Doxycycline-d3 (hyclate)
目录号 : GC45440
一种用于量化多西环素的内部标准
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Doxycycline-d3 is intended for use as an internal standard for the quantification of doxycycline by GC- or LC-MS. Doxycycline is a broad-spectrum tetracycline antibiotic.1,2 It inhibits bacterial protein synthesis by binding to ribosomes.2,3 Doxycycline also selectively inhibits human matrix metalloproteinase-8 (MMP-8) and MMP-13 over MMP-1 with 50, 60, and 5% inhibition, respectively, when used at a concentration of 30 μM.4 It can be used as a regulator for inducible gene expression systems where expression depends on either the presence (Tet-On) or absence (Tet-Off) of doxycycline.5,6 Formulations containing doxycycline have been used in the treatment of bacterial infections and the prevention of malaria.
References
1. Williamson, G.M. The in vitro activity of vibramycin (doxycycline). Chemotherapia (Basel) 13(Suppl. 1), 1-6 (1968).
2. Griffin, M.O., Ceballos, G., and Villarreal, F.J. Tetracycline compounds with non-antimicrobial organ protective properties: Possible mechanisms of action. Pharmacol. Res. 63(2), 102-107 (2011).
3. Chopra, I. Tetracycline analogs whose primary target is not the bacterial ribosome. Antimicrob. Agents Chemother. 38(4), 637-640 (1994).
4. Smith, G.N., Jr., Mickler, E.A., Hasty, K.A., et al. Specificity of inhibition of matrix metalloproteinase activity by doxycycline: Relationship to structure of the enzyme. Arthritis Rheum. 42(6), 1140-1146 (1999).
5. Gould, D.J., Berenstein, M., Dreja, H., et al. A novel doxycycline inducible autoregulatory plasmid which displays "on"/"off" regulation suited to gene therapy applications. Gene Ther. 7(24), 2061-2070 (2000).
6. Li, Z., Michael, I.P., Zhou, D., et al. Simple piggyBac transposon-based mammalian cell expression system for inducible protein production. Proc. Natl. Acad. Sci. U.S.A. 110(13), 5004-5009 (2013).
| Cas No. | SDF | ||
| 分子式 | 2[C22H21D3N2O8].2HCl.XH2O.C2H6O | 分子量 | 1013.9 |
| 溶解度 | DMSO: slightly soluble,Methanol: slightly soluble | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9863 mL | 4.9315 mL | 9.8629 mL |
| 5 mM | 0.1973 mL | 0.9863 mL | 1.9726 mL |
| 10 mM | 0.0986 mL | 0.4931 mL | 0.9863 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Systematic review and meta-analysis on the nonsurgical treatment of chronic periodontitis by means of scaling and root planing with or without adjuncts
J Am Dent Assoc 2015 Jul;146(7):508-24.e5.PMID:26113099DOI:10.1016/j.adaj.2015.01.028.
Background: Conduct a systematic review and meta-analysis on nonsurgical treatment of patients with chronic periodontitis by means of scaling and root planing (SRP) with or without adjuncts. Methods: A panel of experts convened by the American Dental Association Council on Scientific Affairs conducted a search of PubMed (MEDLINE) and Embase for randomized controlled trials of SRP with or without the use of adjuncts with clinical attachment level (CAL) outcomes in trials at least 6 months in duration and published in English through July 2014. The authors assessed individual study bias by using the Cochrane Risk of Bias Tool and conducted meta-analyses to obtain the summary effect estimates and their precision and to assess heterogeneity. The authors used funnel plots and Egger tests to assess publication bias when there were more than 10 studies. The authors used a modified version of the US Preventive Services Task Force methods to assess the overall level of certainty in the evidence. Results: The panel included 72 articles on the effectiveness of SRP with or without the following: systemic antimicrobials, a systemic host modulator (subantimicrobial-dose doxycycline), locally delivered antimicrobials (chlorhexidine chips, doxycycline hyclate gel, and minocycline microspheres), and a variety of nonsurgical lasers (photodynamic therapy with a diode laser, a diode laser, neodymium:yttrium-aluminum-garnet lasers, and erbium lasers). Conclusions and practical implications: With a moderate level of certainty, the panel found approximately a 0.5-millimeter average improvement in CAL with SRP. Combinations of SRP with assorted adjuncts resulted in a range of average CAL improvements between 0.2 and 0.6 mm over SRP alone. The panel judged the following 4 adjunctive therapies as beneficial with a moderate level of certainty: systemic subantimicrobial-dose doxycycline, systemic antimicrobials, chlorhexidine chips, and photodynamic therapy with a diode laser. There was a low level of certainty in the benefits of the other included adjunctive therapies. The panel provides clinical recommendations in the associated clinical practice guideline.
