Delving into the Latest Updates on Pirenoxine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Pirenoxine (JP17/INN), Catalin, Catalin-K

+ [3]

Target-

Mechanism-

Therapeutic Areas

Eye Diseases

Active Indication

Cataract

Inactive Indication-

Originator Organization

Senju Pharmaceutical Co., Ltd.

Active Organization

Wuhan Wuyao Pharmaceutical Co., Ltd.

Hubei Dongsheng Pharmaceutical Co. Ltd.Senju Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (01 Dec 1958),

Cataract

Regulation-

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Structure

Molecular FormulaC16H8N2O5

InChIKeyOKPNYGAWTYOBFZ-UHFFFAOYSA-N

CAS Registry1043-21-6

OBJECTIVETo evaluate the effects of Dajizhi (Euphorbium) on selenite-induced cataracts.METHODSWistar rat pups were divided into 9 groups. Rats in group 1 were subcutaneously injected with saline, and rats in the other groups were injected with sodium-selenite. Every right eye was treated with 5 μL eye drops 3 times per day, and the left eye received no treatment. The eyes of rats in group 3 were treated with pirenoxine; rats in groups 4, 5, 6, 7, 8 and 9 were respectively treated with Dajizhi (Euphorbium) (25 mg/mL), Dajizhi (Euphorbium) (5 mg/mL), Dajizhi (Euphorbium) methanol extract (25 mg/mL), Dajizhi (Euphorbium) methanol extract (5 mg/mL), euphol (25 mg/mL), euphol (5 mg/mL). Cataracts were observed by a slit lamp before and after treatment. Electroretinograms were acquired at set intervals. The morphological changes of the rat eyes were observed in vitro, and the levels of glutathione peroxidase (GSH-Px) and superoxide dismutase (SOD) in the lenses and aqueous humour were estimated at set intervals.RESULTSSlit lamp examination showed decreased degrees of cataracts after administration of the different treatments. Morphological comparison showed that Dajizhi (Euphorbium) can reduce the turbidity of the lenses, meaning that Dajizhi (Euphorbium) has the anti-cataract effects. Low-concentration of Dajizhi (Euphorbium), its methanol extract and euphol treatment prevented the b-wave amplitudes of the electroretinograms from falling. Euphorbium treatment significantly restored GSH-Px and SOD levels in the lenses and aqueous humour, especially after 10 and 25 d of administration. Euphorbium may help lenses fight oxidative stress caused by selenite.CONCLUSIONThe administration of Dajizhi (Euphorbium) can inhibit selenite-induced cataracts.

01 May 2017·YAKUGAKU ZASSHIQ4 · MEDICINE

Improvement of Dissolution Rate and Stability in a Pirenoxine Ophthalmic Suspension by the Bead Mill Methods

Q4 · MEDICINE

Article

Author: Kotake, Takeshi ; Ito, Yoshimasa ; Yamaoka, Sakie ; Nakazawa, Yosuke ; Nagai, Noriaki ; Ueno, Akina

Foreign matter sensation and blurred vision following instillation of ophthalmic suspension are often observed, and remaining of solid particle on cornea is related these side effects. In addition, low dispersion stability in the ophthalmic suspension affects the therapeutic effect. In this study, we have attempted to enhance the dissolution rate and stability of commercially available pirenoxine ophthalmic suspension (CA-pirenoxine eye drops), anti-cataract eye drops, by changes in particle size. Methylcellulose, zirconia beads (0.1 mm) and Micro Smash were used to mill the pirenoxine (bead mill method), and the distribution of particle size was changed to approximately 60-900 nm (nanodispersions) from 70 nm-3 μm (CA-pirenoxine eye drops). The dissolution rate of pirenoxine increased by the bead mill, and the dissolution rate constant in pirenoxine nanodispersions was 2.1-fold than that in CA-pirenoxine eye drops. Moreover, the dispersion stability in nanodispersions also significant higher in comparison with the CA-pirenoxine eye drops. The dispersion ratio in CA-pirenoxine eye drops and pirenoxine nanodispersions at 2 d after suspension was 48%, 99%, respectively. In conclusion, we showed that the dissolution rate and dispersion stability of CA-pirenoxine eye drops were enhanced by the bead mill method. These findings provide significant information that can be used in the design of ophthalmic suspension.

01 Aug 2014·Spectrochimica Acta Part A: Molecular and Biomolecular SpectroscopyQ2 · CHEMISTRY

Interaction between pirenoxine and bovine serum albumin in aqueous solution

Q2 · CHEMISTRY

Article

Author: Yi, Pinggui ; Yao, Qing ; Yu, Xianyong ; Liao, Zhixi

This work concerns the interaction of prenoxine sodium (PRX) and bovine serum albumin (BSA), which was conducted by spectroscopic means: fluorescence spectra, ultraviolet-visible spectra (UV-vis) and circular dichroism spectra (CD spectra) in physiological conditions. The results revealed the PRX can quench the fluorescence of BSA remarkably in aqueous solution. The quench mechanism has been obtained after corrected the fluorescence intensities for inner filter effects. The binding constants (Ka) were calculated according to the relevant fluorescence data at different temperatures. Moreover, from a series of analyses, we have obtained the binding sites, the binding distance and binding force. The effect of PRX on the conformation of BSA has been analyzed using synchronous fluorescence under experimental conditions. In addition, the CD spectra proved that the secondary structure of BSA changed in the presence of PRX in aqueous solution.

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