TW200400197A - Pharmaceutical compositions of azithromycin - Google Patents

Pharmaceutical compositions of azithromycin Download PDF

Info

Publication number: TW200400197A
Authority: TW; Taiwan
Prior art keywords: azithromycin; pharmaceutical composition; grams; monohydrate; patent application
Prior art date: 2002-06-20

Application number

TW092116536A

Other languages

English (en)

Chinese (zh)

Inventor

Franz Xaver Schwarz

Johannes Raneburger

Original Assignee

Sandoz Ag

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.)

2002-06-20

Filing date

2003-06-18

Publication date

2004-01-01

2003-06-18 Application filed by Sandoz Ag filed Critical Sandoz Ag

2004-01-01 Publication of TW200400197A publication Critical patent/TW200400197A/zh

Links

229960004099 azithromycin Drugs 0.000 title claims abstract description 24
MQTOSJVFKKJCRP-BICOPXKESA-N azithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 MQTOSJVFKKJCRP-BICOPXKESA-N 0.000 title claims abstract description 23
239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 13
150000004682 monohydrates Chemical class 0.000 claims abstract description 14
239000000945 filler Substances 0.000 claims abstract description 8
239000003765 sweetening agent Substances 0.000 claims abstract description 8
239000002562 thickening agent Substances 0.000 claims abstract description 8
239000000796 flavoring agent Substances 0.000 claims abstract description 7
235000003599 food sweetener Nutrition 0.000 claims abstract description 6
239000000725 suspension Substances 0.000 claims description 11
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 8
239000007788 liquid Substances 0.000 claims description 8
235000019634 flavors Nutrition 0.000 claims description 6
239000008187 granular material Substances 0.000 claims description 5
239000000843 powder Substances 0.000 claims description 5
229920001285 xanthan gum Polymers 0.000 claims description 5
239000000839 emulsion Substances 0.000 claims description 4
235000013599 spices Nutrition 0.000 claims description 4
239000000230 xanthan gum Substances 0.000 claims description 4
235000010493 xanthan gum Nutrition 0.000 claims description 4
229940082509 xanthan gum Drugs 0.000 claims description 4
108010011485 Aspartame Proteins 0.000 claims description 3
229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 3
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 3
229930006000 Sucrose Natural products 0.000 claims description 3
239000000605 aspartame Substances 0.000 claims description 3
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 3
229960003438 aspartame Drugs 0.000 claims description 3
235000010357 aspartame Nutrition 0.000 claims description 3
239000001863 hydroxypropyl cellulose Substances 0.000 claims description 3
235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 3
238000002156 mixing Methods 0.000 claims description 3
239000001488 sodium phosphate Substances 0.000 claims description 3
239000000126 substance Substances 0.000 claims description 3
239000005720 sucrose Substances 0.000 claims description 3
RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims description 3
229910000406 trisodium phosphate Inorganic materials 0.000 claims description 3
235000019801 trisodium phosphate Nutrition 0.000 claims description 3
239000002552 dosage form Substances 0.000 claims description 2
239000006172 buffering agent Substances 0.000 claims 2
HQUPLSLYZHKKQT-WVVFQGGUSA-N (2r,3s,4r,5r,8r,10r,11r,12s,13s,14r)-11-[(2s,3r,4s,6r)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-3,4,10-trihydroxy-13-[(2r,4r,5s,6s)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-o Chemical compound O.O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 HQUPLSLYZHKKQT-WVVFQGGUSA-N 0.000 claims 1
GJCOSYZMQJWQCA-UHFFFAOYSA-N 9H-xanthene Chemical compound C1=CC=C2CC3=CC=CC=C3OC2=C1 GJCOSYZMQJWQCA-UHFFFAOYSA-N 0.000 claims 1
CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
235000003704 aspartic acid Nutrition 0.000 claims 1
229960003256 azithromycin monohydrate Drugs 0.000 claims 1
OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 1
239000002775 capsule Substances 0.000 claims 1
239000001913 cellulose Substances 0.000 claims 1
229920002678 cellulose Polymers 0.000 claims 1
230000000694 effects Effects 0.000 claims 1
239000008203 oral pharmaceutical composition Substances 0.000 claims 1
239000002304 perfume Substances 0.000 claims 1
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
229960004793 sucrose Drugs 0.000 claims 1
239000004480 active ingredient Substances 0.000 abstract description 2
235000000346 sugar Nutrition 0.000 description 7
