CN107669742A - Treat pharmaceutical composition, pharmaceutical preparation and the application of hemorrhoid - Google Patents
Treat pharmaceutical composition, pharmaceutical preparation and the application of hemorrhoid Download PDFInfo
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- CN107669742A CN107669742A CN201710995293.5A CN201710995293A CN107669742A CN 107669742 A CN107669742 A CN 107669742A CN 201710995293 A CN201710995293 A CN 201710995293A CN 107669742 A CN107669742 A CN 107669742A
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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- A61K31/19—Carboxylic acids, e.g. valproic acid
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- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
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- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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Abstract
The present invention relates to a kind of pharmaceutical composition for treating hemorrhoid, pharmaceutical preparation and application.The pharmaceutical composition and pharmaceutical preparation contain the monomer component of caulis lonicerae, kuh-seng, golden cypress, Chinese gall etc..Calculate by weight, 0.40 0.66 parts of loganin, 0.47 0.66 parts of matrine, 1.15 1.48 parts of jamaicin, 0.12 0.16 parts of phellodendrine, 53.46 65.34 parts of gallic acid, Osthole 1.86 2.66,4.79 5.85 parts of digua fig stem and leaf general flavone.Above-mentioned each Chinese medicinal material monomer component is chosen, auxiliary material is added, pharmaceutical preparation is made according to conventional formulation technique.The pharmaceutical composition of the present invention and its manufactured pharmaceutical preparation have the effect of removing toxic substances eliminating dampness, arresting bleeding and treating cutaneous pyogenic infection, good therapeutic effect is obtained applied to the malaise symptoms such as the internal piles caused by damp-heat accumulation, external piles, mixed hemorrhoid and the bleeding showed, swelling and pain, itch, toxicity is relatively low simultaneously, is more satisfactory medicine.
Description
Technical field
The present invention relates to the technical field of medicine for the treatment of hemorrhoid, more particularly to one kind removing toxic substances eliminating dampness, astringing to arrest bleeding
For the pharmaceutical composition of hemorrhoid, pharmaceutical preparation and application.
Background technology
Hemorrhoid are hemorrhoid, anal fistula, anal fissure, prolapse of the anus, constipation, the anorectal disease such as have blood in stool is commonly called as, and are that the mankind are distinctive common
Disease, frequently-occurring disease.Show according to relevant reconnaissance information, the incidence of disease of the anorectal disease such as hemorrhoid is 59.1%, and wherein hemorrhoid account for institute
Have the 87.2% of anorectal disease, hemorrhoid are again most commonly seen with internal piles, account for the 52.19% of all anorectal diseases.Men and women can fall ill,
The incidence of disease of women is 67%, and the incidence of disease of male is 53.9%, and the women incidence of disease is higher than male, because female patient is general not
Hope receives hemorrhoid treating, therefore the data of part clinical treatment hemorrhoid are shown, male's hemorrhoid incidence of disease is higher than women.Any age is all
It can fall ill, and the people of 20~40 years old is more common, and can gradually be aggravated with the increase at age, therefore it is said that nine out ten suffer from hemorrhoids.
In the prior art, haemorrhoids commercialized product has haemorrhoids washing lotion, haemorrhoids bolt etc., is born with clearing heat and detoxicating, dispelling wind dredging collateral
Winter rattan is monarch drug in a prescription, is aided with Miao ethnic group of Guizhou Province common drug digua fig stem and leaf among the people, the kuh-seng, detoxification sore treatment in addition combined with heat-clearing and damp-drying drug
The frutus cnidii of golden cypress, the convergent Chinese gall of hemostasis and wind dispelling insecticide, according to ethnic group's medication custom and reasonable group of theory of traditional Chinese medical science
Fang Zucheng pure Chinese medicinal preparation, there is the effect of clearing heat and detoxicating, eliminating dampness and astringing sores, cure mainly internal piles volume of savings, external hemorrhoid welling and pain etc..It is existing
There is document report, played a leading role respectively with a certain composition or some compositions in above-mentioned six kinds of medicinal materials, these compositions are coordinated jointly
Synergy, medicine is set to have certain effect to treatment hemorrhoid.
In the prior art, the preparation method of haemorrhoids bolt is：Chinese gall crushes on a small quantity, remaining Chinese gall and remaining caulis lonicerae etc.
