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Rabia Bushra, Attaur Rehman, Sana Ghayas, Farya Zafar, Huma Ali, Yousra Shafiq, Farah Khalid, Maqsood Ahmed Khan, Anas Hanif, Omer Mustapha
Cinitapride hydrogen tartarate is relatively a new prokinetic agent that widely prescribed for GERD and epigastric pain. Present study was aimed to develop and optimize cinitapride (1 mg) immediate release (IR) tablet formulation(s) by direct compression using central composite rotatable technique. Overall nine formulations (FC1-FC9) were generated by varying the composition of binder avicel PH 102 (X1) and superdisintegrant crospovidone (X2). The effect of interaction of excipients on hardness (Y1), friability (Y2), disintegration (Y3) and dissolution at 15 min (Y4) were analyzed by RSM plotting...
November 2018: Pakistan Journal of Pharmaceutical Sciences
Mubashir Hassan, Hussain Raza, Muhammad Athar Abbasi, Ahmed A Moustafa, Sung-Yum Seo
Novel drug development is onerous, time consuming and overpriced process with particularly low success and relatively high enfeebling rates. To overcome this burden, drug repositioning approach is being used to predict the possible therapeutic effects of FDA approved drugs in different diseases. Herein, we designed a computational and enzyme inhibitory mechanistic approach to fetch the promising drugs from the pool of FDA approved drugs against AD. The binding interaction patterns and conformations of screened drugs within active region of AChE were confirmed through molecular docking profiles...
January 2019: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Boovizhikannan Thangabalan, Getu Kahsay, Tadele Eticha
A precise and reliable reversed-phase high-performance liquid chromatographic method with ultraviolet detection was developed and validated to determine cinitapride in human plasma. After liquid-liquid extraction, chromatographic separation was achieved on a Nucleosil C18 (25 cm × 4.6 mm, 5  µ m) column with an isocratic elution consisting of 10 mM ammonium acetate (pH 5.2), methanol, and acetonitrile, 40 : 50 : 10, v/v/v. The developed method was validated as per US FDA guidelines for its linearity, selectivity, sensitivity, precision, accuracy, and stability...
2018: Journal of Analytical Methods in Chemistry
Attaur Rehman, Rabia Bushra, Anwar Ejaz Beg, Huma Ali, Farya Zafar, Maria Ashfaq, Shazia Alam, Omer Mustapha, Shumaila Shafique
The initiation of newer techniques and development of mouth dissolving (MD) products has created new avenues of higher patients' compliance. MD formulations are actually lessen the difficulties associated with solid swallowing with better bioavailability of especially poorly soluble drugs. In the current study mouth dissolving tablet (MDT) formulations of cinitapride (1 mg) were prepared by direct compression method using various proportion and combination of superdisintegrants. Nine formulations in three batches were compressed by incorporating low (2%), intermediate (6%) and higher (10%) levels of crospovidone, croscarmellose sodium, sodium starch glycolate...
March 2018: Pakistan Journal of Pharmaceutical Sciences
Xiong Zhang, Ying Wang, Junlin Cheng, Yunfang Hu, Jianghui Liu, Jing Chen, Xingye Yang, Hongwei Fan
Cinitapride (CIN) is a drug for functional dyspepsia. The purpose of the study was to investigate the pharmacokinetics and tolerability of CIN in healthy Chinese volunteers. A randomized, open-label, single- and multiple-dose study was conducted in 12 healthy volunteers. Three different doses of CIN (1, 2, 4 tablets) were given to six groups in the single-dose study, and one tablet (1 mg) of CIN was administered three times a day in the multiple-dose study. Blood samples were collected at predetermined time intervals after CIN dosing and analyzed by LC-MS/MS...
March 28, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Attaur Rehman, Anwar Ejaz Beg, Rabia Bushra, Maria Ashfaq, Farya Zafar, Huma Ali, Mehwish Rizvi
A simple stability indicating UV-spectrophotometric method has been developed and validated for the determination of cinitapride hydrogen tartrate (CHT) in bulk and solid pharmaceutical dosage form. Drug absorption was measured in different analytical mediums however; maximum absorption was seen in 0.1 N HCl at wavelength (λmax) of 266 nm. The calibration curve was found to be linear over the concentration range from 6 to14μg/mL with the correlation coefficient value (r) of 0.999. The LOD and LOQ were estimated to be 0...
