CN111511368A - 含有哌拉西林的组合物、其药物制剂及其应用 - Google Patents
含有哌拉西林的组合物、其药物制剂及其应用 Download PDFInfo
- Publication number
- CN111511368A CN111511368A CN201780097174.6A CN201780097174A CN111511368A CN 111511368 A CN111511368 A CN 111511368A CN 201780097174 A CN201780097174 A CN 201780097174A CN 111511368 A CN111511368 A CN 111511368A
- Authority
- CN
- China
- Prior art keywords
- sulbactam
- piperacillin
- ampicillin
- composition
- acinetobacter baumannii
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 45
- 229960002292 piperacillin Drugs 0.000 title claims abstract description 39
- 239000000825 pharmaceutical preparation Substances 0.000 title claims abstract description 14
- IVBHGBMCVLDMKU-GXNBUGAJSA-N piperacillin Chemical compound O=C1C(=O)N(CC)CCN1C(=O)N[C@H](C=1C=CC=CC=1)C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 IVBHGBMCVLDMKU-GXNBUGAJSA-N 0.000 title claims abstract description 7
- FKENQMMABCRJMK-RITPCOANSA-N sulbactam Chemical compound O=S1(=O)C(C)(C)[C@H](C(O)=O)N2C(=O)C[C@H]21 FKENQMMABCRJMK-RITPCOANSA-N 0.000 claims abstract description 32
- 229960005256 sulbactam Drugs 0.000 claims abstract description 29
- 229940079593 drug Drugs 0.000 claims abstract description 17
- 239000003814 drug Substances 0.000 claims abstract description 17
- 229960004682 cefoperazone Drugs 0.000 claims abstract description 12
- GCFBRXLSHGKWDP-XCGNWRKASA-N cefoperazone Chemical compound O=C1C(=O)N(CC)CCN1C(=O)N[C@H](C=1C=CC(O)=CC=1)C(=O)N[C@@H]1C(=O)N2C(C(O)=O)=C(CSC=3N(N=NN=3)C)CS[C@@H]21 GCFBRXLSHGKWDP-XCGNWRKASA-N 0.000 claims abstract description 12
- KMEGBUCIGMEPME-LQYKFRDPSA-N (2s,5r,6r)-6-[[(2r)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;(1r,4s)-3,3-dimethyl-2,2,6-trioxo-2$l^{6}-thiabicyclo[3.2.0]heptane-4-carboxylic acid Chemical compound O=S1(=O)C(C)(C)[C@H](C(O)=O)C2C(=O)C[C@H]21.C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 KMEGBUCIGMEPME-LQYKFRDPSA-N 0.000 claims abstract description 9
- AVKUERGKIZMTKX-NJBDSQKTSA-N ampicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 AVKUERGKIZMTKX-NJBDSQKTSA-N 0.000 claims description 21
- 229960000723 ampicillin Drugs 0.000 claims description 16
- 238000002347 injection Methods 0.000 claims description 16
- 239000007924 injection Substances 0.000 claims description 16
- 241000894006 Bacteria Species 0.000 claims description 14
- 206010059866 Drug resistance Diseases 0.000 claims description 14
- 239000000843 powder Substances 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 7
- 239000000243 solution Substances 0.000 claims description 7
- 208000035143 Bacterial infection Diseases 0.000 claims description 3
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 239000008176 lyophilized powder Substances 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 241000588626 Acinetobacter baumannii Species 0.000 abstract description 30
- 208000015181 infectious disease Diseases 0.000 abstract description 12
- YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 abstract description 4
- 239000003242 anti bacterial agent Substances 0.000 abstract description 3
- 229940088710 antibiotic agent Drugs 0.000 abstract description 3
- WCMIIGXFCMNQDS-IDYPWDAWSA-M piperacillin sodium Chemical compound [Na+].O=C1C(=O)N(CC)CCN1C(=O)N[C@H](C=1C=CC=CC=1)C(=O)N[C@@H]1C(=O)N2[C@@H](C([O-])=O)C(C)(C)S[C@@H]21 WCMIIGXFCMNQDS-IDYPWDAWSA-M 0.000 description 37