239000008122 artificial sweetener Substances 0.000 description 6
235000021311 artificial sweeteners Nutrition 0.000 description 6
244000018633 Prunus armeniaca Species 0.000 description 5
235000009827 Prunus armeniaca Nutrition 0.000 description 5
244000290333 Vanilla fragrans Species 0.000 description 5
235000009499 Vanilla fragrans Nutrition 0.000 description 5
235000012036 Vanilla tahitensis Nutrition 0.000 description 5
150000004683 dihydrates Chemical class 0.000 description 4
239000000203 mixture Substances 0.000 description 4
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
-1 Klucel LF® Polymers 0.000 description 3
238000002441 X-ray diffraction Methods 0.000 description 3
150000008163 sugars Chemical class 0.000 description 3
235000015149 toffees Nutrition 0.000 description 3
244000099147 Ananas comosus Species 0.000 description 2
235000007119 Ananas comosus Nutrition 0.000 description 2
229920003091 Methocel™ Polymers 0.000 description 2
235000011034 Rubus glaucus Nutrition 0.000 description 2
244000235659 Rubus idaeus Species 0.000 description 2
235000009122 Rubus idaeus Nutrition 0.000 description 2
239000001768 carboxy methyl cellulose Substances 0.000 description 2
238000001035 drying Methods 0.000 description 2
235000013399 edible fruits Nutrition 0.000 description 2
239000003205 fragrance Substances 0.000 description 2
238000005259 measurement Methods 0.000 description 2
229920000609 methyl cellulose Polymers 0.000 description 2
239000001923 methylcellulose Substances 0.000 description 2
229940100692 oral suspension Drugs 0.000 description 2
239000000377 silicon dioxide Substances 0.000 description 2
235000012239 silicon dioxide Nutrition 0.000 description 2
MIDXCONKKJTLDX-UHFFFAOYSA-N 3,5-dimethylcyclopentane-1,2-dione Chemical compound CC1CC(C)C(=O)C1=O MIDXCONKKJTLDX-UHFFFAOYSA-N 0.000 description 1
229910002012 Aerosil® Inorganic materials 0.000 description 1
244000144730 Amygdalus persica Species 0.000 description 1
229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 1
244000307700 Fragaria vesca Species 0.000 description 1
235000016623 Fragaria vesca Nutrition 0.000 description 1
235000011363 Fragaria x ananassa Nutrition 0.000 description 1
235000006040 Prunus persica var persica Nutrition 0.000 description 1
240000001890 Ribes hudsonianum Species 0.000 description 1
235000016954 Ribes hudsonianum Nutrition 0.000 description 1
235000001466 Ribes nigrum Nutrition 0.000 description 1
DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
239000003242 anti bacterial agent Substances 0.000 description 1
SRMPHJKQVUDLQE-KUJJYQHYSA-N azithromycin dihydrate Chemical compound O.O.O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 SRMPHJKQVUDLQE-KUJJYQHYSA-N 0.000 description 1
239000012928 buffer substance Substances 0.000 description 1
235000013736 caramel Nutrition 0.000 description 1
235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
239000008112 carboxymethyl-cellulose Substances 0.000 description 1
229910052681 coesite Inorganic materials 0.000 description 1
150000001875 compounds Chemical class 0.000 description 1
229910052802 copper Inorganic materials 0.000 description 1
239000010949 copper Substances 0.000 description 1
239000006071 cream Substances 0.000 description 1
229910052906 cristobalite Inorganic materials 0.000 description 1
238000007429 general method Methods 0.000 description 1
239000008240 homogeneous mixture Substances 0.000 description 1
239000004615 ingredient Substances 0.000 description 1
150000002894 organic compounds Chemical class 0.000 description 1
229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
238000002360 preparation method Methods 0.000 description 1
XTUSEBKMEQERQV-UHFFFAOYSA-N propan-2-ol;hydrate Chemical compound O.CC(C)O XTUSEBKMEQERQV-UHFFFAOYSA-N 0.000 description 1
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
230000006641 stabilisation Effects 0.000 description 1
238000011105 stabilization Methods 0.000 description 1
229910052682 stishovite Inorganic materials 0.000 description 1
235000020357 syrup Nutrition 0.000 description 1
239000006188 syrup Substances 0.000 description 1
229910052905 tridymite Inorganic materials 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
- 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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Public Health (AREA)
Organic Chemistry (AREA)
Epidemiology (AREA)
Molecular Biology (AREA)
Biotechnology (AREA)
Biochemistry (AREA)
Genetics & Genomics (AREA)
Engineering & Computer Science (AREA)
Communicable Diseases (AREA)
Oncology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Medicinal Preparation (AREA)

