# US 2021/0275578 A1 · Drug and production method therefor

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- Number: US 2021/0275578 A1
- Document ID: US20210275578A1
- Status: Published application
- Kind: A1
- Application number: 17/236,891
- Filed: 2021-04-21
- Published: 2021-09-09
- Earliest claimed: 2017-07-27
- Assignees: Osaka University
- Applicants: Osaka University
- Inventors: Hikaru KOBAYASHI; Yuki KOBAYASHI; Ryoichi IMAMURA; Norio NONOMURA
- Web page: https://patentgrep.com/patent/US20210275578A1

## CPC

- A61K 33/00: Medicinal preparations containing inorganic active ingredients
- C01B 3/06: by reaction of inorganic compounds containing electro-positively bound hydrogen with inorganic reducing agents
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/167: {with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface (with further drug-free outer coating A61K9/5073)}
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 13/12: of the kidneys
- A61P 39/06: Free radical scavengers or antioxidants
- C01B 33/02: Silicon (forming single crystals or homogeneous polycrystalline material with defined structure C30B)
- C01P 2004/50: Agglomerated particles
- C01P 2004/64: Nanometer sized, i.e. from 1-100 nanometer
- Y02E 60/36: Hydrogen production from non-carbon containing sources, e.g. by water electrolysis
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C01B: NON-METALLIC ELEMENTS; COMPOUNDS THEREOF; {METALLOIDS OR COMPOUNDS THEREOF NOT COVERED BY SUBCLASS C01C}
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C01P: INDEXING SCHEME RELATING TO STRUCTURAL AND PHYSICAL ASPECTS OF SOLID INORGANIC COMPOUNDS
- Y02E: REDUCTION OF GREENHOUSE GAS [GHG] EMISSIONS, RELATED TO ENERGY GENERATION, TRANSMISSION OR DISTRIBUTION

## Abstract

One drug (solid preparation) 100 of the present invention is a drug for a disease of kidney that contains a silicon fine particle, an aggregate of the silicon fine particles, or a crystal grain of silicon having a hydrogen-generating ability. Hydrogen generated from the silicon fine particle in the drug can contribute to the prevention and/or treatment of the kidney disease.

## Claims

### Claim 1

A drug for a disease of kidney, comprising a silicon fine particle, an aggregate of the silicon fine particles or a crystal grain of silicon,
wherein hydrogen is generated by bringing a water-containing liquid in an intestine into contact with the silicon fine particle, the aggregate or the crystal grain.

### Claim 2 (depends on 1)

The drug according to claim 1, wherein the disease is at least one selected from a group of renal fibrosis, acute kidney injury, renal ischemia reperfusion injury, drug-induced renal dysfunction, and chronic kidney disease.

### Claim 3 (depends on 1)

The drug according to claim 1, wherein the drug is prepared to be suitable for oral ingestion.

### Claim 4 (depends on 1)

The drug according to claim 1, wherein
the silicon fine particle does not pass through a cell membrane of an intestinal tract and between cells of the intestinal tract,
the aggregate does not pass through the cell membrane and between the cells, and
the crystal grain does not pass through the cell membrane and between the cells.

### Claim 5 (depends on 1)

The drug according to claim 1, further comprising a pH value adjusting agent that sets a pH value of a water-containing liquid to more than 7 and less than 9 when the drug is disintegrated in pure water.

### Claim at position 6

-8. (canceled)

### Claim 9 (depends on 1)

The drug according to claim 1, wherein the silicon fine particle substantially includes a silicon fine particle having a crystallite diameter of 1 nm or more and 100 nm or less.

### Claim 10 (depends on 1)

The drug according claim 1, wherein an oxidative stress on the kidney is reduced or eliminated by reacting hydroxyl radicals with hydrogen in an intestine and/or blood.

### Claim 11 (depends on 1)

A production method for producing the drug according to claim 1, the production method comprising contacting a mixture of hydrogen peroxide and water with treatment step of bringing the silicon fine particle, the aggregate, or the crystal grain into contact with hydrogen peroxide water.

### Claim 12 (depends on 11)

The production method according to claim 11, further comprising a step of forming the silicon fine particle, the aggregate, or the crystal grain by grinding a silicon particle in an ethanol solution before the contacting the silicon fine particle, the aggregate or the crystal grain with the mixture of the hydrogen peroxide and water treatment step.

### Claim 13 (depends on 11)

The production method according to claim 11, further comprising combining the silicon fine particle, the aggregate or the crystal grain with a pH value adjusting agent and a physiologically acceptable base material after contacting the silicon fine particle, the aggregate or the crystal grain with the mixture of hydrogen peroxide and water.

### Claim 14 (depends on 2)

The drug according to claim 2, wherein the drug is prepared to be suitable for oral ingestion.

### Claim 15 (depends on 2)

The drug according to claim 2, wherein
the silicon fine particle does not pass through a cell membrane of an intestinal tract and between cells of the intestinal tract,
the aggregate does not pass through the cell membrane and between the cells, and
the crystal grain does not pass through the cell membrane and between the cells.

### Claim 16 (depends on 3)

The drug according to claim 3, wherein
the silicon fine particle does not pass through a cell membrane of an intestinal tract and between cells of the intestinal tract,
the aggregate does not pass through the cell membrane and between the cells, and
the crystal grain does not pass through the cell membrane and between the cells.

### Claim at position 15

-19. (canceled)

### Claim 20 (depends on 12)

The production method according to claim 12, further comprising combining the silicon fine particle, the aggregate or the crystal grain with a pH value adjusting agent and a physiologically acceptable base material after contacting the silicon fine particle, the aggregate or the crystal grain with the mixture of hydrogen peroxide and water.

### Claim 21 (depends on 1)

The drug according to claim 1, wherein the drug treats the disease of the kidney by reducing renal tubulointerstitial fibrosis or a depleted glomerulus.

### Claim 22 (depends on 1)

The drug according to claim 1, wherein the drug prevents the disease of the kidney by reducing renal tubulointerstitial fibrosis or a depleted glomerulus.

### Claim 23 (depends on 1)

The drug according to claim 1,
further comprising at least one of the following (a), (b), or (c):
(a) an enteric coating agent coating on an outermost layer of the silicon fine particle, the aggregate orthe crystal grain;
(b) an enteric capsule encapsulating the silicon fine particle, the aggregate or the crystal grain; or
(c) an enteric microcapsule encapsulating the silicon fine particle, the aggregate or the crystal grain.

### Claim 24 (depends on 1)

The drug according to claim 1,
further comprising at least one of the following (a), (b), or (c):
(a) a coating agent having a sustained release property and coating an outermost layer of the silicon fine particle, the aggregate or the crystal grain;
(b) a capsule having a sustained release property and encapsulating the silicon fine particle, the aggregate or the crystal grain; or
(c) a microcapsule having a sustained release property and encapsulating the silicon fine particle, the aggregate or the crystal grain.
