Formulation Of Floating Tablets Research Articles

EPLERENONE FLOATING MICROSPHERES: RADIOGRAPHIC AND PHARMACOKINETIC STUDIES IN RABBITS

Objective: The objective of the present investigation was to evaluate gastro-retentive performance and pharmacokinetic parameters of Eplerenone-optimized floating microspheres compared with formulated floating tablets. Methods: Microsphere contains antihypertensive drug Eplerenone as a core material encapsulated with the polymeric membrane for sustained drug release were prepared by solvent diffusion-evaporation technique. The prepared microspheres were evaluated for qualitative and quantitative parameters. The optimized formulation showed favorable in vitro floating and drug release profile. The gamma scintigraphy of the formulation was carried out in rabbit in order to determine the floating ability of the final formulation with barium sulfate. Prolonged gastric residence time of over 12 h was achieved in all the animals. Eplerenone-loaded optimized formulation was orally administered to rabbit and blood samples were used to determine pharmacokinetic parameter by using WinNonlin software 3.0 version. Results: Eplerenone floating microsphere, which are compared with pharmacokinetic parameters of the Floating tablet showed improved parameters of Cmax; similarly, time to reach peak plasma concentration (t-max) for Eplerenone Floating microspheres was 4 times increased against Floating tablet formulation. The area under the curve (AUC) for formulated floating tablet was found to be 9.69 µg/ml, whereas for floating microspheres it was 16.28 µg/ml, for formulated floated tablet absorption rate constant Ka was 1.61 h, elimination rate constant was 0.112 h and elimination half-life 6.2 h. The comparison of these data undoubtedly shows that the Cmax was not much valid, but AUC was increased to about 1.68 times in case of floating microspheres, absorption rate constant was found to be decrease 3.22 times when related to the floating microspheres, whereas Ke was found to be decrease 2.11 times when equated to floating microspheres, elimination half-life was increased by almost about two times. Conclusion: Eplerenone floating microsphere, which are compared with pharmacokinetic parameters of the floating tablets showed enhanced parameters of the formulated due to floating nature of the present designed formulation.

In-vitro Evaluation and Optimization of Sacubitril and Valsartan Floating Tablet using Natural Polymer

Oral systems have become gradually extensive for human consumption because of their numerous advantages, such as formulation efficiency, cost-effectiveness, and patient safety compliance. These systems offer a versatile platform for controlled drug release, allowing precise targeting of absorption site in the gastrointestinal tract. Accomplishing ideal therapeutic results for certain medications often requires precise control of drug release at specific locations within the gastrointestinal tract. In this study, our goal was to create a floating drug delivery system for two vital cardiovascular medications, sacubitril and valsartan. Our specific objectives were to extend floating time, prolong stomach residency, and reduce floating lag time. The strategy involved harnessing the synergistic potential of natural polymers in optimal proportions to enhance drug activity. Following the principles of quality by design (QbD), we systematically explored various formulation factors to optimize the drug delivery system. Analysis of tablet characteristics revealed significant variations in key parameters, such as swelling index, floating lag time (FLT), total floating time (TFT), and drug content for both sacubitril and valsartan. The enhanced formulation (F12) stood out with a remarkable swelling index of 93.4%, a floating lag time of 6.7 seconds, and an impressive total floating time of 12 hours. Furthermore, high drug content percentages were achieved, with sacubitril at 98.70% and valsartan at 94.65%. The successful development and optimization of the floating tablet formulation carry substantial clinical implications. The extended gastric retention, controlled drug release, and high drug content of the optimized formulation suggest enhanced bioavailability and therapeutic efficacy for both sacubitril and valsartan. The prolonged total floating time offers convenience to patients, potentially improving medication adherence in managing cardiovascular diseases. In conclusion, this study highlights the formulation and optimization of floating tablets as a noteworthy advancement in drug delivery technology, promising improved therapeutic outcomes and enhanced patient convenience.

