CN1939398A - Use of gentiin in analgesic for treating arthritis - Google Patents
Use of gentiin in analgesic for treating arthritis Download PDFInfo
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- CN1939398A CN1939398A CN 200610104732 CN200610104732A CN1939398A CN 1939398 A CN1939398 A CN 1939398A CN 200610104732 CN200610104732 CN 200610104732 CN 200610104732 A CN200610104732 A CN 200610104732A CN 1939398 A CN1939398 A CN 1939398A
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Abstract
An application of the gentiopicroside extracted from large-leaf gentian root or Chinese gentian in preparing the medicines for relieving pain and treating arthritis is disclosed.
Description
Technical field
The present invention relates to gentiopicrin or contain the new purposes of the Radix Gentianae total glucosides of gentiopicrin more than 50% in analgesia and arthritis drug.
Background technology
Arthritis is poverty, the commonly encountered diseases of backward areas, frequently-occurring disease, especially in mountain area and rural area.The arthritis performance has inflammation and pain, because the cause of disease it be unclear that, doctor trained in Western medicine does not have desirable Drug therapy, also can produce toxic and side effects.
Summary of the invention
The object of the present invention is to provide gentiopicrin or contain the new purposes of the Radix Gentianae total glucosides of gentiopicrin more than 50%, i.e. new application in pharmacy.
The present invention relates to gentiopicrin or contain the Radix Gentianae total glucosides of gentiopicrin more than 50% as the application in the medicine of preparation treatment of arthritis.
The present invention relates to gentiopicrin or contain the Radix Gentianae total glucosides of gentiopicrin more than 50%, for example contain gentiopicrin 60%, 70%, 80%, 90% etc. as the application in the preparation treatment analgesic.
The technical scheme that solves the problems of the technologies described above employing is, prepares Radix Gentianae total glucosides (containing gentiopicrin about 70%) from Radix Gentianae Macrophyllae, re-refines into gentiopicrin, two this be used for analgesia and antiinflammatory action, can be used for preparing the medicine of treatment of arthritis.
The preparation technology of gentiopicrin is as follows:
Get Radix Gentianae Macrophyllae, decoct 3 times, each 15 minutes, merge decoction liquor, the centrifuging and taking supernatant with 5-20 times of water gaging; D101 macroporous resin column on the decocting liquid, 0.8mL medicinal liquid on every gram resin, macroporous resin is with the water elution of 2～6 times of amounts, abandon or adopt water lotion, the ethanol elution that the macroporous resin reuse is 3～10 times 30% reclaims the ethanol in the eluent, decompressing and extracting, get residue, be Radix Gentianae total glucosides (containing gentiopicrin more than 70%), will go up macroporous resin, 30% ethanol elution behind the Radix Gentianae total glucosides water dissolution more as stated above, residue behind the recovery eluent is dissolved in 95% ethanol of 2～5 times of amounts, filter, reclaim ethanol and drain reuse 95% dissolve with ethanol, drain again, be dissolved at last in the dense ethanol, place, separate out crystallization, filter, get the pure product of gentiopicrin.
Effective ingredient uses with the form of conventional pharmaceutical formulation with the medicine that the gentiopicrin preparation suppresses hepatitis B virus; Described conventional medicine with preparation contain as active component in preparation with pharmaceutically acceptable carrier as being suitable in the gastrointestinal and the solid or the liquid excipient of the organic or inorganic of parenteral mix, this pharmaceutical formulation can be solid form such as tablet, capsule, powder, pill, granule, also can be liquid form such as injection, Emulsion etc.
Can contain auxiliary substance, stabilizing agent, wetting agent and other additive commonly used in the above-mentioned preparation, as lactose, citric acid, tartaric acid, magnesium stearate, Gypsum Fibrosum powder, sucrose, corn starch, Pulvis Talci, gelatin, agar, pectin, Oleum Arachidis hypogaeae semen, olive oil, cocoa butter, ethylene glycol, ascorbic acid, mannitol etc.
Above-mentioned preparation can be made according to the preparation technology of various preparation routines.
For understanding essence of the present invention better, will its new purposes in pharmaceutical field be described with the pharmacological testing and the result of gentiopicrin below.
