CN1582938A - Vaginal effervescent tablets of ofloxacin - Google Patents

Vaginal effervescent tablets of ofloxacin Download PDF

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Publication number
CN1582938A
CN1582938A CN 200410044302 CN200410044302A CN1582938A CN 1582938 A CN1582938 A CN 1582938A CN 200410044302 CN200410044302 CN 200410044302 CN 200410044302 A CN200410044302 A CN 200410044302A CN 1582938 A CN1582938 A CN 1582938A
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China
Prior art keywords
acid
levofloxacin
sodium
vagina
vagina effervescence
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Pending
Application number
CN 200410044302
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Chinese (zh)
Inventor
张艳秋
朱毅
唐菲
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HAINAN PHARMACEUTICAL INST
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HAINAN PHARMACEUTICAL INST
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Publication date
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Priority to CN 200410044302 priority Critical patent/CN1582938A/en
Publication of CN1582938A publication Critical patent/CN1582938A/en
Pending legal-status Critical Current

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A vaginal effervescent tablet of levo-ofloxacin for treatig vaginitis and cervicitis is prepared from levo-ofloxacin or its salts, foaming agent, foam stabilizer and filler.

Description

The levofloxacin vagina effervescence
Technical field
The present invention relates to a kind of levofloxacin vagina effervescence.
Background technology
1. vaginitis, cervicitis are commonly encountered disease, frequently-occurring disease, serious harm women's health, and these diseases cause cervical cancer easily as can not get in time treatment fully.The medicine of present commercially available treatment female vagina, cervicitis is a lot, all kinds of antibiotic of bacterial vaginitis and Chinese patent medicine have been played positive effect to women's health, it is bacteriostatic that these medicines mostly are, sterilizing power is poor, and along with the increase of usage frequency, fastbacteria has also produced, the trend that medication number of times and dosage is had increase, caused the imbalance of vagina normal flora simultaneously, more increased the weight of the state of an illness, caused repeatedly.The principal agent levofloxacin is the new drug that goes on the market in recent years among the present invention, isomer for ofloxacin, its bactericidal action is 2 times of ofloxacin, not only to Escherichia, Klebsiella, Enterobacter, Proteus, Serratia, Salmonella, Shigella, Pseudomonas aeruginosa belongs to, gram negative bacillis such as hemophilus influenza have stronger antibacterial action, and to staphylococcus, streptococcus pneumoniae, micrococcus scarlatinae, gram positive coccus effects such as enterococcus are also very strong, to the digestibility streptococcus and the gonococcus of anaerobe, mycoplasma, chlamydia also has good bactericidal action.Improved general quinolones strong to the gram positive coccus antibacterial activity not as gram negative bacilli, to the active dissatisfactory weak point of anaerobe.And levofloxacin also has effect to the beta-lactam antibiotic Resistant strain.
2. at present levofloxacin mainly contains oral and injection type, and levofloxacin has been one of choice drug of bacterial vaginitis at present, but along with wide model is used, and the untoward reaction of systemic administration has report also the time.Change the levofloxacin route of administration, make vagina effervescence intravaginal local application, medicine directly acts on focus, the drug level height, and effect is lasting, rapid-action rapidly, can avoid or reduce the untoward reaction that systemic administration produces.
Summary of the invention
The purpose of this invention is to provide a kind of levofloxacin vagina effervescence.
Levofloxacin or its salt (levofloxacin hydrochloride that will have bactericidal action, levofloxacin lactate and Levofloxacin M. S. A) make and be suitable for treating by the sensitive strain in gram-negative bacteria and the gram positive bacteria and by gonococcus, vaginitis due to the chlamydia trachomatis, the most preferred dosage form of gynecological inflammations such as cervicitis, the vaginal effervescent tablet agent adopts chance water can produce the soda acid system of carbon dioxide as foaming agent, it can make this kind tablet principal agent is distributed to fast each position and the corner of vagina in the rapid foaming disintegrate of vagina suction back, comprise that infectious bacterias such as cervix uteri can arrive part, increase contact area, contact focus to greatest extent, give full play to the effect of its local bactericidal, other dosage form drug effects of same dosage of comparing are more obvious; This product is a slice every night, and is easy to use.
