一种新型口服可用头孢曲松制剂与胆汁酸阳离子类似物形成物理复合物在大鼠体内的药代动力学。
Pharmacokinetics of a new, orally available ceftriaxone formulation in physical complexation with a cationic analogue of bile acid in rats.
作者信息
Lee Seulki, Kim Sang Kyoon, Lee Dong Yun, Chae Su Young, Byun Youngro
机构信息
College of Pharmacy, Seoul National University, San 56-1, Shillim-dong, Gwanak-gu, Seoul 151-742, Korea.
出版信息
Antimicrob Agents Chemother. 2006 May;50(5):1869-71. doi: 10.1128/AAC.50.5.1869-1871.2006.
Abstract
Oral administration of ceftriaxone associated with a bile acid-based new oral carrier, cholylethylenediamine, in 50% propylene glycol to rats at doses of 25 and 50 mg/kg of body weight resulted in a significant increase in intestinal absorption, as evidenced by 55% improvement in the bioavailability, whereas ceftriaxone alone showed a bioavailability of less than 1%.
摘要
将头孢曲松与一种基于胆汁酸的新型口服载体胆酰乙二胺，以50%丙二醇作为溶剂，按25毫克/千克和50毫克/千克体重的剂量口服给予大鼠，结果显示肠道吸收显著增加，生物利用度提高了55%，而单独使用头孢曲松时生物利用度不到1%。
相似文献
1
Pharmacokinetics of a new, orally available ceftriaxone formulation in physical complexation with a cationic analogue of bile acid in rats.一种新型口服可用头孢曲松制剂与胆汁酸阳离子类似物形成物理复合物在大鼠体内的药代动力学。
Antimicrob Agents Chemother. 2006 May;50(5):1869-71. doi: 10.1128/AAC.50.5.1869-1871.2006.
2
Cationic analog of deoxycholate as an oral delivery carrier for ceftriaxone.
J Pharm Sci. 2005 Nov;94(11):2541-8. doi: 10.1002/jps.20478.
3
Pharmacokinetics and dosage regimen of ceftriaxone in buffalo calves.头孢曲松在水牛犊牛体内的药代动力学及给药方案
Vet Res Commun. 2004 May;28(4):331-8. doi: 10.1023/b:verc.0000026658.45361.ce.
4
Oral delivery of ionic complex of ceftriaxone with bile acid derivative in non-human primates.口服给药：头孢曲松与胆酸衍生物的离子复合物在非人类灵长类动物中的应用。
Pharm Res. 2013 Apr;30(4):959-67. doi: 10.1007/s11095-012-0932-0. Epub 2013 Jan 5.
5
Mixed Micelles Loaded with Bile Salt: An Approach to Enhance Intestinal Transport of the BCS Class III Drug Cefotaxime in Rats.负载胆盐的混合胶束：增强大鼠体内BCS III类药物头孢噻肟肠道转运的一种方法。
Eur J Drug Metab Pharmacokinet. 2017 Aug;42(4):635-645. doi: 10.1007/s13318-016-0375-9.
6
Ceftriaxone Absorption Enhancement for Noninvasive Administration as an Alternative to Injectable Solutions.将头孢曲松用于非肠道给药以增强吸收，作为替代注射溶液的方法。
Antimicrob Agents Chemother. 2018 Nov 26;62(12). doi: 10.1128/AAC.01170-18. Print 2018 Dec.
7
Novel Cationic Prodrug of Ubiquinol-10 Enhances Intestinal Absorption via Efficient Formation of Nanosized Mixed-Micelles with Bile Acid Anions.新型泛醇 10 阳离子前药通过与胆汁酸阴离子形成高效纳米混合胶束增强肠道吸收。
Molecules. 2020 Jan 27;25(3):546. doi: 10.3390/molecules25030546.
8
Pharmacokinetics of florfenicol after treatment of pigs with single oral or intramuscular doses or with medicated feed for three days.单剂量口服或肌肉注射氟苯尼考，或用加药饲料连续投喂三天后猪体内氟苯尼考的药代动力学。
Vet Rec. 1999 Oct 2;145(14):397-9. doi: 10.1136/vr.145.14.397.
9
Pharmacokinetics and dosage regimen of ceftriaxone in E. coli lipopolysaccharide induced fever in buffalo calves.
J Vet Sci. 2005 Jun;6(2):147-50.
10
Enteral, oral, and rectal absorption of ceftriaxone using glyceride enhancers.使用甘油酯增强剂对头孢曲松进行肠内、口服和直肠吸收研究。
Chemotherapy. 1988;34(2):77-84. doi: 10.1159/000238551.
引用本文的文献
1
The effects of repeated fecal transplantation and activated charcoal treatment on gut dysbiosis induced by concurrent ceftriaxone administration in mice.重复粪便移植和活性炭处理对小鼠同时给予头孢曲松所致肠道菌群失调的影响。
Sci Rep. 2025 Apr 22;15(1):13908. doi: 10.1038/s41598-025-96701-4.
2
Endotoxin-Induced Sepsis on Ceftriaxone-Treated Rats' Ventilatory Mechanics and Pharmacokinetics.内毒素诱导的脓毒症对头孢曲松治疗大鼠通气力学和药代动力学的影响
Antibiotics (Basel). 2024 Jan 15;13(1):83. doi: 10.3390/antibiotics13010083.
3
Oligonucleotide Solid Nucleolipid Nanoparticles against Antibiotic Resistance of ESBL-Producing Bacteria.用于对抗产超广谱β-内酰胺酶细菌抗生素耐药性的寡核苷酸固体核脂质纳米颗粒
Pharmaceutics. 2022 Jan 27;14(2):299. doi: 10.3390/pharmaceutics14020299.
