CN1067245C - Application of N-aceto-D-aminoglucose in medicinal preparation for curing respiratory tract diseases - Google Patents

Abstract

The present invention discloses a new use of a known compound N-acetyl-D-glucosamine in the medicinal field. A liquid or solid preparation is prepared in a way that the N-acetyl-D-glucosamine is used as an active component which is combined with various kinds of excipient or/and carriers which can be accepted in pharmacy with known methods, such as mixing, granulating, sheet forming, sugar coating or film coating, etc. The liquid or solid preparation is used for treating respiratory diseases, and has the advantages of conspicuous curative effect, simple preparing method and no side effect.

Description

The application of N-acetyl-D-amino glucose in the medicine of preparation treatment respiratory tract disease

The present invention relates to the application of N-acetyl-D-amino glucose as medicine, the particularly N-acetyl-D-amino glucose application in the medicine of preparation treatment respiratory tract disease

N-acetyl-D-amino glucose is as a chemical reagent, public offering on market.Zui Da reagent company-Sigma company obtains this product with chemical synthesis with the acetylation of amino Fructus Vitis viniferae a kind of farm tools in the world, is to use as a kind of biochemical analysis reagent always.

External research work about N-acetyl-D-amino glucose therapeutical effect starts from Grevenlien in 1991 and is used for mouse test with it, find that N-acetyl-D-amino glucose can make cartilage glycosaminoglycans increase, thereby alleviate the pathological change of cartilage; Garceion in 1987 etc. will contain N-acetyl-D-amino glucose preparation RHINAAXIA and try out in clinical, and 186 Allergic Rhinitis are treated, and obtain curative effect preferably.

Biochemical studies show that can produce N-acetyl-D-amino glucose under the human body normal condition.As a chemical compound, it can be in human body normal presence.Since atomic at normal human's intensive amount, more deep research is not carried out in its metabolism, and biochemical research also never relates to the influence of this material to human body physiological function.In recent years; the Japan scientist recognizes the effect of hyaluronic acid in human body gradually in the researching human body scientific process; hyaluronic acid is a kind of viscoelastic material; the macromolecular compound that the N-acetyl-D-amino glucose of medium molecule and D-glucuronic acid are formed; hyaluronic acid and water form viscous gel, and effect lubricated and the protection cell is arranged.And contain hyaluronidase in some antibacterial, malignant tumor and the snake venom; hyaluronic acid is decomposed; viscosity reduces; pathogen is invaded and is propagated; therefore say that hyaluronic acid is the important substance of protection body health, and have great importance too as the N-acetyl-D-amino glucose of one of synthetic hyaluronic raw material.

We have set up antibacterial fluctuation growth model when carrying out " biological ripple " Study on Theory, to this fluctuation its intrinsic regulatory mechanism is arranged through study and cognition, mainly finish by some chemical substance.These chemical substances with regulating action can promote biological fluctuation, and the order slow wave of morbid state is transformed into the fast wave that is chaos state normally, and we call the short ripple factor to this material.Its separation and Extraction is come out and identify, be confirmed as N-acetyl-D-amino glucose at last, what its short ripple effect may be with its pair cell is lubricated relevant with protective effect, because of its short ripple effect, is called as and urgees the ripple amino sugar.Many functions of human body need be urged the ripple factor and assist to finish, and then can cause unusual condition when this short ripple factor lacks in the body.

After the upper respiratory tract infection and the concurrent bacterial infection of catching a cold are the due to illness former infection of tissue adherence cell, produce damage, cause the bacterial infection of secondary.Therefore, treatment must consider that promptly tissue adherence resumes treatment and antibacterial therapy from two aspects.And existing conventional is treated the antibiotic directed toward bacteria effect of adopting, and can not improve the damaged tissues situation, and because clusters of bacteria tolerates phenomenon to antibiotic ecology, so that the concurrent bacterial infection in flu back almost is inevitable.

The objective of the invention is to: the new pharmaceutical usage that utilizes N-acetyl-D-amino glucose to be had, make treatment upper respiratory tract infection and flu back bacterial infection medicine, to overcome the deficiency that the existing conventional medicine in use exists.

Above-mentioned purpose of the present invention is achieved in that promptly adopting structural formula is that the chemical compound of (I) is made active component; with multiple pharmaceutically acceptable excipient or/and carrier combine; adopt mixing, granulation, in flakes, known methods such as sweet tablet or film coating are prepared into liquid state or solid formulation form, are used for the treatment of upper respiratory tract infection and flu back bacterial infective diseases.

