CN101543479A - Terbinafine hydrochloride vaginal effervescent tablet and preparation method thereof - Google Patents
Terbinafine hydrochloride vaginal effervescent tablet and preparation method thereof Download PDFInfo
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- CN101543479A CN101543479A CN200810015601A CN200810015601A CN101543479A CN 101543479 A CN101543479 A CN 101543479A CN 200810015601 A CN200810015601 A CN 200810015601A CN 200810015601 A CN200810015601 A CN 200810015601A CN 101543479 A CN101543479 A CN 101543479A
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- terbinafine hydrochloride
- effervescent tablet
- vaginal effervescent
- hydrochloride vaginal
- terbinafine
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Abstract
The invention discloses a terbinafine hydrochloride vaginal effervescent tablet and a preparation method thereof. The terbinafine hydrochloride vaginal effervescent tablet mainly comprises a basic remedy of terbinafine hydrochloride, an effervescent auxiliary material and other auxiliary materials, wherein the effervescent auxiliary material consists of organic acid and carbonate; and other auxiliary materials consist of one or more of a disintegrant, a binding agent, a diluting agent and a lubricating agent and a surfactant. The invention is suitable for women to administrate in vagina; and the medicament can be disintegrated in a shortest time, generates fine and even foam and is favorable for fully absorbing pharmacodynamical ingredients, so patients are easy to accept the medicament, and the medicament is suitable to be clinically popularized and applied. The invention also discloses the preparation method which ensures that the quality of products is stable, the preparation process is simple, the quality is controllable and the cost is lower, so the preparation method is suitable for industrial large-scale production. The terbinafine hydrochloride vaginal effervescent tablet prepared by the invention is mainly applied to monilial vaginitis and has unique effect.
Description
Invention field
The present invention relates to a kind of terbinafine HCl sheet and preparation method thereof, belong to medical technical field.
Technical background
Terbinafine HCl is the propylene amine antifungal drug of new generation that grows up on the naftifine basis.The terbinafine has a broad antifungal spectrum, Mlc is low, and clinical effectiveness is remarkable.That terbinafine HCl has is antibacterial, dual curative effect sterilizes.Its mechanism of action is that high selectivity suppresses fungus Squalene Cycloxygenase, fungal cell membrane formed is obstructed, thus the bacteriostasis of playing; Simultaneously, after this product suppressed the Squalene Cycloxygenase, the precursor Squalene still gathered in the fungal cell in a large number, causes the fungal cell to be poisoned to death, thereby plays bactericidal action.Clinical trial shows that the cure rate of terbinafine treatment tinea is 80%, and total effective rate 91.7% is 100% to the fungal bacterial strain clearance rate.
Terbinafine HCl was succeeded in developing by Switzerland's Novartis the eighties in last century, went on the market in Britain first in 1991.1996 is the OTC medicine by drugs approved by FDA, and go on the market in the U.S. the same year.At present, more than 90 countries sell in the whole world.Terbinafine HCl has also entered first OTC catalogue of China in 2000.Because it is to the anti-infectious function good to superficial mycosis, external can be cured most dermatomycosiss.Since Terbinafine hydrochloride emulsifiable paste (Lan Meishu) listing of Sino-U.S. SmithKline (Tianjin) company, develop a lot of dosage forms such as tablet, spray, gel, liniment and liniment successively, also embodied the effect of terbinafine HCl aspect antifungal from the side.
Monilial vaginitis is a kind of common vaginitis, due to candida albicans infection.Clinical manifestation is mainly vulva pruritus and the leucorrhoea grow in quantity stiff bean dregs sample that is white in color.The primary disease sickness rate is only second to trichomonal vaginitis.The pH value that is suitable for most the candidiasis breeding is 5.5～6.5, glycogen increases in vagina, when acidity increases, promptly breeding causes inflammation rapidly, so be more common in anemia of pregnant woman, diabetic and accept a large amount of estrogen persons, as prolonged application antibiotics, changed the mutual inhibition relation between the intravaginal microorganism, candidiasis is bred and cause infection.Candidiasis can be present on people's oral cavity, intestinal and the vaginal mucosa and not cause that symptom, the candidiasis at these three positions can infect mutually, susceptible disease when local environmental condition is fit to.Because the characteristics that it is easy to recur have become the common problem of paying close attention to of doctor and patient.
Clinical experiment shows that Terbinafine hydrochloride vaginal effervescent tablet has extremely strong specific aim, determined curative effect for the microbial vaginitis of treatment beads.Qilu Pharmaceutical Factory is existing sells, but because the mannitol of using in its prescription has drug action, and cost of supplementary product is higher, and production technology is more complicated also.
Summary of the invention:
The present invention is a kind of Terbinafine hydrochloride vaginal effervescent tablet, comprises following component, all is weight percentage; Terbinafine HCl 10-75%, effervescent adjuvant 10-50%, other adjuvants 0.5-50%.
The effervescent adjuvant of using among the present invention is the combination of organic acid and carbonate, and used organic acid comprises one or more of citric acid, tartaric acid, fumaric acid, malic acid; Used carbonate is a kind of of sodium carbonate, sodium bicarbonate or both mixture.
