CN1326738A - Minocycline vaginal effervescent tablets - Google Patents
Minocycline vaginal effervescent tablets Download PDFInfo
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- CN1326738A CN1326738A CN 00116301 CN00116301A CN1326738A CN 1326738 A CN1326738 A CN 1326738A CN 00116301 CN00116301 CN 00116301 CN 00116301 A CN00116301 A CN 00116301A CN 1326738 A CN1326738 A CN 1326738A
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- minocycline
- acid
- effervescent tablet
- hydroxypropyl cellulose
- tablet according
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Abstract
The present invention utilizes high and long antiseptic efficiency of Minocycline to prepare veginal effervescent tablets and the vaginal administration has high antiseptic effect and greatly reduced toxic side effect compared with oral administration.
Description
The present invention relates to a kind of minocycline vaginal novel form, more particularly relate to minocycline vaginal effervescent tablets.
Minocycline (Minocycline) has another name called minocycline, and clinical practice often is a hydrochlorate, and its chemical constitution is as follows:
Minocycline is a kind of efficient, long lasting semi-synthetic Tetracyclines antibiotics, its antimicrobial spectrum is similar with tetracycline, but its antibacterial action at Tetracyclines for the strongest, golden Portugal bacterium, streptococcus, escherichia coli to tetracycline resistant are still responsive to it, therefore it often is used to bacterial infection disease, for example urinary tract infection, gastrointestinal infection, respiratory tract infection, gynecological infection, Pyoderma, osteomyelitis, the infection of Eye Ear Nose And Throat portion etc.
Oral post-absorption is rapid, the common once oral 200mg of dosage, and blood drug level can reach the peak after 2-3 hour, average 7 μ g/ml.Mainly discharge in kidney and liver, concentration is about 10～30 times of concentration in the serum in the urine.Still can detect in the urine in ten days after the administration, drain slower.
The side reaction of minocycline is identical with tetracycline, but reaction is lighter, and accidental anaphylaxis even anaphylactic shock take place, and photosensitive also have a discovery.Use this medicine treatment patient, nearly 30%～90% patient has following one or more symptoms to occur, for example: feel sick, vomiting, anorexia, abdomen contracture pain, unable, ataxia, dizzy.This medicine also can cause optimum cranium voltage rise height, and other has report to think that this medicine can have cutaneous pigmentation to produce.
According to national sexually transmitted disease (STD) monitoring point 1993 annual reports: gonorrhea accounts for 70% of whole sexual disease mixed infections, and 45% gonorrhea patient merges chlamydia infection; In the non-gonococcal urethritis (NGU), chlamydia, mycoplasma account for more than 80%.Minocycline is the choice drug of present sexual disease mixed infection, and the dosage form of the clinical use of this medicine at present is mainly tablet, capsule and oral suspension, and route of administration is oral administration.Above-mentioned dosage form is the whole body administration, usually brings side reaction to patient, has directly influenced being extensive use of of this medicine.
The object of the invention provides a kind of can reduce poisonous side effect of medicine, the increase medicine local concentration that the whole body administration causes, more preferably brings into play the curative effect of medicine, improves the effervescent tablet of the vagina administration of compliance of patients.
Vagina effervescence of the present invention contains the principal agent minocycline, adds gas-producing disintegrant, adjuvants such as hydroxypropyl cellulose, lactose, sodium lauryl sulphate, magnesium stearate, and it is as follows specifically to fill a prescription:
Minocycline 8-25%
Acid 2-10%
Basic salt 1-10%
Hydroxypropyl cellulose 1-3%
Lactose 50-70%
Sodium lauryl sulphate 1-3%
Magnesium stearate 0.25-2.0%
Wherein acid can be organic acid, example: tartaric acid, the acid of structure rafter, fumaric acid, or mineral acid such as boric acid;
Basic salt is carbonate or bicarbonate.
Get acid of structure rafter or tartaric acid and an amount of carbonate, for example sodium bicarbonate, sodium carbonate mix as gas-producing disintegrant, mix the back tabletting with principal agent, other adjuvant, produce carbon dioxide behind the gained tablet chance water and make disintegration of tablet, the bubble that is produced is tiny and lasting, medicine is evenly distributed on break up very soon in a large amount of foams to be distributed in each gap of vagina, makes medicine bring into play curative effect rapidly, produce therapeutical effect, be specially adapted to vagina local disease.
Hydroxypropyl cellulose is the lower hydroxypropyl cellulose of substitution value, and its swelling in water becomes colloid solution, is the good disintegrating agent of tablet, and low-substituted hydroxypropyl cellulose also available starches replaces.
Sodium lauryl sulphate is an anion surfactant, has effects such as emulsifying, de-sludging, dispersion, moistening, foaming.
Magnesium stearate mainly is to increase particulate lubricity and flowability, reduces tablet weight variation.