One, is subjected to the reagent thing: injection gentiopicrin injection.
1.1 the unit of providing: Shaanxi Province's biological medicine key lab.
1.2 character: light yellow or subalbous pressed powder, bitter in the mouth.
1.3 specification: 80mg/ bottle.
1.4 solvent: normal saline.
1.5 collocation method: normal saline is mixed with 1.25% and 0.625% solution, pH 5.5-6.0, and it is standby to put refrigerator.
1.6 storage requirement: 4 ℃, airtight preservation is dry.
Two, dosage setting
Mouse mainline (iv) administration records LD
50Be 2.5g/kg; Rat 1.8g/kg.Preliminary experiment is the result show, injection gentiopicrin 125mg/kg is best dosage, and this dosage is LD
501/20, so 30-150mg/kg is used in this experiment.
Three, test material
3.1 the test material hydrocortisone, people pharmaceutical factory of Tianjin aminoacid company produces, lot number 990813: ampicillin, HARBIN PHARMACEUTICAL GROUP CO., LTD. General Pharm. Factory, lot number A20000820; Bifendate 1.5mg * 250 balls, Zhejiang temperature neck pharmaceutical factory, lot number 0003102.
3.2 animal Sprague-Dawley (SD) rat, body weight 180-220g; Provide by The Fourth Military Medical University's Experimental Animal Center, produce the quality certification number and move word 08-014 number for the Shan doctor.Kunming mouse body weight 18-22g; Provide by The Fourth Military Medical University's Experimental Animal Center, produce the quality certification number and move word 08-013 for the Shan doctor.Cavia porcellus 250-300g is provided by Xian Medical Univ's Experimental Animal Center, the moving card of doctor word 08-019 number.Sub-cage rearing in the air conditioning chamber, 23 ± 2 ℃ of room temperatures, relative humidity 45%-60%, automatic control each 12h round the clock, pellet is fed, automatically drinking public water supply.
Four, experimental technique and result
4.1 injection gentiopicrin xylol causes the protective effect of mice auricular concha inflammation.
4.1.1 60 of Kunming mouses, male and female half and half are divided into 5 groups at random by sex and body weight, i.e. normal control group, hydrocortisone (20mgkg
-1) positive controls, gentiopicrin (150,75,37.5mgkg
-1) the administration group.Day every day 8:00 is the gentiopicrin (20mLkg of intramuscular injection (im) various dose respectively
-1), isopyknic normal saline or ip 20mgkg
-1Hydrocortisone, every day 1 time, totally 3 times.Be applied to mouse right ear with dimethylbenzene behind the last administration 0.5h, each 0.01ml of the in ear outside, left ear is coated with same distilled water in contrast.0.5h back repaste one time is put to death animal after 0.5h, gets left and right auricle, beat with No. 9 card punch and get left and right sides ear same area auricle and weigh, the difference that subtracts left auricle weight with auris dextra sheet weight than left auricle weight as auris dextra inflammation swelling degree.
4.1.2 result's (table 1) as seen, big or middle dosage group of gentiopicrin and hydrocortisone group can obviously alleviate the inflammatory reaction that dimethylbenzene causes, present tangible dose-dependence.Show that the mice auricular concha inflammatory reaction that injection gentiopicrin xylol causes has tangible antagonism.
Table 1. injection gentiopicrin xylol causes protection (n=10, the X ± s) of mice auricular concha inflammation
| The auris dextra sheet heavily/(mg) | Left side auricle heavily/(mg) | Swelling degree (%) | |
| Matched group hydrocortisone 20mgkg -1Gentiopicrin 150mgkg -1Gentiopicrin 75mgkg -1Gentiopicrin 37.5mgkg -1 | 25.53±3.35 20.80±3.79 20.05±3.32 23.48±3.19 24.93±6.77 | 16.29±2.60 16.66±1.17 16.27±1.49 17.46±1.58 16.81±1.61 | 57.76±14.05 24.59±18.75 h 24.58±17.88 h 35.61±24.08 h 49.72±45.64 |
aP＜0.05,
bCompare with matched group p＜0.01.
