CN109806245A - A kind of drug to be eased pain as raw material preparation with treatment of arthritis function using cedrol - Google Patents

Abstract

The present invention relates to a kind of using cedrol as the drug of raw material preparation analgesia and treatment of arthritis function.The cedrol is the racemic modification of cedrol, β-CE or their any ratios, and total effective dose is 1-100mg/kg/d.CE is extracted from the extensive natural plants in source.The present invention causes the anti-inflammatory effect of scorching method and adjuvant-induced arthritis observation CE using rat paw Irish moss, as a result the reaction of nonspecific inflammation caused by visible CE Carrageenan has obvious inhibiting effect, while also having significant treatment and prevention to act on adjuvant-induced arthritis.The present invention is using the analgesic activity of tail-flick method observation CE, and as a result visible CE has significant analgesic activity to rat photo-thermal stimulation tail portion.The present invention provides a kind of curative for effect, safe readies, anti-inflammatory and analgesic raw material from a wealth of sources, can combine with pharmaceutically acceptable one or more carriers and cedrol pharmaceutical composition or preparation is made.

Description

A kind of drug to be eased pain as raw material preparation with treatment of arthritis function using cedrol

Technical field

The invention belongs to pharmaceutical technology fields, and in particular to a kind of to prepare analgesia and treatment of arthritis by raw material of cedrol The drug of function.

Background technique

Arthritis is a kind of common chronic disease, refers to the arthritis as caused by inflammation, infection, wound or other factors Venereal disease becomes, and belongs to rheumatism subject disease.It is mainly characterized by redness and swelling of joints, heat, pain and dysfunction.The current arthritis in China is suffered from Person is estimated to be 100,000,000 or more, and number is also being continuously increased, most commonly osteoarthritis and two kinds of rheumatoid arthritis.According to another Statistics, half suffers from osteoarthritis in China 50 years old or more crowd；In over-65s crowd 90% women and 80% male suffer from Osteoarthritis.Illness rate of the rheumatoid arthritis in China is 0.34%~0.36%, it is introduced that, the rheumatoid arthritis state of an illness is tight The severe one service life about shortens 10~15 years.Arthritis can be divided into according to the cause of disease: rheumatic, rheumatoid, traumatic, Osteoarthritis And pyogenic arthritis etc..

Rheumatic arthritis category allergic disease is one of main performance of rheumatic fever.Mostly with febris acuta and pass Pain onset is saved, typical performance is slight or moderate fever, and migratory polyarthritis, affected joints are mostly knee, ankle, shoulder, elbow, wrist Etc. large joints, common to be transferred to another joint by a joint, red, swollen, scorching hot, severe pain, some patients are locally presented in lesion Also have several joints while falling ill, atypical patient only has arthralgia and shows without other inflammation, acute inflammation generally in Subside within 2-4 weeks, does not stay sequelae, but normal recurrent exerbation.If active rheumatism influences heart, myocarditis can occur, or even leave Valve disorder.

Rheumatoid arthritis (rheumatoid arthritis) is a kind of chronic complete characterized by arthrosynovitis Body autoimmune autoimmune disease.The lasting recurrent exerbation of synovitis can lead to the destruction of intra-articular cartilage and bone, close Dysfunction is saved, or even maimed.Vasculitis lesion involves each organ of whole body, therefore this disease is also known as rheumatoid disease.

Rheumatoid arthritis is also known as rheumatoid (RA), is a kind of chronic systemic inflammation disease that the cause of disease is not yet clear Disease belongs to autoimmune inflammatory disease using lesion outside chronic, symmetry, more synovial joints inflammation and joint as main clinical manifestation. The disease is apt to occur in the Minor articulus such as hand, wrist, foot, and recurrent exerbation is symmetric.There are joint red and swollen heat pain and dysfunction in early stage, Advanced joint may occur in which different degrees of stiff deformity, and with the atrophy of bone and skeletal muscle, easily disable.From pathological change From the point of view of angle, rheumatoid arthritis is that mainly involve synovium of joint (can feed through to articular cartilage, bone tissue, pass to one kind later Save ligament and tendon forceps), it is secondly the popularity diseases associated with inflammation of the connective tissues such as serous coat, the heart, lung and eye.Rheumatoid arthritis Systemic manifestation in addition to arthropathy, there are also fever, fatigue and weak, pericarditis, subcutaneous nodule, pleurisy, arteritis, surrounding Neuropathy etc..The rheumatoid arthritis of broad sense further includes the popularity lesion of whole body in addition to the inflammatory disorders of joint part.

