CN105106561A - Miconazole nitrate compound vaginal extended-release effervescent tablets and preparation method thereof - Google Patents
Miconazole nitrate compound vaginal extended-release effervescent tablets and preparation method thereof Download PDFInfo
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Abstract
The invention discloses miconazole nitrate compound vaginal extended-release effervescent tablets and a preparation method thereof. The effervescent tablets comprise miconazole nitrate, Corydalis tuber, Tricyrtis root, lightyellow Sophora root, cutch, Wilson's passion flower, root of Silene tenuis, root-bark of shaggy-fruited dittany, fleeceflower root, Chinese mugwort leaf, sodium alginate, polyoxyethylene, fumaric acid, sodium carbonate, sodium bicarbonate, lauryl sodium sulfate, powdered sugar, and polysorbate. The preparation method includes: preparing materials, extracting effective ingredients of herbal materials, and performing granulating and tableting. The miconazole nitrate compound vaginal extended-release effervescent tablets are a Chinese and western medicine mixture, the defect that miconazole nitrate is only capable of killing germs and diminishing inflammation is effectively overcome, and the herbs are good in synergistic effect. Hydrophilic gel extended-release material is used as a medicinal auxiliary material, acting time of the tablets and administering interval can be prolonged, and bioavailability of the tablets can be improved; the tablets directly act on an affected part, take effect fast, are good in effect, are convenient to use and allow higher patient compliance.
Description
Technical field
The invention belongs to local application field, is specifically a kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet and preparation method.
Background technology
Vaginitis is the modal infectious disease of women, and its common sympton is that vaginal secretions increases, and pruritus vulvae, causalgia can with frequent micturition, dysurea and sexual anhedonias.The visible vaginal secretions of gynecologial examination increases, and vaginal mucosa is congested or be dispersed in hemorrhage speckle, and posterior fornix of vagina has volume leucorrhea, in lark or yellow green purulent secretion, and show bubble or white stiff curdled milk or bean dregs sample sometimes.The visible edema of pudendum, scratch, pattern erythema.
Vaginal mucosa administration has the history of last 100 years, has many advantages compared with traditional oral administration, not only can local application, also can general medication.Medicine, by vaginal mucosa local application, can improve the drug level of local, give full play to curative effect of medication, avoid general action; Medicine plays general action by the absorption of vaginal mucosa, can avoid the first pass effect of hepar of medicine, improves bioavailability, reduces toxic and side effects, it also avoid the gastrointestinal reaction of some drugs.
Miconazole nitrate belongs to antifungal agent this product can suppress most of conk when 4mg/L concentration, and Blastomyces, tissue milk born of the same parents Pseudomonas present extremely sensitive to it, and Cryptococcus, Candida, Coccidioides etc. are also responsive to this product.By the activity of interference cell pigment P-450, thus the biosynthesis of Antifungi cell membrane major sterols class-ergosterol, damage fungal cell membrane also changes its permeability, so that important intracellular matter leaks outside; Also can the triacylglycerol of Antifungi and the biosynthesis of phospholipid, the activity of inhibited oxidation enzyme and peroxidase, causes intracellular hydrogen peroxide to gather and causes the degeneration of cell submicroscopic structure and necrocytosis.It then can be suppressed to change the process of aggressive mycelia into from spore to Candida albicans.
Miconazole nitrate mainly suppresses most of conk, and to fungus-caused colpitic symptom as secretions increase, pruritus vulvae, causalgia, can but not have direct therapeutic effect with frequent micturition, dysurea and sexual anhedonia.Therefore during independent miconazole nitrate treatment vaginitis, slowly effective to fungus-caused colpitic symptom.
Summary of the invention
Colpitic curative effect is treated in order to improve miconazole nitrate, improve the compliance of patient, the invention provides a kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, this effervescent tablet is used for topical therapeutic vaginitis, directly act on affected part, rapid-action, good effect, have no side effect, can treating both the principal and secondary aspects of a disease vaginitis.
