CN104800148A - Clotrimazole emulsifiable paste and preparation method thereof - Google Patents
Clotrimazole emulsifiable paste and preparation method thereof Download PDFInfo
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- CN104800148A CN104800148A CN201510188090.6A CN201510188090A CN104800148A CN 104800148 A CN104800148 A CN 104800148A CN 201510188090 A CN201510188090 A CN 201510188090A CN 104800148 A CN104800148 A CN 104800148A
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Abstract
The invention discloses clotrimazole emulsifiable paste and a preparation method thereof. Every 100 g of the emulsifiable paste contains the following raw materials by weight: 0.5-15.0 g of clotrimazole, 0.4-2.0 g of sorbitan monostearate, 2.0-5.0 g of Tween 60, 2.0-10.0 g of cetostearyl alcohol, 10.0-30.0 g of isopropylmyristate, 1.0-5.0 g of glycerin monostearate, 0.5-2.0 g of phenylcarbinol and the balance of water.
Description
Technical field
The invention belongs to field of chemical medicine preparation, be specifically related to a kind ofly be used for the treatment of clotrimazole cream of monilial vaginitis and the microbial infectious leucorrhea of yeast and preparation method thereof.
Background technology
According to statistics, the sickness rate of gynaecopathia is about 70% in recent years, and most of women all can be subject to the puzzlement of urinary system infection to some extent.And in China, women of child-bearing age's candidal vaginitis is a kind of common gynaecopathia, caused by candida albicans infection.Primary disease cardinal symptom is pruritus vulvae and leucorrhea is white sample, and the sickness rate of primary disease is only second to trichomonal vaginitis.According to estimates, 75% women trimester of pregnancy this disease at least fall ill once, wherein 40% ~ 50% can show effect secondary, adult women's recurrent exerbation of about 5%.Being most suitable for the pH value that candidiasis grows is 5.5 ~ 6.5, and when in vagina, glycogen increases, when acidity increases, namely can cause inflammation generation, therefore be more common in anemia of pregnant woman.Candidiasis can be present in the oral cavity of people, intestinal and vaginal mucosa and not to cause symptom, and the candidiasis at these three positions can infect mutually, the susceptible disease when local environmental conditions is applicable to.
Clotrimazole is imidazoles broad-spectrum antifungal medicine, for candidal vulvovaginitis and the microbial infectious leucorrhea of yeast, has better antibacterial action to multiple fungus especially Candida albicans.Its mechanism of action is the synthesis of Antifungi cell membrane, and affects its metabolic process.Mainly by suppressing the synthesis of ergosterol, cause the 26S Proteasome Structure and Function of cytoplasmic membrane impaired to the suppression of ergosterol synthesis.Clotrimazole all has good antifungal activity with external in vivo, comprising dermatophytes, yeast and mycete etc.At present, what go on the market at home is used for the treatment of the Gyno Canesten (Canesten) that colpitic clotrimazole cream only has Bayer Bitterfeld GmbH (Bayer).
Summary of the invention
The present invention is intended to overcome the deficiencies in the prior art, provides a kind of clotrimazole cream and preparation method thereof.
In order to achieve the above object, technical scheme provided by the invention is:
Containing, for example the raw material of lower weight in clotrimazole cream described in every 100g: clotrimazole 0.5-15.0g, preferred 10.0g; Sorbester p18 0.4-2.0g, preferred 1.0g; Polysorbate60 2.0-5.0g, preferred 3.68g; Cetostearyl alcohol 2.0-10.0g, preferred 4g; Isopropyl myristate 10.0-30.0g, preferred 19.0g; Glyceryl monostearate 1.0-5.0g, preferred 3g; Benzyl alcohol 0.5-2.0g, preferred 1.0g; Surplus is water, preferred purified water.
Wherein, described clotrimazole is present in clotrimazole cream with the state of suspendible, and clotrimazole particle size range is 3 μm-30 μm.
