CN103041046A - Application of callicarpa kwangtungensis and extract thereof in preparation of anti-peptic ulcer medicaments - Google Patents
Application of callicarpa kwangtungensis and extract thereof in preparation of anti-peptic ulcer medicaments Download PDFInfo
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- CN103041046A CN103041046A CN2013100324152A CN201310032415A CN103041046A CN 103041046 A CN103041046 A CN 103041046A CN 2013100324152 A CN2013100324152 A CN 2013100324152A CN 201310032415 A CN201310032415 A CN 201310032415A CN 103041046 A CN103041046 A CN 103041046A
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Abstract
The invention discloses application of callicarpa kwangtungensis and an extract thereof in preparation of anti-peptic ulcer medicaments. Peptic ulcer diseases include a gastric ulcer and a duodenal ulcer. When the callicarpa kwangtungensis is applied to preparation of the medicaments for treating peptic ulcer diseases, the contents of forsythiaside B and poliumoside in the callicarpa kwangtungensis extract at least reach up to either 1.2% or 0.6%. The callicarpa kwangtungensis and the extract thereof have the treatment effects on the peptic ulcer caused by various factors, can obviously promote the ulcer healing, and can prepare the anti-peptic ulcer medicaments.
Description
Technical field
The present invention relates to medical technical field, or rather, specifically relate to Callicarpa kwangtungensis Chun extract and contain its pharmaceutical composition as the purposes of medicament for resisting peptic ulcer.
Technical background
Callicarpa kwangtungensis Chun Callicarpa kwangtungensis Chun is Verenaceae Callicarpa plant, income " Chinese pharmacopoeia First in 2010, its medicinal part is dry stem branch and leaf, has astringing to arrest bleeding, dissipating blood stasis, the function of heat-clearing and toxic substances removing is used for epistaxis, spitting of blood, spit blood, have blood in stool metrorrhagia, traumatic hemorrhage, cough due to lung-heat, laryngopharynx swelling and pain, pathopyretic ulcer, burn due to hot liquid or fire.Miao Ethnomedicine is spitted blood with Callicarpa kwangtungensis Chun stem, leaf treatment stomachache, chest pain, measles, migraine, traumatic hemorrhage (" China National medicine will is wanted ", Jia Min is such as, Li Xingwei, Chinese Medicine science and technology publishing house 2005)." Chinese medicine resource will is wanted " (Chinese Medicinal Materials Co, Science Press, 1994) record Callicarpa kwangtungensis Chun root, stem, leaf can be used for treating chest pain, spit blood migraine, stomachache, traumatic hemorrhage.
Callicarpa kwangtungensis Chun is the primary raw material of Chinese patent medicine " KANGGONGYAN PIAN " and " Kanggongyan capsule ", and Callicarpa kwangtungensis Chun dry extract accounts for 78% of total composition, is mainly used in treating gynecological inflammation (cervicitis, cervical erosion).
Callicarpa kwangtungensis Chun mainly contains the chemical constituents such as flavone, Phenylpropanoid Glycosides, triterpene, phenolic acid.Chinese Pharmacopoeia is with two kinds of lignans constituents---and forsythiaside B (forsythiaside B) and poliumoside (poliumoside) are as the quality control index of Callicarpa kwangtungensis Chun and " KANGGONGYAN PIAN " and " Kanggongyan capsule ".Modern pharmacological research shows that Callicarpa kwangtungensis Chun has the effects such as hemostasis (ethanol extraction), analgesia (total flavones), antibacterial (ethanol extraction, volatile oil), antiinflammatory (total flavones).
Although report shows Callicarpa kwangtungensis Chun and can treat stomachache, and Callicarpa kwangtungensis Chun extract has analgesia, hemostasis, bacteriostasis.But still can not directly know by inference accordingly, any clearly report is not arranged yet, Callicarpa kwangtungensis Chun or its extract have the effect for the treatment of peptic ulcer.The reason of stomachache is very complicated on the one hand, and gastritis, stomach spasm, gastric ulcer can cause that all the stomachache whether Callicarpa kwangtungensis Chun causes all reasons all effectively it be unclear that; On the other hand, analgesia is not the basic goal for the treatment of of peptic ulcer, and the basic goal for the treatment of of peptic ulcer is to make ulcer healing, eases pain and does not mean that ulcer healing.Therefore, Callicarpa kwangtungensis Chun of the present invention or its extract are the discoveries of a novelty in the effect for the treatment of peptic ulcer.
