[Translation] A formal trial of a randomized, open-label, single-dose, two-drug, crossover design to evaluate the bioequivalence of a single oral dose of the test formulation, trimebutine maleate tablets, and the reference formulation, trimebutine maleate tablets (trade name: Debridat®), in healthy Chinese subjects in the fasting and fed state

主要目的：研究空腹及餐后状态下单次口服受试制剂马来酸曲美布汀片（规格：0.2g/片，浙江东亚药业股份有限公司生产）与参比制剂马来酸曲美布汀片（Debridat®，规格：200mg/片；FARMEA生产）在健康受试者体内的药代动力学，评价空腹及餐后状态口服两种制剂的生物等效性。次要目的：研究受试制剂马来酸曲美布汀片和参比制剂马来酸曲美布汀片在健康受试者中的安全性。

[Translation]

Primary objective: To study the pharmacokinetics of the test preparation trimebutine maleate tablets (specification: 0.2g/tablet, produced by Zhejiang East Asia Pharmaceutical Co., Ltd.) and the reference preparation trimebutine maleate tablets (Debridat®, specification: 200mg/tablet; produced by FARMEA) in healthy subjects after single oral administration in fasting and fed state, and to evaluate the bioequivalence of the two preparations after oral administration in fasting and fed state. Secondary objective: To study the safety of the test preparation trimebutine maleate tablets and the reference preparation trimebutine maleate tablets in healthy subjects.

Start Date03 Sep 2024

Sponsor / Collaborator

Zhejiang East Asia Pharmaceutical Co., Ltd.

CTR20242903

/ CompletedNot Applicable

随机、开放、单剂量、两制剂、交叉对照设计，评价中国健康受试者在空腹及餐后状态下单次口服马来酸曲美布汀片后的生物等效性正式试验

[Translation] A randomized, open-label, single-dose, two-formulation, crossover controlled study to evaluate the bioequivalence of trimebutine maleate tablets in Chinese healthy subjects after a single oral administration in the fasting and fed state

主要目的：以浙江昂利康制药股份有限公司提供的马来酸曲美布汀片为受试制剂，按生物等效性试验的有关规定，与Pfizer Holding France持证的马来酸曲美布汀片（商品名：Debridat®，参比制剂）对比在健康人体内的吸收速度及吸收程度，考察两制剂的人体生物等效性。

[Translation]

Main objective: To compare the absorption rate and extent of trimebutine maleate tablets (trade name: Debridat®, reference preparation) in healthy human bodies with trimebutine maleate tablets (trade name: Debridat®, reference preparation) provided by Zhejiang Anlikang Pharmaceutical Co., Ltd. according to the relevant provisions of bioequivalence studies, and to investigate the bioequivalence of the two preparations in humans.

Start Date03 Sep 2024

Sponsor / Collaborator

Zhejiang Anglikang Pharmaceutical Co. Ltd.

NCT06268964

/ RecruitingPhase 1/2IIT

Comparative Effect of Trimebutine and Probiotics on Functional Abdominal Pain Disorders (FAPD) in Children: Randomized Clinical Trial (RCT)

The goal of this clinical trial is to test the effectiveness of trimebutine and probiotics in treating Functional Abdominal Pain Disorders (FAPD) in a pediatric population. The main questions it aims to answer are: Is trimebutine effective in reducing the symptoms of FAPD in children? Are probiotics effective in reducing the symptoms of FAPD in children? Participants will be randomly assigned to one of three treatment groups (trimebutine/probiotics, probiotics/placebo, or trimebutine/placebo). Undergo measurements for pain and other relevant metrics at the start of the study, after 4 weeks, and after 8 weeks.
Researchers will compare the trimebutine/probiotics group to the probiotics/placebo and the trimebutine/placebo groups to see if there are significant differences in the efficacy of these treatments in reducing symptoms of FAPD in children.

Start Date01 Sep 2024

Sponsor / Collaborator

Unversity of Colima

100 Clinical Results associated with Trimebutine Maleate

100 Translational Medicine associated with Trimebutine Maleate

100 Patents (Medical) associated with Trimebutine Maleate

503

Literatures (Medical) associated with Trimebutine Maleate

01 Mar 2025·Nuclear Medicine and Biology

PET imaging of the anticancer drug candidate [11C]trimebutine in a rat glioma model

Article

Author: Lin, Jia-Zhe ; Doorduin, Janine ; Kominia, Maria ; de Vries, Erik F J

PURPOSEPreclinical studies suggest that trimebutine could be a potential treatment for glioblastoma. The aim of this study was to investigate the distribution, kinetics and tumor accumulation of [¹¹C]trimebutine.METHODA proliferation assay and cell scratch healing assay were performed to confirm the antitumor effects of trimebutine on C6 glioma cells in-vitro. Trimebutine was subsequently labeled with ¹¹C. The distribution and kinetics of [¹¹C]trimebutine in health rats and rats with an orthotopic C6 glioma were evaluated by ex-vivo gamma counting and positron emission tomography, respectively. Blocking experiments with an excess of unlabeled trimebutine or the μ-opioid receptor ligand cyprodime were employed to determine if trimebutine exhibits saturable binding in the brain. In addition, plasma stability of the tracer was assessed.RESULTSThe proliferation assay and cell scratch healing assay confirmed that trimebutine has anti-tumor effects in-vitro. [¹¹C]Trimebutine with a radiochemical purity >98 % was synthesized in 15 ± 5 % radiochemical yield. In peripheral organs, the highest accumulation of the tracer was detected in excretion organs. In the brain, the highest tracer uptake was observed in the brainstem and the lowest in the hypothalamus, although differences between regions were small. PET imaging showed rapid brain uptake of [¹¹C]trimebutine, followed by a gradual washout. Administration of an intravenous dose of trimebutine (10 mg/kg) significantly decreased the uptake in all brain regions (p < 0.05), except midbrain. Likewise, administration of cyprodime (2 mg/kg) significantly reduced [¹¹C]trimebutine uptake in the brain (p < 0.01). However, uptake of [¹¹C]trimebutine in the tumor was not significantly different from its brain uptake in rats bearing an orthotopic C6 glioma. The percentage of intact [¹¹C]trimebutine at 60 min post injection was only 1.7 ± 0.6 %.CONCLUSIONTrimebutine exhibits inhibitory effects on the growth and migration of glioma cells in a dose- and time-dependent manner. [¹¹C]Trimebutine was able to penetrate the blood-brain barrier in rats and tracer uptake could be significantly reduced by administration of a μ-opioid receptor antagonist. However, [¹¹C]trimebutine failed to selectively accumulate in orthotopic C6 glioma, which could be caused by low expression levels of the drug target in these tumors, or by fast metabolism of the tracer.