Add water temperature leaching, decoct, concentration, separately take suppository base to be mixed with the thick paste after concentration, medicinal powder, moulding is made.The system of haemorrhoids washing lotion
Preparation Method is：The taste medicinal material of caulis lonicerae etc. 6 adds water temperature leaching, decocted, concentration, takes supernatant to add water to configure after standing, produces.Above-mentioned system
During standby, it is mainly the method using water boiling and extraction to medicinal materials such as caulis loniceraes, obtains the extract of medicinal material, and it is further right
Extract carries out preparation preparation.But no matter using which kind of medicinal material extract method, what is obtained is the total extract of medicinal material, is not only contained
Effective composition, such as polysaccharide, flavonoids, there are other invalid components, this will cause, and the dosage of medicine is big, absorbs and has
Interference, and the mechanism of action of various composition is also indefinite, and this is exactly the limitation place that such medicine is commercially applied.And
And various active components is also unclear with magnitude relation.Therefore, the research to the active ingredient monomer of above-mentioned medicinal material is made further
Go deep into, be the another exploitation to haemorrhoids product, and our researchers are duty-bound in modernization of cmm.
The content of the invention
The technical problems to be solved by the invention are to overcome in existing haemorrhoids product that Chinese medicine dosage is big, active ingredient
A kind of and its indefinite defect of the mechanism of action, there is provided the drug regimen of rapid, safe, the quality controllable treatment hemorrhoid of curative effect
Thing, pharmaceutical preparation and its application.
In order to solve the above technical problems, the present invention was both avoided using the extract monomer of the Six-element Chinese medicinal materials such as caulis lonicerae
It is big using raw medicinal material dosage, specify that each therapeutic component again, have good removing toxic substances eliminating dampness, arresting bleeding and treating cutaneous pyogenic infection, anti-inflammation,
The effect of swelling and pain relieving, achieved in treatment internal piles, external piles, mixed hemorrhoid and its bleeding showed, swelling and pain, itch etc. good
Good therapeutic effect.
Specifically, the invention provides following technical scheme：
A kind of pharmaceutical composition for treating hemorrhoid, is calculated by weight, by loganin 0.40-0.66 parts (0.15-
0.25%) part, matrine 0.47-0.66 parts (0.25-0.35%), jamaicin 1.15-1.48 parts (3.5-4.5%), phellodendrine
0.12-0.16 parts (0.36-0.44%), gallic acid 53.46-65.34 parts (54-66%), Osthole 1.86-2.66
(1.4-2.0%), digua fig stem and leaf general flavone 4.79-5.85 parts (3.6-4.4%) are made.
Further, calculate by weight, by loganin 0.48-0.58 parts (0.18-0.22%) part, matrine 0.53-
0.60 part (0.28-0.32%), jamaicin 1.25-1.39 parts (3.8-4.2%), phellodendrine 0.13-0.14 parts (0.38-
0.42%), gallic acid 57.42-61.38 parts (58-62%), Osthole 2.13-2.39 (1.6-1.8%), digua fig stem and leaf are total
Flavones 5.05-5.59 parts (3.8-4.2%) are made.
Preferably, calculate by weight, by 0.53 part of (0.2%) part of loganin, matrine 0.56 part of (0.30%), barberry
Alkali 1.32 parts (4.0%), phellodendrine 0.13 part (0.4%), gallic acid 59.4 parts (60%), Osthole 2.26 (1.7%),
Digua fig stem and leaf general flavone 5.32 parts (4.0%) is made.
A kind of pharmaceutical preparation for treating hemorrhoid, it is made up of the pharmaceutical composition and auxiliary material of aforementioned therapies hemorrhoid.Its formulation is
Suppository, washing lotion, gel or ointment.
The preparation method of pharmaceutical preparation is made in the pharmaceutical composition of the aforementioned therapies hemorrhoid of the present invention：Take loganin, hardship
Join alkali, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf general flavone, add auxiliary material, routinely preparation process is made
Required formulation in materia medica meaning.
Wherein, loganin isoreactivity composition can be commercially available from the market.Conventional formulation technique alleged by the present invention with
And auxiliary material etc. refers in textbook, national standard, provincial standard disclosed method, technology and auxiliary material.