A kind of levofloxacin vagina effervescence, the effective ingredient that it is characterized in that this effervescent tablet are levofloxacin or its esters (levofloxacin hydrochloride, levofloxacin lactate or Levofloxacin M. S. A); The alkali system that acid system that interpolation organic acid or acid salt are formed in above-mentioned principal agent and carbonate are formed is as effervescent foaming agent and filler, and the well-established law tabletting forms, and the basic prescription of 1000 these effervescent tablets is:
Levofloxacin 20-500g is in levofloxacin;
The soda acid system is as foaming agent 50-800g;
Foam stabilizer 0.04-40g;
Acid is organic acid or acid salt in the above-mentioned soda acid system foaming agent, as one to three kind in citric acid, tartaric acid, potassium hydrogen tartrate, sodium bitartrate or the succinic acid; Alkali is a kind of in sodium bicarbonate or the sodium carbonate.
Described foam stabilizer is one or both in spermol, sodium lauryl sulphate, the Tween-80.
Beneficial effect of the present invention: levofloxacin effervescent tablet pharmacodynamic study proof this product of the present invention is used for the bacterial vaginitis curative effect certainly, and nonirritant.
The pharmacodynamic study of levofloxacin lactate vagina effervescence:
With accomplice rabbit vaginas such as staphylococcus aureus, escherichia coli, gonococcuss, set up rabbit bacterial vaginitis model, give the rabbit vagina medication every day, continuous 7 days, with the antibacterial negative conversion rate of vaginal secretions and the healing degree of vaginal mucosa inflammation is leading indicator, observes the therapeutical effect of levofloxacin vagina effervescence.The result shows, levofloxacin vagina effervescence height, in, low dose group can be eliminated the contrafluxion of vaginitis model rabbit vagina, edema, rotten to the corn, features such as secretions increase, wherein, the cure rate of high dose group (10mg/kg) is 91.7%, effective percentage is 100%: the cure rate of middle dosage group (5mg/kg) is 83.3%, effective percentage is 91.7%: the cure rate 66.7% of low dose group (2.5mg/kg), effective percentage is 83.3%, show that the levofloxacin vagina effervescence can significantly suppress by staphylococcus aureus, escherichia coli, the experimental rabbit bacterial vaginitis that gonococcus etc. form is corrected the pathological change of vagina.
The levofloxacin lactate vagina effervescence is to the irritation test of rabbit vagina mucosa:
Give 1 of rabbit vagina medication/only (every contains levofloxacin lactate 100mg) with the levofloxacin lactate vagina effervescence, single administration or once a day, successive administration 7 days (be equivalent to clinical using dosage 25 times), result of the test shows, this medicine does not have the obvious stimulation effect to the rabbit vagina mucosa, is suitable for clinical use.
The levofloxacin lactate vagina effervescence is to the Cervical irritation test of rabbit:
Give near the rabbit cervix uteri 1 of medication/only (every contains levofloxacin lactate 100mg) with the levofloxacin lactate vagina effervescence, once a day, successive administration is after 7 days (be equivalent to clinical using dosage 25 times), get cervix uteri and do the pathology histological examination, compare with the blank group, each layer tissue structure of the cervix uteri of each treated animal is normal, and cervical mucous membrane is complete, does not change.Show that the levofloxacin lactate vagina effervescence has no stimulation to the rabbit cervix uteri.
Specific embodiment
Embodiment 1:
Prescription: levofloxacin 100g
Citric acid 120g
Lactose 100g
Sodium bicarbonate 180g
Microcrystalline Cellulose 50g
Sodium lauryl sulphate 6g
Pulvis Talci 20g
10% starch is an amount of
Technology: citric acid is mixed with lactose, and levofloxacin mixes with sodium bicarbonate, sodium lauryl sulphate, granulates with 10% starch slurry respectively, and mixing and adding microcrystalline Cellulose, Pulvis Talci mixing are pressed into 1000 behind the dry respectively granulate, promptly.
Embodiment 2:
Prescription: levofloxacin lactate 125g (quite levofloxacin 100g);
Tartaric acid 130g
Potassium hydrogen tartrate 150g
Sodium bicarbonate 160g
Sodium lauryl sulphate 9g
Microcrystalline Cellulose 60g
Magnesium stearate 30g
Technology:, directly be pressed into 1000, promptly with above-mentioned supplementary material mix homogeneously.
Embodiment 3:
Prescription: levofloxacin hydrochloride 115g (quite levofloxacin 100g);
Tartaric acid 120g
Citric acid 100g
Sodium bicarbonate 180g
Hyprolose 60g
Tween-80 10g
5% polyvidone ethanol solution is an amount of
Magnesium stearate 30g
Technology: with levofloxacin, tartaric acid, citric acid, sodium bicarbonate, hyprolose powder mix homogeneously, add the 5% polyvidone ethanol solution that contains Tween-80 and granulate in right amount, drying adds the magnesium stearate mixing behind the granulate, be pressed into 1000, promptly.