FORMULATION AND EVALUATION OF FLOATING TABLET OF RISEDRONATE

FORMULATION AND EVALUATION OF FLOATING TABLET OF RISEDRONATE

FORMULATION AND EVALUATION OF TINIDAZOLE FLOATING TABLETS

FORMULATION AND EVALUATION OF TINIDAZOLE FLOATING TABLETS

UJI FISIK FORMULASI TABLET FLOATING TEOFILIN DENGAN MATRIK HPMC

The purpose of this study was to determine the physical properties of theophylline floating tablet formulation with HPMC as matrix. Floating tablets of theophylline is manufactured by direct compression. Composition per tablet formulation consisting of theophylline 270 mg, HPMC, avicel, magnesium stearate, and sodium bicarbonate. The results of data showed average of tablet weight uniformity 501mg, tablet hardness 6,99 kg, tablet friability 0,593%, disintegration time of tablets 738 seconds, floating lag time (FLT) 584,3 seconds and floating duration time (FDT) more than 8 hours. Floating tablet formulation of theophylline resulted in a good physical test.

FORMULATION AND EVALUATION OF FLOATING TABLET OF ALFUZOSIN HCL

FORMULATION AND EVALUATION OF FLOATING TABLET OF ALFUZOSIN HCL

Formulation Development and Evaluation of Floating Tablets of Zolmitriptan

Zolmitriptan is the antimigraine agent widely used for the treatment of the migraine. It shows the half-life of 2.5 – 3 h which indicate the frequent dosing to achieve proper pharmacological action of the drug. Gastro Retentive Drug Delivery System (GRDDS) is a common approach to decrease the dosing frequency and increase patient compliance, and delivery of drug through such an approach of floating tablet formulation will meet the requirement. This system showed substantial effect on the drug release through floating and swelling properties. The tablets were formulated by using direct compression technique along with hydrophilic polymers and gas generating system. In the preliminary trials, we observed that the tablets were within pharmacopeial limit. % Drug release of the formulations (F1 – F9) was studied up to 6 h and it was found from 52 to 91 %. The cumulative percentage drug release was inversely proportional to polymer concentrations of HPMC K100 M and PVP K 30. The batches follow Higuchi model of drug release which involves the diffusion mechanism. In-vitro dissolution studies showed good percent drug release, which is in accordance with robinson-errikson equation. Good buoyancy for additional 6 h, trailed by the diffusion.

FORMULATION AND EVALUATION OF FLOATING TABLET OF TELMISARTAN

FORMULATION AND EVALUATION OF FLOATING TABLET OF TELMISARTAN

Formulation and evaluation of floating tablet of levofloxacin

Floating drug delivery system is a system to retained the drug in the stomach which is applicable only for poorly soluble and less stable in intestinal fluids. It is basis on the dense on gastric fluids which is float on gastric fluids. Floating tablet Formulations of levofloxacin were prepared by simple blending and punching with carbopol, HPMC K4M, sodium bicarbonate, citric acid and talk for oral application. Levofloxacin is an antibiotic drug having higher protein binding, hepatic metabolism low oral bioavailability and lower half life. The drug requires a drug delivery system that provides a solution of these problems and improves bioavailability. Prepared floating batches were characterized for compatibility study, pre compression and post compression evaluation, % drug content, in-vitro drug release. Major advantages of the system include ease of preparation, high % drug release and long duration over 12 hours. From this study, it was concluded that floating tablet batch F3 offers better sustained release in continuous manner that helpful to maintain bioavailability for long duration and reduces frequency of dose, also reduces dose.

