Delving into the Latest Updates on Linagliptin/Metformin Hydrochloride with Synapse

本研究考察健康受试者在空腹及餐后条件下，单次口服由宁波美诺华天康药业有限公司生产，宁波科尔康美诺华药业有限公司提供的利格列汀二甲双胍片(Ⅱ)（受试制剂，规格：2.5 mg/850 mg）或由 Boehringer Ingelheim (Schweiz) GmbH 持证的利格列汀二甲双胍片(Ⅱ)（参比制剂，商品名：欧双宁®，规格：2.5 mg/850 mg）的药动学特征，评价两制剂的生物等效性及安全性，为该受试制剂注册申请提供依据。

[Translation]

This study investigated the pharmacokinetic characteristics of a single oral dose of linagliptin metformin tablets (II) (test preparation, strength: 2.5 mg/850 mg) produced by Ningbo Menopause Tiankang Pharmaceutical Co., Ltd. and provided by Ningbo Keerkang Menopause Pharmaceutical Co., Ltd. or linagliptin metformin tablets (II) (reference preparation, trade name: Oushuangning®, strength: 2.5 mg/850 mg) certified by Boehringer Ingelheim (Schweiz) GmbH in healthy subjects under fasting and postprandial conditions, evaluated the bioequivalence and safety of the two preparations, and provided a basis for the registration application of the test preparation.

Start Date17 Aug 2024

Sponsor / Collaborator

Ningbo Krka Menovo Pharmaceutical Co., Ltd.

CTR20240895 / CompletedNot Applicable

利格列汀二甲双胍片（II）健康人体生物等效性研究

[Translation] Bioequivalence study of linagliptin and metformin tablets (II) in healthy volunteers

主要目的：本研究以华润赛科药业有限责任公司研发的利格列汀二甲双胍片（II）（规格：2.5 mg/850 mg）为受试制剂，按生物等效性研究的有关规定，以原研厂家Boehringer Ingelheim Pharma GmbH & Co. KG生产的利格列汀二甲双胍片（II）（规格：2.5 mg/850 mg，商品名：欧双宁®）为参比制剂，评估受试制剂和参比制剂在空腹/餐后条件下给药后的生物等效性。次要目的：观察受试制剂利格列汀二甲双胍片（II）和参比制剂利格列汀二甲双胍片（II）（欧双宁®）在健康受试者中的安全性。

[Translation]

Main purpose: This study used Linagliptin Metformin Tablets (II) (Specification: 2.5 mg/850 mg) developed by China Resources Saike Pharmaceuticals Co., Ltd. as the test preparation. According to the relevant regulations of bioequivalence studies, Linagliptin Metformin Tablets (II) (Specification: 2.5 mg/850 mg, trade name: Oushuangning®) produced by the original manufacturer Boehringer Ingelheim Pharma GmbH & Co. KG was used as the reference preparation to evaluate the bioequivalence of the test preparation and the reference preparation after administration under fasting/postprandial conditions. Secondary purpose: Observe the safety of the test preparation Linagliptin Metformin Tablets (II) and the reference preparation Linagliptin Metformin Tablets (II) (Oushuangning®) in healthy subjects.

Start Date07 Apr 2024

Sponsor / Collaborator

China Resources Saike Pharmaceutical Co., Ltd.

CTR20240327 / CompletedNot Applicable

利格列汀二甲双胍片（II）在中国成年健康受试者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、两周期交叉的生物等效性研究

[Translation] A single-center, randomized, open-label, fasting and fed single-dose, two-formulation, two-sequence, two-period crossover bioequivalence study of linagliptin and metformin tablets (II) in healthy Chinese adult subjects

