CN102846655A - Formulation and preparation method of antibacterial spray - Google Patents
Formulation and preparation method of antibacterial spray Download PDFInfo
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- CN102846655A CN102846655A CN2012103938132A CN201210393813A CN102846655A CN 102846655 A CN102846655 A CN 102846655A CN 2012103938132 A CN2012103938132 A CN 2012103938132A CN 201210393813 A CN201210393813 A CN 201210393813A CN 102846655 A CN102846655 A CN 102846655A
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- polyhexamethylene guanidine
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- 230000000844 anti-bacterial effect Effects 0.000 title claims abstract description 32
- 239000007921 spray Substances 0.000 title claims abstract description 25
- 239000000203 mixture Substances 0.000 title claims description 6
- 238000002360 preparation method Methods 0.000 title abstract description 4
- 238000009472 formulation Methods 0.000 title description 3
- 229920001661 Chitosan Polymers 0.000 claims abstract description 49
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims abstract description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 14
- -1 polyhexamethylene guanidine Polymers 0.000 claims abstract description 13
- 229930003427 Vitamin E Natural products 0.000 claims abstract description 9
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims abstract description 9
- 235000011187 glycerol Nutrition 0.000 claims abstract description 9
- 229940046009 vitamin E Drugs 0.000 claims abstract description 9
- 235000019165 vitamin E Nutrition 0.000 claims abstract description 9
- 239000011709 vitamin E Substances 0.000 claims abstract description 9
- 239000004480 active ingredient Substances 0.000 claims abstract description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 12
- 238000003381 deacetylation reaction Methods 0.000 claims description 7
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 6
- 230000006196 deacetylation Effects 0.000 claims description 6
- 238000003756 stirring Methods 0.000 claims description 6
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 3
- PUAQLLVFLMYYJJ-UHFFFAOYSA-N 2-aminopropiophenone Chemical compound CC(N)C(=O)C1=CC=CC=C1 PUAQLLVFLMYYJJ-UHFFFAOYSA-N 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 238000005457 optimization Methods 0.000 claims 2
- 230000008961 swelling Effects 0.000 claims 1
- 210000004400 mucous membrane Anatomy 0.000 abstract description 9
- 230000029663 wound healing Effects 0.000 abstract description 7
- 241000222122 Candida albicans Species 0.000 abstract description 4
- 241000588724 Escherichia coli Species 0.000 abstract description 4
- 241000191967 Staphylococcus aureus Species 0.000 abstract description 4
- 229940095731 candida albicans Drugs 0.000 abstract description 4
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 206010048038 Wound infection Diseases 0.000 abstract description 3
- 244000052616 bacterial pathogen Species 0.000 abstract description 3
- 230000012010 growth Effects 0.000 abstract description 3
- 231100000344 non-irritating Toxicity 0.000 abstract description 3
- 230000002439 hemostatic effect Effects 0.000 abstract description 2
- 239000002904 solvent Substances 0.000 abstract description 2
- 208000027418 Wounds and injury Diseases 0.000 description 6
- 206010052428 Wound Diseases 0.000 description 5
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 230000001580 bacterial effect Effects 0.000 description 3
- 230000023597 hemostasis Effects 0.000 description 3
- 239000003899 bactericide agent Substances 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 230000007794 irritation Effects 0.000 description 2
- 230000005012 migration Effects 0.000 description 2
- 238000013508 migration Methods 0.000 description 2
- 230000035699 permeability Effects 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 230000005855 radiation Effects 0.000 description 2
- 229920002101 Chitin Polymers 0.000 description 1
- 208000004756 Respiratory Insufficiency Diseases 0.000 description 1
- 206010038678 Respiratory depression Diseases 0.000 description 1
- 208000031737 Tissue Adhesions Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 210000001188 articular cartilage Anatomy 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 210000002421 cell wall Anatomy 0.000 description 1
- 230000035605 chemotaxis Effects 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 230000009545 invasion Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 230000036573 scar formation Effects 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 210000002536 stromal cell Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000017423 tissue regeneration Effects 0.000 description 1
- 230000007838 tissue remodeling Effects 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
Classifications
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明公开了一种具有抗菌、止血和促进伤口愈合的抗菌喷雾剂的配方及制备方法，该喷雾剂以水为溶剂，以壳聚糖、甘油、聚六亚甲基胍、维生素E为主要有效成分。本发明对多种病原菌的生长有明显的抑制活性，对金黄色葡萄球菌、大肠杆菌、白色念珠菌的杀灭率可达99％。且对皮肤和粘膜无刺激性，适用于皮肤和粘膜创面感染的治疗，并可促进伤口的愈合。The invention discloses a formula and a preparation method of an antibacterial spray with antibacterial, hemostatic and wound healing promotion properties. The spray uses water as a solvent and mainly uses chitosan, glycerin, polyhexamethylene guanidine and vitamin E. Active ingredients. The invention has obvious inhibitory activity on the growth of various pathogenic bacteria, and the killing rate on Staphylococcus aureus, Escherichia coli and Candida albicans can reach 99%. It is non-irritating to the skin and mucous membrane, and is suitable for the treatment of wound infection of the skin and mucous membrane, and can promote wound healing.
