CN1575797A - New use of medicine containing escin and its salt - Google Patents
New use of medicine containing escin and its salt Download PDFInfo
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- CN1575797A CN1575797A CN 200410062570 CN200410062570A CN1575797A CN 1575797 A CN1575797 A CN 1575797A CN 200410062570 CN200410062570 CN 200410062570 CN 200410062570 A CN200410062570 A CN 200410062570A CN 1575797 A CN1575797 A CN 1575797A
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Abstract
The present invention relates to the new pharmaceutical use of aescin andits salt, and is especially the application of aescin and its salt in preparing post-operation intestinal function recovering medicine. The medicine of aescin and its salt is administrated via intravenous injection.
Description
Technical field
The present invention relates to the new medicine use of aescine and salt thereof, be specifically related to aescine and salt thereof the purposes in preparation treatment postoperative intestine functional recovery medicine.
Background technology
Aescine is the triterpene saponin of the dry mature seed extraction of Chinese medicine Heavenly Teacher chestnut, aescine and salt thereof are oral or be injected at and be usually used in treating the cerebral edema that a variety of causes causes and the brain function imbalance that occurs together, inflammation that a variety of causes (as wound, burn, operation) causes and swelling, venous return obstacle disease etc. clinically, have very strong antiinflammatory, exudation effect, can obviously reduce acutely inflamed oozing out, but whether aescine and salt intravenous injection thereof have the effect that postoperative intestine functional recovers, and do not see bibliographical information.
It is the modal operation of surgery that abdominal operation or other need the operation of lumbar anesthesia or epidural anesthesia, the influence of being performed the operation and/or anaesthetizing, bowel dysfunction often appears in postoperative, mainly show as enterokinesia and disappear, postoperative aerofluxus, bowel movement function obstacle, directly influence patient more after, the 1st evacuation time after the desmopyknosis, recovering normal feed function as early as possible, is extremely important and urgent problem in the patients ' recovery process, also is an important step that promotes that body function recovers.
Summary of the invention
At above technological deficiency, the invention provides a kind of aescine and salt thereof the new purposes in the medicine that preparation treatment postoperative intestine functional recovers.
Aescine of the present invention and salt thereof not only are used for preparing the purposes of the human postoperative intestinal function recovery medicine of treatment, also are applicable to the purposes in other mammal postoperative intestinal function recovery medicines of preparation treatment.
Aescine and salt thereof are free aescine or are the salt of aescine among the present invention, when being aescine salt, its salt is aescine, aescine potassium, arginine aescine or other pharmaceutical salts, be preferably aescine or arginine aescine, wherein the arginine aescine can obtain by the method for describing among the patent application CN1376675, also can obtain by other conventional preparation method.
Aescine of the present invention and salt thereof should meet the requirement to medicine of the relevant drug standard of country.
Aescine of the present invention and salt thereof are in the medicinal application of preparation treatment intestinal function recovery, its administering mode is intravenously administrable (comprising intravenous injection and intravenous drip), injected dose with respect to the adult is: 1～30mg/ day (calculating with aescine), preferred dose is: 5-20mg/ day (in aescine).
Aescine of the present invention and salt thereof can adopt conventional preparation technology to make different dosage forms with different pharmaceutic adjuvants, as injection, injection powder pin, injectable microsphere, injectable emulsion or other injection preparation forms are preferably injection powder pin or injection.
Can the injection of aescine of the present invention and salt thereof be made the product of different size according to needs clinically, but the preferred specification of the present invention is every 5mg or 10mg or 15mg or 20mg or 25mg (calculating with aescine).
Result of the test shows, the present invention can obviously accelerate the slow down enterokinesia of animal pattern of enterokinesia, and gastric emptying is not had obvious influence, postoperative early stage (operation back 1-3 days) vein gives aescine, can obviously shorten postoperative intestine ring sound recovery time, aerofluxus and defecation time in advance, the present invention simultaneously can also alleviate inflammatory reaction, reduce inflammatory exudation, promote enterokinesia to recover.
