JPH06508844A - ベータ−ラクタム抗生物質およびクラブラン酸またはその水溶性塩の医薬製剤 - Google Patents

ベータ−ラクタム抗生物質およびクラブラン酸またはその水溶性塩の医薬製剤

Info

Publication number: JPH06508844A
Authority: JP; Japan
Prior art keywords: acid; pharmaceutical; formulation according; salts; pharmaceutical formulation
Prior art date: 1991-07-11
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.): Pending

Application number

JP5502080A

Other languages

English (en)

Japanese (ja)

Inventor

クラファム，ディビッド

Original Assignee

スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー

Priority date (The priority date 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 date listed.)

1991-07-11

Filing date

1992-07-03

Publication date

1994-10-06

1992-07-03 Application filed by スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー filed Critical スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー

1994-10-06 Publication of JPH06508844A publication Critical patent/JPH06508844A/ja

Status Pending legal-status Critical Current

Links

239000008194 pharmaceutical composition Substances 0.000 title claims description 20
150000003839 salts Chemical class 0.000 title claims description 20
239000003782 beta lactam antibiotic agent Substances 0.000 title claims description 10
239000002132 β-lactam antibiotic Substances 0.000 title claims description 10
229940124586 β-lactam antibiotics Drugs 0.000 title claims description 10
HZZVJAQRINQKSD-UHFFFAOYSA-N Clavulanic acid Natural products OC(=O)C1C(=CCO)OC2CC(=O)N21 HZZVJAQRINQKSD-UHFFFAOYSA-N 0.000 title claims description 6
HZZVJAQRINQKSD-PBFISZAISA-N clavulanic acid Chemical compound OC(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 HZZVJAQRINQKSD-PBFISZAISA-N 0.000 title claims description 6
229960003324 clavulanic acid Drugs 0.000 title claims description 6
KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 31
239000000203 mixture Substances 0.000 claims description 20
238000009472 formulation Methods 0.000 claims description 19
239000000725 suspension Substances 0.000 claims description 17
LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin 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=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 claims description 13
239000001384 succinic acid Substances 0.000 claims description 13
OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 11
150000001768 cations Chemical group 0.000 claims description 10
229960003022 amoxicillin Drugs 0.000 claims description 9
LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 claims description 9
ZDQYSKICYIVCPN-UHFFFAOYSA-L sodium succinate (anhydrous) Chemical compound [Na+].[Na+].[O-]C(=O)CCC([O-])=O ZDQYSKICYIVCPN-UHFFFAOYSA-L 0.000 claims description 9
239000000243 solution Substances 0.000 claims description 9
239000007900 aqueous suspension Substances 0.000 claims description 8
238000000034 method Methods 0.000 claims description 8
239000007864 aqueous solution Substances 0.000 claims description 7
239000000825 pharmaceutical preparation Substances 0.000 claims description 7
208000035143 Bacterial infection Diseases 0.000 claims description 6
230000002378 acidificating effect Effects 0.000 claims description 6
208000022362 bacterial infectious disease Diseases 0.000 claims description 6
150000001991 dicarboxylic acids Chemical class 0.000 claims description 6
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 6
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 4
238000004519 manufacturing process Methods 0.000 claims description 4
239000000546 pharmaceutical excipient Substances 0.000 claims description 4
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 4
241001465754 Metazoa Species 0.000 claims description 3
239000012736 aqueous medium Substances 0.000 claims description 3
230000003115 biocidal effect Effects 0.000 claims description 3
KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims description 3
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 2
229960000723 ampicillin Drugs 0.000 claims description 2
229940079593 drug Drugs 0.000 claims description 2
239000003814 drug Substances 0.000 claims description 2
239000001530 fumaric acid Substances 0.000 claims description 2
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 2
239000011976 maleic acid Substances 0.000 claims description 2
230000001225 therapeutic effect Effects 0.000 claims description 2
125000000217 alkyl group Chemical group 0.000 claims 1
125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
ABVRVIZBZKUTMK-JSYANWSFSA-M potassium clavulanate Chemical compound [K+].[O-]C(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 ABVRVIZBZKUTMK-JSYANWSFSA-M 0.000 claims 1
239000002253 acid Substances 0.000 description 22
