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Maha A Marzouk, Dina A Osman, Amany I Abd El-Fattah
Itopride hydrochloride (ITO HCl) is a prokinetic agent, used in the treatment of gastrointestinal motility disorders. The aim of the study was to develop stable mucoadhesive thermoreversible nasal gel to avoid first pass effect. ITO HCl was incorporated into the blends of thermoreversible polymers like poloxamer 407 and various mucoadhesive polymers in different concentrations to increase the contact of the formulations with nasal mucosa. The compatibility between the drug and the suggested polymers was studied by Fourier transform infrared and differential scanning calorimetry (DSC)...
August 24, 2018: Drug Development and Industrial Pharmacy
Venkatesh Pilla Reddy, Barry C Jones, Nicola Colclough, Abhishek Srivastava, Joanne Wilson, Danxi Li
Our recent paper demonstrated the ability to predict in vivo clearance of flavin-containing monooxygenase (FMO) drug substrates using in vitro human hepatocyte and human liver microsomal intrinsic clearance with standard scaling approaches. In this paper, we apply a physiologically based pharmacokinetic (PBPK) modeling and simulation approach (M&S) to predict the clearance, area under the curve (AUC), and C max values together with the plasma profile of a range of drugs from the original study. The human physiologic parameters for FMO, such as enzyme abundance in liver, kidney, and gut, were derived from in vitro data and clinical pharmacogenetics studies...
September 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Jagadish Das, Debasis Banerjee
Herein, we developed an operational simple, practical, and selective Ni-catalyzed synthesis of secondary amides. Application of renewable alcohols, earth-abundant and nonprecious nickel catalyst facilitates the transformations, releasing water as byproduct. The catalytic system is tolerant to a variety of functional groups including nitrile, allylic ether, and alkene and could be extended to the synthesis of bis-amide, antiemetic drug Tigan, and dopamine D2 receptor antagonist Itopride. Preliminary mechanistic studies revealed the participation of a benzylic C-H bond in the rate-determining step...
March 16, 2018: Journal of Organic Chemistry
Aroosa Ishtiaq Butt, Bushra Tayyaba Khan, Asma Khan, Qamar-Uz-Zaman Khan
BACKGROUND: Gastroparesis and GERD occur concomitantly in 40 percent of the cases. Prokinetic drugs and acid blockers are employed as the main treatment modality. Ranitidine is an acid blocker with additional prokinetic activity and Itopride is a known prokinetic drug. This study was designed to observe the synergistic potentiating prokinetic effect of Ranitidine on itopride on isolated duodenum of rabbits. METHODS: Ranitidine (10-5-10-3) and itopride (10-6-10-5) were added in increasing concentrations to isolated duodenum of rabbits and contractions were recorded on PowerLab Data acquisition unit AHK/214...
October 2017: Journal of Ayub Medical College, Abbottabad: JAMC
Senthamil Selvan Perumal, Sanmuga Priya Ekambaram, Samundeswari Raja
A simple, selective, rapid, and precise reverse-phase high-performance liquid chromatography (RP-HPLC) method for the simultaneous estimation of rabeprazole (RP), pantoprazole (PP), and itopride (IP) has been developed. The compounds were well separated on a Phenomenex C18 (Luna) column (250 mm × 4.6 mm, dp = 5 μm) with C18 guard column (4 mm × 3 mm × 5 μm) with a mobile phase consisting of buffer containing 10 mM potassium dihydrogen orthophosphate (adjusted to pH 6.8): acetonitrile (70:30 v/v) at a flow rate of 1...
December 2014: Journal of Food and Drug Analysis
Robin S T Ho, Vincent C H Chung, Charlene H L Wong, Justin C Y Wu, Samuel Y S Wong, Irene X Y Wu
Prokinetics for functional dyspepsia (FD) have relatively higher number needed to treat values. Acupuncture and related therapies could be used as add-on or alternative. An overview of systematic reviews (SRs) and network meta-analyses (NMA) were performed to evaluate the comparative effectiveness of different acupuncture and related therapies. We conducted a comprehensive literature search for SRs of randomized controlled trials (RCTs) in eight international and Chinese databases. Data from eligible RCTs were extracted for random effect pairwise meta-analyses...
September 4, 2017: Scientific Reports
Barry C Jones, Abhishek Srivastava, Nicola Colclough, Joanne Wilson, Venkatesh Pilla Reddy, Sara Amberntsson, Danxi Li
Flavin-containing monooxygenases (FMO) are metabolic enzymes mediating the oxygenation of nucleophilic atoms such as nitrogen, sulfur, phosphorus, and selenium. These enzymes share similar properties to the cytochrome P450 system but can be differentiated through heat inactivation and selective substrate inhibition by methimazole. This study investigated 10 compounds with varying degrees of FMO involvement to determine the nature of the correlation between human in vitro and in vivo unbound intrinsic clearance...