Specifically, for example, the preparation of the suppository of the present invention can be with the following method：Take formula ratio loganin, kuh-seng
Alkali, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf general flavone, it is sufficiently mixed rear stand-by；Separately suppository base is taken to mend
Football Association measures, and mixing, puts and melting is heated in water-bath, mixes, moulding, produces with above-mentioned thick paste, medicinal powder；The matrix is polyethylene glycol
4000 and Macrogol 6000 mass ratio be 1:1-1.2 mixture.
The preparation of washing lotion can be with the following method：Take formula ratio loganin, matrine, jamaicin, phellodendrine, nutgall
Acid, Osthole, digua fig stem and leaf general flavone, purified water, 0.5% sodium benzoate of total amount 80% are added, is mixed, added water to total
Amount, is produced.
The answering in treatment hemorrhoids disease medicine is prepared the invention also discloses described pharmaceutical composition or pharmaceutical preparation
With the hemorrhoids disease is by the internal piles caused by damp-heat accumulation, external piles, mixed hemorrhoid and the bleeding showed, swelling and pain.
The pharmaceutical composition and pharmaceutical preparation of the present invention passes through eliminating dampness of significantly detoxifying, arresting bleeding and treating cutaneous pyogenic infection, anti-inflammation, detumescence
The effect of analgesic, good effect achieved to treatment hemorrhoid, and directly using the active component of medicine as preparation raw material,
Solve using the problems such as medicine dosage is big made from traditional extraction technique, specific aim is incomplete, and improve and individually make
With any medicine may caused by side effect, make curative effect of medication faster, it is stronger.
Embodiment
The pharmaceutical composition or pharmaceutical preparation of the present invention, directly using the extract list of the Six-element Chinese medicinal materials such as caulis lonicerae
Body, prove that there is concertedness interaction between specific medicinal substances extract by pharmacological evaluation, applicant sends out under study for action
Existing, the digua fig stem and leaf general flavone of low dosage plays the role of anti-oxidant, antibacterial, the loganin of low dosage, matrine, Osthole,
Jamaicin, phellodendrine play the role of that obvious heat-clearing and damp-drying drug, detoxification sore treatment, desinsection be antipruritic, inhibiting bacteria and diminishing inflammation, recycle Chinese gall
Main component gallic acid the effect of, mutually promote between active constituents of medicine, coordinate synergy, strengthen medicine absorption, point
The additive effect of cloth, even more than drug alone.
When being used to treat hemorrhoidal hemorrhage, swelling and pain using each pharmaceutical preparation prepared by the pharmaceutical composition of the present invention, administration
Scheme is as follows：
Suppository：Rectally, once a grain, 2 times a day；Include in anus.
Washing lotion：External application.One bottle of 125ml of this product is taken, adds boiling water to be diluted to about 1000ml, multiplies hot smoking anus, then hip bath 20 divides
Clock.Daily morning, evening are each once.Separately this product is taken to embrocate affected part after severe person's hip bath.
Gel：External application, affected part is smeared, it is appropriate (2.5g or so) every time.
Ointment：External application, affected part is smeared, it is appropriate (2.5g or so) every time.
Embodiment
In order that those of ordinary skill in the art are better understood from the present invention, it is real that the applicant has carried out a series of pharmacodynamics
Research is tested, to prove the effect of the present invention.
Below, enumerate embodiment to further describe the present invention, but the present invention is not limited to following embodiments.
Medicine preparation embodiment：
It is the conventional side in this area to prepare method, instrument and the mode of operation prepared in embodiment used in each preparation below
Method, instrument and mode of operation.
Embodiment 1：The preparation of A1 suppositorys
Prescription：Loganin 0.48g, matrine 0.53g, jamaicin 1.39g, phellodendrine 0.13g, gallic acid 61.38, snake
Machine tool element 2.13g, digua fig stem and leaf general flavone 5.05g
Preparation method：Take formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf always yellow
Ketone, it is sufficiently mixed rear stand-by；Separately take suppository base to supply total amount 637.5g, mix, put and melting is heated in water-bath, it is and above-mentioned thick
Cream, medicinal powder mix, moulding, produce suppository 425, every weight 1.5g；The matrix is Macrogol 4000 and polyethylene glycol
6000 mass ratioes are 1:1 mixture.Every active component about 0.17g.
