CN1559516A - Suppository and effervescence tablet for treating gynecopathy inflammation and its preparation method - Google Patents

Abstract

A Chinese medicine in the form of suppository or effervescent tablet for treating vaginitis, cervicitis and cervical erosion is prepared from 8 Chinese-medicinal materials including rhubarb, myrobalan seed, borax, natural indigo, etc. Its preparing process is also disclosed.

Description

A kind of suppository for the treatment of gynecological inflammation and effervescent tablet and preparation method thereof

Technical field

The present invention relates to a kind of suppository for the treatment of vaginitis, cervicitis, cervical erosion and effervescent tablet and preparation method thereof.

Background technology

Vaginitis, cervicitis, cervical erosion are the women of child-bearing age's commonly encountered diseases, frequently-occurring diseases, and sickness rate accounts for the women of child-bearing age's 60%, the rural area women of child-bearing age even can reach 80%.Build consensus in medical circle because chronic cervicitis, cervical erosion can be brought out cervical cancer, therefore, active prevention and treatment gynecological inflammation are to ensure body of women health, prevent the important channel that cervical cancer takes place.

At present, there are many Western medicine to can be used for the treatment of vaginitis, cervicitis, cervical erosion, but the defective of Western medicine is apparent in view, as act on single, easily develop immunity to drugs, zest, anaphylaxis, internal organs such as Liver and kidney there is bigger toxic and side effects, being unsuitable for anemia of pregnant woman or women breast-feeding their children uses, intravaginal profitable strain (as lactobacillus) had killing action equally, easily cause the intravaginal dysbacteriosis, destroy self-cleaning system of vagina or the like, some medicine itself may be carcinogenic in addition, the potential danger (as metronidazole, metronidazole etc.) of teratogenesis.

Summary of the invention

Invented the prescription of a kind of suppository and effervescent tablet forms and preparation technology for the deficiency that overcomes the many Western medicine that are used for vaginitis, cervicitis, cervical erosion at present.

Technical scheme of the present invention is as follows: it mainly consists of: Radix Et Rhizoma Rhei 5～15g, Fructus Chebulae 5～15g, Fructus Mume 4～12g, Borax 1～5g, Indigo Naturalis 1～5g, Borneolum Syntheticum 1～3g, heat clearing and dampness removing medicine 5～15g, heat removing and blood cooling medicine 5～15g.

Wherein heat clearing and dampness removing medicine is that Cortex Phellodendri, heat removing and blood cooling medicine are Radix Arnebiae (Radix Lithospermi)s.

Preparation method of the present invention is: with heat clearing and dampness removing medicine granule ethanol percolation, collect percolate, decompression recycling ethanol and the relative density that is concentrated into regulation get A; With Radix Et Rhizoma Rhei and heat removing and blood cooling medicine granule, ethanol percolation is collected percolate, and decompression recycling ethanol and the relative density that is concentrated into regulation get B; Fructus Chebulae, the conventional decocting of Fructus Mume decoction pieces, precipitate with ethanol are got C; Indigo Naturalis is added water, boil the back sucking filtration, the precipitation drying under reduced pressure, pulverize D; In A, add a certain amount of Borax, spray drying.After B and C merging, add a certain amount of Borax, spray drying; With dry powder after the above spray drying and Borneolum Syntheticum powder mixing, add in the substrate, make suppository in accordance with the law.Or adding other adjuvant, compacting is in flakes.

During the medicinal ethanol percolation of heat clearing and damp drying, concentration of alcohol is 80% (volumetric concentration), collects the percolate (bulking value multiple) of 12 times of medical material amounts.During the medicinal ethanol percolation of Radix Et Rhizoma Rhei and clearing away heat and cooling blood, concentration of alcohol is 90% (volumetric concentration), collects the percolate (bulking value multiple) of 15 times of medical material amounts.When Fructus Chebulae, water decocted solution of fructus mume precipitate with ethanol, concentration of alcohol is 80% (volumetric concentration).The used substrate of suppository is the semi-synthetic fatty acid esters of 34 types; The used disintegrating agent of effervescent tablet is citric acid and sodium bicarbonate, and sodium bicarbonate is with polyethylene glycol 6000 (PEG6000) inclusion of its half amount, and used adjuvant is dextrin-micropowder silica gel (7: 3) mixture and microcrystalline Cellulose.