Description
技术领域 technical field
本发明涉及一种具有抗菌、止血并能促进伤口愈合的抗菌喷雾剂的配方及制备方法，该喷雾剂以水为溶剂，以壳聚糖、甘油、聚六亚甲基胍、维生素E为主要有效成分。本发明对多种病原菌的生长有明显的抑制活性，对金黄色葡萄球菌、大肠杆菌、白色念珠菌的杀灭率可达99％。且对皮肤和粘膜无刺激性，适用于皮肤和粘膜创面感染的治疗，并可促进伤口的愈合。The invention relates to a formulation and preparation method of an antibacterial spray with antibacterial, hemostatic and capable of promoting wound healing. The spray uses water as a solvent and mainly uses chitosan, glycerin, polyhexamethylene guanidine, and vitamin E. Active ingredients. The invention has obvious inhibitory activity on the growth of various pathogenic bacteria, and the killing rate on Staphylococcus aureus, Escherichia coli and Candida albicans can reach 99%. It is non-irritating to the skin and mucous membrane, and is suitable for the treatment of wound infection of the skin and mucous membrane, and can promote wound healing.
技术背景 technical background
创伤是日常生活中最常见的疾病之一，主要包括皮肤和粘膜创面损伤。市场上治疗创伤的方法主要有粉末类药物、创可贴、软膏类药物和液体辅料等。目前的药物对创面的刺激性已经基本解决，但存在药物的防水性和透气性较差，生物相容性和降解性不够理想等问题。本发明提供了一种抗菌、止血并能促进伤口愈合的喷雾剂，以聚六亚甲基胍为主要抗菌剂，利用壳聚糖的止血和促进伤口愈合的功能，并添加适量的甘油和维生素E来增加喷雾剂和创面的亲和度，用于皮肤和粘膜创面的治疗。该喷雾剂喷于皮肤表面时，会在皮肤表面形成一层几乎不会被察觉的薄膜，没有不舒适的感觉，并能起到防水、防尘、阻止微生物入侵等作用。Trauma is one of the most common diseases in daily life, mainly including skin and mucous membrane wound injuries. The methods for treating wounds on the market mainly include powdered medicines, band-aids, ointment medicines and liquid auxiliary materials. The irritation of the current drugs to the wound surface has been basically solved, but there are problems such as poor water resistance and air permeability of the drugs, and unsatisfactory biocompatibility and degradability. The invention provides a spray that is antibacterial, hemostasis and capable of promoting wound healing. It uses polyhexamethylene guanidine as the main antibacterial agent, utilizes chitosan's functions of hemostasis and wound healing, and adds an appropriate amount of glycerin and vitamin E to increase the affinity of the spray and the wound surface for the treatment of skin and mucous membrane wounds. When the spray is sprayed on the skin surface, it will form a film on the skin surface that is almost imperceptible, without uncomfortable feeling, and can play the roles of waterproof, dustproof, and preventing microbial invasion.
壳聚糖是甲壳质N-脱乙酰基的产物，是一种天然直链状氨基多糖。壳聚糖具有很好的成膜性、通透性、吸附性、生物降解性、生物相容性和生物可吸收性等特点，已广为关注。壳聚糖能促进纤维细胞的迁移，对基质细胞有趋化、迁移、激活的作用，并加速细胞增殖和组织重塑过程，促进皮肤组织修复，有加速伤口愈合和止血作用。壳聚糖的网络结构，使之具有预防组织粘连、抑制疤痕形成以及保护关节软骨等生理功能。Chitosan is the product of N-deacetylation of chitin and is a natural linear amino polysaccharide. Chitosan has the characteristics of good film-forming, permeability, adsorption, biodegradability, biocompatibility and bioabsorbability, and has been widely concerned. Chitosan can promote the migration of fibroblasts, have chemotaxis, migration, and activation effects on stromal cells, accelerate cell proliferation and tissue remodeling, promote skin tissue repair, and accelerate wound healing and hemostasis. The network structure of chitosan enables it to have physiological functions such as preventing tissue adhesion, inhibiting scar formation and protecting articular cartilage.
