Delving into the Latest Updates on Drotaverine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Drotaverin, Drotaverine, Deolin

+ [1]

Target

PDE4

Mechanism

PDE4 inhibitors(Phosphodieterase 4 inhibitors)

Therapeutic Areas

Nervous System DiseasesSkin and Musculoskeletal Diseases

Active Indication

Muscle Spasticity

Inactive Indication-

Originator Organization

CHINOIN Pharmaceutical Co.

Active Organization

CHINOIN Pharmaceutical Co.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC24H32ClNO4

InChIKeyJBFLYOLJRKJYNV-UHFFFAOYSA-N

CAS Registry985-12-6

View All Structures (2)

主要研究目的：按有关生物等效性试验的规定，选择Opella Healthcare为持证商的盐酸屈他维林片（商品名：NO-SPA；规格：40mg）为参比制剂，对石家庄四药有限公司生产并提供的受试制剂盐酸屈他维林片（规格：40mg）进行空腹和餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在空腹和餐后给药条件下的生物等效性。次要研究目的：观察健康志愿受试者口服受试制剂盐酸屈他维林片（规格：40mg）和参比制剂盐酸屈他维林片（商品名：NO-SPA；规格：40mg）的安全性。

[Translation]

The main purpose of the study: According to the relevant provisions of the bioequivalence test, Opella Healthcare was selected as the reference preparation for the drotaverine hydrochloride tablets (trade name: NO-SPA; specification: 40 mg), and the test preparation drotaverine hydrochloride tablets (specification: 40 mg) produced and provided by Shijiazhuang Siyao Co., Ltd. was used for the human bioequivalence test of fasting and postprandial administration. The absorption rate and degree of the drug in the test preparation were compared with the reference preparation to see whether they were within the acceptable range, and to evaluate the bioequivalence of the two preparations under fasting and postprandial administration conditions. The secondary purpose of the study: To observe the safety of oral administration of the test preparation drotaverine hydrochloride tablets (specification: 40 mg) and the reference preparation drotaverine hydrochloride tablets (trade name: NO-SPA; specification: 40 mg) to healthy volunteers.

Start Date03 Dec 2023

Sponsor / Collaborator

Shijiazhuang No. 4 Pharmaceutical Co., Ltd.

CTR20232627

/ CompletedNot Applicable

盐酸屈他维林片生物等效性试验

[Translation] Bioequivalence study of drotaverine hydrochloride tablets

主要研究目的评价中国健康成年受试者空腹及餐后条件下单次单剂量口服江西亿友药业有限公司生产的盐酸屈他维林片（受试制剂，规格：40mg）和Opella Healthcare France SAS持证的盐酸屈他维林片（参比制剂，商品名：NO-SPA®，规格：40mg）后的药代动力学特点和生物等效性。次要研究目的研究盐酸屈他维林片的受试制剂（规格：40mg）和参比制剂（NO-SPA®，规格：40mg）在中国健康成年受试者中的安全性。

[Translation]

Main study objectives To evaluate the pharmacokinetic characteristics and bioequivalence of single oral doses of drotaverine hydrochloride tablets (test preparation, specification: 40 mg) produced by Jiangxi Yiyou Pharmaceutical Co., Ltd. and drotaverine hydrochloride tablets (reference preparation, trade name: NO-SPA®, specification: 40 mg) certified by Opella Healthcare France SAS in healthy Chinese adult subjects under fasting and postprandial conditions. Secondary study objectives To study the safety of the test preparation (specification: 40 mg) and reference preparation (NO-SPA®, specification: 40 mg) of drotaverine hydrochloride tablets in healthy Chinese adult subjects.

Start Date28 Aug 2023

Sponsor / Collaborator

Jiangxi Yiyou Pharmaceutical Co., Ltd.

100 Clinical Results associated with Drotaverine Hydrochloride

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100 Translational Medicine associated with Drotaverine Hydrochloride

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100 Patents (Medical) associated with Drotaverine Hydrochloride

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129

Literatures (Medical) associated with Drotaverine Hydrochloride

01 Nov 2024·Journal of Fluorescence

Spectrofluorimetric Protocol for Estimation of Commonly Used Antispasmodic Drotaverine. Fluorescence Quenching Study

Article

Author: Mahmoud, Nihad A ; Attia, Tamer Z ; Derayea, Sayed M ; Noureldeen, Deena A M

AbstractA fast, simple, accurate, precise, and cheap fluorimetric protocol has been proposed for analysis of a phosphodiesterase-IV inhibitor, namely drotaverine hydrochloride. Fluorimetric protocol is based on estimating the decrease in the eosin Y fluorescence intensity by quantitative addition of drotaverine at pH 3.1 (acetate buffer). An ion pair complex is formed, which leads to quenching in the fluorescence intensity of the dye without need of prior extraction at 534 nm (λex. 339 nm). Different reaction perimeters which influence the production of complex (ion pair between drotaverine and eosin) were deeply investigated and optimized. The developed fluorimetric protocol is capable for quantitative estimation of drotaverine in linear range of 0.4 to 2.5 µg mL−1. After method validation in respect to ICH guidelines, it was applied to determine drotaverine in its commercial preparation. By comparing with other reported method, the developed and validated fluorimetric protocol is capable for estimation of drotaverine in commercial preparation with good accuracy and excellent precision.

