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 / 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 AChE x D2 receptor

100 Translational Medicine associated with AChE x D2 receptor

0 Patents (Medical) associated with AChE x D2 receptor

Literatures (Medical) associated with AChE x D2 receptor

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.

19 Dec 2023·ACS Omega

Polyvinylpyrrolidone-Capped Copper Oxide Nanoparticles-Anchored Pramipexole Attenuates the Rotenone-Induced Phenotypes in a Drosophila Parkinson’s Disease Model

Article

Author: Devaraju, Kuramkote Shivanna ; Venugopal, Deepa Mugudthi ; Heggannavar, Geetha B ; Raghu, Shamprasad Varija ; Hanumanthappa, Ramesha ; Suresh, D ; P C, Nethravathi ; Shaikh, Ahesanulla ; Kariduraganavar, Mahadevappa Y ; Nanjaiah, Hemalatha ; Patil, Akshay A ; B M, Siddaiah

Parkinson's disease (PD) is a progressive, age-related neurodegenerative disease. The disease is characterized by the loss of dopaminergic neurons in the substantia nigra, pars compacta of the midbrain. Pramipexole (PPX) is a novel drug used for the treatment of PD. It has a high affinity for the dopamine (DA) D2 receptor subfamily and acts as a targeted mitochondrial antioxidant. It is less effective in the treatment of PD due to its short half-life, highly inconvenient dosing schedule, and long-term side effects. In recent years, PPX-loaded nanoformulations have been actively reported to overcome these limitations. In the current study, we focused on increasing the effectiveness of PPX by minimizing the dosing frequency and improving the treatment strategy for PD. Herein, we report the synthesis of biodegradable polyvinylpyrrolidone (PVP)-capped copper oxide nanoparticles (PVP-CuO NPs), followed by PPX anchoring on the surface of the PVP-CuO NPs (PPX-PVP-CuO NC), in a simple and inexpensive method. The newly formulated PPX-PVP-CuO NC complex was analyzed for its chemical and physical properties. The PPX-PVP-CuO NC was tested to protect against rotenone (RT)-induced toxicity in the Drosophila PD model. The in vivo studies using the RT-induced Drosophila PD model showed significant changes in negative geotaxis behavior and the level of DA and acetylcholinesterase. In addition, oxidative stress markers such as glutathione-S-transferase, total glutathione, thiobarbituric acid reactive species, and protein carbonyl content showed significant amelioration. The positive changes of PPX-PVP-CuO NC treatment in behavior, neurotransmitter level, and antioxidant level suggest its potential role in mitigating the PD phenotype. The formulation can be used for treatment or pharmacological intervention against PD.

01 Jan 2023·Computers in Biology and Medicine

Network pharmacology and LC-MS approachs to explore the active compounds and mechanisms of Yuanjiang decoction for treating bradyarrhythmia

Article

Author: Zhang, Xuexue ; Wang, Xujie ; Li, Jiaxi ; Zhang, Wantong ; Weng, Weiliang ; Zhao, Mengjie ; Li, Qiuyan ; Fu, Jinyi

BACKGROUNDYuanjiang decoction (YJD), a traditional Chinese medicinal prescription, has been found to have a significant heart rate-increasing effect and is effective in the treatment of symptomatic bradyarrhythmia in previous studies. However, its specific components and potential mechanisms remain unclear.METHODSIn this study, we detected and identified the main compounds of YJD using liquid chromatography-mass spectrometry (LC-MS). Through the approach of network pharmacology, we predicted the core targets of the active components, bradyarrhythmia targets, and obtained potential anti-bradyarrhythmia targets of YJD. We further performed protein to protein interaction (PPI), gene ontology (GO) enrichment analyses and kyoto encyclopedia of genes and genomes (KEGG) signaling pathway analyses for core targets, and constructed network of key active ingredients-core targets of YJD. Finally, molecular docking and molecular dynamics simulation were performed for key active ingredients and core targets.RESULTSThe YJD contains a total of 35 main chemical components. The key active ingredients-core targets network contains 36 nodes and 90 edges, including 20 key active ingredients and 16 core targets. The core targets in the PPI network were TP53, TNF, HRAS, PPARG, IL1B, KCNH2, SCN5A, IDH1, LMNA, ACHE, F2, DRD2, CALM1, KCNQ1, TNNI3, IDH2 and TNNT2. KEGG pathway analysis showed that YJD treatment of bradyarrhythmia mainly involves neuroactive ligand-receptor interaction, adrenergic signaling in cardiomyocytes, cAMP signaling pathway, calcium signaling pathway, cholinergic synaptic and serotonergic synapse signaling pathway. The biological processes mainly include regulation of hormone levels, regulation of cardiac contraction, chemical synaptic transmission, circadian rhythm, positive regulation of heart rate, smooth muscle contraction, response to metal ion, oxidation-reduction process, neurotransmitter transport and import across plasma membrane. Molecular docking and molecular dynamics simulation results showed that hesperidin and tetrahydropalmatine had higher affinity with DRD2 and KCNQ1, respectively.CONCLUSIONThis study reveals the pharmacodynamic material basis of YJD and its potential multicomponent-multitarget-multipathway pharmacological effects, predicted its potential anti-bradyarrhythmia mechanism may be related to the regulation of myocardial autonomic nervous function and related ion channels. Our work demonstrates that YJD has great potential for treating bradyarrhythmias as a complementary medicine, and the results can provide a theoretical basis for the development and clinical application of YJD.

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