Post-traumatic arthritis mostly causes articular cartilage that retrogression occurs or forms spur because of wound or lasting chronic strain, Swollen diseased joints, pain and dyskinesia are shown as, for Yi Fasheng in prudent joint, such as shoulder, knee, ankle joint, sportsman and blueness are strong It is common in year.

Osteoarthritis is a kind of most common arthropathy, and the title of osteoarthritis is extremely more, as hypertrophic osteoarthritis, Degenerative arthritis, degenerative joint inflammation, hyperplastic osteoarthritis or osteoarthropathy refer both to a kind of disease, and the country is unified to use bone Arthritis.Its illness rate increases with the age, and women than men is multiple.Osteoarthritis between proximally and distally the referring to of hand to close Section, knee, elbow and shoulder joint and joint of vertebral column are easy to be involved, and the then less morbidity of wrist, ankle-joint.Osteoarthritis is become by tissue Property and accumulation property strain cause, be more common in the middle-aged and the old of overweight, the position of most commonly-occurring disease is knee, finger, neck, lumbar vertebrae etc. Place, symptom is mainly arthralgia, stiff (pain relief can be felt after light activity), and severe one may occur in which arthroncus, muscle Atrophy etc..

Pyogenic arthritis is often caused by bacterium intrusion articular cavity, is more common in children, is often betided hip joint, main Want symptom red, swollen for part, pain, heat and the systemic toxicity profiles symptom such as dysfunction and high fever.

No matter arthritis or what type of arthritis caused by which kind of reason, should all diagnosis and treatment early, in order to avoid cause permanent Property joint function disturbance even disable.

For treating all kinds of arthritis there are many drug, Western medicine has penicillamine, Salicylic Acid Formulations, indocin, propionate raw Object, immunosuppressor, levamisol etc..But the side effect of Western medicine is increasingly of interest by the world and evaluates, while the disease of patient Treatment sense of self-protection is constantly enhancing, so that many pharmacy corporations increase the day of dynamics of investment and speed research and development effective and safe Right drug.

In conclusion the present invention realizes the medical application novelty that separating obtained chemical component is extracted in natural plants, Meet the demand that arthritic's demand is big, market prospects are good.

Summary of the invention

The purpose of the present invention is to provide the new applications of CE, i.e., the new opplication in pharmacy.

The present invention relates to CE as the application prepared in medicament for treating arthritis.

The present invention relates to CE as the application in preparation treatment analgesic.

The present invention relates to come in the form of conventional galenic preparations when CE is used to prepare arthritis and analgesic using；It is described Conventional galenic preparations containing being such as suitable for having for the enteral and parenteral administration of stomach with pharmaceutically acceptable carrier in the formulation Machine or the mixing of inorganic solid or liquid excipient, which is solid form such as tablet, capsule, powder, ball Agent, granule are also possible to liquid form such as injection, emulsion etc..

Auxiliary substance, stabilizer, wetting agent and other common additives can be contained in above-mentioned preparation, such as lactose, lemon Acid, tartaric acid, magnesium stearate, land plaster, sucrose, cornstarch, talcum powder, gelatin, agar, pectin, peanut oil, olive oil, Cocoa butter, ascorbic acid, mannitol etc..

The invention further relates to application of the pharmaceutical composition using CE as active constituent in anti-inflammatory and analgesic.The drug Combination can be prepared according to method well known in the art.Can by through the compounds of this invention with it is one or more pharmaceutically acceptable Solid or liquid excipient and/or adjuvant combine, and any dosage form used suitable for human or animal is made.The compounds of this invention exists Content (weight) in its pharmaceutical composition is usually 0.1~95%.

CE of the present invention is α-CE and β-CE and the mixture (racemic modification) of their any ratios.

Solve the problems, such as this technology the technical solution adopted is that, preparative separation goes out CE from natural plants, and re-refining keeps its pure Degree reaches 95% or more, for analgesia and anti-inflammatory effect, can be used for preparing treatment of arthritis and analgesic drug.

Above-mentioned preparation can be made according to the preparation process of various preparation routines.

CE of the invention has preferable analgesia and anti-inflammatory effect, and total effective dose is 1-100mg/kg/d.

