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SI20108B - A controlled release formulation for poorly soluble basic drugs - Google Patents

A controlled release formulation for poorly soluble basic drugs Download PDF

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Publication number
SI20108B
SI20108B SI9720096A SI9720096A SI20108B SI 20108 B SI20108 B SI 20108B SI 9720096 A SI9720096 A SI 9720096A SI 9720096 A SI9720096 A SI 9720096A SI 20108 B SI20108 B SI 20108B
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SI
Slovenia
Prior art keywords
composition
alginate
sodium
salt
water
Prior art date
Application number
SI9720096A
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Slovenian (sl)
Other versions
SI20108A (en
Inventor
Neville W Broad
Alan F Carmody
Liam C Feely
Brian C Withers
Original Assignee
Abbott Lab
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Publication date
Application filed by Abbott Lab filed Critical Abbott Lab
Publication of SI20108A publication Critical patent/SI20108A/en
Publication of SI20108B publication Critical patent/SI20108B/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biophysics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A controlled release, oral, solid, pharmaceutical composition for a reduced daily dosage regimen is described where the therapeutic ingredient is a poorly soluble basic drug. The formulation comprises the use of a water-soluble alginate salt, a complex salt of alginic acid and an organic carboxylic acid in admixture with the therapeutic drug. A particular embodiment comprising a once a day dosage form for clarithromycin is also described.

Claims (17)

1 Patentni zahtevki 1. Trden farmacevtski sestavek z nadzorovanim sproščanjem, prilagojen za oralno dajanje, ki obsega: terapevtsko učinkovito količino vsaj enega bazičnega zdravila, ki ima topnost v vodi manjšo od 1 dela na 30 delov vode; v vodi topno alginatno sol; kompleksno sol alginske kisline, kjer je kation, ki da netopno sol, izbran iz skupine, ki sestoji iz kalcija, stroncija, železa in barija; in organske karboksilne kisline, da olajšamo raztapljanje bazičnega zdravila, pri čemer masno razmerje v vodi topne soli proti kompleksni soli alginske kisline variira od 16:1 do 1:1 in molsko razmerje karboksilne kisline proti zdravilu variira od 0,2:1 do 5:1.1. A solid controlled release pharmaceutical composition adapted for oral administration comprising: a therapeutically effective amount of at least one basic drug having a solubility in water of less than 1 part per 30 parts of water; a water-soluble alginate salt; a complex salt of an alginic acid, wherein the cation is an insoluble salt selected from the group consisting of calcium, strontium, iron and barium; and organic carboxylic acids to facilitate the dissolution of the basic drug, wherein the weight ratio of the water soluble salt to the complex salt of the alginic acid varies from 16: 1 to 1: 1 and the carboxylic acid molar ratio of the drug varies from 0.2: 1 to 5: 1. 2. Sestavek po zahtevku 1 v obliki tablete.A composition according to claim 1 in the form of a tablet. 3. Sestavek po zahtevku 1 v obliki enkrat dnevnega dozirnega režima.The composition of claim 1 in the form of a single daily dosing regimen. 4. Sestavek po zahevku 1, kjer je bazično zdravilo makrolid.A composition according to Claim 1, wherein the basic drug is a macrolide. 5. Sestavek po zahtevku 4, kjer je makrolid klaritromicin.The composition of claim 4, wherein the macrolide is clarithromycin. 6. Sestavek po zahtevku 1, kjer je v vodi topna alginatna sol natrijev alginat.The composition of claim 1, wherein the water-soluble alginate salt is sodium alginate. 7. Sestavek po zahtevku 1, kjer je kompleksna sol alginske kisline natrijev-kalcijev alginat.The composition of claim 1, wherein the complex salt of alginic acid is sodium calcium alginate. 8. Sestavek po zahtevku 1, kjer je organska karboksilna kislina izbrana iz skupine, ki sestoji iz vinske, jabolčne, jantarne, glutame, glutamske, maleinske, mandljeve in citronske kisline. 2The composition of claim 1, wherein the organic carboxylic acid is selected from the group consisting of wine, malic, succinic, glutamate, glutamic, maleic, almond and citric acid. 2 9. Sestavek po zahtevku 8, kjer je organska karboksilna kislina citronska kislina.A composition according to claim 8, wherein the organic carboxylic acid is citric acid. 10. Sestavek po zahtevku 1, kjer je masno razmerje natrijevega alginata proti natrijevem-kalcijevem alginatu okoli 16:1 do 1:1.The composition of claim 1, wherein the weight ratio of sodium alginate to sodium calcium alginate is about 16: 1 to 1: 1. 11. Sestavek po zahtevku 1, kjer je masno razmeje natrijevega alginata proti natrijevem-kalcijevem alginatu okoli 8:1 do 2:1.The composition of claim 1, wherein the sodium alginate sodium alginate sodium alginate oil content is about 8: 1 to 2: 1. 12. Sestavek po zahtevku 1, kjer je molsko razmerje organske kisline proti bazičnemu zdravilu okoli 1:1.The composition of claim 1, wherein the molar ratio of the organic acid to the basic drug is about 1: 1. 13. Sestavek po zahtevku 1, kjer je bazično zdravilo izbrano iz skupine, ki sestoji iz sulfametoksazola, metronidazola, cimetidina, indapamida, atenolola in diazepama.The composition of claim 1, wherein the basic drug is selected from the group consisting of sulfamethoxazole, metronidazole, cimetidine, indapamide, atenolol and diazepam. 14. Sestavek po zahtevku 4, kjer je makrolid izbran iz skupine, ki sestoji iz eritromicina, diritromicina, azitromicina, roksitromicina in ABT-229.The composition of claim 4, wherein the macrolide is selected from the group consisting of erythromycin, dithromycin, azithromycin, roxithromycin, and ABT-229. 15. Trden farmacevtski sestavek z nadzorovanim sproščanjem, prilagojen za oralno dajanje enkrat dnevnega dozirnega režima, ki obsega okoli 500 mg klaritromicina; od okoli 75 do 400 mg natrijevega alginata; od okoli 10 do 400 mg natrijevega-kalcijevega alginata; in okoli 128 mg citronske kisline.15. A solid controlled release pharmaceutical composition adapted for oral administration of a single daily dosing regimen comprising about 500 mg of clarithromycin; from about 75 to 400 mg of sodium alginate; from about 10 to 400 mg of sodium calcium alginate; and about 128 mg of citric acid. 16. Sestavek po zahtevku 14, ki obsega od okoli 80 do 200 mg natrijevega alginata in od okoli 10 do 40 mg natrijevega-kalcijevega alginata.The composition of claim 14, comprising from about 80 to 200 mg of sodium alginate and from about 10 to 40 mg of sodium calcium alginate. 17. Sestavek po zahtevku 15, ki obsega okoli 120 mg natrijevega alginata in okoli 15 mg natrijevega-kalcijevega alginata.The composition of claim 15, comprising about 120 mg of sodium alginate and about 15 mg of sodium calcium alginate.
SI9720096A 1997-06-11 1997-06-11 A controlled release formulation for poorly soluble basic drugs SI20108B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1997/010705 WO1998056357A1 (en) 1995-12-19 1997-06-11 A controlled release formulation for poorly soluble basic drugs