Other adjuvants comprise that one or more and surfactant of binding agent, lubricant, diluent, disintegrating agent form.Wherein binding agent is one or more of hydroxypropyl methylcellulose, polyvinylpyrrolidone and dehydrated alcohol; Lubricant is a Pulvis Talci, one or more of micropowder silica gel and magnesium stearate; Diluent is one or more of starch, microcrystalline Cellulose, lactose and dextrin.Disintegrating agent is one or more of low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crospolyvinylpyrrolidone and cross-linking sodium carboxymethyl cellulose.Surfactant is one or more of sodium lauryl sulphate, sodium laurylsulfate and tween, and the present invention is preferably sodium lauryl sulphate.
The preparation method of Terbinafine hydrochloride vaginal effervescent tablet of the present invention can be the arbitrary method in following: a, direct compression; B, wet granule compression tablet; C, dry granulation tabletting
Compare with present prior art, of the present invention have following characteristics:
1) multiformity of adjuvant selection.Confirm that through overtesting this product is more flexible for the selectivity ratios of adjuvant, the collocation of prescription component is more prone to, and has enlarged the scope of screening.Can farthest improve the stability of product, reduce production cost.
2) owing to the terbinafine HCl poorly water-soluble, we have added surfactant in prescription, and tablet can produce trickle foam when disintegrate, and medicine can better disperse, and plays a role.
3) used preparation technology is simple among the present invention, and easy operating can adopt multiple preparation method tabletting, has reduced the limitation to production equipment.
The specific embodiment:
Embodiment 1: Terbinafine hydrochloride vaginal effervescent tablet, and the prescription component is:
Terbinafine HCl 150g
Lactose 70g
Citric acid 100g
Sodium bicarbonate 100g
Low-substituted hydroxypropyl cellulose 30g
Sodium lauryl sulphate 10g
Magnesium stearate 2g
Dehydrated alcohol is an amount of
Make 1000
Preparation process: a) supplementary material is handled: with required supplementary material respectively drying dewater, cross 100 sieves, take by weighing standby by recipe quantity.B) preparation soft material: get terbinafine HCl, lactose, citric acid, sodium bicarbonate, low-substituted hydroxypropyl cellulose and sodium lauryl sulphate mix evenly with the equivalent method of progressively increasing, and prepare soft material with an amount of dehydrated alcohol.C) granulate: the soft material that makes is granulated through 20 eye mesh screens.D) oven dry granulate: place 50 ℃ of dryings of baking oven to take out in 3 hours, with 20 mesh sieve granulate.E) total mixing: add the magnesium stearate that weighs up, evenly mixed.F) tabletting: semi-finished product are measured particulate content and are determined the heavy back of sheet tabletting, promptly.
Estimate: sample disintegration is 3.2 minutes, melts that to become the time limit up to specification (according to two appendix XA of Chinese Pharmacopoeia version in 2005, XB).
Embodiment 2: Terbinafine hydrochloride vaginal effervescent tablet, and the prescription component is:
Terbinafine HCl 150g
Microcrystalline Cellulose 100g
Tartaric acid 140g
Sodium carbonate 130g
Carboxymethyl starch sodium 15g
Sodium lauryl sulphate 15g
Magnesium stearate 10g
5% polyvinylpyrrolidone alcoholic solution is an amount of
Make 1000
Preparation process: a) supplementary material is handled: with required supplementary material respectively drying dewater, cross 100 sieves, take by weighing standby by recipe quantity.B) preparation soft material: get terbinafine HCl, microcrystalline Cellulose, tartaric acid, sodium carbonate, carboxymethyl starch sodium and sodium lauryl sulphate mix evenly with the equivalent method of progressively increasing, and prepare soft material with 5% an amount of polyvinylpyrrolidone ethanol solution.C) granulate: the soft material that makes is granulated through 20 mesh sieves.D) oven dry granulate: place 60 ℃ of dryings of baking oven to take out in 3 hours, with 20 mesh sieve granulate.E) total mixing: add the magnesium stearate that weighs up, evenly mixed.F) tabletting: semi-finished product are measured particulate content and are determined the heavy back of sheet tabletting, promptly.
Estimate: 3.5 minutes disintegrations, melt that to become the time limit up to specification (according to two appendix XA of Chinese Pharmacopoeia version in 2005, XB).
Embodiment 3: Terbinafine hydrochloride vaginal effervescent tablet, and the prescription component is:
Terbinafine HCl 150g
Starch 100g
Citric acid 90g
Sodium bicarbonate 90g
Crospolyvinylpyrrolidone 10g
Sodium lauryl sulphate 10g
Pulvis Talci 5g
Dehydrated alcohol is an amount of
Make 1000
Preparation process: a) supplementary material is handled: with required supplementary material respectively drying dewater, cross 100 sieves, take by weighing standby by recipe quantity.B) preparation soft material: get terbinafine HCl, starch, citric acid, sodium bicarbonate, crospolyvinylpyrrolidone and sodium lauryl sulphate mix evenly with the equivalent method of progressively increasing, and prepare soft material with an amount of ethanol solution.C) granulate: the soft material that makes is granulated through 20 mesh sieves.D) oven dry granulate: place 60 ℃ of dryings of baking oven to take out in 3 hours, with 20 mesh sieve granulate.E) total mixing: add the Pulvis Talci that weighs up, evenly mixed.F) tabletting: semi-finished product are measured particulate content and are determined the heavy back of sheet tabletting, promptly.
