鹽酸克林霉素作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetClindamycin hydrochlorideCat. No.: HY-B0408ACAS No.: 21462-39-5分式: CHClNOS分量: 461.44作靶點(diǎn): Bacterial作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (216.71 mM)* means soluble, but saturation unknown.SolventMass1 mg 5

2、 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.1671 mL 10.8356 mL 21.6713 mL5 mM 0.4334 mL 2.1671 mL 4.3343 mL10 mM 0.2167 mL 1.0836 mL 2.1671 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照

3、In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.42 mM); Clear solution此案可獲得 2.5 mg/mL (5.42 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L

4、25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.42 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (5.42 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900

5、L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.42 mM); Clear solution此案可獲得 2.5 mg/mL (5.42 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Clindamycin hydrochloride種半合成的林可胺類(lèi)抗素，通過(guò)作于 50S ribosom

6、al 來(lái)抑制蛋質(zhì)的合成。體外研究 Clindamycin is a classical inhibitor of bacterial protein synthesis, by binding to the 23S ribosomal RNA of the 50Sribosomal subunit1.體內(nèi)研究 Clindamycin hydrochloride results in fast absorption after oral administration in dogs, with a mean absorption time(MAT) of 0.87 hour, and bioav

7、ailability is 72.55%. Clindamycin hydrochloride results in total clearance (CL) ofClindamycin after both IV and oral administration (0.503 vs. 0.458 L/h/kg) in dogs. Clindamycin hydrochloride resultsin volume of distribution at steady-state (IV) at 2.48 L/kg, indicating a wide distribution of clinda

8、mycin in body fluidsand tissues. Clindamycin serum concentrations after IV and oral administration remain above 0.5 g/mLapproximately for 10 hours1. Clindamycin hydrochloride significantly reduces oral malodor from the dogs baselinelevels through 42 days. Clindamycin hydrochloride also results in si

9、gnificant reductions in dental plaque, dentalcalculus, and gingival bleeding in dogs2. Clindamycin hydrochloride (2.5 mg/Lb), after ultrasonic scaling, rootplaning, and polishing (USRP), has a significant effect on plaque and pocket depth measures of periodontal diseasebut not on gingivitis in canin

10、e3. Clindamycin hydrochloride results in complete remission ratio of 71.4% (15/21) indogs with canine superficial bacterial pyoderma after treat within 14 to 28 days4.PROTOCOLAnimal For the first experimental period, 11 mg/kg BW clindamycin hydrochloride are administered IV to all animals (Day 0),Ad

11、ministration 1 after catheterisation of the left cephalic vein. The catheters (18 G51 mm Abbocath-T) are removed shortly afteradministration of the drug. Blood samples (3 mL) are collected into plastic tubes by aspiration from the catheterizedlateral cephalic vein, prior to (t=0 h) and at 2, 5, 10,

12、15, 20, 30, 45 min, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12 and 24 h afteradministration. The intravenous catheters are flushed with 2 mL 1% heparinized normal saline after each sampling.On Day 28, all dogs receive one Antirobe capsule (150 mg clindamycin hydrochloride). Dose normalisation frommg/anim

13、al to mg/kg BW is carried out in each animal by dividing the total amount of clindamycin received, by itsbody weight. Blood sample collection is performed, following the technique described above, immediately before(t=0 h) and at 15, 30, 45 min, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12 and 24 h after d

14、rug administration. All blood samplesare allowed to stand in a dark place for 20 min. After centrifugation at 1500 g for 10 min, at 4C, the supernatantserum is transferred into 5-mL plastic tubes and is stored at 30C, pending analysis.MCE has not independently confirmed the accuracy of these methods

15、. They are for reference only.REFERENCES1. Batzias GC, et al. Clindamycin bioavailability and pharmacokinetics following oral administration of clindamycin hydrochloride capsules in dogs. Vet J.2005 Nov;170(3):339-45.Page 2 of 3 www.MedChemE2. Warrick JM, et al. Effect of clindamycin hydrochloride o

16、n oral malodor, plaque, calculus, and gingivitis in dogs with periodontitis. Vet Ther. 2000Winter;1(1):5-16.3. Nielsen D, et al. Effects of treatment with clindamycin hydrochloride on progression of canine periodontal disease after ultrasonic scaling. Vet Ther. 2000Summer;1(3):150-8.4. Bloom PB, et al. Efficacy of once-daily clindamycin hydrochloride in the treatment of superficial bacterial pyoderma in dogs. J Am Anim Hosp Assoc.