CN1213749C - Prepn. of obakulactone contd. medicine for treating hemorrhoid, and its use - Google Patents
Prepn. of obakulactone contd. medicine for treating hemorrhoid, and its use Download PDFInfo
- Publication number
- CN1213749C CN1213749C CN 02145371 CN02145371A CN1213749C CN 1213749 C CN1213749 C CN 1213749C CN 02145371 CN02145371 CN 02145371 CN 02145371 A CN02145371 A CN 02145371A CN 1213749 C CN1213749 C CN 1213749C
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- Prior art keywords
- limonin
- parts
- medicine
- starch
- hemorrhoid
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 239000003814 drug Substances 0.000 title claims abstract description 15
- 208000014617 hemorrhoid Diseases 0.000 title claims description 34
- VHLJDTBGULNCGF-UHFFFAOYSA-N Limonin Natural products CC1(C)OC2CC(=O)OCC23C4CCC5(C)C(CC(=O)C6OC56C4(C)C(=O)CC13)c7cocc7 VHLJDTBGULNCGF-UHFFFAOYSA-N 0.000 claims abstract description 74
- KBDSLGBFQAGHBE-MSGMIQHVSA-N limonin Chemical compound C=1([C@H]2[C@]3(C)CC[C@H]4[C@@]([C@@]53O[C@@H]5C(=O)O2)(C)C(=O)C[C@@H]2[C@]34COC(=O)C[C@@H]3OC2(C)C)C=COC=1 KBDSLGBFQAGHBE-MSGMIQHVSA-N 0.000 claims abstract description 74
- 238000002360 preparation method Methods 0.000 claims abstract description 16
- 239000002775 capsule Substances 0.000 claims abstract description 9
- 239000007924 injection Substances 0.000 claims abstract description 7
- 238000002347 injection Methods 0.000 claims abstract description 7
- 239000007788 liquid Substances 0.000 claims abstract description 7
- 235000020357 syrup Nutrition 0.000 claims abstract description 6
- 239000006188 syrup Substances 0.000 claims abstract description 6
- 239000003826 tablet Substances 0.000 claims abstract description 3
- 229920002472 Starch Polymers 0.000 claims description 28
- 235000019698 starch Nutrition 0.000 claims description 28
- 239000008107 starch Substances 0.000 claims description 28
- 239000000203 mixture Substances 0.000 claims description 17
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 14
- 239000012153 distilled water Substances 0.000 claims description 14
- 239000008101 lactose Substances 0.000 claims description 14
- 239000002002 slurry Substances 0.000 claims description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 14
- 239000002994 raw material Substances 0.000 claims description 11
- 150000002629 limonins Chemical class 0.000 claims description 10
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 10
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 8
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 7
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 7
- 229930006000 Sucrose Natural products 0.000 claims description 7
- 235000020374 simple syrup Nutrition 0.000 claims description 7
- 239000005720 sucrose Substances 0.000 claims description 7
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 15
- 239000008280 blood Substances 0.000 abstract description 7
- 210000004369 blood Anatomy 0.000 abstract description 6
- 230000002708 enhancing effect Effects 0.000 abstract description 2
- 238000002474 experimental method Methods 0.000 abstract description 2
- 206010067484 Adverse reaction Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000006838 adverse reaction Effects 0.000 abstract 1
- 230000001900 immune effect Effects 0.000 abstract 1
- 231100000956 nontoxicity Toxicity 0.000 abstract 1
- 238000005303 weighing Methods 0.000 description 10
- 239000008187 granular material Substances 0.000 description 8
- 238000000034 method Methods 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 206010013786 Dry skin Diseases 0.000 description 4
- 208000032843 Hemorrhage Diseases 0.000 description 4
- 230000008034 disappearance Effects 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000007779 soft material Substances 0.000 description 4
- 206010030113 Oedema Diseases 0.000 description 3
- 208000002193 Pain Diseases 0.000 description 3
- 230000000740 bleeding effect Effects 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 201000007772 internal hemorrhoid Diseases 0.000 description 3
- 210000004877 mucosa Anatomy 0.000 description 3
- 230000036407 pain Effects 0.000 description 3
- 108090000386 Fibroblast Growth Factor 1 Proteins 0.000 description 2
- 102100031706 Fibroblast growth factor 1 Human genes 0.000 description 2
- 206010020565 Hyperaemia Diseases 0.000 description 2
- 208000003251 Pruritus Diseases 0.000 description 2
- 230000008033 biological extinction Effects 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 238000011084 recovery Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 208000008035 Back Pain Diseases 0.000 description 1
