Floating Drug Delivery System Research Articles

In-Vitro, In-Vivo Evaluation of Floating Tablets of Clarithromycin.

The main purpose of this research work was to design and process optimization of oral floating drug delivery system of Clarithromycin floating tablets by using the hydrophilic polymer Hydroxylpropyl methyl cellulose and gas generating agent sodium bicarbonate and citric acid. A 32 randomized full factorial design was used to study. In this design 2 factors were evaluated, each at 3 levels and experimental trials were performed at all 9 possible combinations. The independent and dependent variables are selected for optimization study. The radio-labelled floating tablets were prepared by adding barium sulphate in the optimized formulations for in- vivo radiographic study. The Results of multiple regression analysis indicated that both factors X1 and X2 significantly affected on the dependent parameters. The formulation was optimized on the basis of floating ability and in-vitro drug release. It should be concluded that as the time increases, the swelling index was increased, because weight gain by tablet was increased proportionally with rate of hydration. In-vivo radiographic studies of the optimized formulations were performed using New Zeal Albino rabbits by X-ray imaging technique. The in-vivo X-ray imaging and radiographic studies clearly indicated that the prepared optimized floating tablets were retained in the rabbit stomach over a prolonged period of time and had good in-vivo performance. Radiological evidences suggest that the formulated floating tablets of antibiotics were well floated more than 6 h in rabbit stomach.

Formulation and Evaluation of Famotidine Gastroretentive Floating Tablet by Using Biopolymer

HPMC K4M, HPMC K15M, and HPMC K100M polymers are used in this study to make floating tablets of famotidine hydrochloride. Drug Delivery systems that are floating in the stomach have a lower bulk density than gastric fluids, therefore they stay buoyant in the stomach for a lengthy period of time without impacting gastric emptying rate. In the treatment of gastroesophageal reflex disease (GERD) and peptic ulcer (PUD). Famotidine is a histamine H2 receptor antagonist (GERD). Famotidine is an excellent option for a floating drug delivery system because of its short half-life, brief time in the stomach, and repeated doses. Melt-granulation technique was used to make famotidine floating tablets using HPMC K4M, HPMC K15M, and HPMC K100M. In vitro buoyancy, drug polymer compatibility (IR Research), weight fluctuation, hardness, friability, thickness, drug content and invitro dissolution experiments were all performed on the floating tablets. Using in vitro buoyancy and dissolvability experiments, we were able to establish that the micromeritic characteristic were excellent. HPMC K100M-based formulation F4 has an excellent in vitro buoyancy lag time and floating time, and in vitro dissolution investigations demonstrate a 96.78 percent release for 12 hours. As a result of the findings of this research, it can be concluded that famotidine floating tablets provide the potential for longest- term drug delivery and a consequent reduction in dosage frequency. Keywords: Gastroretentive floating tablet, Famotidine, Formulation and Evaluation, Biopolymer

A review on Advanced approaches and polymers used in gastroretentive drug delivery systems

Insufficient pharmacokinetic characteristics may be associated with the widespread use of oral dosage forms in the treatment of disease. In some cases, the drug is barely soluble; in others, the formulation's rapid transit through the gastrointestinal tract (GIT) makes it difficult to achieve therapeutic levels in body; in addition, some drugs must act locally due to a gastric pathology, but they remain in the stomach for only a short time. Numerous studies have focused on the development of formulations that are capable of enhancing all of these characteristics and extending the stomach residence duration. The prolonged stomach retention duration afforded by gastroretentive controlled drug delivery devices increases the therapeutic efficacy of many orally administered drugs. In the present investigation, we reviewed the advanced methods and polymers used to develop effective gastroretentive drug delivery systems. These methods include swelling and expansion, mucoadhesive, high density, low density, ion exchange, raft forming, magnetic, and floating drug delivery systems. The development of gastroretentive devices involves a broad array of polymeric materials. This work intends to expedite the development of innovative methods by offering a comprehensive understanding of unique gastroretentive approaches along with the polymeric materials utilised in the fabrication of gastroretentive drug delivery systems for oral drug delivery.
 Keywords: Gastroretentive; mucoadhesive; floating; raft forming system; mucoadhesive; swellable.