Embodiment 2：The preparation of A2 suppositorys
Prescription：Loganin 0.58g, matrine 0.60g, jamaicin 1.25g, phellodendrine 0.14g, gallic acid 57.42g,
Osthole 2.39g, digua fig stem and leaf general flavone 5.59g
Preparation method：Take formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf always yellow
Ketone, it is sufficiently mixed rear stand-by；Separately take suppository base to supply total amount 637.5g, mix, put and melting is heated in water-bath, it is and above-mentioned thick
Cream, medicinal powder mix, moulding, produce suppository 425, every weight 1.5g；The matrix is Macrogol 4000 and polyethylene glycol
6000 mass ratioes are 1:1.2 mixture.Every active component about 0.16g.
Embodiment 3：The preparation of B washing lotions
Prescription：Loganin 0.53g, matrine 0.56g, jamaicin 1.32g, phellodendrine 0.13g, gallic acid 59.4g, snake
Machine tool element 2.26g, digua fig stem and leaf general flavone 5.32g
Preparation method：Take formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf always yellow
Ketone, purified water, 0.5% sodium benzoate of total amount 80% are added, is mixed, is added water to total amount 1000ml, produce.Per bottled
125ml, per ml active components about 0.07g.
Embodiment 4：The preparation of C gels
Prescription：Loganin 0.4g, matrine 0.66g, jamaicin 1.15g, phellodendrine 0.16g, gallic acid 53.46g, snake
Machine tool element 1.86g, digua fig stem and leaf general flavone 5.85g
Preparation method：10g Acritamer 940s are taken to add in appropriate distilled water, stirring is stood overnight, and makes fully to be swelled, with stirring
15g triethanolamines are added, gel-type vehicle is made；Take formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Asia
Sodium sulphate, Osthole, digua fig stem and leaf general flavone, are sufficiently mixed standby；Medicinal mixture, 0.1% ethyl hydroxy benzoate is taken to be dissolved in 100g
In propane diols and 300ml ethanol, added under stirring condition in gel-type vehicle, then add distilled water to be stirred evenly, i.e., to full dose 1000ml
.Every weight 2.5g, every active component about 0.16g.
Embodiment 5：The preparation of D ointments
Prescription：Loganin 0.66g, matrine 0.47g, jamaicin 1.48g, phellodendrine 0.12g, gallic acid 65.34g,
Osthole 2.66g, digua fig stem and leaf general flavone 4.79g
Preparation method：Take formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, sodium sulfite, Osthole,
Digua fig stem and leaf general flavone, it is sufficiently mixed standby；The ointment bases such as lanolin, vaseline are added, prepares and produces ointment 1000g.Often
Branch weight 2.5g, every active component about 0.19g.
Suppository drug E1 made from 6 low amounts of components of embodiment
Prescription：Loganin 0.32g, matrine 0.38g, jamaicin 0.92g, phellodendrine 0.09g, gallic acid 45.44, snake
Machine tool element 1.50g, digua fig stem and leaf general flavone 4.07g
Preparation method：Take formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf always yellow
Ketone, it is sufficiently mixed rear stand-by；Separately take suppository base to supply total amount 637.5g, mix, put and melting is heated in water-bath, it is and above-mentioned thick
Cream, medicinal powder mix, moulding, produce suppository 425, every weight 1.5g；The matrix is Macrogol 4000 and polyethylene glycol
6000 mass ratioes are 1:1.1 mixture.Every active component about 0.12g.
Suppository drug E2 made from 7 high amounts of components of embodiment
Prescription：Loganin 0.80g, matrine 0.80g, jamaicin 1.78g, phellodendrine 0.2g, gallic acid 78.4, cnidium monnieri
The plain 3.20g of son, digua fig stem and leaf general flavone 7.02g
Preparation method：Take formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf always yellow
Ketone, it is sufficiently mixed rear stand-by；Separately take suppository base to supply total amount 637.5g, mix, put and melting is heated in water-bath, it is and above-mentioned thick
Cream, medicinal powder mix, moulding, produce suppository 425, every weight 1.5g；The matrix is Macrogol 4000 and polyethylene glycol
6000 mass ratioes are 1:1 mixture.Every active component about 0.22g.
Pharmaceutical properties evaluation experimental
Below, each medicine prepared above-mentioned preparation embodiment 1-7, carry out treating hemorrhoid effect experiment and acute poison
The evaluation experimental such as property, excitant, stability.
