EP2566450A2 - Pharmazeutische zusammensetzungen mit cefetamet - Google Patents

Pharmazeutische zusammensetzungen mit cefetamet

Info

Publication number: EP2566450A2
Authority: EP; European Patent Office
Prior art keywords: cefetamet; formulation according; range; combination; weight
Prior art date: 2010-05-04
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 Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

EP11724475A

Other languages

English (en)

French (fr)

Inventor

Mahmut Bilgic

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Individual

Original Assignee

Individual

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.)

2010-05-04

Filing date

2011-05-02

Publication date

2013-03-13

2011-05-02 Application filed by Individual filed Critical Individual

2013-03-13 Publication of EP2566450A2 publication Critical patent/EP2566450A2/de

Status Withdrawn legal-status Critical Current

Links

MQLRYUCJDNBWMV-GHXIOONMSA-N cefetamet Chemical compound N([C@@H]1C(N2C(=C(C)CS[C@@H]21)C(O)=O)=O)C(=O)\C(=N/OC)C1=CSC(N)=N1 MQLRYUCJDNBWMV-GHXIOONMSA-N 0.000 title claims abstract description 53
229960004041 cefetamet Drugs 0.000 title claims abstract description 52
239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 14
238000000034 method Methods 0.000 claims abstract description 14
238000002360 preparation method Methods 0.000 claims abstract description 7
239000000203 mixture Substances 0.000 claims description 65
238000009472 formulation Methods 0.000 claims description 58
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 30
239000000314 lubricant Substances 0.000 claims description 20
229920002472 Starch Polymers 0.000 claims description 10
239000013543 active substance Substances 0.000 claims description 9
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 claims description 8
WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 8
239000011230 binding agent Substances 0.000 claims description 8
DASYMCLQENWCJG-XUKDPADISA-N cefetamet pivoxil Chemical group N([C@@H]1C(N2C(=C(C)CS[C@@H]21)C(=O)OCOC(=O)C(C)(C)C)=O)C(=O)\C(=N/OC)C1=CSC(N)=N1 DASYMCLQENWCJG-XUKDPADISA-N 0.000 claims description 8
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-1 polyoxyethylene Polymers 0.000 claims description 7
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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 claims description 2
229960003438 aspartame Drugs 0.000 claims description 2
239000002585 base Substances 0.000 claims description 2
239000000440 bentonite Substances 0.000 claims description 2
229910000278 bentonite Inorganic materials 0.000 claims description 2
235000012216 bentonite Nutrition 0.000 claims description 2
SVPXDRXYRYOSEX-UHFFFAOYSA-N bentoquatam Chemical compound O.O=[Si]=O.O=[Al]O[Al]=O SVPXDRXYRYOSEX-UHFFFAOYSA-N 0.000 claims description 2
SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 claims description 2
229910000019 calcium carbonate Inorganic materials 0.000 claims description 2
239000001506 calcium phosphate Substances 0.000 claims description 2
229910000389 calcium phosphate Inorganic materials 0.000 claims description 2
235000011010 calcium phosphates Nutrition 0.000 claims description 2
229960005233 cineole Drugs 0.000 claims description 2
235000015165 citric acid Nutrition 0.000 claims description 2
239000003086 colorant Substances 0.000 claims description 2
235000005822 corn Nutrition 0.000 claims description 2
229960001681 croscarmellose sodium Drugs 0.000 claims description 2
229960000913 crospovidone Drugs 0.000 claims description 2
235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 2
HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical class OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 claims description 2
235000019425 dextrin Nutrition 0.000 claims description 2
CEYULKASIQJZGP-UHFFFAOYSA-L disodium;2-(carboxymethyl)-2-hydroxybutanedioate Chemical compound [Na+].[Na+].[O-]C(=O)CC(O)(C(=O)O)CC([O-])=O CEYULKASIQJZGP-UHFFFAOYSA-L 0.000 claims description 2
235000019414 erythritol Nutrition 0.000 claims description 2
UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 2
229940009714 erythritol Drugs 0.000 claims description 2