Summary of the invention
The present inventor studies discovery, and Callicarpa kwangtungensis Chun extract has therapeutical effect to the digestive tract ulcer due to the many reasons, can obviously promote ulcer healing, can be used for preparing medicament for resisting peptic ulcer.The present invention is based on above-mentioned discovery and be accomplished.
An object of the present invention is to provide Callicarpa kwangtungensis Chun for the preparation of purposes and consumption in the medicine for the treatment of peptic ulcer.
Another object of the present invention has provided Callicarpa kwangtungensis Chun extract for the preparation of purposes and consumption in the medicine for the treatment of peptic ulcer.
A further object of the invention has provided a kind of pharmaceutical composition that is used for the treatment of peptic ulcer.
The present invention's technical scheme that adopts of dealing with problems is: Callicarpa kwangtungensis Chun can be used for preparing the medicine for the treatment of peptic ulcer, and wherein said peptic ulcer refers to: gastric ulcer, duodenal ulcer.
The dosage that Callicarpa kwangtungensis Chun is used for the treatment of in the medicine of peptic ulcer is per kilogram of body weight 0.2-2.0g for each person every day, preferred 0.5-1.0g.
Callicarpa kwangtungensis Chun extract also can be for the preparation of the medicine for the treatment of peptic ulcer, and wherein said peptic ulcer refers to: gastric ulcer, duodenal ulcer; Forsythiaside B in the described Callicarpa kwangtungensis Chun extract and the content of poliumoside should reach 1.2%, 0.6% at least.
The dosage that Callicarpa kwangtungensis Chun extract is used for the treatment of in the medicine of peptic ulcer is per kilogram of body weight 6-60mg for each person every day, preferred 15-30mg.
A kind of pharmaceutical composition that is used for the treatment of peptic ulcer, wherein comprise the Callicarpa kwangtungensis Chun of effective dose or the acceptable excipient of pharmacy that Callicarpa kwangtungensis Chun extract is chosen wantonly, described effective dose is for each person every day per kilogram of body weight 0.2-2.0g of Callicarpa kwangtungensis Chun crude drug; Callicarpa kwangtungensis Chun extract is per kilogram of body weight 6-60mg for each person every day, and route of administration is oral administration.
The extracting method of described Callicarpa kwangtungensis Chun extract, according to the following steps preparation: get the Callicarpa kwangtungensis Chun crude drug, be cut into segment or sheet, add the water reflux, extract, secondary of 3～20 times of volumes, 3h for the first time, 2h filters for the second time, and filtrate merges, and filtrate is concentrated, is drying to obtain.
Above-mentioned each medicine will be made the multiple peroral dosage forms such as tablet, granule, capsule, oral liquid.The medicine of above-mentioned various dosage forms all can be according to the conventional method preparation of pharmaceutical field.
The specific embodiment
The below provides specific embodiment and experimental example to further specify the present invention, still, should be understood to, and these embodiment and experimental example are only used for the more detailed usefulness that is described more specifically, and should not be construed as for any form restriction the present invention.
Mutual conversion between animals administer dosage and the human body dosage is according to the medical experiment generic principles, and human body medicine dosage is about 6～7 times of rat drug dose, is about 12 times of mice drug dose.Also can convert according to extract yield between Callicarpa kwangtungensis Chun extract dosage and Callicarpa kwangtungensis Chun crude drug dosage, by the method that the present invention describes, the Callicarpa kwangtungensis Chun extract yield is about 3%.
