CN1116033C - Effervescent tablets for curing vaginitis and its preparing method - Google Patents
Effervescent tablets for curing vaginitis and its preparing method Download PDFInfo
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- CN1116033C CN1116033C CN 99112303 CN99112303A CN1116033C CN 1116033 C CN1116033 C CN 1116033C CN 99112303 CN99112303 CN 99112303 CN 99112303 A CN99112303 A CN 99112303A CN 1116033 C CN1116033 C CN 1116033C
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- effervescent tablet
- sodium bicarbonate
- terbinafine hcl
- mannitol
- hydroxypropyl cellulose
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Abstract
The present invention relates to an effervescent tablet for treating monilial vaginitis, which is composed of terbinafine hydrochloride used as a therapeutical agent, a disintegrating agent, a filling agent, a binding agent, a lubricant, etc. The present invention is used for treating colpitis. The effervescent tablet can be rapidly disintegrated, disintegration time limit is about 2.8 minutes, and the effervescent tablet has the advantages of direct and lasting action, rapid effect, large concentration of local medicine, high therapeutic effect, small medicine doses, safe adjuvant materials, no toxicity, no local irritant effect and general adverse reaction, safe use, advanced preparation technology, reliability, lower cost and high productive efficiency; thus, the present invention is worthy to be popularized and used.
Description
The invention belongs to the Amino-Cerv thing, is the colpitic effervescent tablet of a kind of treatment.
Monilial vaginitis is a kind of common mucosa monilial infection, is more common in gravid woman and diabetics.Have report 75% the women of child-bearing age to have once the infection of this bacterium in life at least, and wherein 45% women have the repeated infection history.Sick all therewith morbidity such as oral contraceptive, diabetes, immunodeficiency and prolonged application antibiotic, environmental factors, nourishment is relevant.In recent years, this disease has the trend that increases gradually.The treatment of this disease mainly contains two kinds of methods at present: a kind of is local topical administration, and medicine commonly used has nystatin cream, suppository, vaginal tablet, clotrimazole, miconazole suppository, cream etc.Clinical application practice for many years shows that this several drugs therapeutic effect is unsatisfactory, and its major defect is that curative effect is not obvious, recurrence easily, and also local irritation is bigger, and the patient is reluctant to use; Another kind method is oral antifungal drug, as oral ketoconazole, fluconazol etc.Oral therapy has convenient and does not have local irritant advantage, but its whole body poison pair effect is bigger, raises liver toxicity etc. as gastrointestinal reaction, headache, liver enzyme.Along with candidiasis tolerates the serious day by day of phenomenon to imidazoles, its therapeutic effect is also also unsatisfactory.Therefore, numerous women patient presses for a kind of ideal medicine and method.
The object of the present invention is to provide a kind of vagina tissue that directly acts on, easy to use, rapid-action, curative effect is high, nontoxic pair of effect, non-irritating treatment monilial vaginitis medicament.
Solution of the present invention is that to select terbinafine HCl for use be therapeutic agent.Said terbinafine HCl is the propylamine antifungal agent of new generation that grows up on the naftifine basis.Its has a broad antifungal spectrum, active high, curative effect is rapid.Its action principle is that highly selective suppresses fungus Squalene Cycloxygenase, and the forming process of fungal cell membrane is obstructed, and reaches the effect of killing or suppressing fungus.
Terbinafine HCl promptly has intensive inhibitory or killing effect to candidiasis under low concentration, the oidiomycetic minimum inhibitory concentration of its dialogue (MIC) value is than low tens times of ketoconazole.In addition, this product also has direct antiinflammatory action, and this point is very useful for treating monilial vaginitis fast and effectively.The domestic existing sale of the ointment machin tablet of these product is mainly used to treat diseases such as tinea manus and pedis, tinea corporis and cruris, tinea versicolor, tinea unguium and cutaneous Candida.