4.2 the injection gentiopicrin causes the protective effect of rat paw edema inflammation to Ovum Gallus domesticus album
4.2.1 50 of SD rats, male and female half and half are divided into 5 groups at random by sex and body weight, comprise the normal control group, hydrocortisone (15mgkg
-1) positive controls, gentiopicrin (120,60,30mgkg
-1) three dosed administration groups.Every day, 8:00 distinguished the gentiopicrin of im various dose, ip hydrocortisone, every day 1 time, totally 3 days.Cause inflammation (every Mus right sufficient plantar subcutaneous injection 0.1ml) with 10% Ovum Gallus domesticus album solution in the last administration after 1 hour, with vernier caliper measurement cause scorching before and cause scorching back 0.5,1.0,2.0,3.0, the 4.0 hours same position of sufficient sole of the foot thickness.
4.2.2 result of the test (table 2) as seen, the big or middle dosage group of hydrocortisone and gentiopicrin all can suppress the inflammatory reaction that Ovum Gallus domesticus album causes, with matched group the significance difference is arranged relatively.
Table 2 gentiopicrin causes protective effect (n=10, the X ± s) of rat paw edema inflammation to Ovum Gallus domesticus album
| Cause scorching front foot sole of the foot thickness (mm) | Cause scorching back-cause scorching before difference (mm) | |||||
| 0.5h | 1.0h | 2.0h | 3.0h | 4.0h | ||
| Matched group hydrocortisone 20mgkg -1Gentiopicrin 150mgkg -1Gentiopicrin 75mgkg -1Gentiopicrin 37.5mgkg -1 | 3.42±0.25 3.41±0.28 3.42±0.25 3.40±0.26 3.41±0.22 | 2.58±0.36 1.92±0.28 b 2.21±0.41 a 2.39±0.22 2.56±0.39 | 2.44±0.32 1.72±0.46 b 1.76±0.39 b 2.03±0.36 a 2.33±0.41 | 2.39±0.29 1.68±0.21 b 1.82±0.31 b 2.01±0.44 a 2.20±0.33 | 2.19±0.37 16.7±0.47 a 1.82±0.44 1.97±0.45 2.18±0.43 | 2.18±0.35 1.67±0.38 1.79±0.42 1.95±0.48 2.18±0.42 |
aP＜0.05,
bCompare with matched group p＜0.01
4.3 the injection gentiopicrin is to the protective effect of the swollen inflammation of rat granuloma
4.3.1 50 of SD rats, male and female half and half are divided into 5 groups at random by sex and body weight: normal control group, hydrocortisone (15mgkg
-1) positive controls, gentiopicrin (120,60,30mgkg
-1) three dosage groups.Under pentobarbital sodium anesthesia, an osculum is cut by strange portion about rat, subcutaneous imbed an aseptic cotton balls (weight is 10 ± 1mg), respectively adds ampicillin 2mg in the wound, sew up wound, the whole surgery process is the sterile working.Operation began the gentiopicrin that im gives various dose the same day, once a day, the next day of the hydrocortisone group ip1 time, continuous 10 days.24h puts to death animal after the last administration, takes out cotton balls, picks most fat preventing tissue, 60 ℃ of baking box oven dry, weighs, and it is heavy to deduct former cotton balls, is granuloma weight.
4.3.2 experimental result (table 3) shows that large, medium and small three the dosage groups of gentiopicrin swell to rat granuloma and present the dose-dependent inhibition effect.
Table 3 gentiopicrin Chinese People's Anti-Japanese Military and Political College Mus granuloma induced by implantation of cotton pellets (n=10, X ± s)
| Group | Granuloma heavy (mg) |
| Matched group hydrocortisone 20mgkg -1Gentiopicrin 150mgkg -1Gentiopicrin 75mgkg -1Gentiopicrin 37.5mgkg -1 | 26.63±3.89 17.93±3.71 b 19.28±2.62 b 23.22±2.96 a 25.23±5.07 |
aP＜0.05,
bCompare with matched group P＜0.01.
