CN114642658A - 一种油溶性小分子天然生物酸类抗病毒、抗菌制剂、其制法及应用 - Google Patents
一种油溶性小分子天然生物酸类抗病毒、抗菌制剂、其制法及应用 Download PDFInfo
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- CN114642658A CN114642658A CN202210078117.6A CN202210078117A CN114642658A CN 114642658 A CN114642658 A CN 114642658A CN 202210078117 A CN202210078117 A CN 202210078117A CN 114642658 A CN114642658 A CN 114642658A
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Abstract
一种小分子生物酸类抗病毒、抗菌油溶性制剂,含有小分子生物酸作为有效药物成分,所述小分子生物酸溶解于油油互溶体或油水互溶体,所述油油互溶体或油水互溶体,是与小分子生物酸互溶性的油类,得到本发明的小分子生物酸类抗病毒、抗菌油溶性制剂。将所述制剂,与可药用赋形剂配制而成多种剂型的小分子生物酸抗病毒、抗菌药物。这种药物,可用作抗鼻病毒、流感病毒以及常感染人的其他病毒、病菌的药物,也可作为用于预防和治疗新型冠状病毒感染的药物。
Description
技术领域
本发明涉及生物制药领域,具体的说是提供一种油溶性小分子天然生物酸类抗病毒、抗菌制剂及其制备方法。本发明提供的制剂可用于作为抗病毒、抗菌的预防和治疗的药物。特别是,在对新型冠状病毒(COVID-19)、流感病毒、鼻病毒等病原体感染方面,也会具有重要的预防和治疗作用。
背景技术
病毒人肉眼不可见,却在地球生态***中非常活跃。病毒也对大量生命体的生存进行了调节,从微生物到大型哺乳动物,无一不受到它们的影响。病毒的作用不仅限于生物,它们还会影响地球的气候、土壤、海洋和淡水。2009年,科学家达娜.威尔纳发现,人的肺里平均驻扎了174种之多的病毒,其中只有10%是已发现的病毒的近亲,而另外90%的病毒是陌生的(见[美]卡尔齐默著;刘旸译;《病毒星球》2019年4月;广西师范大学出版社;001,004,005)。
报刊资料:经常感染人的呼吸***病毒有200多种。经常感染人的肠道病毒有70多种。有的肠道病毒也引起呼吸***感染。呼吸***感染95%是病毒所引起的。“可感染人类的病毒,有400种以上”。普通成人可检测到200种以上的抗病毒抗体。
制造防御物质,以抵抗各种微生物之能力,不独存在于动物体;即属下等植物,甚至细菌(1877年Pasteur与Joubert氏)有时亦能产生物质,以抑制或妨碍他种微生物之生长。此类物质被总称为抗生素(Antibiotics),其在自然界之中虽甚广存,但近代,方被引入治疗界,发挥伟效(见普耳孙著;赵师震译;《药理学》下册1956;商务印书馆;637.)。这就是青霉素上市后的原始性关于抗生素的定义。
经过长期的自然选择,蚁酸(甲酸)、乙二酸(草酸)、丙酸、乳酸、柠檬酸、山梨酸、苯甲酸等,成为动植物的主要天然防御物质。
蚁酸是蚁类和蜂类经久远的自然选择,抑制或妨碍他种微生物生长的防御物质。是地球上2万多种蜂类、1万多种蚁类防御功能的主要成分。
乙二酸以钾盐、钙盐游离状态,广泛存在于植物中,特别是乔木、灌木的木质中,防卫乔木、灌木被腐败微生物侵害而腐烂。