主要目的：考察单次单剂量口服1片（空腹/餐后）受试制剂利格列汀二甲双胍片（II）（规格：每片含利格列汀2.5 mg与盐酸二甲双胍850 mg）与参比制剂利格列汀二甲双胍片（II）（商品名：Trajenta Duo®，规格：每片含利格列汀2.5 mg与盐酸二甲双胍850 mg）在中国成年健康受试者体内的相对生物利用度，分析两种制剂的药代动力学参数，评价两制剂的生物等效性。次要目的：评价单次单剂量口服1片受试制剂和参比制剂（空腹/餐后）在中国健康受试者中的安全性。

[Translation]

Primary objective: To investigate the relative bioavailability of the test preparation Linagliptin Metformin Tablets (II) (Specification: each tablet contains 2.5 mg Linagliptin and 850 mg Metformin Hydrochloride) and the reference preparation Linagliptin Metformin Tablets (II) (Trade name: Trajenta Duo®, Specification: each tablet contains 2.5 mg Linagliptin and 850 mg Metformin Hydrochloride) in healthy adult Chinese subjects, analyze the pharmacokinetic parameters of the two preparations, and evaluate the bioequivalence of the two preparations. Secondary objective: To evaluate the safety of the test preparation and the reference preparation (fasting/after meal) in healthy Chinese subjects after a single oral dose of 1 tablet.

Start Date04 Mar 2024

Sponsor / Collaborator

Anhui Jiahe Pharmaceutical Co., Ltd.Startup

100 Clinical Results associated with Linagliptin/Metformin Hydrochloride

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100 Translational Medicine associated with Linagliptin/Metformin Hydrochloride

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100 Patents (Medical) associated with Linagliptin/Metformin Hydrochloride

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8

Literatures (Medical) associated with Linagliptin/Metformin Hydrochloride

01 Jan 2019·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

A validated LC-MS/MS method for simultaneous determination of linagliptin and metformin in spiked human plasma coupled with solid phase extraction: Application to a pharmacokinetic study in healthy volunteers

Q3 · MEDICINE

Article

Author: Mahrouse, Marianne Alphonse ; Fawzy, Michael Gamal ; Abbas Moussa, Bahia

Combination therapy has a pivotal role in type II diabetes mellitus management in patients unable to maintain normal glycemic level using metformin alone. Addition of linagliptin, dipeptidyl peptidase-IV inhibitor, to metformin improves glycemic control. This study is concerned with the development of an HPLC-MS/MS method for simultaneous quantification of linagliptin and metformin in spiked human plasma. The method was applied to evaluate the potential pharmacokinetic interactions between the cited drugs in healthy volunteers. Solid phase extraction was applied using Strata™ X cartridge. Separation was carried out on Symmetry^® C₁₈ column using methanol: 10 mM ammonium formate buffer (containing 0.2% formic acid) in a ratio of (95: 5, v/v) as mobile phase at flow rate 0.25 mL min^-1. Quantification was performed with multiple reaction monitoring in positive ionization mode. The monitored transitions were set at m/z 473.24 → 419.94, 130.14 → 60.18 and 340.27 → 116.07 for linagliptin, metformin and alogliptin (internal standard), respectively. The method was validated according to FDA guidelines. The method showed excellent linearity over concentration ranges 0.25-10 and 25-2000 ng mL^-1 for linagliptin and metformin, respectively. The validated HPLC-MS/MS method was successfully applied to pharmacokinetic study of linagliptin and metformin in healthy volunteers after oral administration of Jentadueto^® tablets.

01 Aug 2016·The Medical letter on drugs and therapeuticsQ4 · MEDICINE

Jentadueto XR for type 2 diabetes.