Embodiment 1: the preparation of Callicarpa kwangtungensis Chun extract
Get Callicarpa kwangtungensis Chun crude drug 10kg, be cut into segment or sheet, add the water reflux, extract, secondary of 10 times of volumes, 3h for the first time, 2h filters for the second time, and filtrate merges, and filtrate is concentrated, and lyophilization gets extract 356g.With " forsythiaside B in the described HPLC chromatography determination of Chinese pharmacopoeia (2010) Callicarpa kwangtungensis Chun extract and the content of poliumoside.The result is for being respectively 1.6% and 0.9%.
Embodiment 2: the preparation of Callicarpa kwangtungensis Chun extract capsule
Formula table:
| Composition | Every capsule consumption |
| Callicarpa kwangtungensis Chun extract | 100mg |
| Pregelatinized Starch | 50mg |
| Sodium carboxymethyl cellulose | 10mg |
| Magnesium stearate | 20mg |
| 10% polyvidone alcoholic solution | In right amount |
Preparation technology: supplementary material is dry in advance, cross 100 mesh sieves, for subsequent use.With the mentioned component mixing, cross 60 mesh sieves three times by prescription, add an amount of 10% polyvidone ethanol (95%) solution soft material processed, cross 18 mesh sieves and granulate, 40 ℃ of dryings are crossed 16 mesh sieve granulate, are packed in the hard gelatin capsule.
A kind of pharmaceutical composition that is used for the treatment of peptic ulcer of the present invention, wherein comprise the Callicarpa kwangtungensis Chun of effective dose or the acceptable excipient of pharmacy that Callicarpa kwangtungensis Chun extract is chosen wantonly, " the acceptable excipient of pharmacy " that use in the medicine of the present invention can be the excipient of any routine in the pharmaceutical preparation.The selection of special excipient will be depended on administering mode or disease type and the state that is used for the treatment of particular patient.Be used for the preparation method of suitable drug of specific administration pattern fully in drug world technical staff's the ken.For example, can be used as diluent, carrier, filler, binding agent, wetting agent, disintegrating agent, absorption enhancer, surfactant, absorption carrier and the lubricant etc. that the acceptable excipient of pharmacy comprises the pharmaceutical field routine.In case of necessity, can also in medicine, add flavouring agent, preservative and sweetener etc.
Embodiment 3: Callicarpa kwangtungensis Chun extract is to the therapeutical effect of the acute rat gastric ulcer model of aspirin type
40 of the healthy male SD rat of body weight between 180～220g are divided into 6 groups: 1: Normal group at random; 2: the Ulcer Models group; 3:20mg/kg Callicarpa kwangtungensis Chun extract treatment group; 4:50mg/kg Callicarpa kwangtungensis Chun extract treatment group; 5:200mg/kg Callicarpa kwangtungensis Chun extract treatment group; 6:80mg/kg colloidal bismmth pectin treatment group; Every group each 8.Refuse any medicine for 1 group; All the other are respectively organized first fasting and prohibit water 24h, then gavage gives the aspirin of 200mg/kg, behind the 1h, 2 groups of sterilization water gavages that give 5mL/kg, 3～6 groups of disposable 20mg/kg Callicarpa kwangtungensis Chun extract, 50mg/kg Callicarpa kwangtungensis Chun extract, 200mg/kg Callicarpa kwangtungensis Chun extract, 80mg/kg bismuth potassium citrate gavages of giving respectively.Anesthetized animal behind the 4h is got stomach, places fixedly 15min of 1% formalin, dissects, and observation mucosal lesion situation press Guth method calculating ulcer index.The results are shown in Table 1.
Table 1
| Grouping | Ulcer index |
| Normal group | 0.8±0.9 |
| The Ulcer Models group | 46.4±10.1 |
| Callicarpa kwangtungensis Chun extract 20mg/kg group | 28.3±6.7 |
| Callicarpa kwangtungensis Chun extract 50mg/kg group | 15.8±5.9 |
| Callicarpa kwangtungensis Chun extract 200mg/kg group | 4.9±3.1 |
| Colloidal bismmth pectin 80mg/kg group | 11.3±5.4 |
The result shows that 20～200mg/kg Callicarpa kwangtungensis Chun extract can significantly suppress the formation of the rat gastric ulcer due to the aspirin.Be converted to human dose, this dosage range is about each 3mg～30mg/kg, by twice calculating in one day, for each person every day per kilogram of body weight 6～60mg.Be scaled Callicarpa kwangtungensis Chun crude drug amount and be per kilogram of body weight 0.2～2.0g for each person every day.