壳聚糖的主要杀菌机理是壳聚糖分子进入细菌细胞内，破坏DNA到RNA的转录，致细菌繁殖终止或者是带正电荷的壳聚糖分子通过库仑作用吸附带负电荷的细菌细胞壁，使其呼吸抑制而死亡。实验表明，壳聚糖的杀菌效力与其分子量和脱乙酰度有关，以平均分子量1500-4000，脱乙酰度80-95％的壳聚糖的杀菌效力最好。The main bactericidal mechanism of chitosan is that chitosan molecules enter the bacterial cells, destroying the transcription of DNA to RNA, causing the termination of bacterial reproduction or positively charged chitosan molecules adsorbing negatively charged bacterial cell walls through Coulomb action, making He died of respiratory depression. Experiments have shown that the bactericidal effect of chitosan is related to its molecular weight and deacetylation degree, and the bactericidal effect of chitosan with an average molecular weight of 1500-4000 and a degree of deacetylation of 80-95% is the best.
虽然壳聚糖具有一定的杀菌功能，但其杀菌效果并不理想。因此本发明加入聚六亚甲基胍作为杀菌剂，使杀菌效果大幅增加。聚六亚甲基胍是一种高效的杀菌剂，水溶性好，且对皮肤和粘膜无刺激，研究表明本发明对金黄色葡萄球菌、大肠杆菌和白色念珠菌的杀灭率可达99％。Although chitosan has a certain bactericidal function, its bactericidal effect is not ideal. Therefore, the present invention adds polyhexamethylene guanidine as a bactericide, so that the bactericidal effect is greatly increased. Polyhexamethyleneguanidine is a high-efficiency bactericide with good water solubility and no irritation to skin and mucous membranes. Studies have shown that the present invention can kill 99% of Staphylococcus aureus, Escherichia coli and Candida albicans .
基于上述物质各自的生理活性，本发明将其配伍，以制备一种抗菌喷雾剂服务于广大患者。Based on the respective physiological activities of the above substances, the present invention combines them to prepare an antibacterial spray to serve the majority of patients.
发明内容 Contents of the invention
本发明的目的是提供一种抗菌喷雾剂的配方及制备方法。本发明提供的抗菌喷雾剂具有广谱抗菌性，对多种病原菌的生长有明显的抑制活性，对金黄色葡萄球菌、大肠杆菌、白色念珠菌的灭菌率可达99％，且对皮肤和粘膜无刺激性，适用于皮肤和粘膜创面感染的治疗。The object of the present invention is to provide a formula and preparation method of antibacterial spray. The antibacterial spray provided by the invention has broad-spectrum antibacterial property, has obvious inhibitory activity to the growth of various pathogenic bacteria, and can reach 99% to the sterilizing rate of Staphylococcus aureus, Escherichia coli, Candida albicans, and has good effect on skin and skin. Non-irritating to mucous membranes, it is suitable for the treatment of skin and mucous membrane wound infections.
本发明的技术方案如下：Technical scheme of the present invention is as follows:
1、一种抗菌喷雾剂，其特征在于，以壳聚糖、甘油、聚六亚甲基胍、维生素E为主要有效成分。1. An antibacterial spray, characterized in that it takes chitosan, glycerin, polyhexamethyleneguanidine and vitamin E as main active ingredients.
2、根据权利要求1所述的抗菌喷雾剂，其特征在于，壳聚糖的含量为0.01-0.1％，所述的壳聚糖为高聚壳聚糖及低聚壳聚糖，壳聚糖衍生物包括但不局限于，羧甲基壳聚糖、硫酸羧甲基壳聚糖、硫酸壳聚糖、羧化壳聚糖、硫化壳聚糖、羟基化壳聚糖或壳聚糖季铵盐中的至少一种。2. The antibacterial spray according to claim 1, characterized in that the content of chitosan is 0.01-0.1%, and said chitosan is high polychitosan and low polychitosan, chitosan Derivatives include, but are not limited to, carboxymethyl chitosan, carboxymethyl chitosan sulfate, chitosan sulfate, carboxylated chitosan, sulfurized chitosan, hydroxylated chitosan or chitosan quat at least one of the salts.
3、根据权利要求1所述的抗菌喷雾剂，其特征在于，聚六亚甲基胍的含量为0.1-1％。3. The antibacterial spray according to claim 1, characterized in that the content of polyhexamethyleneguanidine is 0.1-1%.
4、根据权利要求1和2所述的抗菌喷雾剂，其特征在于，所述壳聚糖的分子量在1500-6000之间，脱乙酰度为60-95％。4. The antibacterial spray according to claims 1 and 2, characterized in that the chitosan has a molecular weight of 1500-6000 and a deacetylation degree of 60-95%.
5、根据权利要求4所述的抗菌喷雾剂，其特征在于，所述的壳聚糖分子量优化在1500-4000之间，脱乙酰度优化为80-95％。5. The antibacterial spray according to claim 4, characterized in that the chitosan molecular weight is optimally between 1500-4000, and the deacetylation degree is optimally 80-95%.
