CN104363761A - 具有干燥的吡啶硫酮锌的个人护理组合物 - Google Patents
具有干燥的吡啶硫酮锌的个人护理组合物 Download PDFInfo
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- CN104363761A CN104363761A CN201280036638.XA CN201280036638A CN104363761A CN 104363761 A CN104363761 A CN 104363761A CN 201280036638 A CN201280036638 A CN 201280036638A CN 104363761 A CN104363761 A CN 104363761A
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- CN
- China
- Prior art keywords
- personal care
- care composition
- zinc pyrithione
- drying
- soap
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 159
- PICXIOQBANWBIZ-UHFFFAOYSA-N zinc;1-oxidopyridine-2-thione Chemical compound [Zn+2].[O-]N1C=CC=CC1=S.[O-]N1C=CC=CC1=S PICXIOQBANWBIZ-UHFFFAOYSA-N 0.000 title claims abstract description 106
- 229940043810 zinc pyrithione Drugs 0.000 title claims abstract description 105
- 238000000034 method Methods 0.000 claims abstract description 36
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- 238000005728 strengthening Methods 0.000 claims description 5
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- 239000006210 lotion Substances 0.000 claims description 2
- 238000001694 spray drying Methods 0.000 claims description 2
- 229940057950 sodium laureth sulfate Drugs 0.000 claims 1
- SXHLENDCVBIJFO-UHFFFAOYSA-M sodium;2-[2-(2-dodecoxyethoxy)ethoxy]ethyl sulfate Chemical group [Na+].CCCCCCCCCCCCOCCOCCOCCOS([O-])(=O)=O SXHLENDCVBIJFO-UHFFFAOYSA-M 0.000 claims 1
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- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 description 3
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- XFKBBSZEQRFVSL-UHFFFAOYSA-N dipropan-2-yl decanedioate Chemical compound CC(C)OC(=O)CCCCCCCCC(=O)OC(C)C XFKBBSZEQRFVSL-UHFFFAOYSA-N 0.000 description 1
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- 235000008390 olive oil Nutrition 0.000 description 1
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- GRZMEERIPCJGSO-UHFFFAOYSA-N oxalic acid;sodium Chemical compound [Na].[Na].OC(=O)C(O)=O GRZMEERIPCJGSO-UHFFFAOYSA-N 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
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- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
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- DGTNSSLYPYDJGL-UHFFFAOYSA-N phenyl isocyanate Chemical compound O=C=NC1=CC=CC=C1 DGTNSSLYPYDJGL-UHFFFAOYSA-N 0.000 description 1
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- NEOZOXKVMDBOSG-UHFFFAOYSA-N propan-2-yl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OC(C)C NEOZOXKVMDBOSG-UHFFFAOYSA-N 0.000 description 1
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- YBBJKCMMCRQZMA-UHFFFAOYSA-N pyrithione Chemical compound ON1C=CC=CC1=S YBBJKCMMCRQZMA-UHFFFAOYSA-N 0.000 description 1
