provided desirable maximum release with acceptable release profile. Conclusion: The formulated pellets when studied in vivo showed superior pharmacokinetic profile. The drawback associated with apparent solubility and bioavailability of both drugs can thus be alleviated by use of novel pellet formulation.

Formulation and Optimization of Immediate Release Cajanus Cajan Starch-Based Tablets Containing Metronidazole

Starch is found almost in all organs of plants as a carbohydrate reserve. It is considered one of the most commonly used pharmaceutical additives, mainly in tablet dosage forms; it used as a tablet binder when incorporated through the wet granulation process or as a disintegrant. Cajanus cajan has a high level of carbohydrate, which makes it another potential choice as a source for starch. This study aims to investigate and optimize the effect of Cajanus cajan starch concentrations as well as wet massing granulation time on physicochemical properties of metronidazole tablets. The hardness, friability percentage, and disintegration time of prepared tablets were determined, and the central composite design was employed in the optimization process. Then the tablets of optimized batch were compared against those tablets in which maize starch and sodium starch glycolate were used instead of Cajanus cajan starch. The results indicated that metronidazole tablets containing the upper level of starch paste (Cajanus cajan and/or maize starch paste) exhibited better percentage friability, hardness, and disintegration time than those formulated with lower levels and those without starch paste. The study showed that experimental design is a useful technique for optimizing Cajanus cajan starch-based tablets, which enabled a better understanding of how different variables could affect the responses. In addition, the study demonstrated that incorporation of Cajanus cajan starch in tablets formulation led to improvement of its physical properties compared to the formulations of maize starch and sodium starch glycolate respectively.

A Controlled Release Theophylline Delivery System Based on a Bilayer Floating System.

Bilayer floating drug delivery is an approach that helps to overcome the shortcomings of single-layered tablets. There is little or no fluctuation of the drug in the blood stream or tissue, while control is enabled over the time and site of drug release. In the current study, bilayer theophylline matrix tablets were formulated by double compression and evaluated using granules produced by polymeric granulation and simple coacervation techniques. Bilayer floating theophylline tablets containing an immediate release layer (IRL) and a sustained release layer (SRL) were prepared. Granules for the IRL section were produced by wet granulation, while those for the SRL section were produced by polymeric granulation and simple coacervation techniques using Eudragit RL100 and carboxymethyl cellulose (CMC) as binder. The resulting granules were characterized for flowability and packing properties. Granules with adequate flow were compressed into flat-faced tablets 12 mm in diameter using a single punch tableting machine at an arbitrary load of 28 kgF on a load scale. The tablets were evaluated for hardness, weight variability, disintegration, friability, swelling index, floating time, and in vitro drug release. The angle of repose and Hausner ratio were 29.07±0.330 to 40.08±0.660 and 1.07±0.01 to 1.28±0.01, respectively. Tablets hardness values ranged from 4.74±0.36 to 9.84±0.49 kgF, while percentage friability ranged from 0.5% to 1.51%. Floating lag time was between 1±0.41 and 9±0.71 min, while the total floating time was between 1 min and 9 h. Over 50% of the drug was released within 7 h. Drug release from the tablets showed a prompt release phase and an extended release phase. Therefore, appropriate combination of Eudragit and CMC and the right reagent can produce well retarded bilayer floating tablets.

In-vitro Comparative Study of Different Brands of Metoclopramide Hydrochloride Tablets Marketed in Saudi Arabia

Background: Metoclopramide hydrochloride (MCP), a derivative of para-aminobenzoic acid, which is a freely soluble drug, gets rapidly absorbed from the gastrointestinal tract and is used in the management of gastrointestinal disorders such as gastric stasis, gastroesophageal reflux and for the prevention of cancer chemotherapy induced emesis. Several brands of MCP are available in Saudi Arabia. Objectives: The objective of the present study was to evaluate the quality of different marketed products of MCP tablets 10mg, which were purchased from the retail pharmacy outlets in Abha, Riyadh and Jeddah, Saudi Arabia with a view to determine their interchangeability in clinical practice. Methods: The study was carried out on branded tablets by quality control tests such as weight variation, hardness, friability, disintegration and dissolution. The results of all marketed products complied with the official specifications. Results: The results showed that all the parameters for MCP tablets were in accordance with the USP limits. All the tested four brands were bioequivalent and complying with the official tests for weight variation, friability, disintegration and dissolution tests. The percent friability was also within the specified limit. Moreover, all formulations disintegrated within 2-6 min. The percentage content of the active ingredient of four brands of MCP tablets showed values within the monograph specifications (95-105%). Conclusion: All the four brands evaluated in the present work could be considered bio pharmaceutically equivalent and therefore, patients can safely switch from one brand to another when there is the unavailability of a particular brand.