6、根据权利要求1所述的抗菌喷雾剂，其特征在于，壳聚糖和聚六亚甲基胍分别溶于水，并将两者混合均匀后，滴加适量的甘油和维生素E，再混合并定容至所需要体积即可。6. The antibacterial spray according to claim 1, characterized in that chitosan and polyhexamethyleneguanidine are dissolved in water respectively, and after the two are mixed evenly, an appropriate amount of glycerin and vitamin E are added dropwise, and then Mix and make up to the desired volume.
7、根据权利要求1所述的抗菌喷雾剂，其特征在于，壳聚糖的溶解方法为：取壳聚糖适量至烧杯中，加水适量溶胀，静置，如果不溶解可滴加稀醋酸，边滴边搅拌至溶解并放置1-2h。7. The antibacterial spray according to claim 1, characterized in that the dissolving method of chitosan is as follows: take an appropriate amount of chitosan into a beaker, add an appropriate amount of water to swell, let it stand, if it does not dissolve, add dilute acetic acid dropwise, Stir while dripping until dissolved and place for 1-2h.
具体实施方式Detailed ways
实施例1：Example 1:
取羧甲基壳聚糖0.6g至1L的烧杯中，加水300mL溶胀，静置，如不溶解可滴加稀醋酸，边滴加边搅拌至溶解，放置1h。另取聚六亚甲基胍5g加水溶解。将聚六亚甲基胍溶液加入壳聚糖溶液中混合均匀，再加甘油和维生素E适量混合，再加水补足体积，搅拌均匀后，灌装、辐射灭菌，即可。Take 0.6g of carboxymethyl chitosan into a 1L beaker, add 300mL of water to swell, and let it stand still. If it does not dissolve, add dilute acetic acid dropwise, stir while adding dropwise until dissolved, and let stand for 1h. Another 5 g of polyhexamethylene guanidine was dissolved in water. Add the polyhexamethylene guanidine solution into the chitosan solution and mix evenly, then add glycerin and vitamin E to mix in an appropriate amount, add water to make up the volume, stir evenly, fill and sterilize by radiation.
实施例2：Example 2:
取羧甲基壳聚糖0.3g至1L的烧杯中，加水300mL溶胀，静置，如不溶解可滴加稀醋酸，边滴加边搅拌至溶解，放置1h。另取聚六亚甲基胍8g加水溶解。将聚六亚甲基胍溶液加入壳聚糖溶液中混合均匀，再加甘油和维生素E适量混合，再加水补足体积，搅拌均匀后，灌装、辐射灭菌，即可。Take 0.3g of carboxymethyl chitosan into a 1L beaker, add 300mL of water to swell, and let it stand still. If it does not dissolve, add dilute acetic acid dropwise, stir while adding dropwise until dissolved, and let stand for 1h. Another 8 g of polyhexamethylene guanidine was dissolved in water. Add the polyhexamethylene guanidine solution into the chitosan solution and mix evenly, then add glycerin and vitamin E to mix in an appropriate amount, add water to make up the volume, stir evenly, fill and sterilize by radiation.
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| US20140228314A1 (en) * | 2013-02-12 | 2014-08-14 | Kunpoong Bio Co., Ltd | METHOD FOR PREPARATION OF CHITOSAN OLiGOSACCHARIDES COMPOSITION AND MIXTURE OF CHITOSAN OLiGOSACCHARIDES PREPARED THEREFROM |
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| CN104546717A (en) * | 2015-01-27 | 2015-04-29 | 陈金和 | Highly-antibacterial chitosan film-forming agent and preparation method thereof |
| CN104707129A (en) * | 2015-03-27 | 2015-06-17 | 严锋 | Ionic polymer based antibacterial spray |
| CN104740141A (en) * | 2015-04-16 | 2015-07-01 | 广东泰宝医疗科技股份有限公司 | Antibacterialp spray and preparation method thereof |
| CN106176960A (en) * | 2016-07-12 | 2016-12-07 | 泉州亚林新材料科技有限公司 | A kind of natural antibacterial spray |
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| CN109793921A (en) * | 2019-04-02 | 2019-05-24 | 凯斯芙生物科技(北京)有限公司 | A kind of compound wound of guanidine radicals can spray and preparation method thereof |
| CN109793921B (en) * | 2019-04-02 | 2021-08-17 | 凯斯芙生物科技(北京)有限公司 | Guanidyl compound woundplast and preparation method thereof |
| CN111714455A (en) * | 2020-06-08 | 2020-09-29 | 武汉大学 | A kind of quaternized chitin anti-pathogenic microorganism spray, its preparation method and application |
| CN112439064A (en) * | 2020-12-01 | 2021-03-05 | 山东光普医疗科技有限公司 | Bacteriostatic and antiviral spray capable of observing focus area and preparation method and application thereof |
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