Gastroretentive Dosage Form Research Articles

A Comprehensive Review on Role of Natural Polymers in Gastro Retentive Drug Delivery System (GRDDS)

Abstract: This review is to present a general outline of potent & promising natural polymers (on which only slight research is done) along with their attributes & their pharmaceutical functions in the development of GRDDS (gastro retentive drug delivery system). Therefore, there is a need of more attention & focus on some of these natural polymers which are playing a crucial & indispensable role in the fabrication of GRDDS. Recent & current research trends shows that progressively natural polymers are replacing synthetic polymers in the fabrication of GRDDS as they are more safe, non-toxic, biodegradable, biocompatible, economical, regulatory acceptance, etc. Also, it has been noticed by the researchers that natural polymer due to their properties have successfully amplified gastric residence time, dissolution & bioavailability of the gastroretentive dosage forms.

A Comprehensive Review of Xanthan Gum-Based Oral Drug Delivery Systems.

Xanthan gum (XG) is an exopolysaccharide synthesized by the aerobic fermentation of simple sugars using Xanthomonas bacteria. It comprises a cellulosic backbone with a trisaccharide side chain connected to alternative glucose residues in the main backbone through α (1→3) linkage. XG dissolves readily in cold and hot water to produce a viscous solution that behaves like a pseudoplastic fluid. It shows excellent resistance to enzymatic degradation and great stability throughout a broad temperature, pH, or salt concentration range. Additionally, XG is nontoxic, biocompatible, and biodegradable, making it a suitable carrier for drug delivery. Furthermore, the carboxylic functions of pyruvate and glucuronic acid offer a considerable opportunity for chemical modification to meet the desired criteria for a specific application. Therefore, XG or its derivatives in conjunction with other polymers have frequently been studied as matrices for tablets, nanoparticles, microparticles, and hydrogels. This review primarily focuses on the applications of XG in various oral delivery systems over the past decade, including sustained-release formulations, gastroretentive dosage forms, and colon-targeted drug delivery. Source, production methods, and physicochemical properties relevant to drug delivery applications of XG have also been discussed.

Evaluation of floatability characteristics of gastroretentive tablets using VIS imaging with artificial neural networks

Gastroretentive dosage forms are recommended for several active substances because it is often necessary for the drug to be released from the carrier system into the stomach over an extended period. Among gastroretentive dosage forms, floating tablets are a very popular pharmaceutical technology. In this study, it was investigated whether a rapid, nondestructive method can be used to characterize the floating properties of a tablet.To accomplish our objective, the same composition was compressed, and varied compression forces were applied to achieve the desired tablet. In addition to physical examinations, digital microscopic images of the tablets were captured and analyzed using image analysis techniques, allowing the investigation of the floatability of the dosage form. Image processing algorithms and artificial neural networks (ANNs) were utilized to classify the samples based on their strength and floatability. The input dataset consisted solely of the acquired images.It has been shown by our research that visible imaging coupled with pattern recognition neural networks is an efficient way to categorize these samples based on their floatability. Rapid and non-destructive digital imaging of tablet surfaces is facilitated by this method, offering insights into both crushing strength and floating properties.

“Formulation Development and Evaluation of Floating Microspheres of Drotaverine Hydrochloride as Gastroretentive Dosage Form”.

“Formulation Development and Evaluation of Floating Microspheres of Drotaverine Hydrochloride as Gastroretentive Dosage Form”.

Formulation and evaluation of sustained release floating tablets of venlafaxine using natural polymers

Over the past three decades, oral controlled-release dosage forms have been developed due to their therapeutic advantages, such as ease of administration, patient compliance, and flexibility in formulation. However, this approach has faced physiological difficulties, such as the inability to contain and position the controlled drug delivery system within the desired region of the gastrointestinal tract (GIT) due to variable gastric emptying and motility. Venlafaxine is an antidepressant and a serotonin and norepinephrine reuptake inhibitor (SNRI). Its active metabolite, desvenlafaxine, works by blocking the reuptake of serotonin and norepinephrine, which are key neurotransmitters in mood regulation. Gastroretentive dosage forms can stay in the gastric region for several hours and significantly prolong the gastric residence time of drugs. Natural materials have been extensively used in drug delivery because they are readily available, cost-effective, eco-friendly, capable of many chemical modifications, potentially degradable, and compatible due to their natural origin. Keywords: Sustained Release Floating Tablets, Venlafaxine,