Many deficiencies of chemical medicine both can have been overcome by the compound Chinese medicinal preparation of theory of Chinese medical science prescription, can bring into play the incomparable many-sided therapeutical effect of chemical medicine (invigorating blood circulation or the like) again as putrefaction-removing granulation-promoting, astringing to arrest bleeding, dampness removing, can be widely used in pathogenic former caused gynecological inflammation such as antibacterial, fungus, protozoon, chlamydia, mycoplasma, simultaneously, Chinese traditional compound medicine also has the effect of pH buffer agent, by regulating vagina pH, make it to become and normally suppress pathogenic microorganism or protozoacide growth and breeding.In addition, modern disease Neo-Confucianism thinks that human papillomavirus, herpesvirus especially II herpes simplex virus type are one of main inducing of cervical cancer, and Chinese medicine will be better than Western medicine far away to the comprehensive inhibitory action of virus.Therefore, aspect the treatment gynecological inflammation, the exploitation determined curative effect, the pure Chinese medicinal preparation of dosage form novelty has vast market prospect.

Modern chemistry and pharmaceutical research show, main component in the Cortex Phellodendri is to be the alkaloids of representative with berberine, palmatine, jateorhizine, these compositions all have inhibitory or killing effect to antibacterial such as staphylococcus aureus, Streptococcus viridans, dysentery bacterium, trichophyton, acrothesium floccosum, trichophyton, Du Ang Shi sporidiole bacteria difficult to understand, epidermophyton inguinale and fungus, and leptospira, trichomonas vaginitis are also killed or inhibitory action.Radix Et Rhizoma Rhei mainly contains free type and combined anthraquinone compounds, glycoside as emodin, chrysophanol, chrysophanic acid, physcione and mentioned component, in addition, also contain a certain amount of tannin constituents, the dissociated anthraquinone constituents all has stronger inhibitory or killing effect to some gram negative bacteria and fungus, simultaneously, can also significantly reduce the permeability of blood capillary, improve its fragility, exosmose and rhatannin can reduce wound surface body fluid.Radix Arnebiae (Radix Lithospermi) mainly contains the naphthoquinone constituents, as Shikonin etc., staphylococcus aureus, escherichia coli and multiple fungus is had inhibitory action, simultaneously, can significantly reduce the permeability of blood capillary, promotes wound healing.Fructus Chebulae and Fructus Mume mainly contain tannin, organic acid composition, and dysentery bacterium, staphylococcus aureus, bacillus pyocyaneus, Bacillus typhi, Salmonella paratyphi, bacillus subtilis, escherichia coli, Hemolytic streptococcus, Bacillus proteus etc. are all had stronger inhibitory action.Main active in the Indigo Naturalis is indigo and indirubin, and staphylococcus, anthrax bacillus, dysentery bacterium, vibrio cholera are all had inhibitory action, simultaneously, has antitumor action.The main component of Borax is a sodium tetraborate, and sore swollen toxin from the beginning of heat clearing away eliminating stagnation, reducing swelling and alleviating pain effect are arranged, is had the astringent therapy antisepsis to the back skin infection of bursting.The main component of Borneolum Syntheticum is Borneolum Syntheticum and isoborneol, and staphylococcus aureus, streptococcus, escherichia coli and pathogenic dermatophytes are all had inhibitory action.

The test of pesticide effectiveness result of this product is as follows:

1, antiinflammatory test: the peaceful 6g/kg of cervix uteri, 12g/kg, 24g/kg dosage group xylol induced mice auricle edema have certain inhibitory action, suppression ratio is respectively 50%, 50% and 58.3%, relatively has significant difference (P＜0.01, P＜0.001) with the blank group.Have the effect that obvious reduction histamine phosphate induced mice capillary permeability increases simultaneously, relatively have significant difference (P＜0.05, P＜0.01) with the blank group.On Carrageenan causes rat paw edema behind 6g/kg and the 12g/kg dosage group self administration of medication 1h the obvious suppression effect, relatively has significant difference (P＜0.05, P＜0.01) with the blank group.

Prompting: the peaceful xylol of cervix uteri, histamine phosphate and carrageenin cause inflammation all antiinflammatory action preferably.

2, analgesic test: adopt hot plate method, the peaceful 6g/kg of cervix uteri, 12g/kg, 24g/kg dosage group can obviously improve the pain threshold of mice, and act on the length of holding time, and relatively have significant difference (P＜0.05, P＜0.01) with the blank group.Adopt writhing method, the peaceful 6g/kg of cervix uteri, 12g/kg, 24g/kg dosage group Dichlorodiphenyl Acetate be pain caused the obvious suppression effect, can make to turn round the body number of times and reduce, and turns round the body prolongation of latency.

Prompting: cervix uteri rather has stronger analgesic activity.