Niosome-encapsulated Doxycycline hyclate for Potentiation of Acne Therapy: Formulation and Characterization
Pharm Nanotechnol 2022;10(1):56-68.PMID:35209832DOI:10.2174/2211738510666220224103406.
Background: Acne is the pilosebaceous units' disorder. The most important cause of acne is the colonization of bacteria in the follicles. Among antibiotics, doxycycline hyclate kills a wide range of bacteria. Objectives: The study aims to prevent oral administration's side effects, overcome the barriers of conventional topical treatment, and improve the therapeutic effectiveness; this drug was loaded into niosomal nanocarriers for topical application. Methods: Doxycycline hyclate was loaded into four niosomal formulations prepared by the thinfilm hydration method with different percentages of constituents. Drug-containing niosomal systems were evaluated for morphological properties via scanning electron microscopy, particle size, drug entrapment efficiency, zeta potential, in vitro drug release, physical stability after 60 days, in vitro drug permeation through rat skin, in vitro drug deposition in rat skin, toxicity on human dermal fibroblasts (HDF) by MTT method after 72 hours, and antibacterial properties against the main acne-causing bacteria via antibiogram test. Results: The best formulation had the appropriate particle size of 362.88 ± 13.05 nm to target follicles, entrapment efficiency of 56.3 ± 2.1%, the zeta potential of - 24.46±1.39 mV, in vitro drug release of 54.93 ± 1.99% after 32 hours, and the lowest permeation of the drug through the rat skin among all other formulations. Improved cell viability, increased antibacterial activity, and an approximately three-fold increase in drug deposition were the optimal niosomal formulation features relative to the free drug. Conclusion: This study demonstrated the ability of nano-niosomes containing doxycycline hyclate to treat skin acne compared with the free drug.
Biowaiver monographs for immediate release solid oral dosage forms: Doxycycline hyclate
J Pharm Sci 2010 Apr;99(4):1639-53.PMID:19798752DOI:10.1002/jps.21954.
Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing doxycycline hyclate are reviewed. According to the Biopharmaceutics Classification System (BCS), doxycycline hyclate can be assigned to BCS Class I. No problems with BE of IR doxycycline formulations containing different excipients and produced by different manufacturing methods have been reported and hence the risk of bioinequivalence caused by these factors appears to be low. Doxycycline has a wide therapeutic index. Further, BCS-based dissolution methods have been shown to be capable of identifying formulations which may dissolve too slowly to generate therapeutic levels. It is concluded that a biowaiver is appropriate for IR solid oral dosage forms containing doxycycline hyclate as the single Active Pharmaceutical Ingredient (API) provided that (a) the test product contains only excipients present in doxycycline hyclate IR solid oral drug products approved in the International Conference on Harmonization (ICH) or associated countries; and (b) the comparator and the test products comply with the BCS criteria for "very rapidly dissolving" or, alternatively, when similarity of the dissolution profiles can be demonstrated and the two products are "rapidly dissolving.".
Texture and topography analysis of doxycycline hyclate thermosensitive systems comprising zinc oxide
Indian J Pharm Sci 2013 Jul;75(4):385-92.PMID:24302791DOI:10.4103/0250-474x.119807.
