CN1048870C - 血防用吡喹酮涂肤纸巾 - Google Patents
血防用吡喹酮涂肤纸巾 Download PDFInfo
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- CN1048870C CN1048870C CN93111598A CN93111598A CN1048870C CN 1048870 C CN1048870 C CN 1048870C CN 93111598 A CN93111598 A CN 93111598A CN 93111598 A CN93111598 A CN 93111598A CN 1048870 C CN1048870 C CN 1048870C
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- FSVJFNAIGNNGKK-UHFFFAOYSA-N 2-[cyclohexyl(oxo)methyl]-3,6,7,11b-tetrahydro-1H-pyrazino[2,1-a]isoquinolin-4-one Chemical compound C1C(C2=CC=CC=C2CC2)N2C(=O)CN1C(=O)C1CCCCC1 FSVJFNAIGNNGKK-UHFFFAOYSA-N 0.000 title claims abstract description 19
- 229960002957 praziquantel Drugs 0.000 title claims abstract description 19
- 230000002265 prevention Effects 0.000 title claims abstract description 15
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims abstract description 24
- 239000007788 liquid Substances 0.000 claims abstract description 22
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 19
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- 239000004698 Polyethylene Substances 0.000 claims description 4
- 230000000149 penetrating effect Effects 0.000 claims description 4
- -1 polyethylene Polymers 0.000 claims description 4
- 229920000573 polyethylene Polymers 0.000 claims description 4
- 239000004745 nonwoven fabric Substances 0.000 claims description 3
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 abstract description 13
- 201000004409 schistosomiasis Diseases 0.000 abstract description 7
- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 abstract description 6
- 230000001681 protective effect Effects 0.000 abstract description 4
- 238000005269 aluminizing Methods 0.000 abstract description 3
- 239000002131 composite material Substances 0.000 abstract description 3
- 241000242678 Schistosoma Species 0.000 abstract description 2
- 230000035515 penetration Effects 0.000 abstract description 2
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000012528 membrane Substances 0.000 abstract 1
- 241001465754 Metazoa Species 0.000 description 8
- 241000754688 Cercaria Species 0.000 description 7
- 201000010099 disease Diseases 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 7
- 238000011010 flushing procedure Methods 0.000 description 7
- LAOOXBLMIJHMFO-UHFFFAOYSA-N 1-[2-(diethylamino)ethylamino]-4-methylthioxanthen-9-one;hydron;chloride Chemical compound Cl.S1C2=CC=CC=C2C(=O)C2=C1C(C)=CC=C2NCCN(CC)CC LAOOXBLMIJHMFO-UHFFFAOYSA-N 0.000 description 5
- 230000001843 schistosomicidal effect Effects 0.000 description 5