4.4 the influence of the Mice Auricle inflammatory reaction that the injection gentiopicrin causes adrenalectomy dimethylbenzene
4.4.1 36 of Kunming mouses, male and female half and half are divided into the normal control group, adrenalectomy model group, gentiopicrin 150mgkg
-1The administration group.Model group and administration group mice be adrenalectomy under pentobarbital sodium anesthesia, behind the 3d to normal matched group and adrenalectomy model group im (20mLkg
-1) normal saline, administration group im gentiopicrin, once a day, continuous 4d.The last administration is applied to mouse right ear with dimethylbenzene after half an hour, each 0.01ml of the in ear outside, and left ear is coated with distilled water in contrast.0.5h back repaste one time is put to death animal after 0.5h, gets left and right sides ear, beats with No. 9 card punch and gets left and right sides ear same area auricle and weigh, the difference that subtracts left auricle weight with auris dextra sheet weight than left auricle weight as auris dextra inflammation swelling degree.
4.4.2 experimental result (seeing Table 4) shows that gentiopicrin has significant antiinflammatory action.
Table 4 injection gentiopicrin causes scorching influence (X ± s) to the adrenalectomy mouse ear
| Number of animals n | Poor (the X ± s) of auris dextra-left ear | The swelling degree | |
| Matched group model group gentiopicrin 150mgkg -1 | 12 12 12 | 5.16±2.19 9.30±2.85 b 6.85±2.18 c | 71.8％ 140.1％ 83.9％ |
bCompare with matched group P＜0.01;
CCompare with model group P＜0.05.
4.5 annotate not the mouse thymus that hydrocortisone caused with gentiopicrin and the influence of spleen atrophy
4.5.1 60 of Kunming mouses, male and female half and half are divided into the normal control group at random by body weight and sex, the hydrocortisone model group, hydrocortisone ten gentiopicrins (150,75,37.5mgkg
-1) the administration group.Normal group and model group every morning 8:00 intramuscular injection (im) normal saline 20mLkg
-1, the gentiopicrin of administration group im every day equal-volume various dose; Except that the normal control group, all the other each group ip cortisone (20mgkg in administration
-1), continuous 4d.24h gets thymus and spleen is weighed after the last administration.With the weight of thymus and spleen divided by the Mus body weight as index, with the average and the standard deviation of statistical method gauge index.
4.5.2 result's (table 5) as seen, three dosage of gentiopicrin all can resist thymus and the spleen atrophy that hydrocortisone causes.
Table 5 gentiopicrin influences result (n=12, X ± s) to thymus, spleen
| Group | Thymus index | Index and spleen index |
| Normally to group hydrocortisone 20mgkg -1Gentiopicrin 150mgkg -1Gentiopicrin 75mgkg -1Gentiopicrin 37.5mgkg -1 | 3.76±1.12 1.99±0.66 b 3.28±0.51 b 3.13±0.54 d 3.03±0.95 d | 7.09±1.29 4.16±1.09 b 6.59±1.51 b 5.47±1.33 d 6.15±1.59 d |
bCompare with matched group P＜0.01;
dCompare with model group P＜0.01.
4.6 the injection gentiopicrin is to the protective effect of Cavia porcellus alloimmunity liver damage
4.6.1 Cavia porcellus immunologic liver injury model.(1) liver suspension preparation: get one of Cavia porcellus, the anesthesia back makes its heparinization (tongue intravenous injection 1% heparin 0.4ml) under aseptic condition, and blood in portal vein perfusion normal saline eluting vascular shows inherent colour until liver then.The taking-up liver cuts into pieces, again with the normal saline cyclic washing.Get weight in wet base 10g hepatic tissue and add normal saline to 100ml, the glass grinding device grinds, and makes 10% liver homogenate normal saline suspension.(2) Freund's complete adjuvant preparation: liquid paraffin 55ml, anhydrous lanolin 15ml adds 75mgmL behind the autoclaving
-1Bacillus calmette-guerin vaccine 5ml, grind to form Emulsion.(3) liver suspension and Freund were mixed in 1: 1 by volume, with syringe take out repeatedly notes emulsion.Get 90 of healthy adult Cavia porcelluss, male and female are not limit, and are equally divided into 5 groups at random: normal physiological saline control group, model water matched group, model ten bifendate (200gkg
-1) group, and model+gentiopicrin (120,48mgkg
-1) two dosage groups of size.During experiment except that normal saline matched group, every lumbar injections of all the other each treated animals (ip) emulsifying agent 2mL, drug treatment simultaneously, every day 1 time, 30d continuously.Get blood behind the 30d, separation of serum is measured ALT, AST and lactate dehydrogenase isoenzyme L (LDH-L) content.Get liver simultaneously and fix with 10% formalin, section, HE dyeing, the degree of every routine animal immune liver damage and the therapeutical effect of medicine are respectively organized in observation under the light microscopic.
