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Maria Eliza Freitas, Marta Ruiz-Lopez, Susan H Fox
Levodopa remains the most effective treatment for Parkinson's disease and is considered the gold standard therapy. However, disease progression and changes in the gastrointestinal tract result in a declining window of treatment response in a majority of patients. Efforts have been made recently to improve levodopa bioavailability either by developing more effective oral formulations or by innovating routes of administration (intestinal infusion, transcutaneous or inhaled levodopa). IPX066 is a novel levodopa-carbidopa (LD/CD) oral formulation combining immediate-release (IR) and extended-release (ER) LD/CD recently approved in the USA and the EU...
October 14, 2016: CNS Drugs
Kyu-Mok Hwang, Woojin Byun, Cheol-Hee Cho, Eun-Seok Park
The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion-spheronization and sublimation under vacuum. Granules prepared with sublimation at 60°C displayed a slower dissolution rate and smoother surface morphology than those prepared at lower temperatures. This was unexpected as the reported melting point of glyceryl behenate is higher than 69°C...
October 10, 2016: Pharmaceutical Development and Technology
Md Lutful Amin, Tajnin Ahmed, Md Abdul Mannan
PURPOSE: The purpose of this study was to develop and evaluate metronidazole loaded floating-mucoadhesive microsphere for sustained drug release at the gastric mucosa. METHODS: Alginate gastroretentive microspheres containing metronidazole were prepared by ionic gelation method using sodium bicarbonate as gas forming agent, guar gum as mucoadhesive polymer, and Eudragit L100 as drug release modifier. Carbopol was used for increasing the bead strength. The microspheres were characterized by scanning electron microscopy and evaluated by means of drug entrapment efficiency, in vitro buoyancy, and swelling studies...
June 2016: Advanced Pharmaceutical Bulletin
A G Mirani, S P Patankar, V J Kadam
The research envisioned was the development of diltiazem hydrochloride effervescent floating matrix tablet using a risk-based approach. Preliminarily, the in vitro drug release profile was derived which theoretically simulated the in vivo condition after oral administration. Considering this as a rationale, the formulation development was initiated with defining the quality target product profile (QTPP) and critical quality attributes (CQAs). The preliminary studies were conducted to screen material attributes and process parameters followed by their risk assessment studies to select the plausible factors affecting the drug product CQAs, i...
October 2016: Drug Delivery and Translational Research
Jeong Soo Kim, Kwang Ho Cha, Seung Yeob Kang, Donghan Won, Sun Woo Jang, Miwon Son, Moon Ho Son, Ho Jung Choi, Young Won Lee, Myung Joo Kang
OBJECTIVE: DA-9601, an extract of Artemisia asiatica containing eupatilin and jaceosidin as active compounds, has been prescribed to treat gastritis in Asia. In recent times, sustained-release, floating gastroretentive (GR) tablets of DA-9601 are available on the market. In the present study, the physical properties and in vitro drug release profile, in vivo gastric residence time, and gastroprotective effect of GR tablet were compared to those of immediate release (IR) tablets of DA-9601...
2016: Drug Design, Development and Therapy
Carla M Lopes, Catarina Bettencourt, Alessandra Rossi, Francesca Buttini, Pedro Barata
In recent decades, many efforts have been made in order to improve drug bioavailability after oral administration. Gastroretentive drug delivery systems are a good example; they emerged to enhance the bioavailability and effectiveness of drugs with a narrow absorption window in the upper gastrointestinal tract and/or to promote local activity in the stomach and duodenum. Several strategies are used to increase the gastric residence time, namely bioadhesive or mucoadhesive systems, expandable systems, high-density systems, floating systems, superporous hydrogels and magnetic systems...
August 20, 2016: International Journal of Pharmaceutics
Yu Huang, Yumeng Wei, Hongru Yang, Chao Pi, Hao Liu, Yun Ye, Ling Zhao
5-Fluorouracil (5-FU) was loaded in hollow microspheres to improve its oral bioavailability. 5-FU hollow microspheres were developed by a solvent diffusion-evaporation method. The effect of Span 80 concentration, ether/ethanol volume ratio, and polyvinyl pyrrolidone/ethyl cellulose weight ratio on physicochemical characteristics, floating, and in vitro release behaviors of 5-FU hollow microspheres was investigated and optimized. The formulation and technology composed of Span 80 (1.5%, w/v), ether/ethanol (1...