The pharmacodynamic study of 1 pharmaceutical composition of the present invention of experimental example
1.1 experiment material：
Medicine：A1-A2：Suppository made from embodiment 1-2；B：Washing lotion made from embodiment 3；C:Coagulated made from embodiment 4
Jelly；D：Ointment made from embodiment 5；E1：Suppository made from 6 low amounts of components of embodiment；E2：7 high component of embodiment is used
Suppository made from amount；F：Haemorrhoids bolt, every weight 2g, prepares according to WS-10506 (ZD-0506) -2002-2011Z method, makees
For positive control.
Animal：Kunming mouse, 18~22g；Wistar kind rats, 140~160g of body weight；Rabbit, 1.5~2.0kg；
By Guizhou, medical university provides.Above animal is male and female half and half.
1.2 methods and result：
1.2.1 Dichlorodiphenyl Acetate causes the influence of rabbit Perianal ulceration
Rabbit is chosen, if blank control, positive control, embodiment 1-7 amount to 9 groups, rabbit is burst by crissum after modeling
Ulcer degree and sex equilibrium assignment are to each group, every group 10.Specially：Inject 35% glacial acetic acid corrosion rectum and cause ulcer surface,
Bare substrate, haemorrhoids bolt, suppository, washing lotion made of the present composition etc. are smeared after packet respectively, it is daily to apply once, apply dosage
It is 3.27 times/kg of adult's consumption per day, continuous to smear 7 days, the 8th day observation bleeding and ulcer healing situation, to have blood in stool,
Ulcer healing degree is index, observes the therapeutic action of the present composition.It the results are shown in Table 1.
Influence (n=10) of the table 1 to rat anal orifice and rectal intestine ulcer
Note:The * P compared with blank control group<0.05, * * P<0.01
Conclusion：Visually observe, rabbit anus has that different degrees of swelling, hyperemia, ulcer wound surface are obvious after modeling, administration
Afterwards, for administration group compared with blank group, lesion degree has obvious mitigation.Simultaneously under identical medicine dosage, present invention system
Agent is good to the more existing disclosed haemorrhoids bolt of therapeutic effect of rectal ulcer rat model, it was demonstrated that invention formulation is obviously promoted routed
Ulcer heals and anastalsis, and is in good dose-effect relationship；In addition, using suppository made from the low component of monomer of the present invention,
Its therapeutic effect is slightly below existing disclosed haemorrhoids bolt, and high component curative effect is not significantly increased, shown using of the present invention
Amount ranges, work well.
1.2.2 the swelling of rat anus, the influence of vasopermeability are caused to croton oil：With distilled water：Pyridine：Ether：6% bar
Soya-bean oil=1:4:5:10 are made proinflammatory agent, establish rat anus croton oil swelling model, rat is randomly divided into 9 by medicine after modeling
Group (blank group, haemorrhoids bolt group, 1-7 of embodiment of the present invention groups), mouse anum administration, medicine is stained with 10mg cotton balls by every group 10
Thing, cotton balls is filled in rectum, once a day, drug dose is 6 times/kg of adult's consumption per day, continuous to smear 7 days, Yu Mo
30min after secondary administration, each group rat is put to death, cut the rectal tissue of the 15mm from anus fur edge.Weigh, then every group takes
The tissue of 5 rats is soaked 48 hours with acetone physiological saline, and 3000rpm is centrifuged 10 minutes, is taken supernatant to be surveyed in 590nm and is inhaled
Luminosity.Using absorbance (vasopermeability inspection target), swelling coefficient as index, the therapeutic action of the present composition is observed.
It the results are shown in Table 2.
Influence (n=10) of the table 2 to rat anus swelling
| Group | Dosage (g/kg) | Absorbance | Swelling coefficient |
| Blank group | - | 0.152±0.041 | 63.1±8.69 |
| Medicine A1 | 2.04 | 0.103±0.032* | 51.5±9.13* |
| Medicine A2 | 1.92 | 0.107±0.037* | 51.8±8.12* |
| Medicine B | 1.68 | 0.118±0.028* | 52.5±7.78* |
| Medicine C | 1.92 | 0.110±0.022* | 51.9±9.25* |
| Medicine D | 2.28 | 0.105±0.031* | 51.3±8.61* |
| Medicine E1 | 1.44 | 0.129±0.044 | 56.8±10.82 |
| Medicine E2 | 2.64 | 0.102±0.025* | 51.1±8.03* |
| Medicine F | 24 | 0.121±0.027* | 53.6±7.56* |
Note:The * P compared with blank control group<0.05, * * P<0.01
Conclusion：Anus swelling of the medicine of the present invention to rat caused by croton oil is inhibited, can reduce mould well
The rectum vein permeability of type rat, there were significant differences compared with control group.Under identical medicine dosage, medicine of the present invention
It is good with the more existing disclosed haemorrhoids bolt of oedema effect that thing group anti-inflammatory, reduction ooze out, and is in good dose-effect relationship；In addition, using this
Suppository made from the low component of the monomer is invented, its therapeutic effect is suitable with existing disclosed haemorrhoids bolt, and high component curative effect does not have
It is significantly increased, shows to use amount ranges of the present invention, anti-inflammation detumescence works well.