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- 150000003343 selenium compounds Chemical class 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 239000002437 shaving preparation Substances 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicon dioxide Inorganic materials O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- GJPYYNMJTJNYTO-UHFFFAOYSA-J sodium aluminium sulfate Chemical compound [Na+].[Al+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GJPYYNMJTJNYTO-UHFFFAOYSA-J 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- FQENQNTWSFEDLI-UHFFFAOYSA-J sodium diphosphate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]P([O-])(=O)OP([O-])([O-])=O FQENQNTWSFEDLI-UHFFFAOYSA-J 0.000 description 1
- GCLGEJMYGQKIIW-UHFFFAOYSA-H sodium hexametaphosphate Chemical compound [Na]OP1(=O)OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])O1 GCLGEJMYGQKIIW-UHFFFAOYSA-H 0.000 description 1
- 235000019982 sodium hexametaphosphate Nutrition 0.000 description 1
- 229940045998 sodium isethionate Drugs 0.000 description 1
- 229940079862 sodium lauryl sarcosinate Drugs 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- ADWNFGORSPBALY-UHFFFAOYSA-M sodium;2-[dodecyl(methyl)amino]acetate Chemical compound [Na+].CCCCCCCCCCCCN(C)CC([O-])=O ADWNFGORSPBALY-UHFFFAOYSA-M 0.000 description 1
- LADXKQRVAFSPTR-UHFFFAOYSA-M sodium;2-hydroxyethanesulfonate Chemical compound [Na+].OCCS([O-])(=O)=O LADXKQRVAFSPTR-UHFFFAOYSA-M 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000003068 static effect Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
- 235000020238 sunflower seed Nutrition 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
- BORJONZPSTVSFP-UHFFFAOYSA-N tetradecyl 2-hydroxypropanoate Chemical compound CCCCCCCCCCCCCCOC(=O)C(C)O BORJONZPSTVSFP-UHFFFAOYSA-N 0.000 description 1
- DZKXJUASMGQEMA-UHFFFAOYSA-N tetradecyl tetradecanoate Chemical compound CCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCC DZKXJUASMGQEMA-UHFFFAOYSA-N 0.000 description 1
- 235000019818 tetrasodium diphosphate Nutrition 0.000 description 1
- 239000001577 tetrasodium phosphonato phosphate Substances 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000012549 training Methods 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 239000013638 trimer Substances 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 235000021081 unsaturated fats Nutrition 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/10—Washing or bathing preparations
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N59/00—Biocides, pest repellants or attractants, or plant growth regulators containing elements or inorganic compounds
- A01N59/16—Heavy metals; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0241—Containing particulates characterized by their shape and/or structure