- 241000207199 Citrus Species 0.000 description 1
- 206010053567 Coagulopathies Diseases 0.000 description 1
- 235000005956 Cosmos caudatus Nutrition 0.000 description 1
- 244000293323 Cosmos caudatus Species 0.000 description 1
- 108090000379 Fibroblast growth factor 2 Proteins 0.000 description 1
- 102000003974 Fibroblast growth factor 2 Human genes 0.000 description 1
- 102100037362 Fibronectin Human genes 0.000 description 1
- 108010067306 Fibronectins Proteins 0.000 description 1
- 235000003143 Panax notoginseng Nutrition 0.000 description 1
- 241000180649 Panax notoginseng Species 0.000 description 1
- 208000012287 Prolapse Diseases 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 210000002255 anal canal Anatomy 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 210000000436 anus Anatomy 0.000 description 1
- 235000020971 citrus fruits Nutrition 0.000 description 1
- 230000035602 clotting Effects 0.000 description 1
- 230000013872 defecation Effects 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000035876 healing Effects 0.000 description 1
- 208000035861 hematochezia Diseases 0.000 description 1
- 230000023597 hemostasis Effects 0.000 description 1
- 230000002439 hemostatic effect Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229910052957 realgar Inorganic materials 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000017423 tissue regeneration Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to purposes of a medicine treating piles and prepared from limonin, which belongs to the technical field of a medicine and particularly relates to new purposes of the limonin in pharmacy aspect. The experiment verifies that the limonin has obvious curative effects on piles. The medicine for treating piles, which is prepared from the limonin according to a conventional preparation method, can be suitable for all medicinal forms used in clinic, such as tablets, capsules, syrup, oral medicinal liquid, injections, etc. The present invention uses the limonin to treat piles, which has the advantages of no toxicity, less side effect, conspicuous curative effect, no contraindication or adverse reaction, etc. In one week, the effective rate of the medicine is 85%; the medicine is capable of being taken for a long time, is capable of enhancing the immunological competence of an organism and has the functions of resisting cancers and lowering blood fat.
Description
Technical field
The invention belongs to medical technical field, the new purposes of particularly a kind of limonin aspect pharmacy.
Background technology
Hemorrhoid mainly are divided into three kinds of internal hemorrhoid, external hemorrhoid and inside and outside mixed hemorrhoids, belong to a kind of common anal canal disease.Symptoms such as the patient who suffers from hemorrhoids disease often has difficulty in defecation, has blood in stool, anus pruritus, very painful.At present, the medicine and the method for treatment hemorrhoid have a lot, and some has also applied for patent." a kind of powder for the treatment of hemorrhoid and preparation method thereof " that provides as Chinese patent 991056035, it is to adopt Chinese medicine composition, comprises compositions such as Margarita powder, Radix Notoginseng, Realgar in its raw material, and deposited buried mode is applied to the affected part, make that QI-blood circulation is unobstructed, the blood stasis deliquescing, reach therapeutic purposes at last.But fact proved that the effect that a lot of medicines can only ease the pain is repeatedly used and also can't be cured.Though some medicine has certain curative effect, side effect is very big.Operative treatment is a kind of effectively treatment means though adopt to be in hospital, and this mode has increased many miseries to the patient, and the expense height of treatment, long, easily recurrence of time.
Limonin (Limonin) is found in 1989 the earliest and is open in Japanese Patent No. 372432 documents.Limonin has antitumor and antitumaous effect, also has effects such as analgesia and antiinflammatory simultaneously.To this, in Chinese patent 001306227 disclosed " a kind of technology of from the Citrus seed, extracting pharmaceutically active substance " and the Chinese patent 001062859 disclosed " from rue fruit, extracting the method for limonin " explanation is arranged all.But, up to the present, yet there are no the report of using limonin treatment hemorrhoid.