FORMULATION AND EVALUATION OF FLOATING TABLET OF THIOCOLCHICOSIDE

Thiocolchicoside is a centrally acting analgesic and is used to treat moderate to severe pain. Thiocolchicoside is rapidly and almost completely absorbed after oral administration, showing good bioavailability. Hence the main objective of the work was to design, development and in vitro evaluation of natural gum based matrix tablet of Thiocolchicoside. All the batches were evaluated for angle of repose, carr’s index, hausner’s ratio, hardness, thickness, weight variation, drug content and in vitro release characteristics. The results of DSC and IR spectroscopy exhibited that no chemical interaction between drug and polymers and no shifting in the IR peaks was observed. The release kinetics and the mechanism of drug release by regression coefficient analysis were investigated. The optimized tablets having HPMC provided more sustained drug release than other polymers. The drug release from the tablets was sufficiently sustained and non-Fickian transport of the drug from tablets was confirmed. KEYWORDS: Thiocolchicoside, HPMC K15M, Carbopol 934P, MCC PH102.

FORMULATION AND EVALUATION OF FLOATING TABLETS OF TINIDAZOLE

FORMULATION AND EVALUATION OF FLOATING TABLETS OF TINIDAZOLE

Development and Evaluation of Gastro Retentive Floating Drug Delivery System of Ondansetron Hydrochloride

The Aim of the present study was to develop & evaluate Gastro-retentive floating Tablet of Ondansetron hydrochloride. The Objective was to calibrate and validate the UV- spectroscopy analytical method and to prepare and optimize the GR Floating tablets of Ondansetron hydrochloride in terms of dissolution release profile. The FDDS of the drug can minimize the fluctuation of drug plasma levels and result to associated adverse reactions, dosing frequency, and improved patient compliance. Conventionally, Ondansetron hydrochloride is taken up 2-3 times daily in the treatment of nausea and vomiting. Gastro retentive floating tablet of Ondansetron hydrochloride is better suited for treatment of postoperative nausea vomiting. In the present study, nine Gastro retentive Floating tablet formulations (F1, F2.....F9) of Ondansetron hydrochloride were prepared by the method of direct compression and polymers HPMC K15 were used and Guargum and Chitosan, in different quantity to normalise their effect on the’ release profile of drug . Target release profile was >80% release of drug in 12 hours. Tablets were evaluated for various parameters namely: thickness, weight variation’, friability, hardness, assay, in-vitro buoyancy study & drug release. Formulation F8 containing Chitosan (26.66% w/w), Guargum (26.66% w/w) and Sod. Carbonate (25.83% w/w) had the desirable release profile.
 Keywords: Ondansetron hydrochloride; Gastro retentive floating tablet, Chitosan, Guar gum, Drug release

FORMULATION AND EVALUATION OF FENOVERINE FLOATING TABLETS

Objective: The purpose of this research was to develop a fenoverine gastroretentive drug delivery system which, following oral administration should have the ability to enhance and prolong the period of gastric residence time (GRD) with the desired in vitro release profile.
 Methods: In the present study, fenoverine floating tablets were prepared using an effervescent method using sodium bicarbonate and citric acid as a gas-generating agent. The tablets were formulated using direct compression technology using xanthan gum and sodium alginate as polymers. Pre-compression powders were evaluated for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio, and the prepared tablets were evaluated for weight variation, thickness, diameter, hardness, friability, drug content, floating lag time, total floating time, and in vitro dissolution studies. The formulations were optimized for the different concentrations of xanthan gum, sodium alginate, and their combinations.
 Results: All the prepared formulations showed well in vitro buoyancy. The tablets remained buoyant for 6–12 h. The in vitro drug-release pattern of fenoverine floating tablets was adapted to different kinetic models with the highest regression to zero-order and Korsmeyer-Peppas, and the mechanism was found to be a Fickian mechanism.
 Conclusion: Out of all the formulations prepared, in vitro dissolution studies of the F4 formulation were found to be maximum than other batches, which exhibited desired sustained release time followed by acceptable floating properties.

