Spiramycin

Spiramycin 속성

Spiramycin C화학적 특성, 용도, 생산

개요

Spiramycin was found in the culture broth of Streptomyces ambofaciens by Rhone Poulenc in 1954 and its acetate was synthesized by Kyowa Hakko Kogyo Co. in 1965. This antibiotic consists of three closely related macrolide components, I, II, and III, whose ratio is 2 : 1 : 1. Spiramycin shows almost the same antimicrobial spectrum and activity as the other macrolides, but its acetate, acetylspiramycin, has much better pharmacokinetic properties and activity in vivo.

화학적 성질

An antibiotic substance.

용도

Spiramycin I (foromacidin A) is the major analogue of a complex of 16-membered macrocyclic lactones produced by S. ambofaciens and S. spiramyceticus that have broad spectrum antibiotic activity. Spiramycins are unusual among the macrocyclic lactones in that they contain two basic sugars. Spiramycin complex has been used in both human and animal health but its use has not been widespread.

Antimicrobial activity

Enterobacteriaceae are resistant. Spiramycin is also active against anaerobic species: Actinomyces israelii (MIC 2–4 mg/L), Cl. perfringens (MIC 2–8 mg/L) and Bacteroides spp. (MIC 4–14 mg/L). It is also active against Tox. gondii.

위험도

Poison; moderately toxic; teratogen; muta- gen; can cause hypermotility, diarrhea, nausea, or vomiting.

Pharmaceutical Applications

A fermentation product of Streptomyces ambofaciens, composed of several closely related compounds. Spiramycin 1 is the major component (c. 63%); spiramycins 2 and 3 are the acetate and monopropionate esters, respectively. It is available for oral administration and as spiramycin adipate for intravenous infusion. Spiramycins are relatively stable in acid conditions. A derivative, acetylspiramycin, is available in Japan.

Pharmacokinetics

Oral absorption: Variable
Cmax 1 g oral： 2.8 mg/L after 2 h
Plasma half-life：4–8h
Volume of distribution ：383 L
Plasma protein binding ：15%
In healthy volunteers given 2 g orally followed by 1 g every 6 h, peak plasma levels were 1.0–6.7 mg/L. After 1 g orally the AUC was 10.8 mg.h/L, with an apparent elimination halflife of 2.8 h. It is widely distributed in the tissues. It does not reach the CSF. Levels 12 h after a dose of 1 g were 0.25 mg/L in serum, 5.3 mg/L in bone and 6.9 mg/L in pus. Levels of 10.6 mg/L have been found 4 h after dosing in saliva, and concentrations at least equal to those in the serum are seen in bronchial secretions. A concentration of 27 mg/g was found in prostate tissues after repeated dosage. Only 5–15% is recovered from the urine. Most is metabolized, but significant quantities are eliminated via the bile, in which concentrations up to 40 times those in the serum may be found.

부작용

Spiramycin is generally well tolerated, the most common adverse reactions being gastrointestinal disturbances, notably abdominal pain, nausea and vomiting, rashes and sensitization following contact.

Spiramycin 준비 용품 및 원자재

원자재

준비 용품

Spiramycin 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Shaanxi Dideu Medichem Co. Ltd	+86-29-81148696 +86-15536356810	1022@dideu.com	China	3882	58
Wuhan Fortuna Chemical Co., Ltd	+86-027-59207850	info@fortunachem.com	China	5986	58
Hebei Weibang Biotechnology Co., Ltd	+8617732866630	bess@weibangbio.com	China	18194	58
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	deasea125996@gmail.com	China	2472	58
Hangzhou ICH Biofarm Co., Ltd	+86-0571-28186870; +undefined8613073685410	sales@ichemie.com	China	998	58
Hangzhou Hyper Chemicals Limited	+86-0086-57187702781 +8613675893055	info@hyper-chem.com	China	295	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618092446649	sarah@tnjone.com	China	1143	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21639	55
Hefei TNJ Chemical Industry Co.,Ltd.	+86-0551-65418679 +8618949832763	info@tnjchem.com	China	2986	55
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29886	58

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