Stomach Retention Research Articles

Optimization of non-effervescent riboflavin gastroretentive floating tablets using mixture design

Gastroretentive Floating Drug Delivery Systems (GRFDDS) are long-acting oral dosage forms that float on gastric juice and remain in the stomach for an elongated period gradually delivering drug substances to the upper part of the gastrointestinal system. This study aims to develop and enhance the bioavailability and stomach retention of non-effervescent riboflavin floating tablets by using a variety of polymers. In this investigation, both pre-compression evaluation and post-compression of all the tablet materials were performed according to USP specifications. In vitro, buoyancy analyses were carried out to achieve minimum floating lag time and maximum floating duration. The tablet employed direct compression methods using HPMC K17, Carbopol 940p, and polypropylene foam powder. In vitro, buoyancy studies were performed to achieve minimum floating lag time and maximum floating duration. Tablets were evaluated for physicochemical properties according to USP specifications. An optimized tablet with a floating lag time of 0.77 minutes and a floating time of 48.74 minutes was developed using Design of Experiments (DoE). The results indicated that the optimized formulation, designated as Y, performed the best. It consists of 0.45% polypropylene foam powder, 0.15% HPMC K17, and 0% Carbopol 940p. The developed non-effervescent riboflavin floating tablets have the potential to improve the bioavailability and therapeutic efficacy of riboflavin by enhancing its gastric residence time.

Formulation and Evaluation of Bilayered Floating Tablets of Aceclofenac

The objective of this study was to create and assess homogeneous bilayered floating tablets of aceclofenac in order to increase the drug's bioavailability and prolong its stomach release. One of the nonsteroidal anti-inflammatory drugs (NSAID) common side effects is poor solubility and minimal stomach retention, which makes it difficult to treat effectively. As matrix-forming polymers, ten formulations (F1–F10) were made with different amounts of HPMC K15 and additional excipients. Physical properties, buoyancy, in vitro drug release, and kinetic modelling were evaluated for each formulation. With a floating lag time of less than one minute and buoyancy maintained for more than 12 hours, Formulation 5 (F5) showed the most promising findings. With 97.01% of aceclofenac released over 12 hours, it showed a regulated drug release pattern that followed the Korsmeyer-Peppas release model well (R2 = 0.9242). Pre-compression and post-compression values for the optimised formulation F5 were adequate, suggesting good flow characteristics and tablet integrity. FTIR spectroscopy was used to verify the drug-excipient compatibility, guaranteeing stability and the lack of interactions. According to these results, aceclofenac's homogenous bilayered floating tablets, specifically formulation F5, may be able to improve gastric retention time and offer a sustained release profile. This could mean that the medication can be used to treat chronic inflammatory conditions more effectively and with better patient compliance. Keywords: gastric retention, bioavailability, drug excipient compatibility.

Brain Perception of Different Oils on Appetite Regulation: An Anorectic Gene Expression Pattern in the Hypothalamus Dependent on the Vagus Nerve.

(1) Background: We examined the effect of the acute administration of olive oil (EVOO), linseed oil (GLO), soybean oil (SO), and palm oil (PO) on gastric motility and appetite in rats. (2) Methods: We assessed food intake, gastric retention (GR), and gene expression in all groups. (3) Results: Both EVOO and GLO were found to enhance the rate of stomach retention, leading to a decrease in hunger. On the other hand, the reduction in food intake caused by SO was accompanied by delayed effects on stomach retention. PO caused an alteration in the mRNA expression of NPY, POMC, and CART. Although PO increased stomach retention after 180 min, it did not affect food intake. It was subsequently verified that the absence of an autonomic reaction did not nullify the influence of EVOO in reducing food consumption. Moreover, in the absence of parasympathetic responses, animals that received PO exhibited a significant decrease in food consumption, probably mediated by lower NPY expression. (4) Conclusions: This study discovered that different oils induce various effects on parameters related to food consumption. Specifically, EVOO reduces food consumption primarily through its impact on the gastrointestinal tract, making it a recommended adjunct for weight loss. Conversely, the intake of PO limits food consumption in the absence of an autonomic reaction, but it is not advised due to its contribution to the development of cardiometabolic disorders.

