Development and characterization of effervescent floating tablet of famotidine for treatment of peptic ulcer

Floating drug delivery systems (FDDS) are utilized to target drug discharge in the stomach or to the upper parts of intestine. Famotidine has been the most extensively used drug for the management of peptic ulcer for various decades. The current study concerns the development and evaluation of floating tablets of famotidine which, after oral administration, are planned to extend the gastric residence time, enhance drug bioavailability and aim the gastric ulcer. A FDDS was expanded using gas-forming agents, like sodium bicarbonate, citric acid and hydrocolloids, like hydroxypropyl methylcellulose (HPMC) and carbopol 934P. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics, buoyancy, buoyancy lag-time, in vitro release, and swelling index. The formulations were optimized for the different viscosity grades of HPMC, carbopol 934P and its concentrations and combinations. The consequences of the in vitro release studies demonstrated that the optimized formulation (F6) could sustain drug release (98%) for 24 h and remain buoyant for 24 hr. Optimized formulation (F6) showed no considerable change in physical appearance, drug content, total buoyancy time or in vitro dissolution study after storage at 40°C/75% RH for 3 months. Lastly the tablet formulations establish to be economical and may conquer the draw backs associated with the drug during its absorption. Keywords: Famotidine, Floating drug delivery system, Hydrocolloids, Gastric residence time.

Synthesis and Characterization of calcium Starch: A New Controlled Release Polymer for floating tablets of Losartan Potassium

Losartan potassium is used to treat high blood pressure (hypertension). The present study was aimed to prepare a floating drug delivery system to design a controlled release oral dosage form of Losartan potassium. This helps to overcome the demerit of limited residence time of the drug in the gastrointestinal track and hence to increase the duration of release. Hence objective of the present study is to develop Losartan potassium floating tablets by direct compression method using calcium starch as release retarding polymer. The calcium starch was synthesized by gelatinizing potato starch in the presence of sodium hydroxide and cross linking by treatment with calcium chloride. The micromeritic properties studies indicated that calcium starch is a promising pharmaceutical excipient in tablets. Floating tablets of Losartan potassium was formulated by direct compression technique, using different concentration of calcium starch and compared with HPMC K-100 as release retard polymer. As the amount of calcium starch in the tablet increased, the drug release decreased. The formulation F5 containing 125 mg calcium starch showed better controlled release of 76.38% after 12 hours.

Floating Drug Delivery System: An Overview

In recent years scientific and technological advancements have been made in the research and development of rate-controlled oral drug delivery systems by overcoming physiological adversities, such as short gastric residence times (GRT) and unpredictable gastric emptying times (GET). Several approaches are currently utilized in the prolongation of the GRT, including floating drug delivery systems (FDDS), also known as hydrodynamically balanced systems (HBS), swelling and expanding systems, polymeric bioadhesive systems, modified-shape systems, high-density systems, and other delayed gastric emptying devices. The different strategies used in the development of FDDS by constructing the effervescent and noneffervescent type of floating tablets basis of which is buoyancy mechanism. FDDS is a method to deliver the drugs that are active locally with a narrow absorption window in the upper gastrointestinal tract, unstable in the lower intestinal environment, and possess low solubility with higher pH values. The recent developments in floating drug delivery systems are containing the physiological and formulation variables impacting on gastric retention time, approaches to formulating of single-unit and multiple-unit floating systems, and their classification and formulation aspects are discussed in detail. This review also summarizes evaluation parameters and application of floating drug delivery systems.

Floating Drug Delivery System an Aid to Enhance Dissolution Profile of Gastric

With the GRDDS, the dose shape remains controllably in the stomach after oral administration, so that the medication may be continually delivered to its absorption receptors in the intestinal tract. The medicine is delivering in a controlled and extended way. Gastro-retentive dose in the stomach area may last for another few hours and substantially lengthen the gastric residence period of the medicines. While the bulk density in the system for the supply of floating medicines (FDDS) exceeds the gastric fluids, it remains for an extended duration in the stomach without altering the rate of decomposition. The medication distributes gradually as the system floats on the stomach juice. As a consequence, stomach residency takes longer and plasma concentrations are well monitored. The therapy of peptic ulcer illness might be beneficial for local activity in the upper portion of the intestine, i.e., a longer stomach residency. In addition, medicines rapidly absorbed in the GI tract will increase bioavailability through delayed stomach release. The regulated gastric retention of solid dose forms can also be accomplished by the simultaneous administration of pharmacological agents, or by sedimentation, flotation processes, muco-adhesion, expansion, changed shape systems, by delaying the stomach emptying. Keywords: Gastro-retentive drug delivery system, Floating drug delivery system, Muco-adhesion, Bioavailability.

