给予盐酸氨基葡萄糖和硫酸氨基葡萄糖后的氨基葡萄糖药动学和生物利用度研究
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摘要
目的观察盐酸氨基葡萄糖(glucosamine hydrochloride,GH)和硫酸氨基葡萄糖(glucosamine sulfate,GS)中氨基葡萄糖在大鼠体内药动学和生物利用度特征。方法大鼠经口服(ig)和静脉注射(iv)GH或GS后,LC-MS/MS检测血浆中氨基葡萄糖的血药浓度,采用DAS 3.0药动学处理软件,计算药动学参数及生物利用度。结果 GH和GS的T_(1/2)、Vz、绝对生物利用度等参数接近。口服GH的相对生物利用度大于GS,而GS的达峰时间早于GH。结论 GH和GS在药动学参数和生物利用度方面具有一定差异。
Aim To determine the pharmacokinetics and bioavailability of glucosamine after administration of glucosamine hydrochloride(GH) and glucosamine sulfate(GS). Methods GH or GS was given ig and iv to rats, respectively. An LC-MS/MS method was developed to measure the concentrations of glucosamine in plasma. DAS 3.0 was employed to obtain the pharmacokinetical parameters as well as bioavailability. Results There was no marked difference in T_(1/2), Vz and absolute availability between GH and GS. However, the relative bioavailability of GH was higher than that of GS. In addition, T_(max) of GS was shorter than that of GH. Conclusion There are some differences between the glucosamine pharmacokinetics of GH and GS.
Aim To determine the pharmacokinetics and bioavailability of glucosamine after administration of glucosamine hydrochloride(GH) and glucosamine sulfate(GS). Methods GH or GS was given ig and iv to rats, respectively. An LC-MS/MS method was developed to measure the concentrations of glucosamine in plasma. DAS 3.0 was employed to obtain the pharmacokinetical parameters as well as bioavailability. Results There was no marked difference in T_(1/2), Vz and absolute availability between GH and GS. However, the relative bioavailability of GH was higher than that of GS. In addition, T_(max) of GS was shorter than that of GH. Conclusion There are some differences between the glucosamine pharmacokinetics of GH and GS.
引文
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[2] Selvan T, Rajiah K, Nainar M S, et al. A clinical study on glucosamine sulfate versus combination of glucosamine sulfate and NSAIDs in mild to moderate knee osteoarthritis[J]. Sci World J, 2012, 2012: 902676.
[3] Salvatore S, Heuschkel R, Tomlin S, et al. A pilot study of N-acetyl glucosamine, a nutritional substrate for glycosaminoglycan synthesis, in paediatric chronic inflammatory bowel disease[J]. Aliment Pharmacol Ther, 2000, 14: 1567-79.
[4] Jamialahmadi K, Sadeghnia H R, Mohammadi G, et al. Glucosamine alleviates scopolamine induced spatial learning and memory deficits in rats [J]. Pathophysiology, 2013, 20(4): 263-7.
[5] Jamialahmadi K, Arasteh O, Matbou Riahi M, et al. Protective effects of glucosamine hydrochloride against free radical-induced erythrocytes damage [J]. Environ Toxicol Pharmacol, 2014, 38(1): 212-9.
[6] Henrotin Y, Mobasheri A, Marty M, et al. Is there any scientific evidence for the use of glucosamine in the management of human osteoarthritis [J]. Arthritis Res Ther, 2012, 14(1): 201.
[7] McAlindon T E, LaValley M P, Gulin J P, et al. Glucosamine and chondroitin for treatment of osteoarthritis: a systematic quality assessment and meta-analysis[J]. JAMA, 2000, 283(11):1469-75.
[8] 张伟滨, 庄澄宇, 李建民, 等. 盐酸氨基葡萄糖治疗骨性关节炎有效性与安全性评价[J]. 中华外科杂志, 2007, 45(14): 998-1001. Zhang W B, Zhuang C Y, Li J M, et al. Efficacy and safety evaluation of glucosamine hydrochloride in the treatment of osteoarthritis[J]. Chin J Surg, 2007, 45(14): 998-1001.
[9] 张敬茹, 于小桐, 孙宁, 等. 桑黄素和乙酰化白藜芦醇对沙奎那韦在大鼠体内药代动力学的影响[J]. 中国药理学通报, 2017, 33(10): 1414-20. Zhang J R,Yu X T, Sun N, et al. Effects of co-administration with morin and acetyl-resveratrol on pharmacokinetics of saquinavir in rats [J]. Chin Pharmacol Bull, 2017, 33(10): 1414-20.
[10] 卫平, 陈飞龙, 马钦海, 等. 麻黄-桂枝配伍对麻黄类生物碱、桂皮酸及桂皮醇在大鼠体内药动学的影响[J].中国药理学通报, 2016, 32(6): 873-80. Wei P, Chen F L, Ma Q H, et al. Effects of combined administration of Ephedrae-Cinnamomi on pharmacokinetics of ephedra alkaloids,cinamic acid and cinamic alcohol in rats [J]. Chin Pharmacol Bull, 2016, 32(6): 873-80.
[11] Beaudry F, Vachon P. Determination of glucosamine in horse plasma by liquid chromatography tandem mass spectrometry [J]. Biomed Chromatogr, 2008, 22(1): 1-4.
[12] 王大利, 耿成燕, 姜丽平, 等. 关节软骨及骨破坏模型大鼠经盐酸氨基葡萄糖干预的最佳剂量[J]. 中国组织工程研究与临床康复, 2011, 15(28): 5145-8. Wang D L, Geng C Y, Jiang L P, et al. Minimal effective dose of glucosamine hydrochloride on experimental arthritis in rats [J]. J Clin Rehabilit Tiss Eng Res, 2011,15(28): 5145-8.
[13] Sumino T, Ryu J, Seki M, et al. Effect of long-term oral administration of glucosamine hydrochloride and chondroitin sulfate on the progression of cartilage degeneration in a guinea pig model of spontaneous osteoarthritis [J]. Med J Nihon Univ, 2004, 63: 458-67.
[14] Kucharz E J, Kovalenko V, Szántó S. A review of glucosamine for knee osteoarthritis: why patented crystalline glucosamine sulfate should be differentiated from other glucosamines to maximize clinical outcomes [J]. Curr Med Res Opin, 2016, 32(6): 997-1004.