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 19
239000000796 flavoring agent Substances 0.000 description 16
235000019634 flavors Nutrition 0.000 description 15
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 7
229910052700 potassium Inorganic materials 0.000 description 7
239000011591 potassium Substances 0.000 description 7
239000000843 powder Substances 0.000 description 6
239000000377 silicon dioxide Substances 0.000 description 6
229960004920 amoxicillin trihydrate Drugs 0.000 description 5
239000008187 granular material Substances 0.000 description 5
239000000230 xanthan gum Substances 0.000 description 5
229920001285 xanthan gum Polymers 0.000 description 5
229940082509 xanthan gum Drugs 0.000 description 5
235000010493 xanthan gum Nutrition 0.000 description 5
229910002016 Aerosil® 200 Inorganic materials 0.000 description 4
108010011485 Aspartame Proteins 0.000 description 4
235000011034 Rubus glaucus Nutrition 0.000 description 4
244000235659 Rubus idaeus Species 0.000 description 4
235000009122 Rubus idaeus Nutrition 0.000 description 4
239000000605 aspartame Substances 0.000 description 4
IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 4
229960003438 aspartame Drugs 0.000 description 4
235000010357 aspartame Nutrition 0.000 description 4
235000012239 silicon dioxide Nutrition 0.000 description 4
229920003091 Methocel™ Polymers 0.000 description 3
239000003242 anti bacterial agent Substances 0.000 description 3
229940088710 antibiotic agent Drugs 0.000 description 3
239000003795 chemical substances by application Substances 0.000 description 3
239000008119 colloidal silica Substances 0.000 description 3
-1 succinate anion Chemical class 0.000 description 3
239000006188 syrup Substances 0.000 description 3
235000020357 syrup Nutrition 0.000 description 3
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
239000000337 buffer salt Substances 0.000 description 2
239000003826 tablet Substances 0.000 description 2
239000007916 tablet composition Substances 0.000 description 2
239000002562 thickening agent Substances 0.000 description 2
150000004684 trihydrates Chemical group 0.000 description 2
OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
229930186147 Cephalosporin Natural products 0.000 description 1
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
229910019142 PO4 Inorganic materials 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
108010013381 Porins Proteins 0.000 description 1
229910052784 alkaline earth metal Inorganic materials 0.000 description 1
229910000147 aluminium phosphate Inorganic materials 0.000 description 1
239000013011 aqueous formulation Substances 0.000 description 1
235000013527 bean curd Nutrition 0.000 description 1
239000003781 beta lactamase inhibitor Substances 0.000 description 1
229940126813 beta-lactamase inhibitor Drugs 0.000 description 1
239000004067 bulking agent Substances 0.000 description 1
229910052791 calcium Inorganic materials 0.000 description 1
239000011575 calcium Substances 0.000 description 1
150000004649 carbonic acid derivatives Chemical class 0.000 description 1
239000001913 cellulose Substances 0.000 description 1
229920002678 cellulose Polymers 0.000 description 1
229940124587 cephalosporin Drugs 0.000 description 1
150000001780 cephalosporins Chemical class 0.000 description 1
150000001860 citric acid derivatives Chemical class 0.000 description 1
HZZVJAQRINQKSD-PBFISZAISA-M clavulanate Chemical compound [O-]C(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 HZZVJAQRINQKSD-PBFISZAISA-M 0.000 description 1
239000006071 cream Substances 0.000 description 1
239000002274 desiccant Substances 0.000 description 1
230000001627 detrimental effect Effects 0.000 description 1
235000013355 food flavoring agent Nutrition 0.000 description 1
235000003599 food sweetener Nutrition 0.000 description 1
239000003292 glue Substances 0.000 description 1
239000004615 ingredient Substances 0.000 description 1
238000011835 investigation Methods 0.000 description 1
150000003951 lactams Chemical class 0.000 description 1
239000007788 liquid Substances 0.000 description 1
229940049954 penicillin Drugs 0.000 description 1
235000021317 phosphate Nutrition 0.000 description 1
150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
102000007739 porin activity proteins Human genes 0.000 description 1
239000002994 raw material Substances 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000011734 sodium Substances 0.000 description 1
238000003756 stirring Methods 0.000 description 1
238000003860 storage Methods 0.000 description 1
150000003890 succinate salts Chemical class 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1