山梨酸、苯甲酸等,是多种植物的防御物质。水果成熟前,各种生物酸浓度较高,防止了微生物对水果的入侵,水果不易腐烂;水果熟化后,生物酸类物质减少,酸度下降,生物酸类对微生物的防御作用降低,就较易腐烂了。
近百年来,上述来源于动植物产生的防御物质已经成为广泛应用的食品添加剂、消毒剂、防腐剂以及工业医药原料。
但是,将蚁酸、乙二酸、乳酸等消毒、防腐药力最强的生物酸类,制成油溶性制剂,取得应用较小剂量,并用于治疗流感的研究,到目前为止尚未见到报道。
发明内容
本发明将经长期自然选择形成的分子量较小的,具有抗病毒、抗菌的动植物产生的防御物质,归类为小分子生物酸,这类生物酸,也可称为动植物的生命酸。本发明认识到,蚁酸、乙二酸、乳酸、丙酸、山梨酸、苯甲酸等系列小分子生物酸,是水溶性的,又可制造成为油溶性制剂的生物酸类抗生素。
本发明的发明者们对油溶性小分子生物酸类的抗病毒、抗菌性能进行了研究,具体地说,本发明重点进行试验研究的小分子生物酸,包括:
蚁酸,又称甲酸,存在于蜂类、某些蚁类和某些毛虫的分泌物中。最初是由蒸馏蚂蚁得到的,最简单的脂肪酸。分子式为HCOOH。熔点8.4℃,沸点 100.5℃,分子量46.03,无色而有刺激气味的液体,易燃。能与水、乙醇、***和甘油任意混溶,和大多数的极性有机溶剂混溶,在烃中也有一定的溶解性。且有腐蚀性,人类皮肤接触后会起泡红肿。在化学工业中,甲酸被用于橡胶、医药、染料、皮革种类工业。用于制造乙酸盐、乙酸酯(见王箴主编,《化工辞典》第4版;(2000);化学工业出版社;443),也用作消毒剂和防腐剂。它是酸性最强的饱和一元羧酸。
《食品添加剂手册》记载,“所谓ADI值是指在人的一生中,每日连续摄入而不影响健康的最高摄入量”。蚁酸作为食品添加剂的ADI为0— 3mg/kg(FAO/WHO,1973)(见凌关庭王亦芸、唐述潮著;《食品添加剂手册》上册;(1989);化学工业出版社;5;168页03559)即60kg体重每日最大用量为 180mg。
蚁酸存在于数种昆虫(例如红蚁Formica rufa)之制毒器中,西洋民间古来以所谓蚁浴之形式,用于风湿病及神经痛,即探取蚁丘(及其中之蚁)以为之。
乙二酸,即草酸,分子量:126.07;存在于许多植物,特于Rheum(大黄属),Spinacia(菠菜属),以钾盐、钙盐游离状态,广泛存在于植物中,特别是乔木、灌木的木质中。“人体处于正常情形之下,似并不制造草酸;在每日尿中通常可检测到20.0mg草酸”,也不产生草酸中毒现象,但是蓄牧业经常发生草酸中毒现象(见普耳孙著;赵师震译;《药理学》下册1956;商务印书馆; 426)。乙二酸是最重要的化工原料,用于医药生产及聚合物合成等。旧法以木屑为原料,经碱熔成草酸纳而制得(见王箴主编,《化工辞典》第2版;(1979);化学工业出版社;385)。
中国近代中医学家张锡纯所著《中药亲试剂》记载,大黄是治疗疔毒的特效中药。说明,近代医学,已经将含有乙二酸的中药,当作治疗疔毒的特效中药。
乳酸,无色至淡黄色糖浆状液体,几乎无臭,或略有脂肪酸臭,呈强酸味,可与水、丙二醇、甘油、丙酮、***和乙醇混溶。广泛应用于食品的调味及防腐(见凌关庭王亦芸、唐述潮著;《食品添加剂手册》上册;(1989);化学工业出版社;262页05007)。
现代西药《药理学》记载:20世纪50年代之前,西欧医院就已经应用乳酸溶液口服,“治疗婴幼儿泄泻,往往颇有良效”;成人治疗腹泻,应用5%的乳酸口服;又记载,“用20%的乳酸,涂于患处,治疗喉结核”(见普耳孙著;赵师震译;《药理学》下册1956;商务印书馆;423)。
