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Compound medicine screening method, obtained medicines and application thereof

A screening method and drug technology, applied in the field of medicine, to achieve the effects of reducing toxicity, reducing costs and the burden of public medical care, and reducing production and manufacturing costs

Inactive Publication Date: 2012-08-15
程宇镳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A basic premise of such a drug screening mode is to find few monomeric drugs with suitable physical and chemical parameters, toxicological properties, pharmacodynamic parameters and pharmacokinetic parameters from thousands of compounds. In the R&D model, no one doubts whether this premise is always taken for granted

Method used

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  • Compound medicine screening method, obtained medicines and application thereof
  • Compound medicine screening method, obtained medicines and application thereof
  • Compound medicine screening method, obtained medicines and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0079]The sulfonylureas are: gliclazide, glipizide, gliquidone, glimepiride, and glibenclamide. Their hypoglycemic mechanism includes stimulating the islet β cells to secrete insulin in time, that is, by stimulating the secretion of insulin, rather than increasing the synthesis of β cell insulin; therefore, sulfonylurea hypoglycemic drugs should generally be taken before meals; The ureide group is the pharmacophore that the drug acts on. They all have the same core structure.

[0080] 1. Mechanism of STZ-induced diabetes in animals

[0081] The chemical name of streptozotocin is 2-deoxy-2 (3-methyl-3-nitrosoureido) D-glucopyranose. The nitrosourea in the structure is cytotoxic, and the deoxyglucose part makes it easy to enter the β-cell. The α-isomer of STZ has higher toxicity and may have a higher affinity with the glucose receptor on the β-cell membrane. If the glucose moiety was removed, the specific toxicity to β cells was significantly reduced. STZ damages β cells thro...

experiment example 2

[0110] Experimental example 2-clinical case

[0111] Case 1: Male, 30 years old, with fever, dizziness, nausea and vomiting, blood leukocytes 1.7×109 / L, oral administration of ofloxacin, 200 mg / time, divided into 3 times, for 3 consecutive days, the effect is not good, High fever recurred; loss of appetite, and then changed to oral administration of pefloxacin at a dose of 200 mg / time, divided into 2 times, for 3 consecutive days, nausea and vomiting, high fever still recurred.

[0112] Adjust the treatment plan, take ofloxacin and pefloxacin mixed oral administration, the dose is 100 mg / time, divided into 3 times, take the medicine for 1 day, the high fever stops, the appetite recovers, and the drug is stopped after another 3 days After one week of follow-up, all signs returned to normal, and there was no recurrence and adverse signs after another month of follow-up.

[0113] Case 2: Female, 30 years old, had repeated colds, fever of 39.1 degrees, and cough. Conventional do...

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Abstract

The invention belongs to the field of medicines and provides a medicine screening method and relative medicines, a medicine package, a sustained release preparation, a targeting preparation, a controlled release preparation, a quick release preparation and a treatment method. The medicine screening method provided by the invention is used for screening compounds with the same parent nucleus (or the same framework) in a combined manner, wherein the compounds include synthetic compounds and bio-transformed compounds but not include compounds contained in organisms. The compounds only refer to the compounds with the same structural formula, and chemical isomers with the same molecular formula are regarded as one compound. The screening method does not comprise a step of screening the compounds with the same parent nucleus which are obtained through combinatorial chemistry. The medicine screening method, the obtained medicines and the application thereof provided by the invention have the advantages as follows: 1, combinations of chemicals in hundreds of years are retrospectively studied, thereby improving the medicine screening purposiveness and reducinig the development cost and the societal public burden; 2, the treatment effect is improved, and the toxic and side effects are reduced; and 3, the research dimensionality of the quantitative structure-activity relationship (QSAR) is widened.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a drug screening method, a drug, a drug packaging combination, a sustained-release preparation, a controlled-release preparation, a targeting preparation, an immediate-release preparation and a disease treatment method. Background technique [0002] The global pharmaceutical market is mainly composed of chemical drugs, which account for more than 80% of the market share, and the rest are biological drugs and natural drugs. In developed countries in Europe and the United States, the best-selling branded drugs are chemical drugs and biological drugs. [0003] Once the research and development of new drugs is successful, the rewards are very amazing. In recent years, a large number of brand-name drug patents have expired, driving the rapid growth of the generic drug market. Most of the most powerful drugs in the global pharmaceutical market today are chemical drugs developed in...

Claims

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Application Information

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IPC IPC(8): G01N33/15A61K45/00A61K9/00
Inventor 程宇镳乔爱娴
Owner 程宇镳
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