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�й�ҩѧ��־ 2013, Vol. 48 Issue (6) :446-449    DOI: 10.11669/cpj.2013.06.012
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1���ӱ�ʡ�Ƽ����̼����о�����,ʯ��ׯ 050035;2��ʯҩ����������ҩ������ʯ��ׯ���޹�˾,ʯ��ׯ 050035;3�� ����ҩ���Ƽ��븨�Ϲ����ص�ʵ����,ʯ��ׯ 050035;4������ʡҽ����е������,�Ͼ� 210013
ZHANG Lan1,2,3, LI Yan-hui1,2,3, WANG Cai-xia1,2,3, HAO Xiao-fang4, XIU Xian1,2,3, WEI Na1,2,3, LI Chun-lei1,2,3*
1 Hebei Pharmaceutical Technology and Engineering Research Center,Shijiazhuang 050035,China; 2 CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co ,Ltd,Shijiazhuang 050035,China; 3 State Key Lab of Novel Pharmaceutical Preparations and Excipients,Shijiazhuang 050035,China; 4 Jiangsu Institute for Medical Equipment Testing,Nanjing 210013,China

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ժҪ Ŀ�� �Ʊ���ɼ��֬���岢���������ʡ����Լ�ҩЧѧ���г����о������� ��������֬��soybean Phosphatidylcholine,SPC�����໯��֬���Ҵ�����mPEG2000-DSPE������ɼ����100��0.5��5��Ħ���ȣ���ϲ��ܽ����ȷ���,������ˮ����ĥ����,Ȼ���ѹ���ʵķ����Ʊ�֬���塣���õ������ķ��ⶨ������,��̬��ɢ�䷨�ⶨ���ȷֲ�,KM����ж���ʵ��,H22/KMС��Ϊģ�ͽ���ҩЧʵ�顣��� ֬����ƽ������Ϊ��140±10�� nm;ҩ֬Ħ������3%��6%�ڰ����ʾ�����95%;����ʵ�����,��ɼ��֬���壨Pac-lipo������ɼ������ҩ��Pac-free����KM����С���������ܼ�����MTD���ֱ�Ϊ64.8��29.4 mg·kg-1;ҩЧʵ�����,��ɼ��֬������������Ե�������ΰ�H22�������������� ��ɼ��֬������нϸ߰�����,����ɼ������ҩ��ȿ��������������ָ����
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Abstract�� Objective To prepare the paclitaxel liposomes and evaluate its physicochemical property,toxicity and pharmacodynamics. METHODS SPC,mPEG2000-DSPE and paclitaxel were dissolved in chloroform in a mole ratio of 100:0.5:5. Oil phase and water phase were mixed and skived. The emulsion was homogenized to form liposomes. The mean diameter of liposomes was determined by dynamic light scattering (DLS) techniques. Low-speed centrifugation was employed to determine encapsulation efficiency (EE). The maximum tolerated doses (MTD) was determined in normal KM mice,and antitumor effect was evaluated in H22/KM mice xenograft tumor model. RESULTS The mean diameter of paclitaxel liposomes was ��140±10�� nm. The EE was over 95 % when the molar ratio of paclitaxel to SPC ranged from 3% to 6%. The MTDs of Pac-lipo and Pac-free in male KM mice were 64.8 and 29.4 mg·kg-1,respectively. Pac-lipo inhibited H22 tumor weight dose-dependently��CONCLUSION Pac-lipo had a high EE,and could increase the therapeutic index significantly,compared with Pac-free.
Keywords�� paclitaxel ,   liposome ,   maximum tolerated dose ,   pharmacodynamics     
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ͨѶ���� ���,��,��ʿ �о�����ҩ���¼������¼��� Tel����0311��67808803 E-mail�� lchunlei@mail.ecspc.com��ɼ��֬������Ʊ����������ԡ�ҩЧѧ�о� ����1     Email: lchunlei@mail.ecspc.com
���߼��: ����,Ů,˶ʿ �о�����ҩ���¼������¼��� ͨѶ���ߣ����,��,��ʿ �о�����ҩ���¼������¼��� Tel����0311��67808803 E-mail�� lchunlei@mail.ecspc.com
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����, , ������� .��ɼ��֬������Ʊ����������ԡ�ҩЧѧ�о�[J]  �й�ҩѧ��־, 2013,V48(6): 446-449
ZHANG Lan-, , LI Yan-Hui- etc .Preparation of Liposomal Paclitaxel and Its Toxicity and Antitumor Effect[J]  Chinese Pharmaceutical Journal, 2013,V48(6): 446-449
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