Classifications

- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Public Health (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Epidemiology (AREA)
Animal Behavior & Ethology (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Oil, Petroleum & Natural Gas (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)

JP5502080A 1991-07-11 1992-07-03 ベータ−ラクタム抗生物質およびクラブラン酸またはその水溶性塩の医薬製剤 Pending JPH06508844A (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
GB919114950A GB9114950D0 (en)	1991-07-11	1991-07-11	Pharmaceutical formulation
GB9114950.0		1991-07-11
PCT/GB1992/001207 WO1993000898A1 (fr)	1991-07-11	1992-07-03	Formulation pharmaceutique comprenant une beta-lactamine et de l'acide clavulanique ou un sel de celui-ci soluble dans l'eau

Publications (1)

Publication Number	Publication Date
JPH06508844A true JPH06508844A (ja)	1994-10-06

Family

ID=10698173

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP5502080A Pending JPH06508844A (ja)	1991-07-11	1992-07-03	ベータ−ラクタム抗生物質およびクラブラン酸またはその水溶性塩の医薬製剤

Country Status (5)

Country	Link
EP (1)	EP0593573A1 (fr)
JP (1)	JPH06508844A (fr)
AU (1)	AU2230692A (fr)
GB (1)	GB9114950D0 (fr)
WO (1)	WO1993000898A1 (fr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
AR004510A1 (es)	1995-09-07	1998-12-16	Smithkline Beecham Plc	Composiciones que comprenden amoxicilina y clavulanato, procedimientos para su preparacion y el uso de las composiciones para la fabricacion de unmedicamento
US5759579A (en) *	1996-12-05	1998-06-02	American Home Products Corporation	Pharmaceutical suspension systems
DE19706978A1 (de) *	1997-02-21	1998-08-27	Ulrich Dr Posanski	Kombinationspräparat für oral applizierbare Antibiotika
US20010016577A1 (en) *	1998-08-24	2001-08-23	Douglas Joseph Dobrozsi	Oral mucoadhesive compositions containing gastrointestinal actives
US6878386B1 (en)	1999-04-13	2005-04-12	Beecham Pharmaceuticals (Pte) Limited	Method of treating a bacterial infection comprising amoxycillin and potassium clavulanate
US6294199B1 (en)	1999-04-13	2001-09-25	Beecham Pharmaceuticals (Pte) Limited	Method of treating a bacterial infection comprising administering amoxycillin
US7250176B1 (en)	1999-04-13	2007-07-31	Beecham Pharmaceuticals (Pte) Limited	Method of treating a bacterial infection
WO2002030392A2 (fr)	2000-10-12	2002-04-18	Beecham Pharmaceuticals (Pte) Limited	Nouvelle formulation
US6756057B2 (en)	2000-10-12	2004-06-29	Beecham Pharmaceuticals (Pte) Limited	Amoxicillin and potassium clavulanate dosage form
CA2620675C (fr)	2005-09-22	2015-04-14	Meiji Seika Kaisha, Ltd.	Inhibiteur de la metallo-.beta.-lactamase
TR201000688A2 (tr)	2010-01-29	2011-08-22	B�Lg�� Mahmut	Aktif madde olarak sefaklor ve klavulanik asit içeren efervesan formülasyonlar.
EP2568957A1 (fr)	2010-05-14	2013-03-20	Mahmut Bilgic	Composition pharmaceutique comprenant la céfixime et un composé dérivé de l'acide clavulanique
EP2568959A2 (fr)	2010-05-14	2013-03-20	Mahmut Bilgic	Formulations comprenant une céphalosporine et un acide clavulanique de troisième génération
WO2011152808A1 (fr)	2010-06-03	2011-12-08	Mahmut Bilgic	Formulation comprenant du cefpodoxime proxétil et de l'acide clavulanique

