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https://www.readbyqxmd.com/read/29128589/formulation-and-statistical-optimization-of-gastric-floating-alginate-oil-chitosan-capsules-loading-procyanidins-in-vitro-and-in-vivo-evaluations
#1
Rencai Chen, Xiaomin Guo, Xuecong Liu, Haiming Cui, Rui Wang, Jing Han
The aim of the present work was to develop gastric floating capsules containing oil-entrapped beads loading procyanidins. The floating beads were prepared by ionotropic gelation method using sodium alginate, CaCl2 and chitosan. The effect of three independent parameters (concentration of sodium alginate, CaCl2 and chitosan) on entrapment efficiency were analyzed by Box-Behnken design. The floating beads were evaluated for surface morphology, particle size, density, entrapment efficiency, buoyancy, release behavior in vitro and floating ability in vivo...
November 8, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29122714/diethanolamine-modified-pectin-based-core-shell-composites-as-dual-working-gastroretentive-drug-cargo
#2
Hriday Bera, Sanoj Kumar
The current study aimed at developing diethonolamine-modified high-methoxyl pectin (DMP)-alginate (ALG) based core-shell composites for controlled intragastric delivery of metformin HCl (MFM) by combined approach of floating and bioadhesion. DMP with degree of amidation of 48.72% was initially accomplished and characterized by FTIR, DSC and XRD analyses. MFM-loaded core matrices were then fabricated by ionotropic gelation technique employing zinc acetate as cross-linker. The core matrices were further coated by fenugreek gum (FG)-ALG gel membrane via diffusion-controlled interfacial complexation method...
November 6, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28888975/solvent-responsive-floating-liquid-crystalline-molecularly-imprinted-polymers-for-gastroretentive-controlled-drug-release-system
#3
Li-Ping Zhang, Xiao-Lin Wang, Qian-Qian Pang, Yan-Ping Huang, Lei Tang, Meng Chen, Zhao-Sheng Liu
Liquid crystalline-molecularly imprinted polymer (LC-MIP) particles were first found to possess the floating behavior on the aqueous medium. Combined with molecular recognition, the LC-MIP was fabricated as a novel class of the controlled-release gastric retentive DDS. The LC-MIP was made using co-polymerization of methacrylic acid, 4-methyl phenyl dicyclohexyl ethylene (LC monomer with vinyl group), and ethylene glycol dimethacrylate with S-amlodipine (S-AML) as model template drug. The optimum condition of the preparation of LC-MIP has been obtained relying on release behaviors of S-AML from the LC-MIP...
September 6, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28750896/a-novel-mechanical-antrum-model-for-the-prediction-of-the-gastroretentive-potential-of-dosage-forms
#4
Marco Neumann, Felix Schneider, Mirko Koziolek, Grzegorz Garbacz, Werner Weitschies
The development of gastroretentive dosage forms can be significantly enhanced by the reliable estimation of gastroretentive properties in vitro. In this context, it is mandatory to consider the propulsive contraction waves that occur in the antral region of the stomach, since they are regarded as the major physiological hurdle to overcome. Therefore, the aim of this study was to develop an in vitro model that allowed the evaluation of the gastroretentive potential of objects with different properties (e.g. size, shape and elasticity)...
July 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28688948/kondogogu-gum-zn-2-pectinate-emulgel-matrices-reinforced-with-mesoporous-silica-for-intragastric-furbiprofen-delivery
#5
Hriday Bera, Jhansirani Nadimpalli, Sanoj Kumar, Pavani Vengala
Flurbiprofen (FLU), a non-steroidal anti-inflammatory drug, exhibits limited clinical response due to its poor physicochemical properties. This study aimed at developing reliable drug carriers for intrgastric FLU delivery with a view to improve biopharmaceutical characteristics of drug and modulate its release in a controlled manner. In this context, FLU-loaded kondogogu gum (KG)-Zn(+2)-low methoxyl (LM) pectinate emulgel matrices reinforced with calcium silicate (CS) were accomplished by ionotropic gelation technique employing zinc acetate as cross-linker and characterized for their in vitro performances...