Aescine provided by the invention and salt thereof have the low advantage of good effect side effect when using as the intestinal function recovery medicine; Intravenously administrable has overcome after the operation (operation back 1-3 day) in a short time can not oral administration and be unfavorable for the defective of intestinal function recovery.
The specific embodiment
The present invention is further elaborated below in conjunction with embodiment and experimental example, but be not limited to this.
Embodiment 1
Take by weighing the 500mg aescine, water for injection adds to 100ml, charcoal treatment, filter clear filtrate, after the packing, make the aescine sodium injection.
Embodiment 2
Take by weighing 500mg aescine and mannitol 750mg, with the dissolving of 150ml water for injection, charcoal treatment, filter clear filtrate, the packing postlyophilization makes aescin for injection.
Embodiment 3
Take by weighing 1000mg aescine and mannitol 7500mg, with the dissolving of 150ml water for injection, charcoal treatment, filter clear filtrate, spray drying, packing make aescin for injection.
Embodiment 4
Take by weighing 1000mg aescine and mannitol 7500mg, with the dissolving of 150ml water for injection, charcoal treatment, filter clear filtrate, spray drying, packing make aescin for injection.
Embodiment 5
Take by weighing the 2000mg aescine, water for injection adds to 200ml, charcoal treatment, filter clear filtrate, the packing postlyophilization makes aescin for injection.
Embodiment 1 aescine is to the influence of acute inflammation, mice capillary permeability
Test method: get 60 of mices, male, body weight 19～21g is divided into 5 groups at random, and 12 every group, administration volume: 0.20ml/20g, administration was given mouse mainline 0.5% azovan blue solution, administration volume: 0.20ml/20g after 8 hours; The acetic acid 0.20ml of lumbar injection 1.0% put to death mice after 20 minutes immediately, drew the 6.0ml normal saline, injected the abdominal cavity, gently rubbed abdominal part, drew peritoneal fluid, and centrifugal (3000rpm 10min), measures absorption value in 590nm wavelength place, organizes a t check.
The result shows that aescine height, middle dosage group have obvious inhibitory action to the mice capillary permeability, and (P＜0.05) shows that aescine has stronger antiinflammatory action.
Table 1 aescine is to the influence of mice capillary permeability
Group dosage OD
NS????????????????????????????????0.610±0.162
Diclofenac sodium 5mg/kg 0.331 ± 0.123
△ △
Aescine high dose group 3.6mg/kg 0.359 ± 0.135
△ △
Dosage group 1.8mg/kg 0.445 ± 0.121 in the aescine
△
Aescine low dose group 0.9mg/kg 0.549 ± 0.155
Compare with the normal saline group,
△: p＜0.05;
△ △: p＜0.01
The influence of 2 pairs of normal mouse gastric emptyings of test example
(1) test objective: gavaging methyl orange to normal mouse, is index with methyl orange residual rate in the stomach, and the observation vein gives aescine and whether promotes gastric emptying.
(2) content of the test
Be subjected to the reagent thing: aescine; Motilium (10mg/ grain, Xian-Janssen Pharmaceutical Ltd., lot number: 010214002); Methyl orange (chemical reagent station, Chinese Medicine Shanghai, lot number: 000308); Raceanisodamine (tablet, 10mg/ grain, Huanghai Pharmaceutical Plant, Qingdao, lot number: 001137); Sodium bicarbonate (Shanghai reagent four factories, lot number: 000612)
Instrument: centrifuge (DL-4000B refrigerated centrifuger, Anting Scientific Instrument Factory, Shanghai); Spectrophotometer (UV-9100 Beijing Rayleigh scientific instrument factory)
Animal: secondary Kunming kind white mice, male and female half and half, body weight 22-24g, Shandong Province's natural drug Engineering Technical Research Centre Experimental Animal Center provides the animal quality certification: (matter) word 2001003 is moved in the Shandong.
