Effect of plasma protein and tissue binding on the biologic half-life of drugs

1978 ◽  
Vol 24 (1) ◽  
pp. 1-4 ◽  
Author(s):  
Milo Gibaldi ◽  
Gerhard Levy ◽  
Patrick J. McNamara
Keyword(s):  
Plasma Protein ◽  
Half Life ◽  
Tissue Binding

How Well Do Lipophilicity Parameters, MEEKC Microemulsion Capacity Factor, and Plasma Protein Binding Predict CNS Tissue Binding?

2012 ◽  
Vol 101 (5) ◽  
pp. 1932-1940 ◽  
Author(s):  
Maciej J. Zamek-Gliszczynski ◽  
Karen E. Sprague ◽  
Alfonso Espada ◽  
Thomas J. Raub ◽  
Stuart M. Morton ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Capacity Factor ◽  
Tissue Binding ◽  
Lipophilicity Parameters

Do We Need to Optimize Plasma Protein and Tissue Binding in Drug Discovery?

2011 ◽  
Vol 11 (4) ◽  
pp. 450-466 ◽  
Author(s):  
Xingrong Liu ◽  
Cuiping Chen ◽  
Cornelis E.C.A. Hop
Keyword(s):  
Drug Discovery ◽  
Plasma Protein ◽  
Tissue Binding

Rational Use of Plasma Protein and Tissue Binding Data in Drug Design

2014 ◽  
Vol 57 (20) ◽  
pp. 8238-8248 ◽  
Author(s):  
Xingrong Liu ◽  
Matthew Wright ◽  
Cornelis E. C. A. Hop
Keyword(s):  
Drug Design ◽  
Plasma Protein ◽  
Tissue Binding ◽  
Rational Use ◽  
Binding Data

Studies of the Metabolism of Asialotransferrins: The Mechanism for the Hypercatabolism of Human Asialotransferrin in the Rabbit

1974 ◽  
Vol 52 (7) ◽  
pp. 645-651 ◽  
Author(s):  
E. Regoeczi ◽  
M. W. C. Hatton
Keyword(s):  
Sialic Acid ◽  
Plasma Protein ◽  
Half Life ◽  
Hepatic Clearance ◽  
The Other ◽  
Human Transferrin ◽  
Human Control ◽  
Clearance Mechanism ◽  
Catabolic Process

The behavior in vivo of human asialotransferrin in rabbits was studied in such a manner as to permit a comparison of this catabolic process with the generalized hepatic clearance mechanism for asialoglycoproteins described by Ashwell and Morell.Progressive desialylation of human transferrin in the range 50–100% yielded transferrin molecules with circulation times inversely proportional to the loss of sialic acid. The shape of plasma protein-bound radioactivity curves indicated that treatment of transferrin with neuraminidase resulted in at least two types of asialo derivatives. The biological half-life of one of them was close to 60% of that of control transferrin and the other one disappeared from the plasma with a half-life of approximately 1.5–2.5 h. Oxidation of over 50% of the terminal galactosyl groups in human asialotransferrin prolonged the circulation time of asialotransferrin.Assays of tissue radioactivities following mixed injection of human control and asialotransferrins showed that the two proteins possessed the same affinity for lung, kidney, and spleen, but asialotransferrin was preferentially taken up by the liver.On the basis of these observations, it seems likely that the mechanism which has been claimed as a generalized pathway for the clearance of asialoglycoproteins is also responsible for the rapid elimination of heterologous human asialotransferrin in the rabbit.

scholarly journals Studies on the Metabolism of Fibrinogen in Two Patients with Congenital Afibrinogenemia

Blood ◽  
1953 ◽  
Vol 8 (8) ◽  
pp. 679-686 ◽  
Author(s):  
DAVID GITLIN ◽  
WAYNE H. BORGES
Keyword(s):  
Connective Tissue ◽  
Plasma Protein ◽  
Intravenous Administration ◽  
Half Life ◽  
Decay Curve ◽  
Blood Products ◽  
Biopsy Specimens ◽  
Congenital Afibrinogenemia ◽  
Logarithmic Decay

Abstract 1. The rate of disappearance from the plasma of intravenously administered fibrinogen has been studied immunochemically in two children with congenital afibrinogenemia. 2. About half of the administered fibrinogen disappeared from the circulation in the first forty-eight hours, thus emphasizing the importance of the extravascular pool of plasma protein. 3. After the first two days, the fibrinogen followed a logarithmic decay curve, with a half life of four days; this is so close to the half life of 5.6 days estimated from radioisotope turnover studies that it indicates that the fundamental defect in these patients is a failure to synthesize adequate quantities of fibrinogen. 4. Traces of fibrinogen were detected immunochemically in the plasma of each patient; in one of them, the small amount found could not readily be attributed to prior infusion of blood or blood products. 5. The connective tissue in biopsy specimens of skin and muscle from one patient, when examined with fluorescein-labelled antisera, was found to be specifically deficient in fibrinogen. This deficit was quickly rectified by intravenous administration of fibrinogen.

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