With regard to vaginal candida, terbinafine HCl ointment uses very inconvenient, does not adopt substantially clinically.Oral tablet is difficult to come together in a large number vaginal mucosa mainly due to medicine, needs taking dose big, from and can cause the drawback big to the whole body toxic and side effects, so do not see use at present clinically yet.The present invention has developed a kind of effervescent tablet that can directly be used in the terbinafine HCl of vagina.This effervescent tablet is made up of terbinafine HCl, filler mannitol and disintegrating agent etc., its composition (weight %) content is: the 1.0-25.0 terbinafine HCl, 10.0-70.0 mannitol, 11.0-34.2 tartaric acid, 12.4-38.6 sodium bicarbonate, 2.0-15.0 low-substituted hydroxypropyl cellulose (L-HPC), 1.0-8.0 carboxymethyl starch sodium, the polyvinylpyrrolidone of 0.9-2.5 magnesium stearate and 0.1-1.5.
The present invention is the soda acid disintegrating agent with tartaric acid and sodium bicarbonate, meets waterishlogging and gives birth to reaction generation carbon dioxide, thereby make the quick disintegrate of effervescent tablet, and its optimal proportion is 1: 1.13, can certainly replace sodium bicarbonate with sodium carbonate.The molecular weight of the polyvinylpyrrolidone of selecting for use is between 25000-40000, as PVPK
25Or PVPK
30Can use Deng all, the low-substituted hydroxypropyl cellulose that uses in the component, its propoxyl content is generally 7-16%, and molecular weight is between the 50000-650000, the carboxymethyl starch sodium of selecting for use also has the quick disintegration of the effervescent tablet of promotion, and its degree of exchange is generally about 0.3-0.5.
The compound method of this effervescent tablet is: at first terbinafine HCl, mannitol, tartaric acid, sodium bicarbonate, low-substituted hydroxypropyl cellulose (L-HPC) and carboxymethyl starch sodium are micronized to particle diameter below 25 microns, 50-60 ℃ of oven dry down.Magnesium stearate is crossed 100 mesh sieves.Polyvinylpyrrolidone is made into 5% ethanol solution, and sealing is preserved standby,
Then earlier terbinafine HCl, carboxymethyl starch sodium and low-substituted hydroxypropyl cellulose are pressed the formula proportion mix homogeneously, more successively with mannitol, tartaric acid, the sodium bicarbonate employing equivalent method mix homogeneously that progressively increases.Add a certain amount of polyvinylpyrrolidone alcoholic solution then and make soft material.Granulate the back 60-70 ℃ of oven dry with 20 order nylon mesh, and behind the reuse 18 order nylon mesh granulate, the adding magnesium stearate is made lubricant in the whole good granule, equally with the equivalent method mixing that progressively increases.Measuring granule content, after the calculating sheet is heavy, striking out oval effervescent tablet with abnormity.
An important feature of the present invention is that the component of film-making all is micronized to particle diameter earlier less than 25 microns before film-making.Because the terbinafine hydrophobicity is higher, can improve particulate specific surface area after the micronization, make the effervescent tablet disintegrate after medicine more can contact with focus fully.And improved the disintegration rate of effervescent tablet, foreshortened to 2.8 minute from common 4.6 minutes its disintegration, thereby make effervescent tablet rapid-action, greatly improved curative effect.
Another characteristics of the present invention have been simplified preparation technology after being to use polyvinylpyrrolidone to be binding agent.Usually when the preparation effervescent tablet, all need preparation acid respectively, two kinds of granules of alkali earlier; and then mixed pressuring plate; this flaking method; acid, alkali granule mix inhomogeneous; must influence the disintegrating property of effervescent tablet; and the present invention can the mixed once film-making, thereby both can simplify preparation technology widely, has also improved the disintegration rate and the quality of effervescent tablet.Be filler owing to the present invention has selected mannitol for use in addition,, thereby make the terbinafine HCl effervescent tablet in use have more comfort because mannitol is met the water dissolution heat absorption.
Example of following reuse further specifies the process for preparation of this effervescent tablet.
The micronized terbinafine HCl 50 of learning from else's experience restrains, carboxymethyl starch sodium 37 grams and low-substituted hydroxypropyl cellulose (L-HPC) 47 gram mix homogeneously.Then add 470 gram mannitol successively.282 gram tartaric acid and 320 gram sodium bicarbonate are with the equivalent method mix homogeneously that progressively increases.Add 140 milliliters of 5%PVPK then
30Ethanol solution is made soft material.Granulate with 20 order nylon mesh, and,, add 17 gram magnesium stearate, with the equivalent method mixing that progressively increases again with behind the 18 order nylon mesh granulate 60-70 ℃ of oven dry down.After measurement granule content, calculating sheet weigh, strike out oval effervescent tablet with abnormity.So can be pressed into 1000 effervescent tablets.