FORMULATION DESIGN AND OPTIMIZATION OF FAST DISINTEGRATING TABLETS OF VALSARTAN: EFFECT OF SUPERDISINTEGRANTS

Oral disintegrating tablets are a novel attractive dosage form in which the tablet disintegrates or dissolves in the buccal cavity within seconds without the use of water. The major drawback in designing this dosage form is unpleasant taste and low solubility of active entity. Valsartan is an antihypertension drug used in treatment of high blood pressure, congestive heart failure (CHF) and post-myocardial infarction (MI). It is characterized by its bitter taste, which effects the patient’s compliance. Despite this, it belong to the BCS II Classification in which drugs have low solubility and high permeability. The aim of the present research work was to formulate orally disintegrating tablets of valsartan using natural and synthetic superdisintegrants. The drug was characterized according to different compendia methods, on the basis of identification by UV spectroscopy, pH, organoleptic properties and other tests. Drugpolymer compatibility was carried out by FTIR. The values of pre-compression parameters assessed were within specified limits and showed good free flowing properties. The data on post-compression parameters such as weight variation, hardness, friability, wetting time, water absorption ratio, content uniformity, disintegration time and dissolution was found to be within the prescribed limits. Batch F9 with disintegration time 24 sec was selected as the optimized formulation. Batch F9 was also subjected to stability studies for three months and was tested for its appearance, average weight, hardness, disintegration time, percent friability and its release rate, which were in prescribed ranges and satisfactory.

Preparation of mucoahesive tablets of famotidine by wet granulation method and its in-vitro testing

Objective: Famotidine is a histamin H2-receptor antagonist.The aim and objective of the present work is toformulate and evaluate mucoadhesive tablets of famotidine. It is also foused on the selection of mucoadhesivepolymer & its activity in various combinations & ratios. The poor bioavialability & shorter half-life suffice thedevelopment of controlled release mucoadhesive formulation. Method: Mucoadhesive tablets each containing 20mg of famotidine were prepared by conventional wet granulation method employing as mucoadhesive materials. A batch of 50 tablets was prepared, in each case a blend of 1 gm of famotidine with different polymers addition indifferent strengths with required 40mg lactose as diluent achieved after titration which were then grannulated along with a solvent blend if water and ethyl alcohol. Results: The flow properties of all five batches were in between fair and passable. Hardness of tablets ranged from 6.9-8.2 kg/cm2 and the percentage friability was between 0.25-0.79 %. The drug content uniformity in the mucoadhesive tablets was 96.49-104.81%. The surface pH study was within the range from 6.7-7.4. From all formulations, over 20% of the famotidine was release within first hour of dissolution study. In the present study the formulation FT04 (tragacanth & HPMC ) has shown cumulative percent drug release of about 80.762% in 12 h. Conclusion: From the results we concluded that formulation containing famotidine with HPMC & tragacanth has given better drug release property than the other four formulations & the wash-off test has shown that this formulation (FT04) has better mucoadhesive property.

Formulation and Evaluation of Colon Targeted Enteric Coated Tablets of Loperamide

In this study the formulation of safe and effective enteric coated matrix tablet of Loperamide was prepared for the effectual treatment of inflammatory bowel diseases. Direct compression method is used for the formulation of colon targeted matrix tablet of Loperamide. Eudragit FS 30 D polymer and Triethyl citrate this coating material is used for this tablet. This coated tablet evaluated for properties such as average weight, hardness and coat thickness. The In vitro release studies of prepared tablets was carried out for 100 rpm for first 2 hrs. Then replaced with 7.4 pH phosphate buffer and continued for 24 hrs. According to United States Pharmacopoeia (USP) limits, the percentage weight variation, percent friability and content of drug molecule for all the formulations are in the range of USP limits. From the results obtained, Loperamide would be a hopeful formulation to achieve the aim which cure inflammatory bowel diseases without any gastric irritation, which is helpful for patients having pre-history of ulcerative colitis.

