CN1304002C - Vaginal effervescence tablet of secnidazole and its preparation - Google Patents
Vaginal effervescence tablet of secnidazole and its preparation Download PDFInfo
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- CN1304002C CN1304002C CNB2003101090115A CN200310109011A CN1304002C CN 1304002 C CN1304002 C CN 1304002C CN B2003101090115 A CNB2003101090115 A CN B2003101090115A CN 200310109011 A CN200310109011 A CN 200310109011A CN 1304002 C CN1304002 C CN 1304002C
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- secnidazole
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- KPQZUUQMTUIKBP-UHFFFAOYSA-N 1-(2-methyl-5-nitro-1-imidazolyl)-2-propanol Chemical compound CC(O)CN1C(C)=NC=C1[N+]([O-])=O KPQZUUQMTUIKBP-UHFFFAOYSA-N 0.000 title claims abstract description 72
- 229960004076 secnidazole Drugs 0.000 title claims abstract description 71
- 238000002360 preparation method Methods 0.000 title abstract description 3
- 210000001215 vagina Anatomy 0.000 claims abstract description 50
- 239000007938 effervescent tablet Substances 0.000 claims abstract description 24
- 239000002671 adjuvant Substances 0.000 claims abstract description 16
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 10
- 238000004519 manufacturing process Methods 0.000 claims abstract description 10
- 238000002156 mixing Methods 0.000 claims abstract description 3
- 239000011230 binding agent Substances 0.000 claims description 22
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 16
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 12
- 229920000053 polysorbate 80 Polymers 0.000 claims description 12
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 12
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 12
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- 239000000945 filler Substances 0.000 claims description 8
- 235000019359 magnesium stearate Nutrition 0.000 claims description 8
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 239000011975 tartaric acid Substances 0.000 claims description 6
- 235000002906 tartaric acid Nutrition 0.000 claims description 6
- 239000000080 wetting agent Substances 0.000 claims description 6
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 5
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 5
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 5
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 5
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 4
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 4
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- 239000000203 mixture Substances 0.000 claims description 4
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- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 2
- 229920001353 Dextrin Polymers 0.000 claims description 2
- 239000004375 Dextrin Substances 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
- 229930195725 Mannitol Natural products 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- 230000001476 alcoholic effect Effects 0.000 claims description 2
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 claims description 2
- 239000004327 boric acid Substances 0.000 claims description 2
- 235000010338 boric acid Nutrition 0.000 claims description 2
- 235000015165 citric acid Nutrition 0.000 claims description 2
- 229960000935 dehydrated alcohol Drugs 0.000 claims description 2
- 235000019425 dextrin Nutrition 0.000 claims description 2
- 229960004756 ethanol Drugs 0.000 claims description 2
- 239000001530 fumaric acid Substances 0.000 claims description 2
- 235000011087 fumaric acid Nutrition 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 239000000594 mannitol Substances 0.000 claims description 2
- 235000010355 mannitol Nutrition 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 238000012545 processing Methods 0.000 claims description 2
- 239000000741 silica gel Substances 0.000 claims description 2
- 229910002027 silica gel Inorganic materials 0.000 claims description 2
- 239000007779 soft material Substances 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 2
- 238000005303 weighing Methods 0.000 claims description 2
- 239000003814 drug Substances 0.000 abstract description 26
- 230000000694 effects Effects 0.000 abstract description 19
- 229940079593 drug Drugs 0.000 abstract description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 7
- 201000010099 disease Diseases 0.000 abstract description 6
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 abstract description 4
- 238000005516 engineering process Methods 0.000 abstract description 4
- 208000015181 infectious disease Diseases 0.000 abstract description 4
- 241000894006 Bacteria Species 0.000 abstract description 3
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- 239000001569 carbon dioxide Substances 0.000 abstract description 2
- 229910002092 carbon dioxide Inorganic materials 0.000 abstract description 2
- 210000003679 cervix uteri Anatomy 0.000 abstract description 2
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- 238000002347 injection Methods 0.000 abstract description 2
- 239000007924 injection Substances 0.000 abstract description 2
- 230000002085 persistent effect Effects 0.000 abstract description 2
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- 238000005469 granulation Methods 0.000 abstract 1
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- 239000000463 material Substances 0.000 abstract 1
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- 239000011122 softwood Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 8
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 8
- 230000028327 secretion Effects 0.000 description 7
- 238000012360 testing method Methods 0.000 description 6