An Overview of Floating Drug Delivery System

The goal of Floating Drug Delivery Systems (FDDS) is to arrange the current emphasis on the basic flotation mechanism to attain stomach retention time. The most current advancements in FDDS are thoroughly discussed, including the formulation and physiological factors influencing stomach retention, methods for designing floating systems, and the characteristics of their classification and formulation. Since dosage forms stay in the stomach longer than conventional dosage forms, the capacity to extend and control the gastric emptying time is a major asset. Gastric emptying of dosage forms is a highly variable process. Drugs with gastroretentive systems have a much longer residence time in the stomach area, improving bioavailability, decreasing drug waste, and increasing solubility for medications that are less soluble in high pH environments. These benefits are achieved over a period of many hours. This review provides a brief overview of floating medication delivery devices

Floating Microsphere as Gastro-Retentive Drug Delivery System

The goal of writing about floating microspheres is to gather the most recent research, paying particular attention to the basic idea of floatation as a means of achieving stomach retention. When a floating medication delivery system comes into touch with the stomach contents, it is expected to float for an extended period of time, improving the drug's bioavailability. Researchers and developers are currently working on the many floating formulations, which include films, tablets, powders, pills, capsules, granules, and capsules. Floating microspheres (FM) are becoming more and more important due to their wide range of applications in drug delivery to the stomach. These less dense floating microsphere, known as gastro retentive floating microspheres, have the capacity to float and disperse uniformly across the entire gastric fluid, reducing the likelihood of gastric emptying and guarantee a longer duration of drug release. Additionally, the floating microsphere improve patient compliance by reducing the frequency of dosing. FMs could be used to significantly improve the therapeutic efficacy of medications with short half-lives. We will go over the foundations of floating microspheres in this overview, as well as some contemporary uses for them.

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.

Gastroretentive Drug Delivery System in Cancer Chemotherapy.

Chemotherapy for stomach cancer often includes several side effects. The primary reasons for the failure of such treatment approaches are low drug concentrations in target tissues and a short stomach residence time. Gastroretentive controlled drug delivery systems improves the therapeutic performance of chemotherapeutic drugs following oral administration because of the longer gastric retention time. The goal of this study was to find suitable gastroretentive formulations that might be used for the localized treatment of stomach cancer. The purpose of this study is to summarize current advances in gastro-retentive drug administration for oral chemotherapy, with a focus on floating, mucoadhesive, and swellable systems. This article also discusses the potentials and limitations of existing gastroretentive drug delivery systems used in cancer chemotherapy. Due to increased stomach retention and modified drug release properties, gastroretentive controlled drug delivery systems improve the therapeutic performance of anti-cancer drugs used to treat stomach cancer. Gastroretentive drug delivery systems appear to be a promising carrier for localized chemotherapy with smaller doses and better patient compliance. However, selection of drug candidates, drugfood interactions and chemotherapy-induced gastric discomfort remain the key characteristics that must be addressed to improve treatment outcomes.

In vitro and in vivo removal efficacy of insoluble Prussian blue in combination with calcium polystyrene sulfonate for thallium.

The similarities between thallium and potassium have suggested the use of calcium polystyrene sulfonate (CPS), an oral ion exchange resin, as a potential agent against thallium intoxication. Therefore, the study was an attempt to evaluate the efficacy of CPS and Prussian blue when given alone or in combination against thallium toxicity. The effect on binding capacity was investigated in terms of contact time, amount of CPS, influence of pH, simulated physiological solutions and interference of potassium ions. Also, rats were given single dose of thallium chloride (20mgkg-1) and the treatment with PB and CPS was given for 28days as CPS 30gkg-1, orally, twice a day, PB 3gkg-1, orally, twice a day and their combination. The effect of antidotal treatment was evaluated by calculating the thallium levels in various organs, blood, urine and feces. The results of the in vitro study indicated exceedingly quick binding in the combination of CPS and PB as compared to PB alone. Also, it was found that the binding capacity at pH 2.0 was considerably increased for PB with CPS (184.656mgg-1) as compared to PB (37.771mgg-1). Furthermore, statistically significant results were obtained in the in vivo study as after 7th day, thallium levels in blood of rats treated with combination were reduced by 64% as compared to control group and 52% as compared to alone PB treated group. Also, Tl retention in liver, kidney, stomach, colon and small intestine of combination treated rats was significantly reduced to 46%, 28%, 41%, 32% and 33% respectively, as compared to alone PB treated group. These findings demonstrate this as a good antidotal option against thallium intoxication.