Design and Evaluation of Gastro-Retentive Floating Tablets of Ibandronic acid

The objective of this study is Preparation and evaluation of gastro-retentive floating tablets of Ibandronic acid by direct compression method polymers or combination. In this study, Ibandronic acid, the most commonly used biphosphonate for treating osteoporosis, was formulated as gastro retentive dosage form (GRDF) tablets to enhance its oral bioavailability. GRDDs are an approach to prolong gastric residence time, there by targeting site-specific drug release in the upper GIT for local or systemic effect. GRDF tablets of Ibandronic acid (200 mg) were characterized with the effects of Carbopol 934P, HPMC 4KM and Na-CMC at various ratios on swelling, floating, physical integrity. A prolonged dissolution profile of Ibandronic acid GRDF tablets developed in this study was observed for its thickness, friability, hardness, drug content and in-vitro drug release. Formulated Floating tablets of Ibandronic acid gave satisfactory results for various physicochemical parameters like hardness, friability, thickness, weight variation and content uniformity. Sodium bicarbonate has predominant effect on the buoyancy lag time, while HPMC K4M has predominant effect on total floating time and drug release. From the study it is evident that a promising controlled release floating tablets of Ibandronic acid can be developed to increase gastric residence time and thereby increasing its bioavailability. Both doses significantly reduced the occurrence risk of new vertebral fractures by 50–52 percent when compared to the effects of the placebo drug. Keywords: Gastro retention, Ibandronic acid, floating tablet, Carbopol, GRDF, GRFT.

3D printing of multi-unit gastro-retentive tablets for the pulsatile release of artesunate

Pulsatile drug delivery is hardly achieved by conventional gastro-retentive dosage forms. Artesunate as a typical anti-malaria medicine needs oral pulsatile release. Here, artesunate-loaded pulsatile-release multi-unit gastro-retentive tablets (APGTs) were prepared with a semi-solid extrusion three-dimensional (3D) printing method. An APGT was composed of three units: artesunate-loaded immediate and delayed release units and a block unit. The matrix of the immediate/delayed release units consisted of polyvinylpyrrolidone (PVP) K30 and croscarmellose sodium, which improved the rapid release of artesunate when contacting water. The block unit consisted of octadecanol, hydroxypropyl methyl cellulose K15M, PVP K30, and poloxamer F68. APGTs showed multi-phase release in simulated gastric liquids (SGLs). The first immediate release phase continued for 1 h followed by a long block phase for 7 h. The second rapid release phase was initiated when the eroded holes in the block unit extended to the inner delayed release unit, and this phase continued for about 14 h. Low-density APGTs could ensure their long-term floating in the stomach. Oral APGTs remained in the rabbit stomach for about 20 h. 3D printing provides a new strategy for the preparation of oral pulsatile-release tablets.

Formulation and Evaluation of Floating Microspheres

Gastro-retentive dosage forms have potential for use as controlled- release drug delivery systems. Gastro retentive floating drug delivery systems have a bulk density lower than that of gastric fluids and thus increase residence time of drug in stomach and provide controlled delivery of many drugs. The aim of the present study is formulation and characterization of floating microspheres using model drug. Floating microspheres were prepared by oil-in-water emulsion solvent evaporation technique using ethyl cellulose as release retarding polymers. The floating microspheres were evaluated for percentage yield (%), particle size, drug content, drug entrapment efficiency, in-vitro floating ability and in-vitro drug release studies. The surface morphology of prepared microspheres was characterized by scanning electron microscopy. The microspheres were found to be spherical in shape and porous in nature. Compatibility studies were performed by fourier transform infrared (FTIR) technique. The prepared microspheres showed prolonged drug release of 12 h and remain buoyant for more than 12 h. In-vitro release kinetics were studied in different release kinetics models like zero order, first order model. It was concluded that developed floating microspheres offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved

Gastro Retentive ( Floating) Delivery System

Because of its flexibility in formulation, ease of administration, and patient compliance, the oral route of drug administration is the most preferred route. However, this route has some limitations, such as a limited gastric residence time (GRT) for sustained drug delivery systems and drugs that are absorbed from a specific region of the gastrointestinal tract (GIT). To overcome these limitations, various approaches to increasing the gastric retention time of the delivery system in the upper gastrointestinal tract have been proposed. The gastroretentive dosage form (GRDF) extends the GRT by directing drug release to the upper part of the GIT. GRDFs enable continuous and prolonged drug release and improve bioavailability of drugs with a narrow therapeutic window, thereby extending dosing intervals and increasing patient compliance. This article's goal is to compile the various gastroretentive approaches. We have summarized important factors controlling gastric retention in order to understand the various physiological difficulties in achieving gastric retention. Finally, the parameters for evaluating gastroretentive drug delivery systems are discussed. The current review briefly discusses the current state of various leading Until now, gastroretentive drug delivery technologies such as high density (sinking), floating, bio- or mucoadhesive, expandable, unfoldable, super porous hydrogel, magnetic systems, and so on have been developed. Furthermore, important factors controlling gastroretention, benefits, and future potential are discussed.

