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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 PDF

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Publication number
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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CN
China
Prior art keywords
type spray
tween
medicine
solution type
arlacel
Prior art date
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Pending
Application number
CN 02111525
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Chinese (zh)
Inventor
张大志
孙青
姜远英
周廷森
吴义杰
吴秋业
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Second Military Medical University SMMU
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Second Military Medical University SMMU
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Second Military Medical University SMMU filed Critical Second Military Medical University SMMU
Priority to CN 02111525 priority Critical patent/CN1380060A/en
Publication of CN1380060A publication Critical patent/CN1380060A/en
Pending legal-status Critical Current

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明涉及医药技术领域,是外用抗真菌药物的溶液型喷雾剂型及其制备方法。本发明将咪康唑、硫康唑、肟康唑(奥昔康唑)、噻康唑、氯康唑、酮康唑、氟康唑、伊曲康唑或它们的硝酸盐,制成溶液型喷雾剂。其优点在于,使用方便卫生,可直接将药液喷于患处,药物均匀分布于皮肤表面,药物穿过液体基质的速度快,起效快。还可喷于病灶周围部位的鞋袜或其它覆盖物上,起到隔断传染源的作用。The invention relates to the technical field of medicine, and relates to a solution-type spray formulation of antifungal drugs for external use and a preparation method thereof. In the present invention, miconazole, sulconazole, oxiconazole (oxiconazole), tioconazole, cloconazole, ketoconazole, fluconazole, itraconazole or their nitrates are prepared into solutions type spray. The utility model has the advantages that it is convenient and hygienic to use, the medicine liquid can be directly sprayed on the affected part, the medicine is evenly distributed on the skin surface, the speed of the medicine passing through the liquid matrix is fast, and the effect is quick. It can also be sprayed on the footwear or other coverings around the lesion to isolate the source of infection.

Description

Solution type spray of antimycotic medicine for external application and preparation method thereof
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.
CN 02111525 2002-04-28 2002-04-28 Solution type spray of antimycotic medicine for external application and its preparation method Pending CN1380060A (en)

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

Applications Claiming Priority (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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CN1380060A true CN1380060A (en) 2002-11-20

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Cited By (9)

* Cited by examiner, † Cited by third party
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 Anti-ear fungus spray and its preparation method and spray device
CN111249219A (en) * 2018-11-30 2020-06-09 中南大学湘雅三医院 Ear drops for treating ear 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

Cited By (11)

* Cited by examiner, † Cited by third party
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 Preparations containing fish suppressant compounds "Hog" for topical administration and uses
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 Anti-ear fungus spray and its preparation method and spray device
CN111249219A (en) * 2018-11-30 2020-06-09 中南大学湘雅三医院 Ear drops for treating ear 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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