2016: Drug Design, Development and Therapy
Neel Mehta, Iwona Bucior, Shay Bujanover, Rajiv Shah, Amitabh Gulati
BACKGROUND: Postherpetic neuralgia (PHN) interferes with patients' quality of life, and disturbed sleep is a prevalent complaint. Pain-associated sleep interference in turn enhances pain and/or reduces pain tolerance. Therefore, reducing sleep interference by pain, in addition to pain control, may improve patient care. To address this notion, we characterized relationships among changes in pain intensity, sleep interference, and overall impression of improvement in PHN patients treated with gastroretentive gabapentin (G-GR)...
2016: Health and Quality of Life Outcomes
Shweta Agarwal, R S R Murthy
Mucoadhesive tablets have emerged as potential candidates for gastroretentive drug delivery providing controlled release along with prolonged gastric residence time. Gastroretentive mucoadhesive tablets could result in increased bioavailability due to prolonged gastric residence time. A hydrophilic matrix system was developed as mucoadhesion is achievable on appropriate wetting and swelling of the polymers used. The polymers were so chosen so as to provide a balance between swelling, mucoadhesion and drug release...
November 2015: Indian Journal of Pharmaceutical Sciences
Chungang Zhang, Jingya Tang, Dechun Liu, Xuetao Li, Lan Cheng, Xing Tang
In this study a gastric-retentive delivery system was prepared by a novel method which is reported here for the first time. An innovative floating and bioadhesive drug delivery system with a hollow structure was designed and prepared. The floating and bioadhesive drug delivery system was composed of a hollow spherical shell, a waterproof layer (Stearic acid), a drug layer (Ofloxacin), a release retarding film (the novel blended coating materials) and a bioadhesive layer (Carbomer 934P) prepared by using a liquid multi-layering process...
April 30, 2016: International Journal of Pharmaceutics
Giovana Bonat Celli, Wilhelmina Kalt, Marianne Su-Ling Brooks
Several reports have indicated a positive correlation between the consumption of anthocyanins (ACN) and biomarkers relating to the improvement of type 2 diabetes (T2D). However, the results from in vitro studies often do not translate into clinical evidence. Potential causes of these discrepancies are experimental conditions that lack physiological relevancy; extensive degradation of these compounds in vivo due to changes in pH and metabolism; and a short residence time in the absorption window in relation to the absorption rate...
July 2016: Drug Delivery
Rehab Mohammad Yusif, Irhan Ibrahim Abu Hashim, Elham Abdelmonem Mohamed, Mohamed Magdy El Rakhawy
Carbopol (CP) is a biocompatible bioadhesive polymer used as a matrix for gastroretentive (GR) tablets, however, its rapid hydration shortens its bioadhesion and floating when incorporated in effervescent formulae. The interpolymer complexation of CP with polyvinylpyrrolidone (PVP) significantly reduced the excessive hydration of CP, prolonging floating and maintaining the mucoadhesiveness. In early attempts, a lengthy process was followed to prepare such an interpolymer complex. In this study, an in situ interpolymer complexation between CP and two grades of PVP (K25 and K90) in 0...
2016: Chemical & Pharmaceutical Bulletin
Péter Diós, Tivadar Pernecker, Sándor Nagy, Szilárd Pál, Attila Dévay
The object of the present study is to evaluate the effect of application of low-substituted hydroxypropyl cellulose (L-HPC) 11 and B1 as excipients promoting floating in gastroretentive tablets. Directly compressed tablets were formed based on experimental design. Face-centred central composite design was applied with two factors and 3 levels, where amount of sodium alginate (X 1) and L-HPC (X2 ) were the numerical factors. Applied types of L-HPCs and their 1:1 mixture were included in a categorical factor (X 3)...
November 2015: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Rosy Priyadarshini, Gouranga Nandi, Abhijit Changder, Sailee Chowdhury, Sudipta Chakraborty, Lakshmi Kanta Ghosh
Formulation of a gastroretentive extended release tablet of metformin based on polymethacrylamide-g-gellan (Pmaa-g-GG)-tamarind seed gum (TSG) composite matrix is the main purpose of this study. Tablets were prepared employing wet granulation method taking amount of Pmaa-g-GG, TSG and NaHCO3 (SBC, buoyancy contributor) as independent formulation variables. The tablets were then evaluated for in vitro drug release, buoyancy, ex vivo mucoadhesion, swelling and surface morphology. Compatibility between drug and excipients was checked by DSC, FTIR and XRD analysis...
