Rebamipide

Rebamipide

Rebamipide

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1 Kilogram

Negotiable

  • Min.Order :1 Kilogram
  • Purity: 98%
  • Payment Terms : L/C,T/T

Keywords

Rebamipide supplier Rebamipide China Rebamipide 98%

Quick Details

  • Appearance:powder
  • Application:API
  • PackAge:7.5KG
  • ProductionCapacity:|Metric Ton|Day
  • Storage:Room temperature
  • Transportation:by air or by sea

Superiority:

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Details:

1. Introduction of Rebamipide


Rebamipide, with the cas register number of 90098-04-7, can be called (+-)-2-(4-Chlorobenzoylamino)-3-(2(1H)-quinolinon-4-yl)propionic acid, mucosta, proamipide. Rebamipide is a gastroprotective drug, it is a compound selected from over 500 amino acid analogs of 2(1H)-quinolinone tested for gastroprotective action and for efficacy to heal experimental gastric ulcers. This drug stimulates prostaglandin generation in gastric mucosa and improves not only the speed but also the quality of ulcer healing. In addition, it protects the gastric mucosa against acute injury caused by various noxious and ulcerogenic factors.

 

Specification

Items                             Specification                                           Results
Appearance White or almost white crystaline powder Conform
Clarity of solution Clear and colourless                              Conform                        
Loss on drying  ≤3.% 1.8%
Related substance  ≤0.4% 0.13%
Residue on ignition  ≤0.07% 0.05%
Heavy metals ≤10ppm Conform
Assy  ≥99.0% 99.6%

 

2. Basic Information of Rebamipide


Rebamipide, an amino acid derivative of 2(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. It has also been used for the treatment of Beh?et's disease. Some studies have shown effectiveness in presbyacusis (age-related hearing loss).


1) Properties
(1)Polar Surface Area: 95.5;
(2)Index of Refraction: 1.634 ;
(3)Molar Refractivity: 95.077 cm3;
(4)Molar Volume: 265.848 cm3;
(5) Polarizability: 37.692 10-24cm3;
(6)Surface Tension: 58.3219985961914 dyne/cm;
(7)Density: 1.395 g/cm3;
(8)Flash Point: 374.104 °C;
(9)Enthalpy of Vaporization: 106.903 kJ/mol;
(10)Boiling Point: 694.97 °C at 760 mmHg.

 

2) Toxicity

 

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
dog LD50 oral > 2gm/kg (2000mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
mouse LD50 intramuscular 1353mg/kg (1353mg/kg) SENSE ORGANS AND SPECIAL SENSES: OTHER: EYE

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION

BLOOD: CHANGES IN SPLEEN
Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
mouse LD50 intravenous 572mg/kg (572mg/kg) BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

KIDNEY, URETER, AND BLADDER: OTHER CHANGES
Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
mouse LD50 subcutaneous 2637mg/kg (2637mg/kg) LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION

KIDNEY, URETER, AND BLADDER: OTHER CHANGES

SKIN AND APPENDAGES (SKIN): HAIR: OTHER
Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
mouse LDLo oral > 5gm/kg (5000mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
rabbit LD50 oral > 3gm/kg (3000mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
rat LD50 intravenous 700mg/kg (700mg/kg) KIDNEY, URETER, AND BLADDER: OTHER CHANGES Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
rat LDLo intramuscular 1gm/kg (1000mg/kg) BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

KIDNEY, URETER, AND BLADDER: OTHER CHANGES
Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
rat LDLo oral 5gm/kg (5000mg/kg) BEHAVIORAL: FOOD INTAKE (ANIMAL) Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.
rat LDLo subcutaneous 4gm/kg (4000mg/kg) SENSE ORGANS AND SPECIAL SENSES: OTHER CHANGES: OLFACTION

BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION
Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 20, Pg. 362, 1989.

 

 

3) Mechanisms of action and efficacy in mucosal protection and ulcer healing
Rebamipide, a gastroprotective drug, is a compound selected from over 500 amino acid analogs of 2(1H)-quinolinone tested for gastroprotective action and for efficacy to heal experimental gastric ulcers. This drug stimulates prostaglandin generation in gastric mucosa and improves not only the speed but also the quality of ulcer healing. In addition, it protects the gastric mucosa against acute injury caused by various noxious and ulcerogenic factors. Based on these experimental results, rebamipide had been subsequently tested in several clinical trials and approved in Japan for therapeutic use in patients with gastric ulcers and patients with acute gastritis. The main purpose of developing this type of drug was to improve the quality of ulcer healing, especially in that antisecretory drugs lack this advantage. In a preliminary clinical study, rebamipide improved the quality of gastric ulcer healing and reduced future ulcer recurrence. A number of basic research studies have been performed to clarify the mechanisms of rebamipide's action. These studies demonstrated unique properties of rebamipide and convincingly showed that it increases gastric mucus glycoprotein components, stimulates migration and proliferation of wounded epithelial cell monolayers, increases expression of epidermal growth factor and its receptor in normal and ulcerated gastric mucosa, and scavenges active oxygen radicals. The drug also attenuates the activity of neutrophils and the production of inflammatory cytokines stimulated by NSAIDs and/or H. pylori. Therefore, rebamipide can contribute to the management of patients who are taking NSAIDs or are infected with H. pylori. The inhibition of immunoinflammatory responses by rebamipide in H. pylori-infected patients may prevent development of gastritis, peptic ulcer disease, its recurrence, and possibly gastric cancer. Moreover, rebamipide may enhance eradication of H. pylori-infection using standard eradication therapy.

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