- 208000015181 infectious disease Diseases 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 231100000252 nontoxic Toxicity 0.000 description 3
- 230000003000 nontoxic effect Effects 0.000 description 3
- 238000004806 packaging method and process Methods 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 238000012856 packing Methods 0.000 description 2
- 239000004033 plastic Substances 0.000 description 2
- 229920003023 plastic Polymers 0.000 description 2
- 238000005406 washing Methods 0.000 description 2
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 description 1
- 241000242722 Cestoda Species 0.000 description 1
- 206010016322 Feeling abnormal Diseases 0.000 description 1
- 206010016825 Flushing Diseases 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 102000011759 adducin Human genes 0.000 description 1
- 108010076723 adducin Proteins 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 239000004411 aluminium Substances 0.000 description 1
- 230000003616 anti-epidemic effect Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000003640 drug residue Substances 0.000 description 1
- 238000005485 electric heating Methods 0.000 description 1
- 230000001815 facial effect Effects 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 230000002458 infectious effect Effects 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 238000002791 soaking Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000005303 weighing Methods 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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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
血防用吡喹酮涂肤纸巾,是一种用于血防的防护药剂,它采用含有促渗透剂二甲基亚砜的吡喹酮乙醇水溶液配制成护肤液,使护肤液的防血吸虫尾蚴侵袭作用能够在水中维持四小时以上,同时选择纸巾和镀铝复合膜包装袋,制成了防疫现场实用的新剂型药品。
Description
本发明涉及一种使用在血吸虫病疫区,特别是可涂搽在人畜皮肤表面的防护药剂。
在血吸虫病疫区使用的涂搽皮肤的药液,防止血吸虫尾蚴钻入皮肤而造成感染,是血防工作的重要研究项目。几十年来曾建立过多种筛选模型,试验了大量的配方,但都未能推广应用,这是因为它们缺乏实用于血防的护肤药剂所必须具备的几个特点,如:1.含有高效防护作用的主药;2.涂搽皮肤后能耐水冲洗的配方;3.使用方便的药剂;以及一般药品应有的安全无刺激无毒等性质。吡喹酮问世以后,因其在极低浓度下即有杀灭尾蚴的作用,解决了对高效主药的要求,也由此而产生了它的外用配方和喷涂剂型,如西德专利DE3619030.6(见对比文献一)。但在重复试验时,发现该专利的配方在配料选择和设计中未考核所成保护膜的防水冲洗性能。由于血吸虫病传染的形体为尾蚴,尾蚴生活在水中,饲机钻入人畜皮肤而使人畜受到感染,当水温在25~30℃时,尾蚴在水中最活跃,因此,疫水(含尾蚴的水)是传染媒介,耐疫水试验应在四小时以上,才能适应实际防疫的需要。我们发现,不同类型的多种配方,包括前述西德专利中的数种配方,都不能耐受一小时以上的30℃水冲洗,不适应防疫实际要求。
本发明的目的在于针对上述西德专利存在着的防水耐冲洗性能差这一主要问题,提出了一种在血吸虫病疫区使用的,可涂搽在人畜皮肤表面上的防护药剂,后者具有高效、无毒、无刺激性质,尤其是具有强渗透力,能够进入皮肤角质层下从而具有长效耐水浸泡冲洗性能。
本发明所述防疫血吸虫病的涂肤药剂,其药液由主药吡喹酮,促渗透剂二甲基亚砜,溶剂乙醇水溶液组成,吡喹酮在常温下为白色固体粉末,它在药液中的浓度为0.1~5%(W/V);二甲基亚砜在室温下为无色液体,它在药液中的浓度为0.5~20%(W/V);乙醇水溶液在常温下为无色液体,它在药液中的浓度为60~75%(W/V);余量为水。上述药液载体选用无纺布纸巾,它可最大限度地吸收药液,并贮存在纤维孔隙中,纸巾外用聚乙烯镀铝复合膜密封包装。本发明的配制,只需称取吡喹酮与二甲基亚砜,置玻璃或搪玻璃容器内,加入部分乙醇水溶液搅拌溶解,再加乙醇水溶液至所需计量,搅拌均匀,取样测定含量,合格后分装在盛有纸巾的铝塑包装袋中,电热封口,即得。使用时,拆开包装袋,取出纸巾,涂遍人畜皮肤表面与疫水可能接触的那些部位,可以在疫水中经受四小时以上的疫水冲洗。