To characterize the thermal behavior and texture analysis of doxycycline hyclate thermosensitive gels developed for periodontitis treatment containing zinc oxide prepared by using poloxamer (Lutrol(®) F127) as polymeric material and N-methyl pyrrolidone was used as cosolvent. The thermosensitive gel comprising doxycycline hyclate, Lutrol(®) F127, and N-methyl pyrrolidone were characterized for the thermal behavior and texture analysis. The topography of the system after the dissolution test was characterized with scanning electron microscope. Differential scanning calorimetric thermogram exhibited the endothermic peaks in the systems containing high amount of N-methyl pyrrolidone in solvent. The sol-gel transition temperature of the systems decreased as the zinc oxide amount was increased. The addition of doxycycline hyclate, zinc oxide, and N-methyl pyrrolidone affected the syringeability of systems. The addition of zinc oxide into the doxycycline hyclate-Lutrol(®) F127 systems decreased the diameter of inhibition zone against Staphylococcus aureus, Escherichia coli, and Candida albicans since zinc oxide decreased the diffusion and prolonged release of doxycycline hyclate. From scanning electron microscope analysis, the porous surface of 20% w/w Lutrol(®) F127 system was notably different from that of gel comprising doxycycline hyclate which had interconnected pores and smooth surfaces. The number of pores was decreased with increasing zinc oxide and the porous structure was smaller and more compact. Therefore, the addition of zinc oxide could increase the syringeability of doxycycline hyclate-Lutrol(®) F127 system with the temperature dependence. Zinc oxide decreased inhibition zone against test microbes because of prolongation of doxycycline hyclate release and reduced size of continuous cells. Furthermore, zinc oxide also increased the compactness of wall surfaces of Lutrol(®) F127.
Doxycycline hyclate stimulates inducible nitric oxide synthase and arginase imbalance, potentiating inflammatory and oxidative lung damage in schistosomiasis
Biomed J 2022 Dec;45(6):857-869.PMID:34971826DOI:10.1016/j.bj.2021.12.007.
Background: We investigated the relationship between inducible nitric oxide synthase (iNOS) and arginase pathways, cytokines, macrophages, oxidative damage and lung granulomatous inflammation in S. mansoni-infected and doxycycline-treated mice. Methods: Swiss mice were randomized in four groups: (i) uninfected, (ii) infected with S. mansoni, (iii) infected + 200 mg/kg praziquantel (Pzt), (iv) and (v) infected + 5 and 50 mg/kg doxycycline. Pzt (reference drug) was administered in a single dose and doxycycline for 60 days. Results: S. mansoni-infection determined extensive lung inflammation, marked recruitment of M2 macrophages, cytokines (IL-4, IL-5, IFN-γ, TNF-α) upregulation, intense eosinophil peroxidase (EPO) levels, arginase expression and activity, reduced iNOS expression and nitric oxide (NO) production. The higher dose of doxycycline aggravated lung granulomatous inflammation, downregulating IL-4 levels and M2 macrophages recruitment, and upregulating iNOS expression, EPO, NO, IFN-γ, TNF-α, M1 macrophages, protein carbonyl and malondialdehyde tissue levels. The number and size of granulomas in doxycycline-treated animals was higher than untreated and Pzt-treated mice. Exudative/productive granulomas were predominant in untreated and doxycycline-treated animals, while fibrotic/involutive granulomas were more frequent in Pzt-treated mice. The reference treatment with Pzt attenuated all these parameters. Conclusion: Our findings indicated that doxycycline aggravated lung granulomatous inflammation in a dose-dependent way. Although Th1 effectors are protective against several intracellular pathogens, effective schistosomicidal responses are dependent of the Th2 phenotype. Thus, doxycycline contributes to the worsening of lung granulomatous inflammation by potentiating eosinophils influx and downregulating Th2 effectors, reinforcing lipid and protein oxidative damage in chronic S. mansoni infection.