- A61K8/0275—Containing agglomerated particulates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4933—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having sulfur as an exocyclic substituent, e.g. pyridinethione
-
- C—CHEMISTRY; METALLURGY
- C11—ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
- C11D—DETERGENT COMPOSITIONS; USE OF SINGLE SUBSTANCES AS DETERGENTS; SOAP OR SOAP-MAKING; RESIN SOAPS; RECOVERY OF GLYCEROL
- C11D3/00—Other compounding ingredients of detergent compositions covered in group C11D1/00
- C11D3/48—Medical, disinfecting agents, disinfecting, antibacterial, germicidal or antimicrobial compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/41—Particular ingredients further characterized by their size
- A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
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Abstract
本发明提供了一种个人护理组合物,所述个人护理组合物包含干燥的吡啶硫酮锌。还提供了提高抗微生物功效并增强吡啶硫酮锌的沉积的方法。
Description
技术领域
本公开一般涉及包含干燥的吡啶硫酮锌的个人护理组合物、提高抗微生物功效的方法、以及提高吡啶硫酮锌(“ZPT”)沉积的方法。
背景技术
人类健康受到许多微生物实体或微生物诸如致病菌、细菌、真菌、酵母菌、霉菌、病毒等的影响。例如,受包括各种病毒和细菌在内的微生物实体入侵造成各种各样的病痛和疾病。为减少此类入侵,在很多情况下,人们用抗微生物皂洗涤他们的皮肤。抗菌皂通常包括皂与例如抗微生物剂的组合。例如,一种此类抗菌皂为具有非干燥粒状吡啶硫酮锌的条皂。此类条皂通常包含小或细小颗粒形式的非干燥的吡啶硫酮锌。当用抗微生物皂,如具有非干燥的吡啶硫酮锌的条皂洗涤皮肤时,皂的表面活性通常除去皮肤上的大多数微生物实体,同时抗微生物剂,如非干燥的吡啶硫酮锌沉积到皮肤上以对后续入侵提供残余的保护。
然而,如果此类皂沉积更多的抗微生物剂或者如果所述抗微生物剂更加生物可利用,则可改善现有抗菌皂。通过改善生物利用率和/或吡啶硫酮锌的沉积,可存在足够的吡啶硫酮锌颗粒以防止革兰氏阴性细菌诸如大肠杆菌(E.coli)、革兰氏阳性细菌等的后续入侵。因此,希望提供改善抗微生物功效和生物利用率的个人护理组合物和方法。
发明内容
个人护理组合物包含干燥的吡啶硫酮锌。
一种提高吡啶硫酮锌的抗微生物功效的方法,包括将吡啶硫酮锌干燥至按所述吡啶硫酮锌的重量计少于25%水分。
一种增强吡啶硫酮锌沉积的方法包括将个人护理组合物施用到个体的皮肤,其中所述个人护理组合物包含干燥的吡啶硫酮锌。
具体实施方式
I.定义
如本文所用,以下术语应当具有其后指定的含义:
“无水的”是指基本上不含水的那些组合物及其组分。
“条皂”是指旨在局部施用到表面如皮肤或毛发,以例如移除污垢、油等的组合物。条皂可为洗去型制剂,其中将产品局部施用到皮肤或毛发并随后用水在数分钟内从皮肤或毛发中淋洗去。还可使用基质将产品擦去。条皂可为旨在局部施用到皮肤的固体(例如不流动)条皂的形式。条皂还可为适形于身体的软膏的形式。另外,条皂可被包裹在使用期间保留在皂上的基质中。
“干燥的吡啶硫酮锌”是指按所述吡啶硫酮锌的重量计具有约25%或更少水分的吡啶硫酮锌。
“个人护理组合物”是指旨在局部施用到皮肤或毛发的组合物。个人护理组合物可为洗去型制剂,其中可将产品局部施用到皮肤或毛发并随后用水在数分钟内从皮肤或毛发中淋洗去。还可使用基质将产品擦去。在任一种情况下,据信产品的至少一部分保留(即沉积)在皮肤上。个人护理组合物可为液体、半液体霜膏、洗剂、凝胶、固体、或它们的组合的形式,并且旨在局部施用到皮肤和/或毛发。个人护理组合物的例子可包括但不限于条皂、洗发剂、调理洗发剂、沐浴剂、保湿沐浴剂、淋浴凝胶、皮肤清洁剂、洗面奶、洗发和沐浴剂、淋浴中身体保湿剂、宠物香波、剃刮制剂、以及与一次性清洁布结合使用的清洁组合物。
“STnS”是指十三烷基聚氧乙烯醚(n)硫酸钠,其中n可定义每分子的乙氧基化物的平均摩尔数。
“结构化的”是指具有可对个人护理组合物赋予稳定性的流变特性。结构化度通过由一种或多种以下方法测定的特性来确定:杨氏模量方法、屈服应力方法、或零剪切粘度方法或通过超速离心方法,其全部描述于2012年4月17日授权的美国专利8,158,566中。如果清洁相具有一个或多个以下特性,则可认为清洁相是结构化的:(a)至少100帕斯卡-秒(Pa-s)、至少约200Pa-s、至少约500Pa-s、至少约1,000Pa-s、至少约1,500Pa-s、或至少约2,000Pa-s的零剪切粘度;(b)约40%或更大、约45%或更大、约50%或更大、约55%或更大、约60%或更大、约65%或更大、约70%或更大、约75%或更大、约80%或更大、约85%或更大、或约90%或更大的由超速离心方法测量的结构域体积比率;或(c)约2帕斯卡(Pa)或更大、约10Pa或更大、约20Pa或更大、约30Pa或更大、约40Pa或更大、约50Pa或更大、约75Pa或更大、或约100Pa或更大的杨氏模量。
II.干燥的吡啶硫酮锌和个人护理组合物
许多现有的抗菌皂通过将抗微生物剂沉积在皮肤上而起作用。然而,抗菌皂的效应长度取决于所沉积的抗微生物剂的量和所沉积的抗微生物剂的效率二者。已令人惊奇地发现,干燥的吡啶硫酮锌可能对提高其所施用的表面上的抗微生物功效是有效的,并且例如以沉积在个体皮肤表面上的吡啶硫酮锌的质量计,可能对提高效率是有效的。
