CN105267828A - Solid dispersion for treating peptic ulcer - Google Patents
Solid dispersion for treating peptic ulcer Download PDFInfo
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- CN105267828A CN105267828A CN201510809055.1A CN201510809055A CN105267828A CN 105267828 A CN105267828 A CN 105267828A CN 201510809055 A CN201510809055 A CN 201510809055A CN 105267828 A CN105267828 A CN 105267828A
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Abstract
The invention provides solid dispersion for treating peptic ulcer. The solid dispersion comprises raw material powder and polyethylene glycol-6000 according to a ratio of the raw material powder to the polyethylene glycol-6000 of 1-3:1-3w/w. The raw material powder comprises, by weight, 1-3 parts of daphne giraldii nitsche, 0.3-0.6 part of anisodus tanguticus, 6-10 parts of dried ginger and 6-10 parts of sea buckthorn, and the daphne giraldii nitsche, the anisodus tanguticus, the dried ginger and the sea buckthorn are ground to obtain the raw material powder with the size of 300-500 meshes. The solid dispersion has the advantages that the raw material powder is prepared to obtain the solid dispersion, accordingly, the bioavailability of medicines can be improved, and the anti-ulcer activity can be obviously improved.
Description
Technical field
The present invention relates to a kind of solid dispersion for the treatment of peptic ulcer.
Background technology
Taste-blindness rate refers to the circular or oval full-thickness defects of the limitation of Grastiodudenal mucosa, and muscularis mucosae is penetrated, and inevitably leaves fibrous scar after healing, and surface is covered by one deck epithelium, and muscularis mucosae can not regenerate.It is because many reasons causes gastric acid, pepsin to be destroyed the self-digestion of gastric mucosa or gastric mucosal barrier that its cause of disease sums up.Think that the formation of ulcer and gastric Helicobacter pylori infection also have important relationship in recent years.
Chronic erosive gastritis, also known as gastritis verrucosa or varioliform gastritis generally rarely seen glutted, indigestion symptom such as pantothenic acid, belch, irregularities stomachache after meal.There is multiple excipuliform in Stomach in Patients mucosa, expands folded shape or pimple sample protuberance, diameter 5 ~ 10mm, the visible mucomembranous defect in top or umbilicus sample depression, and there is erosion at center, and protuberance is many without blush around, but the normal erythema similar with size, with gastric antrum, portion is common.
The medicine of the above-mentioned disease of Current therapeutic mostly is chemical drugs, and it is expensive, and side effect is large, and it is long to cure required time.Therefore, urgent need one is economical and practical, toxic and side effects is low, and the medicine of the above-mentioned disease of energy rapid healing.
And Chinese medicine in treatment of chronic diseases one to all playing an important role.Someone treats peptic ulcer with Fructus Amomi Rotundus 10g, Rhizoma Atractylodis Macrocephalae 20g, Poria 20g, Herba Pogostemonis 15g, Herba Taraxaci 15g, Radix Ginseng 5g, Folium Perillae 10g, Semen Armeniacae Amarum 10g, Semen Coicis 20g, Herba Artemisiae Scopariae 15g, has certain therapeutic effect.In Chinese patent 201110413686.3, provide the pharmaceutical composition of the good treatment peptic ulcer of a kind of drug activity, be prepared from by Semen Coicis 20 parts, Semen Benincasae 20 parts, Herba Artemisiae Scopariae 15 parts, the Rhizoma Atractylodis Macrocephalae 15 parts, Folium Perillae 10 parts, Semen Armeniacae Amarum 10 parts, Semen Lablab Album 10 parts, Semen Myristicae 10 parts, the Radix Astragali 10 parts, Radix Ginseng 5 parts, Fructus Forsythiae 5 parts.But above-mentioned prescription flavour of a drug are more, and medical material large usage quantity, cost is higher.
Summary of the invention
The object of the present invention is to provide a kind of solid dispersion for the treatment of peptic ulcer.
A kind of solid dispersion for the treatment of peptic ulcer of the present invention, it is by raw material medicated powder: PEG-4000=1 ~ 3:1 ~ 3w/w is prepared from; Wherein, described raw material medicated powder the crude drug of following weight proportion is crushed to 300-500 order prepare:
Daphne giraldii Nitsche 1 ~ 3 part, Radix Anisodi Tangutici 0.3 ~ 0.6 part, Rhizoma Zingiberis 6 ~ 10 parts, Fructus Hippophae 6 ~ 10 parts.
