Delving into the Latest Updates on Rebamipide with Synapse

主要研究目的：研究空腹和餐后状态下单次口服受试制剂瑞巴派特片（规格：0.1g，浙江浙北药业有限公司生产）与参比制剂瑞巴派特片（Mucosta®，规格：0.1g，大塚制药株式会社生产）在健康成年受试者体内的药代动力学，评价空腹和餐后状态口服两种制剂的生物等效性。次要研究目的：评价健康受试者在空腹和餐后状态下，单次口服瑞巴派特片受试制剂和参比制剂后的安全性。

[Translation]

Main research purpose: To study the single oral administration of the test preparation Rebamipide Tablets (specification: 0.1g, produced by Zhejiang Zhebei Pharmaceutical Co., Ltd.) and the reference preparation Rebamipide Tablets (Mucosta®, Specification: 0.1g, produced by Otsuka Pharmaceutical Co., Ltd.) in healthy adult subjects to evaluate the bioequivalence of the two oral preparations in fasting and postprandial states. Secondary study purpose: To evaluate the safety of healthy subjects after a single oral administration of the test preparation and reference preparation of rebamipide tablets in fasting and postprandial states.

Start Date04 Dec 2024

Sponsor / Collaborator

Zhejiang Zhebei Pharmaceutical Co. Ltd.

CTR20242604

/ CompletedNot Applicable

瑞巴派特片采用单中心、随机、开放、单剂量、两制剂、两周期、两序列交叉设计，分为空腹给药和餐后给药的人体生物等效性研究。

[Translation] Rebamipide tablets were studied in a single-center, randomized, open-label, single-dose, two-formulation, two-period, two-sequence crossover design, divided into a human bioequivalence study with fasting administration and postprandial administration.

本试验旨在研究单次空腹和餐后口服安徽省先锋制药有限公司研制、生产的瑞巴派特片（100 mg）的药代动力学特征；以大塚製薬株式会社生产的瑞巴派特片（Mucosta®，100 mg）为参比制剂，比较两制剂中药动学参数Cmax、AUC0-t、AUC0-∞，评价两制剂的人体生物等效性。

[Translation]

This trial aims to study the pharmacokinetic characteristics of rebamipide tablets (100 mg) developed and produced by Anhui Pioneer Pharmaceutical Co., Ltd. after a single fasting and postprandial oral administration; The special tablet (Mucosta®, 100 mg) is the reference preparation. The pharmacokinetic parameters Cmax, AUC0-t, and AUC0-∞ of the two preparations are compared to evaluate the human bioequivalence of the two preparations.

Start Date14 Aug 2024

Sponsor / Collaborator

Anhui Pioneer Pharmaceutical Co. Ltd.

CTR20240809

/ CompletedNot Applicable

健康受试者单次口服瑞巴派特片的随机、开放、两周期、两序列、双交叉，空腹和高脂餐后给药条件下的人体生物等效性试验。

[Translation] A randomized, open-label, two-period, two-sequence, double-crossover bioequivalence study of a single oral dose of rebamipide tablets in healthy subjects under fasting and high-fat meal administration conditions.

主要目的：以药代动力学参数为终点指标，比较空腹和高脂餐后给药条件下，安徽金太阳生化药业有限公司生产的瑞巴派特片与OTSUKA PHARMACEUTICAL Co.,Ltd.（大塚制薬株式会社）原研的瑞巴派特片在健康成年人群中吸收程度和速度的差异，对两制剂的生物等效性进行评价。次要目的：评价空腹和高脂餐后给药条件下，安徽金太阳生化药业有限公司生产的瑞巴派特片在健康成年人群中的安全性。

[Translation]

Main purpose: Using pharmacokinetic parameters as endpoints, compare rebamipide tablets produced by Anhui Golden Sun Biochemical Pharmaceutical Co., Ltd. and OTSUKA PHARMACEUTICAL Co., Ltd. under fasting and high-fat postprandial administration conditions. The bioequivalence of the two preparations was evaluated based on the differences in the degree and rate of absorption of rebamipide tablets originally developed by Tsuka Seiki Co., Ltd. in healthy adults. Secondary purpose: To evaluate the safety of rebamipide tablets produced by Anhui Golden Sun Biochemical Pharmaceutical Co., Ltd. in healthy adults under fasting and high-fat meal administration conditions.