- 241001465754 Metazoa Species 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 9
- 230000000694 effects Effects 0.000 description 9
- 238000002360 preparation method Methods 0.000 description 7
- 241000699666 Mus <mouse, genus> Species 0.000 description 6
- 239000002253 acid Substances 0.000 description 5
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 238000004806 packaging method and process Methods 0.000 description 4
- 108010040201 Polymyxins Proteins 0.000 description 3
- NKZMPZCWBSWAOX-IBTYICNHSA-M Sulbactam sodium Chemical compound [Na+].O=S1(=O)C(C)(C)[C@H](C([O-])=O)N2C(=O)C[C@H]21 NKZMPZCWBSWAOX-IBTYICNHSA-M 0.000 description 3
- 210000000683 abdominal cavity Anatomy 0.000 description 3
- KLOHDWPABZXLGI-YWUHCJSESA-M ampicillin sodium Chemical compound [Na+].C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C([O-])=O)(C)C)=CC=CC=C1 KLOHDWPABZXLGI-YWUHCJSESA-M 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 229960002260 meropenem Drugs 0.000 description 3
- CTUAQTBUVLKNDJ-OBZXMJSBSA-N meropenem trihydrate Chemical compound O.O.O.C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)S[C@@H]1CN[C@H](C(=O)N(C)C)C1 CTUAQTBUVLKNDJ-OBZXMJSBSA-N 0.000 description 3
- 229960005264 piperacillin sodium Drugs 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 229960000614 sulbactam sodium Drugs 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 2
- 229960001931 ampicillin sodium Drugs 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 230000001580 bacterial effect Effects 0.000 description 2
- 244000052616 bacterial pathogen Species 0.000 description 2
- 210000000170 cell membrane Anatomy 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 230000000857 drug effect Effects 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- RBKMMJSQKNKNEV-RITPCOANSA-N penicillanic acid Chemical compound OC(=O)[C@H]1C(C)(C)S[C@@H]2CC(=O)N21 RBKMMJSQKNKNEV-RITPCOANSA-N 0.000 description 2
- 230000035699 permeability Effects 0.000 description 2
- -1 polymorphs Chemical class 0.000 description 2
- 230000001681 protective effect Effects 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 230000002195 synergetic effect Effects 0.000 description 2
- 208000035473 Communicable disease Diseases 0.000 description 1
- 208000028399 Critical Illness Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 241000588747 Klebsiella pneumoniae Species 0.000 description 1
- 206010048723 Multiple-drug resistance Diseases 0.000 description 1
- 206010029155 Nephropathy toxic Diseases 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 229940124350 antibacterial drug Drugs 0.000 description 1
- 230000003385 bacteriostatic effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 229940121657 clinical drug Drugs 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000007694 nephrotoxicity Effects 0.000 description 1
- 231100000417 nephrotoxicity Toxicity 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 206010033675 panniculitis Diseases 0.000 description 1
- 150000002961 penems Chemical class 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 230000008261 resistance mechanism Effects 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000008227 sterile water for injection Substances 0.000 description 1