12 Dec 2023·Expert Opinion on Pharmacotherapy

Pharmacotherapy for gastric and intestinal cramping pain: ‎ current and emerging therapies

Review

Author: Nikfar, Shekoufeh ; Abdollahi, Mohammad ; Mousavi, Taraneh ; Sharifnia, Mohammadhossein

INTRODUCTIONAcute gastrointestinal cramping pain (GICP) is a debilitating condition that affects many people worldwide, significantly reducing their quality of life. As such, prompt treatment is crucial.AREAS COVEREDThis article will explore relevant literature from databases such as PubMed, Scopus, Google Scholar, Cochrane Library, and Web of Science. Additionally, we searched ClinicalTrials.gov and the WHO ICTRP database for the latest clinical trials.EXPERT OPINIONConsensus dictates that antispasmodics such as hyoscine-N-butyl bromide and mebeverine should be the primary treatment for GICP. If these prove ineffective, patients can switch to an antispasmodic with a different mode of action or add acetaminophen/NSAIDs for more severe cases. Currently, several antispasmodics are undergoing clinical trials, including drotaverine, alverine, pinaverium, otilonium bromide, fenoverine, tiropramide, otilonium bromide, trimebutine, and peppermint oil. Well-designed head-to-head studies are necessary to evaluate current antispasmodics' safety, efficacy, pharmacokinetic, and pharmacoeconomics profiles. Recent studies have shown that fixed-dose combinations of antispasmodics + NSAIDs or two different antispasmodics can improve patient compliance and synergistically reduce GICP. Therefore, it is recommended that the global availability and accessibility of these products be enhanced.

01 Sep 2023·Journal of AOAC International

Computer-Aided Design of Eco-Friendly Imprinted Polymer Decorated Sensors Augmented by Self-Validated Ensemble Modeling Designs for the Quantitation of Drotaverine Hydrochloride in Dosage Form and Human Plasma.

Article

Author: Elsonbaty, Ahmed ; E Mostafa, Aziza ; Eissa, Maya S ; A Abdel Salam, Randa ; Attala, Khaled ; M Hadad, Ghada ; Abdelshakour, Mohamed A

BACKGROUNDComputationally designed molecular imprinted polymer (MIP) incorporation into electrochemical sensors has many advantages to the performance of the designed sensors. The innovative self-validated ensemble modeling (SVEM) approach is a smart machine learning-based (ML) technique that enables the design of more accurate predictive models using smaller data sets.OBJECTIVEThe novel SVEM experimental design methodology is exploited here exclusively to optimize the composition of four eco-friendly PVC membranes augmented by a computationally designed magnetic molecularly imprinted polymer to quantitatively determine drotaverine hydrochloride (DVN) in its combined dosage form and human plasma. Furthermore, the application of hybrid computational simulations such as molecular dynamics and quantum mechanical calculations (MD/QM) is a time-saving and eco-friendly provider for the tailored design of the MIP particles.METHODHere, for the first time, the predictive power of ML is assembled with computational simulations to develop four PVC-based sensors decorated by computationally designed MIP particles using four different experimental designs known as central composite, SVEM-LASSO, SVEM-FWD, and SVEM-PFWD. The pioneering AGREE approach further assessed the greenness of the analytical methods, proving their eco-friendliness.RESULTSThe proposed sensors showed decent Nernstian responses toward DVN in the range of 58.60-59.09 mV/decade with a linear quantitative range of 1 × 10-7 - 1 × 10-2 M and limits of detection in the range of 9.55 × 10-8 to 7.08 × 10-8 M. Moreover, the proposed sensors showed ultimate eco-friendliness and selectivity for their target in its combined dosage form and spiked human plasma.CONCLUSIONSThe proposed sensors were validated in accordance with International Union of Pure and Applied Chemistry (IUPAC) recommendations, proving their sensitivity and selectivity for drotaverine determination in dosage form and human plasma.HIGHLIGHTSThis work presents the first ever application of both the innovative SVEM designs and MD/QM simulations in the optimization and fabrication of drotaverine-sensitive and selective MIP-decorated PVC sensors.

100 Deals associated with Drotaverine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Drotaverine Hydrochloride	A03AD02	DB06751

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Muscle Spasticity	CN	CHINOIN Pharmaceutical Co.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WCLC2013	Not Applicable	Advanced Lung Adenocarcinoma	558	Gefitinib treatment	(jqbgzzewly) = eguawhlcdr mhdorafxjg (rektgqedwb )	Positive	30 Oct 2013
				No Gefitinib treatment	(jqbgzzewly) = wsdwbjwdhn mhdorafxjg (rektgqedwb )
NCT00731198 (CTgov)	Phase 3	Pancreatic Diseases \| Bile Duct Diseases	650	Drotaverine hydrochloride (Experimental)	onfucapetu(evfrkyjcnx) = xbqjgzeqxs phllnbjfwa (woasxggghd, irymocjpeu - wspsfjzzsr) View more	-	23 Dec 2009
				Hyoscine-N-butylbromide (Active Comparator)	onfucapetu(evfrkyjcnx) = tzpgzphtfw phllnbjfwa (woasxggghd, efrxzzerwy - rdonmmmxsw) View more
IAS2003	Not Applicable	-	1,290	ZDV -> D4T switch	uivuomzpwq(zwfrnritqo) = dryynhqlba pmjcnyyqbp (lnbnjvwnev )	-	01 Jan 2003
				DDI <-> 3TC switch	uivuomzpwq(zwfrnritqo) = ptxqdspxvh pmjcnyyqbp (lnbnjvwnev )