CN1451388A - 防治病毒引起非典型性肺炎等传染病的药物 - Google Patents
防治病毒引起非典型性肺炎等传染病的药物 Download PDFInfo
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Abstract
一种防治病毒引起非典型性肺炎等传染病的药物,其成分为:利巴韦林、卵磷脂或豆磷脂、D-葡萄糖、乳糖、胆固醇、无水乙醇、磷酸盐缓冲液。该药物制备方法是:将卵磷脂或豆磷脂用乙醇溶解,加入磷酸盐缓冲液,进行减压蒸馏,置组织捣细机搅拌,经过灭菌处理后,加入利巴韦林、D-葡萄糖、乳糖、胆固醇,再加入经灭菌后的0.01ml/L磷酸盐缓冲液至总药液量为1000-2000ml,膜过滤,灌装后冷冻干燥,制成成品。本发明的优点是:将以利巴韦林为有效成分的药物制成脂质体,使药物主要在血液循环***、肝、脾、肺、骨髓等组织器官中蓄积,从而提高了药物的治疗指数,减少了药物的治疗剂量,大大降低药物的毒副作用。
Description
技术领域
本发明涉及一种药物,特别是指一种用于预防和治疗病毒引起的严重呼吸***综合症(非典型性肺炎)、流感、甲型肝炎、肺炎、疱疹、麻疹等传染性疾病的药物。
背景技术
病毒引起的严重呼吸***综合症(非典型性肺炎)、流感、甲型肝炎、肺炎、疱疹、麻疹等传染性疾病,对人的健康危害性很大,甚至会危及人的生命,而且一些疾病具有传染性,对整个社会都会造成很大影响。已知利巴韦林单方制剂(普通制剂)对防治病毒性传染疾病能够起到一定的作用,但需使用较大剂量,而且在使用剂量大的情况下药物同时产生较强的毒副作用,如致畸、对心脏损害、对呼吸***可致患者呼吸困难,胸痛等。
发明内容
本发明的目的在于提供一种防治病毒引起非典型性肺炎等传染病的药物,以利巴韦林为有效成分,将其制成脂质体,使药物主要在血液循环***、肝、脾、肺和骨髓等组织器官中蓄积,提高药物的治疗指数,减少药物的治疗剂量,大大降低药物的毒副作用。
本发明的上述目的可以通过以下技术方案来实现。
一种防治病毒引起非典型性肺炎等传染病的药物,其成分及配比如下:
利巴韦林 50-100克
卵磷脂或豆磷脂 利巴韦林摩尔数的8-10倍
D-葡萄糖 20-30克
乳糖 30-40克
胆固醇 利巴韦林摩尔数的8-10倍
无水乙醇 200-400ml
磷酸盐缓冲液(0.01mol/L 至总量为1000-2000ml
PH值4.0-8.0)
本发明提供的药物经以下工艺制成:
1、将卵磷脂或豆磷脂用乙醇溶解,加入0.01ml/L磷酸盐缓冲液,混合均匀,进行减压蒸馏;
2、待乙醇挥发尽后,置组织捣细机搅拌5-15分钟,在115-125℃下蒸汽灭菌30分钟,用超声波超声搅拌两次,每次10分钟;
3、加入利巴韦林、D-葡萄糖、乳糖、胆固醇,至完全溶解后,再加入经灭菌后的0.01ml/L磷酸盐缓冲液至总药液量为1000-2000ml,用0.22μm的膜过滤;
4、灌装药液,并半加塞,送入冷冻干燥箱内,在-30-40℃和2-50Pa下冷冻干燥,使制品水分≤3%后,压塞,轧盖,成品检验合格,包装入库。
本发明提供的药物其优点是:将以利巴韦林为有效成分的药物制成脂质体,使药物主要在血液循环***、肝、脾、肺、骨髓等组织器官中蓄积,从而提高了药物的治疗指数,减少了药物的治疗剂量,大大降低药物的毒副作用。
具体实施方式
下面提供本发明的实施例。
实施例1:
一种防治病毒引起非典型性肺炎等传染病的药物,其成分及配比如下:
利巴韦林 50克
卵磷脂或豆磷脂 利巴韦林摩尔数的8倍
D-葡萄糖 20克
乳糖 30克
胆固醇 利巴韦林摩尔数的8倍
无水乙醇 200ml
磷酸盐缓冲液(0.01mol/L 至总量为1000ml
PH值4.5)
本药物的制备方法如下:
1、将卵磷脂或豆磷脂用乙醇溶解,加入适量0.01ml/L磷酸盐缓冲液,混合均匀,进行减压蒸馏;
2、待乙醇挥发尽后,置组织捣细机搅拌5-15分钟,在115-125℃下蒸汽灭菌30分钟,用超声波超声搅拌两次,每次10分钟;
3、加入利巴韦林、D-葡萄糖、乳糖、胆固醇,至完全溶解后,再加入经灭菌后的0.01ml/L磷酸盐缓冲液至总药液量为1000ml,用0.22μm的膜过滤;
4、用西林瓶灌装药液,分装成1000支,并半加塞,送入冷冻干燥箱内,在-30-40℃和2-50Pa下冷冻干燥,使制品水分≤3%后,压塞,轧盖,制成冻干针剂,成品检验合格,包装入库。
实施例2:
一种防治病毒引起非典型性肺炎等传染病的药物,其成分及配比如下:
利巴韦林 100克
卵磷脂或豆磷脂 利巴韦林摩尔数的10倍
D-葡萄糖 30克
乳糖 40克
胆固醇 利巴韦林摩尔数的10倍
无水乙醇 400ml
磷酸盐缓冲液(0.01mol/L 至总量为2000ml
PH值6.0-8.0)
本药物的制备方法如下:
1、将卵磷脂或豆磷脂用乙醇溶解,加入适量0.01ml/L磷酸盐缓冲液,混合均匀,进行减压蒸馏;
2、待乙醇挥发尽后,置组织捣细机搅拌5-15分钟,在115-125℃下蒸汽灭菌30分钟,用超声波超声搅拌两次,每次10分钟;
3、加入利巴韦林、D-葡萄糖、乳糖、胆固醇,至完全溶解后,再加入经灭菌后的0.01ml/L磷酸盐缓冲液至总药液量为2000ml,用0.22μm的膜过滤;
4、用西林瓶灌装药液,分装成1000支,并半加塞,送入冷冻干燥箱内,在-30-40℃和2-50Pa下冷冻干燥,使制品水分≤3%后,压塞,轧盖,制成冻干针剂,成品检验合格,包装入库。
本发明也可将冻干针剂按1支溶于含氮酮2-10%,10-20%的无水乙醇的无菌注射用水中,灌入喷雾器瓶中,制成喷雾剂。
Claims (3)
1、一种防治病毒引起非典型性肺炎等传染病的药物,其特征在于它的成分及配比如下:
利巴韦林 50-100克
卵磷脂或豆磷脂 利巴韦林摩尔数的8-10倍
D-葡萄糖 20-30克
乳糖 30-40克
胆固醇 利巴韦林摩尔数的8-10倍
无水乙醇 200-400ml
磷酸盐缓冲液(0.01mol/L 至总量为1000-2000ml
PH值4.0-8.0)