Summary of the invention
The purpose of this invention is to provide the new purposes of limonin aspect the treatment hemorrhoid.
Limonin has the purposes in preparation antihaemorrhoidals thing.Prove that by experiment limonin is having significant curative effect aspect the treatment hemorrhoid.
Limonin is when the treatment hemorrhoid, and its pharmacological action is mainly reflected in:
1, hemostatic function.Limonin can stimulate local vascular to shrink, and significantly reduces amount of bleeding.Simultaneously, also increase hematoblastic quantity, shortened clotting time, reached the hemostasis purpose.Show that through clinical trial adopt limonin treatment hemorrhoid, one week of medication promptly takes effect.
2, promote tissue repair: limonin can make the content of wound surface medium vessels endothelial cell growth factor (ECGF), basic fibroblast growth factor, fibronectin obviously increase, and promotes the healing of wound tissue.
With the medicine of limonin preparation treatment hemorrhoid,, can be any pharmaceutical dosage form that is suitable for clinical use, as tablet, capsule, syrup, oral liquid, injection etc. according to the formulation method of routine.
With the tablet of limonin preparation treatment hemorrhoid, its raw material is made up of limonin, lactose, starch, low-substituted hydroxypropyl cellulose, starch slurry, and the weight proportion of each composition is:
5～50 parts of limonins
20～45 parts of lactose
50～65 parts of starch
3～6 parts of low-substituted hydroxypropyl celluloses
(5%) 5～20 part of starch slurry
Take by weighing limonin, lactose, starch and low-substituted hydroxypropyl cellulose by above-mentioned weight proportion, fully mixing adds starch slurry (5%) and makes suitable soft material in right amount, cross 60 mesh sieves and granulate 60～70 ℃ of dryings, 40 mesh sieve granulate, mix homogeneously, tabletting promptly gets the tablet finished product.
With the capsule of limonin preparation treatment hemorrhoid, its raw material is that limonin, lactose, starch, low-substituted hydroxypropyl cellulose, starch slurry are formed, and the weight proportion of each composition is:
30～100 parts of limonins
20～45 parts of lactose
50～65 parts of starch
3～6 parts of low-substituted hydroxypropyl celluloses
(5%) 5～20 part of starch slurry
Take by weighing limonin, lactose, starch and low-substituted hydroxypropyl cellulose by above-mentioned weight proportion, fully mixing adds starch slurry (5%) and makes suitable soft material in right amount, cross 60 mesh sieves and granulate 60～70 ℃ of dryings, 40 mesh sieve granulate, mix homogeneously, the cover capsule gets product.
With the syrup of limonin preparation treatment hemorrhoid, its raw material is made up of limonin, distilled water and simple syrup, and the weight proportion of each composition is:
5～50 parts of limonins
180～200 parts of distilled water
750～850 parts of simple syrups
Take by weighing limonin by above-mentioned weight proportion, be dissolved in distilled water, add simple syrup and get product.
With the oral liquid of limonin preparation treatment hemorrhoid, its raw material is made up of limonin, sucrose, distilled water, and the weight proportion of each composition is:
5～50 parts of limonins
10～20 parts of sucrose
950～1000 parts of distilled water
Take by weighing limonin by above-mentioned weight proportion, be dissolved in distilled water, promptly get the oral liquid finished product with sucrose.
With the injection of limonin preparation treatment hemorrhoid, its raw material is made up of limonin and normal saline, and the weight proportion of each composition is:
30～100 parts of limonins
900～1000 parts of normal saline
Take by weighing limonin by above-mentioned weight proportion, be dissolved in normal saline and dilution, promptly get the injection finished product.
In order to explore the effectiveness and the safety of limonin treatment hemorrhoid, this is carried out clinical trial by the attached First Academy of Medical College of Zhejiang Univ..Test situation is as follows:
1, research method: adopt open, own control research.Use low dose of limonin treatment hemorrhoid 30 examples.Pharmaceutical formulation is a capsule, every 15mg.Medicine using method: one of every day, serve on ten days.