The present invention seeks to be realized by following technical scheme:
A kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 1 ~ 3 part, Rhizoma Corydalis 20 ~ 25 parts, Radix Tricyrtidis pilosae 15 ~ 20 parts, Radix Sophorae Flavescentis 40 ~ 45 parts, 35 ~ 40 parts, catechu, Herba Passiflorae Wilsonii 60 ~ 70 parts, Radix Silenes Tenuis 30 ~ 40 parts, Cortex Dictamni 30 ~ 40 parts, Radix Polygoni Multiflori 35 ~ 40 parts, Folium Artemisiae Argyi 50 ~ 60 parts, sodium alginate 5 ~ 10 parts, polyethylene glycol oxide 5 ~ 10 parts, fumaric acid 5 ~ 10 parts, sodium carbonate 3 ~ 5 parts, sodium bicarbonate 4 ~ 10 parts, sodium lauryl sulphate 1 ~ 2 part, Icing Sugar 5 ~ 10 parts, Polysorbate 0.5 ~ 1 part.
Further, the object of the invention can also be realized by following technical scheme:
A kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 1 part, Rhizoma Corydalis 20 parts, Radix Tricyrtidis pilosae 15 parts, Radix Sophorae Flavescentis 40 parts, 35 parts, catechu, Herba Passiflorae Wilsonii 60 parts, Radix Silenes Tenuis 30 parts, Cortex Dictamni 30 parts, Radix Polygoni Multiflori 35 parts, Folium Artemisiae Argyi 50 parts, sodium alginate 5 parts, polyethylene glycol oxide 5 parts, fumaric acid 5 parts, sodium carbonate 3 parts, sodium bicarbonate 4 parts, sodium lauryl sulphate 1 part, Icing Sugar 5 parts, Polysorbate 0.5 part.
A kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 2 parts, Rhizoma Corydalis 22 parts, Radix Tricyrtidis pilosae 18 parts, Radix Sophorae Flavescentis 43 parts, 37 parts, catechu, Herba Passiflorae Wilsonii 65 parts, Radix Silenes Tenuis 35 parts, Cortex Dictamni 38 parts, Radix Polygoni Multiflori 36 parts, Folium Artemisiae Argyi 57 parts, sodium alginate 7 parts, polyethylene glycol oxide 6 parts, fumaric acid 8 parts, sodium carbonate 4 parts, sodium bicarbonate 6 parts, sodium lauryl sulphate 1.5 parts, Icing Sugar 9 parts, Polysorbate 0.7 part.
A kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 3 parts, Rhizoma Corydalis 25 parts, Radix Tricyrtidis pilosae 20 parts, Radix Sophorae Flavescentis 45 parts, 40 parts, catechu, Herba Passiflorae Wilsonii 70 parts, Radix Silenes Tenuis 40 parts, Cortex Dictamni 40 parts, Radix Polygoni Multiflori 40 parts, Folium Artemisiae Argyi 60 parts, sodium alginate 10 parts, polyethylene glycol oxide 10 parts, fumaric acid 10 parts, sodium carbonate 5 parts, sodium bicarbonate 10 parts, sodium lauryl sulphate 2 parts, Icing Sugar 10 parts, Polysorbate 1 part.
Present invention also offers a kind of preparation method of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, comprise the following steps:
1) get the raw materials ready, get the raw materials ready according to described component and parts by weight, miconazole nitrate pulverized 120 mesh sieves, and sodium alginate, polyethylene glycol oxide, fumaric acid, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate, Icing Sugar, Polysorbate pulverized 80 mesh sieves respectively;
2) extraction of raw material of Chinese medicine pharmaceutically active ingredient:
1. by mass concentration be 50% ethanol add in Chinese medicine extracting tank, ethanol consumption is 10 times of raw material of Chinese medicine parts by weight, open and stir, by Rhizoma Corydalis, Radix Tricyrtidis pilosae, Radix Sophorae Flavescentis, catechu adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 75 ~ 80 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution A to 1/3rd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 40 ~ 45 DEG C,
2. water is added in Chinese medicine extracting tank, the consumption of water is 8 times of raw material of Chinese medicine parts by weight, open and stir, by Herba Passiflorae Wilsonii, Radix Silenes Tenuis, Cortex Dictamni, Radix Polygoni Multiflori, Folium Artemisiae Argyi adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 95 ~ 100 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution B to 1/2nd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 50 ~ 55 DEG C,
3) granulate:
1. by miconazole nitrate, step 2) gained concentrated solution A, polyethylene glycol oxide, fumaric acid, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule C;
2. by step 2) gained concentrated solution B, sodium alginate, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule D;
4) tabletting, by step 3) gained granule C, granule D mix homogeneously, use high speed tablet press tabletting, specification is every sheet containing miconazole nitrate 20 ~ 40mg.
