INFLUENCE OF BLOOD PROTEINS ON BIOMEDICAL ANALYSIS. III. PHARMACOKINETICS AND PROTEIN BINDING OF GLICLAZIDE

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概要

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• Both pharmacokinetics of total and free gliclazide, a potential hypoglycemic drug, were studied in the healthy (n=12) and diabetic subjects (n=11). The blood level of gliclazide was determined by a high-performance liquid chromatography, and the free gliclazide (unbound to proteins) in the serum separated by means of an ultrafiltration. The binding ratio of gliclazide to the blood proteins was about 96% during the periods of 24hr after administration of the drug. Several pharmacokinetic parameters for the blood gliclazide were derived from the decay curves of the blood drug levels. Each pharmacokinetic parameter was not changed by differences between the healthy and diabetic subjects, the total and free drug levels, and the method of administration of the drug ; each mean parameter, the elimination rate (K_e), the time to peak level (t_<max>), the elimination half-life (t_<1/2>) and the volume of distribution (Vd_β) was 0.07 hr^<-1>, 2.8 hr, 12.3 hr and 16.4 1 (total level), respectively. The serum from healthy subject receiving orally administered gliclazide was gel-filtered on a Sephadex G-150 column. Each fractionated serum protein of macroglobulin (IgM), γ-globulin (IgG), albumin (A) and small molecular substances (F), contained gliclazide at average of 3.7,0.7,82.3 and 13.2%, respectively, during the periods of 24 hr after administration. In in vitro experiment, it was found that the ratio of gliclazide-albumin binding kept a constant level at 96.5% in the range of normal protein levels (3.3-4.8 g/100 ml). In conclusion, the present result shows that the pharmacokinetics of the total blood level of gliclazide reflect the free gliclazide level, moreover, gliclazide predominantly binds with albumin in the blood and its binding ratio is not constant, but variable according to the dose-relation between the drug and the serum protein.

• 公益社団法人日本薬学会の論文

著者

• MATSUOKA Akira

  Department of Clinical Pathology and Clinical Laboratories, Hyogo College of Medicine

• Kitani Yuko

  Faculty Of Pharmaceutical Sciences Mukogawa Women's University

• KIMURA Masako

  Department of Molecular Physiology, The Jikei University School of Medicine

• Kimura Masako

  Department Of Molecular Physiology Jikei University School Of Medicine

• Kimura Yukio

  Faculty Of Pharmaceutical Sciences Mukogawa Women's University

• KOBAYASHI KUNIO

  Department of Clinical Pathology and Clinical Laboratory, Hyogo College of Medicine

• SAKOGUCHI TAKAFUMI

  Department of Clinical Pathology and Clinical Laboratory, Hyogo College of Medicine

• KITANI YUKO

  Department of Clinical Pathology and Clinical Laboratory, Hyogo College of Medicine

• HATA MITSUO

  Department of Clinical Pathology and Clinical Laboratory, Hyogo College of Medicine

• Hata Mitsuo

  Department Of Clinical Pathology And Clinical Laboratory Hyogo College Of Medicine

• Kimura Y

  Mukogawa Women's Univ. Nishinomiya Jpn

• Sakoguchi Takafumi

  Department Of Clinical Pathology And Clinical Laboratory Hyogo College Of Medicine

• Matsuoka Akira

  Department Of Clinical Pathology And Clinical Laboratories Hyogo College Of Medicine

• Kobayashi Kunio

  Department Of Clinical Pathology And Clinical Laboratory Hyogo College Of Medicine

• Matsuoka Akira

  Department Of Clinical Labolatory And Clinical Pathology Hyogo College Of Medicine

• KIMURA Masako

  Department of Integrative Physiology, Kagawa Nutrition University

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