Q4 · MEDICINE

Article

01 Oct 2014·DrugsQ1 · MEDICINE

Linagliptin: An Update of Its Use in Patients with Type 2 Diabetes Mellitus

Q1 · MEDICINE

Review

Author: McKeage, Kate

Linagliptin (Trajenta(®), Tradjenta(®)) is a dipeptidyl peptidase (DPP)-4 inhibitor approved for the treatment of adults with type 2 diabetes mellitus in several countries. A fixed-dose combination of linagliptin/metformin (Jentadueto(®)) is also available. This article reviews the pharmacology, therapeutic efficacy and tolerability of linagliptin in the management of type 2 diabetes, with the aim of updating its place in therapy based on recently published data. In randomized, controlled trials, oral linagliptin 5 mg once daily (or 2.5 mg twice daily when combined with metformin) improved glycaemic control when used alone or in combination with other antidiabetic agents, including metformin, a sulfonylurea, thiazolidinedione or insulin. Improvements in glycaemic control were also shown in patients with renal impairment, including severe impairment, and the elderly (aged ≥70 years). Linagliptin is the first DPP-4 inhibitor to be eliminated primarily via a nonrenal route, enabling its use without dosage adjustment in patients with any degree of renal impairment. Linagliptin is generally well tolerated and, as with other DPP-4 inhibitors, it is associated with a low risk of hypoglycaemia and has no effect on bodyweight. Some data indicate that linagliptin may have beneficial effects on cardiovascular and renal safety profiles in patients with type 2 diabetes, but more data are needed. Meanwhile, the low risk of hypoglycaemia and the nonrenal route of elimination may provide important advantages for some patient groups, including elderly or renally impaired patients.

100 Deals associated with Linagliptin/Metformin Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	US	Boehringer Ingelheim Pharmaceuticals, Inc.	30 Jan 2012

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 3	MY	Boehringer Ingelheim International GmbH	15 Oct 2012
Diabetes Mellitus, Type 2	Phase 3	VN	Boehringer Ingelheim Pharma GmbH & Co., KG	15 Oct 2012
Diabetes Mellitus, Type 2	Phase 3	PH	Boehringer Ingelheim Pharma GmbH & Co., KG	15 Oct 2012
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 3	CN	Boehringer Ingelheim GmbH	01 Oct 2012
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 3	PH	Boehringer Ingelheim GmbH	01 Oct 2012
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 3	MY	Boehringer Ingelheim GmbH	01 Oct 2012
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 3	VN	Boehringer Ingelheim GmbH	01 Oct 2012
Diabetes Mellitus, Type 2	Discovery	MY	Boehringer Ingelheim Pharma GmbH & Co., KG	15 Oct 2012
Diabetes Mellitus, Type 2	Discovery	VN	Boehringer Ingelheim International GmbH	15 Oct 2012
Diabetes Mellitus, Type 2	Discovery	PH	Boehringer Ingelheim International GmbH	15 Oct 2012

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Clinical Result

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Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ADA2023	Not Applicable	Prediabetic State	658	Metformin monotherapy	(contjvlxns) = xosbnrnycg nxmgnvpipf (phxyxirfam ) View more	-	20 Jun 2023
				Linagliptin monotherapy	eddrwxgcmq(lvcgrleulx) = iqdcmdzqkn eymzwjeqbh (sveyhcncvz )
EASD2018	Not Applicable	Prediabetic State	-	Linagliptin 2.5mg/metformin 850mg	plsodzdooy(wydyvvxclc) = ieigpjxltn eiienvgjnx (dnehgblgeh ) View more	Positive	04 Oct 2018
				Metformin 850mg	plsodzdooy(wydyvvxclc) = ehlefazbfq eiienvgjnx (dnehgblgeh ) View more
NCT01708902 (EASD2015)	Phase 3	Diabetes Mellitus, Type 2	733	Linagliptin 5 mg QD	eugasuyntm(rgbvwqxwjt) = low across groups itsiijrnlx (umwadrosto ) View more	Positive	17 Sep 2015
				Metformin 500 mg BID
NCT00993187 (CTgov)	Phase 4	Diabetes Mellitus, Type 2	292	Matching placebo to Sitagliptin/Metformin FDC	sxghpemcse(dcdalupfhp) = zvopvaupyw lalbgmqays (thwarkoowk, gnrshytjxy - zkhdtoegmx) View more	-	15 Sep 2014