Test method: get mice 50, male and female half and half, fasting 12 hours, be divided into 5 groups at random, 10 every group, negative control group gavages distilled water, positive controls gavages 1mg/ml motilium suspension, and the high, medium and low dosage group of aescine vein gives aescine.After the administration 20 minutes, gavage 0.2ml 0.1% methyl orange solution, to 20 minutes execution mices after the methyl orange, cut open the belly, get stomach, stomach is placed the 10ml cillin bottle, the sodium bicarbonate solution that adds 8ml 0.1% is cut off stomach with little shears, gastric content is fully washed in sodium bicarbonate solution, shaken up, get supernatant, insert in the test tube, centrifugal 10 minutes of 2000rpm gets supernatant and measures absorption value, 0.1% sodium bicarbonate solution zeroising in the 420nm place, and shake up the back with the sodium bicarbonate solution that 0.1% methyl orange solution 0.2ml adds 8ml 0.1% and survey trap as radix methyl orange optical density, be calculated as follows methyl orange stomach residual rate: methyl orange stomach residual rate (%)=gastric methyl orange optical density/radix methyl orange optical density * 100%, each organizes t check between methyl orange stomach residual rate employing group, carries out statistical procedures.
(3) result of the test:
The result shows that the motilium group can significantly promote mice gastric emptying (P＜0.01), and each dosage group intravenous injection of aescine does not all have obvious influence (P＞0.05) to gastric emptying, and promptly aescin for injection does not have promotion or inhibitory action to gastric emptying.
Table 2 aescine is to the influence of normal mouse gastric emptying
Group dosage (mg/kg) methyl orange stomach residual rate (%)
Blank group 51.2 ± 12.0
Motilium group 20 32.3 ± 9.3
*
Aescine high dose group 3.6 54.5 ± 7.7
*
Dosage group 1.8 57.2 ± 8.5 in the aescine
*
Aescine low dose group 0.9 53.8 ± 14.5
*
Annotate: compare * P＞0.05, * * P＜0.01 with the blank group
Test example 3: to the slow down influence of mouse small intestine wriggling of enterokinesia
(1) test objective: to the small intestinal peristalsis mouse gavaging active carbon that slows down, be index, observe aescine and whether promote the enterokinesia mouse small intestine wriggling that slows down with the propelling rate of active carbon in small intestinal.
(2) content of the test:
Get 60 of mices, male and female half and half are divided into 6 groups at random, and 10 every group, wherein 5 groups every gavages 1.5mg/ml raceanisodamine suspension 0.5ml, make the enterokinesia model that slows down, and 1 group is the blank group in addition.Modeling group administration every day 1 time, successive administration 3 days.After last is given the raceanisodamine suspension 1 hour, the high, medium and low dosage group of aescine intravenous injection aescine; It is 1mg/ml motilium suspension that positive controls gavages concentration, and model group and blank group gavage distilled water.The administration volume is 0.4ml/20g.Gavaged 5% Insta-Char 0.5ml after the administration in 30 minutes, put to death mice after 20 minutes, the taking-up intestinal tube of cutting open the belly, measure the distance conduct " active carbon intestinal in advance distance " of pylorus to the active carbon forward position, measure the distance conduct full intestinal length of pylorus, be calculated as follows: advance distance (cm) in active carbon propelling rate=active carbon intestinal/full intestinal length (cm) * 100% to caecum.Each organizes t check between active carbon propelling rate employing group, carries out statistical procedures.
Other gets 50 of mices, observes the influence that the arginine aescine promotes small intestinal with said method.
(3) result of the test:
The result shows, motilium can significantly promote mouse small intestine wriggling (P＜0.01), aescine height, middle dosage group can significantly promote intestinal propulsion (P＜0.05), and low dosage is not obvious to the influence of small intestinal peristalsis, and the arginine aescine is similar to aescine to the effect that intestinal promotes.