November 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28572961/development-and-evaluation-of-floating-alginate-microspheres-for-oral-delivery-of-anthocyanins-a-preliminary-investigation
#6
Giovana B Celli, Amyl Ghanem, Marianne S Brooks
The goal of this study was to develop floating microspheres that could be used as gastroretentive systems for the delivery of anthocyanins (ACNs). These compounds are absorbed in the stomach and small intestine, and insufficient residence time in these organs could result in limited absorption and contribute to degradation. The microparticles containing freeze-dried haskap berry extract (321.96 ± 8.35 mg cyanidin 3-glucoside equivalents per g) were prepared by ionotropic gelation of alginate (9%, w/w) with calcium ions (CaCl2 at 2%, w/v) in the gelation bath, with calcium carbonate as the gas-generating compound (added at different ratios in the alginate/extract mixture)...
May 2017: Food Science & Nutrition
https://www.readbyqxmd.com/read/28550603/development-of-novel-high-density-gastroretentive-multiparticulate-pulsatile-tablet-of-clopidogrel-bisulfate-using-quality-by-design-approach
#7
Nilesh Desai, Ravindra Purohit
Myocardial infarction, i.e., heart attack, is a fatal condition which is on the increase all over the world. It is reported that a large number of heart attack occur in morning hours which are attributable to platelet aggregation. Chronotherapy at this stage can be crucial. Clopidogrel bisulfate (CLB) is an antiplatelet agent and has become a drug of choice for prevention of heart attack. It is soluble in acidic pH and has a narrow absorption window. So, its long residence time in stomach is desirable. Therefore, a novel high density tablet was developed comprising multiparticulate pellets with pulsatile release necessary to maintain chronotherapy of heart attack...
November 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28529814/ex-vivo-and-in-vivo-characterization-of-interpolymeric-blend-nanoenabled-gastroretentive-levodopa-delivery-systems
#8
Ndidi C Ngwuluka, Yahya E Choonara, Girish Modi, Lisa C du Toit, Pradeep Kumar, Leith Meyer, Tracy Snyman, Viness Pillay
One approach for delivery of narrow absorption window drugs is to formulate gastroretentive drug delivery systems. This study was undertaken to provide insight into in vivo performances of two gastroretentive systems (PXLNET and IPB matrices) in comparison to Madopar® HBS capsules. The pig model was used to assess gastric residence time and pharmacokinetic parameters using blood, cerebrospinal fluid (CSF), and urine samples. Histopathology and cytotoxicity testing were also undertaken. The pharmacokinetic parameters indicated that levodopa was liberated from the drug delivery systems, absorbed, widely distributed, metabolized, and excreted...
2017: Parkinson's Disease
https://www.readbyqxmd.com/read/28529239/formulation-optimization-of-gastro-retention-tablets-of-paeonol-and-efficacy-in-treatment-of-experimental-gastric-ulcer
#9
Xitong Zhang, Yue Zhang, Han Han, Jun Yang, Benliang Xu, Bing Wang, Tong Zhang
This study aims to develop a gastroretentive sustained-release drug delivery system of paeonol using floating properties and to investigate its therapeutic effects in rat models. The gastric retention tablets of paeonol (GRT-Ps) were prepared by a direct compression method, and the Box-Behnken design was used to optimize its formulation. The optimized formulation containing 15% NaHCO3 and a 2 : 1 ratio of paeonol and HPMC-K4M floated within 1 min and remained afloat for more than 8 h in the simulated gastric fluid (200 mL, pH=1...
August 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28515765/preparation-and-in-vitro-in-vivo-evaluation-of-acyclovir-floating-tablets
#10
Rahim Bahri-Najafi, Abolfazl Mostafavi, Naser Tavakoli, Somayeh Taymouri, Mohammad-Mehdi Shahraki
In the current study, floating dosage form containing acyclovir was developed to increase its oral bioavailability. Effervescent floating tablets containing 200 mg acyclovir were prepared by direct compression method with three different rate controlling polymers including Hydroxypropyl methylcellulose K4M, Carbapol 934, and Polyvinylpyrrolidone. Optimized formulation showed good floating properties and in vitro drug release characteristics with mean dissolution time and dissolution efficacy of about 4.76 h and 54...