FORMULATION AND EVALUATION OF EXTENDED RELEASE PELLETS OF PIOGLITAZONE HYDROCHLORIDE USING NATURAL AND SYNTHETIC POLYMERS BY FLUIDIZED BED COATING TECHNIQUE

Objective: The objective of the current work was to develop Pioglitazone hydrochloride (HCl) pellets coated with natural polymer extracted from peas gum and also to compare the drug release profile with coatings containing semi-synthetic and synthetic polymers.
 Methods: Fluidized bed coating technique was used to develop pellets. A 22 factorial design was employed to study the effect of independent variables (inlet air temperature and spray rate), on dependent variables (percentage entrapment efficiency, percentage friability, and average particle size). Optimization was done by fitting experimental data to the software program. Obtained pellets were subjected to different evaluation parameters which are critical in the development of the dosage form. An in vitro lag phase study was carried out for all batches in simulated gastric fluid (0.1N HCl) for 5 h and in vitro drug release study was carried out for optimized batch (E-2 and P-3) in simulated intestinal fluid (pH 7.4 phosphate buffer).
 Results: The optimized batches E-2 and P-3 showed satisfactory percentage entrapment efficiency of 92.66±1.52, percentage friability of 0.57±0.03, and average particle size of 1424±16 μm. All batches maintained lag phase for 5 h in 0.1N HCl. An optimized batch of two different sizes exhibited a burst release within 30 min in a simulated intestinal fluid with no significant difference in release rate constant (*p>0.05) and followed first-order kinetics.
 Conclusion: Thus, Pioglitazone HCl pulsatile pellets were successfully developed for treating diabetes mellitus by fluidized bed coating technique employing factorial design.

FORMULATION DESIGN AND OPTIMIZATION OF FLOATING MATRIX TABLETS OF CIPROFLOXACIN HCL BY USING HPMC AND ETHYL CELLULOSE WITH EXPERIMENTAL DESIGN

The oral floating matrix tablets of Ciprofloxacin Hydrochloride were formulated by Experimental design by using HPMC K100M and Ethyl Cellulose as the retardant polymers each with three different levels with an approach to increase gastric residence and thereby improve drug bioavailability. From FTIR results it was confirmed that there is no chemical interaction between the drug with the excipients used in tablet formulations. Also, there was no shift in the endotherm of in the drug- excipients mixtures indicating compatibility of drug with all the excipients. All the tablets were prepared by effervescent approach in which Sodium bicarbonate was added as a gas generating agent. Floating Matrix tablets were prepared by direct compression method and prepared tablets were evaluated for weight variation, percentage friability, hardness and drug content studies. All the formulations showed compliance with pharmacopeia standards (I.P. 1996). Floating lag times of all the formulations were within 1 minute and Total floating time of all the formulations were more than 12 hours. In vitro release studies revealed that the release rate decreased with increase polymer proportion of retarding polymers. The formulation CHE9 sustained release of drug for 12 hours with 21% release of drug after 1 hour and more than 97% at the end of 12 hours. From the Kinetic model it was found that the optimized formulation CHE9 showed linearity in case of Zero order (R2: 0.938) and Higuchi model (R2: 0.954). By fitting data to Korsmeyer-Peppas model and ‘n’ value lying above 0.5 indicating non Fickian release.

Formulation Development and Evaluation of Direct compressed Cefpodoxime proxetil Effervescent Tablets

Cefpodoxime proxetil is an orally administered, extended spectrum, semi-synthetic antibiotic of the cephalosporin class. It belongs to BCS class IV drugs and has a limited aqueous solubility of 0.4 mg/ml. Hence the present aim of the study is to enhance the solubility of Cefpodoxime proxetil through complexation with HP-s-cyclodextrin. Binary mixture of sodium bicarbonate and citric acid to be used as effervescent materials. The disintegration to be further enhanced using superdisintegrants such as croscarmellose sodium, sodium starchglycolate and polacrilin K. Seven such formulations were prepared with varying composition and proportion of superdisintegrants. All formulations indicated a fair weight variation with in the pharmacopoeial limit. The result varies from ±1.23% to ±3.58% against ±5%. Thickness range was determined between 4mm - 4.2mm. Hardness test result revealed a good strength of more than 4.5 kg/cm2 in every tablet. The percent friability was found within the specification. All formulation took fair time for completion of effervescence except F1 that don’t contain any superdisintegrant. Drug content of all formulations were found to be excellent with more than 98%. Formulation F7 showed excellent effervescent time as compare to other formulation. It showed a consistent drug release with more than 80 % drug released in just 30 minutes. In the FTIR spectra, presence of all significant peaks of drug and absence of any new peak in the formulations revealed that there was no interaction of drug with the excipients. Hence the present study could be an excellent approach to the delivery of the poorly soluble Cefpodoxime proxetil as effervescent tablet.

