KR940013512A - Aqueous composition of cephalosporin antibiotics and preparation method thereof - Google Patents

Aqueous composition of cephalosporin antibiotics and preparation method thereof Download PDF

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KR940013512A
KR940013512A KR1019920025908A KR920025908A KR940013512A KR 940013512 A KR940013512 A KR 940013512A KR 1019920025908 A KR1019920025908 A KR 1019920025908A KR 920025908 A KR920025908 A KR 920025908A KR 940013512 A KR940013512 A KR 940013512A
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carboxylate
acetamido
cepem
thiomethyl
diamino
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KR960008236B1 (en
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권오룡
김혁년
심창구
이현국
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최근선
주식회사 럭키
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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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

본 발명은 난용성 세파로스 포린계 화합물을 니코틴아미드 수용액에 용해시켜 용해도와 안정성을 향상시킨 조성물과 그 제조방법에 관한 것으로 용액상태에서 주사제등의 제형으로 다양하게 제제화될 수 있다.The present invention relates to a composition and a method for preparing the composition by dissolving a poorly soluble Sepharose porin-based compound in an aqueous nicotinamide solution, and a method for preparing the same.

Description

세파로스포린계 항생제의 수성 조성물 및 그 제조방법Aqueous composition of cephalosporin antibiotics and preparation method thereof

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (5)