The preparation method of above-mentioned clotrimazole cream comprises the steps:
(1) aqueous phase is prepared: drop in aqueous phase tank by benzyl alcohol and weight for the water preparing total Water weight half needed for clotrimazole cream, stir 10-30min in 70 ± 5 DEG C, obtain aqueous phase, for subsequent use;
(2) prepare oil phase: add in oil phase tank by sorbester p18, Part I polysorbate60, cetostearyl alcohol, isopropyl myristate and glyceryl monostearate, stir 20-30min in 75 ± 5 DEG C, obtain oil phase, for subsequent use;
(3) clotrimazole decentralized photo is prepared: Part II polysorbate60 is added weight for preparing in the water of total Water weight half needed for clotrimazole cream, stir 10-20min in 70 ± 5 DEG C, then add clotrimazole, stir 20-40min in 55 ± 5 DEG C, obtain clotrimazole decentralized photo, for subsequent use;
(4) emulsifiable paste is prepared: proceed in emulsion tank by aqueous phase and oil phase, 20-30min is stirred under vacuum 0.03 ± 0.02MPa condition, then homogenizing 10-20min, clotrimazole decentralized photo is added after cooling the temperature to 55 ± 5 DEG C, continue homogenizing 50-70min, be cooled to 45 ± 5 DEG C, namely potting obtains clotrimazole cream;
Wherein, the weight ratio of the described Part I polysorbate60 of step (2) and Part II polysorbate60 is 180-185:1.
Pruritus vulvae caused by urinary system infection and leucorrhea abnormal often allow women patient be difficult to stand, clotrimazole cream specification of the present invention is 10% (w/w), compared with the clotrimazole cream of domestic 1% or 3% specification, be used for the treatment of monilial vaginitis and the microbial infectious leucorrhea of yeast, there is less dosage and the curative effect of Geng Jia.
Detailed description of the invention
Embodiment 1
Containing following weight raw material in every 100g clotrimazole cream: clotrimazole 1.0g, sorbester p18 1.0g, polysorbate60 3.86g, cetostearyl alcohol 4.0g, isopropyl myristate 9.0g, glyceryl monostearate 3.0g, benzyl alcohol 1.0g, surplus is purified water.Wherein, described clotrimazole is present in clotrimazole cream with the state of suspendible, and clotrimazole particle size range is 3 μm-30 μm.
The preparation method of described clotrimazole cream, comprises the steps:
(1) aqueous phase is prepared: drop in aqueous phase tank by benzyl alcohol and weight for the purified water preparing total Water weight half needed for clotrimazole cream, stir 10min in 70 DEG C, obtain aqueous phase, for subsequent use;
(2) prepare oil phase: add in oil phase tank by oil phase material sorbester p18, polysorbate60 3.36g, cetostearyl alcohol, isopropyl myristate and glyceryl monostearate, stir 20min in 75 DEG C, obtain oil phase, for subsequent use;
(3) clotrimazole decentralized photo is prepared: 0.5g polysorbate60 is added weight for preparing in the purified water of total Water weight half needed for clotrimazole cream, stir 20min in 70 DEG C, more slowly add clotrimazole, stir 30min in 55 DEG C, obtain clotrimazole decentralized photo, for subsequent use;
(4) prepare emulsifiable paste: proceed in emulsion tank by above-mentioned aqueous phase and oil phase, in emulsion tank, vacuum is stir 30min under the condition of 0.03MPa, then homogenizing 0min, cool the temperature to 55 DEG C, add clotrimazole decentralized photo, continue homogenizing 50min, be cooled to 45 DEG C, potting and get final product.
Embodiment 2
Containing following weight raw material in every 100g clotrimazole cream: clotrimazole 10.0g, sorbester p18 1.0g, polysorbate60 3.96g (getting 0.1g for the preparation of clotrimazole decentralized photo), cetostearyl alcohol 4.0g, isopropyl myristate 19.0g, glyceryl monostearate 3.0g, benzyl alcohol 1.0g, surplus is purified water.
The preparation method of described clotrimazole cream is with embodiment 1.
Embodiment 3
Containing following weight raw material in every 100g clotrimazole cream: clotrimazole 10.0g, sorbester p18 1.5g, polysorbate60 3.75g, cetostearyl alcohol 3.0g, isopropyl myristate 5.0g, glyceryl monostearate 1.0g, benzyl alcohol 1.0g, surplus is purified water.
The preparation method of described clotrimazole cream is with embodiment 1.
Embodiment 4
Containing following weight raw material in every 100g clotrimazole cream: clotrimazole 10.0g, sorbester p18 1.0g, polysorbate60 3.08g, cetostearyl alcohol 4.0g, isopropyl myristate 20.0g, glyceryl monostearate 3.0g, benzyl alcohol 1.0g, surplus is purified water.
The preparation method of described clotrimazole cream is with embodiment 1.
The different formulation and technology clotrimazole cream of embodiment 5 is on the impact of mice bacterial vaginitis
This experimental study adopts staphylococcus aureus associating escherichia coli to set up mice bacterial vaginitis, observes clotrimazole cream to the colpitic therapeutical effect of mice.