01 Feb 2025·Journal of Fish Diseases

Binding of Infectious Hypodermal and Haematopoietic Necrosis Virus‐Like Particles to Mannose Receptor Stimulates Antimicrobial Responses in Immune‐Related Tissues of Peneaus vannamei

Article

Author: Pooljun, Chettupon ; Chotwiwatthanakun, Charoonroj ; Weerachatyanukul, Wattana ; Jariyapong, Pitchanee

ABSTRACTMannose receptor (MR) is a transmembrane protein and a type of pattern‐recognition receptor (PRR) that plays a critical role in the immunity of mammals and fish. In this study, we examined the role of MR in binding with infectious hypodermal and haematopoietic necrosis virus‐like particle (IHHN‐VLP) and the downstream immune pathway that it triggers in the shrimp Peneaus vannamei. Upon IHHN‐VLP challenge, transcripts of MR in P. vannamei (PvMR) increased significantly in all examined tissues, particularly those related to shrimp immunity, including hemocyte, hepatopancreas and gill tissues. Specifically, IHHN‐VLP bound to the 34‐kDa PvMR protein in shrimp‐tissue extracts. Immunohistochemistry results of hemocytes showed that PvMR was initially localised on the plasma membrane but later internalised and dispersed throughout the cytoplasm after IHHN‐VLP administration. Binding between IHHN‐VLP and PvMR also induced significant upregulation of genes for the antimicrobial peptides (AMPs) penaeidin 3 and crustin, presumably to protect the shrimp against the viral infection. However, knocking down PvMR resulted in down‐regulation of all immune‐related genes examined. Overall, as an immune‐related PRR, PvMR serves as a receptor for invading viruses, which then trigger the expression of AMPs. Strategic designs using PvMR could be developed to either block the interaction of native virus with the host cells or provoke its up‐regulation to enhance shrimp immunity, which could open up opportunities to fight against IHHNV infection in shrimp.

01 Jan 2025·Journal of Pharmaceutical Sciences

Dissolution profiles of high-dose salt-form drugs in bicarbonate buffer and phosphate buffer

Article

Author: Tarumi, Yuki ; Sugano, Kiyohiko

The purpose of the present study was to compare the dissolution profiles of high-dose salt-form drugs in bicarbonate buffer (BCB) and phosphate buffer (PPB) focusing on the pH changes in the bulk phase. The pH titration curves of BCB and PPB (pH 6.5, buffer capacity (β) = 4.4 mmol/L/pH unit) were first theoretically calculated and experimentally validated. For dissolution tests, six drug salts with an acid counterion, one drug salt with a weak base counterion, and one free acid drug were employed (125-800 mg clinical dose). The dose/fluid volume ratio (Dose/FV) was aligned with the clinical condition. In the pH titration study, the pH value decreased below pH 6.0 by adding HCl > 2.8 mmol/L (BCB) or > 1.6 mmol/L (PPB) and increased above pH 7.0 by adding NaOH > 2.0 mmol/L (BCB) or > 2.4 mmol/L (PPB). In the dissolution test, even though the initial pH and β values were the same, the pH value at 4 h was lower in PPB than in BCB in all cases. For the drug salts with an acid counterion, the area under the dissolution curve was 1.2 to 2.6-fold lower in BCB than in PPB. A marked precipitation process was observed in BCB, but less pronounced or absent in PPB. The results of this study suggest the use of BCB and a clinically equivalent Dose/FV may be valuable in predicting the oral absorption of high-dose drug salts.

100 Deals associated with Trimebutine Maleate

External Link

KEGG	Wiki	ATC	Drug Bank
D01500	Trimebutine Maleate	A03AA05	DB09089

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Gastrointestinal Diseases	China	Xinhe Yuansheng Pharmaceutical Co., Ltd.	01 Jan 2000
Gastritis	Japan	-	15 Feb 1984
Irritable Bowel Syndrome	Japan	-	15 Feb 1984

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Irritable Bowel Syndrome	Preclinical	Canada	Labopharm, Inc.	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WJOG11318B (ESMO2021)	Phase 2	Hormone receptor positive HER2 negative breast cancer estrogen receptor-positive \| HER2-negative	-	Bifidobacterial	xqbysbgpkt(wauhgunhna) = nnjrasgajk wmuvfyrbty (bhxbanqfnx ) View more	-	16 Sep 2021
				Bifidobacterial and Trimebutine Maleate	xqbysbgpkt(wauhgunhna) = nsfppbjuzr wmuvfyrbty (bhxbanqfnx ) View more

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