4
Time to abandon ampicillin plus gentamicin in favour of ampicillin plus ceftriaxone in Enterococcus faecalis infective endocarditis? A meta-analysis of comparative trials.是否应该放弃氨苄西林联合庆大霉素，转而采用氨苄西林联合头孢曲松治疗粪肠球菌感染性心内膜炎？一项比较试验的荟萃分析。
Clin Res Cardiol. 2022 Oct;111(10):1077-1086. doi: 10.1007/s00392-021-01971-3. Epub 2021 Nov 9.
5
Evaluation of Ceftriaxone Plus Avibactam in an Intracellular Hollow Fiber Model of Tuberculosis: Implications for the Treatment of Disseminated and Meningeal Tuberculosis in Children.头孢曲松加阿维巴坦在结核分枝杆菌细胞内中空纤维模型中的评价：对儿童播散性和脑膜结核治疗的影响。
Pediatr Infect Dis J. 2020 Dec;39(12):1092-1100. doi: 10.1097/INF.0000000000002857.
6
Bile acid transporter-mediated oral drug delivery.胆汁酸转运体介导的口服药物递送。
J Control Release. 2020 Nov 10;327:100-116. doi: 10.1016/j.jconrel.2020.07.034. Epub 2020 Jul 22.
7
Ceftriaxone Absorption Enhancement for Noninvasive Administration as an Alternative to Injectable Solutions.将头孢曲松用于非肠道给药以增强吸收，作为替代注射溶液的方法。
Antimicrob Agents Chemother. 2018 Nov 26;62(12). doi: 10.1128/AAC.01170-18. Print 2018 Dec.
8
Oral delivery of ionic complex of ceftriaxone with bile acid derivative in non-human primates.口服给药：头孢曲松与胆酸衍生物的离子复合物在非人类灵长类动物中的应用。
Pharm Res. 2013 Apr;30(4):959-67. doi: 10.1007/s11095-012-0932-0. Epub 2013 Jan 5.
9
Enhanced antibacterial effect of ceftriaxone sodium-loaded chitosan nanoparticles against intracellular Salmonella typhimurium.载头孢曲松钠壳聚糖纳米粒对细胞内鼠伤寒沙门氏菌的增强抗菌作用。
AAPS PharmSciTech. 2012 Jun;13(2):411-21. doi: 10.1208/s12249-012-9758-7. Epub 2012 Feb 23.
本文引用的文献
1
A new drug carrier, Nalpha-deoxycholyl-L: -lysyl-methylester, for enhancing insulin absorption in the intestine.一种新型药物载体，Nα-脱氧胆酰-L-赖氨酰甲酯，用于增强肠道内胰岛素的吸收。
Diabetologia. 2005 Mar;48(3):405-11. doi: 10.1007/s00125-004-1658-2. Epub 2005 Mar 1.
2
Solubilizing excipients in oral and injectable formulations.口服和注射用制剂中的增溶剂
Pharm Res. 2004 Feb;21(2):201-30. doi: 10.1023/b:pham.0000016235.32639.23.
3
Enhanced oral bioavailability of poorly absorbed drugs. I. Screening of absorption carrier for the ceftriaxone complex.吸收不佳药物的口服生物利用度增强。I. 头孢曲松复合物吸收载体的筛选。
J Pharm Sci. 2004 Mar;93(3):612-20. doi: 10.1002/jps.10563.
4
Polymeric materials containing bile acids.含有胆汁酸的聚合材料。
Acc Chem Res. 2002 Jul;35(7):539-46. doi: 10.1021/ar0101180.
5
Conjugation of low-molecular-weight heparin and deoxycholic acid for the development of a new oral anticoagulant agent.低分子量肝素与脱氧胆酸的共轭作用用于新型口服抗凝剂的研发。
Circulation. 2001 Dec 18;104(25):3116-20. doi: 10.1161/hc5001.100627.
6
Carrier-mediated delivery of 9-(2-phosphonylmethoxyethyl)adenine to parenchymal liver cells: a novel therapeutic approach for hepatitis B.载体介导的9-(2-膦酰甲氧基乙基)腺嘌呤向肝实质细胞的递送：一种治疗乙型肝炎的新方法。
Antimicrob Agents Chemother. 2000 Mar;44(3):477-83. doi: 10.1128/AAC.44.3.477-483.2000.
7
Early switch from intravenous to oral antibiotics: guidelines and implementation in a large teaching hospital.从静脉注射抗生素到口服抗生素的早期转换：大型教学医院的指南与实施
J Antimicrob Chemother. 1999 Apr;43(4):601-6. doi: 10.1093/jac/43.4.601.
8
Cost-effectiveness and value of an IV switch.静脉输液转换装置的成本效益和价值
Pharmacoeconomics. 1994;5(Suppl 2):20-6. doi: 10.2165/00019053-199400052-00005.
9
Intestinal absorption of peptides by coupling to bile acids.通过与胆汁酸偶联实现肽的肠道吸收。
J Biol Chem. 1994 Apr 8;269(14):10621-7.
10
Pharmacoeconomic benefit of antibiotic step-down therapy: converting patients from intravenous ceftriaxone to oral cefpodoxime proxetil.抗生素降阶梯疗法的药物经济学效益：将患者从静脉注射头孢曲松转换为口服头孢泊肟酯。
Ann Pharmacother. 1995 Jun;29(6):561-5. doi: 10.1177/106002809502900601.
Zotero 插件