FORMULATION DESIGN AND OPTIMIZATION OF ORAL FLOATING MATRIX TABLETS OF CIPROFLOXACIN HCL BY USING HPMC AND XANTHAN GUM WITH EXPERIMENTAL DESIGN

The oral floating matrix tablets of Ciprofloxacin Hydrochloride were formulated by Experimental design by using HPMC K100M and Xanthan gum as the retardant polymers each with three different levels with an approach to increase gastric residence and thereby improve drug bioavailability. From FTIR results confirm the absence of chemical interaction between the drug with the excipients used in tablet formulations. Also, there was no shift in the endotherm of in the drug- excipients mixtures indicating compatibility of drug with all the excipients. All the tablets were prepared by effervescent approach in which Sodium bicarbonate was added as a gas generating agent. Floating Matrix tablets were prepared by direct compression method and prepared tablets were evaluated for weight variation, percentage friability, hardness and drug content studies. All the formulations showed compliance with pharmacopeia standards. Floating lag times of all the formulations were within 1 minute and Total floating time of all the formulations were more than 12 hours. In vitro release studies revealed that the release rate decreased with increase polymer proportion of retarding polymers. The formulation CHX8 sustained release of drug for 12 hrs with 20% release of drug after 1hr and more than 97% at the end of 12 hrs. From the Kinetic model it was found that the optimized formulation CHX8 showed linearity in case of Zero order (R2: 0.952) and Higuchi model (R2: 0.948). By fitting data to Korsmeyer-Peppas model and ‘n’ value lying above 0.5 indicating non Fickian release.

FORMULATION AND EVALUATION OF COLON TARGETED MATRIX TABLET USING NATURAL TREE GUMS

Objective: To develop a novel colon targeted tablet formulation using natural polysaccharides such as kondagogu gum and ghatti gum as carriers and diltiazem hydrochloride as a model drug.Methods: The polymer-drug tablets were prepared by wet granulation technique, coated with two layers viz., inulin as an inner coat followed by shellac as outer coat and evaluated for properties such as average weight, hardness and coat thickness. In vitro release studies of prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid (SCF) in order to mimic the conditions from mouth to colon.Results: Percentage weight variation, percent friability and content of active ingredient for all the formulations were found to be well within United States Pharmacopoeia (USP) limits. Out of both the polymers, the tablets prepared with ghatti gum showed the maximum hardness of 7.1 kg/cm2. The FTIR spectra of pure diltiazem HCl and the formulation KF3 were found to be identical. From the DSC, it was evident that the melting point peak of diltiazem HCl and formulation KF3 were observed at 217.16 and 218.34 °C respectively. In vitro studies revealed that the tablets coated with shellac (2.5% w/w), prevented the drug release in stomach environment and inulin coated tablets (4% w/w) have limited the drug release in the small intestinal environment. The data obtained from in vitro drug release studies were fit into Peppas model and in all the cases the value of A was found to be more than 2, i.e., drug release by a combination of both diffusion and erosion-controlled drug release.Conclusion: The study revealed that polysaccharides as carriers and inulin and shellac as a coating material can be used effectively for colon targeting of drugs for treating local as well as systemic disorders.

FORMULATION AND CHARACTERIZATION OF MATRIX TABLETS USING MUCILAGE OF TINOSPORA CORDIFOLIA AS NATURAL BINDER

Objective: The present research work was to formulate matrix tablets of diclofenac sodium using mucilage extracted from Tinospora cordifolia as a novel binding agent. Also, a comparative study on binding properties of mucilage and carbopol were performed.Methods: Fresh stems of Tinospora cordifolia were collected and mucilage was extracted out using standard method. The isolated mucilage was characterised for physicochemical parameters. Formulation of diclofenac sodium tablets (f1-f6) was done by dry granulation method using 2%, 4%, 6%, 8% and 10% concentration of mucilage of Tinospora cardifolia as natural binder. Carbopol 2% was used as synthetic matrix forming agent. Microcrystalline cellulose was used as diluents, magnesium stearate and talc as lubricant. The formulated tablets were evaluated for parameters such as tablet thickness, hardness, weight variation, disintegration time, percent friability and in vitro drug release characteristics. The drug release mechanism was determined by fitting the release data into different kinetics models.Results: The results revealed that all the pre and post compression parameters of the formulated tablets (f1-f6) were in compliance with pharmacopoeial limits. In vitro drug release studies showed that formulation f6 containing maximum concentration of mucilage release the drug in a most controlled and sustained manner with maximum drug release of 63.6% in 15 h in comparison with f1(2% carbopol) giving 80% release and was found to be stable for 3 mo as indicated by stability studies. The mechanism of drug releases from formulation f1-f6 was found to be polymer disentanglement and erosion. Preformulation studies using FTIR study reveals that there is no incompatibility between the pure drug and mucilage of tinospora cardifolia used.Conclusion: Based on the experimental findings it can be concluded that Tinospora cordifolia mucilage can be used as a release retardant agent in the formulation of sustained release dosage forms.