April 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28435220/formulation-release-characteristics-and-bioavailability-study-of-gastroretentive-floating-matrix-tablet-and-floating-raft-system-of-mebeverine-hcl
#11
Mohamed A El Nabarawi, Mahmoud H Teaima, Rehab A Abd El-Monem, Nagla A El Nabarawy, Dalia A Gaber
To prolong the residence time of dosage forms within the gastrointestinal tract until all drug is released at the desired rate is one of the real challenges for oral controlled-release drug delivery systems. This study was designed to develop a controlled-release floating matrix tablet and floating raft system of Mebeverine HCl (MbH) and evaluate different excipients for their floating behavior and in vitro controlled-release profiles. Oral pharmacokinetics of the optimum matrix tablet, raft system formula, and marketed Duspatalin(®) 200 mg retard as reference were studied in beagle dogs...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28352172/cellulose-nanofiber-aerogel-as-a-promising-biomaterial-for-customized-oral-drug-delivery
#12
Jyoti Bhandari, Harshita Mishra, Pawan Kumar Mishra, Rupert Wimmer, Farhan J Ahmad, Sushama Talegaonkar
Cellulose nanofiber (CNF) aerogels with favorable floatability and mucoadhesive properties prepared by the freeze-drying method have been introduced as new possible carriers for oral controlled drug delivery system. Bendamustine hydrochloride is considered as the model drug. Drug loading was carried out by the physical adsorption method, and optimization of drug-loaded formulation was done using central composite design. A very lightweight-aerogel-with-matrix system was produced with drug loading of 18.98%±1...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28294964/alginate-based-composite-sponges-as-gastroretentive-carriers-for-curcumin-loaded-self-microemulsifying-drug-delivery-systems
#13
Arpa Petchsomrit, Namfa Sermkaew, Ruedeekorn Wiwattanapatapee
Alginate-based composite sponges were developed as carriers to prolong the gastric retention time and controlled release of curcumin-loaded self-microemulsifying drug delivery systems (Cur-SMEDDS). Liquid Cur-SMEDDS was incorporated into a solution made up of a mixture of polymers and converted into a solid form by freeze-drying. The ratio of alginate as the main polymer, adsorbent (colloidal silicon dioxide), and additional polymers-sodium carboxymethyl cellulose (SCMC), hydroxypropyl methylcellulose (HPMC)-was varied systematically to adjust the drug loading and entrapment efficiency, sponge buoyancy, and the release profile of Cur-SMEDDS...
March 15, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28271373/optimization-and-evaluation-of-gastroretentive-ranitidine-hcl-microspheres-by-using-factorial-design-with-improved-bioavailability-and-mucosal-integrity-in-ulcer-model
#14
Abeer Khattab, Nashwah Zaki
The purpose of our investigation was to develop and optimize the drug entrapment efficiency and bioadhesion properties of mucoadhesive chitosan microspheres containing ranitidine HCl prepared by an ionotropic gelation method as a gastroretentive delivery system; thus, we improved their protective and therapeutic gastric effects in an ulcer model. A 3 × 2(2) full factorial design was adopted to study the effect of three different factors, i.e., the type of polymer at three levels (chitosan, chitosan/hydroxypropylmethylcellulose, and chitosan/methylcellulose), the type of solvent at two levels (acetic acid and lactic acid), and the type of chitosan at two levels (low molecular weight (LMW) and high molecular weight (HMW))...
March 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28257881/dual-mechanism-gastroretentive-drug-delivery-system-loaded-with-an-amorphous-solid-dispersion-prepared-by-hot-melt-extrusion
#15
Anh Q Vo, Xin Feng, Manjeet Pimparade, Xinyou Ye, Dong Wuk Kim, Scott T Martin, Michael A Repka
In the present study, we aimed to prepare a gastroretentive drug delivery system that would be both highly resistant to gastric emptying via multiple mechanisms and would also potentially induce in situ supersaturation. The bioadhesive floating pellets, loaded with an amorphous solid dispersion, were prepared in a single step of hot-melt extrusion technology. Hydroxypropyl cellulose (Klucel™ MF) and hypromellose (Benecel™ K15M) were used as matrix-forming polymers, and felodipine was used as the model drug...
