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Method of the administration of drugs with binding affinity for plasma protein and preparation to be used in the methodRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Radionuclide Or Intended Radionuclide Containing; Adjuvant Or Carrier Compositions; Intermediate Or Preparatory Compositions, Attached To Antibody Or Antibody Fragment Or Immunoglobulin; DerivativeMethod of the administration of drugs with binding affinity for plasma protein and preparation to be used in the method description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20060140857, Method of the administration of drugs with binding affinity for plasma protein and preparation to be used in the method. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This is a divisional of application Ser. No. 10/018,745, which was the National Stage of International Application No. PCT/JP00/04039, filed Jun. 21, 2000, the entire disclosures of the prior applications being hereby incorporated by reference. TECHNICAL FIELD [0002] The present invention relates to a method of the administration of drugs with binding affinity for plasma protein and drugs regulating the effective ingredient dose of drugs with binding affinity for plasma protein; and a pharmaceutical preparation whereby the effective ingredient dose of drugs with binding affinity for plasma protein is regulated. BACKGROUND ART [0003] Generally, drugs administered for the purpose of medical treatment or diagnosis once go through the systemic blood circulation, and then take the process of absorption, distribution, metabolism, excretion and the like. In the process of absorption and distribution, the drug moves along on flow of the blood, while it transfers to each spaces of intravascular, interstice and intracellular by diffusion and transportation of a free drug being in the state of unbound form with proteins, and finally the drug arrives at the active region of target. When movement of the drug reaches a steady state, then the free drug concentration in each space become uniform, thus the whole pattern of the concentration of the drug is determined by the binding level with proteins. Hence, in accordance with the property, a drug in vivo, may partially exists in the form of reversible binding state with biopolymers such as plasma proteins. Generally, drugs permeable through capillary wall or cell membrane are free drugs, therefore, the transfer of such free drugs being unbound with plasma proteins to the active region of target may be greatly influenced by the binding level with plasma proteins. [0004] For example, mercaptoacetylglycylglycylglycine labeled with 99m-technetium (.sup.99mTc-MAG.sub.3) is widely used in renal scintigraphy, especially the renal plasma flow can be effectively exhibited by its efficient renal extraction and renal tubular secretion. It is known that about 90% of .sup.99mTc-MAG.sub.3 binds to plasma protein in an ordinary clinical dose (Bubeck B. et al., J. Nucl. Med., 31, 1285-1295, 1990). If the binding of .sup.99mTc-MAG.sub.3 with plasma protein is inhibited by drugs having high binding affinity to the same binding site on protein with .sup.99mTc-MAG.sub.3, then more clear renal imaging can be obtained in the earlier stage after the administration, thus it may be thought that the dose of radioactivity to the patient can be reduced at the same time. [0005] On the contrary, if the binding of drugs with plasma protein is increased, then the concentration of the free drugs in the blood can be kept in lower level for long period, therefore, it may be possible to achieve continuous appearance of pharmacological effects. [0006] However, at the present stage, little is known as the research work for improving therapeutic effect or diagnostic effect of the drugs by regulating the concentrations of the free drugs, using the binding affinity of the second drug with plasma proteins. DISCLOSURE OF THE INVENTION [0007] In consideration of the above-mentioned problems, an object of the present invention is to provide a suitable method of the administration of drugs by regulating the binding affinity of the drug for plasma proteins, and at the same time, to provide a pharmaceutical preparation whereby the binding affinity of the drug for plasma protein can be regulated. [0008] According to the present invention, the suitable administration of the drugs can be achieved by regulating the binding affinity of the drug for plasma protein, and at the same time, a pharmaceutical preparation for such administration can be provided. [0009] The present invention relates to a method of administration of drugs with binding affinity for plasma protein, characterized by regulating the binding affinity of the first drug for plasma protein, when administering the first drug with the binding affinity for plasma protein, the