Claims (4)

1, a kind of levofloxacin vagina effervescence is characterized in that: the effective ingredient of this effervescent tablet is levofloxacin or its esters.
2, levofloxacin vagina effervescence according to claim 1, it is characterized in that: the alkali system that acid system that interpolation acid or acid salt are formed in above-mentioned principal agent and carbonate are formed as foam stabilizer and filler, suppresses the tablet that forms as effervescent foaming agent, interpolation surfactant; The basic prescription of 1000 these effervescent tablets is:
Levofloxacin or its esters 20-500g are in levofloxacin;
The soda acid system is as foaming agent 50-800g;
Foam stabilizer 0.04-40g.
3, levofloxacin vagina effervescence according to claim 2, it is characterized in that: acid is organic acid in the above-mentioned soda acid system foaming agent, as citric acid, tartaric acid, succinic acid, fumaric acid, adipic acid, malic acid, water-soluble amino acid, or acid salt, as potassium hydrogen tartrate, sodium bitartrate, citric acid potassium dihydrogen, fumaric acid sodium, or ore deposit acid, as one in the boric acid to five kinds; Alkali is one or both in sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, calcium bicarbonate or the calcium carbonate.
4, levofloxacin vagina effervescence according to claim 2 is characterized in that: described foam stabilizer is one or both in spermol, sodium lauryl sulphate, the Tween-80.
CN 200410044302 2004-05-21 2004-05-21 Vaginal effervescent tablets of ofloxacin Pending CN1582938A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN 200410044302 CN1582938A (en) 2004-05-21 2004-05-21 Vaginal effervescent tablets of ofloxacin

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN 200410044302 CN1582938A (en) 2004-05-21 2004-05-21 Vaginal effervescent tablets of ofloxacin

Publications (1)

Publication Number Publication Date
CN1582938A true CN1582938A (en) 2005-02-23

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Family Applications (1)

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CN 200410044302 Pending CN1582938A (en) 2004-05-21 2004-05-21 Vaginal effervescent tablets of ofloxacin

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104224744A (en) * 2014-09-28 2014-12-24 严相顺 Ciprofloxacin effervescent tablet for control of silkworm bacterial disease
CN109330983A (en) * 2018-07-27 2019-02-15 江苏中天药业有限公司 A kind of vagina effervescence and preparation method thereof

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104224744A (en) * 2014-09-28 2014-12-24 严相顺 Ciprofloxacin effervescent tablet for control of silkworm bacterial disease
CN109330983A (en) * 2018-07-27 2019-02-15 江苏中天药业有限公司 A kind of vagina effervescence and preparation method thereof

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