Start Date13 Mar 2024

Sponsor / Collaborator

Anhui Golden Sun Biochemical Pharmaceutical Co. Ltd.

100 Clinical Results associated with Rebamipide

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100 Translational Medicine associated with Rebamipide

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100 Patents (Medical) associated with Rebamipide

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952

Literatures (Medical) associated with Rebamipide

01 Jan 2025·European Journal of Pharmaceutics and Biopharmaceutics

Preparation and characterization of the ground mixture of rebamipide commercial tablets and Hydroxypropyl Cellulose-SSL by ball-milling: Application to the dispersoid of mouthwash suspension

Article

Author: Mizobuchi, Senri ; Hirose, Kaoru ; Ishii, Naoko ; Hanawa, Takehisa ; Kawano, Yayoi

In the present study, to prepare dispersoids with high dispersion stability that can be used as mouthwash, ground mixtures of commercial rebamipide (RB) tablets and hydroxypropyl cellulose (HPC-SSL) samples were prepared by dry milling. The physicochemical properties of the ground mixture of HPC-SSL and the powder obtained from the preliminary ground RB tablets were then compared. The dispersoids' physicochemical properties, dispersion stability, retention, and diffusiveness to the mucosal surfaces were evaluated in vitro. By co-grinding with HPC-SSL, RB transformed into fine particles around 303.6 - 361.5 nm that tended to prevent particle agglomeration in solution over time. The sample microparticles formed with HPC-SSL also avoided agglomeration on the mucosal surface for 24 h, improving oral retention. Furthermore, the ground mixture of HPC-SSL and the powder obtained from the preliminary ground RB tablets dispersed and permeated the mucus gel layer on the mucosal surface (24.2 %) but not the mucosal cells, indicating that RB remained on the mucosal surface. These results suggest that ground mixtures of commercial rebamipide (RB) tablets and hydroxypropyl cellulose (HPC-SSL) samples can be applied as a powdered suspension preparation because they showed high dispersion stability and oral mucosal retention.

01 Dec 2024·Pharmacological Research

Antagonising Yin Yang 1 ameliorates the symptoms of lupus nephritis via modulating T lymphocyte signaling

Article

Author: Zhang, Meilian ; Yuan, Haoxing ; Liu, Shuwen ; Li, Honglian ; Lu, Kunyu ; Yang, Chan ; Li, Minmin ; Peng, Zheng

Lupus nephritis (LN) is a chronic complication of systemic lupus erythematosus (SLE). At present, no drugs are capable of delaying the progression of LN without a risk of serious side effects. There is thus a pressing need for further studies of LN pathogenesis to identify novel therapeutic targets and aid in the development of new approaches to treating this debilitating disease. In this study, a multi-omics approach was used to characterize the pathogenesis of LN and to identify disease-related targets, ultimately leading to the identification and validation of Yin Yang 1 (YY1) as a promising therapeutic target in LN. A rapid approach to efficiently screening for candidate YY1 ligands was implemented using drug databases that established rebamipide as a YY1 antagonist suitable for use in the management of LN. Specifically, the YY1 antagonist activity of rebamipide was found to regulate lymphocyte activity, reduce autoantibody production, limit immune complex deposition, and suppress macrophage activation while improving symptoms in a murine model of LN. Results supportive of a similar pathologic mechanism of action were also obtained when analyzing renal tissue sections from LN patients, underscoring the potential clinical significance of YY1 and its antagonist rebamipide, suggesting that rebamipide may have positive effects on lymphocytes and may improve symptoms in treated patients. This study provides a robust foundation for further research focused on the pathogenesis and treatment of LN.