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP0080862B1 (fr) *	1981-12-02	1985-09-25	Beecham Group Plc	Préparation pharmaceutique contenant des antibiotiques béta-lactame
GB9007945D0 (en) *	1990-04-07	1990-06-06	Beecham Group Plc	Pharmaceutical formulation

1991
- 1991-07-11 GB GB919114950A patent/GB9114950D0/en active Pending
1992
- 1992-07-03 AU AU22306/92A patent/AU2230692A/en not_active Abandoned
- 1992-07-03 EP EP92914294A patent/EP0593573A1/fr not_active Withdrawn
- 1992-07-03 WO PCT/GB1992/001207 patent/WO1993000898A1/fr not_active Ceased
- 1992-07-03 JP JP5502080A patent/JPH06508844A/ja active Pending

Also Published As

Publication number	Publication date
GB9114950D0 (en)	1991-08-28
WO1993000898A1 (fr)	1993-01-21
AU2230692A (en)	1993-02-11
EP0593573A1 (fr)	1994-04-27

Publication	Publication Date	Title
JPH06508844A (ja)	1994-10-06	ベータ−ラクタム抗生物質およびクラブラン酸またはその水溶性塩の医薬製剤
US4861592A (en)	1989-08-29	Pharmaceutical compositions
US6726908B2 (en)	2004-04-27	Pharmaceutical formulation
US4676984A (en)	1987-06-30	Rehydratable antacid composition
EP1057828B1 (fr)	2003-03-19	Suspensions de trovafloxacine administrées par voie orale
EP0524579B1 (fr)	1998-03-11	Formulations orales dosées et améliorées de dideoxy purine nucléosides
US5976578A (en)	1999-11-02	Liquid antacid compositions
JPH06504991A (ja)	1994-06-09	組成物
PT1841432E (pt)	2010-10-25	Composições para combater a resistência aos antibióticos mediada pela beta-lactamase usando inibidores da betalactamase úteis para injecção
JPH10316577A (ja)	1998-12-02	液体制酸薬組成物
BG63821B1 (bg)	2003-02-28	Фармацевтичен състав на стабилизиран карбапенемовантибиотик и метод за получаване
EA001878B1 (ru)	2001-10-22	Способ лечения бактериальных инфекций у детей
US4704278A (en)	1987-11-03	Fluidized magaldrate suspension
EP1452169B1 (fr)	2007-01-24	Compositions pharmaceutiques liquides de base aqueuse en forme de suspension destinnees a l'administration par voie orale d'ibuprofene
IL31858A (en)	1972-05-30	Concentrated liquid mixtures against acids
US20130129791A1 (en)	2013-05-23	Preparations of effervescent formulations comprising second and third generation cephalosporin and uses thereof
TW477700B (en)	2002-03-01	Improved process for preparing potassium clavulancate
US4272542A (en)	1981-06-09	Use of di-sodium and di-potassium salts of dicarboxylic amino acids and tri- or di-sodium or potassium phosphate tartrate or citrate to improve the taste of in vivo hydrolysable esters of α-amino penicillins and cephalosporins
JPS61118321A (ja)	1986-06-05	流動化マガルドラート組成物
US20030104017A1 (en)	2003-06-05	Epinastine formulation for oral administration
IL30684A (en)	1972-12-29	Therapeutic compositions containing ampicillin or hetacillin and nystatin
EP0008178A2 (fr)	1980-02-20	Poudre, procédé pour sa préparation, récipient la contenant, et sirop comprenant la poudre reconstituée avec de l'eau
US6265449B1 (en)	2001-07-24	Aqueous compositions comprising ranitidine and LCMT sucrose
JP3364453B2 (ja)	2003-01-08	センノシド含有水性液剤
CA1252045A (fr)	1989-04-04	Suspension fluidisee de magaldrate