235000019325 ethyl cellulose Nutrition 0.000 claims description 2
229920001249 ethyl cellulose Polymers 0.000 claims description 2
239000010642 eucalyptus oil Substances 0.000 claims description 2
229940044949 eucalyptus oil Drugs 0.000 claims description 2
239000001902 eugenia caryophyllata l. bud oil Substances 0.000 claims description 2
229960002217 eugenol Drugs 0.000 claims description 2
239000012458 free base Substances 0.000 claims description 2
239000001530 fumaric acid Substances 0.000 claims description 2
235000011087 fumaric acid Nutrition 0.000 claims description 2
229930182830 galactose Natural products 0.000 claims description 2
239000008273 gelatin Substances 0.000 claims description 2
229920000159 gelatin Polymers 0.000 claims description 2
235000019322 gelatine Nutrition 0.000 claims description 2
235000011852 gelatine desserts Nutrition 0.000 claims description 2
WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 2
235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 2
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
239000003456 ion exchange resin Substances 0.000 claims description 2
229920003303 ion-exchange polymer Polymers 0.000 claims description 2
239000000905 isomalt Substances 0.000 claims description 2
235000010439 isomalt Nutrition 0.000 claims description 2
HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims description 2
239000004310 lactic acid Substances 0.000 claims description 2
235000014655 lactic acid Nutrition 0.000 claims description 2
239000000832 lactitol Substances 0.000 claims description 2
235000010448 lactitol Nutrition 0.000 claims description 2
VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims description 2
229960003451 lactitol Drugs 0.000 claims description 2
229960001375 lactose Drugs 0.000 claims description 2
239000010501 lemon oil Substances 0.000 claims description 2
229930007744 linalool Natural products 0.000 claims description 2
235000019359 magnesium stearate Nutrition 0.000 claims description 2
239000001630 malic acid Substances 0.000 claims description 2
235000011090 malic acid Nutrition 0.000 claims description 2
235000010449 maltitol Nutrition 0.000 claims description 2
239000000845 maltitol Substances 0.000 claims description 2
VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims description 2
229940035436 maltitol Drugs 0.000 claims description 2
229940043353 maltol Drugs 0.000 claims description 2
229960002160 maltose Drugs 0.000 claims description 2
239000001525 mentha piperita l. herb oil Substances 0.000 claims description 2
229940041616 menthol Drugs 0.000 claims description 2
KXKVLQRXCPHEJC-UHFFFAOYSA-N methyl acetate Chemical compound COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims description 2
OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 claims description 2
238000002156 mixing Methods 0.000 claims description 2
ITVGXXMINPYUHD-CUVHLRMHSA-N neohesperidin dihydrochalcone Chemical compound C1=C(O)C(OC)=CC=C1CCC(=O)C(C(=C1)O)=C(O)C=C1O[C@H]1[C@H](O[C@H]2[C@@H]([C@H](O)[C@@H](O)[C@H](C)O2)O)[C@@H](O)[C@H](O)[C@@H](CO)O1 ITVGXXMINPYUHD-CUVHLRMHSA-N 0.000 claims description 2
229940089953 neohesperidin dihydrochalcone Drugs 0.000 claims description 2
235000010434 neohesperidine DC Nutrition 0.000 claims description 2
235000019412 neotame Nutrition 0.000 claims description 2
HLIAVLHNDJUHFG-HOTGVXAUSA-N neotame Chemical compound CC(C)(C)CCN[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 HLIAVLHNDJUHFG-HOTGVXAUSA-N 0.000 claims description 2
108010070257 neotame Proteins 0.000 claims description 2
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 2
239000003921 oil Substances 0.000 claims description 2
235000019198 oils Nutrition 0.000 claims description 2
239000010502 orange oil Substances 0.000 claims description 2
239000010663 parsley oil Substances 0.000 claims description 2
235000019477 peppermint oil Nutrition 0.000 claims description 2
235000011007 phosphoric acid Nutrition 0.000 claims description 2
235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 2
229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 2
239000011736 potassium bicarbonate Substances 0.000 claims description 2