- 208000004926 Bacterial Vaginosis Diseases 0.000 description 5
- HJLSLZFTEKNLFI-UHFFFAOYSA-N Tinidazole Chemical compound CCS(=O)(=O)CCN1C(C)=NC=C1[N+]([O-])=O HJLSLZFTEKNLFI-UHFFFAOYSA-N 0.000 description 5
- 206010047799 Vulvovaginitis trichomonal Diseases 0.000 description 5
- 238000002474 experimental method Methods 0.000 description 5
- 239000002085 irritant Substances 0.000 description 5
- 231100000021 irritant Toxicity 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- 229960005053 tinidazole Drugs 0.000 description 5
- 230000005856 abnormality Effects 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- 229960000282 metronidazole Drugs 0.000 description 4
- VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 description 4
- 210000004877 mucosa Anatomy 0.000 description 4
- 238000011160 research Methods 0.000 description 4
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 4
- 235000017557 sodium bicarbonate Nutrition 0.000 description 4
- 150000004958 5-nitroimidazoles Chemical class 0.000 description 3
- 241000224467 Giardia intestinalis Species 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- 206010030113 Oedema Diseases 0.000 description 3
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 3
- 229940085435 giardia lamblia Drugs 0.000 description 3
- 208000032843 Hemorrhage Diseases 0.000 description 2
- 206010020565 Hyperaemia Diseases 0.000 description 2
- 208000025865 Ulcer Diseases 0.000 description 2
- 206010046914 Vaginal infection Diseases 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 210000003756 cervix mucus Anatomy 0.000 description 2
- 230000007794 irritation Effects 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 231100000397 ulcer Toxicity 0.000 description 2
- 241001148471 unidentified anaerobic bacterium Species 0.000 description 2
- 241000224489 Amoeba Species 0.000 description 1
- 206010001986 Amoebic dysentery Diseases 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 241000606124 Bacteroides fragilis Species 0.000 description 1
- 208000003322 Coinfection Diseases 0.000 description 1
- 241000699798 Cricetulus Species 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 206010052804 Drug tolerance Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- IPWKIXLWTCNBKN-UHFFFAOYSA-N Madelen Chemical compound CC1=NC=C([N+]([O-])=O)N1CC(O)CCl IPWKIXLWTCNBKN-UHFFFAOYSA-N 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 239000004141 Sodium laurylsulphate Substances 0.000 description 1
- 208000007074 Trichomonas Vaginitis Diseases 0.000 description 1
- 208000025206 Trichomonas vaginitis urogenital infection Diseases 0.000 description 1
- 240000008042 Zea mays Species 0.000 description 1
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 description 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- 238000005299 abrasion Methods 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000001572 anti-trichomonad Effects 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
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- 239000002775 capsule Substances 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 235000005822 corn Nutrition 0.000 description 1
- 230000013872 defecation Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 230000003628 erosive effect Effects 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 238000005187 foaming Methods 0.000 description 1
- 201000006592 giardiasis Diseases 0.000 description 1
- 210000004969 inflammatory cell Anatomy 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 238000003771 laboratory diagnosis Methods 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 230000017074 necrotic cell death Effects 0.000 description 1
- 229960002313 ornidazole Drugs 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- FGIUAXJPYTZDNR-UHFFFAOYSA-N potassium nitrate Chemical compound [K+].[O-][N+]([O-])=O FGIUAXJPYTZDNR-UHFFFAOYSA-N 0.000 description 1
- 239000002423 protozoacide Substances 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a secnidazole vagina effervescent tablet and a production method thereof, which belong to the technical field of a western medicine preparation. The secnidazole vagina effervescent tablet contains 25 to 60 wt% of secnidazole used as an active ingredient and an effervescent tablet used as an adjuvant material. The production method comprises technology steps, such as pulverization, weigh according to a prescription, softwood manufacture by an adhesive agent, granulation, drying, mixing, tabletting, etc. The secnidazole vagina effervescent tablet can greatly improve the specificity of medication, and compared with the therapeutic effect of other kinds of medicine for treating congenerous diseases, the therapeutic effect of the secnidazole vagina effervescent tablet are greatly improved; compared with the medical effect of the oral administration medicine and the injection of congenerous medicine, the secnidazole vagina effervescent tablet has maximum medical effect and improves the effects of antibiosis and antiphlogosis. After water is absorbed by the vagina, a disintegrating agent used by the secnidazole vagina effervescent tablet is rapidly foamed and disintegrated to discharge a large number of carbon dioxide air bubbles; particularly, the superfine and persistent air bubbles can generate in the micro physiological environment of the vagina to effectively enlarge the contact area of the medicine, and the medicine can also contact the position, such as the cervix, etc., which is infected by infectious bacteria. Thus, the present invention improves the concentration of local medication, and fully perform the functions of the antibiosis and the antiphlogosis of the medicine.