November 2017: Pakistan Journal of Pharmaceutical Sciences
Aaron de Souza, Rainha J de Souza
No abstract text is available yet for this article.
October 2017: Annals of Indian Academy of Neurology
Gabriel Marcelín-Jiménez, Leticia Contreras, Javier Esquivel, Óscar Ávila, Dany Batista, Alionka P Ángeles, Alberto García-González
AIM: Cinitapride (CIN) is a benzamide-derived molecule used for the treatment of gastroesophageal reflux and dyspepsia. Its pharmacokinetics are controversial due to the use of supratherapeutic doses and the lack of sensitive methodology. Therefore, a sensitive and accurate micromethod was developed for its quantitation in human plasma. RESULTS: CIN was extracted from 300 µl of heparinized plasma by liquid-liquid extraction using cisapride as internal standard, and analyzed with an ultra performance liquid chromatograph employing positive multiple-reaction monitoring-MS...
March 2017: Bioanalysis
Yiqi Du, Tun Su, Xinmiao Song, Jun Gao, Duowu Zou, Changjing Zuo, Weifen Xie, Bangmao Wang, Zhiguang Zhang, Jianming Xu, Dean Tian, Hesheng Luo, Zhenyu Zhang, Shaofeng Wang, Jianping Chen, Jizhong Guo, Lei Gong, Yanbing Ding, Zhaoshen Li
GOALS AND BACKGROUND: Functional dyspepsia (FD) is a complex disease with a variety of dyspeptic symptoms. Little is known about the clinical efficacy of cinitapride, a 5-HT₄ agonist and D₂ antagonist, in treating FD. STUDY: This randomized, double-blind, double-dummy, positive-controlled study compared the efficacy and safety of cinitapride (1 mg) and domperidone (10 mg) tid for 4 weeks in 383 consecutive patients with mild to moderate, postprandial distress syndrome-predominant dyspeptic symptoms according to Rome III criteria...
April 2014: Journal of Clinical Gastroenterology
Muhammad Tariq Baqai, Mahmood Nasir Malik, Faisal Ziauddin
OBJECTIVE: To study the efficacy and safety of cinitapride in the treatment of functional dyspepsia, and to evaluate the improvement of patients' quality of life. METHODS: The prospective cross-sectional multi-centre phase IV study was conducted at Jinnah Hospital, Lahore, Ziauddin Medical University, Karachi and Pakistan Railways General Hospital, Rawalpindi, from July 2009 to June 2010 and comprised 121 patients of functional dyspepsia who were given cinitapride 1mg thrice daily 15 minutes before meals and were followed up for four weeks...
June 2013: JPMA. the Journal of the Pakistan Medical Association
Helena Marquez, Joan Albertí, Miquel Salvà, Javier Saurina, Sonia Sentellas
An ultra-high performance liquid chromatographic method has been utilized to obtain metabolic profiles of cinitapride with liver microsomes of humans and various mammal species such as rats, mice, mini pigs, dogs, and monkeys. Metabolites have been generated by incubation of cinitapride in the presence of microsomes using nicotinamide adenine dinucleotide phosphate as a cofactor. Incubation times from 15 to 60 min have been assayed. Cinitapride and its metabolites have been separated by reversed-phase C(18) mode using ammonium formate aqueous solution (pH 6...
May 2012: Analytical and Bioanalytical Chemistry
Helena Marquez, Joan Albertí, Miquel Salvà, Javier Saurina, Sonia Sentellas
An ultra high-performance liquid chromatographic method was developed to study the cinitapride metabolism. Metabolites were generated from the incubation of cinitapride with human liver microsomes. Cinitapride and its metabolites were separated by reversed-phase mode using a formate aqueous solution (pH 6.5) and acetonitrile as the components of the mobile phase. Chromatographic conditions, including the establishment of an elution gradient, were optimized for obtaining the maximum number of resolved components in the minimum analysis time...
December 2011: Journal of Separation Science
Eusebi Chiner, José Norberto Sancho-Chust, Mónica Llombart, Ana Camarasa, Cristina Senent, Gabriel Mediero, Elia Gómez-Merino
INTRODUCTION: The sleep-related painful erection (SRPE) is a well-established parasomnia characterized by episodes of penile pain during an erection and typically appears during REM sleep. It is associated with nocturnal awakenings, anxiety, and irritability. AIM: To report a case study that highlights the successful treatment of SRPE with cinitapride. METHODS: We present a case report of a 50-year-old man suffering from SRPE that was studied by polysomnography...
