A Bioequivalence Study of Open-label, Randomized, Single Oral Dose, Two-way Crossover Design of Generic Itopride Hydrochloride 50 mg Film Coated Tablets and Reference Product (Ganaton) in Healthy Thai Subjects under Fasting Conditions

Start Date01 Nov 2024

Sponsor / Collaborator-

CTR20241978

/ CompletedNot Applicable

盐酸伊托必利片在健康受试者中单剂量、随机、开放、空腹两周期/餐后四周期、两序列、交叉设计的生物等效性试验

[Translation] A single-dose, randomized, open-label, two-cycle fasting/four-cycle postprandial, two-sequence, crossover bioequivalence study of itopride hydrochloride tablets in healthy subjects

主要研究目的研究空腹和餐后状态下单次口服受试制剂盐酸伊托必利片（规格：50 mg，裕松源药业有限公司生产）与参比制剂盐酸伊托必利片（商品名为力苏®，规格：50 mg，ABBOTT LABORATORIES(M) SDN.BHD持证）在健康成年受试者体内的药代动力学，比较受试制剂和参比制剂药代动力学的差异，同时计算主要药动学参数（Cmax、AUC0-t和AUC0-∞），并进行初步比较。次要研究目的评价健康受试者在空腹和餐后状态下，单次口服盐酸伊托必利片受试制剂和参比制剂后的安全性。

[Translation]

Main study objectives To study the pharmacokinetics of the test preparation itopride hydrochloride tablets (specification: 50 mg, produced by Yusongyuan Pharmaceutical Co., Ltd.) and the reference preparation itopride hydrochloride tablets (trade name Lisu®, specification: 50 mg, ABBOTT LABORATORIES(M) SDN.BHD) in healthy adult subjects after a single oral administration in the fasting and fed state, to compare the differences in pharmacokinetics between the test preparation and the reference preparation, and to calculate the main pharmacokinetic parameters (Cmax, AUC0-t and AUC0-∞), and make a preliminary comparison. Secondary study objectives To evaluate the safety of the test preparation and the reference preparation of itopride hydrochloride tablets after a single oral administration in healthy subjects in the fasting and fed state.

Start Date26 Jun 2024

Sponsor / Collaborator

Yusongyuan Pharmaceutical Co. Ltd.

NCT06217393

/ Active, not recruitingPhase 3

Randomized Multicentre Open-label Study to Investigate the Non-inferiority of Itopride Hydrochloride 150mg Once Daily Versus Itopride Hydrochloride 50 mg Thrice Daily in Subjects With Functional (Non-ulcer) Dyspepsia or Chronic Gastritis

The study is conducted in patients with functional dyspepsia or chronic gastritis. The purpose of this study is to:
* assess whether the dose of Itopride Hydrochloride 150 mg extended release tablets, taken once daily has a similar effect on gastrointestinal symptoms caused by gastric dysmotility and delayed gastric emptying, like bloating sensation, early satiety, postprandial fullness, upper abdominal pain or discomfort, anorexia, heartburn, nausea and vomiting in functional (non-ulcer) dyspepsia or chronic gastritis, as Itopride Hydrochloride 50 mg film coated tablets administered thrice a day.
* investigate assessment of the treatment provided to each participant.
* monitor safety and tolerability of Itopride Hydrochloride 150 mg extended release tablets, taken once daily before one of the main meals (preferably same meal throughout the treatment) and Itopride Hydrochloride 50 mg film coated tablets thrice daily before meals.

Start Date28 Feb 2024

Sponsor / Collaborator

Abbott Laboratories

100 Clinical Results associated with D2 receptor x ACHE

100 Translational Medicine associated with D2 receptor x ACHE

0 Patents (Medical) associated with D2 receptor x ACHE

Literatures (Medical) associated with D2 receptor x ACHE

01 Jun 2025·Toxicology Reports

Ameliorative role of naringenin in MPTP- induced Parkinsonism: Insights from Drosophila melanogaster experimental model combined with computational biology

Article

Author: Abolaji, Amos Olalekan ; Okonta, Clive ; Ogunyemi, Oludare Michael ; Olabuntu, Babatunde

