WO2008053295A2 - Compositions pharmaceutiques d'acide benzoquinolizine-2-carboxylique - Google Patents

Compositions pharmaceutiques d'acide benzoquinolizine-2-carboxylique Download PDF

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Publication number
WO2008053295A2
WO2008053295A2 PCT/IB2007/003115 IB2007003115W WO2008053295A2 WO 2008053295 A2 WO2008053295 A2 WO 2008053295A2 IB 2007003115 W IB2007003115 W IB 2007003115W WO 2008053295 A2 WO2008053295 A2 WO 2008053295A2
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
formula
compound
composition
pharmaceutically acceptable
Prior art date
Application number
PCT/IB2007/003115
Other languages
English (en)
Other versions
WO2008053295A3 (fr
Inventor
Venkatesh Madhavacharya Joshi
Prashant Manohar Mandaogade
Girish Kumar Jain
Original Assignee
Wockhardt Research Centre
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.)
Filing date
Publication date
Application filed by Wockhardt Research Centre filed Critical Wockhardt Research Centre
Publication of WO2008053295A2 publication Critical patent/WO2008053295A2/fr
Publication of WO2008053295A3 publication Critical patent/WO2008053295A3/fr

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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines

Definitions

  • the present invention relates to pharmaceutical compositions of 8- ⁇ 4-[2(S)-Amino- propionyloxy] piperidine-l-yl ⁇ -9-fluoro-5 (S)-methyl- ⁇ , 7-dihydro-l-oxo-lH, 5H- benzo[i,j]quinolizine-2-carboxylic acid or pharmaceutically acceptable salts, esters or products thereof.
  • the invention also relates to processes for the preparation of such compositions.
  • 8- ⁇ 4-[2(S)-Amino-propionyloxy] piperidine-l-yl ⁇ -9-fluoro-5 (S)-methyl- ⁇ , 7-dihydro-l- oxo-lH, 5H-benzo[i,j]quinolizine-2-carboxylic acid of structural Formula I can be used to treat bacterial Gram-positive, Gram-negative and anaerobic infections; especially infections caused by resistant Gram-positive organism and Gram-negative organism, mycobacterial infections and emerging nosocomial pathogen infections.
  • the present invention addresses the pharmaceutical compositions of Compound of Formula I and the processes for preparation of such compositions.
  • a pharmaceutical composition comprising a compound of Formula I or pharmaceutically acceptable salts, esters or products thereof in a unit dosage form optionally, together with one or more pharmaceutically acceptable excipients, wherein the compound of Formula I comprises an amount of from about 40% w/w to about 95% w/w of the composition.
  • the one or more pharmaceutically acceptable excipients may include one or more of fillers, lubricants, disintegrants, and glidants.
  • the pharmaceutically acceptable salts include inorganic acid addition salts and organic acid addition salts.
  • Inorganic and organic acid addition salts may include but not limited to hydrochloride, hydrobromide, hydroiodide, sulfate, phosphate, acetate, lactate, mesylate, besylate, succinate, oxalate, and maleate.
  • a pharmaceutical composition comprising an amount of from about 40% w/w to about 95% w/w of the composition of a compound of Formula I or pharmaceutically acceptable salts, esters or products thereof in a unit dosage form optionally, together with one or more pharmaceutically acceptable excipients, wherein the compound of Fo ⁇ nula I is present as a mesylate salt.
  • a pharmaceutical composition comprising an amount of from about 40% w/w to about 95% w/w of the composition of a compound of Formula I or pharmaceutically acceptable salts, esters or products thereof in a unit dosage fo ⁇ n optionally, together with one or more pharmaceutically acceptable excipients, wherein the compound of Formula I is present as a hydrochloride salt.
  • the one or more pharmaceutically pharmaceutically acceptable excipients may include one or more of fillers, lubricants, disintegrants, and glidants.
  • the compound of Formula I or pharmaceutically acceptable salts, esters or products thereof can be present in an amount between about 200 mg and about 1500 mg w/w of the composition.
