阅读说明：本技术 瑞德西韦在制备治疗糖尿病并发症药物中的应用 (Application of Rudesiwei in preparing medicine for treating diabetic complication ) 是由 崔庆华 周宛露 于 2021-01-19 设计创作，主要内容包括：本发明公开了瑞德西韦(Remdesivir)在制备治疗糖尿病并发症药物尤其是糖尿病肾病及心血管并发症中的应用。本发明证实了瑞德西韦作为糖尿病肾病及心血管并发症预防治疗药物的重大潜力,首次公开了瑞德西韦对糖尿病导致的各种并发症的良好疗效,为糖尿病肾病及其他并发症治疗提供了有效的新型潜在备选药物,扩展了瑞德西韦的适应证,极大的提高了瑞德西韦的应用潜力及市场前景。(The invention discloses application of Remdesivir (Remdesivir) in preparing a medicament for treating diabetic complications, in particular diabetic nephropathy and cardiovascular complications. The invention proves the great potential of the Reidesciclovir as a medicine for preventing and treating diabetic nephropathy and cardiovascular complications, discloses the good curative effect of the Reidesciclovir on various complications caused by diabetes for the first time, provides an effective novel potential alternative medicine for treating the diabetic nephropathy and other complications, expands the indications of the Reidesciclovir, and greatly improves the application potential and market prospect of the Reidesciclovir.)

1. Application of Rudexilvir in preparation of medicine for treating diabetic complications is provided.

2. The use according to claim 1, wherein the Reidesciclovir is useful for the prophylactic treatment of diabetic nephropathy.

3. The use according to claim 1, wherein the Reidesciclovir is useful for the prophylactic treatment of cardiovascular complications of diabetes.

4. The use according to claim 3, characterized in that said cardiovascular pathologies comprise coronary heart disease, atherosclerosis, hyperlipidemia, hypercholesterolemia, etc.

5. Use according to claim 1, wherein the medicament is in the form of a free form or a pharmaceutically acceptable compound of Reidesvir.

6. The use according to claim 1, wherein the effective dose of Reidesciclovir in the medicament is: the weight standard of an adult is set as 60kg, and the effective dose of the adult is 12.5-500 mg per day.

7. The use according to claim 6, wherein the effective dose of Reidesciclovir in the medicament is: the adult weight standard is set as 60kg, and the effective dose of the adult is 100 mg-200 mg per day.

8. The use according to claim 1, wherein the medicament is in a form for oral or injectable administration, including powders, tablets, granules, capsules, oral liquids, emulsions or suspensions.

9. The use of claim 1, wherein the medicament further comprises other excipients, diabetes drugs, nephropathy drugs, and cardiovascular drugs.

10. The use of claim 8, wherein the medicament further comprises a pharmaceutically acceptable carrier comprising a diluent, buffer, suspension, emulsion, granule, encapsulating agent, excipient, filler, adhesive, spray, transdermal absorbent, wetting agent, disintegrant, absorption enhancer, surfactant, colorant, flavoring agent, or adsorbent carrier.

Technical Field

The invention relates to the field of biological medicines, in particular to application of Reidesvir to medicines for treating diabetic complications, especially diabetic nephropathy and diabetic cardiovascular complications.

Background

Remdesivir (RDV, GS-5734) is a nucleoside analog antiviral drug developed by Gilidd science (GILD) that acts by inhibiting viral nucleic acid synthesis.

The general formula of the structure of the Remdesivir (Remdesivir) compound is proposed for the first time in the patent WO2009132123A1, and the Remdesivir compound is used for treating flaviviridae virus infection diseases such as hepatitis C virus infection, dengue fever and the like. Patent WO2012012776a1 suggests the effect of resisitivir in the treatment of diseases infected with viruses of the paramyxoviridae family. RDV has also been proposed in subsequent patents as anti-filovirus, anti-arenavirus and anti-coronavirus agents. According to literature information, the antitumor effect of the Reidesciclovir is not disclosed in domestic and foreign documents at present.

Diabetes Mellitus (DM) is a global public health problem, and the number of people suffering from DM is increasing, and about 6.93 hundred million diabetics are predicted by 2045 years. DM, a chronic metabolic disease, affects physical health in a variety of ways, and damage, dysfunction and failure of body organs (e.g., kidneys, heart, eyes, blood vessels and nerves). According to the statistics of the world health organization, more than 100 diabetic complications are known, and the diabetes is the disease with the most known complications at present. More than half of the deaths due to diabetes are caused by cardiovascular and cerebrovascular diseases, and 10% of the deaths are caused by nephropathy. Patients who have had amputations due to diabetes are 10-20 times of non-diabetic patients. Clinical data show that about 10 years after the onset of diabetes, 30-40% of patients will develop at least one complication, and once the complication occurs, the drug treatment is difficult to reverse, so that the early prevention of the diabetic complication is emphasized.