1.2.3 analgesic experiment：Influence to formalin induced mice writhing response.Take 18-20g mouse, by body weight with
Machine is divided into 9 groups (blank group, haemorrhoids bolt group, 1-7 of embodiment of the present invention groups), every group 10.Mouse anum administration, with 10mg cotton balls
Be stained with medicine, cotton balls filled in rectum, once a day, drug dose be grown up consumption per day 9 times/kg, continuous 3d, last
30min after administration, only, the writhing of mouse in 20 minutes is observed away from the formalin 0.2ml/ of rectal wall injection 5% at anus 3.5cm
Number (stretching, extension hind leg, belly shrink and distortion body).It the results are shown in Table 3.
Analgesic activity (n=10) (x ± s) of the table 3 to mouse
| Group | Dosage (g/kg) | Writhing number (secondary) | Inhibiting rate (%) |
| Control group | - | 39.6±7.41 | - |
| Medicine A1 | 3.06 | 23.8±6.23** | 39.9 |
| Medicine A2 | 2.88 | 24.2±6.62** | 38.9 |
| Medicine B | 2.52 | 25.1±7.47* | 36.6 |
| Medicine C | 2.88 | 24.5±5.82** | 38.1 |
| Medicine D | 3.42 | 23.9±6.26** | 39.6 |
| Medicine E1 | 2.16 | 29.9±7.13 | 24.5 |
| Medicine E2 | 3.96 | 23.7±8.15** | 40.1 |
| Medicine F | 36 | 27.6±7.83* | 30.3 |
Note:The * P compared with medicine F groups<0.05, * * P<0.01
Conclusion：Shown in upper table, medicine group of the present invention can substantially reduce the writhing number of mouse, compared with control group, have
Significant difference, show that medicine of the present invention has obvious inhibitory action to pain caused by chemical irritation.In identical medicine agent
Under amount, the more existing disclosed haemorrhoids bolt of medicine analgesic effect of the present invention is good, and is in good dose-effect relationship；In addition, using the present invention
Suppository made from the low component of the monomer, its therapeutic effect is undesirable, and high component curative effect is not significantly increased, and shows using this
The described amount ranges of invention, analgesic effect are good.
1.3 conclusion：According to above experimental result, medicine of the present invention can obviously improve acute ulcer, Hemorrhage Model animal
General state and the pathological change of perianal tissue, rat anus swelling caused by mitigating croton oil, show that the medical instrument has stronger resist
Scorching, hemostasis, promote ulcer healing effect；Mouse writhing response caused by formalin stimulates can be substantially reduced, shows the medicine pair
The pain that chemical stimulation induces has obvious inhibitory action.Under identical drug dose, the above-mentioned action effect of medicine of the present invention
More existing disclosed haemorrhoids bolt is good；It is in addition, good using amount ranges of the present invention, therapeutic effect.Illustrate the present invention's
Composition and its preparation, there is good result in rush ulcer healing, hemostasis, anti-inflammatory, ease pain.
Experimental example 2：The pharmacological toxicology experimental study of pharmaceutical composition of the present invention
2.1 acute toxicity test：
2.1.1 experiment material：Medicine：A：Suppository made from embodiment 1；B：Glue washing lotion made from embodiment 3；C:Embodiment
Gel made from 4；D：Ointment made from embodiment 5；E1：Suppository made from 6 low amounts of components of embodiment；E2：Embodiment 7
Suppository made from high amounts of components；Animal：Kunming mouse 140,20 ± 2g of body weight, male and female dual-purpose.