Treat colpitic curative effect to improve miconazole nitrate, improve the compliance of patient, the present invention is screened Chinese medicine crude drug, pharmaceutic adjuvant and preparation technology by a large amount of screening test, selected raw material of Chinese medicine medicine:
Rhizoma Corydalis: property is pungent, temperature, nontoxic.Start with, meridian of Foot-TAI YIN, cure mainly: removing blood stasis, married woman's menoxenia, lumps in abdomen, metrorrhagia drench dew, puerperal all disorders of blood, blood transport, sudden and violent blood rushes to, because of damage hematochezia.
Radix Tricyrtidis pilosae: control thirsty fidgets due to deficiency, manic uneasiness, impairment caused by overstrain.
Radix Sophorae Flavescentis: bitter in the mouth, cold in nature; Return liver, kidney, large intestine, small intestinal, bladder, heart channel.Heat clearing and damp drying; Wind dispelling insecticide.Main damp-heat dysentery; Discharging fresh blood stool; Jaundice; Dysuria; Edema; Leukorrhagia; Pudendal pruritus; Scabies; Leprosy; Skin pruritus; Noxious dampness skin infection.
Catechu: this product bitterness convergence, kind removing dampness sore, putrefaction-removing granulation-promoting, thus be usually used in that skin infection is not held back, the card such as eczema flowing water and women's leukorrhagia.
Herba Passiflorae Wilsonii: warm in nature, micro-hardship, for relaxing muscles and tendons to promote blood circulation, removing dampness and killing parasites, treating rheumatic arthritis, injury and bone fracture, hepatitis, malaria, ascariasis.
Radix Silenes Tenuis: bitter in the mouth, property are flat.Removing blood stasis, heat clearing away, diuresis.Control dysuria, odynuria, hematuria, amenorrhea is obstructed.
Cortex Dictamni: heat clearing and damp drying; Dispelling wind for relieving itching; Removing toxic substances.
Radix Polygoni Multiflori: slightly warm in nature, bitter in the mouth, sweet, enter liver, kidney, can be used for treatment bleeding not during menses, skin pruritus, removing toxic substances.
Folium Artemisiae Argyi: dispersing cold for relieving pain, warming the meridian for stopping bleeding, external treatment skin pruritus, decortication.
Selected all medicines: miconazole nitrate, Rhizoma Corydalis, Herba Passiflorae Wilsonii, Cortex Dictamni are used for bactericidal antiphlogistic, heat clearing and damp drying, dispelling wind for relieving itching, removing toxic substances for treating colpitic principal agent; Radix Sophorae Flavescentis, catechu, He Shou, Folium Artemisiae Argyi, Radix Silenes Tenuis crow are used for the treatment of bleeding not during menses, skin pruritus, removing the necrotic tissue and promoting granulation, removing toxic substances, are accessory drugs, for auxiliary treatment vaginitis; Radix Tricyrtidis pilosae, Radix Sophorae Flavescentis, Radix Polygoni Multiflori can improve body immunity, under other medicines therapeutical effect, promote that human body better recovers; Radix Silenes Tenuis, Herba Passiflorae Wilsonii, Rhizoma Corydalis have blood circulation promoting and blood stasis dispelling, promote the effect that other medicines absorb.
Selected pharmaceutic adjuvant and technique make effervescent tablet can good effervescent discharge effective ingredient, action temperature and not stimulating.
Beneficial effect of the present invention:
Miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet of the present invention is Chinese medicine and western medicine mixture, and effectively overcome the defect that miconazole nitrate only has simple bactericidal antiphlogistic, all medicine synergistic action effects are good.Miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet of the present invention overcomes washing liquid and carries the defect storing inconvenience, adopt hydrophilic gel slow-release material as pharmaceutic adjuvant, hydrophilic gel slow-release material is external because its high thickness and bioadhesion effect make medicine not easily get rid of, can the interval of prolong drug action time and administration, be conducive to improving drug bioavailability; This tablet is placed in after in body, and chance body fluid can absorb water rapidly and gelation occurs and be distributed in mucous membrane surface rapidly under gas-producing disintegrant promotes.The effervescent effect of effervescent tablet is kept after the selection of this other pharmaceutic adjuvant of vagina effervescence is conducive to tabletting and tabletting.The present invention adopts local external use to treat colpitic method, directly acts on affected part, and rapid-action, good effect is easy to use, can increase the contact surface of medicine and human body, improve drug effect after effervescent tablet foaming.Employing anti-inflammation, granulation promoting poison holding, method that is bitterly antipruritic, heat-clearing and toxic substances removing of dispelling, treating both the principal and secondary aspects of a disease vaginitis, rapid recovery patient pain, pruritis, make vaginal secretions recover normal, improve the compliance of patient.Miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet of the present invention, use safety, without drug dependence, toxic and side effects is little, cheap.