2、一种如权利要求1所述防治病毒引起非典型性肺炎等传染病的药物的制备方法,其特征在于经过以下工艺步骤:
(1)将卵磷脂或豆磷脂用乙醇溶解,加入0.01ml/L磷酸盐缓冲液,混合均匀,进行减压蒸馏;
(2)待乙醇挥发尽后,置组织捣细机搅拌5-15分钟,在115-125℃下蒸汽灭菌30分钟,用超声波超声搅拌两次,每次10分钟;
(3)加入利巴韦林、D-葡萄糖、乳糖、胆固醇,至完全溶解后,再加入经灭菌后的0.01ml/L磷酸盐缓冲液至总药液量为1000-2000ml,用0.22μm的膜过滤;
(4)用西林瓶灌装,分装成1000支,并半加塞,送入冷冻干燥箱内,在-30-40℃和2-50Pa下冷冻干燥,使制品水分≤3%后,压塞,轧盖,制成脂质体冻干针剂,成品检验合格,包装入库。
3、根据权利要求2所述的防治病毒引起非典型性肺炎等传染病的药物的制备方法,其特征在于:将步骤(4)制得的脂质体冻干针剂按每支溶于含氮酮2-10%,含无水乙醇10-20%,总体积20ml的无菌注射用水中,制成喷雾剂。
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Application Number | Priority Date | Filing Date | Title |
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PCT/US2000/015515 WO2001093683A1 (en) | 2000-06-07 | 2000-06-07 | Treating smooth muscle hyperactivity with (r)-oxybutynin and (r)- desethyloxybutynin |
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CN1451388A true CN1451388A (zh) | 2003-10-29 |
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Application Number | Title | Priority Date | Filing Date |
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CNA2007101418683A Pending CN101108176A (zh) | 2000-06-07 | 2000-06-07 | 用(r)-奥昔布宁和(r)-去乙基奥昔布宁治疗平滑肌机能亢进 |
CN00819623A Pending CN1454054A (zh) | 2000-06-07 | 2000-06-07 | 用(r)-奥昔布宁和(r)-去乙基奥昔布宁治疗平滑肌机能亢进 |
CN03131438A Pending CN1451388A (zh) | 2000-06-07 | 2003-05-16 | 防治病毒引起非典型性肺炎等传染病的药物 |
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CNA2007101418683A Pending CN101108176A (zh) | 2000-06-07 | 2000-06-07 | 用(r)-奥昔布宁和(r)-去乙基奥昔布宁治疗平滑肌机能亢进 |
CN00819623A Pending CN1454054A (zh) | 2000-06-07 | 2000-06-07 | 用(r)-奥昔布宁和(r)-去乙基奥昔布宁治疗平滑肌机能亢进 |
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EP (1) | EP1286591B1 (zh) |
JP (1) | JP5684964B2 (zh) |
CN (3) | CN101108176A (zh) |
AT (1) | ATE483459T1 (zh) |
AU (2) | AU2000255966B2 (zh) |
CA (1) | CA2378754A1 (zh) |
DE (1) | DE60045082D1 (zh) |
ES (1) | ES2350330T3 (zh) |
WO (1) | WO2001093683A1 (zh) |
Cited By (4)
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CN101043904B (zh) * | 2004-08-24 | 2012-04-18 | N·V·努特里奇亚 | 含有不可消化寡糖的营养组合物 |
CN103169660A (zh) * | 2013-04-15 | 2013-06-26 | 石正国 | 一种制备高包封率的利巴韦林脂质体口服乳 |
US9370528B2 (en) | 2011-03-02 | 2016-06-21 | Volant Holdings Gmbh | Compositions, methods of treatment and diagnostics for treatment of hepatic steatosis alone or in combination with a hepatitis C virus infection |
WO2022003200A1 (en) * | 2020-07-03 | 2022-01-06 | pHOxgen Limited | Reduction of viral infections |
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EP1455776A4 (en) * | 2001-12-21 | 2006-05-17 | Bridge Pharma Inc | NON-ARYTHMOGENIC METABOLITE OF OXYBUTYNINE |