Further, crude drug weight proportion is as follows:
Daphne giraldii Nitsche 2 ~ 3 parts, Radix Anisodi Tangutici 0.4 ~ 0.5 part, Rhizoma Zingiberis 8 ~ 10 parts, Fructus Hippophae 8 ~ 10 parts.
Preferably, crude drug weight proportion is as follows:
Daphne giraldii Nitsche 3 parts, Radix Anisodi Tangutici 0.5 part, Rhizoma Zingiberis 9 parts, Fructus Hippophae 10 parts.
Wherein, powder particle diameter to 300 order.
Further, raw material medicated powder: PEG-4000=1:1.
Present invention also offers the preparation method of above-mentioned solid dispersion, it comprises following operating procedure:
(1) weighting raw materials by weight ratio, and be crushed to corresponding particle diameter, obtain raw material medicated powder;
(2) get raw material medicated powder and PEG-4000, mixing, being heated to PEG-4000 is molten condition, stirs, and is placed in 0 DEG C of environment quenching immediately to solidification, pulverizes, obtain solid dispersion.
Daphne giraldii Nitsche is thymelaeceae daphne plant, the root bark of Daphne Giraldii Nitsche and peel of stem, calls as Daphne giraldii Nitsche, Daphne Giraldii Nitsche, rescues greatly, Flos Wikstroemiae Nutantis, yellow dog skin.This product is non-common Chinese crude drug, but applies comparatively extensive after making Chinese patent medicine, is among the peoplely widely used in the diseases such as treatment pain, traumatic injury, rheumatic arthritis and bronchitis.
Radix Anisodi Tangutici is the root of Solanaceae Scopolia plant Radix Anisodi Tangutici ScopoliatanguticaMaxim. [Anisodustanguticus (maxim.) Pasch.].Analgesia spasmolytic, blood circulation and promoting silt, hemostasia and promoting granulation.
In the present invention 4 taste medical material, Daphne giraldii Nitsche, Radix Anisodi Tangutici and Fructus Hippophae are all Qinghai distinguishing products, yet there are no people and are combinationally used by these 3 kinds of medical materials, oral medication erosive gastritis.The present invention, by after above-mentioned 4 taste medical material reasonable compatibilities, after particularly adding Fructus Hippophae, has played synergistic function, effectively can treat gastric ulcer, good analgesic effect, and had good gastric mucosal effect, for clinical application provides a kind of selection newly.
Aforementioned pharmaceutical compositions has also been prepared into the medicated powder of specified particle diameter by the present invention, and under this particle diameter condition, medicated powder specific surface area is comparatively large, can be attached to skin surface better and directly treat, and effectively plays the inhibit activities to ulcer.
Raw material medicated powder is prepared into solid dispersion by the present invention, and improve the bioavailability of medicine, antiulcer activity significantly improves.
Detailed description of the invention
The preparation of embodiment 1 pharmaceutical composition of the present invention
Daphne giraldii Nitsche 3g, Radix Anisodi Tangutici 0.5g, Rhizoma Zingiberis 9g, Fructus Hippophae 10g; After drying, be crushed to 300 orders, after mix homogeneously, obtain raw material medicated powder.
Get raw material medicated powder: PEG-4000=1:1w/w, mixing, being heated to PEG-4000 is molten condition, stirs, and is placed in 0 DEG C of environment quenching immediately to solidification, pulverizes, obtain solid dispersion.
The preparation of embodiment 2 pharmaceutical composition of the present invention
Daphne giraldii Nitsche 1g, Radix Anisodi Tangutici 0.6g, Rhizoma Zingiberis 6g, Fructus Hippophae 10g; After drying, be crushed to 400 orders, after mix homogeneously, obtain raw material medicated powder.
Get raw material medicated powder: PEG-4000=1:3w/w, mixing, being heated to PEG-4000 is molten condition, stirs, and is placed in 0 DEG C of environment quenching immediately to solidification, pulverizes, obtain solid dispersion.
The preparation of embodiment 3 pharmaceutical composition of the present invention
Daphne giraldii Nitsche 1g, Radix Anisodi Tangutici 0.3g, Rhizoma Zingiberis 10g, Fructus Hippophae 6g; After drying, pulverize 500 orders, after mix homogeneously, obtain raw material medicated powder.
Get raw material medicated powder: PEG-4000=3:1w/w, mixing, being heated to PEG-4000 is molten condition, stirs, and is placed in 0 DEG C of environment quenching immediately to solidification, pulverizes, obtain solid dispersion.
Beneficial effect of the present invention is shown further below by way of concrete test example.