4.6.2 Serum ALT, AST, LDH measurement result (seeing Table 6) are as seen, model group Cavia porcellus ALT, AST value all obviously increase, and with matched group significant statistical significance are arranged relatively, and the modeling success is described.Gentiopicrin 120mgkg
-1, 48mgkg
-1, intraperitoneal injection can make ALT, AST, LDH reduce, and with model group the significance difference be arranged relatively in continuous 30 days.
Soak into situation (seeing Table 7) according to hepatocyte edema, acidophilia's change, the necrosis of kitchen range shape, epithelial duct hypertrophy and mononuclearcell in every group of each routine hepatic tissue, make semi-quantitative analysis.Result's (seeing Table 8) shows that tangible degeneration, necrosis appear in the model group animal liver cell, and the administration group has certain mitigation, illustrates that gentiopicrin has certain therapeutical effect to Cavia porcellus alloimmunity liver damage.
Table 6 injection gentiopicrin is to the influence of Cavia porcellus alloimmunity liver damage
| Group | Number of animals (n) | ALT (u/L) | AST (u/L) | LDH (u/L) |
| Matched group model group model+bifendate 200mgkg -1Model+gentiopicrin 120mgkg -1Model+gentiopicrin 48mgkg -1 | 10 13 12 11 10 | 35.5±9.79 175.5±66.64 a 97.1±41.92 b 90.7±37.33 b 132.0±51.18 a | 58.2±20.01 239.1±64.29 a 121.0±42.17 b 126.8±36.83 b 158.5±41.54 a | 216.4±42.3 249.5±48.70 230.6±59.16 234.1±39.40 237.8±37.85 |
aP＜0.01: compare with matched group;
bP＜0.05: compare with model group
Table 7 Cavia porcellus alloimmunity liver damage degree is divided
Table 8 injection gentiopicrin is to the pathology effects of Cavia porcellus alloimmunity liver damage
| Group | Number of animals | The red born of the same parents' degeneration edema of liver/acidophilia becomes | The swollen sample of necrosis/internal bud is died of illness | The epithelial duct hypertrophy | Mononuclearcell soaks into | ||||||||||||
| - | + | ++ | + + + | - | - | + | ++ | + + + | + | + + | + + + | - | + | + + | + + + | ||
| Normal water control group model saline control group model DDB group model+heavy dose of group model+small dose group | 10 10 10 10 10 | 10/10 0/1 | 3/4 2/7 4/6 2/4 | 4/3 6/2 3/2 5/4 | 3/2 2/1 2/1 3/2 | 10/10 2/2 1/2 0/1 | 1/2 3/4 2/3 2/2 | 5/4 3/2 4/3 4/3 | 4/4 2/3 3/2 4/4 | 10 1 1 1 | 8 7 6 8 | 2 2 1 1 | 8 3 3 4 | 2 6 3 3 2 | 2 1 1 2 | 2 2 1 2 | |
This experimental result shows that the reaction of nonspecific inflammations such as gentiopicrin xylol, albumin, granuloma induced by implantation of cotton pellets is inhibited.Can inflammation-inhibiting early stage telangiectasis, permeability be hyperfunction, ooze out and edema, also can the granulomatous formation of inflammation-inhibiting.Proved already that auricular concha edema that dimethylbenzene and albumin cause and pedal swelling all were to increase the acute inflammation model that vascular permeability is main change.The clear self-sustaining plantar subcutaneous injection of egg can cause inflammatory mediator release such as histamine, 5-HT, cause local capillary permeability to strengthen, ooze out and edema, cause that early stage acute inflammation such as red, hot, swollen, pain shows: the rat granuloma model that swells has similar pathological change to some clinical inflammation later stage granulation hyperplasia.17-hydroxy-11-dehydrocorticosterone has tangible antiinflammatory action, behind adrenalectomized mice administration gentiopicrin, still has antiphlogistic effects, illustrates that this medical instrument has direct antiinflammatory action.