TW092116536A 2002-06-20 2003-06-18 Pharmaceutical compositions of azithromycin TW200400197A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GBGB0214277.6A GB0214277D0 (en)	2002-06-20	2002-06-20	Organic compounds

Publications (1)

Publication Number	Publication Date
TW200400197A true TW200400197A (en)	2004-01-01

Family

ID=9938996

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
TW092116536A TW200400197A (en)	2002-06-20	2003-06-18	Pharmaceutical compositions of azithromycin

Country Status (4)

Country	Link
AU (1)	AU2003279392A1 (fr)
GB (1)	GB0214277D0 (fr)
TW (1)	TW200400197A (fr)
WO (1)	WO2004000865A1 (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB0224197D0 (en) *	2002-10-17	2002-11-27	Biochemie Gmbh	Organic compounds
US20070185194A1 (en) *	2003-07-01	2007-08-09	Kamal Mehta	Stable oral compositions of azithromycin monohydrate
US20050013835A1 (en) *	2003-07-15	2005-01-20	Pfizer Inc.	Stable non-dihydrate azithromycin oral suspensions
BRPI0417348A (pt)	2003-12-04	2007-03-13	Pfizer Prod Inc	processo de gelatinização por spray com utilização de uma extrusora para preparação de composições de droga cristalina multiparticulada contendo preferencialmente um poloxámero e um glicerìdeo
US6984403B2 (en)	2003-12-04	2006-01-10	Pfizer Inc.	Azithromycin dosage forms with reduced side effects
US7468428B2 (en)	2004-03-17	2008-12-23	App Pharmaceuticals, Llc	Lyophilized azithromycin formulation
WO2006067577A2 (fr) *	2004-12-21	2006-06-29	Pfizer Products Inc.	Suspension orales stables d'azithromycine sous forme non dihydrate
US8106111B2 (en)	2009-05-15	2012-01-31	Eastman Chemical Company	Antimicrobial effect of cycloaliphatic diol antimicrobial agents in coating compositions

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
HRP20010956B1 (hr) *	1999-06-29	2010-09-30	Biochemie S.A.	Makrolidi
RU2188018C2 (ru) *	2000-06-20	2002-08-27	Нестерук Владимир Викторович	Композиционный состав антибактериального лекарственного средства
ES2172417B1 (es) *	2000-07-31	2003-09-16	Sint Quimica Sa	Nueva forma mejorada de azitromicina monohidrato de menor higroscopicidad, procedimiento de preparacion y composiciones farmaceuticas que la comprenden.
HRP20030430B1 (hr) *	2000-11-27	2011-11-30	Biochemie S.A.	Makrolidni solvati

2002
- 2002-06-20 GB GBGB0214277.6A patent/GB0214277D0/en not_active Ceased
2003
- 2003-06-18 TW TW092116536A patent/TW200400197A/zh unknown
- 2003-06-18 WO PCT/EP2003/006489 patent/WO2004000865A1/fr not_active Ceased
- 2003-06-18 AU AU2003279392A patent/AU2003279392A1/en not_active Abandoned

Also Published As

Publication number	Publication date
AU2003279392A1 (en)	2004-01-06
GB0214277D0 (en)	2002-07-31
WO2004000865A1 (fr)	2003-12-31

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