Gastro Retentive Drug Delivery System: A Review

Gastro Retentive Drug Delivery Systems (GRDDs) are an approach to prolonging gastric residence time by targeting the release of specific drugs at the top of the GIT for local or systemic effect. The Gastro Retentive Dosage Forms (GRDFs) is a very long-term time used to improve treatment with several important drugs. GRDDs are one example of a novel strategy to extending gastric residence duration, concentrating on the local or systemic effects of particular medications released in the stomach. GRDFs can provide prolonged and continuous drug release to the upper part of the Gastro Intestinal System (GIT), which greatly extends the duration of the drug release, improves the bioavailability of drugs with narrow therapeutic windows, and thus extends the dose interval and improves the patient's compliance. GRDFs enable the drug to be released longer and continuously to the upper part of GIT, thereby significantly extending the time when the drug is released and improving the bioavailability of a drug with narrow therapeutic windows, thus prolonging the dose interval and increasing patient compliance.

Developing gastro-retentive dosage forms by innovative hotmelt technics

Developing gastro-retentive dosage forms by innovative hotmelt technics

A Review for Gastro - Retentive Drug Delivery System

Inadequate pharmacokinetic properties may be connected with the widespread use of oral dose forms in disease treatment. Because of the formulation's rapid transit through the gastrointestinal tract (GIT), it can be challenging to achieve therapeutic levels of the medicine in specific situations when it is barely soluble; In addition, some medications must work locally due to a gastric disease, although they only last a short period in the stomach. Numerous studies have been done to identify formulations that can enhance all of these characteristics while extending stomach residence time. Many orally delivered medications advantageous for from the extended stomach retention time provided by gastroretentive controlled drug delivery systems.With a focus on current methods for extending stomach residence duration, the study's objective was to examine, gather, and present the preceding and contemporary literatures in a shorter format. The current review briefly discusses the need for GRDDS., Pharmaceutical importance’s of GRDDS, Physiology of stomach, Stomach functionalities, Approaches of GRDDS, factors controlling gastric retention, advantages , disadvantages, Method of preparation of Gastro-retentive Multiparticulate system, Polymeric material in gastroretentive formulations, Evaluation of Gastroretentive dosage form, comparsion between Conventional and Gastroretentive drug delivery system.

Formulation and Evaluation of Floating Microspheres of Sitagliptin

Gastro retentive dosage forms have potential for use as controlled- release drug delivery systems. Gastro retentive floating drug delivery systems have a bulk density lower than that of gastric fluids and thus increase residence time of drug in stomach and provide controlled delivery of many drugs. The aim of the present study is formulation and characterization of floating microspheres using Sitagliptin as a model drug for the management of type-2 diabetes mellitus. Floating microspheres were prepared by oil-in-water emulsion solvent evaporation technique using ethyl cellulose and eudragit S-100 as release retarding polymers. The floating microspheres were evaluated for percentage yield (%), particle size, drug content, drug entrapment efficiency, in-vitro floating ability and in-vitro drug release studies. The surface morphology of prepared microspheres was characterized by scanning electron microscopy. The microspheres were found to be spherical in shape and porous in nature. Compatibility studies were performed by fourier transform infrared (FTIR) technique. The prepared microspheres showed prolonged drug release of 12 h and remain buoyant for more than 12 h. In-vitro release kinetics were studied in different release kinetics models like zero order, first order, higuchi and korsmeyer peppas model and the best fit model was found to be higuchi plot with release exponent n value less than 0.89. It was concluded that developed floating microspheres of Sitagliptin offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved.

In Vitro and In Vivo Evaluation of Carbopol 71G NF-Based Mucoadhesive Minitablets as a Gastroretentive Dosage Form.