In addition, gentiopicrin can resist mouse thymus and the spleen atrophy that hydrocortisone causes: also can resist the hepatic injury that immunoreation causes.Show that gentiopicrin may have immunoregulation effect.
Five, gentiopicrin is to the analgesic activity (tail-flick method) of mice
[principle] is thermic pain source with 55 ℃ ± 1 ℃ water bath with thermostatic control, after mice is fixing the above 5cm in its tail tip put into hot water, and the entry of record mouse tail is to the response time that throws away the water surface.The analgesic activity that reflects medicine by the change of measuring the administration mice response time.
[material] animal: mice.
Equipment: constant water bath box, stopwatch, syringe.
Medicine: gentiopicrin (clinical research official written reply 2003L03260,80mg/ props up) morphine hydrochloride (1mg/1ml).
[method]
1. adjusting constant water bath box, temperature is controlled at 55 ℃ ± 1 ℃.
2. observe drug effect normal saline group, morphine hydrochloride group, the equal subcutaneous injection administration of three various dose administration group mices, after the administration after 20,40 minutes, above 5cm puts into hot water with the mouse tail tip, and the entry of record mouse tail is to the response time that throws away the water surface.
Table 9 gentiopicrin injection is to analgesic activity (tail-flick method) (X ± S, n=20) second of mice
| Group | Dosage (mg/kg) | The differential responses time after the administration | |
| 20min | 40min | ||
| Matched group | 10 | 4.4±0.9 | 4.3±1.1 |
| Morphine hydrochloride | 10 | 20.8±1.7 ** | 5.4±1.5 ** |
| Gentiopicrin I | 50 | 5.4±4.3 | 6.8±5.8 * |
| Gentiopicrin II | 100 | 5.9±2.2 ** | 6.7±1.6 ** |
| Gentiopicrin III | 200 | 17.0±5.6 ** | 5.2±1.4 ** |
Annotate: the t check is with the matched group ratio between group
*P＜0.05,
*P＜0.01
Six, gentiopicrin is to the analgesic activity (hot plate method) of mice
The foot of [principle] mice contact hot plate, irriate and produce pain reaction (promptly licking metapedes) is a pain threshold to produce the time that pain reacts required.The analgesic activity that reflects medicine by the change of measuring administration mice pain threshold.
[material] animal: mice.
Equipment: intelligent hot-plate instrument, stopwatch, syringe.
Medicine: gentiopicrin (clinical research official written reply 2003L03260,80mg/ prop up), morphine hydrochloride (1mg/1ml).
[method]
1. the hot plate preheating is 10 minutes, regulates intelligent hot-plate instrument temperature controller and makes temperature be controlled at (55 ± 0.5) ℃.
2. screening qualified mouse, to get 18～22g female, and each 1 is placed on the hot plate, and mice is from being placed on the hot plate to the pain threshold of metapedes required time (second) as this Mus occurring licking.Allly lick the metapedes time less than 5 seconds or give it up greater than 30 seconds or leaper.Qualified mice is divided into 5 groups at random, 20 every group, repeat to survey its normal pain threshold, get two subnormal threshold of pain meansigma methodss, as pain threshold before this Mus administration.
3. observe drug effect normal saline group, morphine hydrochloride group, the equal subcutaneous injection administration of three various dose administration group mices, 15,35 minutes survey mice pain thresholds after the administration.As 60 seconds still reactionless, mice is taken out, in order to avoid scald, its bitterly the value of cutting off from calculated with 60 seconds.