雌性哺乳动物的外生殖道都生长有乳酸杆菌,并不断分泌乳酸,防止病毒、病菌从外生殖道侵入机体,保护哺乳动物的健康。文献记载,0.18%的乳酸,就可杀灭大肠杆菌;0.36%的乳酸就可杀灭葡萄球菌的生长。
小分子生物酸的水溶性制剂,在人体内,迅速从尿路排出体外,呼吸***、消化***的药物浓度低,往往达不到在体内呼吸***、消化***靶点的抗病毒、抗菌的药效浓度。本发明为了解决这一药剂学、药理学难点,选用油油互溶体、油水互溶体做小分子生物酸的溶剂载体,研制成功油溶性蚁酸抗病毒制剂。
文献记载,蚁酸用于消毒防腐的食品添加剂,60kg体重每日最大剂量为 180mg(ADI为0—3mg/kg)。本发明的发明者研制成的油溶性蚁酸口服剂、透皮吸收剂,60kg体重每日剂量为8-16mg,与其水溶性作为食品添加剂每日最大剂量180mg相比,降低了10倍。而经治疗流感的临床实践证明,本发明油溶性蚁酸制剂,治疗流感发挥了显著的解除鼻塞,止咳、痰容易咳出的抗病毒效果。
本发明涉及的小分子生物酸油油互溶体、油水互溶体制剂应用后,在药动学吸收、分布、***过程中,消化***(肝、胆、肠)呼吸***(肺、气管) 的动态药物浓度较高,泌尿***的排出量较少,治疗剂量不发生毒副反应。
微生物对分子量小的,物理、化学性质稳定的生物酸,产生耐药性的,生物学机能不健全。所以,病原微生物,不容易对小分子生物酸产生耐药性。例如:微生物对乳酸、蚁酸、乙酸,不易产生耐药性。
在选用油剂时,单纯应用一种油剂,尚达不到小分子生物酸药剂学、药理学、毒理学的最佳要求,从多种油剂中选择顺应小分子生物酸理化性质的油剂,以达到药理作用显著提高的目的。
《合成实用香料手册》记载,目前,国外已经认定能安全食用的香料有1700 多种。包括:烃类及其衍生物、醇类、醚类、酚类及其衍生物、醛类、缩醛类、酮类、内酯类、酸类、酯类、含硫含氮化合物……。本发明经过多年的实验研究,发现只有醇类、酮类和酯类的精油适合做小分子生物酸的溶剂载体,具有一定的实用性。
在上述研究的基础上,为了提供可以用作预防和治疗鼻病毒、流感病毒、新型冠状病毒等多种病毒、细菌感染的小分子生物酸药物,本发明的第一方面是,提供一种小分子生物酸类抗病毒、抗菌油溶性制剂,含有小分子生物酸作为有效药物成分,所述小分子生物酸溶解于油油互溶体或油水互溶体,所述油油互溶体或油水互溶体,是与小分子生物酸互溶性的油类,得到本发明的小分子生物酸类抗病毒、抗菌油溶性制剂。将所述小分子生物酸油溶性制剂,与可药用赋形剂配制而成多种剂型的小分子生物酸抗病毒、抗菌药物。这种药物,可用作抗鼻病毒、流感病毒以及常感染人的其他病毒、病菌的药物,是可首选用于预防和治疗新型冠状病毒感染的药物。
优选的,所述油水互溶体或油油互溶体的油类含有醇类、酮类和/或酯类的精油。
优选的,所述小分子生物酸,包括蚁酸(甲酸)、乙二酸(草酸)、乳酸、丙酸、山梨酸或苯甲酸。
优选的,所述精油,包括:油酸乙酯、苯乙酸甲酯、三硬脂酸甘油酯等酯类,2-丁酮、2-戊酮、3-庚酮、左旋香芹酮等酮类,丙二醇、丙三醇、苯甲醇、十八醇等醇类或硬脂酸中一种或者一种以上。
本发明的第二方面是,提供一种透皮吸收涂剂,含有蚁酸作为有效药物成分,蚁酸溶剂载体为油油互溶体,包括:
蚁酸:1440.0-1920.0mg
油酸乙酯:259.2-345.6g
酮类精油:28.8-38.4g
酯类精油:28.8-38.4g
十八醇:40.0-80.0g
硬脂酸:40.0-80.0g
乳化剂(吐温-80)70.0-90.0g
其余蒸馏水总量1200.0g
制成每克含蚁酸1.2-1.6mg的透皮吸收涂剂。