Gastroretentive dosage forms are intended to stay inside the stomach for a long period of time while releasing an active pharmaceutical ingredient. Such systems may offer significant benefits for numerous drugs compared to other sustained release systems, such as improved pharmacokinetics/bioavailability and reduced intake frequency and thereby improved adherence to the medical therapy. However, there is no gastroretentive product on the market with proven reliable gastroretentive properties in humans. A major obstacle is the motility pattern of the stomach in the fasting state in humans, which reliably ensures gastric emptying of even large indigestible objects into the small intestine. One promising approach to avoid gastric emptying is adhesion of the drug delivery system to the gastric mucosa. In order to achieve mucoadhesive properties, minitablets containing Carbopol 71G NF were developed and compared to minitablets without adhesive properties. In a specialized mucoadhesive test system, the adhesion time was prolonged for adhesive minitablets (240 min) compared to non-adhesive minitablets (30 min). The in vivo transit behavior was investigated using magnetic resonance imaging in 11 healthy volunteers in fasted state in a crossover setup. It was found that the gastric residence time (GRT) of the adhesive minitablets (median of 37.5 min with IQR = 22.5-52.5) was statistically significantly prolonged compared to the non-adhesive minitablets (median of 7.5 with IQR = 7.5-22.5), indicating a delay in gastric emptying by adhesion to the gastric mucosa. However, the system needs further improvement to create a clinical benefit. Furthermore, it was observed that for 9 of 22 administrations (three minitablets were given simultaneously with every administration), the minitablets were not emptied together but showed different GRTs.

Development of Gastroretentive Carriers for Curcumin-Loaded Solid Dispersion Based on Expandable Starch/Chitosan Films.

Curcumin, a polyphenolic extract from the rhizomes of turmeric, exhibits antioxidant, anti-inflammatory, and anticancer activities, which are beneficial for the treatment of gastric diseases. However, curcumin's therapeutic usefulness is restricted by its low aqueous solubility and short gastric residence time. In this study, curcumin-loaded solid dispersion (ratio 1:5) was prepared using Eudragit® EPO (Cur EPO-SD), resulting in an approximately 12,000-fold increase in solubility to 6.38 mg/mL. Expandable films incorporating Cur EPO-SD were subsequently prepared by solvent casting using different types of starch (banana, corn, pregelatinized, and mung bean starch) in combination with chitosan. Films produced from banana, corn, pregelatinized and mung bean starch unfolded and expanded upon exposure to simulated gastric medium, resulting in sustained release of 80% of the curcumin content within 8 h, whereas films based on pregelatinized starch showed immediate release characteristics. Curcumin-loaded expandable films based on different types of starch exhibited similar cytotoxic effects toward AGS cells and more activity than unformulated curcumin. Furthermore, the films resulted in increased anti-inflammatory activity against RAW 264.7 macrophage cells compared with the NSAID, indomethacin. These findings demonstrate the potential of expandable curcumin-loaded films as gastroretentive dosage forms for the treatment of gastric diseases and to improve oral bioavailability.

Design, Development and Evaluation of Gastroretentive Drug Delivery System of Antacids

Magaldrate is an antacid have been widely used in the treatment of various gastric and duodenal disorders such as heartburn, reflux esophagitis, acid indigestion, gastritis, sour stomach, upset stomach, irritable stomach, gastric and duodenal ulcers. The conventional antacids dosage forms have a short duration of action which is about 2-3 hours due to gastric emptying process. A gastroretentive dosage form of antacid is needed since the healing of gastric ulcers occurs when gastric pH is kept above 3-4 during 24 hours. The present study was aimed at developing Gastro retentive bilayer drug delivery systems containing Magaldrate to minimize the side effect, improve the prolongation of action, to reduce the frequency of drug administration. A wet granulation technique was used to formulate 9 batches. Superdisintegrants like Polyplasdone XL-10, Ac-Di-Sol, and sodium starch glycolate was used for immediate release layer and HPMC K4 M, Ac-Di-Sol and lactose like polymers were used in floating layer. Preformulation studies were carried out to optimize the ratios required for various grades of polymers. The prepared floating tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, buoyancy lag time, total floating time, water uptake (swelling index), and in vitro dissolution studies. Successful formulation was developed having floating lag time as low as 30 sec and drug release was sustained up to 12 hrs. A biphasic drug release can be obtained by using bilayer tableting technology which involved compression of immediate and sustained release layer together. Bilayered floating tablets with release characteristics offer critical advantages such as, site specificity with improved absorption and efficacy. This technology can be inculcated to various medicaments which have stomach as the major site of absorption.
 Keywords: Magaldrate, Antacid, Gastroretentive dosage form, Bilayer floating tab, Superdisintegrant

