CN104382908A - 注射用头孢哌酮钠他唑巴坦钠组合物 - Google Patents

注射用头孢哌酮钠他唑巴坦钠组合物 Download PDF

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CN104382908A
CN104382908A CN201410481486.5A CN201410481486A CN104382908A CN 104382908 A CN104382908 A CN 104382908A CN 201410481486 A CN201410481486 A CN 201410481486A CN 104382908 A CN104382908 A CN 104382908A
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sodium
tazobactam
cefoperazone
cefoperazone sodium
lidocaine hydrochloride
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包莹
刘萍
陈继源
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Sichuan Pharmaceutical Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions

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  • Health & Medical Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明公开了一种注射用头孢哌酮钠他唑巴坦钠组合物，该组合物包括头孢哌酮钠、他唑巴坦钠和盐酸利多卡因，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，盐酸利多卡因为头孢哌酮钠重量的0.002-0.006。本发明简单、成本低，制备出的产品稳定性好，药效好，能够在节约用药成本的同时在注射过程中能够减轻病员的痛苦。

Description

注射用头孢哌酮钠他唑巴坦钠组合物
 
技术领域
本发明涉及医药生物领域，具体地，涉及注射用头孢哌酮钠他唑巴坦钠组合物。
背景技术
头孢哌酮钠的中文别名 7-(((4-乙基-2,3-二氧代-1-哌嗪基)甲酰氨基)(4-羟基苯基)乙酰氨基)-3-((1-甲基-1H-四唑-5-基)硫甲基)-8-氧代-5-硫-1-氮杂双环(4.2.0)辛-2-烯-2-甲酸钠盐，对阴性杆菌产生的广谱β-内酰胺酶有一定的稳定性，但较某些第三代头孢菌素差，抗阴性杆菌的作用优于第一、二代头孢菌素，但对绿脓杆菌有较好的抗菌活性。抗阳性菌的作用不如第一、二代头孢菌素，但对肺炎球菌、化脓性链球菌均有较好的作用。对厌氧菌的抗菌作用较弱。肠球菌及相当比例的肠杆菌科致病菌对该品耐药，支原体、衣原体、军团菌对头孢哌酮均耐药。抗菌性能与头孢噻肟相似。对革兰阳性菌的作用较弱，仅溶血性链球菌和肺炎链球菌较为敏感。对数的革兰阴性菌，该品的作用略次于头孢噻肟，对绿脓杆菌的作用较强。用于敏感产酶菌引起的各种感染的治疗，如呼吸系统、生殖泌尿系统、胆道、胃肠道、胸腹腔、皮肤软组织感染的治疗，及对流感杆菌、脑膜炎球菌引起的脑内感染也有较好的疗效。治疗绿脓杆菌引起的感染，头孢哌酮是一较好的第三代头孢菌素。
他唑巴坦钠与青霉素类和头孢菌素类抗生素具有明显的协同作用，因此临床上常常将他唑巴坦钠和青霉素类、头孢菌素类抗生素联合制剂以增强单一药剂的药效。但现有的注射用头孢哌酮钠他唑巴坦钠组合物复杂，且稳定性不好。
发明内容
本发明所要解决的技术问题是提供注射用头孢哌酮钠他唑巴坦钠组合物，该组合物简单、成本低，制备出的产品稳定性好，药效好，且在节约用药的同时减低病人的疼痛。
本发明解决上述问题所采用的技术方案是：
注射用头孢哌酮钠他唑巴坦钠组合物，包括头孢哌酮钠、他唑巴坦钠和盐酸利多卡因，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，盐酸利多卡因为头孢哌酮钠重量的0.002-0.006。
所述盐酸利多卡因为头孢哌酮钠重量的0.003-0.005。
所述头孢哌酮钠的休止角为24.0-30.0°。
所述他唑巴坦钠的休止角为24.0-30.0°。
制备注射用头孢哌酮钠他唑巴坦钠组合物，将头孢哌酮钠先投入混料机中分散均匀，再投入他唑巴坦钠和头孢哌酮钠混合均匀，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，再加入头孢哌酮钠重量的0.002-0.006的盐酸利多卡因，使三者混合均匀，再加入注射用水溶解后冷冻干燥，制得注射用头孢哌酮钠他唑巴坦钠。
盐酸利多卡因为酰胺类局麻药。血液吸收后或静脉给药，对中枢神经系统有明显的兴奋和抑制双相作用，且可无先驱的兴奋，血药浓度较低时，出现镇痛和嗜睡、痛阈提高；随着剂量加大，作用或毒性增强，亚中毒血药浓度时有抗惊厥作用。因此盐酸利多卡的用量不宜过多，研究发现盐酸利多卡的用量为他唑巴坦钠用量的0.002-0.006之间能够减轻疼痛且不影响药效，还能节约用药成本。
冷冻干燥之前还包括用pH调节剂调节他唑巴坦钠、头孢哌酮钠和盐酸利多卡因的注射用水溶液pH为6.0-7.0。pH调节剂为氢氧化钾或者氢氧化钠。调pH值之后还用微孔滤膜进行过滤。
综上，本发明的有益效果是：
本发明制备方法简单、成本低，制备出的产品稳定性好，药效好，能够在节约用药成本的同时在注射过程中能够减轻病员的痛苦。
具体实施方式
下面结合实施例，对本发明作进一步地的详细说明，但本发明的实施方式不限于此。
实施例1：
注射用头孢哌酮钠他唑巴坦钠组合物，包括头孢哌酮钠、他唑巴坦钠和盐酸利多卡因，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，盐酸利多卡因为头孢哌酮钠重量的0.002。
所述头孢哌酮钠的休止角为24.0-30.0°。
所述他唑巴坦钠的休止角为24.0-30.0°。
制备注射用头孢哌酮钠他唑巴坦钠组合物，将头孢哌酮钠先投入混料机中分散均匀，再投入他唑巴坦钠和头孢哌酮钠混合均匀，再加入盐酸利多卡因，使三者混合均匀，再加入注射用水溶解后冷冻干燥，制得注射用头孢哌酮钠他唑巴坦钠。
盐酸利多卡因为酰胺类局麻药。血液吸收后或静脉给药，对中枢神经系统有明显的兴奋和抑制双相作用，且可无先驱的兴奋，血药浓度较低时，出现镇痛和嗜睡、痛阈提高；随着剂量加大，作用或毒性增强，亚中毒血药浓度时有抗惊厥作用。因此盐酸利多卡的用量不宜过多，研究发现盐酸利多卡的用量为他唑巴坦钠用量的0.002-0.006之间能够减轻疼痛且不影响药效，还能节约用药成本。
冷冻干燥之前还包括用pH调节剂调节他唑巴坦钠、头孢哌酮钠和盐酸利多卡因的注射用水溶液pH为6.0-7.0。pH调节剂为氢氧化钾或者氢氧化钠。调pH值之后还用微孔滤膜进行过滤。pH调节剂为氢氧化钾或者氢氧化钠。调pH值之后还用微孔滤膜进行过滤。
实施例2
注射用头孢哌酮钠他唑巴坦钠组合物，包括头孢哌酮钠、他唑巴坦钠和盐酸利多卡因，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，盐酸利多卡因为头孢哌酮钠重量的0.003。
所述头孢哌酮钠的休止角为24.0-30.0°。
所述他唑巴坦钠的休止角为24.0-30.0°。制备方法如实施例1。
实施例3
注射用头孢哌酮钠他唑巴坦钠组合物，包括头孢哌酮钠、他唑巴坦钠和盐酸利多卡因，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，盐酸利多卡因为头孢哌酮钠重量的0.005。
所述头孢哌酮钠的休止角为24.0-30.0°。
所述他唑巴坦钠的休止角为24.0-30.0°。制备方法如实施例1。
实施例4
注射用头孢哌酮钠他唑巴坦钠组合物，包括头孢哌酮钠、他唑巴坦钠和盐酸利多卡因，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，盐酸利多卡因为头孢哌酮钠重量的0.006。
所述头孢哌酮钠的休止角为24.0-30.0°。
所述他唑巴坦钠的休止角为24.0-30.0°。制备方法如实施例1。

