gastroretentive

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No abstract text is available yet for this article.

No abstract text is available yet for this article.

No abstract text is available yet for this article.

The study aims to design and optimize the floating formulations of the aqueous extract of Desmostachya bipinnata (ADB) to treat peptic ulcers. The trial concentrations of HPMC E50, HPMC K4M, and Carbopol 940 were used as factors, and floating lag time, total floating time, and % drug release at 12 h were used as responses. The formulation underwent evaluation for different parameters: aspirin-induced ulcers in rats assessed the antiulcer activity, and X-ray studies in rabbits evaluated the gastroretentive nature...

Capsaicin (CAP) has been implicated as a gastroprotective agent in the treatment of peptic ulcers. However, its oral administration is hampered by its poor aqueous solubility and caustic effect at high administered doses. To address these limitations, we describe the development of gastric floating, sustained release electrospun films loaded with CAP. The nanofiber films were formulated using the polymers Eudragit RL/RS and sodium bicarbonate (SB) as the effervescent agent. The films were tested for their physicochemical properties, and film buoyancy and in vitro release of CAP were assessed in simulated gastric fluid...

OBJECTIVES: Efficacy and compliance of type II diabetes treatment would greatly benefit from dosage forms providing controlled release of metformin in the upper gastrointestinal tract. In this respect, the feasibility of a new system ensuring stomach-retention and personalized release of this drug at its absorption window for multiple days was investigated. METHODS: The system proposed comprised of a drug-containing core and a viscoelastic umbrella-like skeleton, which were manufactured by melt-casting and 3D printing...

Luteolin, a natural flavonoid, is gaining growing attention for its potential in the treatment of gastric cancer. However, its clinical application is limited by factors such as poor aqueous solubility. This study aimed to develop a novel gastroretentive drug delivery system (GRDDS) to both enhance the oral bioavailability of luteolin and prolong its release and in vivo circulation time. Out of 10 luteolin-loaded PLA-based shape memory films prepared in this study, the LPC-PLA/PEG(7/3) formulation incorporated with PEG, HPMC, and NaHCO3 exhibited optimal properties in terms of drug release and inhibitory activity against SGC-7901 cells...

INTRODUCTION: Sustaining a healthy weight is a great challenge and obesity has become a pandemic with associated risk of co-morbidities, hence a major concern for public health bodies worldwide. Surgical interventions, such as bariatric surgery, have shown a great promise for many where pharmacological and lifestyle interventions failed to work. However, challenges and limitations associated with bariatric surgery has pushed the demand for less invasive, reversible (anatomically) interventions, such as intragastric balloons (IGBs)...

The stomach and upper part of the small intestine are where furosemide is primarily absorbed when treating edema brought on by congestive heart failure (CHF), hepatic cirrhosis, renal impairment, and nephrotic syndrome. This narrow absorption window is responsible for furosemide's limited oral bioavailability. So creating a gastroretentive floating tablet could be beneficial. Natural polymers are advised for use in medication delivery because they are readily available in nature, biodegradable, relatively inexpensive, biocompatible, and nontoxic...

The current research attempted to design and evaluate sustained stomach-specific ofloxacin delivery by single-unit hydrodynamically balanced system (HBS)-based floating capsules. These HBS-based floating capsules of ofloxacin were prepared using two oppositely ionic polymers, namely cationic-natured low molecular mass chitosan (LMMCH) and anionic-natured carboxymethyl tamarind gum (CMTG). FTIR results indicated the in situ formation of a polyelectrolyte complex in-between two oppositely charged polymers (i...

Drug delivery systems (DDS) control the amount, rate, and site of administration of drug substances in the body as well as their release and ADME (absorption, distribution, metabolism, excretion). Among the various types of DDS, amount-controlled DDS for solubilization and absorption increase the bioavailability. Time- and amount-controlled DDS are controlled release formulations classified as (1) membrane-type, (2) matrix-type, (3) osmotic-type, and (4) ion-exchange type. Timed-release formulations also control the time and amount of release and the absorption of drugs...