本发明的第三方面是,提供一种蚁酸静脉滴注剂,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油水互溶体,包括:
蚁酸:600.0-800.0mg
2-丁酮:120.0-160.0g
2-戊酮:12.0-16.0g
3-庚酮:12.0-16.0g
其余为生理注射用水,液体总量25000.0ml,制成一次剂量为每250ml滴注剂含6.0-8.0mg蚁酸的静脉滴注剂。
本发明的第四方面是,提供一种蚁酸口服胶囊,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油油互溶体,包括:
蚁酸:12000.0mg
油酸乙酯:1320.0g
苯乙酸甲酯:480.0g
谷朊粉:4788.0g
制成总量:12000粒,每粒重量0.55g,每粒含蚁酸1.0mg的口服胶囊。
本发明的第五方面是,提供一种蚁酸油溶性口服软胶囊,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油油互溶体,包括:
蚁酸:6000.0mg
油酸乙酯:660.0g
苯乙酸甲酯:240.0g
三硬脂酸甘油酯:300.0g
明胶及***胶、增塑剂等软胶囊用材料适量,制成:总量为6000粒的蚁酸油溶性口服软胶囊,每粒含蚁酸1.0mg。
本发明的第六方面是,提供一种油溶性蚁酸口服丸剂,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油油互溶体,包括:
蚁酸:12000.0mg
油酸乙酯:1320.0g
苯乙酸甲酯:480.0g
淀粉:适量
谷朊粉:适量
中蜂蜂蜜:适量
制成蚁酸口服丸剂2000丸,每丸6.15g,每丸含蚁酸6.0mg。
由于中蜂蜂蜜属于中药原料药,所以该丸剂也可称为中西药结合的丸剂。
本发明的第七方面是,提供一种乙二酸油溶性口服软胶囊,含有乙二酸作为有效药物成分,其特征在于,乙二酸溶剂载体为油油互溶体,包括:
乙二酸:4500.0—6000.0mg
苯乙酸甲酯:720.0—960.0g
左旋香芹酮:225.0—300.0g
三硬脂酸甘油酯:150.0-280.0g
明胶及***胶、增塑剂等软胶囊用材料适量,制成:总量为3000粒的乙二酸油溶性口服软胶囊,每粒含乙二酸1.5—2.0mg,每日2次,每次2粒。每天 6.0-8.0mg。
本发明的第八方面是,提供一种油溶性乙二酸口服丸剂,含有乙二酸作为有效药物成分,其特征在于,乙二酸溶剂载体为油油互溶体,包括:
乙二酸:5200.00-7600.0mg
苯乙酸甲酯:832.00-1216.0g
左旋香芹酮:260-380.0g
淀粉:2225.7-2098.0g
谷朊粉:2225.7-2098.0g
中蜂蜂蜜:4451.0-4197.0g
制成乙二酸口服丸剂2000丸,每丸5.0g,每丸含乙二酸2.6-3.8mg。
本发明的第九方面是,提供一种乳酸油溶性消毒防护口罩液,含有乳酸作为有效药物成分,其特征在于,乳酸溶剂载体为油水互溶体,按下列成份:
乳酸:25.0-42.0g(占总量的0.25%—0.42%)
丙三醇:9863.0-9732.0g
苯甲醇:10.0-20.0g(占总量的0.1%—0.2%)
余量为蒸馏水:100.0-200.0g。制得乳酸油溶性防护口罩液10000ml。将所得溶剂喷涂在载体上,制成含乳酸溶液口罩。
本发明的第十方面是,提供一种蚁酸油溶性防护口罩液,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油水互溶体,按下列成份:
