Ciprofloxacin is a broad-spectrum antibiotic that is proposed for pulmonary administration. In this work micronization of ciprofloxacin was performed by the Supercritical Antisolvent Technique (SAS) using ciprofloxacin base (CIP) in ethanol/acetic acid and ciprofloxacin hydrochloride salt (CIP·HCl) in methanol at 40–60 ºC and 100–150 bar. Yields ranged from 40 % to 90 %. CIP precipitated incorporating acetate whilst CIP·HCl precipitated as the AH1 anhydrous form. CIP and CIP·HCl particles exhibited an acicular morphology (0.2–0.9 μm wide × 1–4 μm long). Micronization adding lactose, PVP K-10 and K-30 modified the precipitate morphology. CIP·HCl:lactose and CIP·HCl:PVP K-30 at a 4:1 drug:excipient mass ratio precipitated like flakes. CIP·HCl:PVP K-10 precipitated as submicron globular particles suitable for oral formulation. Increasing the PVP content, the morphology changed to sheets and flakes, which could be used for pulmonary administration. The antibacterial activity of the samples for Staphylococcus epidermidis was confirmed.

中文翻译：

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通过超临界反溶剂 （SAS） 技术对环丙沙星进行微粉化


环丙沙星是一种广谱抗生素，建议用于肺部给药。在本研究中，使用乙醇/乙酸中的环丙沙星碱 （CIP） 和盐酸环丙沙星盐 （CIP·HCl） 在 40–60 ºC 和 100–150 bar 的甲醇中。产量从 40 % 到 90 % 不等。CIP 沉淀掺入乙酸盐，而 CIP·HCl 沉淀为 AH1 无水形式。CIP 和 CIP·HCl 颗粒表现出针状形态（0.2-0.9 μm 宽× 1-4 μm 长）。添加乳糖、PVP K-10 和 K-30 的微粉化改变了沉淀物形态。CIP·HCl：乳糖和 CIP·HCl：PVP K-30 以 4：1 的药物：赋形剂质量比沉淀成薄片。CIP·HCl：PVP K-10 沉淀为亚微米球状颗粒，适用于口服制剂。增加 PVP 含量，形态变为片状和片状，可用于肺部给药。证实了表皮葡萄球菌样品的抗菌活性。