Floating Drug Delivery Systems (FDDS) Review

This review on floating drug delivery systems (FDDS) was written with the intention of gathering the most recent research with a particular focus on the main mechanism of flotation to induce stomach retention. The most current advancements in FDDS are reviewed in depth, along with the physiological factors and formulation factors impacting stomach retention, design strategies for single-unit and multiple-unit floating systems, and their classification and formulation characteristics. The techniques used in vitro, the in vivo tests used to gauge the effectiveness and use of floating systems, and the applications of these systems are all summarized in this paper. These systems are helpful for a number of issues that arise during the creation of a pharmaceutical dosage form

Review on Gastroretentive Drug Delivery System

GRDDSs are an innovative tactic in this area (Gastro Retentive Drug Delivery System). GRDDSs can improve the regulated administration of drugs with an absorption window by continuously releasing the drug for a long period before it reaches its absorption site. The aim of this study was to investigate, compile, and succinctly summarise both recent and older literatures, with a focus on methods being applied right now to prolong gastric residency duration. They include of high density systems, floating systems, swelling and expanding systems, bio/mucoadhesive systems, and various delayed gastric emptying devices. The current study briefly discusses the categorization, formulation concerns for gastroretentive drug delivery systems, variables affecting stomach retention, advantages, limitations, and applications. To understand the many physiological hurdles involved in establishing stomach retention, we have highlighted important factors impacting it. Then, we assessed the various gastroretentive techniques that have been devised and developed up to this point, including high density (sinking), floating, bio- or mucoadhesive, expandable, unfoldable, ultra porous hydrogel, and magnetic systems. Additionally, the advantages of gastroretentive medicine administration systems were thoroughly covered.

Floating Tablet for Drug Delivery System

The purpose of developing novel delivery systems was to address some issues with the physicochemical properties of pharmaceutical compounds as well as formulation creation, as well as some flaws in conventional dosage forms. The controlled release floating system is a way of medication administration that shows promise. Device for dispensing a potential drug with a narrowing window of absorption. Medicines are insoluble or just very slightly soluble, as well as those that release locally in the stomach and have a low rate of absorption in the colon. Under the floating drug delivery system is a continuous supply gastroretentive medicine administration system. minimally soluble medications are delivered to the absorption site in a controlled manner. These points discuss the floating drug delivery system's advantages and disadvantages in comparison to more conventional drug administration technique. The floating medication delivery system is covered in great length in the review, along with its benefits and drawbacks compared to more traditional drug administration methods.These considerations must be examined when developing dosage forms. There are numerous ways that this dosage type was developed. The review's primary objectives were the formulation and evaluation of the effervescent floating medication delivery system. The goal of this comprehensive study is to bring together the ongoing research on this delivery method, which highlights the different effects that can affect and lessen stomach retention and offers crucial information on its formulation.

A Review on Techniques and Applications of Gastroretentive Drug Delivery System

A Controlled release dose forms have been widely utilized to enhance treatment with a number of significant medications. However, a number of physiological challenges, including the inability to control and localize the system within the target region of the gastrointestinal tract and the extremely changeable nature of the gastric emptying process, pose challenges to the development processes. The bioavailability and periods needed to reach peak plasma levels may be unpredictable as a result of this diversity. The goal of this review on gastro retentive drug delivery systems was to gather the most recent research with a special emphasis on the numerous gastro retentive technologies that have lately emerged as leading approaches in the area of site-specific oral controlled release drug delivery. We have included crucial elements in order to comprehend numerous physiological challenges to achieve stomach retention.