EP1424079A1 (en) * | 2002-11-27 | 2004-06-02 | Boehringer Ingelheim International GmbH | Combination of a beta-3-receptor agonist and of a reuptake inhibitor of serotonin and/or norepinephrine |
US8920392B2 (en) | 2009-05-05 | 2014-12-30 | Watson Laboratories, Inc. | Method for treating overactive bladders and a device for storage and administration of topical oxybutynin compositions |
CA2836904C (en) | 2011-06-03 | 2019-09-24 | Signpath Pharma Inc. | Liposomal mitigation of drug-induced long qt syndrome and potassium delayed-rectifier current |
US10449193B2 (en) | 2011-06-03 | 2019-10-22 | Signpath Pharma Inc. | Protective effect of DMPC, DMPG, DMPC/DMPG, lysoPG and lysoPC against drugs that cause channelopathies |
US10238602B2 (en) | 2011-06-03 | 2019-03-26 | Signpath Pharma, Inc. | Protective effect of DMPC, DMPG, DMPC/DMPG, LysoPG and LysoPC against drugs that cause channelopathies |
US10349884B2 (en) | 2011-06-03 | 2019-07-16 | Sighpath Pharma Inc. | Liposomal mitigation of drug-induced inhibition of the cardiac ikr channel |
US10117881B2 (en) | 2011-06-03 | 2018-11-06 | Signpath Pharma, Inc. | Protective effect of DMPC, DMPG, DMPC/DMPG, LYSOPG and LYSOPC against drugs that cause channelopathies |
US12004868B2 (en) | 2011-06-03 | 2024-06-11 | Signpath Pharma Inc. | Liposomal mitigation of drug-induced inhibition of the cardiac IKr channel |
US20160151321A1 (en) | 2012-11-13 | 2016-06-02 | Dinesh C. Patel | Methods for the treatment of sialorrhea |
US20140135392A1 (en) * | 2012-11-13 | 2014-05-15 | NeuRx Pharmaceuticals LLC | Methods for the treatment of sialorrhea |
CA2933204C (en) * | 2013-12-18 | 2020-04-28 | Signpath Pharma, Inc. | Liposomal mitigation of drug-induced inhibition of the cardiac ikr channel |
AU2015269699B2 (en) | 2014-06-03 | 2020-08-13 | Avanti Polar Lipids, Inc. | Protective effect of DMPC, DMPG, DMPC/DMPG, EGPG, LysoPG and LysoPC against drugs that cause channelopathies |
US11806401B2 (en) | 2016-04-27 | 2023-11-07 | Signpath Pharma, Inc. | Prevention of drug-induced atrio-ventricular block |
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IT1231237B (it) * | 1987-09-21 | 1991-11-26 | Angeli Inst Spa | Derivati eterociclici |
US5677346A (en) * | 1995-01-31 | 1997-10-14 | Sepracor, Inc. | Treating urinary incontinence using (S)-desethyloxybutynin |
US5973182A (en) * | 1998-10-22 | 1999-10-26 | Sepracor Inc. | Carbonate Intermediates useful in the preparation of optically active cyclohexylphenylglycolate esters |
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- 2000-06-07 CN CNA2007101418683A patent/CN101108176A/zh active Pending