Detailed description of the invention
According to following embodiment, the present invention may be better understood.But those skilled in the art will readily understand, concrete material proportion, process conditions and result thereof described by embodiment only should can not limit the present invention described in detail in claims yet for illustration of the present invention.
Embodiment 1
A kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 1 part, Rhizoma Corydalis 20 parts, Radix Tricyrtidis pilosae 15 parts, Radix Sophorae Flavescentis 40 parts, 35 parts, catechu, Herba Passiflorae Wilsonii 60 parts, Radix Silenes Tenuis 30 parts, Cortex Dictamni 30 parts, Radix Polygoni Multiflori 35 parts, Folium Artemisiae Argyi 50 parts, sodium alginate 5 parts, polyethylene glycol oxide 5 parts, fumaric acid 5 parts, sodium carbonate 3 parts, sodium bicarbonate 4 parts, sodium lauryl sulphate 1 part, Icing Sugar 5 parts, Polysorbate 0.5 part.
A preparation method for miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, comprises the following steps:
1) get the raw materials ready, get the raw materials ready according to described component and parts by weight, miconazole nitrate pulverized 120 mesh sieves, and sodium alginate, polyethylene glycol oxide, fumaric acid, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate, Icing Sugar, Polysorbate pulverized 80 mesh sieves respectively;
2) extraction of raw material of Chinese medicine pharmaceutically active ingredient:
1. by mass concentration be 50% ethanol add in Chinese medicine extracting tank, ethanol consumption is 10 times of raw material of Chinese medicine parts by weight, open and stir, by Rhizoma Corydalis, Radix Tricyrtidis pilosae, Radix Sophorae Flavescentis, catechu adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 75 ~ 80 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution A to 1/3rd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 40 ~ 45 DEG C,
2. water is added in Chinese medicine extracting tank, the consumption of water is 8 times of raw material of Chinese medicine parts by weight, open and stir, by Herba Passiflorae Wilsonii, Radix Silenes Tenuis, Cortex Dictamni, Radix Polygoni Multiflori, Folium Artemisiae Argyi adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 95 ~ 100 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution B to 1/2nd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 50 ~ 55 DEG C,
3) granulate:
1. by miconazole nitrate, step 2) gained concentrated solution A, polyethylene glycol oxide, fumaric acid, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule C;
2. by step 2) gained concentrated solution B, sodium alginate, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule D;
4) tabletting, by step 3) gained granule C, granule D mix homogeneously, use high speed tablet press tabletting, specification is every sheet containing miconazole nitrate 20mg.
Usage and dosage: clean pudendum before use, is placed in vagina deep with the finger wearing sterilization fingerstall by this effervescent tablet, is used in conjunction 7 days or follows the doctor's advice, 1 time every night, each 1 ~ 2, or following the doctor's advice.
Embodiment 2
A kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 2 parts, Rhizoma Corydalis 22 parts, Radix Tricyrtidis pilosae 18 parts, Radix Sophorae Flavescentis 43 parts, 37 parts, catechu, Herba Passiflorae Wilsonii 65 parts, Radix Silenes Tenuis 35 parts, Cortex Dictamni 38 parts, Radix Polygoni Multiflori 36 parts, Folium Artemisiae Argyi 57 parts, sodium alginate 7 parts, polyethylene glycol oxide 6 parts, fumaric acid 8 parts, sodium carbonate 4 parts, sodium bicarbonate 6 parts, sodium lauryl sulphate 1.5 parts, Icing Sugar 9 parts, Polysorbate 0.7 part.