Floating Drug Delivery System: As A Novel Approach for Drug Delivery

The retention period of the drug and dosage form in the stomach is very challenging for the treatment of gastrointestinal disease. To solve this problem and improve the efficacy and bioavailability of the drug, most researchers develop a novel carrier system that is called a Floating drug delivery system (FDDS). The goal of this review on floating drug delivery systems (FDDS) is to synthesise contemporary material with a particular concentration on the main mechanism of flotation for stomach retention. The physiology of the stomach (including gastric pH and movement) has been shown a major effect on gastrointestinal holding period and drug delivery behaviour in both intra- and inter-subject variability. The most recent advancements in the Floating drug delivery system (FDDS) are thoroughly reviewed, including the physiological and formulation factors that influence stomach retention, design methods for single-unit and multiple-unit floating systems, and their categorization and formulation characteristics. A synopsis of the research that has been done to determine the effectiveness and utility of floating systems, as well as uses for such systems, is also included in this review. This study covers the most recent Floating drug delivery system (FDDS) technology advances, including patented delivery techniques and commercial devices, along with their benefits and potential applications for oral controlled drug administration in the future.
 Keywords: Floating drug delivery system, Gastric-emptying time, Inter-digestive myoelectric cycle (IDMC), Polymers, Bioavailability, Membrane permeability.

Floating Drug Delivery System: A Novel apporach for Delivery of Drug on Targated Organ

The goal of this review on floating drug delivery systems (FDDS) was to compile latest data with a particular focus on the main mechanism of flotation for stomach retention. Drug delivery systems that float instantly when they come into contact with gastric fluids are promising approaches for increasing the bioavailability of drugs within absorption window in the stomach or upper small intestine. They are unstable in the intestinal or colonic environment and have low solubility at high pH values. The Current pharmaceutical scenario focuses on the development of sustained drug delivery systems to achieve required therapeutic concentration with less amount of dose. Oral delivery of the drug is the preferable drug delivery system. Because of the ease of administration, patient compliance and formulation flexibility. The ability to delay and control the emptying period of a dosage form in the stomach is an extremely variable process. For dosage forms that stay in the stomach for longer periods of time than standard dosage forms so the gastric transit time is a valuable asset for this system. The goal of this review article is to provide detailed information on the pharmaceutical basis of their design, classification, advantages, in vitro and in vivo evaluation parameters, and applications of floating systems. These systems can help with a variety of issues that arise during the development of a pharmaceutical dosage form, as well as the potential of FDDS in the future. This review article makes an attempt to introduce readers to current developments in floating drug delivery systems.

IN VIVO MONITORING STRATEGIES FOR EVALUATION OF FLOATING DRUG DELIVERY SYSTEMS

In recent years, various advancements have been introduced in the development of controlled drug release devices for resolving different physiological problems for example, gastric retention inconsistency along with erratic gastric emptying time. Gastroretentive delivery formulations receive considerable attention to overcome these drawbacks and in optimizing the absorption of different medicaments. Gastroretentive technologies considerably extend the stomach retention time of dosage forms with increased bioavailability as well as therapeutic efficacy. Gastroretention can be successfully achieved utilizing gastric floating system. The rationale of the present manuscript focuses on current advancements of gastric floating systems so as to accomplish appropriate drug bioavailability and, subsequently drug targeting to the stomach. In vivo evaluation parameters, especially pivotal imaging techniques including roentgenography, gamma scintigraphy, gastroscopy, magnetic marker monitoring, magnetic resonance imaging, ultrasonography, 13C octanoic acid breath test etc. have been emphasized in this manuscript for monitoring drug formulation behavior which extensively revolutionized thorough understanding in the avenue of improved bioavailability of gastroretentive systems.

Formulation and Evaluation of Extended Release Gastroretentive Tablets of Metroprolol Succinate