February 10, 2016: Carbohydrate Polymers
Nijaguni Revansiddayya Rudraswamy-Math, Vankdari Rama-Mohan Gupta
Alfuzosin hydrochloride is a novel drug used in the treatment of urinary incontinency. The purpose of this research was to develop controlled release floating matrix formulations of Alfuzosin HCl. Floating matrix tablets of Alfuzosin HCl were prepared using hydroxypropyl methylcellulose (HPMC), Polyethylene oxide (PEO), Carbopol 971P NF polymer (Direct compressible) and Blend of Polyvinyl Acetate and Povidone 30 (80:19:1(0.8% sodium laury sulfate and 0.2% silica)). Combination of citric acid and sodium bicarbonate were also used as gas forming agent...
November 2015: Pakistan Journal of Pharmaceutical Sciences
Krishna Devarakonda, Kenneth Kostenbader, Michael J Giuliani, Jim L Young
BACKGROUND: Biphasic immediate-release (IR)/extended-release (ER) hydrocodone bitartrate (HB)/acetaminophen (APAP) 7.5/325-mg tablets are formulated with gastroretentive ER drug delivery technology that has been associated with clinically meaningful food effects in other approved products. Two phase 1 studies evaluated potential effects of food on single-dose pharmacokinetics of IR/ER HB/APAP tablets. METHODS: These were single-center, open-label, randomized, single-dose, 3-period crossover studies in healthy volunteers (aged 18-55 years)...
2015: BMC Pharmacology & Toxicology
Kamla Pathak, Nida Akhtar, Sonam Singh
Gastroretentive drug-delivery systems have the potential to prolong the gastric retention time and provide controlled/sustained release of a drug at the absorption site, thereby improving the bioavailability. Advantageous features include reduction in dose, side effects and dosing frequency. Research inputs have led to exploration of novel gastroretentive systems. The present review explores various patents issued on gastroretentive drug delivery on the basis of the therapeutic category of drugs. It traces US, EP and WIPO patents issued in the last 10 years...
2015: Pharmaceutical Patent Analyst
Sanjay Bansal, Sarwar Beg, Babita Garg, Abhay Asthana, Gyati S Asthana, Bhupinder Singh
The objective of the present studies was systematic development of floating-bioadhesive gastroretentive tablets of cefuroxime axetil employing rational blend of hydrophilic polymers for attaining controlled release drug delivery. As per the QbD-based approach, the patient-centric target product profile and quality attributes of tablet were earmarked, and preliminary studies were conducted for screening the suitability of type of polymers, polymer ratio, granulation technique, and granulation time for formulation of tablets...
October 2016: AAPS PharmSciTech
Ju-Hee Oh, Ji Eun Lee, Yu Jeong Kim, Tack-Oon Oh, SungKyun Han, Eun Kyung Jeon, Kyungmin Shin, Dong-Hyun Kim, Chi Hye Park, Young-Joo Lee
Patients with type 2 diabetes mellitus have a high risk of cardiovascular disease mainly caused by dyslipidemia. Metformin and atorvastatin are preferentially used to treat type 2 diabetes mellitus and dyslipidemia, respectively. The aim of this study was to develop a once-a-day fixed-dose combination tablet containing metformin and atorvastatin. For this purpose, we designed gastroretentive bilayer tablets consisting of 500 mg metformin in a sustained release layer and 10 mg atorvastatin in an immediate release layer...
2016: Drug Development and Industrial Pharmacy
Marc Lemieux, Patrick Gosselin, Mircea Alexandru Mateescu
Carboxymethyl starch microspheres (CMS-MS) were produced from carboxymethyl starch powder (CMS-P) with a degree of substitution (DS) from 0.1 to 1.5 in order to investigate the influence of DS on physicochemical, drug release and mucoadhesion properties as well as interactions with gastrointestinal tract (GIT) epithelial barrier models. Placebo and furosemide loaded CMS-MS were obtained by emulsion-crosslinking with sodium trimetaphosphate (STMP). DS had an impact on increasing equilibrium water uptake and modulating drug release properties of the CMS-MS according to the surrounding pH...
December 30, 2015: International Journal of Pharmaceutics
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