2, curative effect determinate standard:
(1), internal hemorrhoid, mixed hemorrhoid
Recovery from illness: do not have hemorrhagely after an action of the bowels, do not have prolapsus, it is normal that anoscopy hemorrhoid mucosa recovers, the blood stasis atresia.
Produce effects: do not have hemorrhagely after an action of the bowels, nothing is deviate from.The blood stasis redness obviously disappears, anoscopy, and internal hemorrhoid mucosa mild hyperaemia, blood stasis diminishes.
Effectively: still have after an action of the bowels hemorrhage on a small quantity, companion slightly the prolapsus, anoscopy hemorrhoid mucosa mild hyperaemia.
Invalid: symptom and body sheet do not have improvement before the treatment, even increase the weight of.
(2), external hemorrhoid
Clinical recovery: sings and symptoms all disappears.
Produce effects: transference cure, sign is improved.
Effectively: sings and symptoms improves.
Invalid: sings and symptoms does not all have improvement.
3, MethodsThe cases enrolled:
Selected 30 examples.Man's 17 examples, women 13 examples, the age 15, average 38 years old, sick time 1 to 30 year wherein had bleeder's 27 examples, and pain person's 13 examples are arranged, and the person's of deviating from 22 examples are arranged, and edema person's 4 examples are arranged, and pruritus person's 2 examples are arranged to 74 years old.
4, therapeutic outcome:
(1), treatment back stopped bleeding rate:
Limonin treatment after 3,7,10 days the stopped bleeding rate be respectively 50%, 85%, 100%.
(2) treatment back pain disappearance rate:
Limonin treatment after 3,7,10 days the pain disappearance rate be respectively 35%, 70%, 90%.
(3) treatment back edema extinction rate:
Limonin treatment after 3,7,10 days the edema extinction rate be respectively 20%, 50%, 75%.
(4) treatment back prolapsus disappearance rate:
Limonin is treated the disappearance rate that prolapses after 3,7,10 days and is respectively 34%, 60%, 80%.
(5) untoward reaction:
Do not find tangible untoward reaction during the limonin treatment.
5, conclusion:
The acute attack of limonin treatment hemorrhoid is evident in efficacy and do not have any untoward reaction, is worth further research.
Compare with the medicine of existing treatment hemorrhoid, the present invention adopts limonin treatment hemorrhoid to have following advantage:
1, because limonin is formed by the all-natural product extraction, there are not any toxicity, few side effects, no contraindication and untoward reaction.
2, limonin has features good taste, stay-in-grade characteristics, is convenient to take and store.
3, adopt the evident in efficacy of limonin treatment hemorrhoid, all effective percentage can reach 85%.
4, safe and reliable, can take for a long time, immunocompetence that can also enhancing body, and have effect anticancer, that remove blood fat.
The specific embodiment
Embodiment 1
Make tablet with limonin, its prescription following (1000 amounts):
Limonin 25g
Lactose 25g
Starch 50g
Low-substituted hydroxypropyl cellulose 5g
Starch slurry (5%) 15g
Take by weighing limonin, lactose, starch and low-substituted hydroxypropyl cellulose by prescription, fully mixing adds starch slurry (5%) and makes suitable soft material in right amount, and cross 60 mesh sieves and granulate, 60～70 ℃ of dryings, 40 mesh sieve granulate, mix homogeneously, tabletting gets product.
Embodiment 2
Make capsule with limonin, its prescription following (1000 amounts):
Limonin 70g
Lactose 25g
Starch 55g
Low-substituted hydroxypropyl cellulose 5g
Starch slurry (5%) 15g
Take by weighing limonin, lactose, starch and low-substituted hydroxypropyl cellulose by prescription, fully mixing adds starch slurry (5%) and makes suitable soft material in right amount, and cross 60 mesh sieves and granulate, 60～70 ℃ of dryings, 40 mesh sieve granulate, mix homogeneously, the cover capsule gets product.