229910000028 potassium bicarbonate Inorganic materials 0.000 claims description 2
235000015497 potassium bicarbonate Nutrition 0.000 claims description 2
229910000027 potassium carbonate Inorganic materials 0.000 claims description 2
235000011181 potassium carbonates Nutrition 0.000 claims description 2
239000001508 potassium citrate Substances 0.000 claims description 2
229960002635 potassium citrate Drugs 0.000 claims description 2
QEEAPRPFLLJWCF-UHFFFAOYSA-K potassium citrate (anhydrous) Chemical compound [K+].[K+].[K+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O QEEAPRPFLLJWCF-UHFFFAOYSA-K 0.000 claims description 2
235000011082 potassium citrates Nutrition 0.000 claims description 2
TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims description 2
235000011118 potassium hydroxide Nutrition 0.000 claims description 2
229940069328 povidone Drugs 0.000 claims description 2
235000019260 propionic acid Nutrition 0.000 claims description 2
IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims description 2
235000002020 sage Nutrition 0.000 claims description 2
239000001632 sodium acetate Substances 0.000 claims description 2
235000017281 sodium acetate Nutrition 0.000 claims description 2
WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 2
239000004299 sodium benzoate Substances 0.000 claims description 2
235000010234 sodium benzoate Nutrition 0.000 claims description 2
229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 2
235000017557 sodium bicarbonate Nutrition 0.000 claims description 2
229910000029 sodium carbonate Inorganic materials 0.000 claims description 2
235000017550 sodium carbonate Nutrition 0.000 claims description 2
229920003109 sodium starch glycolate Polymers 0.000 claims description 2
239000008109 sodium starch glycolate Substances 0.000 claims description 2
229940079832 sodium starch glycolate Drugs 0.000 claims description 2
239000003381 stabilizer Substances 0.000 claims description 2
238000010561 standard procedure Methods 0.000 claims description 2
239000008107 starch Substances 0.000 claims description 2
229940032147 starch Drugs 0.000 claims description 2
239000008117 stearic acid Substances 0.000 claims description 2
229940013618 stevioside Drugs 0.000 claims description 2
OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims description 2
235000019202 steviosides Nutrition 0.000 claims description 2
235000019408 sucralose Nutrition 0.000 claims description 2
BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 2
235000000346 sugar Nutrition 0.000 claims description 2
150000008163 sugars Chemical class 0.000 claims description 2
239000004094 surface-active agent Substances 0.000 claims description 2
239000006188 syrup Substances 0.000 claims description 2
235000020357 syrup Nutrition 0.000 claims description 2
239000000454 talc Substances 0.000 claims description 2
229910052623 talc Inorganic materials 0.000 claims description 2
235000012222 talc Nutrition 0.000 claims description 2
239000011975 tartaric acid Substances 0.000 claims description 2
235000002906 tartaric acid Nutrition 0.000 claims description 2
239000000892 thaumatin Substances 0.000 claims description 2
235000010436 thaumatin Nutrition 0.000 claims description 2
229960000790 thymol Drugs 0.000 claims description 2
QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 2
239000001993 wax Substances 0.000 claims description 2
239000009637 wintergreen oil Substances 0.000 claims description 2
MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 1
229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
239000008187 granular material Substances 0.000 description 7
239000003826 tablet Substances 0.000 description 6
239000002552 dosage form Substances 0.000 description 5
239000000843 powder Substances 0.000 description 4
238000004090 dissolution Methods 0.000 description 3
239000000725 suspension Substances 0.000 description 3
238000011282 treatment Methods 0.000 description 3
239000003814 drug Substances 0.000 description 2
230000000694 effects Effects 0.000 description 2
239000007911 effervescent powder Substances 0.000 description 2
238000005469 granulation Methods 0.000 description 2
230000003179 granulation Effects 0.000 description 2