蚁酸:1.0—2.0g(占总量的0.01%—0.02%)
丙三醇:9799.0-9598.0g
丙二醇:100.0-200.0g(占总量的1%—2%)
余量为蒸馏水:100.0-200.0g。制得蚁酸油溶性防护口罩液10000ml。将所得溶剂喷涂在载体上,制成含蚁酸溶液防护口罩或湿巾。
本发明的第十一方面是,提供一种乙二酸油溶性防护口罩液,含有乙二酸作为有效药物成分,其特征在于,乙二酸溶剂载体为油水互溶体,按下列成份:
乙二酸:6.0-12.0g(占总量的0.06%—0.12%)
丙三醇:9794.0-9588.0g
丙二醇:100.0-200.0g(占总量的1%—2%)
余量为蒸馏水,制得乙二酸油溶性防护口罩液10000ml。将所得溶剂喷涂在载体上,制成含乙二酸溶液口罩。
本发明的第十二方面是,提供一种制备抗新冠病毒生态抗生素灭活疫苗用的蚁酸抗生素溶体,其特征在于,所述溶体为蚁酸油油互溶体、蚁酸油水互溶体、乙二酸或者乳酸油油互溶体制备而成的灭活口服疫苗。
下面,通过实施例对本发明的技术方案给予进一步的说明。
具体实施方式
这里将详细地对示例性实施例进行说明,以下示例性实施例中所描述的实施方式并不代表与本发明相一致的所有实施方式。它们仅是进一步所详述地说明本发明一些方面相一致的小分子生物酸油油互溶体、油水互溶体及其配制方法的例子。
在下面实施例中使用的原料:
1、蚁酸等小分子生物酸原料为现有技术得到的优级品。
2、其它原料为精制工业品。
实施例1
制备油油互溶体的透皮吸收涂剂,按下列成份:
蚁酸:1440.0-1920.0mg
油酸乙酯:259.2-345.6g
酮类精油:28.8-38.4g
酯类精油:28.8-38.4g
十八醇:40.0-80.0g
硬脂酸:40.0-80.0g
乳化剂(吐温-80)70.0-90.0g
其余蒸馏水总量1200.0g
制成每克含蚁酸1.2-1.6mg的透皮吸收涂剂。
60kg成人每天在胸、背、四肢健康皮肤涂抹3次,每次应用3.0g该皮肤吸收涂剂,该皮肤吸收涂剂中含蚁酸10.08-14.4mg。该制剂通过淋巴***进入血液循环,在呼吸道、肠道靶点药物浓度高,治疗流感等呼吸***感染,疗效显著。可优先选用于治疗鼻病毒、流感病毒、新型冠状病毒等病毒、病菌的感染。
实施例2
制备蚁酸静脉滴注剂,按下列成份:
蚁酸:600.0-800.0mg
2-丁酮:120.0-160.0g
2-戊酮:12.0-16.0g
3-庚酮:12.0-16.0g
其余为生理注射用水,液体总量25000.0ml;制成一次剂量为每250ml滴注剂含6.0-8.0mg蚁酸的静脉滴注剂。
应用于不适合透皮吸收剂及口服剂的患者。每日静脉滴注2次,每天蚁酸计量为12.0-16.0mg。可选用于治疗新型冠状病毒、流感病毒等病毒、病菌感染的危重症患者。
实施例3
制备蚁酸口服胶囊,按下列成份:
蚁酸:12000.0mg
油酸乙酯:1320.0g
苯乙酸甲酯:480.0g
谷朊粉:4788.0g
制成总量:12000粒,每粒重量0.55g,每粒含蚁酸1.0mg的口服胶囊。
60kg成人,每日2次,每次4—6粒,每日蚁酸剂量约为8.0-12.0mg。可优先选用于治疗鼻病毒、流感病毒、新型冠状病毒等病毒、病菌的感染。
实施例4
制备蚁酸油溶性口服软胶囊,按下列成份:
蚁酸:6000.0mg
油酸乙酯:660.0g
苯乙酸甲酯:240.0g
三硬脂酸甘油酯:300.0g
明胶及***胶、增塑剂等软胶囊用材料适量,制成:总量为6000粒的蚁酸油溶性口服软胶囊,每粒含蚁酸1.0mg。