3, extracorporeal bacteria inhibitor test: cervix uteri rather has stronger inhibitory action to clinical SEPARATION OF GOLD Staphylococcus aureus, staphylococcus hominis, Bacillus alcaligenes, citrobacter, Bacillus proteus, Candida albicans, table staphylococcus etc., and MIC is between 3.13～6.25mg/ml.

Prompting: cervix uteri rather has the good in-vitro bacteriostasis.

4, antipruritic test: the peaceful 3g/kg of cervix uteri, 6g/kg and 12g/kg dosage group can obviously improve the itch-threshold that histamine phosphate causes Cavia porcellus, relatively have significant difference (P＜0.05, P＜0.01, P＜0.001) with model group.

Prompting: cervix uteri rather has itching-relieving action preferably.

5, to the therapeutic test of experimental rat cervicitis model: the peaceful 0.4g/kg of cervix uteri, 0.8g/kg and 1.6g/kg dosage group are to experimental rat cervicitis model due to the 25% phenol rubber cement, transvaginal administration 10 days, can obviously reduce PGE content in uterus and the vagina tissue, relatively has significant difference (P＜0.05 with model group, P＜0.01), and total white blood cells and neutrophilic granulocyte are significantly reduced, with model group significant difference (P＜0.05) is arranged relatively.The result of histopathologic examination shows that also it has the good curing effect to experimental rat cervicitis model.

6, to the inactivation test of herpes simplex virus I I type (HSV-2): when the peaceful concentration of cervix uteri is 12.5mg/ml, but 5 minutes complete inactivation HSV-2 of effect; When concentration is 25mg/ml, but 1 minute complete inactivation HSV-2 of effect.

Prompting: the peaceful external effect of cervix uteri with deactivation HSV-2.

7, anti-gonococcus test: rather when concentration was 3.125mg/ml, effect 1min can kill 49.9% gonococcus to cervix uteri; When concentration was 12.5mg/ml, effect 1min can kill 100% gonococcus.

Prompting: the peaceful external gonococcal effect of killing that has of cervix uteri.

8, anti-trichomonal vaginitis test: rather when concentration was 12.5mg/ml, effect 3min cultivated 3d to cervix uteri, does not see the activity trichomonal vaginitis.Cultivate 7d, concentration is also seen small number of activity polypide (about 30%) when 50mg/ml.

Prompting: the peaceful nothing of cervix uteri is killed but the effect that suppresses trichomonal vaginitis is arranged.

9, to the test of killing of chlamydia trachomatis: when the peaceful concentration of cervix uteri was 6.25mg/ml, effect 1min had killing action to chlamydia trachomatis.

Prompting: the peaceful external effect of killing chlamydia trachomatis that has of cervix uteri.

10, to the test of killing of Ureaplasma urealyticum: when the peaceful concentration of cervix uteri was 6.25mg/ml, effect 1min can kill Ureaplasma urealyticum.

Prompting: the peaceful external effect of killing Ureaplasma urealyticum that has of cervix uteri.

The specific embodiment

A kind of suppository and effervescent tablet prescription for the treatment of gynecological inflammation of the present invention is: Cortex Phellodendri 5～15g, Radix Et Rhizoma Rhei 5～15g, Radix Arnebiae (Radix Lithospermi) 5～15g, Fructus Chebulae 5～15g, Fructus Mume 4～12g, Borax 1～5g, Indigo Naturalis 1～5g, Borneolum Syntheticum 1～3g.

Concrete preparation process is: the Gan Cortex Phellodendri powder is broken into the granule about 8 orders, and with 60% ethanol percolation routinely, percolation speed is 5ml/min.kg, the percolate of 12 times of amounts of collection, and decompression recycling ethanol also is concentrated into about 1.05 (60～80 ℃) of relative density.

Radix Et Rhizoma Rhei, Radix Arnebiae (Radix Lithospermi) are ground into granule about 8 orders, and with 90% ethanol percolation routinely, percolation speed is 8ml/min.kg, collects the percolate of 15 times of amounts, and decompression recycling ethanol also is concentrated into about 1.05 (60～80 ℃) of relative density.

With Fructus Chebulae, Fructus Mume decoction pieces, add 10 times of water gagings, flooded conventional decoction 2 times, each 2 hours 1 hour, collecting decoction, be evaporated to about 1.15 (50～60 ℃) of relative density, add ethanol to containing alcohol amount 80%, precipitate with ethanol is more than 8 hours, sucking filtration, decompression filtrate recycling ethanol also is concentrated into about 1.05 (60～80 ℃) of relative density.

The Borax that in Cortex Phellodendri fluid, adds 1/5th amounts, parboiling, No. 6 sieve filters (precipitate drying under reduced pressure, pulverizing, cross sieve No. 6, merge with spray drying powder), spray drying, dry powder is airtight standby.