Preparation and preformualation estimation method of floating microsphere of ofloxacin

Floating drug delivery systems are mainly expected to remain buoyant in gastric contents and consequently to enhance the bioavailability of drugs Microsphere is loaded with a drug in their outer polymer shells was prepared by a novel emulsion-solvent diffusion method. It is floated continuously over the surface of acidic dissolution media containing the surfactant for invitro time 12 hours. Floating microspheres of ofloxacin were prepared by novel o/w emulsion solvent evaporation technique using Ethyl cellulose polymers order to retain drug in body for longer period of time. Ofloxacin has short half-life of 9 hrs. So we prepared a microsphere for increasing their activity.

Floating Drug Delivery System – A Review

The principal objective behind the writing of this article on the floating drug delivery system (FDDS) was to systematize the recent literature with the core process of floatation in acquiring gastric retention. The novel methodologies in FDDS include approaches to design a single unit and multiple-unit floating systems, the physiological and formulation variability affecting gastric retention along with the use of recently invented and developed polymers. FDDS is the drug delivery system that floats immediately upon contact with gastric fluids present promising approaches for increasing the bioavailability of drugs with absorption windows in the upper small intestine. However immediate floating can only be achieved if the density of them device is low at the very beginning. This review also summarizes the in vitro techniques, in vivo studies to evaluate the performance and application of floating systems. Floating dosage forms can be delivered in conventional forms like tablets, capsules with the addition of suitable ingredients along with the gas generating agent. This review also throws light on some approaches to prepare a floating system, evaluation methods and characterization for FDDS pharmaceutical dosage form and also it’s classification and different techniques used in developing floating dosage forms along with current and novel advancements.

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.

Fabrication and Applications of Raft-Forming System - An Emerging Trend in Gastro-retentive Drug Delivery System

Background and Objective: In the past several decades, the gasto-retentive drug delivery system is considered as a novel approach and has gained immense popularity in the field of novel drug delivery systems. Among several approaches to achieve gastric retention raft forming system which comes under the classification of floating drug delivery system is a subject of special research interest. This advanced drug delivery system has the potential to attain a prolonged and predictable drug delivery at specific sites of the GI tract mainly in the stomach and intestine thereby exhibiting a relatively constant plasma profile. Thus, the floating raft forming system finds useful over conventional therapeutics to treat several gastrointestinal disorders viz., gastro esophageal reflux disorder, acid reflux, peptic ulcer, oesophagitis, etc. Methods: In this current manuscript, an extensive search is performed for original research papers using databases viz., Google Scholar, PubMed, Science Direct, etc. Further, painstaking efforts are made to compile and update the recent findings of the formulation scientists working exclusively in the area of raft forming systems. This article portrays a detailed survey about several applications of raft forming systems in the form of tables. Conclusion: The floating raft forming system has the potential for controlled drug release in the upper part of the GI tract and exerts improved bioavailability of the medications having a narrow absorption window. Thus, it is concluded that this advanced dosage form is the caliber candidate for the treatment of several gastrointestinal ailments.

Green synthesis of polyacrylamide grafted Neem Gum for gastro retentive floating drug delivery of Ciprofloxacin Hydrochloride: In vitro and in vivo evaluation

Gastro retentive Floating Drug Delivery Systems (GFDDS) are typically designed to enhance the efficiency of drugs; absorbed in the stomach and possess a short elimination half-life by controlling the drug release rate. This study presents, that Acrylamide Grafted Neem gum (AAm-g-NG) was synthesized for the development of tablet-based GFDDS by using the Microwave-assisted technique for the delivery of Ciprofloxacin Hydrochloride (CFX.HCL). Formulations were evaluated for pre-and post-compression studies like bulk, tapped density, angle of repose and hardness, friability, drug content, weight variation, and drug release, which satisfied all the official requirements of the tablet dosage form. The Structural characterization of the synthesized AAm-g-NG was studied by various analytical techniques like NMR, DSC, FTIR, XRD, and SEM. AAm-g-NG showed a significant swelling index, Water Retention Capacity, Waterlogged capacity, viscosity, and in vitro buoyancy compared to NG and HPMC K100 M. AAm-g-NG was also studied for hemolysis and cytotoxicity; found to be biodegradable and exhibited no toxicity in the Caco-2 cell line. The optimized batch F5 showed controlled drug release of 89% ± 3.56 at 12 h in pH 1.2 and in vivo gastric retention was approx. 8 h in rabbits. The ability of AAm-g-NG graft copolymer to extend the drug release with enhanced gastric retention is well supported by in vivo buoyancy studies and its satisfactory physicochemical properties make it a promising vehicle for gastro retentive system.

