max為(2 148.22±448.5) ng/mL,AUC0-t為(660.21±96.47) h·μg/mL。環(huán)酯紅霉素原料藥肺部給藥后,達峰時間為0.09 h,與iv給藥相當,而Cmax(231.54±177.19) ng/mL和0-t 29.37±27.08) h·μg/mL較iv組顯著降低(P<0.05),其絕對生物利用度僅為3.72%。納米晶肺部給藥后,達峰時間為0.14 h,與原料藥iv給藥相比顯著延長(P<0.05);納米晶肺部給藥的Cmax為(1 958.34±1 209.41) ng/mL,AUC0-t為(773.11±473.49) h·μg/mL,均與iv給藥相當,而顯著高于原料藥肺部給藥(P<0.05);其絕對生物利用度為117.10%。結論大鼠肺部給藥環(huán)酯紅霉素納米晶后可明顯提高環(huán)酯紅霉素的生物利用度,提示納米晶用于肺部制劑的可行性。;Objective Investigate the pharmacokinetics of erythromycin cyclic 11, 12-car-bonate nanocrystals for pulmonary administration and investigate the characteristics of pulmonary administration. Methods A liquid chromatography tandem mass spectrometry (LC-MS/MS) method was established for the determination of erythromycin cyclic 11, 12-car-bonate in human plasma, the specificity, precision, accuracy and stability, extraction recovery were investigated. SD rats were was injected 15 mg/kg of erythromycin cyclic 11,12-car-bonate. At the same time,15 mg/kg of pure drug and nanocrystals were delivered by the lungs. Blood was taken from the orbit at 0.033, 0.083, 0.167, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8 h after administration, and the level of erythromycin cyclic 11,12-car-bonate content in the rat plasma was measured. By analyzing the pharmacokinetics, the bioavailability improvement of erythromycin cyclic 11, 12-car-bonate nanocrystals for pulmonary administration was evaluated. Results The chromatographic column was ACQUITY UPLC HSS T3 1.8 m (100 mm×2.1 mm); the mobile phase was 5 mmol/L ammonium acetate solution (0.02% formic acid)-methanol (0.02% formic acid) (85 : 15); volume flow 0.3 mL/min; electrospray ion source (ESI), positive ion mode multi reaction monitoring (MRM).The methodology tests of LC-MS/MS was all for compliance with the test requirements. The peak time was 0.03 h, Cmax was (2 148.22 ±448.5) ng/mL, AUC0-t was (660.21 ±96.47) h·μg/mL of erythromycin cyclic 11, 12-car-bonate iv group. After lung administration, the peak time of erythromycin cyclamate was 0.09 h, which was equivalent to iv administration. Cmax (231.54 ±177.19) ng/mL and AUC0-t (29.37 ±27.08) h·μg/mL were significantly lower than those in iv administration group (P < 0.05), and its absolute bioavailability was only 3.72%. After erythromycin cyclic 11, 12-car-bonate nanocrystals lung administration, the peak time was 0.14 h, which was significantly longer than that of iv administration (P < 0.05); the Cmax and AUC0-t of lung administration were (1 958.34 ±1 209.41) ng/mL and (773.11 ±473.49) h·μg/ mL, which were equivalent to iv administration, but significantly higher than API of lung administration (P < 0.05); the absolute bioavailability was 117.10%. Conclusion After pulmonary administration in rats, the bioavailability of erythromycin cyclic 11,12-car-bonate nanocrystals can be significantly improved, suggesting the feasibility of erythromycin cyclic 11, 12-car-bonate for pulmonary preparations."/>

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首頁 > 過刊瀏覽>2021年第44卷第4期 >2021,44(4):762-766. DOI:10.7501/j.issn.1674-6376.2021.04.013
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環(huán)酯紅霉素納米晶的大鼠肺部噴霧給藥藥動學研究

Pharmacokinetics of erythromycin cyclic 11, 12-car-bonate nanocrystals pulmonary administration

發(fā)布日期:2021-04-07
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