Description
Technical field
The invention belongs to the Western medicine preparation technical field, be specifically related to a kind of secnidazole vagina effervescence and production method thereof.
Background technology
Just find that as far back as the fifties 5-nitroimidazoles medicine has protozoacide, antibacterial activity, and successfully be applied to protozoon and multiple anaerobic Gram-positive and negative bacterial infections such as clinical treatment infusorian, ameba.Secnidazole belongs to the 5-nitro imidazole derivatives, and its chemical name is: 1-(2-hydroxypropyl)-2-methyl-5-nitro imidazoles semihydrate.Secnidazole is mainly used in diseases such as infection, especially trichomonal vaginitis that treatment multiple anaerobic Gram-positive and negative bacteria and protozoon cause, amoeba histolytica, giardia lamblia clinically.To trichomonal vaginitis and bacillary vagina, enteral, the outer ameba disease of intestinal, the diseases such as diarrhoea that giardiasis causes all have curative effect preferably.Secnidazole is at first developed success the eighties by French rhone-poulenc drugmaker, this medicine anti-trichomonal, anti-ameba and antibiotic evident in efficacy, clinical research shows: infect ameba with cricetulus auratus and cause liver and intestinal amebiasis, the anti-ameba effect of secnidazole is better than tinidazole and metronidazole; Its anaerobe resistant bacteroides fragilis effect is better than tinidazole and ornidazole.The characteristics that are even more important are that secnidazole has long elimination half-life (t
1/2 β17-29 hour), in similar medicine action time longer, and untoward reaction is little.When the clinical treatment trichomonal vaginitis, the disposable secnidazole 2g that gives, its cure rate reaches 80-100%, curative effect to repeatedly use metronidazole or tinidazole in treatment effect similar.Though the domestic developmental research that has just begun to carry out the secnidazole medicine, but its mechanism of action and pharmacological action have been existing known technology, main dosage form has tablet, capsule and granule, and its clinical suitable disease is more extensive, and therapeutic effect also is better than similar 5-nitroimidazoles medicine.Do not see as yet in the world at present that technology report and product that the secnidazole effervescent tablet that is exclusively used in vagina is arranged come out.
Summary of the invention
The object of the present invention is to provide a kind of good effect, side effect low, safe in utilization, help improving the medication specificity and can more preferably bring into play the secnidazole vagina effervescence of curative effect of medication and the technical scheme of production method thereof.
The secnidazole vagina effervescence is characterized in that this effervescent tablet contains active component secnidazole and effervescent tablet adjuvant, and wherein secnidazole accounts for the 25-60% of its gross weight.The content that present patent application relates to is weight percentage.
Described secnidazole vagina effervescence is characterized in that described effervescent tablet adjuvant is: medicinal disintegrating agent, binding agent, lubricant, wetting agent, filler.Described disintegrating agent is one or more in tartaric acid, boric acid, citric acid, fumaric acid, sodium bicarbonate, the low-substituted hydroxypropyl cellulose; Described binding agent is one or more the alcoholic solution in Tween 80, polyvinylpyrrolidone, the low viscosity hypromellose, and content of effective accounts for the 10-20% of binding agent gross weight in its binding agent, preferred 15-20%; Described lubricant is magnesium stearate and/or ethanol; Described wetting agent is one or more in magnesium stearate, micropowder silica gel, the Polyethylene Glycol; Described filler is one or more in starch, dextrin, Icing Sugar, lactose, microcrystalline Cellulose, calcium sulfate, the mannitol.
Described secnidazole vagina effervescence is characterized in that secnidazole accounts for the 30-55% of its gross weight; The ratio that described disintegrating agent, binding agent, lubricant, wetting agent account for its gross weight is respectively: 12-30%, 12-25%, 0.2-1%, 0.2-1%, surplus is a filler.
Described secnidazole vagina effervescence is characterized in that secnidazole accounts for the 40-50% of its gross weight; The ratio that described disintegrating agent, binding agent, lubricant, wetting agent account for its gross weight is respectively: 15-25%, 15-20%, 0.5-1%, 0.5-1%, surplus is a filler.