In the present part, models are developed for in vivo expansion, gastric residence time, and drug concentration in blood after administering a slow-release, gastroretentive fibrous dosage form to dogs. The tyrosine kinase inhibitor nilotinib, which is slightly soluble in low-pH gastric fluid but practically insoluble in high-pH intestinal fluid, is used as a model drug. The models suggest that upon ingestion, the fibrous dosage form expands, is retained in the stomach for prolonged time, and releases drug into the gastric fluid at a constant rate...

In this final part, the models of in vivo expansion, gastric residence time, and drug concentration in blood developed in Part 3 are validated on dogs. Both slow-release gastroretentive fibrous and immediate-release particulate dosage forms containing 200 mg nilotinib were tested. As predicted by the model, in the stomach the fibrous dosage form expanded linearly with time to about 1.5 times the initial radius by 4 hours. The expanded dosage form fractured after about 10 hours, and then passed into the intestines...

At present, the efficacy and safety of many sparingly soluble tyrosine kinase inhibitors (TKIs) are compromised due to the drug's pH-dependent solubility, and the associated excessive fluctuations in the drug concentration in blood. To mitigate this limitation, in this four-part study gastroretentive fibrous dosage forms that deliver drug into the low-pH gastric fluid (and into the blood) for prolonged time are presented. The dosage form comprises a cross-ply fibrous structure of water-absorbing, high-molecular-weight hydroxypropyl methylcellulose (HPMC) fibers coated with a strengthening, enteric excipient...

In Part 1, we have introduced gastroretentive fibrous dosage forms with expandable, strengthened excipient fibers, and drug-loaded inter-fiber space for prolonged delivery of sparingly soluble tyrosine kinase inhibitors. The in vitro expansion rate, post-expansion mechanical strength, and drug release rate were modeled for a dosage form containing 200 mg of nilotinib. In the present part, the dosage form was prepared and tested in vitro to validate the models. Upon immersing in a dissolution fluid, the fibrous dosage form expanded at a constant rate to a normalized radial expansion of 0...

Novel in situ gelling liquid formulations incorporating garcinia extract were developed to achieve prolonged delivery of hydroxycitric acid (HCA), an active compound displaying anti-obesity function, following oral administration. The optimized formulation was composed of sodium alginate (1.5% w / v ), hydroxypropyl methylcellulose (HPMC K100) (0.25% w / v ), calcium carbonate (1% w / v ) and garcinia extract (2% w / v ). The formulation displayed rapid gelation in less than a minute on exposure to 0.1 N hydrochloric acid (pH 1...

Drug delivery systems capable of being retained within hollow organs allow the entire drug dose to be delivered locally to the disease site or to absorption windows for improved systemic bioavailability. A novel Organ-Retentive Osmotically Driven System (ORODS) was here proposed, obtained by assembling drug-containing units having prolonged release kinetics with osmotic units used as increasing volume compartments. Particularly, prototypes having H-shape design were conceived, manufactured and evaluated. Such devices were assembled by manually inserting a tube made of regenerated cellulose (osmotic unit) into the holes of two perforated hydrophilic tableted matrices containing paracetamol as a tracer drug...

In the present study, novel gastroretentive bilayer tablets were developed that are promising for the once-a-day oral delivery of the drug candidate MT-1207. The gastroretentive layer consisted of a combination of hydrophilic and hydrophobic polymers, namely polyethylene oxide and Kollidon® SR. A factorial experiment was conducted, and the results revealed a non-effervescent gastroretentive layer that, unlike most gastroretentive layers reported in the literature, was easy to prepare, and provided immediate tablet buoyancy (mean floating lag time of 1...

Sangelose® (SGL) is a novel hydroxypropyl methylcellulose (HPMC) derivative that has been hydrophobically modified. Due to its high viscosity, SGL has the potential as a gel-forming and release-rate-controlled material for application in swellable and floating gastroretentive drug delivery systems ( sf GRDDS). The aim of this study was to develop ciprofloxacin (CIP)-loaded sf GRDDS tablets comprised of SGL and HPMC in order to extend CIP exposure in the body and achieve optimal antibiotic treatment regimes...