Floating Microsponge: An Emerging Drug Delivery System

Floating microsponges are a method to extend gastric residence time, there with the aid of using concentrated on site-responsive medicament liberate withinside the top GIT for locally or systemic effect. Gastro retentive dosage forms (GRDFs) are getting utilized from a totally long term to enhance treatment with numerous main medications. Floating microsponge significantly enhances the therapy of stomach with the aid of using liberating the medication locally and for that reason used for medication selecting at specific organ. This may be sustained over an extended period of time. Floating drug delivery allow extended and non-stop release of the drug to the top a part of Gastro intestinal tract and this expressively amplify the period of drug release and enhance pharmacokinetic of medication which have slim healing window, with the aid of using this method dosing frequency and affected person compliance is increased. A microsponge’s drug delivery system is a particularly cross-linkage, spongy, polymeric microsphere, polymeric device consisting permeable microspheres. Microsponges are prepared with the aid of using numerous techniques consisting of liquid-liquid suspension polymerization and quasi emulsion solvent diffusion method. Microsponge,s preparations are strong over variety of pH 1 to 11; microsponge,s preparations are strong on the temperature as much as 1300C well suited with maximum vehicles and ingredients. The present assessment introduces microsponge,s technology at the side of its techniques of preparation, characterization, advantages, evaluation and release mechanism of microsponge,s drug delivery system, advertised product and up to date studies regarding microsponge.
 Keywords: Floating microsponge, Oral administration, Controlled release, Quasi emulsion, Target release.

Preparation and Evaluation of anti-viral drug Zanamivir using different polymers

The dosage forms that stay in the stomach for longer period of time are much more effective to treat any disease. Thus, most approachable and feasible way is to prolong the drug delivery and controlling gastric residence time (GRT) and such kind of dosage forms are known as gastro retentive dosage forms (GRDF). The present study is focused to develop GRDF of Zanamivir. About four formulations of Zanamivir tablets were prepared with different ratios of drug and polymers. The prepared tablets were further evaluated on the basis of precompression and post-compression parameters. The dissolution study of the formulations revealed that formulation F3 using polymer (guar gum) showed 93.4% of in vitro drug release for 8 hours and is the optimized formulation. It was thus concluded that guar gum complies all the properties of floating tablets. Keywords: Zanamivir, Dissolution, Gastro retentive drug delivery system, First pass elimination, Influenza, Prophylaxis

HPMC Based Gastro Retentive Drug Delivery System of Effervescent Guifenesine Tablet for Dry Cough

Recent advances in Novel Drug Delivery System is aim to enhance safety and efficacy of drug molecule by formulating a convenient dosage form for administration and to achieve better patient compliance. The controlled release drug delivery systems owning the capacity to be engaged in the stomach remains entitled as Gastro Retentive Drug Delivery Systems. One of the novel approaches for better patient compliance is floating drug delivery. Number of Gastro Retentive dosage forms has been designed to prolong gastric residence time. We are trying to overcome less gastric retention time and trying to reduce the dosing frequency. Gastroretentive systems can remain in the gastric region for several hours and hence significantly prolong the gastric residence time of drugs. Present study involves preparation of floating tablet of Guaifenesin with HPMC K10 and K15M floating tablet were designed to achieve the extended release or retention in GIT, which may result enhance in absorption and leads to increase in bioavaibility. The aim of the present work is to develop safe, effective HPMC based gastro retentive drug delivery system of effervescent Guaifenesin tablet for dry cough with extended release profile.

Organogel investigations as a floating oral system with depot property

In this work we investigate span 40, span 60 and SA as a gelators and olive oil (OO) as apolar liquid phase to discover the ability of organogel formed to be floating in acidic media and gain a unique gastroretentive dosage form. In addition, take advantage of the chemical
 
 and physical properties of cinnarizine (CN) as a model drug suitable for gastroretentive systems. The floating parameters were studied where the floating lag time and floating duration for organogel in both solid and liquid states. Organogels charecterization were accomplished through the folowing investigatational techniques and analytical methods: table top rheology, optical microscope, Fourier-transform infrared spectroscopy (FTIR) and in- vitro release study. The results showed that all organogels immediately floated and they were floating in both states. Moreover, table top rheology showed that the transition temperature was reversible and higher than 37 ºC except for 7% w/w and 10% w/w SA in OO organogels where, optical images of organogel showed fibrillar network. The FTIR showed peaks associated to carbonyl groups indicated to form gelator-gelator interactions. Moreover, in vitro release study of organogel system showed continuous release CN for 9-12 hours.