Embodiment 3
Make syrup with limonin, its prescription following (1000ml amount):
Limonin 20g
Distilled water 180ml
Simple syrup adds to 1000ml
Take by weighing limonin by prescription, be dissolved in distilled water, add simple syrup to 1000ml promptly.
Embodiment 4
Make oral liquid with limonin, its prescription following (1000ml amount):
Limonin 30g
Sucrose 10g
Distilled water adds to 1000ml
Take by weighing limonin by recipe quantity, be dissolved in distilled water, with sucrose to 1000ml promptly.
Embodiment 5
Make injection with limonin, its prescription following (1000ml amount):
Limonin 50g
Normal saline 1000ml
Take by weighing limonin by prescription, be dissolved in normal saline, be diluted to 1000ml promptly.
Claims (7)
1, limonin has the purposes in preparation antihaemorrhoidals thing.
2, purposes according to claim 1 is characterized in that medicine with limonin preparation treatment hemorrhoid is to be suitable for a kind of in the following pharmaceutical dosage form of clinical use: tablet, capsule, syrup, oral liquid, injection.
3, purposes according to claim 2 is characterized in that its raw material is made up of limonin, lactose, starch, low-substituted hydroxypropyl cellulose, starch slurry with the tablet of limonin preparation treatment hemorrhoid, and the weight proportion of each composition is:
5～50 parts of limonins
20～45 parts of lactose
50～65 parts of starch
3～6 parts of low-substituted hydroxypropyl celluloses
5～20 parts of 5% starch slurries
4, purposes according to claim 2 is characterized in that the capsule with limonin preparation treatment hemorrhoid, and its raw material is that limonin, lactose, starch, low-substituted hydroxypropyl cellulose, starch slurry are formed, and the weight proportion of each composition is:
30～100 parts of limonins
20～45 parts of lactose
50～65 parts of starch
3～6 parts of low-substituted hydroxypropyl celluloses
5～20 parts of 5% starch slurries
5, purposes according to claim 2 is characterized in that its raw material is made up of limonin, distilled water and simple syrup with the syrup of limonin preparation treatment hemorrhoid, and the weight proportion of each composition is:
5～50 parts of limonins
180～200 parts of distilled water
750～850 parts of simple syrups
6, purposes according to claim 2 is characterized in that its raw material is made up of limonin, sucrose, distilled water with the oral liquid of limonin preparation treatment hemorrhoid, and the weight proportion of each composition is:
5～50 parts of limonins
10～20 parts of sucrose
950～1000 parts of distilled water.
7, purposes according to claim 2 is characterized in that its raw material is made up of limonin and normal saline with the injection of limonin preparation treatment hemorrhoid, and the weight proportion of each composition is:
30～100 parts of limonins
900～1000 parts of normal saline.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02145371 CN1213749C (en) | 2002-11-21 | 2002-11-21 | Prepn. of obakulactone contd. medicine for treating hemorrhoid, and its use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02145371 CN1213749C (en) | 2002-11-21 | 2002-11-21 | Prepn. of obakulactone contd. medicine for treating hemorrhoid, and its use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1418623A CN1418623A (en) | 2003-05-21 |
| CN1213749C true CN1213749C (en) | 2005-08-10 |
Family
ID=4750876
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02145371 Expired - Lifetime CN1213749C (en) | 2002-11-21 | 2002-11-21 | Prepn. of obakulactone contd. medicine for treating hemorrhoid, and its use |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1213749C (en) |
-
2002
- 2002-11-21 CN CN 02145371 patent/CN1213749C/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CN1418623A (en) | 2003-05-21 |
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Address after: 310000 No. 829, changfuhang Road, Qianjin Street, Qiantang District, Hangzhou City, Zhejiang Province Patentee after: Zhejiang sukean Pharmaceutical Co.,Ltd. Address before: No.829, changfuhang Road, dajiangdong Industrial Cluster District, Hangzhou, Zhejiang 311200 Patentee before: HANGZHOU SUPOR SOUTH OCEAN PHARMACEUTICAL CO.,LTD. |
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