This study probed the ameliorative effects of naringenin in a D. melanogaster model of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced parkinsonism, incorporating computational analysis. Initially, flies were treated with naringenin (100-500 µM) and MPTP (250-750 µM) for 14 days in two separate studies to determine the optimum concentrations for the treatments. Following this, optimum naringenin concentrations (100 and 300 µM) were administered to MPTP (500 µM)-exposed flies in a 4-day study. Motor function, survival rate, and neurotoxicity biomarkers were assessed alongside biological network analysis and molecular docking simulation. Results indicate that naringenin exhibits hormetic behavior, with 100-300 µM providing optimal neuroprotection. The treatments significantly improved negative geotaxis and acetylcholinesterase activity, and reduced MPTP-induced oxidative stress as indicated by reduced nitric oxide, hydrogen peroxide, and protein carbonyl levels. Furthermore, naringenin restored thiol contents, and enhanced catalase and glutathione-S-transferase activities. Network analysis helped to identify key targets, including DRD4, DRD2, NFKB1, MAOB, MAPK14, and CYP2A6, which function in dopaminergic signaling and oxido-inflammatory pathways. Molecular docking analysis revealed strong binding interactions of naringenin with DRD2, MAO, MAPK, and NF-κB protein targets, primarily through hydrogen bonding and hydrophobic interactions. Overall, these findings suggest that naringenin mitigates MPTP-induced neurotoxicity by enhancing dopaminergic neurotransmission and suppressing oxidative stress and inflammation. This study further supports the neuroprotective potential of naringenin and could be suggested as a promising nutraceutical/drug candidate for Parkinson's disease.

01 Jan 2025·Therapeutic Advances in Gastroenterology

Itopride in functional dyspepsia: open-label, 1-year treatment follow-up of two multicenter, randomized, double-blind, placebo-controlled trials

Article

Author: Broeders, Bert ; Talley, Nicholas J. ; Tack, Jan

Background: Functional dyspepsia (FD) is common but few efficacious therapies exist. Itopride, a prokinetic, acts via dopamine D2 receptor antagonism and acetylcholinesterase inhibition, and is now approved in Japan, Mexico, and Europe for FD. However, long-term efficacy and safety data have not been published. Objective: To evaluate the long-term safety and potential effectiveness of itopride. Design: A long-term open-label drug effectiveness study. Methods: Males and females, 18–65 years, with FD (Rome II) and the absence (by upper endoscopy) of any relevant structural disease were recruited. After the double-blind treatment phase, patients were treated in an open-label extension phase. Results: A total of 798 patients were included in these two open-label trials and received at least one dose of study medication; 551 patients (69.0%) completed 6 months of treatment, and 294 patients (36.8%) completed a 12-month period. Response rates based on the global physician assessment were 61.7%, 64.8%, 69.0 %, 69.1%, 70.1%, 73.1%, and 77.9% at weeks 8, 16, 24, 32, 40, 48, and 52, respectively. Compliance was above 95%. The safety and tolerability profiles were as expected, with the majority of adverse events being gastrointestinal. Prolactin elevations occurred in 3% of the cases but were not clinically significant. No ECG changes were identified. Conclusion: In this population, itopride, given for up to 12 months, was safe, and up to two-thirds appeared to maintain symptom benefit. Trial registration: NCT00110968 and NCT00112203.

01 Dec 2024·Central Nervous System Agents in Medicinal Chemistry

The Role of Ocimene in Decreasing α-Synuclein Aggregation using Rotenone-induced Rat Model

Article

Author: Vellapandian, Chitra ; Sood, Aarita ; Suresh, Ankul Singh

Background:Parkinson’s disease is defined by the loss of dopaminergic neurons in the midbrain of substantia nigra associated with Lewy bodies. The precise mechanism is not yet entirely understood.Objective:The study aims to determine whether ocimene has antiparkinsonian activity by reducing α-Synuclein aggregation levels in the brains of rotenone-induced rat models.Methods:36 male rats were used for six groups, with six animals in each group. Vehicle, control (rotenone, 2.5 mg/kg, i.p), standard (L-Dopa, 10 mg/kg, i.p), Test drug of low dose (66.66 mg/kg, i.p), medium dose (100 mg/kg, i.p), and high dose (200 mg/kg, i.p) were administered to the rats. The open field, actophotometer, hanging wire, and catalepsy tests were used to assess the rat’s motor performance. The expressions of biomarkers such as AchE, D2 Receptor, and α- Synuclein were evaluated, and their level of expression in the brain samples was checked using ELISA. Histopathological analysis was also carried out to determine the degree of neuron degeneration in the brain samples.Results:The open field test showed significant anxiety levels, whereas test groups showed fewer anxiety levels but increased motor activity. The biochemical tests revealed that rotenonetreated rats had higher levels of AchE, but ocimene-treated rats had a significant decrease in AchE levels. The test drug-treated rats also expressed high levels of D2 receptors. In ocimenetreated rats, α-Synuclein aggregation was reduced, however, in rotenone-treated rats' brain samples, higher clumps of α-Synuclein were observed.Conclusion:Ocimene has neuroprotective properties. As a result, this essential oil might be helpful as a therapeutic treatment for Parkinson's disease.

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