1. experiment material
1.1 test sample
Clotrimazole cream technique A, B, C, thered is provided by Hunan Province's Experimental Animal Center, content: 10%w/w, specification: 100mg/g, lot number: 150301,150302,150303, formulation and technology is respectively embodiment 1 (A), embodiment 2 (B) and embodiment 3 (C), valid until in February, 2017.
1.2 positive reference substance
Clotrimazole cream (commercially available) is purchased from Bayer HealthCare Co, content: 10%w/w, specification: 100mg/g, lot number: 2B2002, valid until in October, 2015.
1.3 laboratory animal
ICR mice 90, SPF level, female, body weight 18 ~ 22g, above animal is all purchased from Hunan Si Laike Jing Da laboratory animal company limited, laboratory animal production licence number: SCXK (Hunan) 2011-0003, the Quality of Experimental Animals quality certification number: NO.43004700010625; Raise at Drug Safety Evaluation Center of Hunan Province's barrier environment, the laboratory animal usage license
Card number: SYXK (Hunan) 2010-0008.
1.4 experimental strain
Clinical strains: staphylococcus aureus (10
9cfu/ml), escherichia coli (10
9cfu/ml) the scorching patient of recurrent vaginal, provided by microorganism teaching and research room of Hunan University of Traditional Chinese Medicine and identified, above-mentioned 2 kinds of pathogenic bacterium equal-volumes are mixed into modeling bacterium.
1.5 instrument
Photobiology microscope YS-100 (Japanese Nikon instrument plant product); Absorbable gelatin sponge, Xiang En medical science and technology Development Co., Ltd of Jiangxi Province, No. 3641709th, state's pencil tool (standard) word 2012
2. test method
By female mice subcutaneous injection phthalic acid estradiol suspension,sterile 2mg/ml 0.05ml, continuous 3 times, 2 days 1 time.In the 6th day, 20 μ l antibacterial mixing modeling liquid are injected sponge, to inject the sponge plug of strain in mouse vagina, adopt vaginal secretions smear with aseptic little cotton swab, Grams dyeing microscopic examination in postvaccinal 4th day, observe the growing state of mycelia and blastopore, to determine to infect successfully.Select 50 vaginitis model mices and be divided into 5 groups, be respectively model control group, clotrimazole cream, clotrimazole cream technique A, B, C group, separately establish blank group (do not infect and do not treat).Every day smears corresponding emulsifiable paste with intravaginal, continuous 10 days, every day 1 time.Observe the pathogen negative conversion rate of each treated animal vaginal secretions and the healing degree of vaginal mucosa inflammation.
3. statistical method
Adopt SPSS16.0 to carry out statistical analysis, the level set of statistical significance is P<0.05.Counting ranked data adopt frequency to represent, carry out the rank test of ranked data.
4. result
4.1 clotrimazole creams are on the impact of mouse vagina bacterial infection
As shown in table 1, the negative conversion rate of clotrimazole cream A, B, C group to staphylococcus aureus is respectively 30%, 60%, 20%, 20%, 60%, 10% is respectively to colibacillary negative conversion rate, compare with model control group, clotrimazole cream B infects staphylococcus aureus to mouse vagina, escherichia coli have significance therapeutical effect.The results are shown in Table 1.
The therapeutical effect of table 1 pair mouse vagina bacterial infection
Note: compare with blank group
+p<0.05,
++p<0.01; Compare with model control group
*p<0.05,
*p<0.01
5. discuss
Above result shows, clotrimazole cream technique B infects staphylococcus aureus to mouse vagina, escherichia coli have obvious therapeutical effect.
Claims (4)
1. a clotrimazole cream, is characterized in that, containing, for example the raw material of lower weight in clotrimazole cream described in every 100g: clotrimazole 0.5-15.0g; Sorbester p18 0.4-2.0g; Polysorbate60 2.0-5.0g; Cetostearyl alcohol 2.0-10.0g; Isopropyl myristate 10.0-30.0g; Glyceryl monostearate 1.0-5.0g; Benzyl alcohol 0.5-2.0g; Surplus is water.
2. clotrimazole cream as claimed in claim 1, is characterized in that, containing, for example the raw material of lower weight in clotrimazole cream described in every 100g: clotrimazole 10.0g; Sorbester p18 1.0g; Polysorbate60 3.68g; Cetostearyl alcohol 4g; Isopropyl myristate 19.0g; Glyceryl monostearate 3g; Benzyl alcohol 1.0g; Surplus is water.