2.1.2 test method：Healthy mice 140 is taken, is randomly divided into 7 groups, every group 20, male and female half and half.Will before experiment
Animal fasting 16 hours, not water restriction, then each group mouse difference anum administration (medicine is stained with 10mg cotton balls, by cotton balls
Fill in rectum), wherein blank group gives bare substrate, and remaining each group dosage is：Medicine A：6.8g active components/kg；
B：5.6g active components/kg；C：6.4g active components/kg；D：7.6g active components/kg；E1：4.8g active components/kg；E2：
8.8g active components/kg.Observation 7 days, normal diet, drinking-water, observe mouse ordinary circumstance (changes of weight, diet, fur,
Behavior, secretion, excreta etc.) and poisoning, death condition.
2.1.3 result：Acute toxicity test shows that animal activity is normal after the administration of medicine each group, and none is dead in the observation period
Die.In addition to E2 groups, remaining each group diet and activity are normal, and fur is smooth, the no abnormality seen secretion such as mouth, nose, eye；Medicine E2 groups
After administration in 2 days, there is that a small number of mouse part skin furs are fluffy and disorderly, occur it is dispirited it is few it is dynamic wait toxic reaction, but hereafter gradually recover
Normally.
2.2 mucomembranous pungency test
2.2.1 experiment material：Medicine：A：Suppository made from embodiment 1；B：Glue washing lotion made from embodiment 3；C:Embodiment
Gel made from 4；D：Ointment made from embodiment 5；E1：Suppository made from 6 low amounts of components of embodiment；E2：Embodiment 7
Suppository made from high amounts of components；Animal：Rabbit 60,2.2 ± 2kg of body weight, male and female dual-purpose.
2.2.2 test method：Every group of rabbit gives experiment medicine respectively by the clinical 5 times of amounts of adult, is taken twice daily,
Interval 2 hours or so, continuous 7 days.24 hours each groups put to death rabbit 5 after last dose, observe the stimulate the reaction of rectum, go forward side by side
Row histopathologic examination.Remaining animal is observed day by day, puts to death within the 14th day after drug withdrawal, observes the stimulate the reaction of rectum, go forward side by side
Row histopathologic examination.
2.2.3 result：Trial drug A-E groups are showed no in multiple dosing phase and convalescence to be there is rectum hyperemia, oedema, divides
Phenomena such as secretion；Case control shows that administration phase and convalescence family's rabbit rectum near-end, middle-end, the gut wall structure of each section of distal end are clear
Chu, mucomembranous epithelial cell, lamina propria and muscle layer boundary are clear.Show that preparation made of the present composition is made without obvious stimulation
With.
2.3 conclusion：Understood according to this experimental result, the present composition and its preparation are acted on very Mouse Acute Toxicity
It is low, without obvious stimulation act on, it is contemplated that the high amounts of components of monomer of the present invention can cause mild toxicity, therefore, clinically
It is not recommended that the high amounts of components using monomer of the present invention.
The study on the stability of 3 pharmaceutical preparation of the present invention of experimental example
Accelerated stability test：Randomly select obtained each portion of sample, numbering 1-4, in temperature in embodiment 1,3,4,5
40 DEG C ± 2 DEG C, placed under conditions of relative humidity 75% ± 5%, respectively 1st month, 2 months, 3 months, 6 during experiment
The end of month sampling is once investigated.
Investigate using product characteristics, discriminating, gallic acid content, kuh-seng alkali number as index, check the stability of product.As a result
It is shown in Table 4.
The accelerated stability test result of table 4
Conclusion：The composition for the treatment of hemorrhoid prepared by the present invention is stored under the conditions of accelerated test, and result is investigated from acceleration
From the point of view of, each investigation project loses exception, and significant change does not also occur, meets quality criteria requirements for active constituent content.
Pass through above-mentioned curative effect, acute toxicity, excitant, stability experiment, it can be seen that using the present composition and system
Standby preparation, therapeutic effect is better than existing disclosed haemorrhoids bolt, and toxicity and excitant are low, and preparation has good stability, and is to control
The hemorrhoids diseases such as internal piles, external piles mixed hemorrhoid are treated, lower the another good selection of the symptoms such as bleeding, swelling and pain.In addition, by above-mentioned implementation
Example as can be seen that although low consumption proportion toxicity is low but therapeutic effect is undesirable, although and high consumption proportion curative effect improves,
It is that there is certain toxicity, therefore, when the dosage of each component is in the range of the pharmaceutical composition of the present invention, solving can
Treat disease toxicity and the low technical barrier of excitant again simultaneously.