Flaxseed Mucilage Hydrogel based Floating Drug Delivery System: Design and Evaluation

Natural polymer-based plant polysaccharides and proteins have been most widely explored as an adjuvant in the dosage form formulation. Here we design a novel gastro-retentive floating tablet, based on a polysaccharide material from Flaxseed (Linum usitatissimum L.) for Domperidone. After oral administration; Domperidone showed good solubility in acidic pH but significantly reduced solubility in alkaline medium. So that to increase the absorption and bioavailability of Domperidone, it is necessary to increase the retention time in the upper part of the Gastrointestinal tract (GIT) by developing a floating sustained drug delivery system. The directly compressible floating tablets of domperidone were formulated using varying amount of hydroxypropyl methylcellulose K 100 M (HPMC K100 M), Carbopol 934 and Flaxseed mucilage. Hardness, friability, weight variation, thickness, disintegration time of tablet formulations were within acceptable limits. The overall results explained that the optimized formulation F5 prepared by the exact ratio of Flaxseed mucilage, HPMC K100 M, Carbopol, could be more efficient on floating and sustained release of Domperidone in the upper part of GIT as compared to the tablets prepared by using HPMC K100 M and Carbopol 934 only. These findings indicated that Flaxseed can be used to develop novel gastro-retentive sustained release drug delivery system with the double advantage of sustained drug release at the upper part of GIT.

A complete review on floating drug delivery system

The aim of writing this review on FDDS to focus on the system of floatation to attain gastric retention, or to attain desired concentration of drug in blood or tissues. Today’s condition focus on the formulation of the FDDS. Effervescent FDDS release carbon dioxide gas, thus decreases the density of the system and remain floatable in stomach for a longer period of time and released the drug at slowly conveniently in order to improve bioavailability of drug. The study summarizes the application of the system, factors that affect floating system, mechanism, advantages, disadvantages and preparation.

DEVELOPMENT AND CHARACTERIZATION OF GASTRO RETENTIVE TABLETS OF CLARITHROMYCIN FOR ANTIULCER EFFECT

Gastroretentive floating drug delivery system (GFDDS) is used to prolong the gastric residence time after oral administration, at a particular site and controlled or modified the release of drug from the formulation.The purpose of the present study is to develop a gastro retentive floating drug delivery system to achieving controlled release so that is improves bioavailability of the formulation, Structure activity relationship based on Biopharmaceutical Properties of Clarithromycin indicates good biopharmaceutical Properties. Floating dosage form of Clarithromycin was designed for the treatment of gastric ulcer caused by Helicobacter pylori. The granules were prepared by wet granulation method and evaluated for flow property, Carrs' index, bulk density, tapped density and Hausner ratio. The dosage form was designed by using polymers of different viscosity as gelling agents, sodium bicarbonate as gas generating agent and other excipients. The granules were further subjected to tablet preparation and the prepared tablets were subjected for evaluated on the basis of different evaluation parameters like hardness, in vitro buoyancy, in vitro drug release. Incorporation of gas generating agent together with polymer improved drug release Optimized formulation (F7) containing Clarithromycin, HPMC, 90 SH , HPMC K4M , sodium bicarbonate, released approximately 86.6% drug in 10 hrs. and the floating lag time was found to be 25 sec. KEYWORDS: GFDDS, Helicobacter pylori, gelling agents, in vitro buoyancy, HPMC, wet granulation.

품질관리 향상을 위한 다양한 생체고분자의 영향과 동결건조 부유약제의 특성 분석

Conventional oral drug systems are unable to keep drug concentration within the therapeutic range, and administration of the dosage form several times a day can cause significant fluctuations in plasma drug concentration. Therefore, floating drug delivery systems are being developed. In this study, floating tablets with a model drug (ampicillin sodium-Amp.Na) were successfully prepared using different polymers by the lyophilization technique. This study aims to prepare and characterize floating lyophilized tablets to understand the effect of different biopolymers on quality control parameters more clearly. Within the scope of characterization studies, many parameters were evaluated successfully. All tablets showed 24-hour release and had a mesoporous structure, as understood from the Brunauer-Emmett-Teller (BET) analysis. It has been determined from the Fourier transform infrared (FTIR) and X-ray diffraction (XRD) analyses that Amp.Na doesn’t interact with excipients and is an amorphous form. These formulations can be used for other drugs in the future, and optimum properties can be easily characterized.

