CN105476960A - 一种恩诺沙星乳剂及其制备方法 - Google Patents
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- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims abstract description 19
- 239000000787 lecithin Substances 0.000 claims abstract description 18
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- PORPENFLTBBHSG-MGBGTMOVSA-N 1,2-dihexadecanoyl-sn-glycerol-3-phosphate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=O)OC(=O)CCCCCCCCCCCCCCC PORPENFLTBBHSG-MGBGTMOVSA-N 0.000 claims abstract description 4
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- 229940083466 soybean lecithin Drugs 0.000 claims abstract description 4
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- ZWZWYGMENQVNFU-UHFFFAOYSA-N Glycerophosphorylserin Natural products OC(=O)C(N)COP(O)(=O)OCC(O)CO ZWZWYGMENQVNFU-UHFFFAOYSA-N 0.000 claims abstract description 3
- 102000002322 Egg Proteins Human genes 0.000 claims description 6
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- 241000287828 Gallus gallus Species 0.000 claims description 6
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- 210000004681 ovum Anatomy 0.000 claims description 6
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- 239000008346 aqueous phase Substances 0.000 claims description 4
- 150000002148 esters Chemical class 0.000 claims description 4
- 229940075529 glyceryl stearate Drugs 0.000 claims description 4
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- 229920001214 Polysorbate 60 Polymers 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims description 2
- 229960001231 choline Drugs 0.000 claims description 2
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 claims description 2
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- 239000003814 drug Substances 0.000 abstract description 3
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- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 4
- 241000894006 Bacteria Species 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 229940124350 antibacterial drug Drugs 0.000 description 2
- MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 229940124307 fluoroquinolone Drugs 0.000 description 2
- 108020000946 Bacterial DNA Proteins 0.000 description 1
- 108020004414 DNA Proteins 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 241000192125 Firmicutes Species 0.000 description 1
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- SUMISBZQLDQCJI-UHFFFAOYSA-N N1=C(C=CC2=CC=CC=C12)C(=O)O.[F] Chemical compound N1=C(C=CC2=CC=CC=C12)C(=O)O.[F] SUMISBZQLDQCJI-UHFFFAOYSA-N 0.000 description 1
- 206010034133 Pathogen resistance Diseases 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
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- 239000008280 blood Substances 0.000 description 1
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- 229960003405 ciprofloxacin Drugs 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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Abstract