The production method of above-mentioned secnidazole vagina effervescence comprises following processing step:
(a) with secnidazole, effervescent tablet adjuvant pulverize separately, it is standby to cross 100 mesh sieves;
(b) take by weighing secnidazole, effervescent tablet adjuvant by proportional quantity;
(c) with the effervescent tablet adjuvant: one or more in Tween 80, polyvinylpyrrolidone, the low viscosity hypromellose are dissolved in the dehydrated alcohol, mix homogeneously, make binding agent, wherein the binding agent content of effective accounts for the 10-20% of binding agent gross weight, preferred 15-20%;
(d) with secnidazole and effervescent tablet adjuvant: medicinal disintegrating agent, filler mixing, cross 60 mesh sieves, with binding agent system soft material, 20 orders are granulated, and 50-55 ℃ was toasted 1-3 hour;
(e) with 20 mesh sieve granulate, add remaining effervescent tablet adjuvant, mix homogeneously, tabletting makes.
Secnidazole vagina effervescence of the present invention adopts the reasonable compatibility of active component secnidazole and effervescent tablet adjuvant, can improve the specificity of medication greatly, the curative effect of medication of other treatment congenerous disease has large increase relatively, compare with oral medicine, the injection of similar medicine, its drug effect is also brought into play to greatest extent, has improved local antibacterial antiinflammatory effect.The disintegrating agent that is adopted, in the foaming disintegrate rapidly of vagina suction back, emit the great amount of carbon dioxide bubble, particularly in the micro-physiological environment of vagina, produce the contact area that fine and persistent bubble can enlarge medicine effectively, comprise that infectious bacteria such as cervix uteri can arrive part, improve the concentration of local application, give full play to the effect of the anti-inflammation of medicine.
The specific embodiment
Prescription 1: secnidazole 500 grams, tartaric acid 50-150 gram, sodium bicarbonate 80-120 gram, microcrystalline Cellulose 45-60 gram, low-substituted hydroxypropyl cellulose 15-25 gram, magnesium stearate 8-12 gram, Tween 80 15-20 gram, polyvinylpyrrolidone 1-5 gram, Tween 80, polyvinylpyrrolidone 150ml anhydrous alcohol solution.
Prescription 2: secnidazole 500 grams, tartaric acid 100 grams, sodium bicarbonate 100 grams, microcrystalline Cellulose 50 grams, low-substituted hydroxypropyl cellulose 20 grams, magnesium stearate 10 grams, Tween 80 18 grams, polyvinylpyrrolidone 3 grams, Tween 80, polyvinylpyrrolidone 150ml anhydrous alcohol solution.
Prescription 3: secnidazole 500 grams, tartaric acid 140 grams, sodium bicarbonate 120 grams, microcrystalline Cellulose 50 grams, low-substituted hydroxypropyl cellulose 20 grams, magnesium stearate 10 grams, Tween 80 12 grams, polyvinylpyrrolidone 2 grams, Tween 80, polyvinylpyrrolidone 150ml anhydrous alcohol solution.
Prescription 4: secnidazole 500 grams, tartaric acid 150 grams, sodium bicarbonate 120 grams, sodium lauryl sulphate 10 grams, low-substituted hydroxypropyl cellulose 20 grams, magnesium stearate 10 grams, Tween 80 12 grams, polyvinylpyrrolidone 5 grams, Tween 80, polyvinylpyrrolidone 150ml anhydrous alcohol solution.
By above prescription, concrete production method as previously mentioned.
The irritant experiment of secnidazole vagina effervescence: single and multiple dosing irritant experiment
Be subjected to the reagent thing: secnidazole vagina effervescence, every 500mg; Animal: white hair rabbit, female, body weight 2-2.5kg; Administering mode and dosage: to the rabbit vagina administration, at every turn by rabbit body weight 250mg/kg administration; Standards of grading: see Table 1.
Table 1 is a local mucous membrane irritant reaction grade scale
| Form changes | Rank scores |
| (1) do not have change or nothing and obviously change (2) mild hyperaemia, a small amount of secretions (3) moderate hyperemia, secretions more (4) severe blood stasis, edema, secretions is a lot, mucosal degeneration | 0 1 2 3 |
Annotate: mean scores is nonirritant at 0-0.4; Mean scores is slight zest at 0.41-1.5; Mean scores is the moderate zest at 1.51-2.5; Mean scores is the severe zest＞2.5.
Test result and conclusion: single-dose irritant experiment result: respectively organized the no abnormal secretions of rabbit vagina mouth, the general situation of whole body (appetite, spirit, defecation etc.) no abnormality seen after the single-dose drug withdrawal in 24 hours; 24 hours vaginal mucosa perusal after the single-dose drug withdrawal, each organizes vagina no abnormality seen secretions, hemorrhage, edema, ulcer, rotten to the corn downright bad.Appraisal result sees Table 2.