Formulation and Evaluation of Stomach Specific Floating Tablets of Eluxadoline

Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The study included formulation of floating tablets using polymers like Hydroxypropylmethylcellulose K4M and Carbopol 934 as matrix forming agents. The tablets were directly compressed using multi station rotary punching machine. FTIR studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the Pharmacopoeias limit. Tablet showed buoyancy for >12 h. The in- vitro drug release pattern of floating tablets was fitted to different kinetic models which showed highest regression for higuchi model. Formulation E6 found stable during 1 month stability study.

Gastro retentive floating drug delivery system of model drug using central composite design

The work plans to build up a Gastro retentive floating drug delivery system of Model drug using central composite design. The model drug is a drug which is used in the treatment of antiulcer. Extended-release tablets of model drug provide constant plasma concentration with a less frequent administration and also reduce the side effects to some extent. This could extend its safe administration and improve patient compliance. The present study aims to develop floating tablets of model drug using HPMC K4M, Carbopol 934 and an effervescent agent which can float on gastrointestinal fluid for sustained release and evaluate the model drug tablets in-vitro for their TFT, FLT, and drug release pattern. Gastro retentive drug delivery system (GRDDS) refers to systems in which the drug retained in the stomach for a prolonged period that improves the bioavailability of drug substances. Any delivery system aims to deliver a therapeutic amount of drug to the specific site in the body to obtain rapid and then maintain a requisite amount of drug. The formulated tablets evaluated for both pre-compression and post compression parameters including weight variation, hardness, friability, in vitro drug release and different pharmacokinetic plots. Final formulation was agreeable when assessed for all assessment parameters.

Recent Trends in Floating Drug Delivery System

Conventional immediate release dosage forms does not control the drug release which leads to low oral bioavailability and more toxic effects. This happens due to multiple dosing and fluctuations in the plasma drug concentrations. Retention of the dosage forms in a specific region of the GIT provides more benefits, for those drugs which have poor absorption in stomach, low solubility and degradation in alkaline pH. FDDS is one among the important system with gastric retention properties. Formulations designed as FDDS, controls the rate of drug release by prolonging the gastric retention for extended hours and improves the absorption as well as bioavailability. This article provides information on recent trends of research and development in FDDS with a special emphasis on its importance for oral controlled drug delivery system. This review article also provides information on category of drugs and different polymers used for FDDS.

Recent Development in Floating Drug Delivery System: An Overview

Floating medicines work well to increase drug absorption in the stomach. On the basis of current literature, a drug for a novel drug delivery system (NDDS) is established to explicate the floating drug delivery system (FDDS). The most recent FDDS progress involves the formulation as well as physiological aspects that may affect gastric retention and formulation. This review also discusses certain ways of producing a floating system, as well as evaluation methods, characterization, and classification for the FDDS pharmaceutical dosage form. By overcoming physiological hurdles such as short stomach residence times and unexpected gastric emptying times, scientific and technological achievements have been made in the study and development of controlled-release oral drug delivery systems in recent years. So, in general, float dose systems are key technological medication delivery systems that have a stomach-retentive nature and provide a variety of options. Floating drug delivery systems (FDDS), also known as hydro dynamically balanced systems (HBS), swelling and expanding systems, polymeric bio-adhesive systems, modified-shape systems, high-density systems, and other delayed gastric emptying devices are now used to extend the GRT. The latest technological breakthroughs of FDDS, including patented delivery methods and commercialized products, are covered in this study, as well as their advantages and future possibilities for oral controlled drug administration.
 Keywords- A novel drug gastrointestinal tract, types of FDDS, gastric residence time, evaluation of FDDS

DESIGN, OPTIMIZATION, AND EVALUATION OF RAFT FORMING GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF LAFUTIDINE USINGBOX–BEHNKEN DESIGN