Table 10 gentiopicrin injection is to analgesic activity (hot plate method) (x ± S, n=20) second of mice
| Group | Dosage (mg/kg) | The preceding threshold of pain of administration (s) | The different time threshold of pain after the administration | |
| 15min | 35min | |||
| Matched group | 10 | 21.5±5.1 | 18.2±6.6 | 21.2±5.0 |
| Morphine hydrochloride | 10 | 20.2±2.7 | 22.6±7.0 * | 20.3±7.2 |
| Gentiopicrin I | 50 | 21.2±4.7 | 24.7±4.7 ** | 22.6±8.0 |
| Gentiopicrin II | 100 | 21.2±5.7 | 27.4±8.7 ** | 23.1±6.4 |
| Gentiopicrin III | 200 | 21.8±4.2 | 60.0±0.0 ** | 46.8±12.9 ** |
Annotate: the t check is with the matched group ratio between group
*P＜0.05,
*P＜0.01
Seven, gentiopicrin is to the analgesic activity (writhing method) of mice
[principle]
Adopt mouse peritoneal injected chemical medicine, cause acute peritonitis and produce persistent pain stimulation, cause mice to produce " turning round body " reaction.Whether can reduce the writhing response number of times of mice after the observation administration, the analgesic activity of reflection medicine.
[material] animal: mice.
Equipment: syringe, syringe needle, enumerator.
Medicine: gentiopicrin (clinical research official written reply 2003 L03260,80mg/ prop up), morphine hydrochloride (1mg/1ml), HAC (6g/L).
[method]
Get 100 of mices, be divided into 5 groups at random, normal saline group, morphine hydrochloride group, three various dose administration groups, all subcutaneous injection by body weight.After the administration 20 minutes, each organizes mice all by body weight lumbar injection HAC, observes in 15 minutes and 30 minutes and respectively organizes the number of times that writhing response appears in mice, calculates this medicine analgesia percentage rate.
Table 11 gentiopicrin injection to the analgesic activity (writhing method) of mice (X ± S, n=20) inferior
| Group | Dosage (mg/kg) | Turn round the body number of times | Analgesia percentage rate (%) | ||
| 15min | 30min | 15min | 30min | ||
| Matched group | 10 | 51.1±9.3 | 24.1±4.4 | ||
| Morphine hydrochloride | 0.5 | 25.4±5.1 ** | 7.0±3.19 ** | 50.3 | 71.0 |
| Gentiopicrin I | 50 | 42.0±8.4 ** | 20.7±8.2 | 17.8 | 14.1 |
| Gentiopicrin II | 100 | 35.8±6.0 ** | 19.4±6.7 ** | 29.9 | 19.5 |
| Gentiopicrin III | 200 | 18.8±9.0 ** | 15.1±5.8 ** | 63.2 | 37.3 |
Annotate: t checks with the matched group ratio between group,
*P＜0.05,
*P＜0.01
From above result, can draw and the invention has the advantages that: this research is to have extracted the main component gentiopicrin to have carried out analgesia, antiinflammatory test first from Radix Gentianae Macrophyllae, proves the preparation that can be used for the arthritis medicine.
The specific embodiment
Embodiment 1
The pharmaceutical formulation gentiopicrin is prepared into tablet, is that example is raw materials used as follows with adjuvant and weight proportion thereof to produce 1000 of tablet products:
Gentiopicrin 200g
Starch 100g
Or
Radix Gentianae total glucosides (containing gentiopicrin about 70%) 285g
Starch 100g
Its preparation technology is undertaken by the common process of galenic pharmacy tablet, every heavy 0.3g, and every contains gentiopicrin 200mg.
Usage and dosage: oral, each 1,1 time on the one, children's is cut down according to the circumstance, and 30 days is a course of treatment.
Embodiment 2
The pharmaceutical formulation gentiopicrin is prepared into capsule, is that example is raw materials used as follows with adjuvant and weight proportion thereof to produce 1000 of capsule products:
Gentiopicrin 200g
Starch 100g
Or
Radix Gentianae total glucosides (containing gentiopicrin about 70%) 285g
Starch 100g
Its preparation technology is undertaken by the common process of galenic pharmacy capsule, every heavy 0.3g, and every contains gentiopicrin 200mg.