October 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Vladimir Jekl, Karel Hauptman, Zdenek Knotek
The number of exotic companion pet rodents seen in veterinary practices is growing very rapidly. According to the American Veterinary Medical Association's surveys, more than 2,093,000 pet rodents were kept in US households in 2007 and in 2012 it was more than 2,349,000 animals. This article summarizes the most important evidence-based knowledge in exotic pet rodents (diagnostics of the hyperadrenocorticism in guinea pigs, pituitary tumors in rats, urolithiasis in guinea pigs, use of itopride as prokinetics, use of deslorelin acetate in rodents, cause of dental disease, and prevention of mammary gland tumors in rats)...
September 2017: Veterinary Clinics of North America. Exotic Animal Practice
N B Lishchuk, V I Simanenkov, S V Tikhonov
AIM: To investigate the clinical and pathogenetic features of the non-acidic types of gastroesophageal reflux disease (GERD) and to evaluate the impact of combined therapy versus monotherapy on the course of this disease. SUBJECTS AND METHODS: The investigation enrolled 62 patients with non-acidic GERD. The follow-up period was 6 weeks. The patients were divided into 2 groups: 1) weakly acidic gastroesophageal refluxes (GER); 2) weakly alkaline GER. Then each group was distributed, thus making up 4 groups: 1) 19 patients with weakly acidic GER who received monotherapy with rabeprazole 20 mg/day; 2) 21 patients with weakly acidic GER had combined therapy with rabeprazole 20 mg and itopride; 3) 8 patients with weakly alkaline GER who received ursodeoxycholic acid (UDCA) monotherapy; and 4) 14 patients with weakly alkaline GER who had combined therapy with UDCA and itopride, The clinical symptoms of the disease, the endoscopic pattern of the upper gastrointestinal tract (GIT) mucosa, histological changes in the esophageal and gastric mucosa, and the results of 24-hour impedance pH monitoring were assessed over time...
2017: Terapevticheskiĭ Arkhiv
Takeshi Kamiya, Michiko Shikano, Eiji Kubota, Tsutomu Mizoshita, Tsuneya Wada, Satoshi Tanida, Hiromi Kataoka, Hiroshi Adachi, Makoto Hirako, Noriaki Okuda, Takashi Joh
The aims of this study were to compare the therapeutic effects of a proton pump inhibitor (PPI), rabeprazole (RPZ), and a prokinetic agent, itopride (ITO), and to investigate the role of PPI in the treatment strategy for Japanese functional dyspepsia (FD) patients. We randomly assigned 134 patients diagnosed by Rome III criteria to 4 weeks treatment with RPZ 10 mg/day ( n  = 69) or ITO 150 mg/day ( n  = 65). Dyspeptic symptoms were evaluated using FD scores at baseline and after 1, 2 and 4 weeks of treatment...
March 2017: Journal of Clinical Biochemistry and Nutrition
Wangda Zhou, Helen Humphries, Sibylle Neuhoff, Iain Gardner, Eric Masson, Nidal Al-Huniti, Diansong Zhou
Itopride, a substrate of FMO3, has been used for the symptomatic treatment of various gastrointestinal disorders. Physiologically based pharmacokinetic (PBPK) modeling was applied to evaluate the impact of FMO3 polymorphism on itopride pharmacokinetics (PK). The Asian populations within the Simcyp simulator were updated to incorporate information on the frequency, activity and abundance of FMO3 enzyme with different phenotypes. A meta-analysis of relative enzyme activities suggested that FMO3 activity in subjects with homozygous Glu158Lys and Glu308Gly mutations (Lys158 and Gly308) in both alleles is ~47% lower than those carrying two wild-type FMO3 alleles...
September 2017: Biopharmaceutics & Drug Disposition
Shahab Abid, Wasim Jafri, Maseeh Uz Zaman, Rakhshanda Bilal, Safia Awan, Aamir Abbas
AIM: To study the effect of itopride on gastric accommodation, gastric emptying and drinking capacity in functional dyspepsia (FD). METHODS: Randomized controlled trial was conducted to check the effect of itopride on gastric accommodation, gastric emptying, capacity of tolerating nutrient liquid and symptoms of FD. We recruited a total of 31 patients having FD on the basis of ROME III criteria. After randomization, itopride was received by 15 patients while 16 patients received placebo...
February 6, 2017: World Journal of Gastrointestinal Pharmacology and Therapeutics
Sayed M Ahmed, Adel Ahmed Ali, Ahmed Ma Ali, Omiya A Hassan
PURPOSE: The aim of the present study was to improve the bioavailability of itopride (ITO) and sustain its action by formulating as a floating dosage form. MATERIALS AND METHODS: Sustained-release floating tablets of ITO hydrochloride (HCl) were prepared by direct compression using different hydrocolloid polymers such as hydroxypropyl methylcellulose and ethylcellulose and/or methacrylic acid polymers Eudragit RSPM and Carbopol 934P. The floating property was achieved using an effervescent mixture of sodium bicarbonate and anhydrous citric acid (1:1 mol/mol)...
