CN1380060A - Solution type spray of antimycotic medicine for external application and its preparation method - Google Patents
Solution type spray of antimycotic medicine for external application and its preparation method Download PDFInfo
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- CN1380060A CN1380060A CN 02111525 CN02111525A CN1380060A CN 1380060 A CN1380060 A CN 1380060A CN 02111525 CN02111525 CN 02111525 CN 02111525 A CN02111525 A CN 02111525A CN 1380060 A CN1380060 A CN 1380060A
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Abstract
The preparation method of solution type spraying agent for external application resisting eumycetes is characterized by that it uses micronazole, sulconazolenitrate, oxiconazole, thioconazole, chloconazole, ketoconazole, fluconazole, itraconazole or their nitrates as raw material and makes them into the invented solution type spraying agent which can be directly sprayed on the affected region, and can quickly obtain therapeutic effect, also can be sprayed on the shoe, sock or other cover round the focus so as to produce the action of isolating source of infection.
Description
Technical field: the present invention relates to medical technical field, is solution type spray of antimycotic medicine for external application and preparation method thereof.
Background technology: miconazole, sulconazole, oxime health azoles (oxiconazole), tioconazole, croconazole, ketoconazole, fluconazol, itraconazole or their nitrate, it is the antifungal drug of wide spectrum, efficient, low toxicity, be widely used in clinically both at home and abroad, the effect of treatment dermatophytosis, monilial infection is obvious.Its dosage form has cream, liniment, powder spray agent.But do not see solution type spray so far.The deficiency of cream is to pass cream base by medicine, and arrive to suffer from the speed of surface layer slower, thereby onset is slower.And painting medicine uses inconvenience, and often crawling is even to position that hair growth is arranged, is also wiped easily.The powder spray agent for be subject to medicated clothing friction or keratinization serious the position not too suitable, drug distribution is also inhomogeneous.
Summary of the invention: the present invention makes solution type spray with miconazole, sulconazole, oxime health azoles (oxiconazole), tioconazole, croconazole, ketoconazole, fluconazol, itraconazole or their nitrate.Its advantage is, health easy to use can directly be sprayed on the affected part with medicinal liquid, and medicine can be uniformly distributed in skin and suffer from surface layer, and it is fast that medicine passes the speed of fluid matrix, rapid-action.Be particularly useful for the large-area infection of body surface and the fungal infection at hair growth position.In addition, solution type spray also can be sprayed on the footgear or other covering at position around the focus, makes it play the effect that cuts off the source of infection.
The prescription and the proportioning of solution type spray of the present invention are as follows:
Antifungal drug 5-20g
Antioxidant 0.1-0.5g
Surfactant 5-60g
Propylene glycol 50-300ml
95% medicinal alcohol 400-800ml
Distilled water adds to 1000ml
Total amount 1000ml
Concrete preparation method is:
Proportioning by prescription is dissolved in antifungal agent and antioxidant 95% medicinal alcohol routinely, after the heating for dissolving, add surfactant and propylene glycol, stirring and evenly mixing, being placed to temperature is 25 ℃, adding distil water to cumulative volume is 1000ml, use membrane filtration, pack the medicinal liquid branch into medical airtight bottle, or the Manual pressure aerosol can, or the air-blast atomizing jar.
Above-described antifungal drug is miconazole, sulconazole, oxime health azoles (oxiconazole), tioconazole, croconazole, ketoconazole, fluconazol, itraconazole or their nitrate, and its concentration in preparation is 0.5-2% (w/v);
Described antioxidant can be selected 2,6 ditertiary butyl p cresol, BHA, thioglycerol for use; Its concentration in preparation is 0.01-0.05% (w/v);
Described surfactant can be selected tween 20, Tween-40, Tween-60, tween 80, the tween 85 of Tweens for use, the Arlacel-20 of spans, Arlacel-40, Arlacel-60, Arlacel-80, Arlacel-85, the poloxamer 188 of poloxamer class, poloxamer 338, poloxamer 407 can be selected any one independent use wherein for use; Also can select two class surfactants simultaneously for use, promptly any two apoplexy due to endogenous wind in above-mentioned three class surfactants respectively selects one, the mixing use; Also can select three class surfactants simultaneously for use, promptly in above-mentioned three class surfactants, respectively select one, mix and use; Its concentration in preparation is 0.5-6% (w/v);
The concentration of propylene glycol in preparation is 5-30% (v/v);
The concentration of ethanol in preparation is 40-80% (v/v).