Embodiment 4: Callicarpa kwangtungensis Chun extract is to the therapeutical effect of mice bundle water stress gastric ulcer model
30 of Kunming mouses, male and female half and half, body weight 18～22g, fasting, the free 12h that drinks water are divided into 3 groups: model group, 100mg/kg Callicarpa kwangtungensis Chun processed group, 200mg/kg Callicarpa kwangtungensis Chun processed group at random.Model group gives the normal saline of equal volume.After each organizes once daily 30min, the binding of mice extremity is fixed on the special Mus plate, the neat xiphoid-process of the water surface, uprightly be dipped in the water bath with thermostatic control of (22 ± 1) ℃, take out behind the water logging 10h and put to death, get stomach, place fixedly 15min of 1% formalin, dissect, microscopically is observed ulcer, calculates ulcer index.The results are shown in Table 2.
Table 2
| Grouping | Ulcer index |
| The Ulcer Models group | 48.6±18.2 |
| Callicarpa kwangtungensis Chun extract 100mg/kg group | 35.1±9.6 |
| Callicarpa kwangtungensis Chun extract 200mg/kg group | 22.5±7.3 |
The result shows that 100～200mg/kg Callicarpa kwangtungensis Chun extract can significantly suppress the generation of mice stress ulcer.Be converted to human dose, this dosage range is about each 8mg～16mg/kg, by twice calculating in one day, for each person every day per kilogram of body weight 16～32mg.Be scaled Callicarpa kwangtungensis Chun crude drug amount and be per kilogram of body weight 0.5～1.0g for each person every day.
Embodiment 5: the Callicarpa kwangtungensis Chun extract Dichlorodiphenyl Acetate burns the therapeutical effect of rat gastric ulcer model
30 of the healthy male SD rat of body weight between 180～220g are divided into 3 groups at random: model group, 50mg/kg Callicarpa kwangtungensis Chun extract processed group, 100mg/kg Callicarpa kwangtungensis Chun extract processed group.Every group each 10.Before the art, fasting 24h freely drinks water.Etherization is opened the abdominal cavity, and internal diameter 5mm glass tubing is vertically placed near on the body of stomach serosal surface at pylorus place, adds glacial acetic acid 0.1mL in tube chamber, and is local with the normal saline cleaning with the cotton swab glacial acetic acid that exhausts behind the 1min, covers omentum majus, sews up stomach wall.The postoperative normal diet begins gastric infusion from second day, and model group gives the tap water of equal volume, and one day 2 times, successive administration 10 days.Put to death rat on the 11st day, get stomach, place fixedly 15min of 1% formalin, cut off stomach, measure transverse diameter and the vertical footpath (mm) of ulcer kitchen range, calculate ulcer area (mm
2) as ulcer index.The results are shown in Table 3.
Table 3
| Grouping | Ulcer index |
| The Ulcer Models group | 3.2±0.5 |
| Callicarpa kwangtungensis Chun extract 50mg/kg group | 2.1±0.6 |
| Callicarpa kwangtungensis Chun extract 100mg/kg group | 0.9±0.4 |
Rat gastric ulcer due to the result's demonstration, 50～100mg/kg Callicarpa kwangtungensis Chun extract Dichlorodiphenyl Acetate has significant promotion Healing.Be converted to human dose, this dosage range is about each 8mg～16mg/kg, one day twice be per kilogram of body weight 16～32mg for each person every day.Be scaled Callicarpa kwangtungensis Chun crude drug amount and be per kilogram of body weight 0.5～1.0g for each person every day.
The clinical treatment case
46 years old male, body weight 57kg has a stomachache, returns acid for a long time.Be diagnosed as gastric ulcer through gastroscopy.Recurrence after the routine of western medicine treatment.Give the Callicarpa kwangtungensis Chun crude drug, 18g every day (per kilogram of body weight 0.32g every day), decocting 2 times merges and fries in shallow oil juice, takes at twice continuous 1 month.After 2 days, stomachache obviously alleviates, and stomachache is basic after 1 week disappears, gastroscope check after 1 month, gastric ulcer healing.