2016: Drug Design, Development and Therapy
F Carbone, A Vandenberghe, L Holvoet, T Vanuytsel, L Van Oudenhove, M Jones, J Tack
BACKGROUND: A validated patient-reported outcome instrument is lacking for the functional dyspepsia/postprandial distress syndrome. AIM: To validate the Leuven Postprandial Distress Scale (LPDS). METHODS: The LPDS diary, comprising eight symptoms with verbal descriptors rated for severity (0-4), was derived from focus groups and cognitive debriefing. It was used in a 2-week run-in, 8-week double-blind placebo-controlled trial of itopride 100 mg t...
November 2016: Alimentary Pharmacology & Therapeutics
F M Abdel-Haleem, Adel Madbouly, R M El Nashar, N T Abdel-Ghani
We report here for the first time on the use of Molecularly Imprinted Polymers as modifiers in bulk optodes, Miptode, for the determination of a pharmaceutical compound, itopride hydrochloride as an example in a concentration range of 1×10(-1)-1×10(-4)molL(-1). In comparison to the optode containing the ion exchanger only (Miptode 3), the optode containing the ion exchanger and the MIP particles (Miptode 2) showed improved selectivity over the most lipophilic species, Na(+) and K(+), by more than two orders of magnitude...
November 15, 2016: Biosensors & Bioelectronics
Jae Seung Soh, Kyung-Jo Kim
Optimal bowel preparation increases the cecal intubation rate and detection of neoplastic lesions while decreasing the procedural time and procedural-related complications. Although high-volume polyethylene glycol (PEG) solution is the most frequently used preparation for bowel cleansing, patients are often unwilling to take PEG solution due to its large volume, poor palatability, and high incidence of adverse events, such as abdominal bloating and nausea. Other purgatives include osmotic agents (e.g., sodium phosphate, magnesium citrate, and sodium sulfate), stimulant agents (e...
March 14, 2016: World Journal of Gastroenterology: WJG
Amjad Khan, Zafar Iqbal, Ibrahim Khadra, Lateef Ahmad, Abad Khan, Muhammad Imran Khan, Zia Ullah, Ismail
Domperidone and Itopride are pro-kinetic agents, regulating the gastric motility and are commonly prescribed as anti emetic drugs. In the present study a simple, rapid and sensitive RP-HPLC/UV method was developed for simultaneous determination of Domperidone and Itopride in pharmaceutical samples and human plasma, using Tenofavir as internal standard. Experimental conditions were optimized and method was validated according to the standard guidelines. Combination of water (pH 3.0) and acetonitrile (65:35 v/v) was used as mobile phase, pumped at the flow rate of 1...
March 20, 2016: Journal of Pharmaceutical and Biomedical Analysis
K Ito, M Kawachi, Y Matsunaga, Y Hori, T Ozaki, K Nagahama, M Hirayama, Y Kawabata, Y Shiraishi, M Takei, T Tanaka
Acotiamide is a first-in-class prokinetic drug approved in Japan for the treatment of functional dyspepsia. Given that acotiamide enhances gastric motility in conscious dogs and rats, we assessed the in vitro effects of this drug on the contraction of guinea pig stomach strips and on acetylcholinesterase (AChE) activity in stomach homogenate following fundus removal. We also investigated the serotonin 5-HT4 receptor agonist mosapride, dopamine D2 receptor and AChE inhibitor itopride, and representative AChE inhibitor neostigmine...
April 2016: Drug Research
Myung-Gyu Choi, Poong-Lyul Rhee, Hyojin Park, Oh Young Lee, Kwang Jae Lee, Suck Chei Choi, Sang Young Seol, Hoon Jai Chun, Jong-Sun Rew, Dong Ho Lee, Geun Am Song, Hwoon Yong Jung, Hyung Yong Jeong, In Kyung Sung, Joon Seong Lee, Soo Teik Lee, Sung Kook Kim, Yong Woon Shin
BACKGROUND/AIMS: Therapies of functional dyspepsia (FD) are limited. DA-9701 is a novel prokinetic agent formulated with Pharbitis semen and Corydalis Tuber. We aimed to assess the efficacy of DA-9701 compared with itopride in FD patients. METHODS: Patients with FD randomly received either itopride 50 mg or DA-9701 30 mg t.i.d after a 2-week baseline period. After 4 weeks of treatment, 2 primary efficacy endpoints were analyzed: the change from baseline in composite score of the 8 dyspep-tic symptoms and the overall treatment effect...
July 30, 2015: Journal of Neurogastroenterology and Motility
Fawzia Ibrahim, Jenny Jeehan Nasr
Two simple, rapid and sensitive methods, namely, fourth-derivative synchronous spectrofluorimetry (method I) and HPLC with fluorescence detection (method II) were developed for the simultaneous analysis of a binary mixture of itopride HCl (ITP) and domperidone (DOM) without prior separation. The first method was based on measuring the fourth derivative of the synchronous fluorescence spectra of the two drugs at Δλ = 40 nm in methanol. The different experimental parameters affecting the synchronous fluorescence of the studied drugs were carefully optimized...
February 2016: Luminescence: the Journal of Biological and Chemical Luminescence
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