- 210000004304 subcutaneous tissue Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/495—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
-
- 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
-
- 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
-
- 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
- A61K47/02—Inorganic compounds
-
- 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
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明提供了一种含有哌拉西林的组合物,该组合物中含有哌拉西林,还含有一定比例的氨苄西林和舒巴坦。本发明还提供了其药物制剂和应用。本发明的组合物和药物制剂可显著抑制耐药性鲍曼不动杆菌,特别是对碳青霉烯类抗生素或对头孢哌酮舒巴坦耐药的鲍曼不动杆菌感染能起到很好的治疗作用。
Description
PCT国内申请,说明书已公开。
Claims (10)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/CN2017/118177 WO2019126910A1 (zh) | 2017-12-25 | 2017-12-25 | 含有哌拉西林的组合物、其药物制剂及其应用 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN111511368A true CN111511368A (zh) | 2020-08-07 |
CN111511368B CN111511368B (zh) | 2023-05-09 |
Family
ID=67064369
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201780097174.6A Active CN111511368B (zh) | 2017-12-25 | 2017-12-25 | 治疗耐药性鲍曼不动杆菌感染的含哌拉西林钠和舒巴坦钠的组合物 |
Country Status (4)
Country | Link |
---|---|
US (1) | US11534438B2 (zh) |
EP (1) | EP3733176B1 (zh) |
CN (1) | CN111511368B (zh) |
WO (1) | WO2019126910A1 (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107875154A (zh) * | 2017-12-25 | 2018-04-06 | 北京新天宇科技开发有限公司 | 含有哌拉西林的组合物、其药物制剂及其应用 |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1836659A (zh) * | 2005-03-21 | 2006-09-27 | 山东瑞阳制药有限公司 | 阿洛西林/舒巴坦抗菌组合药物 |
CN1850046A (zh) * | 2006-06-01 | 2006-10-25 | 济南帅华医药科技有限公司 | 一种含β-内酰胺酶抑制剂的缓释制剂及其应用 |
US20090311234A1 (en) * | 2006-11-28 | 2009-12-17 | Ipsat Therapies Oy | Use of beta-lactamase |
NZ553119A (en) * | 2004-08-13 | 2010-11-26 | Schering Plough Ltd | Pharmaceutical formulation comprising an antibiotic, a triazole and a corticosteroid |
CN102475703A (zh) * | 2010-11-26 | 2012-05-30 | 丽珠医药集团股份有限公司 | 一种抗鲍曼不动杆菌的药物组合物及其用途 |
-
2017
- 2017-12-25 CN CN201780097174.6A patent/CN111511368B/zh active Active
- 2017-12-25 EP EP17936693.5A patent/EP3733176B1/en active Active
- 2017-12-25 WO PCT/CN2017/118177 patent/WO2019126910A1/zh unknown
- 2017-12-25 US US16/771,429 patent/US11534438B2/en active Active
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ553119A (en) * | 2004-08-13 | 2010-11-26 | Schering Plough Ltd | Pharmaceutical formulation comprising an antibiotic, a triazole and a corticosteroid |
CN1836659A (zh) * | 2005-03-21 | 2006-09-27 | 山东瑞阳制药有限公司 | 阿洛西林/舒巴坦抗菌组合药物 |
CN1850046A (zh) * | 2006-06-01 | 2006-10-25 | 济南帅华医药科技有限公司 | 一种含β-内酰胺酶抑制剂的缓释制剂及其应用 |
US20090311234A1 (en) * | 2006-11-28 | 2009-12-17 | Ipsat Therapies Oy | Use of beta-lactamase |
CN102475703A (zh) * | 2010-11-26 | 2012-05-30 | 丽珠医药集团股份有限公司 | 一种抗鲍曼不动杆菌的药物组合物及其用途 |
Non-Patent Citations (1)
Title |
---|
严汝庆: "鲍曼不动杆菌耐药性分析", 《贵阳中医学院学报》 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107875154A (zh) * | 2017-12-25 | 2018-04-06 | 北京新天宇科技开发有限公司 | 含有哌拉西林的组合物、其药物制剂及其应用 |
CN107875154B (zh) * | 2017-12-25 | 2021-05-14 | 湘北威尔曼制药股份有限公司 | 含有哌拉西林的组合物、其药物制剂及其应用 |
Also Published As
Publication number | Publication date |
---|---|
WO2019126910A1 (zh) | 2019-07-04 |
EP3733176B1 (en) | 2022-05-11 |
US11534438B2 (en) | 2022-12-27 |
CN111511368B (zh) | 2023-05-09 |
US20210069183A1 (en) | 2021-03-11 |
EP3733176A4 (en) | 2021-08-11 |
EP3733176A1 (en) | 2020-11-04 |
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