例如,下表1示出了用包含0.2%FPS吡啶硫酮锌(比较例8)的条皂和包含0.2%干燥的吡啶硫酮锌粉末的条皂(本发明实例5)处理猪皮之后的猪皮残余功效测试的结果。数据包括五小时培养期之后log cfu的减少测量值,并且所述减少相对于安慰剂处理中cfu的量来量化。如图所示,相对于包含胶态吡啶硫酮锌的条皂,用包含干燥的吡啶硫酮锌的条皂处理表现出更大的抗微生物功效(即更大的CFU减少(log))。下文描述了猪皮残余功效测试。
表1:CFU减少(log)
比较例8 | 本发明实例5 | |
平均 | 1.17 | 2.59 |
SD | 1.11 | 1.55 |
SE | 0.55 | 1.09 |
另外,表2示出杯洗擦测试的结果,所述测试用于测量用包含0.2%FPS吡啶硫酮锌(比较例8)的条皂和包含0.2%干燥的吡啶硫酮锌的条皂(本发明实例5)处理猪皮之后,吡啶硫酮锌在猪皮上的沉积。如图所示,相对于胶态吡啶硫酮锌,由干燥的吡啶硫酮锌构成的制剂提供抗菌成分对皮肤的增强的沉积。
表2:用包含0.2%ZPT的条皂处理之后的ZPT沉积(μg/cm
2
)
比较例8 | 本发明实例5 | |
平均 | 未检测到 | 0.053 |
SD | - | 0.077 |
SE | - | 0.038 |
表3示出杯洗擦测试的结果,所述测试用于测量用包含0.5%FPS吡啶硫酮锌(比较例7)的条皂和包含0.5%喷雾干燥的吡啶硫酮锌的条皂(本发明实例4)处理猪皮之后,吡啶硫酮锌在猪皮上的沉积。如表3中所示,包含喷雾干燥的吡啶硫酮锌的制剂比包含胶态吡啶硫酮锌的制剂沉积更多的抗菌成分。另外,尽管当以0.5%存在于条皂制剂中时,FPX ZPT以可检测的含量沉积,但是当以0.2%存在于条皂制剂中时,其不以可检测的含量沉积。从而,来自表2和3的数据的组合示出,当以远低于FPS ZPT的含量存在于组合物中时,干燥的ZPT能够沉积。
表3:用包含0.5%ZPT的条皂处理之后的ZPT沉积(μg/cm
2
)。
比较例7 | 本发明实例4 | |
平均 | 0.160 | 0.335 |
SD | 0.101 | 0.229 |
SE | 0.032 | 0.066 |
常规的吡啶硫酮锌可例如通过使1-羟基-2-吡啶硫酮(即吡啶硫酮酸)或它们的可溶性盐与锌盐(例如硫酸锌)反应以形成吡啶硫酮锌沉淀来制备,如美国专利2,809,971中所述,并且可使用例如音波能量形成吡啶硫酮锌或将吡啶硫酮锌加工为薄片,如美国专利6,682,724中所示。然而,这些加工不包括干燥。常规的吡啶硫酮锌常常为浆液形式(即水中的颗粒),并且浆液形式的常规ZPT的一个例子为具有约52%含水量的FPS ZPT。
干燥的吡啶硫酮锌可由多种干燥方法中的一种或多种形成。此类干燥方法的例子可包括但不限于喷雾干燥、托盘干燥、隧道干燥、滚筒干燥、流化床干燥、气动式干燥、转动干燥、槽式干燥、箱式干燥、带式干燥、真空干燥、转筒干燥、红外干燥、微波干燥和射频干燥。
可利用干燥方法以减少吡啶硫酮锌中的水分量。干燥的吡啶硫酮锌可具有按所述干燥的吡啶硫酮锌的重量计约25%或更少的含水量。例如通过进一步干燥,干燥的吡啶硫酮锌可具有甚至更低的含水量,并且按所述干燥的吡啶硫酮锌的重量计,所述含水量可为22%、20%、18%、15%、12%、10%、8%、6%、5%、3%、或1%。尽管本文例示了干燥的一些类型,但是可使用任何适当的方法以减少水分含量。
根据具体应用的要求,可使干燥的吡啶硫酮锌经受进一步加工,如铣削。铣削的例子可包括但不限于销式铣削和喷射铣削。
在用于个人护理组合物中之前,可进一步处理干燥的吡啶硫酮锌。例如,可使吡啶硫酮锌稳定以抵抗絮凝。从而,用于个人护理组合物中的干燥的吡啶硫酮锌(例如颗粒和/或薄片形式)可在其上具有表面改性以防止颗粒和/或薄片彼此附接。表面改性可包括例如通过表面上的电荷或空间阻隔提供稳定性的聚萘磺酸酯或任何其它适宜的硫酸盐、磺酸盐、羧酸盐、或其它化合物。
吡啶硫酮锌的原生颗粒可由沉淀方法形成,并且在干燥时,可接合在一起以形成较大的聚集体颗粒。干燥的吡啶硫酮锌的原生颗粒可例如为颗粒、薄片、或它们的组合的形式。原生颗粒可例如包含约0.1μm至约5μm的平均原生粒度。干燥的吡啶硫酮锌原生颗粒可例如包含约0.3μm至约15μm或约0.5μm至约10μm的平均粒度。平均粒度可包含约0.3微米至约25微米的聚集体平均粒度。测定聚集体颗粒的一种方法是用粉末的常规光散射技术,其使用例如Malvern Mastersizer。
原生颗粒和聚集体颗粒可在干燥工艺期间通过原子或分子力结合。吡啶硫酮锌可用赋形剂,例如增强生物活性的材料来干燥。适宜的生物活性增强赋形剂的例子包括金属碳酸盐、辅助活性物质如硒化合物、有机活性物质如三氯生或三氯碳酰苯胺、酸性或碱性活性物质、它们的组合等。另外,可操纵聚集体颗粒的性能以便改变生物利用率。例如,可形成聚集体颗粒以便不包含内部孔隙率,或者聚集体颗粒可以空隙空间形成以具有高内部孔隙率,使得聚集体颗粒可维持与表面积相关的性能。
不受理论的束缚,据信包含干燥的吡啶硫酮锌的个人护理组合物可提供具有原生粒度、聚集体粒度和易碎性的吡啶硫酮锌以提高功效和沉积。具体地,据信聚集体颗粒可更容易接合个体皮肤的表面,并且当聚集体颗粒分裂成原生颗粒时,干燥的吡啶硫酮锌可更容易地沉积在皮肤上,从而增强吡啶硫酮锌的沉积。聚集体颗粒可为耐久的以在加工成个人护理组合物时保留。然而,聚集体颗粒也可为易碎的,使得施用到皮肤和/或毛发期间所用的研磨力能够从聚集体颗粒中释放原生颗粒。另外,据信提高吡啶硫酮锌的表面积提高了其生物利用率并且这提高了其功效。这可例如通过制备较薄的颗粒或通过将空隙空间引入颗粒中来完成。据信由于其结构包含空隙空间,所以干燥的ZPT可具有提高的表面积。
个人护理组合物
个人护理组合物可包含干燥的吡啶硫酮锌。按所述个人护理组合物的重量计,所述吡啶硫酮锌可以约0.01%至约5%存在。其可以甚至更小的量存在,例如按所述个人护理组合物的重量计约0.05%至约2%、约0.1%至约2%、或约0.5%。
许多个人护理组合物可为水基的。因此,个人护理组合物可包含按所述个人护理组合物的重量计约0.1%至约35%、约0.3%至约20%、或约10%的水。应当理解,水量可在制备个人护理组合物的工艺期间,或者随后,随着水被周围的包装(例如硬纸板盒)吸收等而损失,即蒸发。从而,个人护理组合物还可包括趋于结合水的材料,使得水能够在个人护理组合物中被维持在期望的含量。此类材料的例子可包括碳水化合物结构剂以及润湿剂如甘油。然而,应当理解个人护理组合物可为无水的。