Test example 1 pharmaceutical composition of the present invention is to the treatment of gastric ulcer
Gastric Ulcer standard: upper abdomen dull pain, dull pain or burn sample pain, alleviate after taking alkalescent medicine, such pain has rhythmicity, many appearance in 1 hour after the meal, alleviated gradually after 1 ~ 2 hour, generally also there will be acid regurgitation, belch, heartburn, the indigestion symptom such as Abdeminal pain, Nausea and vomiting; The visible niche of upper digestive tract radiography; Endoscopy, can in stomach see circle or oval, bottom is smooth, the ulcer of neat in edge, ulcer surface is greyish white or brown tongue film covers, edge swelling, color and luster ruddy, smooth and soft (i.e. gastric ulcer activity time).Accept 30 examples altogether for medical treatment, endoscopy confirms as gastric ulcer.
Criterion of cure: epigastrium pain disappears, endoscopy, and visible ulcer surface white fur disappears, become red congested cicatrix, visible pleat concentrates (i.e. cicatricial phase).
Effective standard: epigastrium pain disappears or alleviates, endoscopy, and tongue film is thinning, and ulcer reduces, the blush of visible mucous epithelium regeneration around it; Or ulcer surface almost disappears, it there is few thin coating (i.e. healing stage).
Therapeutic Method: the decoction that Example 1 prepares, every bu is taken for 3 times, period in a medicine, avoids eating anything raw or cold, maror.
Criterion of cure: take medicine continuously by Therapeutic Method, treats 30 ~ 50 days, cures 25 examples, accounts for 83% of total case; Effective 5 examples, account for 17% of total case.Total effective rate reaches 100%.
The screening of test example 2 pharmaceutical composition of the present invention
Get SD rat, male and female half and half fasting is after 12 hours, rats by intraperitoneal injection 3% is anaesthetized without barbital sodium, to sterilize skin with alcohol cotton stick, cut abdominal cavity open, in glandular stomach portion, antetheca hole body intersection serosal surface sticks the circular filter paper 30s soaking into glacial acetic acid, diameter 5mm, repeat 3 times, close abdomen sewing-up cut, be coated with penicillin.Postoperative routine feeding, the 4th day by animal random packet, model group gavage 10mlkg
-1distilled water, positive drug ranitidine group gavage 30mgkg
-1, each screening group 4g crude drug/kg body weight (extracting method is with test example 1) of the present invention.The 2nd day after grouping starts gastric infusion, and administration every day 1 time, dosage is 10mlkg
-1, continuous 5 days, last administration is de-cervical vertebra execution animal after 12 hours, cut open the belly and get stomach, use brine gastric content, stomach is fixed in 10% formaldehyde, stomach is lain on glass surface ware after 15 minutes, measure major diameter and the minor axis of ulcer surface under magnifier with slide gauge, and calculate ulcer surface.
Calculate ulcer inhibition rate: ulcer inhibition rate=(matched group ulcer area-administration group ulcer area)/matched group ulcer area x100%, observe ulcer healing degree.
Experimental result is in table 1.
Table 1
Note: compared with model group, * is p<0.05, * * is p<0.01; Compared with group 1, △ is p<0.05
Wherein, the compatibility of each screening group is as follows:
Group 1: Daphne giraldii Nitsche 3 parts, Radix Anisodi Tangutici 0.5 part, Rhizoma Zingiberis 9 parts, Fructus Hippophae 10 parts;
Group 2: Daphne giraldii Nitsche 3 parts, Radix Anisodi Tangutici 0.5 part, Rhizoma Zingiberis 9 parts.
Above-mentioned each group of compound recipe, flavour of a drug are identical, but medical material consumption proportion difference has appreciable impact to the drug activity of compound recipe: group 1,2, all has certain inhibitory action (p<0.05) to the gastric ulcer of animal pattern; But the prescription proportioning of employing group 1, can significantly improve the therapeutic activity of compound medicine, and its activity is significantly better than group 2 (p<0.05) under identical crude drug dosage, and therefore, the present invention preferably organizes the prescription proportioning of 1.Above-mentioned test shows, pharmaceutical composition of the present invention, under specific flavour of a drug compatibility, has played synergistic function.
