PACLITAXEL INJECTION COMPOSITION HAVING ULTRAFINE PARTICLE SHAPE PREPARED BY MIXING PACLITAXEL, SOLID LIPID AND STABILIZER AT ROOM TEMPERATURE TO IMPROVE SOLUBILIZING PROPERTY AND STABILITY OF PACLITAXE

摘要

PURPOSE: A paclitaxel injection composition having a shape of ultrafine particles is provided which is prepared in the by mixing paclitaxel, solid lipids as a carrier and a stabilizer at room temperature to improve the solubilizing property and stability of paclitaxe. The composition has a particle size of 100 to 500nm, is intravenously injectable and very stable when stored at room temperature and hardly causes adverse side effect of Cremophor EL as an injection formulation. CONSTITUTION: The paclitaxel injection composition contains: 0.1 to 5% by weight of paclitaxel; 1 to 20% by weight of one or more solid lipids selected from tricaprin, trilaurin, trimyristin, tristearin and tripalmitin; 1 to 10% by weight of one or more stabilizers selected from polyethyleneglycol-modified phospholipid, lecithin and poloxamer; and 40 to 80% by weight of water. The poloxamer is one or more selected from P188, P237, P338 and P407. The polyethyleneglycol-modified phospholipid is one or more selected from 1,2-diacyl-sn-glycero-3-phosphatidyl ethanolamine-N-(poly(ethyleneglycol) 2000) or 1,2-diacyl-sn-glycero-3-phosphatidyl ethanolamine-N-(poly(ethyleneglycol) 5000).