In this study a new intravenous (i.v.) bolus dosage form of doxycycline was prepared by electrospinning. A tetracycline-type antibiotic with low water solubility (doxycycline (DOX)) was used with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) as solubilizer. The new solid formulation could be produced with high (~80 g/h) productivity rate using high-speed electrospinning (HSES) from a water-based precursor solution. Freeze-dried DOX-HP-β-CD was also prepared from the same precursor solution as HSES for comparison. Raman mapping showed that the amorphous DOX was uniformly distributed in the fibrous powder making precise dosing of the API possible. The new formulation's viability as an i.v. bolus product was examined with reconstitution test. The samples contained 100 mg of pure DOX (similarly to the products currently on the market). To ensure i.v. bolus applicability, the dissolution was carried out in 1.5 mL water. The final DOX concentration was 66.7 mg/(mL solvent), which is 7 times higher than the currently marketed formulation. The drug release was followed by UV-VIS spectrophotometry. The results confirmed that the reconstitution solution could be applied as an i.v. bolus dosage form. Moreover, the work confirmed that the continuous high-speed electrospinning process can be a viable high productivity alternative to freeze-drying.

译文

:在这项研究中,通过静电纺丝制备了一种新的多西环素静脉内(静脉)推注剂型。将水溶性低的四环素类抗生素(强力霉素(DOX))与2-羟丙基-β-环糊精(HP-β-CD)一起用作增溶剂。新的固体配方可以使用高速前纺(HSES)从水基前体溶液中以高(〜80 g / h)的生产率生产。还从与HSES相同的前体溶液中制备了冻干的DOX-HP-β-CD,用于比较。拉曼作图表明,无定形的DOX均匀地分布在纤维粉末中,从而使API的精确定量成为可能。新配方的i.v.推注产品经重构试验检查。样品中含有100 mg的纯DOX(类似于当前市场上的产品)。为了确保i.v.推注适用性,在1.5 mL水中溶解。最终的DOX浓度为66.7 mg /(mL溶剂),比目前市场上出售的制剂高7倍。药物释放后用UV-VIS分光光度法测定。结果证实,该重构溶液可以作为静脉注射应用。推注剂型。此外,这项工作证实,连续高速静电纺丝工艺可以替代冷冻干燥,是一种可行的高生产率方法。

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