Diquafosol sodium
INS 365
CAS: 211427-08-6
Molecular Formula: C18H22N4Na4O23P4
Diquafosol sodium - Names and Identifiers
| Name | INS 365 |
| Synonyms | D03864 INS 365 Diquafosol sodium Diquafosol tetrasodium Diquafosol sodium (jan) Diquafosol Impurity 7(UP4U) Diquafosol tetrasodium (usan) |
| CAS | 211427-08-6 |
| EINECS | 253-874-2 |
Diquafosol sodium - Physico-chemical Properties
| Molecular Formula | C18H22N4Na4O23P4 |
| Molar Mass | 878.23 |
| Solubility | H2O: ≥ 32 mg/mL |
| Storage Condition | -20℃ |
| Physical and Chemical Properties | Bioactive Diquafosol Tetrasodium (INS-365) is a P2Y2 receptor agonist useful in the treatment of dry eye. |
| Use | Tetra-diquasozole (tetra-diquasodium) has a chemical name of P1, p4-bis (uridine 5 '-tetraphosphate) sodium, which is jointly developed by Shentian pharmaceutical company and intrire pharmaceutical company, launched in Japan in 0.1 billion, the trade name is Diquas, and the sales of diquasol tetrasodium eye drops in was about US $. The first P2Y2 receptor agonist eye drops approved by the worldwide chemical book is diquasol tetra-sodium eye drops, which acts on P2Y2 receptors on conjunctival epithelium and goblet cell membrane by increasing intracellular calcium concentration, promote the secretion of water and mucin, so as to improve the symptoms of dry eye, so that the tear film is closer to the normal state. In addition, diquasol Tetra sodium eye drops are expected to be developed as a expectorant or Pneumonia therapeutic agent having an action of inducing expectoration. |
Diquafosol sodium - Preparation Method of P2Y2 receptor agonist diquasol tetrasodium
from Palm Bridge research
Application (patent) number:
CN202010370868.6
application date:
2020-04-30
Public/Announcement Number:
CN111454312A
Public/announcement date:
2020.07.28
applicant (patent):
China Pharmaceutical University; Changzhou four Pharmaceutical Co., Ltd.
inventor:
Li Zhiyu , Wang Hai , bianjinlei , Xu Pengfei , Tu Yongrui , fan Xinhua , Sun Yongqiang , Peng Peng
National and provincial code:
CN320115
Abstract:
The invention discloses a preparation method of a P2Y2 receptor agonist diquophosphorus tetrasodium. The pyrophosphate compound represented by Formula II is salified with a long-chain organic amine to obtain a compound of Formula III, further, the pyrophosphate active compound Formula IV is obtained by activation of carbonyl diimidazole, and the uridine monophosphate compound represented by formula V is salified with a long-chain organic amine to obtain the compound formula VI, the reaction of Formula IV with formula VI is carried out by Lewis acid catalysis in a hydrophilic solvent to obtain the target product of formula I, tetrasodium diquasol. The method uses cation exchange resin to treat the reaction raw materials which are cheap and easy to be stored, and uses organic base to salt with the reaction raw materials to improve the thermal stability. Finally, the target product is purified by anion exchange chromatography. The method is efficient, the product is easy to separate and the yield is high.
Last Update：2024-01-02 23:10:35
Diquafosol sodium - A kind of tetrasodium diquasol eye drops containing chelating agent
from Palm Bridge research
Application (patent) number:
CN201810319191.6
application date:
2018-04-11
Public/Announcement Number:
CN108403625A
Public/announcement date:
2018.08.17
applicant (patent):
Dongguan Jieshi Pharmaceutical Technology Co., Ltd.
inventor:
National and provincial code:
CN441900
Abstract:
The invention belongs to the technical field of eye drops, and provides a kind of diquasol tetrasodium eye drops containing chelating agent, comprising diquasol tetrasodium, pharmaceutically additive, first chelating agent, pH Adjusting Agent and water, the concentration of tetrasodium diquasol is 3%(w/v), the first chelating agent is selected from diethylenetriaminepentaacetic acid, one or more of ethylenediaminetetramethylene phosphonic acid and its salts. The present invention provides eye drops containing 3% of tetrasodium descusox, which has better safety and stability, can reduce the occurrence of adverse reactions, has a small number of insoluble particles, and meets the relevant standards of higher requirements.
Last Update：2023-08-16 22:05:47
Diquafosol sodium - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.139 ml | 5.693 ml | 11.387 ml |
| 5 mM | 0.228 ml | 1.139 ml | 2.277 ml |
| 10 mM | 0.114 ml | 0.569 ml | 1.139 ml |
| 5 mM | 0.023 ml | 0.114 ml | 0.228 ml |
Last Update：2024-01-02 23:10:35
Diquafosol sodium - Diquasol sodium eye drops and preparation method thereof
from Palm Bridge research
patent type:
invention patent
Application (patent) number:
CN201811118247.8
application date:
20180926
Public/Announcement Number:
CN108853016A
Public/announcement date:
20181123
applicant (patent):
Guangzhou Daguang Pharmaceutical Co., Ltd.
inventor:
Chen Weihan , Huang Weijing , Li Tao Ying
National and provincial code:
CN440116
Abstract:
The invention provides a classical preservative-free Diquas（diauafosol sodium eye drops） and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The present invention solves Diquas（diauafosol sodium eye drops） side effects such as adverse reactions of eyes caused by long-term administration of dry eye. The eye drops of the present invention are almost non-irritating to eyes, and the property of the product is stable.
Last Update：2023-08-16 22:05:47
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