February 28, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28247292/design-and-development-of-clopidogrel-bisulfate-gastroretentive-osmotic-formulation-using-quality-by-design-tools
#16
Nilesh Desai, Ravindra Purohit
Clopidogrel bisulfate (CBS) is antiplatelet drug and it is becoming a drug of choice in the treatment and management of prevention of heart attacks and strokes. CBS is stable and soluble in acidic pH; therefore, retention in stomach for prolonged period appears to be beneficial for controlling the bioavailability. The gastroretentive osmotic system (GROS) facilitates prolonged retention of drug in stomach and provides zero-order drug release. A complex formulation like GROS poses many challenges, and QbD tools can help in designing robust formulation which takes all aspects of product and process development in order to deliver a robust product...
February 28, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28219750/release-kinetics-of-highly-porous-floating-tablets-containing-cilostazol
#17
Kyu-Mok Hwang, Cheol-Hee Cho, Nguyen-Thach Tung, Ju-Young Kim, Yun-Seok Rhee, Eun-Seok Park
This study focuses on developing a highly porous floating tablet containing cilostazol. The underlying release mechanism of cilostazol from porous and floating tablets in dissolution media containing surfactants was investigated. The tablets were prepared by compressing granules and excipients with a sublimating agent, followed by sublimation under vacuum. The volatile material for the sublimating agent was chosen based on its flow properties using conventional methods as well as the twisted blade method. Resultant tablets could float immediately and had significantly higher tensile strengths than conventional tablets of similar porosities, holding a promising potential for increasing gastroretentive properties...
February 20, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28123987/bioadhesive-floating-microsponges-of-cinnarizine-as-novel-gastroretentive-delivery-capmul-gmo-bioadhesive-coating-versus-acconon-mc-8-2-ep-nf-with-intrinsic-bioadhesive-property
#18
Smita Raghuvanshi, Kamla Pathak
INTRODUCTION: The study was aimed at the development of low-density gastroretentive bioadhesive microsponges of cinnarizine by two-pronged approach (i) coating with bioadhesive material and (ii) exploration of acconon MC 8-2 EP/NF as bioadhesive raw material for fabrication. MATERIALS AND METHODS: Microsponges were prepared by quasi-emulsion solvent diffusion method using 3(2) factorial design. Capmul GMO was employed for bioadhesive coating. In parallel, potential of acconon for the fabrication of bioadhesive floating microsponges (A8) was assessed...
October 2016: International Journal of Pharmaceutical Investigation
https://www.readbyqxmd.com/read/28031701/gastroretentive-behavior-of-orally-administered-radiolabeled-tamarind-seed-formulations-in-rabbits-validated-by-gamma-scintigraphy
#19
Mahboubeh Razavi, Hamed Karimian, Chai Hong Yeong, Mehran Fadaeinasab, Si Lay Khaing, Lip Yong Chung, Didi Erwandi B Mohamad Haron, Mohamed Ibrahim Noordin
This study aimed to formulate floating gastroretentive tablets containing metformin hydrochloric acid (HCl), using various grades of hydrogel such as tamarind powders and xanthan to overcome short gastric residence time of the conventional dosage forms. Different concentrations of the hydrogels were tested to determine the formulation that could provide a sustained release of 12 h. Eleven formulations with different ratios of tamarind seed powder/tamarind kernel powder (TKP):xanthan were prepared. The physical parameters were observed, and in vitro drug-release studies of the prepared formulations were carried out...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27995102/a-simple-and-sensitive-high-performance-liquid-chromatography-method-for-determination-of-ciprofloxacin-in-bioavailability-studies-of-conventional-and-gastroretentive-prolonged-release-formulations
#20
Jaber Emami, Mahboubeh Rezazadeh
BACKGROUND: A very simple, sensitive, and accurate high-performance liquid chromatography (HPLC) method with ultraviolet detector was developed and applied to determine ciprofloxacin in human plasma following administration of a gastroretentive formulation developed in our laboratory. MATERIALS AND METHODS: HPLC analysis was performed on a C18 μ-Bondapack column (250 mm × 3.9 mm) using acetonitrile: potassium dihydrogen phosphate solution 0.1 M (20:80, v/v, pH 3) at a flow rate of 1...
2016: Advanced Biomedical Research
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