Wherein, the chemical name of structural formula (1) is N-acetyl-D-glucamine (N-Acetyl-D-glucosamine), molecular formula: C ₈H ₁₅NO ₆, structure is expressed as follows:

The pharmaceutical usage that the present invention provides the formula I chemical compound is because after the upper respiratory tract infection and the concurrent bacterial infection of catching a cold be the due to illness former infection of tissue adherence cell, produce damage, causes the bacterial infection of secondary.According to relevant biological ripple Study on Theory, find that the formula I chemical compound has the function that promotes the biological cell fluctuation, this function may show as effect lubricated and the protection cell, with infringement and the propagation of pathogen in cell of avoiding the pathogen pair cell.Result of the test through antibacterium field planting effect shows, formula (1) is not though chemical compound has the bactericidal effect, but the antibacterial to the respiratory mucosa surface has anti-field planting effect, it can cooperate the ciliary movement on respiratory tract surface to get rid of antibacterial external, simultaneously by promoting that cell distributes again, improve and repair local damaged tissues, thereby play the purpose of anti-inflammatory.

The toxicological test of formula I chemical compound comprises:

1. acute toxicity test: comprise oral, intravenous injection and maximum limit amount medicine-feeding test;

2.Ames test;

3. mouse marrow cell micro nuclear test;

4. the abnormal property of Mus sperm test;

5. mouse testis chromosomal aberration test;

6. show the chronic lethal test;

7. subchronic toxicity (feeding in 90 days) test;

8. traditional teratogenicity test.

Conclusion (of pressure testing) shows: formula I chemical compound acute toxicity test dosage surpasses 29/kg, is 300 times of people's injected dose, does not occur the acute poisoning reaction yet; In long term toxicity test, maximum dose level has reached 1g/kg, and toxic reaction does not appear in experimental observation around the warp; In reproduction test, feed mice from routine dose 7mg/kg, go down to posterity through three times, prove the formula I chemical compound to mice become pregnant, gestation, childbirth, suckling and filial mice growth all do not have influence.Proof formula I chemical compound belongs to innocuous substance.

The formula I chemical compound shows that in clinical a large amount of situations on probation this medicine can effectively prevent or treat the upper respiratory tract active chronic inflammation.Acute upper respiratory tract infection comprises acute pharyngitis, acute laryngitis, acute sinusitis, shows through 300 routine clinical employing buccal tablet result on trial, and the formula I chemical compound reaches more than 90% the effective percentage of treatment acute upper respiratory tract infection; It should be noted that to the emergency case patient, escalated dose is answered in first and second day administration.Chronic upper respiratory tract infection comprises chronic pharyngitis, chronic laryngitis, chronic rhinitis, shows through 150 routine clinical oral administration administration result on trial, and the formula I chemical compound is 62% to the cure rate of treatment chronic upper respiratory tract infection.

Formula (1) chemical compound can pass through common administration, and parenterai administration for example is as intravenous injection or oral administration.Dosage depends on patient's age, body weight, condition of illness and route of administration.Optimal dose for adult dosage 150-300mg/ day, intravenous injection once, oral or intramuscular injection divides three times; Seven days is a course of treatment, adheres to 2-3 the administration course of treatment.

Can adopt conventional method to prepare the pharmaceutically pharmaceutical composition of suitable formulations form.For example, the preparation that is used for liquid form used for intravenous injection or for oral use can be a solvent with sterilized water or Sterile Saline.The suspension of intramuscular injection or solution can adopt in the carrier Peroral solid dosage form forms such as sterilized water, olive oil, ethyl oleate, glycols, for example tablet or capsule, remove formula I active ingredient beyond the region of objective existence, also can comprise diluent, as lactose, glucose, cellulose, starch; Lubricant is as silicon, Talcum, magnesium stearate or calcium and Polyethylene Glycol; Bonding agent is as starch, Radix Acaciae senegalis, methylcellulose, carboxymethyl cellulose, polyvinylpyrrolidone; Depolymerizing agent is as starch, alginic acid, alginate, sodium starch glycol; Foaming mixture; Coloring agent; Sweeting agent; Lubricant is as lecithin, many ethoxies fat ether etc.; General nontoxic and pharmacology goes up inert matter and can be used in the pharmaceutical preparation.Said pharmaceutical preparation can prepare with known method, for example utilize mixing, granulation, in flakes, methods such as sugar-Bao Biao or film coating

Formula I chemical compound disclosed by the invention is different from the new medical usage of its known application, enlarged the range of application of N-acetyl-D-amino glucose, having improved its exploitation is worth, with it is that active substance is except that being used to prepare the medicine for the treatment of respiratory tract disease, also can be used as additive and be used for health product, help the prevention of respiratory tract disease.Have special effect and remarkable, compound method is simple, and advantage without any side effects from promoting that cell distributes again, is adjusted the angle of biological ripple, has innovative characteristics.

Claims (1)

1, the application of N-acetyl-D-amino glucose in the medicine of preparation treatment respiratory tract disease.