01 Dec 2024·International Journal of Pharmaceutics

Coamorphous systems of rebamipide: Selection of amino acid coformers based on protein-ligand docking, in vitro assessment and study of interactions by computational and multivariate analysis

Article

Author: Sharma, Abhishek ; Shah, Saurabh ; Sapkal, Rekha ; Srivastava, Saurabh ; Dey, Soumyajit ; Naga Sidhartha, Nagamalli ; Dikundwar, Amol G

Three coamorphous systems of Rebamipide (REB) with the amino acids namely, Tryptophan (TRP), Phenylalanine (PHE) and Arginine (ARG) are reported. A unique approach for the virtual screening of amino acid coformers is presented by employing molecular docking studies based on interactions of the drug molecule with various amino acid fragments in the drug-receptor cocrystal structure. Successful formation of stable coamorphous systems with ARG, TRP and PHE served as the proof-of-concept along with negative benchmarking standards Histidine and Aspartic acid, wherein coamorphous systems could not be obtained despite multiple trials which resulted in crystalline physical mixtures. The coamorphous systems were characterized by a halo pattern in Powder XRD and a single glass transition temperature (Tg) in modulated DSC. Physical stability assessments of the coamorphous systems showed direct correlation of Tg with the observed stability of the amorphous phase which was found in the order ARGREB > TRPREB ≥ PHEREB. To determine the specific functional groups engaged in the interactions, multivariate analysis was performed on the FTIR spectra. These interactions were further validated by DFT and QTAIM analysis, which revealed key noncovalent interactions in the three coamorphous systems. All three coamorphous systems showed excellent release profiles of the API as demonstrated by the f2 and DE parameters in the order ARGREB ≥ TRPREB > PHEREB ≥ amorphous drug, far exceeding that of the crystalline drug. The interplay of multivariate analysis and QTAIM can be useful in estimating the interactions within the coamorphous systems which can further contribute to stability and physicochemical properties of the systems.

100 Deals associated with Rebamipide

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External Link

KEGG	Wiki	ATC	Drug Bank
D01121	Rebamipide	A02BX14	DB11656

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Gastritis	Japan	Otsuka Holdings Co., Ltd.	01 Jun 1994
Stomach Ulcer	Japan	Otsuka Holdings Co., Ltd.	28 Sep 1990

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Dry Eye Syndromes	NDA/BLA	South Korea	SAMIL PHARMACEUTICAL Co., Ltd.	-
Acute gastritis	Phase 1	South Korea	Korea Otsuka Pharmaceutical Co., Ltd.	30 Dec 2019
Ankylosing Spondylitis	Phase 1	South Korea	Korea Otsuka Pharmaceutical Co., Ltd.	01 Dec 2007
Osteoarthritis	Phase 1	South Korea	Korea Otsuka Pharmaceutical Co., Ltd.	01 Dec 2007
Rheumatoid Arthritis	Phase 1	South Korea	Korea Otsuka Pharmaceutical Co., Ltd.	01 Dec 2007
Toxicity	Phase 1	South Korea	Korea Otsuka Pharmaceutical Co., Ltd.	01 Dec 2007
Chronic gastritis	Phase 1	Indonesia	PT Otsuka Indonesia	01 Oct 2007
Dyspepsia	Phase 1	Indonesia	PT Otsuka Indonesia	01 Oct 2007
Sjogren's Syndrome	Phase 1	Japan	Otsuka Pharmaceutical Co., Ltd.	15 Apr 2005
Kerato conjunctivitis sicca	Phase 1	United States	Otsuka Pharmaceutical Development & Commercialization, Inc.	01 May 2004