还可向个人护理组合物中加入多种任选的成分。此类适宜的成分可包括但不限于结构剂、润湿剂、脂肪酸、无机盐、以及其它抗微生物剂或活性物质。
个人护理组合物还可任选地包含亲水性结构剂如碳水化合物结构剂和树胶。一些适宜的碳水化合物结构剂包括生淀粉(玉米、稻、马铃薯、小麦等)以及预胶化淀粉。一些适宜的树胶包括角叉菜胶和黄原胶。个人护理组合物可包含按所述个人护理组合物的重量计约0.1%至约30%、约2%至约25%、或约4至约20%的碳水化合物结构剂。
个人护理组合物还可任选地包含一种或多种润湿剂。此类润湿剂的例子可包括多羟基醇。另外,润湿剂如甘油可由于生产或作为附加的成分包含在个人护理组合物中。例如,甘油可为个人护理组合物皂化之后的副产物。包含附加的湿润剂可导致许多有益效果,诸如改善个人护理组合物的硬度,降低个人护理组合物的水活度,以及降低由于水蒸发而导致的个人护理组合物随时间流逝的重量损失率。
个人护理组合物可任选地包含无机盐。无机盐可有助于维持特定的含水量或个人护理组合物含量,并且改善个人护理组合物的硬度。无机盐还可有助于将水结合在个人护理组合物中以防止水通过蒸发或其它方式而损失。个人护理组合物可任选地包含按所述个人护理组合物的重量计约0.01%至约15%、约1%至约12%、或约2.5%至约10.5%的无机盐。适宜的无机盐的例子可包括硝酸镁、磷酸三镁、氯化钙、碳酸钠、硫酸铝钠、磷酸二钠、聚偏磷酸钠、琥珀酸镁钠、三聚磷酸钠、硫酸铝、氯化铝、水合氯化铝、水合三氯化铝锆、水合三氯化铝锆甘氨酸配合物、硫酸锌、氯化铵、磷酸铵、乙酸钙、硝酸钙、磷酸钙、硫酸钙、硫酸铁、氯化镁、硫酸镁和焦磷酸四钠。
个人护理组合物还可任选地包含可用于进一步增强个人护理组合物的抗微生物效果的一种或多种附加的抗菌剂。个人护理组合物可包含例如按所述个人护理组合物的重量计约0.001%至约2%、约0.01%至约1.5%、或约0.1%至约1%的一种或多种附加的抗菌剂。适宜的抗菌剂的例子可包括碳酰苯胺、三氯卡班(还称为三氯碳酰苯胺)、三氯生、以DP-300购自Ciba-Geigy的卤代二苯醚、六氯酚、3,4,5-三溴水杨酰苯胺、以及2-吡啶硫醇-1-氧化物、水杨酸和其它有机酸的盐。其它适宜的抗菌剂描述于美国专利6,488,943中。
固体个人护理组合物
如本文所述,个人护理组合物可采用多种形式。一种适宜的形式为固体个人护理组合物。固体组合物可采用多种形式如粉末、粒料、条等。本文中一般将这些形式描述为条皂,但是应当理解固体组合物可为另一种形式或形状。条皂个人护理组合物的一个例子可包含按所述个人护理组合物的重量计约0.1%至约35%的水,按所述个人护理组合物的重量计约45%至约99%的皂,以及按所述个人护理组合物的重量计约0.01%至约5%的干燥的吡啶硫酮锌。另一种适宜的抗微生物条皂可包含例如按所述个人护理组合物的重量计约0.1%至约30%的水,按所述个人护理组合物的重量计约40%至约99%的皂,以及按所述个人护理组合物的重量计约0.01%至约1%的干燥的吡啶硫酮锌。
条皂组合物可称为常规的固体(即非流动)条皂组合物。一些条皂组合物包含常规的皂,同时其它包含合成表面活性剂,并且另外其它包含皂与合成表面活性剂的混合物。条皂组合物可包含例如约0%至约45%的合成阴离子表面活性剂。适宜的常规皂的例子可包括无助洗剂的碾磨的香皂条(即包含约5%或更少的水溶性表面活性助洗剂)。
个人护理条皂组合物可包含例如按所述个人护理组合物的重量计约45%至约99%、或约50%至约75%的皂。此类皂可包括典型的皂,即烷烃-或烯烃单羧酸的碱金属或链烷醇铵盐。可适于个人护理组合物的是钠阳离子、镁阳离子、钾阳离子、钙阳离子、单乙醇铵阳离子、二乙醇铵阳离子和三乙醇铵阳离子、或它们的组合。个人护理组合物中包含的皂可包括钠皂或钠皂与约1%至约25%铵、钾、镁、钙的组合,或这些皂的混合物。另外,所述皂可为熟知的具有约12至约22个碳原子,或约12至约18个碳原子的链烷酸或链烯酸的碱金属盐。另一种适宜的皂可为具有约12至约22个碳原子的烷烃或烯烃的碱金属羧酸盐。附加的适宜皂组合物描述于美国专利申请序列号13/036,889中。
个人护理组合物还可包含具有脂肪酸的皂。例如,一种条皂组合物可使用C8-C24或C10-C20脂肪酸的约40%至约95%的可溶性碱金属皂。脂肪酸可例如具有可提供广泛分子量范围下限的椰子油分布或可提供广泛分子量范围上限的花生油或油菜籽油或它们的氢化衍生物的脂肪酸分布。其它此类组合物可包含牛脂和/或植物油的脂肪酸分布。牛脂可包含脂肪酸混合物,所述脂肪酸混合物可通常具有2.5%C14、29%C16、23%C18、2%棕榈油酸、41.5%油酸以及3%亚油酸的大致碳链长度分布。牛脂还可包含具有类似分布的其它混合物,如衍生自各种动物油脂和/或猪油的脂肪酸。在一个例子中,牛脂还可被硬化(即氢化),使得一些或全部不饱和脂肪酸部分可转换成饱和脂肪酸部分。
适宜植物油的例子包括棕榈油、椰子油、棕榈仁油、棕榈油硬脂精、大豆油、以及氢化稻米糠油、或它们的混合物,因为此类油可为其中更容易获得的脂肪。适宜椰子油的一个例子可包括比例为约85%的至少12个碳原子的脂肪酸。当可使用其中主要链长可为C16以及更高的椰子油和脂肪如牛脂、棕榈油或非热带坚果油或脂肪的混合物时,此类比例可能更大。个人护理组合物中包含的皂可为例如钠皂,所述钠皂具有约67-68%牛脂、约16-17%椰子油、约2%甘油和约14%水的混合物。
根据商业上可接受的标准,个人护理组合物中包含的皂还可为不饱和的。例如,个人护理组合物中包含的皂可包括不饱和度在约37%至约45%的范围内的皂化材料。
个人护理组合物中包含的皂可例如由经典釜沸腾工艺或现代连续皂制造工艺制得,其中可使用那些本领域技术人员熟知的程序,用碱金属氢氧化物皂化天然脂肪和油如牛脂或椰子油或它们的等同物。皂还可通过用碱金属氢氧化物或碱金属碳酸盐中和脂肪酸诸如月桂酸(C12)、肉豆蔻酸(C14)、棕榈酸(C16)、或硬脂酸(C18)而制得。
个人护理组合物中包含的皂还可通过连续皂制造工艺制得。所述皂可经由真空闪速干燥工艺加工成皂条粒。适宜皂条粒的一个例子包含按所述皂条粒的重量计约67.2%牛脂皂、约16.8%椰子皂、约2%甘油、以及约14%水。然后可将皂条粒用于铣削工艺中以制成个人护理组合物。
个人护理组合物还可任选地包括一种或多种游离脂肪酸,所述游离脂肪酸的量按所述个人护理组合物的重量计为约0.01%至约10%,约0.5%至约2%,或约0.75%至约1.5%。游离脂肪酸可被包含在个人护理组合物中以提供增强的皮肤感觉有益效果如更柔软且更光滑感的皮肤。适宜的游离脂肪酸可包括牛脂脂肪酸、椰油脂肪酸、棕榈脂肪酸和棕榈仁脂肪酸。