This study aimed to produce a gastroretentive floating tablet of Metoprolol succinate and examine the effects of release retardant on in vitro drug release. Metoprolol succinate is a β1 selective antagonist used as an Anti-hypertensive, Antiarrhythmic, and Anti Angina. Metoprolol succinate has 48% oral bioavailability due to limited absorption from the lower gastrointestinal tract. The Metoprolol succinate floating tablets were designed to increase stomach retention, prolong drug release, and enhance drug bioavailability. To shorten the floating lag time, hydrophilic polymers like Hydroxypropyl methyl cellulose (HPMC K4M, K15M, and K100M), polyethylene oxide (PEO 303), and sodium bicarbonate as a gas-producing agent were incorporated into the formulation of the floating tablets. Different batches of Metoprolol succinate floating tablets were prepared by direct compression. All the formulations were evaluated for various quality control tests, such as weight variation, hardness, friability, swelling index, floating lag time, and total floating time. As a dissolution medium, 0.1 N HCl was used to conduct an in vitro release investigation on the tablets. The present study demonstrates the potential of the sustained-release floating tablets of Metoprolol succinate as an alternative to conventional formulations.
 Keywords: Bioavailability, Floating tablet, antihypertensive drugs, extended release, Metoprolol succinate, Hydroxypropyl methyl cellulose.

Polymer-coated BiOCl nanosheets for safe and regioselective gastrointestinal X-ray imaging.

Bismuth-based compounds are considered to be the best candidates for computed tomography (CT) imaging of gastrointestinal (GI) tract due to high X-ray absorption. Here, we report the introduction of polymer-coated bismuth oxychloride (BiOCl) nanosheets for highly efficient CT imaging in healthy mice and animal with colitis. We demonstrate simple, low cost and fast aqueous synthesis protocol which provides gram-quantity yield of chemically stable BiOCl nanosheets. The developed contrast gives 2.55-fold better CT enhancement compared to conventional contrast with negligible in vivo toxicity. As a major finding we report a regioselective CT imaging of GI tract by using nanoparticles coated with differentially charged polymers. Coating of nanoparticles with a positively charged polymer leads to their fast accumulation in small intestine, while the coating with negatively charged polymers stimulates prolonged stomach retention. We propose that this effect may be explained by a pH-controlled aggregation of nanoparticles in stomach. This feature may become the basis for advancement in clinical diagnosis of entire GI tract.

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.

A Novel Drug Delivery System: Floating Microspheres in the Development of Gastroretentive Drug Delivery System

Gastric emptying is a complicated process in the human body because it is very inconstant, resulting in ambiguous in vivo drug delivery system efficacy. To combat this variability, scientists have been working on developing a regulated medication delivery system with a long gastric residence period. This review article on gastroretentive drug delivery systems (GRDDS) focuses on numerous gastroretentive approaches that have recently emerged as a leading methodology in the field of site-specific orally administered controlled release drug administration. Gastroretentive medicines come in a variety of forms on the market, including tablets, granules, capsules, floating microspheres, laminated films, and powders. Floating microspheres are currently garnering more attention than previous techniques because of their benefits, which include more consistent drug absorption and a lower risk of local discomfort. The primary goal of this method is to increase gastric retention time in the GIT, which is defined as more than 12 hours in the stomach with an absorption window in the upper small intestine. Longer stomach retention improves bioavailability, reduces drug waste, and boosts solubility for medications that are less soluble in a high pH environment. The medicines are released into the stomach for a long time and consistently thanks to the floating microsphere systems. The current study compiles the most recent research on the techniques of production, characterization, and numerous aspects that impact the performance of floating microspheres for oral administration.

Optimasi Hydroxypropyl Methylcellulose dan Chitosan pada Tablet Floating-Mucoadhesive Diltiazem Hidroklorida Menggunakan Desain Faktorial

Diltiazem HCl is one of the drugs used for hypertension treatment. It requires frequent dosing, which is why diltiazem HCl needs to be formulated into preparations using a controlled release drug delivery system. The combination of floating and the mucoadhesive system is expected to increase the stomach's retention of the dosage form. This study aimed to determine the optimum composition of hydroxypropyl methylcellulose (HPMC K100M) and chitosan for floating mucoadhesive diltiazem HCl tablet. Tablets that have been prepared were evaluated for the tablet's physical characterization, powder flowability test, dissolution test, floating ability, and mucoadhesive test. Tablets were optimized using a factorial design, and the data were analyzed using design expert 11.0.0. The results showed that the optimum formula for polymer combination in diltiazem HCl tablet was 175 mg for HPMC K100M and 50 mg for chitosan. The combination of polymers with this amount can produce a floating lag time of 45,333 seconds, floating duration time >12 hours, and the strength of mucoadhesive is 81,633 grams.