다음 일반식(VII)으로 표시되는 세파로스포린 화합물 5 내지 41중량%, 니코틴아미드 10 내지 60중량%, 및 증류수 25 내지 85중량%로 구성되어 있는 수성 조성물.An aqueous composition composed of 5 to 41% by weight of the cephalosporin compound represented by the following formula (VII), 10 to 60% by weight nicotinamide, and 25 to 85% by weight of distilled water. 상기 일반식에서 R1은 -COOH를 포함하지 않는 C1-4알킬기, C3-4알케닐기 또는 C3-4알킬닐기이고, R2는 C1-4알킬기, C3-4알케닐기 또는 C3-7사이클로 알킬기를 나타내며, R3는 수소 또는 C1-4알킬기이고, Q는 N 또는 CH이다.In the general formula, R 1 is a C 1-4 alkyl group, C 3-4 alkenyl group or C 3-4 alkylyl group, which does not contain -COOH, and R 2 is a C 1-4 alkyl group, C 3-4 alkenyl group or C 3-7 cycloalkyl group, R 3 is hydrogen or C 1-4 alkyl group, Q is N or CH. 제1항에 있어서, 상기 세파로스포린 화합물이 7[(z)-2-(2-아미노티아졸-4-일)-(에톡시이미노)아세토아미도]-3-(4,6-디아미노-1-메틸피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(5-아미노-1,2,4-티아디아졸-3-일)-2-(에톡시이미노)아세트아미도]-3-(4,6-디아미노-1-메틸피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(2-프로핀-1-옥시이미노)아세트아미도]-3-(4,6-디아미노-1-메틸피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(메톡시이미노)-아세트아미도]-3-(4,6-디아미노-1-메틸피리미디늄-2-일)티오메틸-3-세핌-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(에톡시이미노)아세트아미도]-3-(4,6-디아미노-1-에틸피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(에톡시이미노)아세트아미도]-3-(1,4,6-트리아미노피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(5-아미노-1,2,4-티아디아졸-3-일)-2-(에톡시이미노)아세트아미도]-3-(1,4,6-트리아미노피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(2-프로핀-1-옥시이미노)아세트아미도]-3-(1,4,6-트리아미노피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(메톡시이미노)아세트아미도]-3-(1,4,6-트리아미노피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(5-아미노-1,2,4-티아디아졸-3-일)-2-(에톡시이미노)아세트아미도]-3-(4,6-디아미노-1-에틸피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(5-아미노-1,2,4-티아디아졸-3-일)-2-(에톡시이미노)아세트아미도]-3-(4,6-디아미노-1-프로필피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(5-아미노-1,2,4-티아디아졸-3-일)-2(-에톡시이미노)아세트아미도]-3-(1-알릴-4,6-디아미노프로필리미디늄-2-일)-3-세펨-4-카르복실레이트, 7-[(z)-2-(5-아미노-1,2,4-티아디아졸-3-일)-2-(메톡시이미노)아세트아미도]-3-(4,6-디아미노-1-메틸피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7[(z)-2-(5-아미노-1,2,4-티아디아졸-3-일)-2-(메톡시이미노)아세트아미도]-3-(4,6-디아미노-1-에틸피리미티늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(에톡시이미노)아세트아미도]-3-(4,6-디아미노-1-페닐피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(에톡시이미노)아세트아미도]-3-(1-(4-클로로페닐)-4,6-디아미노피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(에톡시이미노)아세트아미도]-3-(4,6-디아미노-1-(2,4-디메틸페닐)피리미디늄-2-일]티오메틸-3-세펨-4-카르복실레이트, 7[(z)-2-(2-아미노티아졸-4-일)-2-(2-프로핀-1-옥시이미노)아세트아미도]-3-(4,6-디아미노-1-에틸피리미디늄-2-일]티오메틸-3-세핌-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(2-프로펜-1-옥시이미노)아세트아미도]-3-(4,6-디아미노-1-메틸피리미디늄-2-일)-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(2-프로펜-1-옥시이미노)아세트아미도]-3-(4,6-디아미노-1-에틸피리미디늄-2-일)-3-세펨-4-카르복실레이트, 7-[(z)-2-(2-아미노티아졸-4-일)-2-(메톡시이미노)아세트아미도]-3-(4,6-디아미노-1-에틸피리미디늄-2-일)티오메틸-3-세펨-4-카르복실레이트로 구성된 군에서 선택된 화합물인 것을 특징으로 하는 수성 조성물.The method of claim 1, wherein the cephalosporin compound is 7 [(z) -2- (2-aminothiazol-4-yl)-(ethoxyimino) acetoamido] -3- (4,6-dia) Mino-1-methylpyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7-[(z) -2- (5-amino-1,2,4-thiadiazole- 3-yl) -2- (ethoxyimino) acetamido] -3- (4,6-diamino-1-methylpyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate , 7-[(z) -2- (2-aminothiazol-4-yl) -2- (2-propyn-1-oxyimino) acetamido] -3- (4,6-diamino- 1-methylpyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7-[(z) -2- (2-aminothiazol-4-yl) -2- (methoxydi Mino) -acetamido] -3- (4,6-diamino-1-methylpyrimidin-2-yl) thiomethyl-3-sepim-4-carboxylate, 7-[(z) -2 -(2-aminothiazol-4-yl) -2- (ethoxyimino) acetamido] -3- (4,6-diamino-1-ethylpyrimidin-2-yl) thiomethyl-3 Cefem-4-carboxylate, 7-[(z) -2- (2-aminothiazole-4 -Yl) -2- (ethoxyimino) acetamido] -3- (1,4,6-triaminopyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7- [(z) -2- (5-amino-1,2,4-thiadiazol-3-yl) -2- (ethoxyimino) acetamido] -3- (1,4,6-triamino Pyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7-[(z) -2- (2-aminothiazol-4-yl) -2- (2-propyne- 1-oxyimino) acetamido] -3- (1,4,6-triaminopyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7-[(z) -2 -(2-aminothiazol-4-yl) -2- (methoxyimino) acetamido] -3- (1,4,6-triaminopyrimidin-2-yl) thiomethyl-3-cepem -4-carboxylate, 7-[(z) -2- (5-amino-1, 2,4-thiadiazol-3-yl) -2- (ethoxyimino) acetamido] -3- (4,6-diamino-1-ethylpyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7-[(z) -2- (5-amino-1,2, 4-thiadiazol-3-yl) -2- (ethoxyimino) acetamido] -3- (4,6-diamino-1-propyl Rimidinium-2-yl) thiomethyl-3-cepem-4-carboxylate, 7-[(z) -2- (5-amino-1,2,4-thiadiazol-3-yl)- 2 (-ethoxyimino) acetamido] -3- (1-allyl-4,6-diaminopropylliminium-2-yl) -3-cepem-4-carboxylate, 7-[(z ) -2- (5-amino-1,2,4-thiadiazol-3-yl) -2- (methoxyimino) acetamido] -3- (4,6-diamino-1-methylpyridine Midinium-2-yl) thiomethyl-3-cepem-4-carboxylate, 7 [(z) -2- (5-amino-1,2,4-thiadiazol-3-yl) -2- (Methoxyimino) acetamido] -3- (4,6-diamino-1-ethylpyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7-[(z) -2- (2-aminothiazol-4-yl) -2- (ethoxyimino) acetamido] -3- (4,6-diamino-1-phenylpyrimidin-2-yl) thiomethyl -3-cepem-4-carboxylate, 7-[(z) -2- (2-aminothiazol-4-yl) -2- (ethoxyimino) acetamido] -3- (1- ( 4-chlorophenyl) -4,6-diaminopyrimidin-2-yl) thiomethyl-3-cepem-4-carboxylate, 7- [ (z) -2- (2-aminothiazol-4-yl) -2- (ethoxyimino) acetamido] -3- (4,6-diamino-1- (2,4-dimethylphenyl) Pyrimidin-2-yl] thiomethyl-3-cepem-4-carboxylate, 7 [(z) -2- (2-aminothiazol-4-yl) -2- (2-propyn-1 -Oxyimino) acetamido] -3- (4,6-diamino-1-ethylpyrimidin-2-yl] thiomethyl-3-sepime-4-carboxylate, 7-[(z)- 2- (2-aminothiazol-4-yl) -2- (2-propene-1-oxyimino) acetamido] -3- (4,6-diamino-1-methylpyrimidinium-2 -Yl) -3-cepem-4-carboxylate, 7-[(z) -2- (2-aminothiazol-4-yl) -2- (2-propene-1-oxyimino) acetami Fig.]-3- (4,6-Diamino-1-ethylpyrimidin-2-yl) -3-cepem-4-carboxylate, 7-[(z) -2- (2-aminothiazole -4-yl) -2- (methoxyimino) acetamido] -3- (4,6-diamino-1-ethylpyrimidin-2-yl) thiomethyl-3-cepem-4-carboxyl An aqueous composition, characterized in that the compound selected from the group consisting of the rate. 제1항에 있어서, 상기 세파로스포린 화합물 5 내지 15중량%, 니코틴아미드 10 내지 50중량% 및 증류수 45 내지 85중량%로 구성된 것을 특징으로 하는 주사제용 수성 조성물.The aqueous composition for injection according to claim 1, which comprises 5 to 15% by weight of the cephalosporin compound, 10 to 50% by weight of nicotinamide and 45 to 85% by weight of distilled water. 증류수에 니코틴아미드를 첨가하여 니코틴아미드 용액을 제공하는 단계와 상기 니코틴아미드 용액에 다음 일반식(VII)로 표시되는 세파로스포린 화합물을 첨가하여 용해시키는 단계와 상기 세파로스포린 화합물의 수용액으로부터 용해되지 않는 과량의 세파로스포린 화합물을 여과하여 제거하는 단계를 포함하는 것을 특징으로 하는 제1항의 수성 조성물의 제조방법.Adding nicotinamide to distilled water to provide a nicotinamide solution, and adding and dissolving the cephalosporin compound represented by the following general formula (VII) to the nicotinamide solution and dissolving from the aqueous solution of the cephalosporin compound A method for preparing the aqueous composition of claim 1, comprising the step of filtering out the excess cephalosporin compound. 상기 일반식에서 R1은 -COOH를 포함하지 않는 C1-4알킬기, C3-4알케닐기 또는 C3-4알키닐기이고, R2는 C1-4알킬기, C3-4알케닐기 또는 C3-9사이클로 알킬기를 나타내며, R3는 수소 또는 C1-4알킬기이고, Q는 N 또는 CH이다.In the general formula, R 1 is a C 1-4 alkyl group, C 3-4 alkenyl group or C 3-4 alkynyl group that does not contain -COOH, R 2 is a C 1-4 alkyl group, C 3-4 alkenyl group or C A 3-9 cycloalkyl group, R 3 is hydrogen or a C 1-4 alkyl group, and Q is N or CH. 제4항에 있어서, 상기 수성 조성물을 동결건조시키는 단계를 더 포함하는 것을 특징으로 하는 방법.5. The method of claim 4, further comprising lyophilizing the aqueous composition. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019920025908A 1992-12-28 1992-12-28 Cephalosporin water soluble composition KR960008236B1 (en)

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