With Radix Et Rhizoma Rhei, Radix Arnebiae (Radix Lithospermi) and Fructus Chebulae, the merging of Fructus Mume two extracting section liquid, add the Boraxs of 4/5ths amounts, parboiling, No. 6 sieve filters (precipitate drying under reduced pressure, pulverizing, cross sieve No. 6, merge with spray drying powder), spray drying, dry powder is airtight standby.

Indigo Naturalis is added 8～10 times of water gagings, boil 10min, cooling back sucking filtration, precipitation drying under reduced pressure (60～70 ℃) is pulverized, crosses sieve No. 6.

Take by weighing the substrate of amount of calculation, heating in water bath makes fusing, gets above three part medicated powder, adds Borneolum Syntheticum (crossing sieve No. 6), mixing, cross sieve No. 6, add in the substrate, fully stir evenly, inject the bolt mould that had been coated with lubricant, wait solidify fully after, cut and overflow part, open the bolt mould, promptly.

Or get above three part medicated powder, add dextrin-micropowder silica gel (7: 3) mixture to 520g (add to 1.04g/ people. day), adding citric acid (cross No. 6 sieve) 69.88g, mixing is crossed sieve in the lump No. 6.Ethanol about 80% is wetting agent, No. 1 sieve series grain, oven dry about 80 ℃, granulate.

Take by weighing NaHCO ₃91.55g, add among the PEG6000 that has melted in the 45.78g water-bath, stir evenly, cooling (can put refrigerator and cooled but a few hours) is pulverized, and crosses sieve No. 5.

With above two partially mixed, add Borneolum Syntheticum (crossing sieve No. 6) and 30g microcrystalline Cellulose (0.06g/ people. day),

Mixing is weighed, and adds 0.3% magnesium stearate, and mixing is pressed into oval special-shaped sheet.

Claims (7)

1, a kind of suppository and effervescent tablet for the treatment of gynecological inflammation, it mainly consists of: Radix Et Rhizoma Rhei 5～15g, Fructus Chebulae 5～15g, Fructus Mume 4～12g, Borax 1～5g, Indigo Naturalis 1～5g, Borneolum Syntheticum 1～3g, heat clearing and dampness removing medicine 5～15g, heat removing and blood cooling medicine 5～15g.

2, suppository according to claim 1 and effervescent tablet is characterized in that heat clearing and dampness removing medicine is that Cortex Phellodendri, heat removing and blood cooling medicine are Radix Arnebiae (Radix Lithospermi)s.

3, a kind of preparation method for the treatment of the suppository and the effervescent tablet of gynecological inflammation, its preparation process is: with heat clearing and dampness removing medicine granule ethanol percolation, collect percolate, decompression recycling ethanol and the relative density that is concentrated into regulation get A; With Radix Et Rhizoma Rhei and heat removing and blood cooling medicine granule, ethanol percolation is collected percolate, and decompression recycling ethanol and the relative density that is concentrated into regulation get B; Fructus Chebulae, the conventional decocting of Fructus Mume decoction pieces, precipitate with ethanol are got C; Indigo Naturalis is added water, boil the back sucking filtration, the precipitation drying under reduced pressure, pulverize D; In A, add a certain amount of Borax, spray drying.After B and C merging, add a certain amount of Borax, spray drying; With dry powder after the above spray drying and Borneolum Syntheticum powder mixing, add in the substrate, make suppository in accordance with the law.Or adding other adjuvant, compacting is in flakes.

4, preparation method according to claim 3, when it is characterized in that the medicinal ethanol percolation of heat clearing and damp drying, concentration of alcohol is 80% (volumetric concentration), collects the percolate (bulking value multiple) of 12 times of medical material amounts.

5, preparation method according to claim 3, when it is characterized in that the medicinal ethanol percolation of Radix Et Rhizoma Rhei and clearing away heat and cooling blood, concentration of alcohol is 90% (volumetric concentration), collects the percolate (bulking value multiple) of 15 times of medical material amounts.

6, preparation method according to claim 3, when it is characterized in that Fructus Chebulae, water decocted solution of fructus mume precipitate with ethanol, concentration of alcohol is 80% (volumetric concentration).

7, preparation method according to claim 3 is characterized in that the used substrate of suppository is the semi-synthetic fatty acid esters of 34 types; The used disintegrating agent of effervescent tablet is citric acid and sodium bicarbonate, and sodium bicarbonate is with polyethylene glycol 6000 (PEG6000) inclusion of its half amount, and used adjuvant is dextrin one micropowder silica gel (7: 3) mixture and microcrystalline Cellulose.