A preparation method for miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, comprises the following steps:
1) get the raw materials ready, get the raw materials ready according to described component and parts by weight, miconazole nitrate pulverized 120 mesh sieves, and sodium alginate, polyethylene glycol oxide, fumaric acid, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate, Icing Sugar, Polysorbate pulverized 80 mesh sieves respectively;
2) extraction of raw material of Chinese medicine pharmaceutically active ingredient:
1. by mass concentration be 50% ethanol add in Chinese medicine extracting tank, ethanol consumption is 10 times of raw material of Chinese medicine parts by weight, open and stir, by Rhizoma Corydalis, Radix Tricyrtidis pilosae, Radix Sophorae Flavescentis, catechu adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 75 ~ 80 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution A to 1/3rd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 40 ~ 45 DEG C,
2. water is added in Chinese medicine extracting tank, the consumption of water is 8 times of raw material of Chinese medicine parts by weight, open and stir, by Herba Passiflorae Wilsonii, Radix Silenes Tenuis, Cortex Dictamni, Radix Polygoni Multiflori, Folium Artemisiae Argyi adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 95 ~ 100 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution B to 1/2nd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 50 ~ 55 DEG C,
3) granulate:
1. by miconazole nitrate, step 2) gained concentrated solution A, polyethylene glycol oxide, fumaric acid, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule C;
2. by step 2) gained concentrated solution B, sodium alginate, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule D;
4) tabletting, by step 3) gained granule C, granule D mix homogeneously, use high speed tablet press tabletting, specification is every sheet containing miconazole nitrate 30mg.
Usage and dosage: clean pudendum before use, is placed in vagina deep with the finger wearing sterilization fingerstall by this effervescent tablet, is used in conjunction 7 days or follows the doctor's advice, 1 time every night, each 1 ~ 2, or following the doctor's advice.
Embodiment 3
A kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 3 parts, Rhizoma Corydalis 25 parts, Radix Tricyrtidis pilosae 20 parts, Radix Sophorae Flavescentis 45 parts, 40 parts, catechu, Herba Passiflorae Wilsonii 70 parts, Radix Silenes Tenuis 40 parts, Cortex Dictamni 40 parts, Radix Polygoni Multiflori 40 parts, Folium Artemisiae Argyi 60 parts, sodium alginate 10 parts, polyethylene glycol oxide 10 parts, fumaric acid 10 parts, sodium carbonate 5 parts, sodium bicarbonate 10 parts, sodium lauryl sulphate 2 parts, Icing Sugar 10 parts, Polysorbate 1 part.
A preparation method for miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, comprises the following steps:
1) get the raw materials ready, get the raw materials ready according to described component and parts by weight, miconazole nitrate pulverized 120 mesh sieves, and sodium alginate, polyethylene glycol oxide, fumaric acid, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate, Icing Sugar, Polysorbate pulverized 80 mesh sieves respectively;
2) extraction of raw material of Chinese medicine pharmaceutically active ingredient:
1. by mass concentration be 50% ethanol add in Chinese medicine extracting tank, ethanol consumption is 10 times of raw material of Chinese medicine parts by weight, open and stir, by Rhizoma Corydalis, Radix Tricyrtidis pilosae, Radix Sophorae Flavescentis, catechu adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 75 ~ 80 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution A to 1/3rd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 40 ~ 45 DEG C,
2. water is added in Chinese medicine extracting tank, the consumption of water is 8 times of raw material of Chinese medicine parts by weight, open and stir, by Herba Passiflorae Wilsonii, Radix Silenes Tenuis, Cortex Dictamni, Radix Polygoni Multiflori, Folium Artemisiae Argyi adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 95 ~ 100 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution B to 1/2nd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 50 ~ 55 DEG C,
3) granulate:
1. by miconazole nitrate, step 2) gained concentrated solution A, polyethylene glycol oxide, fumaric acid, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule C;
2. by step 2) gained concentrated solution B, sodium alginate, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule D;
4) tabletting, by step 3) gained granule C, granule D mix homogeneously, use high speed tablet press tabletting, specification is every sheet containing miconazole nitrate 40mg.
Usage and dosage: clean pudendum before use, is placed in vagina deep with the finger wearing sterilization fingerstall by this effervescent tablet, is used in conjunction 7 days or follows the doctor's advice, 1 time every night, each 1, or following the doctor's advice.
Embodiment 4 checks disintegration
Inspection method: get 1, put in 250ml beaker, fill 200ml water in beaker, water temperature is 37 ± 1 DEG C, has numerous air-bubble to release, and when the gas around tablet or fragment stops overflowing, tablet all dissolves, left without the granule assembled.Check 6 as stated above, each all should disintegrate in 5min, can not disintegrate completely if any 1, separately should get 6 retrials, all should conform with the regulations.
Vagina slowly-releasing effervescent tablet of the present invention meets the regulation of whole disintegrate in 5 minutes after testing.