During use, put into one of above-mentioned effervescent tablet in non-menstruation in aspire to vagina, every night once, 8 of logotypes are a course of treatment, the back check of one week of drug withdrawal.
For showing that superiority of the present invention done treatment monilial vaginitis clinical effectiveness by Hospital Affiliated to Shandong Medical College and observed, and compare with miconazole and nystatin effervescent tablet.Case source: be the prescription on individual diagnosis person of this gynecological of institute, year order is 25-40 year married woman.Course of disease 3-15 days.The age of two groups of cases and course of disease zero difference.
Its inclusion criteria: leucorrhoea grow in quantity, vulvovaginal are scratched where it itches or burn feeling are arranged; Gynecologial examination, vulvovaginal hyperemia, secretions increase; Vaginal secretions finds candidiasis.
Administration and follow-up method: non-menstrual phase is put into effervescent tablet a slice in intravaginal, every night once, is a course of treatment with 8.Drug withdrawal one week check, and inquiry transference cure situation.
Efficacy assessment standard:
(1) recovery from illness: symptom and sign disappear, and vaginal secretions is checked the candidiasis feminine gender.
(2) effective: symptom and sign alleviate, and vaginal secretions is checked the candidiasis feminine gender.
(3) invalid: symptom and sign no change, vaginal secretions inspection still have candidiasis to exist.
Result of the test shows: test group 10 examples all obtain the recovery from illness effect, do not find untoward reaction during the medication.Matched group miconazole 5 examples are all fully recovered, and have an example anaphylaxis to occur.The 4 example recoveries from illness of nystatin effervescent tablet, 1 routine sx, but vaginal secretions checks that candidiasis is still positive.
By above-mentioned clinical trial, observe by 10 routine patients' treatment, show that terbinafine HCl effervescent tablet treatment monilial vaginitis is effective, curative effect is high and have no side effect nonirritant.
The several examples of following reuse further specify effect of the present invention.
The patient, woman 28 years old, because of pudendum itch, bitterly, leucorrhea is many, be diagnosed as monilial vaginitis at my gate, obviously alleviate with 4 sensory symptomses of terbinafine HCl effervescent tablet, 8 (course of treatment) backs of medication symptom, sign disappear, and vaginal secretions is checked candidiasis feminine gender, no any untoward reaction during the medication.
Also 5 routine model cases have been carried out clinical observation and followed up a case by regular visits in addition, followed up a case by regular visits to after one week of drug withdrawal for the first time, followed up a case by regular visits to after the menstruation first time after the drug withdrawal for the second time, twice Follow-up results is identical, 4 examples of fully recovering, produce effects 1 example.Clinical manifestation before and after 5 routine patient's medications is seen Table 1 table 1
Clinical manifestation before and after 5 routine patient's medications
| Sick clinical example performance | Example 1 | Example 2 | Example 3 | Example 4 | Example 5 | |
| Before the medication | A cheese sample secretions B smear is looked into the hyperemia of bacterium C itching of vulva D vaginal mucosa | + + + + | + + + + | + + + + | + + + + | + + + + |
| After the medication | A B C D | - - - - | - - - - | - - - - | - - - - | - - - ± |
(-) is that produce effects (+) is for invalid for recovery from illness (±).
More than use the result to show that advantage of the present invention is clearly, effervescent tablet drug dose of the present invention is little, and therefore the adjuvant safety non-toxic had not both had local irritant effect, did not have systemic adverse reactions yet, safe in utilization.Disintegration rate is fast, and directly and lasting, rapid-action, local drug concentration is big in effect, and the clinical principium test shows that this product treatment vaginal candidiasis is better than existing medicine commonly used.This pharmaceutical preparation advanced person, reliable, cost is lower, and obvious social and economic benefit are arranged, be worthy of popularization.
The several examples of following reuse further specify the present invention, are not confined to certainly in these several examples.Following example is to produce the Formulation Example of 1000 effervescent tablets.