The specific embodiment:
Embodiment one: prepare 1% sulconazole nitrate spray
Prescription:
Sulconazole nitrate 10.0g
2,6 ditertiary butyl p cresol (BHT) 0.1g
Tween 80 20.0g
Propylene glycol 100.0ml
95% medicinal alcohol 600.0ml
Distilled water adds to 1000ml
Total amount 1000ml
The concrete operations step:
With sulconazole nitrate 10.0g, 2,6-ditertbutylparacresol 0.1g is dissolved in 95% medicinal alcohol 600ml, after the 30-50 ℃ of heating for dissolving, add 20.0g tween 80,100ml propylene glycol, stirring and evenly mixing, being placed to temperature is 25 ℃, adding distil water to cumulative volume is 1000ml, use membrane filtration, with the medicinal liquid Manual pressure aerosol can of packing into.
Embodiment two: prepare 0.5% sulconazole nitrate spray
Prescription:
Sulconazole nitrate 5.0g
2,6 ditertiary butyl p cresol (BHT) 0.1g
Tween 80 20.0g
Propylene glycol 100.0ml
95% medicinal alcohol 600.0ml
Distilled water adds to total amount 1000ml
Total amount 1000ml
The concrete operations step:
With sulconazole nitrate 5.0g, 2,6-ditertbutylparacresol 0.1g is dissolved in 95% medicinal alcohol 600ml, after the 40-60 ℃ of heating for dissolving, add 20.0g tween 80,100ml propylene glycol, stirring and evenly mixing, being placed to temperature is 25 ℃, adding distil water to cumulative volume is 1000ml, use membrane filtration, with the medicinal liquid Pneumatic pressure aerosol can of packing into.
The prepared medicinal liquid of the present invention also can be used as liniment or lotion uses.The preparation method of the solution type spray of other antifungal agent is the same.
The animal efficacy of medicine observing of the solution type spray of external anti-fungal infection:
With the sulconazole nitrate spray is example:
Each 30 of Cavia porcelluss, male and female are not limit, and are divided into three groups, 10 every group.The back unhairing is used the sand paper scratch mark, inoculates the normal saline solution of Trichophyton mentagrophytes, makes the infection model of Trichophyton mentagrophytes, occurs erythema and edema after three days, implements administration.Give normal saline first group of every day, spray with 1% sulconazole nitrate spray second group of every day, and spray with 0.5% sulconazole nitrate spray the 3rd group of every day.Once a day, each consumption is that medicinal liquid evenly covers affected part.Respectively at administration the 5th day and 10 days, the skin lesion of observing Cavia porcellus improved situation and fungus removing situation.The index that skin lesion obviously improves is no erythema, no edema.The investigation method that fungus is removed situation is, gets the tissue of infection site and cultivates, and whether observe has conk.As do not have conk and be fungus and thoroughly remove.Observed result sees Table 1..
The animal efficacy of medicine observing of table 1. sulconazole nitrate spray
| Observing time | Observation index | The normal saline group | 0.5% sulconazole | 1% sulconazole |
| After the administration the 5th day | Skin lesion obviously improves number of animals (only) | ????0 | ????3 | ????8 |
| Fungus is thoroughly removed number of animals (only) | ????0 | ????1 | ????6 | |
| After the administration the 10th day | Skin lesion obviously improves number of animals (only) | ????2 | ????10 | ????10 |
| Fungus is thoroughly removed number of animals (only) | ????0 | ????10 | ????10 |
By table 1 as seen, 0.5% and 1% sulconazole nitrate spray is very obvious to the therapeutic effect that Trichophyton mentagrophytes infects Cavia porcellus.
Claims (4)
1. the solution type spray of antimycotic medicine for external application, formulated by antifungal drug, antioxidant, surfactant, propylene glycol, medicinal alcohol and water, it is characterized in that described antifungal drug is selected from miconazole, sulconazole, oxime health azoles (oxiconazole), tioconazole, croconazole, ketoconazole, fluconazol, itraconazole, or their nitrate.
2. by the solution type spray of the described antimycotic medicine for external application of claim 1, it is characterized in that described antioxidant is selected from 2,6 ditertiary butyl p cresol, or BHA, or thioglycerol.
3. press the solution type spray of claim 1 or 2 described antimycotic medicine for external application, it is characterized in that described surfactant is selected from 1-3 surfactant of Tweens, spans and poloxamer apoplexy due to endogenous wind, wherein Tweens selects one of tween 20, Tween-40, Tween-60, tween 80, tween 85, spans selects one of Arlacel-20, Arlacel-40, Arlacel-60, Arlacel-80, Arlacel-85, and the poloxamer class is selected one of poloxamer 188, poloxamer 338, poloxamer 407.