液体个人护理组合物
个人护理组合物可采用许多形式并且那些适宜形式之一可为液体形式。液体形式的个人护理组合物的例子可包括洗手皂、沐浴剂、洗手液等。此类液体基个人护理组合物可包含清洁相和/或有益相(即单相或多相组合物)。清洁相或有益相中的每一种可包含多种组分。液体组合物可具有以不同组合的多相。例如,个人护理组合物可包括两种清洁相、清洁相和有益相、两种有益相、或相的任何可接受的组合。另外,可将多相组合物中的相共混、分离、或它们的组合。相还可形成图案(例如条纹状)。个人护理组合物可为胶束、层状、或它们的组合。个人护理组合物可包括至少70%层状结构。可将干燥的ZPT置于清洁相中。
清洁相可为含水的或无水的。清洁相还可例如包含醇。清洁相可包含表面活性剂。适用于本文的表面活性剂包括阴离子表面活性剂、两性离子表面活性剂、两性表面活性剂、以及它们的组合。适宜表面活性剂的一个例子包含月桂基聚氧乙烯醚-1硫酸钠,使得干燥的吡啶硫酮锌可被用于胶束沐浴剂中,如下文中更详细地描述。
清洁相可包含按所述个人护理组合物的重量计约5%至约20%的含水结构化表面活性剂相。此类结构化表面活性剂相可包括例如十三烷基聚氧乙烯醚(n)硫酸钠,下文中为STnS,其中n可定义乙氧基化的平均摩尔数。n可在约0至约3、约0.5至约2.7、约1.1至约2.5、约1.8至约2.2的范围内,或者n可为约2。当n可为小于3时,STnS可提供改善的稳定性,有益剂在个人护理组合物内改善的相容性,以及个人护理组合物提高的温和性,STnS的此类所述有益效果公开于美国专利申请序列号13/157,665中。
清洁相还可包含两性表面活性剂和两性离子表面活性剂中的至少一种。适宜两性或两性离子表面活性剂可包括例如描述于美国专利5,104,646和美国专利5,106,609中的那些。
清洁相还可包含结构化体系。结构化体系的一个例子包括非离子乳化剂、缔合聚合物、电解质、或它们的组合。
个人护理组合物可任选地不含月桂基硫酸钠,下文中为SLS。然而,当SLS存在时,适宜SLS的例子描述于美国专利申请序列号12/817,786中。
个人护理组合物可包含按所述个人护理组合物的重量计约0.1%至20%的辅助表面活性剂。辅助表面活性剂可包括两性表面活性剂、两性离子表面活性剂、或它们的混合物。适宜两性或两性离子表面活性剂的例子可包括描述于美国专利5,104,646和美国专利5,106,609中的那些。
两性表面活性剂可包括可广泛描述为脂族仲胺和叔胺衍生物的那些,其中脂族基团可为直链或支链的,并且其中脂族取代基可包含约8至约18个碳原子,使得一个碳原子可包含阴离子水增溶基团,例如羧基、磺酸根、硫酸根、磷酸根、或膦酸根。属于该定义内的化合物的例子可为3-十二烷基-氨基丙酸钠、3-十二烷基氨基丙烷磺酸钠、月桂基肌氨酸钠、N-烷基牛磺酸(如根据美国专利2,658,072的教导,通过使十二烷基胺与羟乙基磺酸钠反应制备的那些),N-高级烷基天冬氨酸(如根据美国专利2,438,091的教导所制得的那些)、以及描述于美国专利2,528,378中的产品。两性表面活性剂的其它例子可包括月桂酰两性基乙酸钠、椰油酰两性基乙酸钠、月桂酰两性基乙酸二钠、椰油酰两性基二乙酸二钠、以及它们的混合物。也可使用两性基乙酸盐(Amphoacetates)和两性基二乙酸盐(diamphoacetates)。
适用的两性离子表面活性剂可包括被广泛描述为脂族季铵、和锍化合物衍生物的那些,其中脂族基团可为直链或支链的,并且其中脂族取代基可包含约8至约18个碳原子,使得一个碳原子可包含阴离子基团,例如羧基、磺酸根、硫酸根、磷酸根或膦酸根。其它两性离子表面活性剂可包括甜菜碱,所述甜菜碱包括椰油酰氨基丙基甜菜碱。
可在清洁相中包含其它任选的添加剂,其包括例如乳化剂(例如非离子乳化剂)和电解质。适宜的乳化剂和电解质描述于美国专利申请序列号13/157,665中。
个人护理组合物还可包含有益相。有益相可为疏水的和/或无水的。所述有益相还可基本上不含或不含表面活性剂。有益相还可包括有益剂。具体地,有益相可包含按所述个人护理组合物的重量计约0.1%至约50%的有益剂,或者按所述个人护理组合物的重量计约0.5%至约20%的有益剂。有益剂的例子可包括凡士林、单油酸甘油酯、矿物油、甘油三酯、大豆油、蓖麻油、大豆低聚物、以及它们的混合物。有益剂的附加例子可包括水不溶性或疏水性有益剂。其它适宜的有益剂描述于美国专利申请序列号13/157,665中。有益相还可包含干燥的吡啶硫酮锌。
适于用作本文疏水性皮肤有益剂的甘油脂的非限制性例子可包括蓖麻油、红花油、玉米油、胡桃油、花生油、橄榄油、鳕鱼肝油、杏仁油、鳄梨油、棕榈油、芝麻油、植物油、向日葵籽油、大豆油、植物油衍生物、椰子油和衍生的椰子油、棉籽油和衍生的棉籽油、霍霍巴油、可可油、以及它们的组合。
适于用作本文疏水性皮肤有益剂的烷基酯的非限制性例子可包括脂肪酸异丙酯和长链(即C10-C24)脂肪酸的长链酯例如蓖麻油酸鲸蜡酯,其非限制性例子可包括棕榈酸异丙酯、肉豆蔻酸异丙酯、蓖麻油酸鲸蜡酯和蓖麻油酸硬脂酸酯。其它例子可包括月桂酸己酯、月桂酸异己酯、肉豆蔻酸十四烷基酯、棕榈酸异己酯、油酸癸酯、油酸异癸酯、硬脂酸鲸蜡酯、硬脂酸癸酯、异硬脂酸异丙酯、己二酸二异丙酯、己二酸二异己酯、己二酸二己基癸酯、癸二酸二异丙酯、酰基异壬酸酯、乳酸月桂酯、乳酸肉豆蔻酯、乳酸鲸蜡酯、以及它们的组合。
适于用作本文疏水性皮肤有益剂的烯基酯的非限制性例子可包括肉豆蔻酸油基酯、硬脂酸油基酯、油酸油基酯、以及它们的组合。
适于用作本文疏水性皮肤有益剂的脂肪酸聚甘油酯的非限制性例子可包括二硬脂酸十甘油酯、二异硬脂酸十甘油酯、单肉豆蔻酸十甘油酯、单月桂酸十甘油酯、单油酸六甘油酯、以及它们的组合。
适于用作本文疏水性皮肤有益剂的羊毛脂和羊毛脂衍生物的非限制性例子可包括羊毛脂、羊毛脂油、羊毛脂蜡、羊毛脂醇、羊毛脂脂肪酸、羊毛脂酸异丙酯、乙酰化羊毛脂、乙酰化羊毛脂醇、亚油酸羊毛脂醇酯、蓖麻油酸羊毛脂醇酯、以及它们的组合。
适于用作本文疏水性皮肤有益剂的硅油的非限制性例子可包括二甲基硅氧烷共聚多元醇、二甲基聚硅氧烷、二乙基聚硅氧烷、混合的C1-C30烷基聚硅氧烷、苯基二甲基硅氧烷、二甲基硅氧烷醇、以及它们的组合。可用于本文的硅油的非限制性例子描述于美国专利5,011,681中。另外其它适宜的疏水性皮肤有益剂可包括牛奶甘油三酯(如羟基化牛奶甘油酯)和多元醇脂肪酸聚酯。
方法