Objective: The current research was aimed to formulate and evaluate raft forming gastro retentive floating drug delivery systems of Lafutidine for improving gastric residence time and sustained drug release for an extended time. Methods: Using Box–Behnken experimental design 17 formulations of lafutidine GRDDS were designed and evaluated for various parameters like physical appearance, pH, In vitro gelling study, in vitro buoyancy study, measurement of viscosity, density measurement, gel strength, drug content, acid neutralization capacity, the profile of neutralization, in vitro dissolution, release kinetic and stability studies. Results: All the evaluations were performed and observed that the values were within range, and the buoyancy lag time ranged within 14.76 to 25.84 sec and the formulations remained buoyant for more than 8h with the gelling time of 12h, the drug content was ranging from 98.96 to 99.55 %, and in vitro release was 86.86 to 99.34% by the end of 12h. The release kinetics followed zero-order with Higuchi’s model that indicating that drug release was found to be followed by the matrix diffusion process. Conclusion: Out of all formulations F3 was the optimized formulation and it was further characterized for FTIR, DSC, and stability studies, which exposed that there were no interactions amongst drug and excipients and no major change in the formulation and found to be stable.

A Critical Review on Floating Tablets as a Tool for Achieving Better Gastric Retention.

Most of the oral drug delivery systems demand better retention of drug in the gastrointestinal tract (GIT) for better bioavailability. One of the tools for better gastric retention of the drug is to administer it as a floating drug delivery system (FDDS) by reducing its density, compared to the gastric fluids. This system is helpful to overcome the problems associated with the conventional pharmaceutical dosage forms. The present work is an effort to systematically review the latest advancements in FDDS with a major spotlight on how these systems act to make the dosage form float in the gastric fluid for the slow release, better gastric retention, and improved bioavailability of the orally administered drug. As managing diseases through medicines is going in a new age in which innovative delivery system is being used as well as made accessible for remedial use. The excipients used for making such oral gastro-retention dosage forms (GRDF) to provide sustained release profile of drugs along with the work done so far by different scientists in the past two decades; the patents filed in this area; the evaluation methods for checking the quality of FDDS; and their applications are the major highlights of this work.

Formulation and Evaluation of Floating Drug Delivery System for Oxcarbazepine

Formulation and Evaluation of Floating Drug Delivery System for Oxcarbazepine

Development and Characterization of Repaglinide Loaded Floating Microparticles

Sustained release drug delivery has been successfully achieved using microparticles made from natural or synthetic polymers. The aim of this study is to develop and test floating microparticles of Repaglinide in order to improve drug bioavailability by extending gastric residence time. Repaglinide, an oral hypoglycemic, is a lipophilic drug that is rapidly absorbed from the stomach and eliminated with a half-life of just 1 h, so suitable to be formulated as floating drug delivery system for sustained release.Repaglinide floating microparticles were developed using an ionotropic gelation method that included calcium chloride as a cross-linking agent, sodium alginate, and different concentrations of hydroxypropyl methylcellulose (HPMC), ethyl cellulose (EC), and sodium bicarbonate (NaHCO3). A three factor, three-level Box-Behnken design was used to study the effect of independent variables on dependent variables. In the formulation of microparticles, the amount of hydroxypropyl methylcellulose (X1), ethyl cellulose (X2), and sodium bicarbonate (X3) were three independent variables, while percentage buoyancy (Y1) and percentage drug release at 10 h (Y2) were dependent variables. Micromeritic properties, percent yield, percent drug entrapment performance, surface morphology, percent buoyancy, in-vitro drug release, and drug excipient compatibility were all assessed in the formulations.FTIR studies revealed no interaction between the drug and the excipients.SEM for surface morphology studies revealed that their surface is spherical and smooth. The mean particle size of formulations was found to be between 415- 689 µm, the drug entrapment efficiency was found to be between 44.65% - 76.55% and percent buoyancy was noted to be between 63%- 78.33%. The results revealed that entrapment efficiency increased as polymer concentration was increased. The cumulative percent drug release after 10 h was noted to be between 76.87- 88.12%. Percent drug release decreased as polymers concentration was increased. The buoyancy was increased with increasing concentration of sodium bicarbonate. The developed microparticles could successfully retard the release of the drug.