60kg成人治疗呼吸***病毒、细菌感染,每日2次,每次4—6粒。相当于含纯蚁酸8.0—12.0mg。可用于治疗、预防流感和新型冠状病毒感染。
实施例5
制备油溶性蚁酸口服丸剂,按下列成份:
蚁酸:12000.0mg
油酸乙酯:1320.0g
苯乙酸甲酯:480.0g
淀粉:适量
谷朊粉:适量
中蜂蜂蜜:适量
制成蚁酸口服丸剂2000丸,每丸6.15g,每丸含蚁酸6.0mg。
60kg成人,每天2次,每次1丸。可优先选用于治疗和预防新型冠状病毒、流感病毒等病毒、病菌的感染。由于中蜂蜂蜜属于中药原料药,所以该丸剂也可称为中西药结合的丸剂。
实施例6
制备乙二酸油溶性口服软胶囊,按下列成份:
乙二酸:4500.0—6000.0mg
苯乙酸甲酯:720.0—960.0g
左旋香芹酮:225.0—300.0g
三硬脂酸甘油酯:150.0-280.0g
明胶及***胶、增塑剂等软胶囊用材料适量,制成:总量为3000粒的乙二酸油溶性口服软胶囊,每粒含乙二酸1.5—2.0mg。成人每天2次,每次2粒,即,应用乙二酸含量为6.0-8.0mg。可选用于治疗和预防新型冠状病毒、流感病毒及以其他常感染人的病毒、病菌的在呼吸道的感染。
实施例7
制备油溶性乙二酸口服丸剂,按下列成份:
乙二酸:7600.0mg
苯乙酸甲酯:1216.0g
左旋香芹酮:380.0g
淀粉:2098.0g
谷朊粉:2098.0g
中蜂蜂蜜:4197.0g
制成乙二酸口服丸剂2000丸,每丸重5.0g,每丸含乙二酸3.8mg。
实施例8
一种乳酸油溶性防护口罩液,按下列成份:
乳酸:25.0-42.0g(占总量的0.25%—0.42%)
丙三醇:9863.0-9732.0g
苯甲醇:10.0-20.0g(占总量的0.1%—0.2%)
余量为蒸馏水,制得乳酸油溶性防护口罩液10000ml。将所得溶剂喷涂在载体上,制成含乳酸油溶性液防护口罩。
实施例9
一种蚁酸油溶性消毒防护口罩液,按下列成份:
蚁酸:1.0—2.0g(占总量的0.01%—0.02%)
丙三醇:9799.0-9598.0g
丙二醇:100.0-200.0g(占总量的1%—2%)
余量为蒸馏水,制得蚁酸油溶性消毒防护口罩液10000ml。将所得溶剂喷涂在载体上,制成含蚁酸溶液消毒口罩、湿巾。
实施例10
一种乙二酸油溶性防护口罩液,按下列成份:
乙二酸:6.0-12.0g(占总量的0.06%—0.12%)
丙三醇:9794.0-9588.0g
丙二醇:100.0-200.0g(占总量的1%—2%)
余量为蒸馏水,制得乙二酸油溶性防护口罩液10000ml。将所得溶剂喷涂在载体上,制成含乙二酸溶液防护口罩。
临床应用实例
利用本发明制备的制剂进行临床使用,收到明显效果。
1、对其中5名新冠病毒症状明显的疑似人员,利用实施例3制备的蚁酸口服胶囊,按60kg成人,每日2次,每次6粒,每日蚁酸剂量约为12.0mg。每次应用6.0mg,应用12小时后,鼻塞、发热症状消失,咳嗽症状减轻。24小时后,痰较易咳出。用药3日后,自觉症状消失,停止用药。
2、对其中12名普通感病人,出现的流涕、鼻塞,浑身无力,咳嗽的患者,利用实施例5制备的蚁酸丸剂,每天2次,每次1丸,每次应用6.0mg,应用1 日后,乏力、咳嗽,流涕、鼻塞症状减轻,应用4日后,患者自觉症状消失,停止用药。
3、对20多名申请人公司的工作人员及其亲属,应用实施例8、实例9制备的含乳酸、蚁酸油溶性防疫口罩液,在人员流动(出差)前,将该液体均匀的喷到一性次口罩外层,该口罩使用2-4天丢弃更换。在国内疫情流行区流动(出差),经过多次实验,使用该种防疫口罩的人员均保持健康,没有出现新型冠状病毒核酸阳性的试用者。
