Delving into the Latest Updates on Bendazac Lysine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Bendazac lysine (BAN), Bendalina

Target

AKR1B1

Mechanism

AKR1B1 inhibitors(Aldose reductase inhibitors)

Therapeutic Areas

Eye DiseasesEndocrinology and Metabolic DiseaseUrogenital Diseases

Active Indication

CataractDiabetic Nephropathies

Inactive Indication-

Originator Organization

Zhejiang Shapuaisi Pharmaceutical Co. Ltd.

Active Organization

Zhejiang Shapuaisi Pharmaceutical Co. Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC22H28N4O5

InChIKeyOCOCFNMFLNFNIA-ZSCHJXSPSA-N

CAS Registry81919-14-4

View All Structures (2)

BACKGROUNDThe search for a simple and scalable approach that can improve the two key biopharmaceutical processes (solubility and permeability) for BCS Class II and BCS Class IV has still been unmet need.PURPOSEIn this study, L-lysine was investigated as a potential excipient to tackle problems with solubility and permeability. Bendazac (Class II); quercetin and rutin (Class IV) were employed.METHODSDrugs-lysine complexes in 1:1 M ratios were prepared by co-precipitation and co-grinding; characterized for solubility, partition coefficient, DSC, FTIR, SEM, dissolution rate and permeability. Chemical stability of quercetin-lysine and rutin-lysine was studied by assessing antioxidant capacity using Trolox and CUPRAC assays.RESULTS AND CONCLUSIONDrugs-lysine salt/complexes were confirmed. Solubility enhancement factors ranged from 68- to 433-fold increases and dissolution rates were also significantly enhanced by up to 6-times, compared with drugs alone. With the exception of rutin-lysine, P_app for bendazac-lysine and quercetin-lysine enhanced by 2.3- to 4-fold. P_app for quercetin (Class IV) benefited more than bendazac (Class II) when complexed with lysine. This study warrants the use of L-lysine as a promising excipient for enhanced solubility and permeability of Class II and Class IV, providing that the solubility of the drug is ensured at 'the door step' of absorption sites.

01 Jan 2016·Case Reports in Ophthalmological Medicine

A Gel Formulation Containing a New Recombinant Form of Manganese Superoxide Dismutase: A Clinical Experience Based on Compassionate Use-Safety of a Case Report

Article

Author: Prete, Antonio Del ; Ortosecco, Giovanni ; Mancini, Aldo ; Prete, Salvatore Del ; Grumetto, Lucia ; Borrelli, Antonella

Background. We report a case of bilateral posterior subcapsular cataracts (PSCs) in a 24-year-old man with an allergic conjunctivitis history caused by a long-term therapy with glucocorticoids.Case Presentation. The patient showed a visual acuity of 9/10 for both eyes. He followed a therapy with ketotifen and bilastine for four years. During the last six months before our evaluation, he was treated with chloramphenicol and betamethasone, interrupted for onset of cataracts and increased intraocular pressure. We treated him with ophthalmic gel preparation containing a new recombinant form of manganese superoxide dismutase (rMnSOD) at a concentration of 12.5 μg/mL, only for the right eye, while left eye was treated with standard protocol of Bendazac-lysine g 0.5.Conclusion. This case report shows the protective effects of rMnSOD versus PSC disease, probably due to the capacity of rMnSOD of countering free radical species.

01 Mar 2015·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

Characterization of a novel process-related impurity in commercial bendazac lysine eye drops by LC–ESI-QTOF/MS/MS and NMR

Q3 · MEDICINE

Article

Author: Luo, Lei ; Zhu, Peixi ; He, Jiajia ; Yang, Weifeng ; Hong, Liya ; Chen, Juanjuan ; Cheng, Qiaoyuan

A simple and sensitive method was developed for characterization of two impurities from commercial bendazac lysine eye drops, by using liquid chromatography combined with electrospray ionization and QTOF mass analyzer (LC-ESI-QTOF MS/MS). A known impurity was characterized rapidly by comparison with the retention time and MS/MS data of the reference standard. Based on high resolution mass spectrometry (HRMS) and the nuclear magnetic resonance (NMR), a new impurity, purified by preparative HPLC, was identified as 2-(1,5-dibenzyl-1H-indazol-3-yloxy)acetic acid. In addition, a plausible mechanism for the formation of the impurities was also proposed.

100 Deals associated with Bendazac Lysine

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