3. clotrimazole cream as claimed in claim 1 or 2, it is characterized in that, described clotrimazole is present in clotrimazole cream with the state of suspendible, and clotrimazole particle size range is 3 μm-30 μm.
4. the preparation method of clotrimazole cream as claimed in claim 1 or 2, it is characterized in that, described method comprises the steps:
(1) aqueous phase is prepared: drop in aqueous phase tank by benzyl alcohol and weight for the water preparing total Water weight half needed for clotrimazole cream, stir 10-30min in 70 ± 5 DEG C, obtain aqueous phase, for subsequent use;
(2) prepare oil phase: add in oil phase tank by sorbester p18, Part I polysorbate60, cetostearyl alcohol, isopropyl myristate and glyceryl monostearate, stir 20-30min in 75 ± 5 DEG C, obtain oil phase, for subsequent use;
(3) clotrimazole decentralized photo is prepared: Part II polysorbate60 is added weight for preparing in the water of total Water weight half needed for clotrimazole cream, stir 10-20min in 70 ± 5 DEG C, then add clotrimazole, stir 20-40min in 55 ± 5 DEG C, obtain clotrimazole decentralized photo, for subsequent use;
(4) emulsifiable paste is prepared: proceed in emulsion tank by aqueous phase and oil phase, 20-30min is stirred under vacuum 0.03 ± 0.02MPa condition, then homogenizing 10-20min, clotrimazole decentralized photo is added after cooling the temperature to 55 ± 5 DEG C, continue homogenizing 10-50min, be cooled to 45 ± 5 DEG C, namely potting obtains clotrimazole cream;
Wherein, the weight ratio of the described Part I polysorbate60 of step (2) and Part II polysorbate60 is 180-185:1.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105012229A (en) * | 2015-08-25 | 2015-11-04 | 广东华润顺峰药业有限公司 | Clotrimazole cream and preparation method thereof |
| ES2562985A1 (en) * | 2015-12-31 | 2016-03-09 | Enrique Blanxart Sena | Pharmaceutical composition for the treatment of skin lesions (Machine-translation by Google Translate, not legally binding) |
| CN105456183A (en) * | 2015-12-15 | 2016-04-06 | 刘云 | Clotrimazole cream with good curative effect and stable quality and preparation method of clotrimazole cream |
| CN107998072A (en) * | 2017-12-26 | 2018-05-08 | 重庆希尔安药业有限公司 | clotrimazole cream and preparation method thereof |
| CN110237025A (en) * | 2019-06-12 | 2019-09-17 | 嘉实（湖南）医药科技有限公司 | A kind of clotrimazole cream and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1931163A (en) * | 2006-09-20 | 2007-03-21 | 西北农林科技大学 | Nanometer clotrimazole emulsion medicine and its prepn process |
| CN101890003A (en) * | 2009-11-16 | 2010-11-24 | 江苏亚邦强生药业有限公司 | Method for preparing novel chlorhexidine acetate cream |
-
2015
- 2015-04-20 CN CN201510188090.6A patent/CN104800148A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1931163A (en) * | 2006-09-20 | 2007-03-21 | 西北农林科技大学 | Nanometer clotrimazole emulsion medicine and its prepn process |
| CN101890003A (en) * | 2009-11-16 | 2010-11-24 | 江苏亚邦强生药业有限公司 | Method for preparing novel chlorhexidine acetate cream |
Non-Patent Citations (1)
| Title |
|---|
| 周秋松: "基质对克霉唑乳膏含量的影响", 《中国卫生产业》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105012229A (en) * | 2015-08-25 | 2015-11-04 | 广东华润顺峰药业有限公司 | Clotrimazole cream and preparation method thereof |
| CN105456183A (en) * | 2015-12-15 | 2016-04-06 | 刘云 | Clotrimazole cream with good curative effect and stable quality and preparation method of clotrimazole cream |
| ES2562985A1 (en) * | 2015-12-31 | 2016-03-09 | Enrique Blanxart Sena | Pharmaceutical composition for the treatment of skin lesions (Machine-translation by Google Translate, not legally binding) |
| CN107998072A (en) * | 2017-12-26 | 2018-05-08 | 重庆希尔安药业有限公司 | clotrimazole cream and preparation method thereof |
| CN110237025A (en) * | 2019-06-12 | 2019-09-17 | 嘉实（湖南）医药科技有限公司 | A kind of clotrimazole cream and preparation method thereof |
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Application publication date: 20150729 |