Rifaximin
- CAS No.
- 80621-81-4
- Chemical Name:
- Rifaximin
- Synonyms
- XIFAXAN;RIFAMIXIN;l105;normix;l105sv;Riimim;RIFACOL;Rifaxin;Ritacol;RIFAXIMIN
- CBNumber:
- CB5244184
- Molecular Formula:
- C43H51N3O11
- Molecular Weight:
- 785.89
- MOL File:
- 80621-81-4.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/16 18:25:32
| Melting point | 200-2050C (dec) |
|---|---|
| Density | 1.36±0.1 g/cm3(Predicted) |
| storage temp. | Sealed in dry,Store in freezer, under -20°C |
| solubility | ethanol: soluble1mg/mL |
| pka | 2.83±0.70(Predicted) |
| form | powder |
| color | dark orange |
| Merck | 14,8220 |
| Stability | Hygroscopic |
| InChIKey | NZCRJKRKKOLAOJ-XRCRFVBUSA-N |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H312-H361-H332-H335 | |||||||||
| Precautionary statements | P261-P271-P304+P340-P312-P201-P202-P281-P308+P313-P405-P501-P280-P302+P352-P312-P322-P363-P501 | |||||||||
| WGK Germany | 2 | |||||||||
| RTECS | KD1576000 | |||||||||
| HS Code | 2941.90.3000 | |||||||||
| Toxicity | LD50 orally in rats: >2000 mg/kg (Borelli, Bertoli) | |||||||||
| NFPA 704 |
|
Rifaximin price More Price(8)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | R9904 | Rifaximin | 80621-81-4 | 1G | ₹9959 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | R9904 | Rifaximin | 80621-81-4 | 5G | ₹36783.35 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | PHR1946 | Rifaximin Pharmaceutical Secondary Standard; Certified Reference Material | 80621-81-4 | 300MG | ₹19863.88 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | 33999 | Rifaximin VETRANAL?, analytical standard | 80621-81-4 | 100MG | ₹11528.63 | 2022-06-14 | Buy |
| TCI Chemicals (India) | R0101 | Rifaximin | 80621-81-4 | 1G | ₹8000 | 2022-05-26 | Buy |
Rifaximin Chemical Properties,Uses,Production
Description
Rifaximin is an antibiotic structurally related to rifamycin. It is reported to be efficacious in the treatment of gastrointestinal infections and hepatic encephalopathy, being highly active against Gram-positive and -negative aerobic and anaerobic bacteria. Due to poor systemic absorption, rifaximin is effective in presurgical sterilization of the GI tract.It displays good activity against a wide spectrum of bacteria, including Salmonella spp., S. aureus, and E. coli.
Chemical Properties
Red-Orange Crystalline Powder
Uses
Rifaximin is a non-absorbable semisynthetic Rifamycin antibiotic.
Definition
ChEBI: A semisynthetic member of the class of rifamycins and non-systemic gastrointestinal site-specific broad spectrum antibiotic. Used in the treatment of traveller's diarrhoea, hepatic encephalopathy and irritable bowel syndrome.
Antimicrobial activity
The in-vitro activity is slightly inferior to that of rifampicin. The MIC90 for Gram-positive cocci is well below 1 mg/L, with the exception of enterococci (MIC 2–8 mg/L). Among intestinal pathogens C. difficile is sensitive (MIC90 0.8 mg/L), Esch. coli, Salmonella spp. and Shigella spp. are inhibited by 4–8 mg/L. Campylobacter jejuni is mostly insensitive.
Pharmaceutical Applications
A semisynthetic derivative of rifamycin S formulated for oral administration. It is poorly absorbed from the gastrointestinal tract, where its high concentrations are effective against a variety of gastrointestinal pathogens.
Mechanism of action
The mechanism of action of pyrazinamide is unknown, but recent findings suggest that pyrazinamide may be active either totally or in part as a pro-drug. Susceptible organisms produce pyrazinamidase, which is responsible for conversion of pyrazinamide to pyrazinoic acid intracellularly. Mutation in the pyrazinamidase gene (pncA) results in resistant strains of M . tuberculosis. Pyrazinoic acid has been shown to possess biological activity at a pH 5.4 or lower, in contract in vitro tests that show pyrazinoic acid is 8- to 16-fold less active than pyrazinamide . Pyrazinoic acid may lower the pH in the immediate surroundings of the M . tuberculosis to such an extent that the organism is unable to grow, but this physicochemical property appears to account for only some of the activity. The protonated pyrazinoic acid also can permeate the mycobacterial membrane to lower the pH of the cytoplasm. Recent evidence suggests that pyrazinoic acid decreases membrane potential in older, nonreplicating bacilli, thus decreasing membrane transport, and interferes with the energetics of the membrane.
Pharmacokinetics
Oral absorption is very low. However, a fraction of the dose may be absorbed and rapidly eliminated through the bile. A 400 mg oral dose produces a maximum plasma concentration of 3.8 mg/L after 1.2 h. The plasma half-life is 5.8 h. Up to 90% of the administered dose is concentrated in the gut, less than 0.2% in the liver and kidney, and less than 0.01% in other tissues.
Clinical Use
It is used for a variety of gastrointestinal diseases, including the treatment of traveler’s diarrhea. Preliminary results suggest clinical efficacy in the therapy of hepatic encephalopathy and of C. difficile infections.
Side effects
Oral doses up to 100 mg/kg for 6 months produced no significant signs of toxicity to rats. Teratogenic effects in rats and rabbits have been reported (pregnancy category C).
Very few adverse effects were reported during human treatment, mostly gastrointestinal discomfort. Prolonged therapy was associated with infrequent urticarial skin reactions.
Metabolism
Pyrazinamide is readily absorbed after oral administration, but little of the intact molecule is excreted unchanged. The major metabolic route consists of hydrolysis by hepatic microsomal pyrazinamidase to pyrazinoic acid, which may then be oxidized by xanthine oxidase to 5-hydroxypyrazinoic acid. The latter compound may appear in the urine either free or as a conjugate with glycine.
Rifaximin Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| AVD pharmaceuticals Pvt Ltd | +919860835260 | Pune, India | 102 | 58 | Inquiry |
| Siddhivinayakchemicals | +91-912225190111 +91-9819773074 | Mumbai, India | 42 | 58 | Inquiry |
| TYNDAL LABS PVT LTD | +91-8008166674 +91-8008166674 | AndhraPradesh, India | 95 | 58 | Inquiry |
| Sekhment pharmaventures | +91-9030088669 +91-9030088669 | Mumbai, India | 105 | 58 | Inquiry |
| Styrax Pharma Pvt Ltd | +91-4048583333 +91-9848912103 | Telangana, India | 24 | 58 | Inquiry |
| Apotex Pharmachem India Pvt Ltd | +91-8022891034 +91-8022891000 | Karnataka, India | 109 | 58 | Inquiry |
| Mankind Pharma Limited | +91-1146541111 +91-1146541111 | New Delhi, India | 23 | 58 | Inquiry |
| HRV Global Life Sciences | +91-9820219686 +91-9820219686 | Telangana, India | 379 | 58 | Inquiry |
| Synergene Active Ingredients Pvt. Ltd. | +91-04023700774 +91-04023700774 | Telangana, India | 96 | 58 | Inquiry |
| Basil Drugs AND Pharmaceuticals Pvt Ltd | +91-2249700250 +91-9619320820 | Mumbai, India | 108 | 58 | Inquiry |
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- Mar 28，2022
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