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�й�ҩѧ��־ 2012, Vol. 47 Issue (4) :296-302     DOI:
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Department of Pharmacy�� Huashan Hospital�� Fudan University�� Shanghai 200040��China

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ժҪ Ŀ�� ���۹�������Ī˾��������������Ī˾�ڷ�Һ���й������������ڵ������Ч�ԡ����� ��ѡ22�����Խ���־Ը�ߣ�������浥����po����Ī˾���һ�����Ī˾�ڷ�Һ5 mg��Һ�����÷��ⶨȫѪ������Ī˾Ũ�ȡ���� ����Ī˾���Ҽ��ڷ�Һ��ҩ��ѧ�����ֱ����£���max�ֱ�Ϊ(26.62��9.97)��(25.28��5.98) ng��mL-1��tmax�ֱ�Ϊ(2.27��0.55)��(1.91��2.33) h��t1/2�ֱ�Ϊ(73.07��13.81)��(65.49��17.00) h��AUC0-t�ֱ�Ϊ(372.3��146.2)��(368.2��275.0) ng��h��mL-1��AUC0-���ֱ�Ϊ(466.8��194.3)��(442.3��324.4) ng��h��mL-1������������ö�F0-t (112.4��34.61)%��F0-��(117.2��39.93)%����˫����t����ȷ�ϣ�2���Ƽ�����max��AUC0-t��AUC0-������Ч���Dz����������������ҩ����Ī˾���ҵ�tmax�Ȳαȿڷ���Һ���������Բ��죨P<0.05�������� ��tmax�⣬��������Ī˾��������������Ī˾�ڷ�Һ����max��AUC0-t�����Ч��
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Abstract�� OBJECTIVE To evaluate the bioequivalence of domestic sirolimus capsules and commercially available sirolimus oral solution in healthy Chinese volunteers. METHODS Twenty-two healthy Chinese male volunteers were enrolled and orally administered 5 mg sirolimus capsules or oral solution randomly. The concentrations of sirolimus in whole blood were determined by LC-MS/MS. RESULTS The pharmacokinetic parameters of sirolimus capsules and oral solution were as following�� ��max (26.62��9.97) and (25.28��5.98) ng�� mL-1��tmax (2.27��0.55) and (1.91��2.33) h��t1/2 (73.07��13.81) and (65.49��17.00) h��AUC0-t (372.3��146.2) and (368.2��275.0) ng��h��mL-1��AUC0-�� (466.8��194.3) and (442.3��324.4) ng��h��mL-1�� respectively. The relative bioavailability F0-t was (112.4��34.61)% and F0-�� was (117.2��39.93)%. Two-sided t-test of ��max�� AUC0-t and AUC0-�� indicated that the preparations were equivalent�� and non-parametric test showed that sirolimus capsules had larger tmax than the reference preparation with a significant difference (P<0.05). CONCLUSION The domestic sirolimus capsule is bioequivalent to the marketed sirolimus oral solution with significantly different tmax.
Keywords�� sirolimus,   pharmacokinetics,   bioequivalence     
�ո�����: 2011-05-30;
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.����Ī˾�����������ڵ������Ч������[J]  �й�ҩѧ��־, 2012,V47(4): 296-302
.Evaluation of Bioequivalence of Sirolimus Capsules in Healthy Chinese Male Volunteers[J]  Chinese Pharmaceutical Journal, 2012,V47(4): 296-302
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