238000007873 sieving Methods 0.000 description 2
239000004562 water dispersible granule Substances 0.000 description 2
239000004565 water dispersible tablet Substances 0.000 description 2
IPYWNMVPZOAFOQ-NABDTECSSA-N (6r,7r)-7-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-(carboxymethoxyimino)acetyl]amino]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;trihydrate Chemical compound O.O.O.S1C(N)=NC(C(=N\OCC(O)=O)\C(=O)N[C@@H]2C(N3C(=C(C=C)CS[C@@H]32)C(O)=O)=O)=C1 IPYWNMVPZOAFOQ-NABDTECSSA-N 0.000 description 1
QNVKOSLOVOTXKF-UHFFFAOYSA-N 4-[(2-amino-3,5-dibromophenyl)methylamino]cyclohexan-1-ol;hydron;chloride Chemical compound Cl.NC1=C(Br)C=C(Br)C=C1CNC1CCC(O)CC1 QNVKOSLOVOTXKF-UHFFFAOYSA-N 0.000 description 1
229910002016 Aerosil® 200 Inorganic materials 0.000 description 1
241000894006 Bacteria Species 0.000 description 1
208000035143 Bacterial infection Diseases 0.000 description 1
229930186147 Cephalosporin Natural products 0.000 description 1
208000035473 Communicable disease Diseases 0.000 description 1
208000019505 Deglutition disease Diseases 0.000 description 1
108090000204 Dipeptidase 1 Proteins 0.000 description 1
241000588914 Enterobacter Species 0.000 description 1
241000192125 Firmicutes Species 0.000 description 1
206010018612 Gonorrhoea Diseases 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
206010021531 Impetigo Diseases 0.000 description 1
206010024971 Lower respiratory tract infections Diseases 0.000 description 1
208000016604 Lyme disease Diseases 0.000 description 1
241000588653 Neisseria Species 0.000 description 1
206010033078 Otitis media 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
201000007100 Pharyngitis Diseases 0.000 description 1
206010037596 Pyelonephritis Diseases 0.000 description 1
208000006311 Pyoderma Diseases 0.000 description 1
206010057190 Respiratory tract infections Diseases 0.000 description 1
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
206010062255 Soft tissue infection Diseases 0.000 description 1
241000194017 Streptococcus Species 0.000 description 1
238000010521 absorption reaction Methods 0.000 description 1
229960000985 ambroxol hydrochloride Drugs 0.000 description 1
208000022362 bacterial infectious disease Diseases 0.000 description 1
102000006635 beta-lactamase Human genes 0.000 description 1
230000003115 biocidal effect Effects 0.000 description 1
229960002129 cefixime Drugs 0.000 description 1
229940124587 cephalosporin Drugs 0.000 description 1
150000001780 cephalosporins Chemical class 0.000 description 1
201000003146 cystitis Diseases 0.000 description 1
239000006185 dispersion Substances 0.000 description 1
239000007938 effervescent tablet Substances 0.000 description 1
229940041006 first-generation cephalosporins Drugs 0.000 description 1
208000001786 gonorrhea Diseases 0.000 description 1
208000015181 infectious disease Diseases 0.000 description 1
239000007788 liquid Substances 0.000 description 1
239000007935 oral tablet Substances 0.000 description 1
229940096978 oral tablet Drugs 0.000 description 1
229940049954 penicillin Drugs 0.000 description 1
238000011321 prophylaxis Methods 0.000 description 1
230000002685 pulmonary effect Effects 0.000 description 1
208000020029 respiratory tract infectious disease Diseases 0.000 description 1
229940041008 second-generation cephalosporins Drugs 0.000 description 1
201000009890 sinusitis Diseases 0.000 description 1
206010040872 skin infection Diseases 0.000 description 1
239000011734 sodium Substances 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
235000015424 sodium Nutrition 0.000 description 1
NZQJSIPYDOTDFS-JJHIVTNASA-M sodium;(6r,7r)-7-[[(2e)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate Chemical compound [Na+].N([C@@H]1C(N2C(=C(C)CS[C@@H]21)C([O-])=O)=O)C(=O)/C(=N/OC)C1=CSC(N)=N1 NZQJSIPYDOTDFS-JJHIVTNASA-M 0.000 description 1
239000002904 solvent Substances 0.000 description 1
239000000126 substance Substances 0.000 description 1
206010044008 tonsillitis Diseases 0.000 description 1
208000000143 urethritis Diseases 0.000 description 1
239000004554 water soluble tablet Substances 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
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent

Definitions

the present invention relates to pharmaceutical compositions comprising cefetamet or any pharmaceutically acceptable derivative thereof, and the use of said compositions in the treatment of bacterial infections.
Cefetamet which has the chemical name (6R,7R)-7-[[(2Z)-2-(2-amino-4- thiazolyl)(methoxyimino)acetyl] amino] -3 -methyl- 8-oxo-5 -thia- 1 -azabicyclo [4.2.0]
oct-2-ene- 2-carboxylic acid is a third generation cephalosporin antibiotic that has a perfect effect particularly on the species streptococcus, enterobacter, neisseria, hemophilus. It was first disclosed in the patent numbered US4396681 and its strong effect on gram positive and gram negative bacteria was indicated in that patent document.
Cefetamet is more durable against the enzyme beta-lactamase compared to penicillin, first and second generation cephalosporins.
the formulation comprising the active agent cefetamet is marketed in 250 mg and 500 mg oral tablet forms.
the tablet forms comprising 250 and 500 mg active agent in a single dose are formulated with excipients, they become quite large in size and this made the use of this dosage form inconvenient in patients with dysphagia, particularly in pediatric and geriatric patients.
suspension forms have been developed to overcome said problems in the prior art.
the patent application numbered in CN 1650868 discloses a medicine in the form of oral liquid or suspension for treating pulmonary infectious diseases which is prepared from ambroxol hydrochloride and one of cefixime, cefetamet sodium and cefetamet hydrochloride.
suspension forms comprising cefetamet are not preferred since they have the potential of high and/or uncontrolled dose intake and are not physically and chemically stable.
Cefetamet has a low solubility in water. For that reason, it is generally observed that water dispersible formulations comprising cefetamet cannot quickly disperse since cefetamet cannot dissolve in water entirely. Accordingly, the desirable amount of cefetamet cannot be absorbed and this leads to low bioavailability of it.
the inventors have surprisingly found that the water dispersible dosage forms comprising cefetamet and its any pharmaceutically acceptable derivative pertaining to the present invention overcome the problems encountered in the prior art.
the present invention relates to the water dispersible powder, tablet and granules comprising cefetamet and/or pharmaceutically acceptable salts, hydrates, solvates, esters, amorphous and crystal forms of cefetamet and/or combination thereof; their formulations and the procedures for their preparation.
cefetamet in which d 50 value of the molecule cefetamet is in the range of 10-50 ⁇ solubility problem of cefetamet can be overcome and the formulation comprising it can disperse entirely and quickly.
the inventors have found that the water dispersible formulations comprising cefetamet in which d 0 value of the cefetamet is in the range of 10-50 ⁇ , has increased solubility of cefetamet and thus the rapid and entire dispersion of said formulations. This provides the increase of the absorption of cefetamet as the active agent and hence the increase of its bioavailability.
the first aspect of the present invention is the water dispersible formulations comprising cefetamet wherein d 50 value of the molecule cefetamet is in the range of 10-50 ⁇ .
water dispersible formulations present in the text comprises effervescent tablets, effervescent granules, effervescent powders, water dispersible tablets, water dispersible powders, water dispersible granules, water soluble tablets, water soluble powders and water soluble granules.
the formulation pertaining to the present invention comprises 5-60%, preferably 5-50%, more preferably 10-40% of cefetamet as the active agent or a pharmaceutically acceptable derivative thereof in an amount equivalent to that.
Cefetamet which is comprised in the water dispersible formulation pertaining to the present invention, can be in the form of its pharmaceutically acceptable hydrates, solvates, esters, enantiomers, polymorphs, crystal forms, amorphous forms, salts or in free base form and/or a combination thereof.
Cefetamet comprised in the water dispersible formulation pertaining to the present invention is in ester form. It is preferably cefetamet pivoxil.
Cefetamet pivoxil comprised in the water dispersible formulation pertaining to the present invention is preferably in salt form. It is preferably cefetamet pivoxil hydrochloride.
another aspect of the present invention is the water dispersible formulations comprising cefetamet pivoxil hydrochloride wherein d 50 value of the molecule cefetamet pivoxil hydrochloride is in the range of 10-50 ⁇ .