26 years old women, body weight 47kg, long-term stomachache, take on an empty stomach and night as acute, reach after the meal and can alleviate after taking medicament for resisting peptic ulcer.Be diagnosed as superficial gastritis through gastroscopy, duodenal ulcer.Because of undesirable this Drug therapy that transfers to of western medicine effect.Give the Callicarpa kwangtungensis Chun crude drug, 30g every day (per kilogram of body weight 0.64g every day), decocting 2 times merges and fries in shallow oil juice, takes at twice continuous 1 first quarter moon.After 2 days, stomachache obviously alleviates, and pain disappears substantially after 1 week, gastroscope check after treatment finishes, and superficial gastritis takes a turn for the better, and duodenum heals substantially.
Claims (8)
- Callicarpa kwangtungensis Chun for the preparation of the treatment peptic ulcer medicine in purposes, wherein said peptic ulcer refers to: gastric ulcer, duodenal ulcer.
- 2. the dosage that is used for the treatment of in the medicine of peptic ulcer of Callicarpa kwangtungensis Chun is per kilogram of body weight 0.2-2.0g for each person every day.
- 3. the dosage that is used for the treatment of in the medicine of peptic ulcer of described Callicarpa kwangtungensis Chun is per kilogram of body weight 0.5-1.0g for each person every day according to claim 2.
- Callicarpa kwangtungensis Chun extract for the preparation of the treatment peptic ulcer medicine in purposes, wherein said peptic ulcer refers to: gastric ulcer, duodenal ulcer; Forsythiaside B in the described Callicarpa kwangtungensis Chun extract and the content of poliumoside should reach 1.2%, 0.6% at least.
- 5. the dosage that is used for the treatment of in the medicine of peptic ulcer of Callicarpa kwangtungensis Chun extract is per kilogram of body weight 6-60mg for each person every day.
- 6. the dosage that is used for the treatment of in the medicine of peptic ulcer of described Callicarpa kwangtungensis Chun extract is per kilogram of body weight 15-30mg for each person every day according to claim 5.
- 7. pharmaceutical composition that is used for the treatment of peptic ulcer, wherein comprise the Callicarpa kwangtungensis Chun of effective dose or the acceptable excipient of pharmacy that Callicarpa kwangtungensis Chun extract is chosen wantonly, described effective dose is for each person every day per kilogram of body weight 0.2-2.0g of Callicarpa kwangtungensis Chun crude drug; Callicarpa kwangtungensis Chun extract is per kilogram of body weight 6-60mg for each person every day.
- 8. the extracting method of a claim 5 or 7 described Callicarpa kwangtungensis Chun extracts, according to the following steps preparation: get the Callicarpa kwangtungensis Chun crude drug, be cut into segment or sheet, add the water reflux, extract, secondary of 3～20 times of volumes, 3h for the first time, 2h filters for the second time, filtrate merges, and filtrate is concentrated, is drying to obtain.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104983598A (en) * | 2015-06-17 | 2015-10-21 | 新疆医科大学第一附属医院 | Application of poliumoside in skin pigmentation inhibiting and cosmetic whitening |
| CN105250514A (en) * | 2015-11-19 | 2016-01-20 | 吴斌 | Medicine for treating duodenal ulcer |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1403104A (en) * | 2001-09-03 | 2003-03-19 | 陈益青 | Recipe of gastropathy treating Chinese herbal medicine |
| CN1322890C (en) * | 2004-03-29 | 2007-06-27 | 刘尚东 | Medicine for treating gastric ulcer |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104983598A (en) * | 2015-06-17 | 2015-10-21 | 新疆医科大学第一附属医院 | Application of poliumoside in skin pigmentation inhibiting and cosmetic whitening |
| CN105250514A (en) * | 2015-11-19 | 2016-01-20 | 吴斌 | Medicine for treating duodenal ulcer |
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