利用超临界反溶剂（SAS）技术微粉化环丙沙星

IF 3.4 3区工程技术 Q2 CHEMISTRY, PHYSICAL

Journal of Supercritical Fluids Pub Date : 2024-09-17 DOI:10.1016/j.supflu.2024.106413

Fouad Zahran , Pablo Marzal , Helga K. Ruiz , Eduardo Pérez , Lourdes Calvo , Albertina Cabañas

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引用次数: 0

摘要

环丙沙星是一种广谱抗生素，建议用于肺部用药。本研究采用超临界反溶剂技术（SAS），在 40-60 ºC 和 100-150 bar 的温度条件下，使用乙醇/乙酸中的环丙沙星碱（CIP）和甲醇中的环丙沙星盐酸盐（CIP-HCl）对环丙沙星进行微粉化。产率从 40 % 到 90 % 不等。CIP 以醋酸盐形式沉淀，而 CIP-HCl 则以 AH1 无水形式沉淀。CIP 和 CIP-HCl 颗粒呈现针状形态（宽 0.2-0.9 μm × 长 1-4 μm）。加入乳糖、PVP K-10 和 K-30 的微粉化改变了沉淀形态。CIP-HCl:lactose 和 CIP-HCl:PVP K-30 的药物与辅料质量比为 4:1，沉淀物呈片状。CIP-HCl:PVP K-10 以亚微米球状颗粒沉淀，适合口服制剂。随着 PVP 含量的增加，其形态变为片状和薄片状，可用于肺部给药。样品对表皮葡萄球菌的抗菌活性得到了证实。

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Micronization of ciprofloxacin by the Supercritical Antisolvent (SAS) Technique

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.

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来源期刊

Journal of Supercritical Fluids 工程技术-工程：化工

CiteScore

7.60

自引率

10.30%

发文量

236

审稿时长

56 days

期刊介绍： The Journal of Supercritical Fluids is an international journal devoted to the fundamental and applied aspects of supercritical fluids and processes. Its aim is to provide a focused platform for academic and industrial researchers to report their findings and to have ready access to the advances in this rapidly growing field. Its coverage is multidisciplinary and includes both basic and applied topics. Thermodynamics and phase equilibria, reaction kinetics and rate processes, thermal and transport properties, and all topics related to processing such as separations (extraction, fractionation, purification, chromatography) nucleation and impregnation are within the scope. Accounts of specific engineering applications such as those encountered in food, fuel, natural products, minerals, pharmaceuticals and polymer industries are included. Topics related to high pressure equipment design, analytical techniques, sensors, and process control methodologies are also within the scope of the journal.