本发明公开了一种恩诺沙星乳剂及其制备方法,该恩诺沙星乳剂由恩诺沙星、乳化剂、卵磷脂、水组成,其中卵磷脂为大豆卵磷脂、蛋黄卵磷脂、二硬脂酰磷脂酰胆碱、棕榈酰磷脂酰?胆碱、磷脂酰丝氨酸、磷脂酸、氢化卵磷脂中的一种或其组合物。该恩诺沙星乳剂稳定性高,药物分散均匀,可任意比例与水混溶。
Description
技术领域
本发明属于恩诺沙星制剂制备领域,具体涉及一种恩诺沙星乳剂及其制备方法。
背景资料
恩诺沙星(Enrofloxacin),又名恩氟奎林羧酸,属于氟奎诺酮类(Fluoroquinolones)之化学合成抑菌剂,为微黄色或淡黄色结晶性粉末,味苦,不溶于水。
本品为合成的第三代喹诺酮类抗菌药物,又名乙基环丙沙星,1996年10月4日获FDA批准,为畜禽和水产专用喹诺酮类抗菌药物,能与细菌DNA回旋酶亚基A结合,从而抑制了酶的切割与连接功能,阻止了细菌DNA的复制,而呈现抗菌作用。具有广谱抗菌活性、具有很强的渗透性,本品对革兰氏阴性菌有很强的杀灭作用,对革兰氏阳性菌也有良好的抗菌作用,口服吸收好,血药浓度高且稳定,能广泛分布于组织中,其代谢产物为环丙沙星,仍有强大抗菌作用。几乎对水生动物所有病原菌的抗菌活性均较强。对由耐药性致病菌引起的严重感染有效,与其它抗菌素无交叉耐药性。
恩诺沙星难溶于水,影响其使用后的吸收和方便性,给其应用带来限制。
发明内容
为克服现有技术不足,本发明提供了一种恩诺沙星乳剂。
为实现上述目的,本发明的技术方案是这样实现的:
一种恩诺沙星乳剂由恩诺沙星、乳化剂、卵磷脂、水组成。
进一步,所述卵磷脂包括大豆卵磷脂、蛋黄卵磷脂、二硬脂酰磷脂酰胆碱、棕榈酰磷脂酰胆碱、磷脂酰丝氨酸、磷脂酸、氢化卵磷脂中的一种或其组合物。
进一步,所述乳化剂为吐温-60、span60、甘油硬脂酸酯柠檬酯中的一种或其组合物。
进一步,所述组成成分的重量百分比为恩诺沙星5~20%、乳化剂1~10%、卵磷脂2~20%、余量为水。
本发明还提供了该恩诺沙星乳剂的制备方法,具体包括以下步骤:a.准确称量卵磷脂,将卵磷脂加热溶解,得液态油相;b.准确称量恩诺沙星,加入到步骤a制备的液态油相中,加热完全溶解;c.准确称量乳化剂和水,将乳化剂和水混合后加热溶解,得水相;d.将步骤b制备的溶液加入步骤c制备的水相中,混合均匀,加入设定到一定温度的、压力为60Mpa的高用均质机均质10~30min,冷却至室温即可。
进一步,高用均质机设定的温度为60℃~80℃。
有益效果
本发明提供了一种恩诺沙星乳剂及其制备方法,解决了恩诺沙星难溶于水,不能通过水溶后使用的缺陷,产品稳定性高,药物分散均匀,可任意比例与水混溶,且工艺简单,易于工业化生产。
具体实施方式
实施例组方1:
按重量百分比计,恩诺沙星5%、吐温601%、大豆卵磷脂2%、余量为水。
实施例组方2:
按重量百分比计,恩诺沙星20%、span6010%、磷脂酸20%、余量为水。
实施例组方3:
按重量百分比计,恩诺沙星7.5%、甘油硬脂酸酯柠檬酯5%、二硬脂酰磷脂酰胆碱和蛋黄卵磷脂的混合物10%、余量为水。其中二硬脂酰磷脂酰胆碱:蛋黄卵磷脂=5:5。
实施例组方4:
按重量百分比计,恩诺沙星10%、甘油硬脂酸酯柠檬酯5%、二硬脂酰磷脂酰胆碱和蛋黄卵磷脂的混合物10%、余量为水。其中二硬脂酰磷脂酰胆碱:蛋黄卵磷脂=5:5。
试验例:观察本发明实施例1~4的稳定性
分别取实施例1~4所制备的恩诺沙星乳剂5ml,用去离子水稀释5倍、10倍、50倍、100倍,然后在室温条件相爱将本发明制备的实施例1~4分别在离心机上4000rpm转速相爱离心30min,观察稀释液有无肉眼可见的沉淀物,结果如下表1。
表1本发明实施例1~4水稀释液离心结果
稀释倍数 | 5倍 | 10倍 | 50倍 | 100倍 |
实施例1 | 无 | 无 | 无 | 无 |
实施例2 | 无 | 无 | 无 | 无 |
实施例3 | 无 | 无 | 无 | 无 |
实施例4 | 无 | 无 | 无 | 无 |
由表1结果可知,本发明所制备的实施例1~4性质稳定,乳剂分散均匀,与水任意比例混合稀释。
以上所述仅为本发明的较佳实施例而已,并不用以限制本发明,凡在本发明的精神和原则之内,所作的任何修改、等同替换、改进等,均应包含在本发明的保护范围之内。
Claims (6)
1.一种恩诺沙星乳剂,其特征在于,由恩诺沙星、乳化剂、卵磷脂、水组成。
2.根据权利要求1所述的一种恩诺沙星乳剂,其特征在于,所述卵磷脂包括大豆卵磷脂、蛋黄卵磷脂、二硬脂酰磷脂酰胆碱、棕榈酰磷脂酰胆碱、磷脂酰丝氨酸、磷脂酸、氢化卵磷脂中的一种或其组合物。
3.根据权利要求1所述的一种恩诺沙星乳剂,其特征在于,所述乳化剂为吐温-60、span60、甘油硬脂酸酯柠檬酯中的一种或其组合物。
4.根据权利要求1~3任一项所述的一种恩诺沙星乳剂,其特征在于,所述组成成分的重量百分比为恩诺沙星5~20%、乳化剂1~10%、卵磷脂2~20%、余量为水。
5.一种制备如权利要求1所述的恩诺沙星乳剂及其制备方法的方法,其特征在于,包括以下步骤:a.准确称量卵磷脂,将卵磷脂加热溶解,得液态油相;b.准确称量恩诺沙星,加入到步骤a制备的液态油相中,加热完全溶解;c.准确称量乳化剂和水,将乳化剂和水混合后加热溶解,得水相;d.将步骤b制备的溶液加入步骤c制备的水相中,混合均匀,加入设定到一定温度的、压力为60Mpa的高用均质机均质10~30min,冷却至室温即可。
6.根据权利要求5所述的方法,其特征在于,高用均质机设定的温度为60℃~80℃。
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Citations (1)
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CN101744763A (zh) * | 2010-02-09 | 2010-06-23 | 河南科技学院 | 一种恩诺沙星纳米乳液及其制备方法 |
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CN101744763A (zh) * | 2010-02-09 | 2010-06-23 | 河南科技学院 | 一种恩诺沙星纳米乳液及其制备方法 |
Non-Patent Citations (2)
Title |
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杨雪峰 等: "恩诺沙星纳米乳的制备及其质量评价", 《浙江大学学报(农业与生命科学版)》 * |
王建新 等: "固体脂质纳米粒的研究进展", 《中国药学杂志》 * |
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