The inspection of embodiment 5 gas release
Inspection method: 10,20ml tool scale test tube, internal diameter 1.5cm, precision adds water 3ml, and drop into this film after 5 minutes in 37 ± 1 DEG C of water-baths, after 30min, maximum gas release on average should be not less than 13.0ml, and be less than 10.0ml must not more than 2.
After vagina slowly-releasing effervescent tablet of the present invention meets 30min after testing, maximum gas release on average should be not less than the regulation of 13.0ml.
The inspection of embodiment 6 bacteriostatic test
Adopt effervescence tablet of miconazole nitrate for vagina to contrast, specification is 20mg/ sheet; Embodiment 1 gained miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet is that experimental group carries out antibacterial inspection.
The preparation of culture medium: take in the water-soluble 800mL of beef extract 5g, adds peptone 10g and dissolves, and adds casein 34g and dissolves, then adds NaCl5g dissolving, is adjusted to pH7.6 ~ 7.8, is diluted to 1000mL.Add agar powder 18g, autoclaving 15min, when being cooled to 40 DEG C ~ 50 DEG C, a kind of rhyme scheme in Chinese operas serving as the prelude to a complete score for voices, solidifies, and the 4 DEG C of refrigerators placing no bacteria pollution are for subsequent use.
Strain is: candidiasis
Matched group antibacterial liquid is prepared: be dissolved in respectively in 10ml sterile deionized water by 3 effervescence tablet of miconazole nitrate for vagina, diluted respectively by liquor strength, with stock solution than being 1:2,1:4,1:8,1:16,1:32.
Experimental group antibacterial liquid is prepared: be dissolved in respectively in 10ml sterile deionized water by 3 miconazole nitrate compound recipe vagina slowly-releasing effervescent tablets, diluted respectively by liquor strength, with stock solution than being 1:2,1:4,1:8,1:16,1:32.
Antibacterial result is as follows:
Conclusion: miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet of the present invention has better bactericidal effect.
The inspection of embodiment 7 Transdermal absorption
Reference substance is effervescence tablet of miconazole nitrate for vagina, and specification is 20mg/ sheet; Trial target is that specification is: containing miconazole nitrate 20mg/ sheet with embodiment 1 obtained miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet.Respectively 6 control samples, 6 test specimens are dissolved with pure water.
This inspection method skin is: mouse skin after process
This inspection method instrument is: skin permeation test in vitro instrument does skin permeation test in vitro, measures agent permeates therethrough amount by HPLC.
Test method: " Chinese Pharmacopoeia " 2010 version (two) about transdermal patch drug release determination method, all in 0.5,1,2,4 samplings.
Result of the test:
As can be seen from the test results, miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet Transdermal absorption better effects if of the present invention, during test specimen 4h, Transdermal absorption is substantially complete.
Above embodiment is only for illustrating technical conceive of the present invention and feature; its object is to allow person skilled in the art understand content of the present invention and to be implemented; can not limit the scope of the invention with this; all equivalences done according to spirit of the present invention change or modify, and all should be encompassed in protection scope of the present invention.
Claims (5)
1. a miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, it is characterized in that, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 1 ~ 3 part, Rhizoma Corydalis 20 ~ 25 parts, Radix Tricyrtidis pilosae 15 ~ 20 parts, Radix Sophorae Flavescentis 40 ~ 45 parts, 35 ~ 40 parts, catechu, Herba Passiflorae Wilsonii 60 ~ 70 parts, Radix Silenes Tenuis 30 ~ 40 parts, Cortex Dictamni 30 ~ 40 parts, Radix Polygoni Multiflori 35 ~ 40 parts, Folium Artemisiae Argyi 50 ~ 60 parts, sodium alginate 5 ~ 10 parts, polyethylene glycol oxide 5 ~ 10 parts, fumaric acid 5 ~ 10 parts, sodium carbonate 3 ~ 5 parts, sodium bicarbonate 4 ~ 10 parts, sodium lauryl sulphate 1 ~ 2 part, Icing Sugar 5 ~ 10 parts, Polysorbate 0.5 ~ 1 part.