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AAAAI2024	Not Applicable	Post Acute COVID 19 Syndrome CRP	62	Rebamipide 100 mg + Omeprazole 20 mg	myopghqvdm(glgrdmfzlk) = wwjkmzpjep qqqpatjikk (ggxlxskegx, [1.85 - 2.62])	Positive	23 Feb 2024
				Omeprazole 20 mg	myopghqvdm(glgrdmfzlk) = rekkzlnllc qqqpatjikk (ggxlxskegx, [2.68 - 3.9])
NCT00463151 (CTgov)	Phase 2	Colitis, Ulcerative	124	Rebamipide (Rebamipide 60 mg)	kxbvwbzzvz(sdahptvgfl) = smphlryyzg gqxmsjoegp (sozyevvurf, pgmfymlpox - nsffeglrmu) View more	-	20 Jul 2021
				Rebamipide (Rebamipide 150 mg)	kxbvwbzzvz(sdahptvgfl) = ehlaiqepre gqxmsjoegp (sozyevvurf, nvuwwzabqj - iohvgldeyj) View more
NCT01471093 (CTgov)	Phase 1	Dry Eye Syndromes	100	OPC-12759 (OPC-12759 Solution With Nasal Root Pressed/Not Pressed)	hrbvaapkkb(ddsukqxzsf) = vntolcmeyd kjfapwbhmd (hxpycjngqk, dxtminjoml - vferpleuun) View more	-	29 Jun 2021
				OPC-12759 (OPC-12759 Suspension With Nasal Root Pressed/Not Pressed)	hrbvaapkkb(ddsukqxzsf) = canyriytpb kjfapwbhmd (hxpycjngqk, numzltwpna - mpmlfsmdfl) View more
NCT01660256 (CTgov)	Phase 3	Dry Eye Syndromes	209	Placebo	sbtuglayoh(hkuggsaqyp) = wehkubpith bjfrhwmrko (rlvdrctumx, xadrcrxkus - xkugkrwkxh) View more	-	05 May 2021
NCT02085460 (CTgov)	Phase 2	radiation oral mucositis \| Head and Neck Neoplasms	94	2% Rebamipide liquid (2% Rebamipide Liquid)	rezcivxfpj(fwaskhtkas) = bxivzmwaez fikfjwyybv (zafydnlzkv, rgarezwiep - bneqlkjvvq) View more	-	06 Apr 2021
				4% Rebamipide liquid (4% Rebamipide Liquid)	rezcivxfpj(fwaskhtkas) = dxmdlnmoir fikfjwyybv (zafydnlzkv, bbtmazusua - yhjnxyeitm) View more
UEGW2018	Not Applicable	Esophagitis	-	PPI+rebamipide	(tjesdjkazw) = qkqeunmhxp ogwdlmvgtz (aeuynhcdkt ) View more	-	01 Oct 2018
				PPI	(tjesdjkazw) = nzvclganbz ogwdlmvgtz (aeuynhcdkt ) View more
UEGW2017	Not Applicable	Gastroesophageal Reflux Adjuvant IL-8 \| PAF	109	Lansoprazole	jmwqacgbgi(mxwhrznhyf) = ympmadqzfy pamukydhgx (duldjlxure )	Negative	01 Oct 2017
				Lansoprazole+Rebamipide	jmwqacgbgi(mxwhrznhyf) = mvoxpffgdm pamukydhgx (duldjlxure )
NCT01493180 (CTgov)	Phase 2	Corneal epithelial defect	102	OPC-12759 ophthalmic suspension (OPC-12759 Ophthalmic Suspension)	dlribynwwe(jfymdpflmw) = rynyagiago kygqnjnpyn (zzkqsovnzl, bpzjkwkxra - byutylnjsb) View more	-	03 Mar 2014
				Sodium hyaluronate ophthalmic solution (Sodium Hyaluronate Ophthalmic Solution)	dlribynwwe(jfymdpflmw) = iinhazyvpq kygqnjnpyn (zzkqsovnzl, lldwmgibeb - tbhmktiyoy) View more
NCT00234078 (CTgov)	Phase 2	Dry Eye Syndromes	290	0.5% OPC-12759 (0.5% OPC-12759)	aqrvtwvktr(gmtiozejfj) = bnltivhuyr mebyhnzkir (uowksufuqp, fnnlhjisij - wzeovlfibe) View more	-	28 Feb 2014
				1% OPC-12759 (1% OPC-12759)	aqrvtwvktr(gmtiozejfj) = ieoovyewiz mebyhnzkir (uowksufuqp, rmgovhqjzw - cmultrtmat) View more
NCT00818324 (CTgov)	Phase 3	Dry Eye Syndromes	154	rebamipide	zcumhbbufg(iwtiofuyhn) = ygggmauagx nhvsealhgd (qgjnvgqasi, yrdwwobmgm - uagezcydtn) View more	-	26 Feb 2014