UJI FISIK FORMULASI TABLET FLOATING TEOFILIN DENGAN MATRIK HPMC

The purpose of this study was to determine the physical properties of theophylline floating tablet formulation with HPMC as matrix. Floating tablets of theophylline is manufactured by direct compression. Composition per tablet formulation consisting of theophylline 270 mg, HPMC, avicel, magnesium stearate, and sodium bicarbonate. The results of data showed average of tablet weight uniformity 501mg, tablet hardness 6,99 kg, tablet friability 0,593%, disintegration time of tablets 738 seconds, floating lag time (FLT) 584,3 seconds and floating duration time (FDT) more than 8 hours. Floating tablet formulation of theophylline resulted in a good physical test.Keyword: floating, theophylline, HPMC, tablet

Design, Formulation and In Vitro Evaluation of Oxybutynin HCl Floating Matrix Tablets

The goal of this study was to prepare and test a hydrodynamically balanced floating matrix controlled Oxybutynin HCl drug delivery system. The muscarinic acetylcholine receptor subtypes M1, M2, and M3 are competitively antagonized by oxybutynin HCl. It is used to treat urinary and bladder problems. It has a 10-12 h elimination half-life. The effervescence produced by the combination of sodium bicarbonate with hydrochloric acid in the stomach causes the Oxybutynin HCl tablets to float in the stomach. Twelve alternative floating tablet formulations were made utilizing direct compression using hydrophilic polymers like HPMC K4M, K15M, and K100M and hydrophobic polymers such ethyl cellulose in various ratios. The produced formulation was characterized using FTIR and DSC analysis. In terms of general appearance, content consistency, hardness, friability, and buoyancy, the examination found that all formulations meet the specifications of official pharmacopoeias and/or standard reference. Formulation F11, which contained 25% HPMC K100M and 12.5% ethyl cellulose, had the best in vitro drug release up to 99% after 12 hours. The formulations with more than 12.5% NaHCO3 had a floating time of more than 12 hours. In vitro drug release kinetics of improved formulation F11 were discovered to be zero order, with anomalous diffusion coupled with erosion being the drug release mechanism. At the conclusion of 90 days, accelerated stability studies revealed negligible change in physicochemical attributes and drug release profiles, indicating that all the formulations were stable.

Improving Bioavailability of Cefpodoxime Proxetil by Increasing Retention Time in Stomach with the Help of Natural Polymer: Formulation and Evaluation

Background: Cefpodoxime proxetil is an orally administered, extendedspectrum, semi-synthetic antibiotic of the cephalosporin class. Cefpodoxime proxetil has a short elimination half-life and also possesses high solubility, chemical, enzymatic stability and absorption profiles in acidic pH which makes Cefpodoxime proxetil suitable candidate for formulating it as a gastro retentive dosage form for improved bioavailability. Methods: The formulation of floating tablets of Cefpodoxime proxetil was prepared by the direct compression technique using Pomegranate peel powder as release retarded material. The floating tablets of Cefpodoxime proxetil are prepared by applying design of experiment in that 32 Factorial Design was selected. In vivo gastro-retention of the optimized floating formulation was determined by X-ray imaging studies on healthy rabbits. Results: The F3 Formulation containing Pomegranate peel powder peel powder of 50mg and sodium bicarbonate 100 mg has shown sustained release for 24 hr. The Floating lag time of all the prepared batches was found to be from 49±0.5 to 57±0.5 in sec. The minimum lag time was 49 sec. The in vitro release data of optimized formulation was treated with mathematical equations and was concluded that drug release followed zero-order kinetics with anomalous transport mechanism. In vivo Gastro retention of the optimized formulation F3 determined by X-ray imaging studies on healthy rabbits shows retention of the tablet in stomach for sufficient period of time. Conclusion: The prepared gastro retentive floating tablet formulation using Pomegranate peel powder as rate control polymer shows betterfloating properties and effective gastro retention when Pomegranate peel powder and drug is used in the ration of 1:2.5. Hence CFP floating tablet formulation can be a suitable alternative to immediate release CFP tablets to increase gastric residence time and thereby improving its bioavailability.

