盐酸克林霉素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetClindamycin hydrochlorideCat. No.: HY-B0408ACAS No.: 21462-39-5分式: CHClNOS分量: 461.44作靶点: Bacterial作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (216.71 mM)* means soluble, but saturation unknown.SolventMass1 mg 5

2、 mg 10 mgConcentration制备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照

3、In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.42 mM); Clear solution此案可获得 2.5 mg/mL (5.42 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L

4、25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.42 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (5.42 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900

5、L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.42 mM); Clear solution此案可获得 2.5 mg/mL (5.42 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Clindamycin hydrochloride种半合成的林可胺类抗素，通过作于 50S ribosom

6、al 来抑制蛋质的合成。体外研究 Clindamycin is a classical inhibitor of bacterial protein synthesis, by binding to the 23S ribosomal RNA of the 50Sribosomal subunit1.体内研究 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.