The drug activity preliminary study of test example 3 solid dispersion of the present invention
Get SD rat, fasting is after 12 hours, and rats by intraperitoneal injection 3% is anaesthetized without barbital sodium, to sterilize skin with alcohol cotton stick, cut abdominal cavity open, in glandular stomach portion, antetheca hole body intersection serosal surface sticks the circular filter paper 30s soaking into glacial acetic acid, diameter 5mm, repeat 3 times, close abdomen sewing-up cut, be coated with penicillin.Postoperative routine feeding, is divided into 4 groups at random by animal on the 4th day, and often organize 10, male and female half and half, are respectively model group (10mlkg
-1distilled water), water extraction group of the present invention (test example 2 group 1), solid dispersion group of the present invention (4 crude drugs/kg body weight, prepared by embodiment 1), positive drug ranitidine group (30mgkg
-1).The 2nd day after grouping starts gastric infusion, and administration every day 1 time, dosage is 10mlkg
-1, continuous 5 days, last administration is de-cervical vertebra execution animal after 12 hours, cut open the belly and get stomach, use brine gastric content, stomach is fixed in 10% formaldehyde, stomach is lain on glass surface ware after 15 minutes, measure major diameter and the minor axis of ulcer surface under magnifier with slide gauge, and calculate ulcer surface.
Calculate ulcer inhibition rate: ulcer inhibition rate=(matched group ulcer area-administration group ulcer area)/matched group ulcer area x100%, observe ulcer healing degree.
Experimental result is in table 2.
Table 2
Note: compared with model group, * is p<0.05, * * is p<0.01; Compared with solid dispersion group, △ is p<0.05.
Brief summary:
As shown in Table 2, the present invention improves bioavailability after raw material medicated powder is prepared into solid dispersion, and antiulcer activity is more good, is obviously better than the water extract under Isodose.
In sum, pharmaceutical composition of the present invention is after reasonable compatibility, and pharmaceutical composition of the present invention has played synergistic function, effectively can treat gastric ulcer, selects for clinical treatment peptic ulcer provides a kind of new medication.
Claims (6)
1. treat a solid dispersion for peptic ulcer, it is characterized in that: it is by raw material medicated powder: PEG-4000=1 ~ 3:1 ~ 3w/w is prepared from; Wherein, described raw material medicated powder the crude drug of following weight proportion is crushed to 300-500 order prepare:
Daphne giraldii Nitsche 1 ~ 3 part, Radix Anisodi Tangutici 0.3 ~ 0.6 part, Rhizoma Zingiberis 6 ~ 10 parts, Fructus Hippophae 6 ~ 10 parts.
2. crude drug according to claim 1, is characterized in that: crude drug weight proportion is as follows:
Daphne giraldii Nitsche 2 ~ 3 parts, Radix Anisodi Tangutici 0.4 ~ 0.5 part, Rhizoma Zingiberis 8 ~ 10 parts, Fructus Hippophae 8 ~ 10 parts.
3. crude drug according to claim 2, is characterized in that: crude drug weight proportion is as follows:
Daphne giraldii Nitsche 3 parts, Radix Anisodi Tangutici 0.5 part, Rhizoma Zingiberis 9 parts, Fructus Hippophae 10 parts.
4. the raw material medicated powder according to claim 1-3, is characterized in that: powder particle diameter to 300 order.
5. solid dispersion according to claim 1, is characterized in that: raw material medicated powder: PEG-4000=1:1.
6. the preparation method of solid dispersion described in Claims 1 to 5 any one, is characterized in that: it comprises following operating procedure:
(1) weighting raw materials by weight ratio, and be crushed to corresponding particle diameter, obtain raw material medicated powder;
(2) get raw material medicated powder and PEG-4000, mixing, being heated to PEG-4000 is molten condition, stirs, and is placed in 0 DEG C of environment quenching immediately to solidification, pulverizes, obtain solid dispersion.
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| CN201510809055.1A CN105267828A (en) | 2015-11-20 | 2015-11-20 | Solid dispersion for treating peptic ulcer |
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| CN201510809055.1A CN105267828A (en) | 2015-11-20 | 2015-11-20 | Solid dispersion for treating peptic ulcer |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102068682A (en) * | 2010-12-27 | 2011-05-25 | 湖南九典制药有限公司 | Chinese medicinal composition for treating digestive system diseases and preparation method thereof |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102068682A (en) * | 2010-12-27 | 2011-05-25 | 湖南九典制药有限公司 | Chinese medicinal composition for treating digestive system diseases and preparation method thereof |
Non-Patent Citations (5)
| Title |
|---|
| 周秋丽等: "《现代中药基础研究与临床》", 30 June 2012 * |
| 彭成等: "《中药药理学》", 31 December 2014 * |
| 李小芳等: "《药剂学》", 31 August 2014 * |
| 第一五七医院等: "《新编中医学》", 31 October 1980 * |
| 郭凡剑等: "《食疗保健200典》", 30 June 2011 * |
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