对应用本发明的临床应用结果表明,本发明对新型冠状病毒、流感病毒等病毒、病菌的感染方面,会具有重要的预防和治疗效果。
本领域技术人员在考虑说明书所公开的内容后,将容易想到本发明的其它实施方案。本申请旨在涵盖本发明的任何变型、用途或者适应性变化,这些变型、用途或者适应性变化遵循本发明的一般性原理并包括本发明未公开的本技术领域中的公知常识或惯用技术手段。说明书和实施例仅被视为示例性的,本发明的真正范围和精神由权利要求书指出。
应当理解的是,本发明并不局限于上面已经描述的精确结构,并且可以在不脱离其范围进行各种修改和改变。本发明的范围仅由权利要求书来限制。
Claims (14)
1.一种小分子生物酸类抗病毒、抗菌油溶性制剂,含有小分子生物酸作为有效药物成分,其特征在于,是将所述小分子生物酸溶解于油油互溶体或油水互溶体,所述的小分子生物酸类,包括:蚁酸、乙二酸、乳酸、丙酸、山梨酸或苯甲酸,所述油油互溶体或油水互溶体,是与小分子生物酸互溶性的油类。
2.根据权利要求1所述的小分子生物酸类抗病毒、抗菌制剂,其特征在于,所述油类,包括:油酯类、醇类、酮类和/或内酯类的精油。
3.根据权利要求2所述的小分子生物酸类抗病毒、抗菌制剂,其特征在于,所述精油,包括:油酸乙酯、苯乙酸甲酯、三硬脂酸甘油酯等油酯类,2-丁酮、2-戊酮、3-庚酮、左旋香芹酮等酮类、丙二醇、丙三醇、苯甲醇、十八醇等醇类或硬脂酸中一种或者一种以上。
4.一种透皮吸收涂剂,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油油互溶体,按下列成份:
蚁酸:1440.0-1920.0mg
油酸乙酯:259.2-345.6g
酮类精油:28.8-38.4g
酯类精油:28.8-38.4g
十八醇:40.0-80.0g
硬脂酸:40.0-80.0g
乳化剂(吐温-80)70.0-90.0g
其余蒸馏水总量1200.0g
制成每克含蚁酸1.2-1.6mg的透皮吸收涂剂。
5.一种蚁酸静脉滴注剂,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油水互溶体,按下列成份:
蚁酸:600.0-800.0mg
2-丁酮:120.0-160.0g
2-戊酮:12.0-16.0g
3-庚酮:12.0-16.0g
其余为生理注射用水:液体总量25000.0ml;制成一次剂量为每250ml滴注剂含6.0-8.0mg蚁酸的静脉滴注剂。
6.一种蚁酸口服胶囊,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油油互溶体,按下列成份:
蚁酸:12000.0mg
油酸乙酯:1320.0g
苯乙酸甲酯:480.0g
谷朊粉:4788.0g
制成总量:12000粒,每粒重量0.55g,每粒含蚁酸1.0mg的口服胶囊。
7.一种蚁酸油溶性口服软胶囊,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油油互溶体,按下列成份:
蚁酸:6000.0mg
油酸乙酯:660.0g
苯乙酸甲酯:240.0g
三硬脂酸甘油酯:300.0g
明胶及***胶、增塑剂等软胶囊用材料适量,制成:总量为6000粒的蚁酸油溶性口服软胶囊,每粒含蚁酸1.0mg。
8.一种油溶性蚁酸口服丸剂,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油油互溶体,按下列成份:
蚁酸:12000.0mg
油酸乙酯:1320.0g
