医药发展肠外冻干aplidine的新抗肿瘤药剂的配方。
文章的细节
-
引用
复制到剪贴板 -
Nuijen B, Bouma M, Henrar再保险公司Floriano P,港务局JM, Talsma H, Kettenes-van窝博世JJ, AJ,布尔特,Beijnen JH
医药发展肠外冻干aplidine的新抗肿瘤药剂的配方。
54 PDA J制药Sci抛光工艺。2000 May-Jun; (3): 193 - 208。
- PubMed ID
-
10927911 (在PubMed]
- 文摘
-
Aplidine是地中海的天然循环depsipeptide孤立被囊类动物Aplidium白色的。Aplidine显示有前途的体外和体内抗肿瘤活动对各种固体人类肿瘤异种移植,因此开发了临床测试。本研究的目的是开发一个稳定的注射用药物的药品剂型为临床第一阶段测试。Aplidine原材料使用几个色谱和光谱技术的特点。这些实验表明,aplidine存在两个同分异构体。一个stability-indicating高效液相色谱法测定。溶解性测试表明aplidine展品非常贫穷的溶解度。因为随着aplidine显示大量退化在光和热压力测试条件下,它是决定开发一个冻干剂型。冷冻干燥法进行了500微克/毫升溶液在40% (v / v) tert-butanol aplidine注射用水(注射用水)包含25毫克/毫升D-mannitol作为填充剂。应用差示扫描量热法来确定最佳冻干周期参数。 The prototype, containing 500 micrograms aplidine and 25 mg D-mannitol per vial, was found to be the optimal formulation in terms of solubility, length of lyophilization cycle, and dosage requirements in the forthcoming Phase I clinical studies. Quality control of the freeze-dried formulation demonstrates that the manufacturing process does not affect the integrity of aplidine. The optimal reconstitution solution was found to be 15/15/70% (v/v/v) Cremophor EL/ethanol/WfI (CEW). Both reconstituted product and dilutions of the reconstituted product with normal saline (up to 1:100 v/v) appeared to be stable for at least 24 hours after preparation. Shelf-life data, available thus far, show that the lyophilized formulation is stable for at least 1 year when stored at +2-8 degrees C in the dark.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物