为提高吡啶硫酮锌的抗微生物功效和/或沉积,可将包含干燥的吡啶硫酮锌的个人护理组合物施用到个体的皮肤。干燥的吡啶硫酮锌可例如具有约15%或更少的含水量。一种示例性个人护理组合物包含按所述个人护理组合物的重量计约0.1%至约35%的水;按所述个人护理组合物的重量计约45%至约99%的皂;以及按所述个人护理组合物的重量计约0.01%至约5%的干燥的吡啶硫酮锌。尽管为简明起见仅讨论了与该方法相关联的几种个人护理组合物成分和性能,但是本文的个人护理组合物可包含如上文所讨论的成分和/或性能中的任一种。
另外,并且如表3中所示,增强吡啶硫酮锌沉积的方法可对皮肤进行约0.05μg/cm2或更大的干燥的吡啶硫酮锌沉积。增强吡啶硫酮锌沉积的方法可对皮肤进行约0.1μg/cm2至约1.0μg/cm2的干燥的吡啶硫酮锌沉积。如上文所讨论,在皮肤上沉积更多的吡啶硫酮锌具有增加的有益效果。所述方法可包括,例如将包含干燥的吡啶硫酮锌的个人护理组合物施用到个体的皮肤。尽管为简明起见仅讨论了与该方法相关联的几种个人护理组合物成分和性能,但是本文的个人护理组合物可包含如上文所讨论的成分和/或性能中的任一种。
III.程序
A.用于制备干燥的吡啶硫酮锌的干燥技术
喷雾干燥
吡啶硫酮锌可作为细粒度(FPS)Zinc的49%活性悬浮液的浆液而获得,其通过表面吸收聚萘磺酸盐来稳定。吡啶硫酮锌颗粒具有如通过光散射测定的约0.75微米的平均直径。浆液使用具有200℃入口温度和100℃出口温度的Büchi微型喷雾干燥器B290来喷雾干燥。浆液流量通过调节蠕动泵控制至35%的最大泵速度来控制。将进料分散体的压缩空气流量设定为大约600L/hr。通过光学显微镜观察到喷雾干燥的吡啶硫酮锌聚集体颗粒具有约10微米至约100微米的粒度,其中平均直径为约60微米,同时由不同的原生颗粒亚基构成,所述原生颗粒亚基为原始的FPS颗粒。所述颗粒为球形。原生颗粒之间的空隙空间可提高聚集体的表观表面积,使得颗粒可具有性能,如通过原生颗粒的特定界面调控的约9×105cm2/cm3的溶解速率。有利的是,在合理施加的力下,颗粒是可崩解的、或易碎的,在对显微镜盖玻片施加的压力下破裂。
托盘干燥
吡啶硫酮锌可作为细粒度(FPS)Zinc的49%活性悬浮液的浆液而获得,其通过表面吸收聚萘磺酸盐来稳定。FPS吡啶硫酮锌颗粒具有如通过光散射测定的约0.75微米的平均直径。将浆液置于铝箔船中,随后将所述铝箔船置于干燥烘箱中(温度=45℃)。一旦完全干燥,就将所述材料从箔中取出,并机械破碎成小颗粒。使用美国标准筛将级分过筛以基于所示筛孔尺寸产生粒度级分。
B.猪皮残余功效测试
为制备安慰剂,实施一种洗涤/淋洗性能方案。具体地,通过用得自胰酶大豆琼脂(TSA)划线接种板的一个菌落接种50mL的TSB,产生大肠杆菌(E.coli)(菌株10536、8879、或11259)的过夜细菌培养物。在干燥摇动器中,在37℃,200rpm下,使培养物生长17-18小时。
为测定条皂的功效,对猪皮进行条皂体内性能测试。首先,获得、清洁、冷冻、并照射(25-40kGy)猪皮。在-20℃下储存经照射的猪皮直至测试。为测试条皂组合物,将10×10cm猪皮解冻至室温并持续1小时,并且使用无菌手术刀将猪皮切割成5×10cm部分。
使用带手套的手,如下洗涤猪皮:在33-36℃下用流量为4至4.2L/min的自来水淋洗5×10cm猪皮并持续15秒。在流水中润湿条皂组合物并持续5秒,将条皂组合物平坦地放置在猪皮表面上,然后使用往复运动立即横跨整个猪皮表面轻轻磨擦条皂组合物并持续15秒,并且轻微的手压与常规手洗期间的手压类似。然后,通过用手连续摩擦猪皮45秒来产生泡沫(例如缺少条皂组合物)。用自来水淋洗猪皮15秒,其通过将组织保持在45度角下并使得水冲击在顶部表面上并瀑布状流下整个表面而进行。用无菌薄纸轻拍猪皮干燥,并使得猪皮在低光照条件下在静室空气中干燥5-10分钟。
将猪皮切割成2×2.5cm的片,并通过使用得自如上所述过夜培养物的胰酶大豆液体培养基(TSB)的10μL1:20稀释液,用106-107个菌落接种每个片。使得细菌在猪皮表面的片上干燥20分钟,然后将所述猪皮的片置于加湿室(60%RH,33℃)中,并将所述片培养0小时、2小时、或5小时。培养后,将所述片置于包含改性Leethen液体培养基与1.5%Tween-80和1%卵磷脂(MBL-T)的50mL冰冷中和缓冲液的广口瓶中,并且剧烈摇晃其中具有片的缓冲液并持续1分钟以洗脱细菌。必要时,在MBL-T中稀释悬浮液并将悬浮液置于胰酶大豆琼脂(TSA)板上以获得细胞计数。在33℃和60%相对湿度下将所述板培养24小时。然后,对所述TSA板(例如其cfu)计数以计算cfu/mL,并且使用4.1版GraphPad Prism产生生长曲线。进行一次上述测试以计算cfu/mL并产生生长曲线。(注:上述测试可进行多次并且可将每次重复的数据平均)
C.测量沉积的杯洗擦程序
如本文所述,可使用杯洗擦程序以辅助确定有多少含锌和/或吡啶硫酮材料沉积到猪皮上。首先,在流水(流量=4.5L/min,温度=35-38℃)下润湿目标基质表面并持续大约15秒。接着,将剂量为1mL的沐浴剂(经由一次性注射器)施用到目标基质表面。通过用手摩擦施用沐浴剂并持续大约15秒而在目标基质上持续产生泡沫。15秒发泡过程后,使泡沫静置在猪皮上并持续附加的15秒。在15秒等待结束时(发泡过程开始后30秒),将猪皮淋洗大约10秒,从而使得流水接触目标基质表面并瀑布状流下(朝向远侧表面)。淋洗后,使用纸巾拍打表面来干燥。
程序的下一部分涉及包含皮肤接触边缘上的硅氧烷填缝材料小珠的2-cm直径玻璃圆筒,其将被牢固压向猪皮表面以防止萃取流体渗漏。可将1mL萃取溶剂移入玻璃圆筒中。为测定有多少吡啶硫酮锌被沉积,例如,萃取溶剂可为80:200.05M EDTA:EtOH。尽管使用移液管或玻璃棒,但是玻璃圆筒内的整个区域可使用适度的压力洗擦约30秒。然后将溶液移除并移入标记的玻璃样品小瓶中。可使用新鲜萃取溶液重复杯洗擦程序,其将与初始萃取液一起汇集在标记的小瓶中。
每次使用后,可清洁玻璃圆筒和棒。清洁可例如通过将每个圆筒和棒浸入稀释的溶液中并用手指或软毛刷洗擦来完成。然后可将圆筒和棒浸入IPA中。最后,用Kimwipe或其它无棉薄纸擦干圆筒和棒以除去任何可见的残余物。可在每天结束时或当在其底部中发现残余物的任何可见层时,改变洗擦溶液。另外,可将样品储存在4℃(±3℃)下直至可提交样品用于HPLC分析。然后使用HPLC分析以测定沉积量。然后,用2-2’-二硫代吡啶使溶液中的游离吡啶硫酮衍生化,并随后经由HPLC利用UV检测分析。结果报告为每mL溶液的吡啶硫酮锌的μg数。
IV.实例
实例1
如上文在喷雾干燥方法中所述制备喷雾干燥的吡啶硫酮锌。然后将该喷雾干燥的吡啶硫酮锌配制成如下所述的制剂。
