Delving into the Latest Updates on Clopidogrel Resinate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Pregrel

Target

P2Y12 receptor

Mechanism

P2Y12 receptor antagonists(Purinergic receptor P2Y12 antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Thrombosis

Inactive Indication-

Originator Organization

Chong Kun Dang Pharmaceutical Corp.

Active Organization

Chong Kun Dang Pharmaceutical Corp.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

KR (01 Jan 2007),

Thrombosis

Regulation-

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In this study, chloroquine resinates were prepared at a 1:1 (w:w) drug-to-resin ratio using the batch method with polacrilex (PC), sodium polystyrene sulfonate (SPS), and polacrilin potassium (PP) ion exchange resins (IER). The influence of drug/resin ratio and pH of the medium on drug loading efficiency was explored. UV-VIS spectrophotometric analysis showed that SPS resin had high loading efficiency for chloroquine diphosphate (CLP), above 89%, regardless of the pH. PP resin was more effective at pH 5.0 (90.68%) than at pH 1.0 (2.09%), and PC resin had only 27.63% of CLP loading efficiency. CLP complexation with IER yielded amorphous mixtures according to results from differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD), thus indicating drug-resin interaction. The taste masking efficiency was evaluated with in vitro methods using an adapted dissolution test and an electronic tongue system. During dissolution tests, SPS released only 1.0% of CLP after 300 s, while PP released over 10% after 90 s in simulated saliva solution. The electronic tongue distinguished the samples containing CLP, resins, and resinates by using multidimensional projection techniques that indicated an effective drug taste masking. In an accelerated stability study, the drug contents did not decrease in chloroquine resinates, and there was no physical degradation of the resinates after 60 days. Using chloroquine resinates therefore represents a novel way to evaluate taste masking in vitro which is relevant for the early formulation development process.

01 Jun 2018·Cell Biology and ToxicologyQ2 · MEDICINE

Effects of aspirin and clopidogrel on neural stem cells

Q2 · MEDICINE

Article

Author: Hwang, Mina ; Lee, Kyu-Yong ; Koh, Seong-Ho ; Lee, Young Joo ; Park, Hyun-Hee ; Choi, Hojin

Cerebral infarction causes severe morbidity and mortality. Most patients with cerebral infarction should take antiplatelet drugs daily, so the effects of those drugs on the regeneration of the brain need to be investigated. Aspirin and clopidogrel are the most widely used antiplatelet drugs for the prevention of ischemic stroke. We investigated the effects of aspirin and clopidogrel on neural stem cells (NSCs). NSCs were dissociated from fetal rat cortex and cultured with basic fibroblast growth factor and N2 medium. To measure the effects of aspirin and clopidogrel on NSCs, NSCs were treated with several concentrations of aspirin, clopidogrel bisulfate, and clopidogrel resinate for 24 h. After the treatment, we measured cell viability by cell counting kit-8, MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay, trypan blue staining, flow cytometry, and lactate dehydrogenase assay. To evaluate their effects on NSC proliferation, we performed BrdU cell proliferation assay and colony-forming unit assay. We compared the intracellular protein level in the NSCs treated with aspirin and two types of clopidogrel, by proteomics analysis. Various viability tests showed that clopidogrel resinate and clopidogrel bisulfate did not affect the viability and proliferation of NSCs whereas aspirin decreased them even at low concentrations which are clinically relevant. Moreover, through the proteomics, it was confirmed that the toxicity of aspirin to NSCs might be associated with the alteration of several intracellular proteins. Taken together, these results suggest that clopidogrel resinate and clopidogrel bisulfate are safe but aspirin could be toxic to NSCs. Therefore, when these antiplatelet agents are prescribed over the long-term, the finding that aspirin could be toxic to NSCs should be considered.

02 Oct 2016·Drug Development and Industrial PharmacyQ4 · MEDICINE

Development and physicochemical characterization of clindamycin resinate for taste masking in pediatrics

Q4 · MEDICINE

Article

Author: Helms, Richard ; Alayoubi, Alaadin ; Daihom, Baher ; Almoazen, Hassan ; Wang, Lijia ; Mishra, Sanjay ; Ma, Dejian

PURPOSETo evaluate the physicochemical characteristics of clindamycin HCl in a complex form (resinate) with ion exchange resin (IER) (Amberlite IRP69).METHODSDrug-resin complex was prepared by simple aqueous binding method. Drug binding study was carried out at different drug and resin concentrations. Several physicochemical characterization studies were conducted to evaluate the resinate complex. These studies included flow properties, in vitro drug release in SGF and SIF, DSC, TGA, mass spectroscopy and XPRD evaluations. In addition, stability study of resinate complex was conducted at 25 and 40 °C for up to 1 month.RESULTSClindamycin and Amberlite IRP69 have formed a complex (resinate) and have shown good flow properties, good thermal properties and chemical stability (short term over 4 weeks) at 25 and 40 °C. Clindamycin release profiles from resinate in SGF and SIF have shown immediate release characteristics and release in simulated saliva has shown dependence on water volume.CONCLUSIONThe clindamycin stable complex with IER (Amberlite IRP69) has the potential for further development as a compatible pediatric liquid formulation (suspension) or a fast disintegrating tablet.

100 Deals associated with Clopidogrel Resinate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	B01AC04	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Thrombosis	KR	Chong Kun Dang Pharmaceutical Corp.	01 Jan 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00947843 (Pubmed \| Med Lett Drugs Ther)	Phase 4	Coronary Disease	314	Clopidogrel resinate	axtmnyxnsq(vkskwhhuyt) = qqpmdqncig eipsutveek (sxhlvyxqhl )	-	01 Aug 2011
				Clopidogrel bisulfate	axtmnyxnsq(vkskwhhuyt) = yrrfqdkuig eipsutveek (sxhlvyxqhl )