second drugs, which have the binding affinity for the same plasma protein, for which the first drug has binding affinity, is administered simultaneously with the first drug or before or after the administration of the first drug. [0010] Particularly, in the case of regulating the binding affinity of the first drug for plasma protein, it is preferable that the first drug and the second drugs bind to the same binding sites on the plasma protein. Further, the second drug may be administered before, after or simultaneously with the administration of the first drug, and such administration timing of the second drug can be suitably selected in connection with the timing when the free drug concentration of the first drug reaches to the level so as to obtain an adequate effect. Additionally, a single drug may be used as the second drug, or plural drugs may be used as the second drugs when synergistic effect can be expected. [0011] In case of administering the first drug and the second drug simultaneously, the pharmaceutical preparations comprising the first drug and the second drug may be supplied. Further, the first drug and the second drug may be filled in a container separately, and may be supplied as a kit form. In case of such a kit form with separate containers, they may be administered simultaneously by mixing it together when used, or each one of the first drug and the second drug can be administered in different times separately or by different route. Furthermore, both of or either one of these first and second drugs may be commercially available pharmaceuticals. [0012] When the first drug is radiodiagnosic agent for in vivo use or radiotherapeutic drug for in vivo use, the radioactive nuclides can be selected from the group comprising 11-carbon (.sup.11C), 15-oxygen (.sup.15O), 18-fluorine, (.sup.18F), 32-phosphorus (.sup.32p) , 59-iron (.sup.59Fe), 67-copper (.sup.67Cu), 67-gallium (.sup.67Ga), 81m-krypton (.sup.81mKr), 81-rubidium (.sup.81Rb), 89-strontium (.sup.89Sr), 90-yttrium (.sup.90Y), 99m-technetium (.sup.99mTc), 111-indium (.sup.111In), 123-iodine (.sup.123I), 125-iodine (.sup.125I), 131-iodine (.sup.131I), 133-xenon (.sup.133Xe), 117m-tin (.sup.117mSn), 153-samarium (.sup.153Sm), 186-rhenium (.sup.186Re) , 188-rhenium (.sup.188Re), 201-thallium (.sup.201T1) , 212-bismuth (.sup.212Bi), 213-bismuth (.sup.213Bi) and 211-astatine (.sup.211At). [0013] In this case, compounds, such as chelating group or receptor ligand, of the first drug labeled with the above-mentioned nuclides can be selected from bisaminothiol or its derivatives, monoaminomonoamidobisthiol or its derivatives, bisamido-bisthiol or its derivatives, mercaptoacetylglycylglycyl-glycine or its derivatives, hexamethylpropylene-amineoxime or its derivatives, ethylenebis[bis(2-ethoxyethyl)phosphine](tetrofosmin) or its derivatives, 2,3-dimercaptosuccinic acid or its derivatives, ethylenecysteine dimer derivatives, methoxyisobutylisonitrile derivatives, polyamine derivatives, pyridoxylydeneaminate derivatives, methylene diphosphonate, hydroxymethylene diphodphonate derivatives, .beta.-methyl-.omega.phenylpentadecanoic acid or its derivatives, N-isopropyl-amphetamine, hippuric acid, benzylguanidine, tropane derivatives and the like. [0014] The second drug may be selected from, for example, bucolome, cefazolin, etoposide, phenylbutazone, aspirine, salicylic acid, cefatriaxone, sulfamethizole, valproic acid, nabumetone, 6-methoxy-2-naphtyl acetic acid, ibuprofen, probenecid, dansyl-L-asparagine (DNSA), verapamil or disopyramide and the like. BRIEF DESCRIPTION OF THE DRAWINGS [0015] FIG. 1 shows the free fraction of .sup.99mTc-MAG.sub.3 in human plasma in the presence of site specific agent. [0016] FIG. 2 shows the free fraction of .sup.99mTc-MAG.sub.3 in rat plasma in the presence of site specific agent. [0017] FIG. 3 shows the effect of bucolome on blood clearance of .sup.99mTc-MAG.sub.3 in rat. [0018] FIG. 4 shows the effect of bucolome on the free fraction of .sup.99mTc-MAG.sub.3 in rat blood after administration of bucolome. [0019] FIG. 5 shows the effect of bucolome on the accumulation of .sup.99mTc-MAG.sub.3 in rat kidney after administration of bucolome. [0020] FIG. 6 shows the effect of bucolome loading on the biodistribution of .sup.99mTc-MAG.sub.3 in rat. Continue reading about Method of the administration of drugs with binding affinity for plasma protein and preparation to be used in the method... Full patent description for Method of the administration of drugs with binding affinity for plasma protein and preparation to be used in the method Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Method of the administration of drugs with binding affinity for plasma protein and preparation to be used in the method patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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