Diabetic nephropathy (DKD) is a common microvascular complication of diabetes, which has become a major cause of end-stage renal disease (ESRD) and renal failure. About 21.3% of diabetic patients in China are troubled by diabetic nephropathy, which seriously affects the quality of life of the diabetic patients. No specific medicine for treating the disease exists in clinic, and a new medicine is urgently needed to be developed.

Disclosure of Invention

The invention aims to provide a new indication of Reidesvir drugs. The Reidesciclovir can be used as a medicine for treating diabetic complications, particularly diabetic nephropathy and diabetic cardiovascular complications, can effectively protect renal functions, reduce blood fat and reduce cardiovascular risks, and provides a new alternative medicine for preventing and treating the diabetic complications.

In order to achieve the purpose, the invention adopts the following technical scheme:

the inventor of the present invention predicted the preventive and therapeutic effects of Reidesciclovir on diabetic complications such as diabetic nephropathy using an autonomous computer program.

The invention firstly provides the application of the Rudexiluwei in the preparation of the medicine for treating the diabetic complications.

The complications of the invention not only aim at diabetic nephropathy and diabetic cardiovascular complications, but also comprise other complications, such as diabetic neuropathy, eye diseases and the like. Therefore, in addition to the treatment effect on diabetic nephropathy and hyperlipidemia, the application of the Reidesvir as a medicament for treating diabetes and complications thereof to other symptoms is also within the protection scope of the invention.

Further, the medicament comprises redciclovir in free form or in the form of a pharmaceutically acceptable compound.

In the above-mentioned use of the present invention, the medicament contains an effective dose of redexivir. An effective dose is a unit dosage form (e.g., content of a tablet, a needle, a pill, or a dose of a drug) or unit dose (e.g., unit weight dose) of the patient to be treated. In the present invention, the subject of drug treatment is mammalian, including human, canine, rodent, etc. The effective dose conversion of different animals can be based on the equivalent dose conversion relationship between experimental animals and human in the field (usually refer to the guidance of drug administration such as FDA, SFDA, etc., and also refer to the "Huang-Ji-Han, etc.. equivalent dose conversion between animals and human in pharmacological test. Chinese clinical pharmacology and therapeutics, 2004 Sep; 9 (9): 1069 and 1072), that is, the unit weight dose of human can be deduced from the dose of experimental animals. For example, the conversion relationship between the mouse and the adult is about 12:1 for a commonly used experimental animal mouse according to the above-mentioned document.

In the invention, the effective dose (by content) for obviously treating diabetes-related complications in db/db mice aged 8 weeks is 2.5-100 mg/kg, preferably 20-40 mg/kg.

Preferably, the effective dose of the adult is 12.5-500 mg per day, preferably 100-200 mg per day by setting the adult weight standard to 60kg according to the conversion relation of the effective doses of the mouse and the adult.

Preferably, the medicament also comprises other diabetes, nephropathy and cardiovascular diseases.

Preferably, the medicament further comprises a pharmaceutically acceptable carrier.

The carrier provided by the invention is a pharmaceutically acceptable carrier, and refers to: one or more compatible solid or liquid fillers or gel substances. They are suitable for human use and must be of sufficient purity and sufficiently low toxicity. By "compatible" is meant herein that the components of the composition are capable of being combined with the active ingredients of the present invention and with each other without significantly diminishing the efficacy of the active ingredient.

Preferably, the vectors include, but are not limited to: diluents, buffers, suspensions, emulsions, granules, encapsulating agents, excipients, fillers, adhesives, sprays, transdermal absorbents, wetting agents, disintegrants, absorption enhancers, surfactants, colorants, flavors, or adsorptive carriers.

The medicine can be prepared into any available dosage form in medicine according to the requirement, and preferably, the dosage form of the medicine is suitable for oral administration or injection; preferably, the dosage form includes oral liquid, injection, tablet, capsule, etc.

Has the advantages that:

the invention proves the great potential of the Reidesciclovir as a medicament for treating diabetic complications, particularly diabetic nephropathy and diabetic cardiovascular complications, discloses the good curative effect of the Reidesciclovir on the diabetic nephropathy for the first time, provides an effective novel potential alternative medicament for treating related complications, expands the indications of the Reidesciclovir, and greatly improves the application potential and market prospect of the Reidesciclovir.