Lactose does not chemically react to most of medicine, so it is good diluent because dew is put no change in the air.Be easy to grasp in the tablet manufacturing process when making diluent with lactose, the tablet of making is bright and clean attractive in appearance, accuracy influence to the assay result is less, to make price higher but because lactose is by extracting in the animal milk, sometimes can adopt starch, dextrin, Icing Sugar proper proportion replace lactose, can reduce cost like this.
Usually the method for effervescent tablet making has:
1, bronsted lowry acids and bases bronsted lowry is granulated respectively before tabletting, mixes, before the system granule, must make soft material earlier, the adjuvant fine powder put in the mixer add an amount of wetting agent or binding agent after mixing, the gained soft material is generally with can be agglomerating with hand-tight holding, and press agglomerate with light finger is spallation person be advisable (pharmaceutics, People's Health Publisher).
2, form to divide in will writing out a prescription and granulate with on-aqueous liquid;
3, select meticulously to form to divide, so that the mixture direct compression, and omit granulation step;
4, control granulation water quantities is so that make the dissolving of part composition form granule.
Above-mentioned several method is all on the books in " pharmaceutics " book.
Preparation method of the present invention is:
1, principal agent is even by different mixed with various adjuvants, be that binding agent is made soft material with polyvinylpyrrolidone (PVP), the after drying of granulating again.
2, add the magnesium stearate mix homogeneously behind the granulate again.
3, measuring tablet content weighs according to the content stator.
Provide embodiments of the invention below invention is further described, but do not limit the present invention.
Embodiment 1:
Minocycline 50mg
Tartaric acid 15mg
Sodium bicarbonate 13mg
Low-substituted hydroxypropyl cellulose 5mg
Lactose 200mg
Sodium lauryl sulphate 5mg
Magnesium stearate 3mg
Take by weighing 500 milligrams of minocyclines, 150 milligrams in tartaric acid, 130 milligrams of sodium bicarbonate, lactose 2 grams, 50 milligrams of mix homogeneously of sodium lauryl sulphate.The 10%PVP alcoholic solution is made soft material as binding agent, granulate by 20 mesh sieves, 60 ℃ of dryings add 1% magnesium stearate mix homogeneously behind the reuse 18 mesh sieve granulate.Measure tabletting behind its content, make 10 altogether.
Embodiment 2
The minocycline effervescent tablet vagina 1/week of deep administration of the foregoing description 1 gained, every 3-4 time is a course of treatment, to women's bacterial infection disease, urinary tract infection for example, the mixed infection of sexually transmitted disease (STD) and other gynecological infection diseases have obvious curative effects, through clinical 15 example tests, effective percentage reaches 93%, cure rate is 82%, feels sick, side reactions such as vomiting, anorexia obviously reduce, and the patient who has does not have the toxicity of medicine substantially.
Claims (6)
1, a kind of minocycline effervescent tablet is characterized in that: the consisting of of effervescent tablet:
Minocycline 8-25%
Acid 2-10%
Basic salt 1-10%
Hydroxypropyl cellulose 1-3%
Lactose 50-70%
Sodium lauryl sulphate 1-3%
Magnesium stearate 0.1-2%
2, minocycline effervescent tablet according to claim 1 is characterized in that described acid is organic acid or mineral acid, and organic acid is a tartaric acid, and the acid of structure rafter, fumaric acid, mineral acid are boric acid.
3, minocycline effervescent tablet according to claim 1 is characterized in that described basic salt is carbonate or bicarbonate.
4, minocycline effervescent tablet according to claim 1 is characterized in that the low-substituted hydroxypropyl cellulose that described hydroxypropyl cellulose is.
5, minocycline effervescent tablet according to claim 1 is characterized in that the hydroxypropyl cellulose available starches replaces.
6, minocycline effervescent tablet according to claim 1 is characterized in that using in vagina local application preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB001163019A CN1181824C (en) | 2000-06-02 | 2000-06-02 | Minocycline vaginal effervescent tablets |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB001163019A CN1181824C (en) | 2000-06-02 | 2000-06-02 | Minocycline vaginal effervescent tablets |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1326738A true CN1326738A (en) | 2001-12-19 |
| CN1181824C CN1181824C (en) | 2004-12-29 |
Family
ID=4585710
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB001163019A Expired - Fee Related CN1181824C (en) | 2000-06-02 | 2000-06-02 | Minocycline vaginal effervescent tablets |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1181824C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102058559A (en) * | 2010-12-24 | 2011-05-18 | 郑州百瑞动物药业有限公司 | Doxycycline hydrochloride effervescent tables for milk cows and preparation method thereof |
-
2000
- 2000-06-02 CN CNB001163019A patent/CN1181824C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102058559A (en) * | 2010-12-24 | 2011-05-18 | 郑州百瑞动物药业有限公司 | Doxycycline hydrochloride effervescent tables for milk cows and preparation method thereof |
| CN102058559B (en) * | 2010-12-24 | 2012-06-20 | 郑州百瑞动物药业有限公司 | Doxycycline hydrochloride effervescent tables for milk cows and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1181824C (en) | 2004-12-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20041229 Termination date: 20100602 |