Claims (4)

1.注射用头孢哌酮钠他唑巴坦钠组合物，其特征在于，包括头孢哌酮钠、他唑巴坦钠和盐酸利多卡因，其中头孢哌酮钠和他唑巴坦钠的质量比为4：1，盐酸利多卡因为头孢哌酮钠重量的0.002-0.006。
2.根据权利要求1所述的注射用头孢哌酮钠他唑巴坦钠组合物，其特征在于，所述盐酸利多卡因为头孢哌酮钠重量的0.003-0.005。
3.根据权利要求1所述的注射用头孢哌酮钠他唑巴坦钠，其特征在于，所述头孢哌酮钠的休止角为24.0-30.0°。
4.根据权利要求1所述的注射用头孢哌酮钠他唑巴坦钠，其特征在于，所述他唑巴坦钠的休止角为24.0-30.0°。
CN201410481486.5A 2014-09-21 2014-09-21 注射用头孢哌酮钠他唑巴坦钠组合物 Pending CN104382908A (zh)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102552275A (zh) * 2012-01-17 2012-07-11 山东罗欣药业股份有限公司 头孢哌酮钠和他唑巴坦钠组合物注射用粉针剂

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102552275A (zh) * 2012-01-17 2012-07-11 山东罗欣药业股份有限公司 头孢哌酮钠和他唑巴坦钠组合物注射用粉针剂

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