药物动力学的肠溶半胱胺酒石酸氢盐在健康成人:一个试点研究。

文章的细节

引用
复制到剪贴板

施奈德Gangoiti JA,费德勒M,卡布瑞拉提单,是的,Barshop英航,Dohil R

药物动力学的肠溶半胱胺酒石酸氢盐在健康成人:一个试点研究。

Br中国新药杂志。2010年9月,70 (3):376 - 82。doi: 10.1111 / j.1365-2125.2010.03721.x。

PubMed ID
20716238 (在PubMed
]
文摘

已知的关于这一主题:半胱胺酒石酸氢盐终身,每6 h和胱氨酸病的治疗。最近的研究使用半胱胺对其他疾病,如神经退行性疾病对半胱胺采用相同的给药方案。常规的半胱胺酒石酸氢盐(Cystagon)可能导致一些患者上消化道症状。这个研究补充道:这是唯一提供药代动力学数据的研究半胱胺在正常人enteric-release准备交付。EC-cysteamine非常良好的耐受性,不会引起胃泌激素浓度增加,即使在相对高剂量。EC-cysteamine在高剂量结果更好的药物吸收以Cmax AUC,更有可能是有效的。目的:半胱胺酒石酸氢盐(Cystagon)是通过胱氨酸病治疗。可怜的遵从性和病人可能发生的结果,因为药物需要每6 h和在一些病人由于hypergastrinaemia引起胃肠道症状。半胱胺的配方要求每天两次摄入会改善这些患者的生活质量。本研究比较了药物动力学及胃泌激素生产后半胱胺酒石酸氢盐non-enteric-coated和半胱胺酒石酸氢盐肠衣在正常健康的主题。 METHODS: Enteric-coated cysteamine was prepared. Following single doses of cysteamine bitartrate non-enteric-coated 450 mg and cysteamine bitartrate enteric-coated 450 mg and 900 mg, serial plasma cysteamine and gastrin concentrations were measured. Two subjects also received cysteamine bitartrate non-enteric-coated 900 mg. Gastrointestinal (GI) symptoms were recorded. RESULTS: Six healthy adults (mean age 20.7 years, range 18-24 years; mean weight 59.3 kg) received drug. All post-dose gastrin concentrations were within the normal range (<100 pg ml(-1)). The tmax following cysteamine bitartrate non-enteric-coated (mean and SD is 75+/-19 min) was shorter than cysteamine bitartrate enteric-coated (220+/-74 min) (P=0.001), but only the Cmax and AUC estimates following 900 mg cysteamine bitartrate enteric-coated were significantly greater than any of the other preparations or doses (P<0.05). One patient had GI symptoms following both 900 mg cysteamine bitartrate non-enteric-coated and cysteamine bitartrate enteric-coated. CONCLUSION: Although patient numbers were low, single high doses of cysteamine bitartrate enteric-coated were better tolerated than similar doses of cysteamine bitartrate non-enteric-coated in the healthy subjects and all had normal gastrin concentrations. The delayed tmax following cysteamine bitartrate enteric-coated suggested that the cysteamine was released enterically.

DrugBank数据引用了这篇文章

药物