Table 3 aescine is to the slow down influence of mouse small intestine wriggling of enterokinesia
Group dosage (mg/kg) active carbon propelling rate (%)
Blank group 68.2 ± 7.3
Model group 48.0 ± 10.4
Motilium group 20 63.1 ± 8.4
*
Aescine high dose group 3.6 59.9 ± 9.2
*
Dosage group 1.8 57.8 ± 10.3 in the aescine
*
Aescine low dose group 0.9 53.9 ± 8.6
Annotate: administration group and model group be than * P＜0.05, * * P＜0.01
Table 4 arginine aescine is to the slow down influence of mouse small intestine wriggling of enterokinesia
Group dosage (mg/kg) active carbon propelling rate (%)
Blank group 67.9 ± 8.1
Model group 49.2 ± 9.1
Motilium group 20 65.0 ± 9.9
*
Arginine aescine high dose group 3.6 58.8 ± 7.1
*
Arginine aescine low dose group 0.9 52.6 ± 9.3
Annotate: administration group and model group be than * P＜0.05, * * P＜0.01
Test example 4 arginine aescine promote postoperative intestine functional to recover test
Test method: select 16 of healthy Beagle dogs, male and female half and half are divided into 2 groups at random.After the fasting 12 hours, at first give the atropine intramuscular injection, adopt penthiobarbital (25mg/kg) intravenous anesthesia after 1 hour, the animal respirator assisted respiartion, row small bowel resection anastomosis (the long 5cm of excision intestinal segment, surgical field of view exposes 1h, from first to last checks small intestinal 3 times in the operation process).Postoperative intravenous drip arginine aescine 0.5mg/kg, successive administration 5 days is observed the influence to the dog intestinal function recovery.The result shows, gives the arginine aescine and can obviously shorten time and the defecation time that postoperative intestine ring sound occurs, and shows that the arginine aescine can promote the recovery of postoperative intestine functional.
Table 1 arginine aescine is to the influence of dog intestinal resection and anastomosis postoperative intestinal function recovery
| Group | Borborygmus recovery time (h) | Defecation time (h) |
| Matched group | ????14.5±3.22 | ??29.26±6.12 |
| Arginine aescine group | ????9.0±3.35 * | ??19.68±4.91 * |
Compare * P＜0.01 with matched group
Test example 5: aescine is to the influence of abdominal postoperative intestinal function recovery
Aescine is clinical to be used for the treatment of the cerebral edema that a variety of causes causes and the brain function imbalance that occurs together, inflammation that a variety of causes (as wound, burn, operation) causes and swelling, venous return obstacle disease etc.Select abdominal part gastrointestinal procedures patient (60 examples, be divided into matched group and aescine group at random, every group 30 example) and non-gastrointestinal procedures patient (30 examples, be divided into matched group and aescine group at random, every group 15 example), in with aescine treatment operation back inflammation and swelling, observe its influence to gastrointestinal function.
Dosage is the 0.4mg/kg body weight, but the highlyest is no more than 25mg/ day.
The result shows, to gastrointestinal procedures and non-gastrointestinal procedures patient, the time that the intravenous drip aescine all can make aerofluxus and defecation is (p＜0.01) in advance, reduces that non-gastrointestinal procedures patient feels sick and the incidence rate of abdominal distention, shows the recovery of its back gastrointestinal peristalsis function that can promote to perform the operation.