Estimate: 2.9 minutes disintegrations, melt that to become the time limit up to specification (according to two appendix XA of Chinese Pharmacopoeia version in 2005, XB).
Embodiment 4: Terbinafine hydrochloride vaginal effervescent tablet, and its prescription consists of:
Terbinafine HCl 150g
Lactose 100g
Tartaric acid 120g
Sodium bicarbonate 130g
Crospolyvinylpyrrolidone 15g
Sodium lauryl sulphate 10g
Micropowder silica gel 10g
Make 1000
Preparation process: a) supplementary material is handled: required supplementary material is all crossed 100 sieves and is handled.B) batch mixing: the supplementary material that takes by weighing recipe quantity is according to the equivalent method mix homogeneously that progressively increases.C) granulate: adopt rolling process to make the medicine cake, granulate through 20 mesh sieves.D) total mixing: add the lubricant of recipe quantity, evenly mixed.E) tabletting: semi-finished product are measured drug content and are determined the heavy back of sheet tabletting, promptly.
Estimate: 2.8 minutes disintegrations, melt that to become the time limit up to specification (according to two appendix XA of Chinese Pharmacopoeia version in 2005, XB).
Claims (9)
1, a kind of Terbinafine hydrochloride vaginal effervescent tablet comprises following component, all is weight percentage; Terbinafine HCl 10-75%, effervescent adjuvant 10-50%, other adjuvants 0.5-50%.
2, a kind of according to claim 1 Terbinafine hydrochloride vaginal effervescent tablet is characterized in that, the effervescent adjuvant is the combination of organic acid and carbonate, and used organic acid comprises one or more of citric acid, tartaric acid, fumaric acid, malic acid; Used carbonate is a kind of of sodium carbonate, sodium bicarbonate or both mixture.
3, a kind of according to claim 1 Terbinafine hydrochloride vaginal effervescent tablet is characterized in that, other adjuvants comprise that one or more and surfactant of binding agent, lubricant, diluent, disintegrating agent form.
4, as other adjuvants of Terbinafine hydrochloride vaginal effervescent tablet as described in the claim 3, binding agent is one or more of hydroxypropyl methylcellulose, polyvinylpyrrolidone and dehydrated alcohol.
5, as other adjuvants of Terbinafine hydrochloride vaginal effervescent tablet as described in the claim 3, lubricant is a Pulvis Talci, one or more of micropowder silica gel and magnesium stearate.
6, as other adjuvants of Terbinafine hydrochloride vaginal effervescent tablet as described in the claim 3, diluent is one or more of starch, microcrystalline Cellulose, lactose and dextrin.
7, as other adjuvants of Terbinafine hydrochloride vaginal effervescent tablet as described in the claim 3, disintegrating agent is one or more of low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crospolyvinylpyrrolidone and cross-linking sodium carboxymethyl cellulose.
8, as Terbinafine hydrochloride vaginal effervescent tablet as described in the claim 3, it is characterized in that surfactant is one or more of sodium lauryl sulphate, sodium laurylsulfate and tween, the present invention is preferably sodium lauryl sulphate.
9, a kind of according to claim 1 Terbinafine hydrochloride vaginal effervescent tablet is characterized in that adopting following prepared: a, direct compression; B, wet granule compression tablet; C, dry granulation tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810015601A CN101543479A (en) | 2008-03-24 | 2008-03-24 | Terbinafine hydrochloride vaginal effervescent tablet and preparation method thereof |
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| CN200810015601A CN101543479A (en) | 2008-03-24 | 2008-03-24 | Terbinafine hydrochloride vaginal effervescent tablet and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102670561A (en) * | 2012-05-25 | 2012-09-19 | 济南康和医药科技有限公司 | Vaginal effervescent tablet with biological adhesiveness and preparation process thereof |
| 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 |
| 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 |
| CN112220763A (en) * | 2020-10-21 | 2021-01-15 | 上海桓华制药有限公司 | Terbinafine hydrochloride effervescent tablet and use method thereof |
-
2008
- 2008-03-24 CN CN200810015601A patent/CN101543479A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102670561A (en) * | 2012-05-25 | 2012-09-19 | 济南康和医药科技有限公司 | Vaginal effervescent tablet with biological adhesiveness and preparation process thereof |
| 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 |
| 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 |
| CN112220763A (en) * | 2020-10-21 | 2021-01-15 | 上海桓华制药有限公司 | Terbinafine hydrochloride effervescent tablet and use method thereof |
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Addressee: Shao Changkai Document name: Notification of Publication of the Application for Invention |
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Open date: 20090930 |