表1吡喹酮残留量与小鼠尾蚴感染的防护作用的关系水流冲洗时间(小时)
0 2 4 8药物残留量(μg) 50 5 3 0防护率(%) 100 97.5 92.1 62.8*在检出限度以下注:此表处方含吡喹酮0.5g,二甲基亚砜2.0g,95%乙
醇水溶液加至100ml表2 不同配方对尾蚴的防护效果处方号 水流冲洗时间(小时)
0 2 41 防护率(%) 100 97.5 92.12 防护率(%) 100 100 100
注:处方1号含吡喹酮0.5g,二甲基亚砜2.0g,95%乙
醇加至100ml
处方2号含吡喹酮2.0g,二甲基亚砜8.0g,95%乙
醇加至100ml
本发明提出了新的血防药物及包装形式,利用人畜皮肤表层作为药物贮库,选用安全、无毒、价廉、被卫生部门认可的化合物作促渗透剂,可使药物滞留在皮肤表层,防止血吸虫尾蚴钻入人畜皮肤从而使人畜受到感染,具有长效、耐水冲洗的功能,其耐疫水浸泡冲洗可达4小时以上。为了使药物方便地适用于血防现场,本发明采用纸巾剂型,它是血防用新的药物剂型,该纸巾具有最大的吸储药液能力,最小的不能被利用的药液体积比,最好的耐磨、耐拉性和柔软感,并且不含有影响药液稳定性及含量测定的添加剂。纸巾包装袋选用具有良好的抗渗透力、耐高温的镀铝复合聚乙烯膜,它可抵抗60℃二小时水浸泡,40℃一个月以上的恒温干燥和三天日光曝晒。
本发明的方案通过以下方法实施:
取吡喹酮2g,二甲基亚砜8g,加入30ml的95%乙醇水溶液,搅拌至溶解,继续加入95%乙醇水溶液至100ml,搅拌均匀,此时吡喹酮在溶液中的浓度为2%(W/V),二甲基亚砜的浓度为8%(W/V),乙醇在溶液中的浓度为70%(W/V),其余为水。
药液配成后,用无纺布纸巾吸收药液20ml,装入镀铝复合聚乙烯塑料袋,电热压封口。使用时拉开包装袋,用纸巾涂搽与疫水接触的皮肤1~2遍可防止尾有蚴感染。防护作用在水中可达四小时以上。
本药液的配方,也可以采用二甲基甲酰胺、氮酮和它们及它们与二甲基亚砜的复合配方作为促渗透剂,将主药吡喹酮贮入皮肤角质层以下,达到长效防护的目的。
Claims (2)
1.一种血防用吡喹酮涂肤纸巾,其药液由主药吡喹酮,促渗透剂二甲基亚砜,溶剂乙醇水溶液组成,吡喹酮在药液中的浓度为0.1~5%(W/V);二甲基亚砜在药液中的浓度为0.5~20%(W/V);乙醇在药液中的浓度为60~75%(W/V);余量为水。
2.根据权利要求1所述的血防用吡喹酮涂肤纸巾,它的药液载体选用无纺布纸巾,使用聚乙烯镀铝复合膜密封包装。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN93111598A CN1048870C (zh) | 1993-07-30 | 1993-07-30 | 血防用吡喹酮涂肤纸巾 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN93111598A CN1048870C (zh) | 1993-07-30 | 1993-07-30 | 血防用吡喹酮涂肤纸巾 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1085428A CN1085428A (zh) | 1994-04-20 |
| CN1048870C true CN1048870C (zh) | 2000-02-02 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN93111598A Expired - Fee Related CN1048870C (zh) | 1993-07-30 | 1993-07-30 | 血防用吡喹酮涂肤纸巾 |
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| CN (1) | CN1048870C (zh) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102860981A (zh) * | 2012-10-26 | 2013-01-09 | 天津必佳药业集团有限公司 | 牛羊用抗血吸虫病吡喹酮透皮溶液及其制备方法 |
| CN203815368U (zh) * | 2013-04-17 | 2014-09-10 | 惠美世界有限公司 | 卷筒型湿纸巾分配器 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3619030A1 (de) * | 1986-06-06 | 1987-12-10 | Bayer Ag | Topisch anwendbare zubereitungen |
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1993
- 1993-07-30 CN CN93111598A patent/CN1048870C/zh not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3619030A1 (de) * | 1986-06-06 | 1987-12-10 | Bayer Ag | Topisch anwendbare zubereitungen |
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| Publication number | Publication date |
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| CN1085428A (zh) | 1994-04-20 |
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