Table 2 single-dose irritation test reaction appraisal result
| Group | Animal number | Average mark | |||||
| 1 | 2 | 3 | 4 | 5 | 6 | ||
| Blank group secnidazole vagina effervescence | 0 0 | 0 0 | 0 0 | 0 0 | 0 0 | 0 0 | 0 0 |
Conclusion: secnidazole vagina effervescence single-dose belongs to nonirritant to vaginal mucosa.
Multiple dosing irritant experiment result: each organizes the general situation no abnormality seen of rabbit whole body, 24 hours vaginal mucosa perusal after successive administration 1 all drug withdrawals: blank group group rabbit no abnormality seen; The 3rd day to the 7th day rabbit vagina of secnidazole vagina effervescence group rabbit vagina has a small amount of white secretions, but do not see hemorrhage, edema, ulcer, erosion, necrosis and abnormal secretion thing.Appraisal result sees Table 2.
Many times administration irritation test reactions of table 2 appraisal result
| Group | Animal number | Average mark | |||||
| 7 | 8 | 9 | 10 | 11 | 12 | ||
| Blank group secnidazole vagina effervescence | 0 1 | 0 2 | 0 1 | 0 1 | 0 1 | 0 2 | 0 1.3 |
Conclusion: secnidazole vagina effervescence multiple dosing belongs to slight zest to vaginal mucosa, infers relevant with mechanical abrasion after the administration.
Secnidazole vagina effervescence pharmacodynamics and clinical research testing data: the external of secnidazole vagina effervescence is used for the treatment of the infection that trichomonal vaginitis, vagina giardia lamblia and other vagina are responsive facultative and anaerobic bacteria causes.Adopt the secnidazole vagina effervescence to give 500mg, vagina administration, once a day, one week of logotype.In addition, in conjunction with oral secnidazole treatment, the curative effect multiplication treats the disposable 2g single oral dose that gives of secnidazole in conjunction with secnidazole vagina effervescence external curing better effects if, can cure the colpitis that sensitive bacterial causes substantially.
1. the treatment of trichomonal vaginitis: the effect that secnidazole treatment trichomonas vaginitis infects is directly proportional with dosage, disposable single dose 2g secnidazole is treated, found to cure the patient of 92.6-95.6% in 2-3 days, and observed after 20 days, 100% patient can obtain radical cure; Studies confirm that through clinical treatment one group of patient gives to treat secnidazole 500mg/ day 4 days, make secnidazole use total amount to reach 2g, its cure rate is 97.5%; Another is organized disposable single dose and gives secnidazole 2g treatment, and its cure rate reaches 100%; After observing 5 days, its curative effect has not been seen notable difference.Also confirm through clinical treatment research, morning and medication in evening, as if curative effect is constant, still, finds that also the medication in evening more is easy to generate Drug tolerance than the medication in morning in this experiment.
Secnidazole oral administration and two administrations of vagina are compared discover that disposable oral secnidazole 2g amounts to 5 days with 500mg transvaginal administration once a day separately, its curative effect simultaneously oral with vagina topical administration curative effect for poor.
2. the treatment of bacterial vaginitis: the common characteristic of bacterial vaginitis disease is with multiple microorganism mixed infection, increases to feature as the quantity with vagina giardia lamblia stiles, anaerobic bacteria flora.The incidence rate of bacillary vaginal infection about 5-45%, is decided with the different women colonies that are studied usually.Usually at first see white, malodorous vagina Excreta clinically, though it may be asymptomatic that many patients are arranged, all patients that include the secnidazole test in all have laboratory diagnosis, and the diagnosis of bacillary vagina comprises the pH value of vaginal secretions greater than 4.5, the existence of inflammatory cell etc.The bacterial vaginitis women who includes random double blind test in accepts plug gram nitre 2g single-dose treatment, and clinical symptoms and sign improvement rate are 90.8% (n=65), and after the tinidazole 2g single-dose treatment, its clinical symptoms and sign improvement rate are 87.5% (n=64).The microbiology cure rate is respectively: secnidazole 81.5%, and tinidazole 78.5%, its criterion is cultivated based on vaginal secretions and is turned out cloudy.