2. a kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet according to claim 1, it is characterized in that, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 1 part, Rhizoma Corydalis 20 parts, Radix Tricyrtidis pilosae 15 parts, Radix Sophorae Flavescentis 40 parts, 35 parts, catechu, Herba Passiflorae Wilsonii 60 parts, Radix Silenes Tenuis 30 parts, Cortex Dictamni 30 parts, Radix Polygoni Multiflori 35 parts, Folium Artemisiae Argyi 50 parts, sodium alginate 5 parts, polyethylene glycol oxide 5 parts, fumaric acid 5 parts, sodium carbonate 3 parts, sodium bicarbonate 4 parts, sodium lauryl sulphate 1 part, Icing Sugar 5 parts, Polysorbate 0.5 part.
3. a kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet according to claim 1, it is characterized in that, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 2 parts, Rhizoma Corydalis 22 parts, Radix Tricyrtidis pilosae 18 parts, Radix Sophorae Flavescentis 43 parts, 37 parts, catechu, Herba Passiflorae Wilsonii 65 parts, Radix Silenes Tenuis 35 parts, Cortex Dictamni 38 parts, Radix Polygoni Multiflori 36 parts, Folium Artemisiae Argyi 57 parts, sodium alginate 7 parts, polyethylene glycol oxide 6 parts, fumaric acid 8 parts, sodium carbonate 4 parts, sodium bicarbonate 6 parts, sodium lauryl sulphate 1.5 parts, Icing Sugar 9 parts, Polysorbate 0.7 part.
4. a kind of miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet according to claim 1, it is characterized in that, component and the parts by weight of this effervescent tablet comprise: miconazole nitrate 3 parts, Rhizoma Corydalis 25 parts, Radix Tricyrtidis pilosae 20 parts, Radix Sophorae Flavescentis 45 parts, 40 parts, catechu, Herba Passiflorae Wilsonii 70 parts, Radix Silenes Tenuis 40 parts, Cortex Dictamni 40 parts, Radix Polygoni Multiflori 40 parts, Folium Artemisiae Argyi 60 parts, sodium alginate 10 parts, polyethylene glycol oxide 10 parts, fumaric acid 10 parts, sodium carbonate 5 parts, sodium bicarbonate 10 parts, sodium lauryl sulphate 2 parts, Icing Sugar 10 parts, Polysorbate 1 part.
5. a preparation method for miconazole nitrate compound recipe vagina slowly-releasing effervescent tablet, is characterized in that, comprise the following steps:
1) get the raw materials ready, get the raw materials ready according to the component described in any one of Claims 1 to 4 and parts by weight, miconazole nitrate pulverized 120 mesh sieves, and sodium alginate, polyethylene glycol oxide, fumaric acid, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate, Icing Sugar, Polysorbate pulverized 80 mesh sieves respectively;
2) extraction of raw material of Chinese medicine pharmaceutically active ingredient:
1. by mass concentration be 50% ethanol add in Chinese medicine extracting tank, ethanol consumption is 10 times of raw material of Chinese medicine parts by weight, open and stir, by Rhizoma Corydalis, Radix Tricyrtidis pilosae, Radix Sophorae Flavescentis, catechu adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 75 ~ 80 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution A to 1/3rd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 40 ~ 45 DEG C,
2. water is added in Chinese medicine extracting tank, the consumption of water is 8 times of raw material of Chinese medicine parts by weight, open and stir, by Herba Passiflorae Wilsonii, Radix Silenes Tenuis, Cortex Dictamni, Radix Polygoni Multiflori, Folium Artemisiae Argyi adds in Chinese medicine extracting tank, temperature of charge in Chinese medicine extracting tank is warming up to 95 ~ 100 DEG C of constant temperature and extracts 30min, 100 orders cross leaching filtrate, filtering residue returns in Chinese medicine extracting tank and repeats to extract once, 100 orders cross leaching filtrate, merge twice gained filtrate, vacuum concentration obtains concentrated solution B to 1/2nd of filtrate volume, vacuum concentration condition is: pressure-0.07 ~-0.08Mpa, temperature 50 ~ 55 DEG C,
3) granulate:
1. by miconazole nitrate, step 2) gained concentrated solution A, polyethylene glycol oxide, fumaric acid, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule C;
2. by step 2) gained concentrated solution B, sodium alginate, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate parts by weight 1/2nd, 1/2nd of Icing Sugar parts by weight, 1/2nd mix homogeneously of Polysorbate parts by weight, wet granulation, and granulate obtains granule D;
4) tabletting, by step 3) gained granule C, granule D mix homogeneously, use high speed tablet press tabletting, specification is every sheet containing miconazole nitrate 20 ~ 40mg.
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