Usage and dosage: oral, each 1,1 time on the one, children's is cut down according to the circumstance.30 days is a course of treatment.
Embodiment 3
The pharmaceutical formulation gentiopicrin is prepared into granule, is that example is raw materials used as follows with adjuvant and weight proportion thereof to produce granule product 1000g:
Gentiopicrin 200g
Sucrose 400g
Dextrin 400g
Or
Radix Gentianae total glucosides (containing gentiopicrin about 70%) 285g
Sucrose 400g
Dextrin 400g
Preparation technology is undertaken by the common process of galenic pharmacy granule, every bag heavy 1g, and 1g contains gentiopicrin 200mg.
Usage and dosage: oral, each 1 bag, 1 time on the one, children's is cut down according to the circumstance.30 days is a course of treatment.
Embodiment 4
The pharmaceutical formulation gentiopicrin is prepared into syrup, is that example is raw materials used as follows with adjuvant and weight proportion thereof to produce syrup 1000mL:
Gentiopicrin 20g
Sucrose 600g
Distilled water adds to 1000mL
Or
Radix Gentianae total glucosides (containing gentiopicrin about 70%) 280g
Sucrose 600g
Distilled water adds to 1000mL
Its preparation technology is undertaken by the common process of galenic pharmacy syrup, and every bottle of 10mL, 1mL contain gentiopicrin 20mg.
Usage and dosage: oral, each 1 bottle, 1 time on the one, children's is cut down according to the circumstance.30 days is a course of treatment.
Embodiment 5
The pharmaceutical formulation gentiopicrin is prepared into injection, is that example is raw materials used as follows with adjuvant and weight proportion thereof to produce 1000 of injection products:
Gentiopicrin 200g
Injection mannitol 20g
Or
Radix Gentianae total glucosides (containing gentiopicrin about 70%) 285g
Injection mannitol 20g
Preparation technology is undertaken by the common process of galenic pharmacy injection, and every heavy 0.22g contains gentiopicrin 200mg.
Usage and dosage: intravenous drip, each 1, be dissolved in the 250mL glucose for injection injection, 1 time on the one, children's is cut down according to the circumstance.30 days is a course of treatment.
Claims (3)
1. gentiopicrin or contain the purposes of the Radix Gentianae total glucosides of gentiopicrin more than 50% in preparation treatment of arthritis medicine.
2. gentiopicrin or contain the Radix Gentianae total glucosides of gentiopicrin more than 50% in the purposes of preparation in the analgesic.
3. purposes according to claim 1 and 2 is characterized in that the medicine for preparing adopts tablet, capsule, powder, pill, granule, injection or Emulsion.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610104732 CN1939398A (en) | 2006-10-13 | 2006-10-13 | Use of gentiin in analgesic for treating arthritis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610104732 CN1939398A (en) | 2006-10-13 | 2006-10-13 | Use of gentiin in analgesic for treating arthritis |
Publications (1)
| Publication Number | Publication Date |
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| CN1939398A true CN1939398A (en) | 2007-04-04 |
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| CN 200610104732 Pending CN1939398A (en) | 2006-10-13 | 2006-10-13 | Use of gentiin in analgesic for treating arthritis |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104857008A (en) * | 2015-04-22 | 2015-08-26 | 宁夏医科大学 | Application of Gentiopicroside, Gent as a medicament for the treatment of neuropathic pain |
| CN106727652A (en) * | 2016-12-30 | 2017-05-31 | 福建中医药大学 | A kind of molecule Chinese medicine sustained release tablets for relief from osteoarthritis pain and preparation method thereof |
-
2006
- 2006-10-13 CN CN 200610104732 patent/CN1939398A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104857008A (en) * | 2015-04-22 | 2015-08-26 | 宁夏医科大学 | Application of Gentiopicroside, Gent as a medicament for the treatment of neuropathic pain |
| CN106727652A (en) * | 2016-12-30 | 2017-05-31 | 福建中医药大学 | A kind of molecule Chinese medicine sustained release tablets for relief from osteoarthritis pain and preparation method thereof |
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Open date: 20070404 |