4. the preparation method of the solution type spray of the described antimycotic medicine for external application of claim 3, it is characterized in that the concentration of each composition in preparation is respectively: antifungal drug 0.5-2% (W/V), antioxidant 0.01-0.05% (W/V), surfactant 0.5-6% (W/V), propylene glycol 5-30% (V/V), medicinal alcohol 40-80% (V/V), by this proportioning antifungal agent and antioxidant are dissolved in 95% medicinal alcohol, after the heating for dissolving, add surfactant and propylene glycol, stirring and evenly mixing, being placed to temperature is 25 ℃, and adding distil water filters to corresponding volume again, pack the medicinal liquid branch into medical airtight bottle, as liniment or lotion; Be sub-packed in aerosol can, as spray.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02111525 CN1380060A (en) | 2002-04-28 | 2002-04-28 | Solution type spray of antimycotic medicine for external application and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02111525 CN1380060A (en) | 2002-04-28 | 2002-04-28 | Solution type spray of antimycotic medicine for external application and its preparation method |
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| Publication Number | Publication Date |
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| CN1380060A true CN1380060A (en) | 2002-11-20 |
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| CN 02111525 Pending CN1380060A (en) | 2002-04-28 | 2002-04-28 | Solution type spray of antimycotic medicine for external application and its preparation method |
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102198153A (en) * | 2011-06-14 | 2011-09-28 | 李平 | Nano-silver spray for treating skin diseases, and preparation method thereof |
| CN102321036A (en) * | 2011-07-13 | 2012-01-18 | 王健祥 | Preparation method of fluconazole soluble salt |
| WO2016196928A1 (en) * | 2015-06-04 | 2016-12-08 | PellePharm, Inc. | Topical formulations for delivery of hedgehog inhibitor compounds and use thereof |
| CN106580929A (en) * | 2016-12-02 | 2017-04-26 | 贺敏 | Skin disease medicine composition, preparation method and application thereof |
| CN108379343A (en) * | 2018-03-09 | 2018-08-10 | 广州卡士德汽车用品有限公司 | A kind of shoes bactericidal deodorant and preparation method thereof |
| CN111249233A (en) * | 2018-11-30 | 2020-06-09 | 中南大学湘雅三医院 | Ear canal fungus resisting spray, preparation method thereof and spraying device |
| CN111249219A (en) * | 2018-11-30 | 2020-06-09 | 中南大学湘雅三医院 | Ear drop for treating ear canal fungus and preparation method thereof |
| CN112043714A (en) * | 2020-09-25 | 2020-12-08 | 安徽省公众检验研究院有限公司 | Preparation method of compound miconazole spraying agent |
| CN112957319A (en) * | 2021-02-05 | 2021-06-15 | 王京海 | Antifungal liquid and preparation method and application thereof |
-
2002
- 2002-04-28 CN CN 02111525 patent/CN1380060A/en active Pending
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102198153A (en) * | 2011-06-14 | 2011-09-28 | 李平 | Nano-silver spray for treating skin diseases, and preparation method thereof |
| CN102321036A (en) * | 2011-07-13 | 2012-01-18 | 王健祥 | Preparation method of fluconazole soluble salt |
| WO2016196928A1 (en) * | 2015-06-04 | 2016-12-08 | PellePharm, Inc. | Topical formulations for delivery of hedgehog inhibitor compounds and use thereof |
| IL256070A (en) * | 2015-06-04 | 2018-01-31 | Pellepharm Inc | Topical formulations for delivery of hedgehog inhibitor compounds and use thereof |
| CN106580929A (en) * | 2016-12-02 | 2017-04-26 | 贺敏 | Skin disease medicine composition, preparation method and application thereof |
| CN108379343A (en) * | 2018-03-09 | 2018-08-10 | 广州卡士德汽车用品有限公司 | A kind of shoes bactericidal deodorant and preparation method thereof |
| CN111249233A (en) * | 2018-11-30 | 2020-06-09 | 中南大学湘雅三医院 | Ear canal fungus resisting spray, preparation method thereof and spraying device |
| CN111249219A (en) * | 2018-11-30 | 2020-06-09 | 中南大学湘雅三医院 | Ear drop for treating ear canal fungus and preparation method thereof |
| CN111249219B (en) * | 2018-11-30 | 2023-08-11 | 中南大学湘雅三医院 | Ear drops for treating fungus in auditory canal and preparation method thereof |
| CN112043714A (en) * | 2020-09-25 | 2020-12-08 | 安徽省公众检验研究院有限公司 | Preparation method of compound miconazole spraying agent |
| CN112957319A (en) * | 2021-02-05 | 2021-06-15 | 王京海 | Antifungal liquid and preparation method and application thereof |
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