实例2
获得具有约5微米平均直径的干燥的吡啶硫酮锌粉末。颗粒为具有约1微米原生粒度的原生颗粒的不规则形状的聚集体。在显微镜载片上分散于矿物油中,颗粒不容易重新分散成它们的原生颗粒。
实例3A、3B和3C
如上所述制备托盘干燥的吡啶硫酮锌。利用不同的筛,收集以下颗粒分布。
实例3A <600微米
实例3B 600-850微米
实例3C 850-1,500微米
实例4-8,条皂
制备包含喷雾干燥的吡啶硫酮锌的条皂。在混合器中,将经由涉及粉碎步骤和真空干燥步骤的常规工艺制得的皂条粒与干燥的吡啶硫酮锌共混。然后使皂混合物通过常规的铣削、模制和压印步骤加工以产生成品条皂组合物。
实例9,胶束沐浴剂
制备包含干燥的吡啶硫酮锌的胶束沐浴剂。表面活性剂与过量水一起添加并搅拌直至均匀。聚合物可由20%溶液添加,并且然后可加入除了盐和乙二醇二硬脂酸酯(EGDS)之外的所有其它成分,将它们加入并搅拌直至均匀。EGDS作为与SLS的浓缩物通过从热溶液中沉淀来单独制备,并作为浓缩的预混物添加。将pH调节至6.0。最后加入氯化钠以获得2.01/秒剪切速率下的9,000cP的布氏粘度(Brookfield viscosity)。
实例10,结构化的表面活性剂沐浴剂
可通过常规的制剂和混合技术制备清洁相。通过首先将水、皮肤有益组分和增稠剂加入混合容器中并搅拌直至形成均匀分散体来制备清洁相。然后按以下顺序加入:表面活性剂、乙二胺四乙酸二钠、防腐剂以及一半氯化钠和所有其它防腐剂和微量组分,除了芳香剂和剩余的氯化钠之外。维持在环境温度下,同时搅拌混合容器。在单独的容器中,用芳香剂将结构化聚合物预润湿并与剩余的氯化钠同时加入混合容器中,同时搅拌。加入干燥的吡啶硫酮锌和大豆油。持续搅拌直至均匀,并且然后泵送通过静态混合元件以分散任何聚合物块,以完成该批次。
本文所公开的量纲和值不旨在被理解为严格地限于所引用的精确数值。相反,除非另外指明,每个此类量纲旨在表示所引用的值和围绕该值的功能上等同的范围。例如,公开为“40mm”的尺寸旨在表示“约40mm”。
应当理解,在该说明书全文中给出的每一最大数值限度包括每一较低数值限度,就像此类较低数值限度在本文中明确写出一样。在本说明书全文中给出的每一最小数值限度将包括每一较高数值限度,如同该较高数值限度在本文中明确写出一样。在本说明书全文中给出的每一数值范围将包括落入此类较宽数值范围内的每一较窄数值范围,如同此类较窄数值范围在本文中明确写出一样。
本文引用的每一文献,包括任何交叉引用的或相关的专利或申请,均据此以引入的方式全文并入本文,除非明确地排除在外或换句话讲限制。对任何文献的引用均不是承认其为本文公开的或受权利要求书保护的任何发明的现有技术、或承认其独立地或以与任何其它一个或多个参考文献的任何组合、提出、建议或公开任何此类发明。此外,当本文献中术语的任何含义或定义与引入本文以供参考的文献中相同术语的任何含义或定义冲突时,将以本文献中赋予该术语的含义或定义为准。
虽然已经举例说明和描述了本发明的具体实施例,但是对于本领域技术人员来说将显而易见的是,在不背离本发明实质和范围的情况下可作出多种其它的改变和变型。因此,所附权利要求书旨在涵盖本发明范围内的所有此类改变和变型。
Claims (15)
1.一种个人护理组合物,包含干燥的吡啶硫酮锌。
2.根据权利要求1所述的个人护理组合物,其中所述个人护理组合物为沐浴剂、条皂、洗发剂、洗剂、或洗手液的形式。
3.根据前述权利要求中任一项所述的个人护理组合物,其中所述干燥的吡啶硫酮锌由喷雾干燥方法形成。
4.根据前述权利要求中任一项所述的个人护理组合物,其中所述干燥的吡啶硫酮锌为颗粒、薄片、或它们的组合的形式。
5.根据权利要求4所述的个人护理组合物,其中所述颗粒包含0.1μm至20μm的平均粒度。
6.根据权利要求5所述的个人护理组合物,其中所述颗粒包含0.5μm至10μm的平均粒度。
7.根据前述权利要求中任一项所述的个人护理组合物,其中所述干燥的吡啶硫酮锌包含按所述干燥的吡啶硫酮锌的重量计15%或更少,更优选10%或更少,或甚至更优选5%或更少的含水量。
8.根据前述权利要求中任一项所述的个人护理组合物,还包含清洁相,其中所述清洁相包含至少一种表面活性剂。
9.根据权利要求9所述的个人护理组合物,其中所述至少一种表面活性剂选自月桂基聚氧乙烯醚硫酸钠、月桂基硫酸钠、十三烷基聚氧乙烯醚硫酸钠、以及它们的组合。
10.根据权利要求1-7中任一项所述的个人护理组合物,还包含:
a)按所述个人护理组合物的重量计0.1%至35%的水;
b)按所述个人护理组合物的重量计45%至99%的皂;
c)按所述个人护理组合物的重量计0.01%至5%的干燥的吡啶硫酮锌。
11.根据前述权利要求中任一项所述的个人护理组合物,包含按所述个人护理组合物的重量计0.05%至2%的干燥的吡啶硫酮锌。
12.一种增强吡啶硫酮锌的沉积的方法,所述方法包括将个人护理组合物施用到个体的皮肤,所述个人护理组合物包含干燥的吡啶硫酮锌。
13.根据权利要求12所述的方法,其中所述个人护理组合物包含按所述个人护理组合物的重量计0.05%至2%的干燥的吡啶硫酮锌。
14.根据权利要求12-13中任一项所述的方法,其中将0.05μg/cm2或更多的干燥的吡啶硫酮锌沉积到个体的皮肤。
15.根据权利要求12-14中任一项所述的方法,其中所述干燥的吡啶硫酮锌包含按所述干燥的吡啶硫酮锌的重量计15%或更少,更优选10%或更少,或甚至更优选5%或更少的含水量。
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BR112015023254A2 (pt) | 2013-03-14 | 2017-07-18 | Procter & Gamble | composições concentradas sólidas contendo zinco piritiona |
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WO2013025743A3 (en) | 2014-12-31 |
US20130045961A1 (en) | 2013-02-21 |
BR112014002758A2 (pt) | 2017-02-21 |
CA2843899A1 (en) | 2013-02-21 |
WO2013025743A2 (en) | 2013-02-21 |
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