Publications (2)

Publication Number Publication Date
SI20108A SI20108A (en) 2000-06-30
SI20108B true SI20108B (en) 2001-12-31

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SI9720096A SI20108B (en) 1997-06-11 1997-06-11 A controlled release formulation for poorly soluble basic drugs

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NO (1) NO310095B1 (en)
SI (1) SI20108B (en)
SK (1) SK282427B6 (en)
WO (1) WO1998056357A1 (en)

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WO2000066174A2 (en) * 1999-04-29 2000-11-09 Russinsky Limited Compounds
EP1118333A1 (en) * 2000-01-18 2001-07-25 Eurand International S.P.A. Compositions with enhanced oral bioavailability
CN100341886C (en) * 2000-11-27 2007-10-10 桑多斯股份公司 Macrolide solvates
EP1492504A2 (en) * 2002-04-03 2005-01-05 Ranbaxy Laboratories, Ltd. Taste masked compositions of erythromycin a and derivatives thereof
SI21300A (en) * 2002-10-08 2004-04-30 Krka, Tovarna Zdravil, D.D., Novo Mesto Pharmaceutical compositions with alginates
CN100336511C (en) * 2002-11-15 2007-09-12 江苏豪森药业股份有限公司 Release-controlled oral Roxithromycin formulation
EP1638529B1 (en) * 2003-06-16 2016-08-10 ANDRX Pharmaceuticals, LLC. Oral extended-release composition
US6984403B2 (en) 2003-12-04 2006-01-10 Pfizer Inc. Azithromycin dosage forms with reduced side effects
BRPI0417348A (en) 2003-12-04 2007-03-13 Pfizer Prod Inc spray gelatinization process using an extruder for preparing multiparticulate crystalline drug compositions preferably containing a poloxamer and a glyceride
US11304960B2 (en) 2009-01-08 2022-04-19 Chandrashekar Giliyar Steroidal compositions
US9358241B2 (en) 2010-11-30 2016-06-07 Lipocine Inc. High-strength testosterone undecanoate compositions
US9034858B2 (en) 2010-11-30 2015-05-19 Lipocine Inc. High-strength testosterone undecanoate compositions
US20180153904A1 (en) 2010-11-30 2018-06-07 Lipocine Inc. High-strength testosterone undecanoate compositions
US20120148675A1 (en) 2010-12-10 2012-06-14 Basawaraj Chickmath Testosterone undecanoate compositions
WO2016033549A2 (en) 2014-08-28 2016-03-03 Lipocine Inc. (17-ß)-3-OXOANDROST-4-EN-17-YL TRIDECANOATE COMPOSITIONS AND METHODS OF THEIR PREPARATION AND USE
WO2016033556A1 (en) 2014-08-28 2016-03-03 Lipocine Inc. BIOAVAILABLE SOLID STATE (17-β)-HYDROXY-4-ANDROSTEN-3-ONE ESTERS
US20160361322A1 (en) 2015-06-15 2016-12-15 Lipocine Inc. Composition and method for oral delivery of androgen prodrugs
EP3544614B1 (en) 2016-11-28 2025-12-31 Lipocine Inc. ORAL TESTOSTERONE UNDECANOATE THERAPY
JP2021531348A (en) 2018-07-20 2021-11-18 リポシン,インク. Liver disease

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JPS60163823A (en) * 1984-02-03 1985-08-26 Taisho Pharmaceut Co Ltd Orally administered formulation
EP0188040B1 (en) * 1985-01-11 1991-08-14 Abbott Laboratories Limited Slow release solid preparation
US5705190A (en) * 1995-12-19 1998-01-06 Abbott Laboratories Controlled release formulation for poorly soluble basic drugs

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Publication number Publication date
SK161299A3 (en) 2000-05-16
NO996161L (en) 1999-12-13
NO310095B1 (en) 2001-05-21
NO996161D0 (en) 1999-12-13
SI20108A (en) 2000-06-30
WO1998056357A1 (en) 1998-12-17
SK282427B6 (en) 2002-01-07

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Effective date: 20160404