NOVEL FLOATING AGENT SACCHAROMYCES BOULARDII FORMULATION BASED FLOATING DRUG DELIVERY SYSTEM

Objective: The objective is to design and optimize a floating tablet of furosemide using a novel floating agent Saccharomyces boulardii. Methods: In this study floating tablet based on principle of combination of floating and swelling prepared by direct compression technique. Saccharomyces boulardii probiotics preparation is used as a floating agent due to its bloating property i.e. production of CO2 gas and hydrophilic polymer HPMC E LV 15 used as swellable polymer. Furosemide is a BCS class IV drug selected as model drug which shows pH dependent solubility and permeability and it is better absorbed from the gastric region, hence to improve dissolution and residence at absorption site of such drug, floating drug delivery system is needed. Calcium hydroxide used as pH modifier which increase rate of dissolution of furosemide and also maintain integrity of tablet matrix. Formulation designed and developed using central composite design response surface methodology technique, so as to explore the effect of formulation variables such as amount of Saccharomyces boulardii preparation and calcium hydroxide on floating lag time and % drug release after 12h. Results: The numerical and graphical optimization technique were used to choose the optimal formulation. Floating lag time was found to be 12.6 min and 88.18% drug release for the optimized formulation. In vivo buoyancy studies depicted that formulation stay more then 6h in stomach. Conclusion: Study indicate that Saccharomyces boulardii is a promising floating agent, and the formulation containing this novel floating agent is suitable for gastro retention and it increases bioavailability of furosemide.

Evaluation of Metformin Hydrochloride Floating Drug Delivery System: In vitro Study and In vivo Prediction

Aim: This research work was aimed to evaluate Metformin hydrochloride (MH) floating dosage form by In vitro evaluation/In vivo prediction and to evaluate it’s predictability through it’s application during the R&D using Insilico technique in WINONLIN Software. MH was examined as a model drug, which is a biguanide and is an hypoglycemic agent administered orally. The study was aimed to determine the the systemic concentrations of MH using In-vivo prediction. Study Design: Fabrication and assessment of Metformin hydrochloride floating drug delivery system: In Vitro evaluation /In Vivo prediction. Biorelevant media was selected for dissolution profile of 12 units of dosage form. Software assisted program used for data feeding and results output. Methodology: The absorption window for MH is the upper portion of the small gut in which the GI absorption is complete after 6 h. Hence gastroretentive formulation was developed and validity of dissolution study was extended by In vivo pharmacokinetic prediction using WinNonlin Software. A mechanistic oral absorption model was built in Phoenix WinNonlin® software. In the presented work, significant yet crucial, gastrointestinal (GI) variables are considered for biopredictive dissolution testing to account for a valuable input for physiologically-based pharmacokinetic (PBPK) platform programs. While simulations are performed and mechanistic insights are gained from such simulations from the WinNonlin program. Results: These floating tablets were observed for In vitro release and studied for In vivo pharmacokinetic prediction. From the obtained values, a meaningful In vivo prediction was done. interestingly from the results attained floating tablets showed sustained drug release and extended drug absorbed in 24h. Fascinatingly, from the data it was proved that drug formulation resides for desired time. The absorption of MH from the developed CR tablet was 1.4 fold higher than its marketed tablet and it had higher AUC0–t values than the marketed product which indicates superior bioavailability of test product compared to marketed tablet with similar dose in Invivo pharmacokinetic prediction. The mean value of biological half-life (t1/2) and Tmax of MH from test formulation is two times more, Test product has shown higher MRT, showing that the drug is maintained longer in the body in comparison to marketed product indicates controlled absorption. Conclusion: Here we concluded that, a comparative prediction pharmacokinetic evaluation of the fabricated controlled release tablets and the marketed formulation indicates that the fabricated controlled release tablets are well absorbed and the degree of absorption is greater than that of the marketed ER formulation with larger gastric residence time.

A Review on Floating Multi-particulate Drug Delivery System

The objective of writing this review on Floating Drug Delivery Systems (FDDS) was to accumulate new work with a special focus on the primary floatation mechanism for gastric retention. Drug delivery systems are those that instantly float on contact with gastric fluids and present promising approaches to improve the bioavailability of drugs with absorption windows in the stomach or upper small intestine, imbalanced in the intestinal or colonic environment, and exhibit low solubility at high pH standards. It is a novel drug delivery system that takes full advantage of effectiveness and compliance. Physical problems such as short gastric residence time and unpredictable gastric emptying time were overcome with the use of floating dosage forms that provide the possibility of local and systemic effects. The floating drug delivery system allows prolonged and continuous entry of the drug into the upper part of the gastric retention pathway and increases the bioavailability of the medication characterized by a narrow absorption window. This review provides detailed information on the pharmaceutical basis of its Introduction, Advantages, Disadvantages, Factors Affecting Gastric Emptying, and Criteria for Suitable Drug Products for Floating Gastric-Retention, Classification of Floating Multiparticulate Drug Delivery System, and Characterization of Floating Multiparticulate Drug Delivery System. These systems are beneficial for various difficulties encountered during the development of a pharmaceutical dosage form and the future potential of FDDS. This review article has attempted to announce to readers about the floating drug delivery system.

A Brief Review on Floating Drug Delivery System

Floating drug delivery systems (FDDS) was most convenient and widely used drug delivery for systemic intervention, oral administration. The main purpose of developing the FDDS is to enhance therapeutic benefits such as ease of dosing administration, patient compliance, and formulation versatility. In pharmaceuticals industries we are approaches to design single-unit and multiple-unit floating systems, and classification and formulation of FDDS aspects are covered in detail. This review summarizes the tablet, Floating Drug Delivery System, Type, Mechanism, and also the Advantages & Disadvantages. This sort of medication delivery method is beneficial because it has enough buoyancy to float above gastric contents and stay buoyant in the stomach for a long time. Keywords:- FDDS, Floating Drug Delivery System, Therapeutic, Design, Buoyant, Gastric