Specific embodiment

Below with reference to embodiment, the present invention will be further described

Embodiment: the influence to rat assist agent arthritis

Method: taking SD rat 60, is divided into 5 groups by weight average: (1) 1%TW-80 (solvent)；(2) positive control drug Sai meter Song phosphoric acid saline injection 2.5mg/kg；(3)α-CE25mg/kg；(4)α-CE50mg/kg；(5)α-CE100mg/kg.Adopt With gastric infusion (ig) mode.It is injected in behind the right side in vola with Freund ' s Freund's complete adjuvant 0.1ml (contain BCG vaccine 0.5mg).Note 30min gastric infusion is primary before penetrating adjuvant.Pedal swelling situation behind the primary right side of 18h measurement, observes CE to morning after injection adjuvant The prevention effect of phase acute inflammation, is then discontinued；Start gastric infusion after a week, one time a day, continuous 7 days, measures one in d15 Secondary left back pedal swelling situation observes CE to the prevention effect of secondary affection, is then discontinued；Therapeutic give is carried out since d19 Medicine, one time a day, until d28 experiment terminates, therapeutic effect of the primary part observation CE to secondary affection is daily to measure from d21 to d28 Primary left back pedal swelling situation, it is secondary by " study of tcm new drug guide " related adjuvant-induced arthritis daily from d22 to d28 Venereal disease becomes point system, and incidence, tubercle number or the severity of observation sufficient pawl swelling degree, forelimb and tail portion lesion score by 5 grades Method: 0: without redness；1: small toe joint is slightly swollen；2: toe joint and pedal swelling；3: foot swelling below ankle-joint；4: including ankle-joint Whole sufficient pawl swellings inside.Rat is put to death after experiment, dissection takes out immune organ thymus gland and spleen weighing, calculates internal organs Coefficient；And the neat knee joint of the left and right metapedes of rat is cut off, weighing.

As a result: α-CE100mg/kg and dexamethasone 2.5mg/kg group treatment after d3 just work, surveyed daily from d21 to d28 Fixed 1 left back pedal swelling result and the secondary arthritis appraisal result analysis from d22 to d28 have significant compared with the control group Sex differernce (P < 0.05~0.001), α-CE50mg/kg group also have notable difference (P < 0.05~0.01) in most number of days, It is shown in Table 2 and table 3.Put to death rat after d28 experiment, by the neat knee joint cutting weighing of the left and right metapedes of rat, as a result with d28 The pedal swelling situation of measurement matches, and is shown in Table 4.α-CE25mg/kg group and dexamethasone phosphate 2.5mg/kg group are in injection 30min gastric infusion causes the swelling of vola pedis early stage acute inflammatory (P < 0.05) after capable of obviously inhibiting adjuvant injection before adjuvant；α- Cause after CE100mg/kg, 50mg/kg and the obvious prevention adjuvant injection of administration in dexamethasone 2.5mg/kg group continuous 7 days vola pedis after The swelling reaction of hair property, see Table 5 for details.Thymus gland and spleen is taken to weigh, α-CE inhibits to make to immune organ in dose-dependant as the result is shown With.Show that the anti-inflammatory effect of α-CE is related to immunosuppressive action.

Claims (6)

1. a kind of using cedrol as the drug of raw material preparation analgesia and treatment of arthritis function.

2. purposes according to claim 1, it is characterised in that: the total effective dose of the cedrol is 1-100mg/kg/ d。

3. purposes according to claim 1, it is characterised in that: the cedrol be from arbor-vitae, Selaginella tamariscina, cypress, deodar, Lycopodium calvatum, fructus viticis, centering rattan, Heiguteng exract, ginger, Coleus forskohlii, Ranunculus sieboldii, common bombax flower, the big feverfew of red heart, in smilax It is prepared.

4. purposes according to claim 1, it is characterised in that: the arthritis includes rheumatic, rheumatoid, wound Property, Osteoarthritis and pyogenic arthritis.

5. purposes according to claim 1, it is characterised in that: the cedrol can be with pharmaceutically acceptable one kind Or variety carrier or excipient combine and cedrol pharmaceutical composition are made, content in the composition is 0.1~95%.

6. purposes according to claim 1, it is characterised in that: the cedrol can be prepared into tablet, capsule, dissipate Agent, granule, injection, emulsion, plaster, liniment, tincture, finish, presses agent, film, gelling agent, cataplasm at pill.