November 2010: Journal of Sexual Medicine
M L González Gutiérrez, M Rubio Pérez, S Vázquez Cortés, B Martínez González de Lema
No abstract text is available yet for this article.
2010: Journal of Investigational Allergology & Clinical Immunology
Piero Portincasa, Fermin Mearin, Marta Robert, M Josep Plazas, Marta Mas, Joan Heras
INTRODUCTION AND OBJECTIVE: Functional dyspepsia is a highly common disorder. The physiopathological mechanisms of this entity are not yet completely known and prokinetic drugs seem to be useful. The aim of this study was to evaluate the prokinetic effect of cinitapride in patients with dysmotility-like dyspepsia and delayed gastric emptying. METHODS: Nineteen patients were randomized to receive 1mg of an oral solution of cinitapride t.i.d or placebo for 4 weeks in two consecutive periods, following a crossover and double-blind design...
December 2009: Gastroenterología y Hepatología
Ernesto J Fernández Tagarro, Raquel de Gracia Núñez, Rafael J Sánchez Villanueva, Carmen Riñón Aguilar, Rafael Selgas Gutiérrez
Granulomatous interstitial nephritides are uncommon entities in routine clinical practice. These entities are usually associated with infectious diseases such as tuberculosis, or immune diseases, such as sarcoidosis, systemic lupus erythematosus or cryoglobulinemia. However, these diseases are most frequently associated with drug intake, especially antibiotics, proton pump inhibitors and nonsteroidal anti inflammatory drugs. An association with prokinetic agents has not previously been reported. We report the case of a 64-year-old woman who developed acute renal failure with this histological pattern after taking the motility promoter cinitapride without her physician's knowledge...
December 2007: Gastroenterología y Hepatología
Marta Robert, Miquel Salvà, Rosa Segarra, Marco Pavesi, Ramón Esbri, David Roberts, Georg Golor
The present clinical trial was designed to evaluate the possible pharmacokinetic and electrocardiographic interactions of the gastroenteric prokinetic drug cinitapride with ketoconazole. The safety and tolerability of the study treatments were also evaluated. After a placebo-controlled, double-blind, crossover design, 16 healthy male (n = 8) and female (n = 8) volunteers were randomized into four treatment groups of four subjects (two males and two females): cinitapride (CTP; 1 mg t.i.d.) + ketoconazole (KET; 200 mg b...
July 2007: Drug Metabolism and Disposition: the Biological Fate of Chemicals
P Rivera, L Ferrer, J A Tuset, S Pamos, J López Mut, M Luján, A Tomé, E Medina
Esophageal compression by a vascular structure is a rare cause of dysphagia, the aberrant right subclavian artery being the most common congenital abnormality. Aortica dysphagia is usually observed in the elderly, especially in hypertensive women with cardiopathy and degenerative osteopathy. We report a 73-year-old woman with dysphagia, caused by a non-aneurysmatic aortic elongation, who presented progressive dysphagia, which ended in aphagia associated with heart failure. The diagnostic approach to these patients is discussed...
August 1999: Gastroenterología y Hepatología
C Alarcón de la Lastra, C La Casa, M J Martin, V Motilva
OBJECTIVE AND DESIGN: The aim of the present study was to examine the effects of cinitapride, a novel prokinetic benzamide-stimulating gastrointestinal motility agent, on gastric secretion and ulceration in rats and elucidate some possible vascular and anti-oxidant mechanisms of such protection. MATERIAL: Male Wistar rats. TREATMENT: Cinitapride (CNT, Lab. Almirall, S.A.) (0.25, 0.5, and 1 mg/kg) and 5-hydroxytryptamine (5-HT, Sigma Chemical Co...
March 1998: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
C Alarcón-de-la-Lastra Romero, A López, M J Martín, C la Casa, V Motilva
This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol. Results were compared with those for 5-hydroxytryptamine (5-HT: 10 mg kg-1). The possible involvements of gastric mucus secretion, endogenous prostaglandins (PGs) and sulfhydryl compounds (SH) in the protection mediated by CNT were also examined. Intraperitoneal administration of CNT (0...
April 1997: Pharmacology
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