the water dispersible formulation pertaining to the present invention can comprise one or more of the excipients including binders, lubricants, disintegrants, diluents, flavoring agents, sweeteners, coloring agents, surfactants, anti-foam agent, stabilizing agents, viscosity agents in addition to the cefetamet.
excipients including binders, lubricants, disintegrants, diluents, flavoring agents, sweeteners, coloring agents, surfactants, anti-foam agent, stabilizing agents, viscosity agents in addition to the cefetamet.
the lubricant that is used in the pharmaceutical formulation of the present invention can be selected from, but not limited to, a group comprising talc, magnesium stearate, stearic acid, sodium stearil fumarate, polyoxyethylene glycol, leucine, alanine, glycine, sodium benzoate, sodium acetate, fumaric acid or a combination thereof.
the present invention relates to water dispersible dosage formulations comprising cefetamet wherein the amount of lubricant used is in the range of 1 - 8% by weight.
the ratio of cefetamet to lubricant is an important parameter on both dissolution and flowability of the formulations. It is observed that the desired flowability and solubility can be provided in the case that the ratio of cefetamet to lubricant is in the range of 20:1 to 1 :1, preferably 15:1 to 2:1, more preferably 10:1 to 5: 1 by weight.
the present invention relates to water dispersible dosage formulations comprising cefetamet wherein the ratio of cefetamet to lubricant is in the range of 20:1 to 1 : 1 by weight.
the effervescent acid that is optionally used in the water dispersible formulations pertaining to the present invention can be selected from, but not limited to, a group comprising acetic acid, citric acid, lactic acid, malic acid, phosphoric acid, propionic acid, tartaric acid or a combination thereof.
the effervescent base that is optionally used in the water dispersible formulations pertaining to the present invention can be selected from, but not limited to, a group comprising potassium carbonate, potassium bicarbonate, potassium citrate, potassium hydroxide, sodium carbonate, sodium hydrogen carbonate, sodium hydrogen citrate or a combination thereof.
the binder that is used in the pharmaceutical formulation of the present invention can be selected from, but not limited to, a group comprising starches such as potato starch, corn starch, wheat starch; sugars such as sucrose, glucose, dextrose, lactose, maltodextrin; natural and synthetic gums; gelatin; cellulose derivatives such as microcrystalline cellulose, HPC, HEC, HPMC, carboxymethyl cellulose, methyl cellulose, ethyl cellulose; polyvinylpyrrolidone (povidone), polyethylene glycol (PEG); waxes; calcium carbonate; calcium phosphate; alcohols such as sorbitol, xylitol, mannitol, and water or a combination thereof.
starches such as potato starch, corn starch, wheat starch
sugars such as sucrose, glucose, dextrose, lactose, maltodextrin
natural and synthetic gums such as cellulose derivatives such as microcrystalline cellulose, HPC, H
the disintegrant that is used in the pharmaceutical formulation of the present invention can be selected from, but not limited to, a group comprising starches such as potato starch, corn starch, wheat starch, pregelatinized starch, sodium starch glycolate; cellulose derivatives such as croscarmellose sodium or microcrystalline cellulose; polyvinylpyrrolidone; crospovidone; alginic acid and its salts; clays such as xanthan gum or Veegum; ion exchange resins or a combination thereof.
starches such as potato starch, corn starch, wheat starch, pregelatinized starch, sodium starch glycolate
cellulose derivatives such as croscarmellose sodium or microcrystalline cellulose
polyvinylpyrrolidone such as crospovidone
alginic acid and its salts such as xanthan gum or Veegum
ion exchange resins or a combination thereof such as xanthan gum or Veegum
the diluent that is used in the pharmaceutical formulation of the present invention can be selected from, but not limited to, a group lactose, maltose, dextrin, maltodextrin, mannitol, sorbitol, starch or a combination thereof.
the flavoring agent that is used in the pharmaceutical formulation of the present invention can be selected from, but not limited to, a group comprising natural aroma oils (peppermint oil, wintergreen oil, clove bud oil, parsley oil, eucalyptus oil, lemon oil, orange oil), menthol, eucalyptol, cinnamon, 1 -methyl acetate, sage, eugenol, oxanone, lemon, orange, blackberry, propenyl guaetol acetyl, cinnamon, vanilla, thymol, linalool or a combination thereof.