苯乙酸甲酯:480.0g
淀粉:适量
谷朊粉:适量
中蜂蜂蜜:适量
制成蚁酸口服丸剂2000丸,每丸6.15g,每丸含蚁酸6.0mg。
9.一种乙二酸油溶性口服软胶囊,含有乙二酸作为有效药物成分,其特征在于,乙二酸溶剂载体为油油互溶体,按下列成份:
乙二酸:4500.0—6000.0mg
苯乙酸甲酯:720.0—960.0g
左旋香芹酮:225.0—300.0g
三硬脂酸甘油酯:150.0-280.0g
明胶及***胶、增塑剂等软胶囊用材料适量,制成:总量为3000粒的乙二酸油溶性口服软胶囊,每粒含乙二酸1.5—2.0mg。
10.一种油溶性乙二酸口服丸剂,含有乙二酸作为有效药物成分,其特征在于,乙二酸溶剂载体为油油互溶体,按下列成份:
乙二酸:7600.0mg
苯乙酸甲酯:1216.0g
左旋香芹酮:380.0g
淀粉:2098.0g
谷朊粉:2098.0g
中蜂蜂蜜:4197.0g
制成乙二酸口服丸剂2000丸,每丸重5.0g,每丸含乙二酸3.8mg。
11.一种乳酸油溶性防护口罩液,含有乳酸作为有效药物成分,其特征在于,乳酸溶剂载体为油水互溶体,按下列成份:
乳酸:25.0-42.0g
丙三醇:9863.0-9732.0g
苯甲醇:10.0-20.0g
余量为蒸馏水,制得乳酸油溶性防护口罩液10000ml。
12.一种蚁酸油溶性防护口罩液,含有蚁酸作为有效药物成分,其特征在于,蚁酸溶剂载体为油水互溶体,按下列成份:
蚁酸:1.0—2.0g
丙三醇:9799.0-9598.0g
丙二醇:100.0-200.0g
余量为蒸馏水,制得蚁酸油溶性防护口罩液10000ml。
13.一种乙二酸油溶性防护口罩液,含有乙二酸作为有效药物成分,其特征在于,乙二酸溶剂载体为油水互溶体,按下列成份:
乙二酸:6.0-12.0g
丙三醇:9794.0-9588.0g
丙二醇:100.0-200.0g
余量为蒸馏水,制得乙二酸油溶性防护口罩液10000ml。
14.一种制备抗新型冠状病毒的生态抗生素灭活疫苗用的蚁酸抗生素溶体,其特征在于,所述溶体为蚁酸油油互溶体、蚁酸油水互溶体、乙二酸或者乳酸油油互溶体制备而成的灭活口服疫苗。
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US6133317A (en) * | 1995-11-15 | 2000-10-17 | Hart; Francis J. | Oxalic acid or oxalate composition and method of treatment |
CN113855668A (zh) * | 2020-05-25 | 2021-12-31 | 甘肃芫美药业有限公司 | 一种斑蝥素抗病毒、抗菌制剂、其制备方法及用作预防和治疗新型冠状病毒感染 |
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US6133317A (en) * | 1995-11-15 | 2000-10-17 | Hart; Francis J. | Oxalic acid or oxalate composition and method of treatment |
CN113855668A (zh) * | 2020-05-25 | 2021-12-31 | 甘肃芫美药业有限公司 | 一种斑蝥素抗病毒、抗菌制剂、其制备方法及用作预防和治疗新型冠状病毒感染 |
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