Table 5 aescine to gastrointestinal procedures after the influence of restoration of gastrointestinal function
| Group | Borborygmus recovery time (h) | Evacuation time (h) | Defecation time (h) |
| Matched group | 33.4±5.98 | ?42.91±6.22 | ?55.26±9.12 |
| The aescine group | 26.0±4.39 * | ?33.32±5.65 * | ?42.36±6.03 * |
Compare * P＜0.01 with matched group
Table 6 aescine to non-gastrointestinal procedures after the influence of restoration of gastrointestinal function
| Group | Nauseating incidence rate | The abdominal distention incidence rate | Evacuation time (h) | Defecation time (h) |
| Matched group | ????73.3 | ????46.7 | ??43.86±9.45 | ??51.46±11.23 |
| The aescine group | ????20.0 * | ????6.67 * | ??31.89±6.99 * | ??39.98±7.87 * |
Compare * P＜0.01 with matched group
Claims (7)
1. aescine and salt thereof are preparing the purposes for the treatment of in the postoperative intestine functional recovery medicine.
2. purposes according to claim 1 is characterized in that injection aescine and salt thereof the purposes in preparation treatment postoperative intestine functional recovery medicine.
3. purposes according to claim 1 and 2 is characterized in that aescine salt is aescine or arginine aescine.
4. purposes according to claim 1 and 2 is characterized in that aescine and salt thereof can make powder pin or injection separately or with pharmaceutically acceptable carrier combinations.
5. purposes according to claim 1 and 2 is characterized in that aescine and salt thereof adult injected dose is 1-30mg/ day (in an aescine).
6. purposes according to claim 5 is characterized in that aescine and salt thereof adult's injected dose is 5-20mg/ day (in an aescine).
7. purposes according to claim 4 is characterized in that the lyophilized injectable powder of aescine and salt thereof or the specification of injection are every 5mg or 10mg or 15mg or 20mg or 25mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410062570 CN1575797A (en) | 2003-07-05 | 2004-07-02 | New use of medicine containing escin and its salt |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN03147314.8 | 2003-07-05 | ||
| CN03147314 | 2003-07-05 | ||
| CN 200410062570 CN1575797A (en) | 2003-07-05 | 2004-07-02 | New use of medicine containing escin and its salt |
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|---|---|
| CN1575797A true CN1575797A (en) | 2005-02-09 |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100357312C (en) * | 2005-07-15 | 2007-12-26 | 武汉爱民制药有限公司 | Lysine aescin saponin, its preparation and use |
| CN100428940C (en) * | 2005-07-15 | 2008-10-29 | 武汉爱民制药有限公司 | Notoginsenoside pharmaceutical composition and method for preparing the same and use thereof |
| CN101084911B (en) * | 2006-06-08 | 2011-07-20 | 中国科学院上海药物研究所 | Notoginsenoside sodium freezing-dried emulsion and preparation method thereof |
| CN102755297A (en) * | 2011-04-29 | 2012-10-31 | 天津药物研究院 | Escin B freeze-dried powder injection and preparation method and application thereof |
| CN102836133A (en) * | 2012-08-31 | 2012-12-26 | 武汉普生制药有限公司 | Sodium aescinate freeze-dried powder injection and preparation method thereof |
-
2004
- 2004-07-02 CN CN 200410062570 patent/CN1575797A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100357312C (en) * | 2005-07-15 | 2007-12-26 | 武汉爱民制药有限公司 | Lysine aescin saponin, its preparation and use |
| CN100428940C (en) * | 2005-07-15 | 2008-10-29 | 武汉爱民制药有限公司 | Notoginsenoside pharmaceutical composition and method for preparing the same and use thereof |
| CN101084911B (en) * | 2006-06-08 | 2011-07-20 | 中国科学院上海药物研究所 | Notoginsenoside sodium freezing-dried emulsion and preparation method thereof |
| CN102755297A (en) * | 2011-04-29 | 2012-10-31 | 天津药物研究院 | Escin B freeze-dried powder injection and preparation method and application thereof |
| CN102836133A (en) * | 2012-08-31 | 2012-12-26 | 武汉普生制药有限公司 | Sodium aescinate freeze-dried powder injection and preparation method thereof |
| CN102836133B (en) * | 2012-08-31 | 2014-03-12 | 武汉普生制药有限公司 | Sodium aescinate freeze-dried powder injection and preparation method thereof |
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