natural aroma oils peppermint oil, wintergreen oil, clove bud oil, parsley oil, eucalyptus oil, lemon oil, orange oil
menthol eucalyptol
cinnamon 1 -methyl acetate
sage eugenol
oxanone lemon, orange
blackberry propenyl guaetol acetyl
cinnamon vanilla
the sweetener that is used in the pharmaceutical formulation of the present invention can be selected from, but not limited to, a group comprising sucralose, sucrose, fructose, glucose, galactose, xylose, dextrose, laevulose, lactose, maltose, maltodextrin, mannitol, maltitol, maltol, sorbitol, xylitol, erythritol, lactitol, isomalt, corn syrup, saccharine, saccharine salts, acesulfame potassium, aspartame, D-tryptophane, monoammonium glycyrrhizinate, neohesperidin dihydrochalcone, thaumatin, neotame, alitame, stevioside and cyclamates or a combination thereof.
the viscosity agent that is used in the pharmaceutical formulation of the present invention can be selected from, but not limited to, a group comprising carboxymethyl cellulose, methyl cellulose, xanthan gum, gummi tragacanthae, gum arabic, aerosil 200, collidone, agar-agar, bentonite, hydroxyethyl cellulose or a combination thereof.
the formulation in water dispersible form pertaining to the present invention comprises; cefetamet in the range of 5-60% by weight
disintegrant in the range of 0- 10% by weight
binder in the range of 0-20% by weight.
the pharmaceutical composition of the present invention can be prepared through a process which is comprised of dry blending or dry granulation or wet granulation of the components or a combination thereof and generally known standard techniques and manufacture procedures in technology.
the present invention relates to the use of water dispersible dosage forms comprising cefetamet or its any pharmaceutically acceptable derivative in the treatment of the infections caused by gram negative and gram positive bacteria.
the present invention relates to the use of the pharmaceutical compositions in water dispersible dosage forms comprising cefetamet or any pharmaceutically acceptable derivative thereof in the manufacture of a medicament so as to be used in upper respiratory infections such as ear, nose, throat, otitis media, sinusitis, tonsillitis, pharyngitis; lower respiratory tract infections such as pyelonephritis, cystitis and urethritis; skin or soft tissue infections such as froncle, pyoderma, impetigo in the treatment and prophylaxis of gonorrhea and lyme diseases.
upper respiratory infections such as ear, nose, throat, otitis media, sinusitis, tonsillitis, pharyngitis
lower respiratory tract infections such as pyelonephritis, cystitis and urethritis
skin or soft tissue infections such as froncle, pyoderma, impetigo in the treatment and prophylaxis of gonorrhea and lyme diseases
Example 1 Formulation and process for the preparation of effervescent powder, granules or tablets
the process in scope of the present invention comprises granulating a mixture comprising effervescent couple and sweetener with the granulation solution comprising binder and a solvent through conventional wet and/or dry granulation methods, then sieving the mixture; adding cefetamet pivoxil hydrochloride, lubricant and other excipients into the obtained granules, and optionally compressing the obtained mixture in tablet compressing machine.
Example 2 Formulation and process for the preparation of water dispersible powder, granules or tablets
the process in scope of the present invention comprises granulating a mixture comprising cefetamet and binder and the other excipients with the granulation solution comprising the diluent through conventional wet and/or dry granulation methods, then sieving the mixture; adding sweetener and the lubricant into the obtained granules, and optionally compressing the obtained mixture in tablet compressing machine.

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Health & Medical Sciences (AREA)
Epidemiology (AREA)
Animal Behavior & Ethology (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
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Public Health (AREA)
General Health & Medical Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Medicinal Preparation (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Cephalosporin Compounds (AREA)

EP11724475A 2010-05-04 2011-05-02 Pharmazeutische zusammensetzungen mit cefetamet Withdrawn EP2566450A2 (de)

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PCT/TR2011/000133 WO2011139255A2 (en)	2010-05-04	2011-05-02	Pharmaceutical compositions comprising cefetamet

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