Example 123
Component (weight portion)
Terbinafine HCl 25 75 100
Mannitol 1,275 382 42.4
Tartaric acid 300 222 112
Sodium bicarbonate 340 251 126.4
Low-substituted hydroxypropyl cellulose (L-HPC) 325 80 8
Carboxymethyl starch sodium 150 40 4.4
Magnesium stearate 55 17 4.4
Polyvinylpyrrolidone (PVPK30) 30 8 2.4
Claims (4)
1. effervescent tablet for the treatment of monilial vaginitis, form by components such as binding agent, filler, disintegrating agent and therapeutic agents, it is characterized in that said effervescent tablet is the terbinafine HCl effervescent tablet, it forms content (weight %): the 1.0-25.0 terbinafine HCl, 10.0-70.0 mannitol, 11.0-34.2 tartaric acid, 12.4-38.6 sodium bicarbonate, 2.0-15.0 low-substituted hydroxypropyl cellulose, 1.0-8.0 carboxymethyl starch sodium, 0.9-2.5 magnesium stearate, the 0.1-1.5 polyvinylpyrrolidone.
2. according to the described effervescent tablet of claim 1, the particle diameter of terbinafine HCl, mannitol, tartaric acid, sodium bicarbonate, low-substituted hydroxypropyl cellulose and carboxymethyl starch sodium that it is characterized in that being used for film-making is below 25 microns.
3. according to the described effervescent tablet of claim 1, the relative weight ratio that it is characterized in that component mesotartaric acid and sodium bicarbonate is 1: 1.13.
4. according to the compound method of the described effervescent tablet of claim 1, it is characterized in that comprising following preparation steps:
(1) terbinafine HCl, mannitol, tartaric acid, sodium bicarbonate, low-substituted hydroxypropyl cellulose and carboxymethyl starch sodium being micronized to particle diameter is below 25 microns, and magnesium stearate is crossed 100 mesh sieves, oven dry;
(2) the polyvinylpyrrolidone ethanol solution of preparation 5%;
(3) at first terbinafine HCl, carboxymethyl starch sodium and low-substituted hydroxypropyl cellulose are pressed the proportional quantity mix homogeneously, again successively with mannitol, tartaric acid, sodium bicarbonate with the equivalent method mix homogeneously that progressively increases, add 5% polyvinylpyrrolidone alcoholic solution then and make soft material;
(4) granulate with 20 order nylon mesh, dry the back down with 18 order nylon mesh granulate at 60-70 ℃;
(5) in the granule of whole good grain, add magnesium stearate, with the equivalent method mixing that progressively increases;
(6) measure granule content, after the calculating sheet is heavy, be pressed into oval tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 99112303 CN1116033C (en) | 1999-07-08 | 1999-07-08 | Effervescent tablets for curing vaginitis and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 99112303 CN1116033C (en) | 1999-07-08 | 1999-07-08 | Effervescent tablets for curing vaginitis and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1279944A CN1279944A (en) | 2001-01-17 |
| CN1116033C true CN1116033C (en) | 2003-07-30 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 99112303 Expired - Lifetime CN1116033C (en) | 1999-07-08 | 1999-07-08 | Effervescent tablets for curing vaginitis and its preparing method |
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| Country | Link |
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| CN (1) | CN1116033C (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR034813A1 (en) * | 2001-07-20 | 2004-03-17 | Novartis Ag | PHARMACEUTICAL COMPOSITIONS AND USE OF THE SAME |
| CN100364520C (en) * | 2006-04-24 | 2008-01-30 | 魏锐 | Tebinaifen hydrochloride suppository and its preparation method |
| CN101548958B (en) * | 2008-04-03 | 2012-10-17 | 万特制药(海南)有限公司 | Dispersing tablet containing terbinafine hydrochloride |
| CN102335152B (en) * | 2010-07-20 | 2015-07-08 | 杭州赛利药物研究所有限公司 | Terbinafine hydrochloride vagina sustained release tablet and its preparation method |
| CN109674757A (en) * | 2019-02-22 | 2019-04-26 | 济南康和医药科技有限公司 | A kind of terbinafine HCl composition and preparation method thereof |
| CN111346068A (en) * | 2020-04-24 | 2020-06-30 | 云南伦扬科技有限公司 | Vaginal bactericidal effervescent tablet and preparation method thereof |
-
1999
- 1999-07-08 CN CN 99112303 patent/CN1116033C/en not_active Expired - Lifetime
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| CN1279944A (en) | 2001-01-17 |
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