Utilization of biodiesel waste in the development of botanical-based floating tablet formulation against early stages of mosquitoes

The current paper has elaborated the efficient utilization of liquid biodiesel waste in combination with dillapiole and citronella essential oil as active ingredients. Sawdust, cellulose and hydrophobic silica were used as inert ingredients, which make the tablet to float over the water surface. ATR-FTIR analysis of tablet confirmed the compatibility with citronella oil, dillapiole, liquid biodiesel waste in tablet composition after compression. Physico-chemical analysis studies show that tablet parameters are in standard limits. SEM analysis shows some porous structures in tablet composition which confirms the floating nature of the tablets. The specific ratio (2:2:1) of citronella oil, dillapiole and liquid biodiesel waste showed maximum mortality, i.e. 95% after 24 h. After application, the tablet is nontoxic towards the aquatic organisms and water quality remains unaffected. The better performance of the tablets has been evaluated in terms of characterization studies, viz. ATR-FTIR and SEM studies and bioefficacy trials which confirmed the presence of active ingredients responsible for insecticidal activity.

DEVELOPMENT OF COPROCESSED EXCIPIENTS OF XANTHAN GUM AND ACACIA GUM AS A CONTROLLED RELEASE MATRIX FOR FAMOTIDINE FLOATING TABLETS

Objective: Controlled release floating tablets require excipients, which act as a matrix to control the release of the active drug and facilitatethe tablet floating in the gastric milieu. One potential excipient is coprocessed excipients of xanthan gum and acacia gum (Co-XG-GA), which isa physical modification of the two natural polymers. In this study, we produced several Co-XG-GA and used them as matrices in floating tabletformulations.Methods: Several coprocessed excipients were prepared from xanthan gum and acacia gum at ratios of 1:1, 1:2, 2:1, 1:3, and 3:1. The obtainedexcipients were then characterized physically, chemically, and functionally. The coprocessed excipients were then formulated in floating tablets usingfamotidine as the drug model. The floating tablets were then evaluated in terms of the tablet floating capabilities and the drug release in HCl mediumat pH 1.2 for 8 h.Results: Our results showed that the coprocessed excipients were a fine powder, odorless, and a grayish-white color. The excipients had a goodswelling index, fairly large viscosity, and good gel strength; hence, they were suitable to be applied as the matrices of floating tablet formulations. Thefloating tablets of F2, which contained the Co-XG-GA 1:2, demonstrated the best characteristics with 8.33±0.58 min of floating lag time and 24 h oftotal floating time. Further release studies revealed that the famotidine floating tablets, which used Co-XG-GA (F1–F5) as matrices, controlled drugrelease with zero-order release kinetics and could be used for controlled release dosage forms.Conclusion: Collectively, our results indicate that the Co-XG-GA can be applied as matrices in controlled release floating tablets

Optimization of Floating Tablet Containing Glibenclamide Using Simplex Lattice Design

Glibenclamide is a second generation sulfonyl ureas drug that are widely used in diabetes type 2 therapy. Glibenclamide in floating tablet formulations is used to improve the bioavailability. The aim of this study was to determine the optimum composition of floating tablets of glibenclamide by simplex lattice design. The tablets were prepared by wet granulation technique, using HPMC K100LV and Carbopol 940 as polimers. The optimum formula was determined based on numeric method with physical properties, floating characters, and dissolution profile of tablets. the results of the study show that glibenclamide floating tablets have good physicochemical properties. The combination of HPMC K100LV and Carbopol 940 decreases floating lag time and dissolution rate of floating glibenclamide tablets. The optimum composition of glibenclamide floating tablet was HPMC K100LV 44.29 mg and Carbopol 940 15.71 mg with desirability value 0.989.

FORMULATION AND EVALUATION OF FLOATING TABLETS OF CEFUROXIME AXETIL

FORMULATION AND EVALUATION OF FLOATING TABLETS OF CEFUROXIME AXETIL