Treat at random in the double-blind trial of bacterial vaginitis at another, the curative effect of secnidazole single dose 2g (n=146) treatment bacterial vaginitis is better than using 7 days (n=147) metronidazole 800mg/ day, adopting the clinical cure rate of secnidazole treatment is 73%, adopting the clinical cure rate of metronidazole treatment is 58%, significant difference (P＜0.01).
Claims (5)
1, secnidazole vagina effervescence, its spy is to contain active component secnidazole and effervescent tablet adjuvant, and wherein secnidazole accounts for the 50-55% of its gross weight;
Described effervescent tablet adjuvant is: medicinal disintegrating agent 15-25%, binding agent 15-20%, lubricant 0.5-1%, wetting agent 0.5-1%, and surplus is a filler;
Described disintegrating agent is one or more in tartaric acid, boric acid, citric acid, fumaric acid, sodium bicarbonate, the low-substituted hydroxypropyl cellulose;
Described binding agent is one or more the alcoholic solution in Tween 80, polyvinylpyrrolidone, the low viscosity hypromellose;
Described lubricant is magnesium stearate and/or ethanol;
Described wetting agent is one or more in magnesium stearate, micropowder silica gel, the Polyethylene Glycol;
Described filler is one or more in starch, dextrin, Icing Sugar, lactose, microcrystalline Cellulose, calcium sulfate, the mannitol.
2, secnidazole vagina effervescence as claimed in claim 1, its spy is that content of effective in the binding agent accounts for the 10-20% of binding agent gross weight.
3, secnidazole vagina effervescence as claimed in claim 1, its spy is that content of effective in the binding agent accounts for the 15-20% of binding agent gross weight.
4, a kind of production method of secnidazole vagina effervescence as claimed in claim 1 comprises following processing step:
(a) with secnidazole, effervescent tablet adjuvant pulverize separately, it is standby to cross 100 mesh sieves;
(b) take by weighing secnidazole, effervescent tablet adjuvant by proportional quantity;
(c) with the effervescent tablet adjuvant: one or more in Tween 80, polyvinylpyrrolidone, the low viscosity hypromellose are dissolved in the dehydrated alcohol, mix homogeneously, make binding agent, wherein the binding agent content of effective accounts for the 10-20% of binding agent gross weight;
(d) with secnidazole and effervescent tablet adjuvant: medicinal disintegrating agent, filler mixing, cross 60 mesh sieves, with binding agent system soft material, 20 orders are granulated, and 50-55 ℃ was toasted 1-3 hour;
(e) with 20 mesh sieve granulate, add remaining effervescent tablet adjuvant, mix homogeneously, tabletting makes.
5, the production method of secnidazole vagina effervescence as claimed in claim 4 is characterized in that the middle binding agent content of effective of step (c) accounts for the 15-20% of binding agent gross weight.
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| CNB2003101090115A CN1304002C (en) | 2003-12-02 | 2003-12-02 | Vaginal effervescence tablet of secnidazole and its preparation |
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| CN101874799B (en) * | 2010-06-13 | 2011-08-31 | 西安万隆制药有限责任公司 | Composition of secnidazole and lactose and preparation method thereof |
| CN102266284A (en) * | 2011-06-20 | 2011-12-07 | 湖北东信药业有限公司 | Secnidazole pessary and preparation process thereof |
| US10335390B2 (en) * | 2014-09-05 | 2019-07-02 | Symbiomix Therapeutics, Llc | Secnidazole for use in the treatment of bacterial vaginosis |
| WO2016196653A1 (en) | 2015-06-01 | 2016-12-08 | Symbiomix Therapeutics, Llc | Novel nitroimidazole formulations and uses thereof |
| KR20210065958A (en) * | 2018-09-05 | 2021-06-04 | 루핀 인코포레이티드 | Deuterated secnidazole and methods and uses thereof for use in the treatment of bacterial vaginosis |
| US12280037B2 (en) | 2020-09-22 | 2025-04-22 | Evofem Biosciences, Inc. | Method and pharmaceutical composition for treating or preventing trichomoniasis and uses thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1174187A (en) * | 1967-11-03 | 1969-12-17 | Prodotti Antibiotici Spa | Compositions with an Activitiy Against Protozoa |
| GB1212704A (en) * | 1967-11-21 | 1970-11-18 | Prodotti Antibiotici Spa | Vaginal suppositories |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1174187A (en) * | 1967-11-03 | 1969-12-17 | Prodotti Antibiotici Spa | Compositions with an Activitiy Against Protozoa |
| GB1212704A (en) * | 1967-11-21 | 1970-11-18 | Prodotti Antibiotici Spa | Vaginal suppositories |
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