- 2000-06-07 ES ES00941235T patent/ES2350330T3/es not_active Expired - Lifetime
- 2000-06-07 AU AU2000255966A patent/AU2000255966B2/en not_active Expired
- 2000-06-07 JP JP2002501260A patent/JP5684964B2/ja not_active Expired - Fee Related
- 2000-06-07 WO PCT/US2000/015515 patent/WO2001093683A1/en active IP Right Grant
- 2000-06-07 EP EP00941235A patent/EP1286591B1/en not_active Expired - Lifetime
- 2000-06-07 CA CA002378754A patent/CA2378754A1/en not_active Abandoned
- 2000-06-07 AU AU5596600A patent/AU5596600A/xx active Pending
- 2000-06-07 AT AT00941235T patent/ATE483459T1/de not_active IP Right Cessation
- 2000-06-07 DE DE60045082T patent/DE60045082D1/de not_active Expired - Lifetime
- 2000-06-07 CN CN00819623A patent/CN1454054A/zh active Pending
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2003
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Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
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CN101043904B (zh) * | 2004-08-24 | 2012-04-18 | N·V·努特里奇亚 | 含有不可消化寡糖的营养组合物 |
US9730951B2 (en) | 2010-03-03 | 2017-08-15 | Volant Holdings Gmbh | Compositions, methods of treatment and diagnostics for treatment of hepatic steatosis alone or in combination with a Hepatitis C virus infection |
US10245277B2 (en) | 2010-03-03 | 2019-04-02 | Volant Holdings Gmbh | Compositions, methods of treatment and diagnostics for treatment of hepatic steatosis alone or in combination with a hepatitis C virus infection |
US9370528B2 (en) | 2011-03-02 | 2016-06-21 | Volant Holdings Gmbh | Compositions, methods of treatment and diagnostics for treatment of hepatic steatosis alone or in combination with a hepatitis C virus infection |
CN103169660A (zh) * | 2013-04-15 | 2013-06-26 | 石正国 | 一种制备高包封率的利巴韦林脂质体口服乳 |
CN103169660B (zh) * | 2013-04-15 | 2015-04-08 | 石正国 | 一种制备高包封率的利巴韦林脂质体口服乳 |
WO2022003200A1 (en) * | 2020-07-03 | 2022-01-06 | pHOxgen Limited | Reduction of viral infections |
Also Published As
Publication number | Publication date |
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EP1286591A1 (en) | 2003-03-05 |
CA2378754A1 (en) | 2001-12-13 |
CN101108176A (zh) | 2008-01-23 |
AU2000255966B2 (en) | 2005-03-24 |
WO2001093683A1 (en) | 2001-12-13 |
CN1454054A (zh) | 2003-11-05 |
AU5596600A (en) | 2001-12-17 |
AU2000255966A1 (en) | 2002-03-07 |
EP1286591B1 (en) | 2010-10-06 |
JP2003535110A (ja) | 2003-11-25 |
JP5684964B2 (ja) | 2015-03-18 |
ES2350330T3 (es) | 2011-01-21 |
EP1286591A4 (en) | 2007-04-04 |
ATE483459T1 (de) | 2010-10-15 |
DE60045082D1 (de) | 2010-11-18 |
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