Claims (8)
1. a kind of pharmaceutical composition for treating hemorrhoid, is calculated by weight, by loganin 0.40-0.66 parts (0.15-0.25%)
Part, matrine 0.47-0.66 parts (0.25-0.35%), jamaicin 1.15-1.48 parts (3.5-4.5%), phellodendrine 0.12-
0.16 part (0.36-0.44%), gallic acid 53.46-65.34 parts (54-66%), Osthole 1.86-2.66 (1.4-
2.0%), digua fig stem and leaf general flavone 4.79-5.85 parts (3.6-4.4%) are made.
2. pharmaceutical composition according to claim 1, is calculated by weight, by loganin 0.48-0.58 parts (0.18-
0.22%) part, matrine 0.53-0.60 parts (0.28-0.32%), jamaicin 1.25-1.39 parts (3.8-4.2%), phellodendrine
0.13-0.14 parts (0.38-0.42%), gallic acid 57.42-61.38 parts (58-62%), Osthole 2.13-2.39
(1.6-1.8%), digua fig stem and leaf general flavone 5.05-5.59 parts (3.8-4.2%) are made.
3. pharmaceutical composition according to claim 1, is calculated by weight, by loganin 0.53 part of (0.2%) part, kuh-seng
Alkali 0.56 part (0.30%), jamaicin 1.32 parts (4.0%), phellodendrine 0.13 part (0.4%), 59.4 parts of gallic acid
(60%), Osthole 2.26 (1.7%), digua fig stem and leaf general flavone 5.32 parts (4.0%) are made.
4. a kind of pharmaceutical preparation for treating hemorrhoid, it is made up of the pharmaceutical composition described in technical scheme any one of 1-3 and auxiliary material.
5. the pharmaceutical preparation for the treatment of hemorrhoid according to claim 4, its formulation are suppository, washing lotion, gel, ointment.
6. the pharmaceutical preparation for the treatment of hemorrhoid according to claim 4, the preparation method of suppository are：
Formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf general flavone are taken, it is fully mixed
It is stand-by after conjunction；Separately take suppository base to supply total amount, mix, put and melting is heated in water-bath, mixed with above-mentioned thick paste, medicinal powder, moulding,
Produce；The matrix is Macrogol 4000 and Macrogol 6000 mass ratio is 1:1-1.2 mixture.
7. the pharmaceutical preparation for the treatment of hemorrhoid according to claim 4, the preparation method of washing lotion are：
Formula ratio loganin, matrine, jamaicin, phellodendrine, gallic acid, Osthole, digua fig stem and leaf general flavone are taken, is added total
The purified water of amount 80%, 0.5% sodium benzoate, mix, add water to total amount, produce.
8. the pharmaceutical preparation described in pharmaceutical composition or claim 4 or 5 described in claim any one of 1-3 is preparing treatment
Application in hemorrhoids disease medicine, the hemorrhoids disease is by the internal piles caused by damp-heat accumulation, external piles, mixed hemorrhoid and what is showed go out
Blood, swelling and pain, itch.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710995293.5A CN107669742A (en) | 2017-10-23 | 2017-10-23 | Treat pharmaceutical composition, pharmaceutical preparation and the application of hemorrhoid |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201710995293.5A CN107669742A (en) | 2017-10-23 | 2017-10-23 | Treat pharmaceutical composition, pharmaceutical preparation and the application of hemorrhoid |
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Family
ID=61141466
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101264155A (en) * | 2008-04-25 | 2008-09-17 | 贵州拜特制药有限公司 | Medicine for treatment of piles and preparation method thereof |
| CN105831541A (en) * | 2016-02-29 | 2016-08-10 | 武汉华康臣生物科技有限公司 | Solid beverage applicable to patients with hyperuricemia and gout, and preparation method thereof |
-
2017
- 2017-10-23 CN CN201710995293.5A patent/CN107669742A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101264155A (en) * | 2008-04-25 | 2008-09-17 | 贵州拜特制药有限公司 | Medicine for treatment of piles and preparation method thereof |
| CN105831541A (en) * | 2016-02-29 | 2016-08-10 | 武汉华康臣生物科技有限公司 | Solid beverage applicable to patients with hyperuricemia and gout, and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 徐君飞等: "响应面法优化水提地瓜藤中总黄酮工艺", 《食品研究与开发》 * |
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