  • a pharmaceutical composition comprising the compound of Formula I or pharmaceutically acceptable salts, esters or products thereof, wherein the formulation exhibits a dissolution profile such that within 30 minutes more than 80% of the compound of Formula I or a pharmaceutically acceptable salts, esters or products thereof is released, wherein the release rate is measured in Apparatus 2 (USP, Dissolution, paddle, 50 rpm) using 900 ml of 0.1 N HCl at 37 degree C.
  • Embodiments of the pharmaceutical composition may include one or more of the following features.
  • the pharmaceutical composition may include one or more pharmaceutically acceptable excipients.
  • the pharmaceutically acceptable excipients may include one or more of fillers, lubricants, glidants, disintegrants, and the like.
  • composition for oral administration to mammals and refers to tablets, capsules, granules, beads, caplets, disc, pills, sachet, suspension, spheroids, minitablets, granules in a capsule, beads in a capsule, minitablets in a capsule, and the like.
  • the present inventors have noticed that by providing a high loading of the compound of Formula I in an amount of from about 40% w/w to about 95% w/w of the composition, the overall size of the finished dosage form can be reduced.
  • the pharmaceutical composition may be prepared by mixing the compound of Formula I with other pharmaceutically acceptable excipients to form a mixture.
  • the mixture may be granulated with other pharmaceutically acceptable excipients.
  • the granules may be dried, mixed with other pharmaceutically acceptable excipients and may be converted into a suitable dosage form.
  • compositions as described herein may include other pharmaceutically acceptable excipients in addition to the compound of Fo ⁇ nula I.
  • examples of other pharmaceutically acceptable excipients as used herein include binders, fillers, lubricants, disintegrants, glidants, and the like.
  • binders include one or more of povidone, starch, stearic acid, gums, celluloses, and the like.
  • fillers include microcrystalline cellulose, lactose, mannitol, calcium phosphate, calcium sulfate, kaolin, dry starch, powdered sugar, and the like.
  • lubricants include magnesium stearate, zinc stearate, calcium stearate, stearic acid, sodium stearyl fumarate, and the like.
  • glidants examples include colloidal silicon dioxide, talc or com starch, and the like.
  • disintegrants include one or more of starches, croscarmellose sodium, crospovidone, sodium starch glycolate, and the like.
  • the pharmaceutical compositions of the present invention may be in the form of tablets, capsules, granules, beads, caplets, disc, pills, sachet, suspension, spheroids, minitablets, granules in a capsule, beads in a capsule, minitablets in a capsule, and the like.
  • the tablets may optionally be coated with film forming agents and/or pharmaceutically acceptable excipients.
  • film forming agents and/or pharmaceutically acceptable excipients.
  • Particularly suitable for use are commercially available coating compositions comprising film-forming polymers marketed under various trade names, such as Opadry ® and Eudragit ® .
  • the coating layers over the tablet may be applied as solution/dispersion of coating ingredients using conventional techniques known in the art.
  • Table 1 provides the composition of batches of the present invention.
  • Table 2 provides the dissolution data for the compound of formula I or pharmaceutically acceptable salts, esters or products thereof tablets prepared as per the formula given in Table 1.
  • USP Type 2 Apparatus rpm 50
  • 0.1 N hydrochloric acid 900 ml

Abstract

La présente invention concerne des compositions pharmaceutiques d'acide 8-{4-[2(S)-amino-propionyloxy] pipéridine-1-yl}-9-fluoro-5 (S)-méthyl-6, 7-dihydro-1-oxo-1H, 5H- benzo[i,j]quinolizine-2-carboxylique (Composé de Formule I) ou des sels esters ou produits de celui-ci, pharmaceutiquement acceptables. L'invention concerne également des procédés destinés à la préparation de telles compositions.
PCT/IB2007/003115 2006-10-30 2007-10-18 Compositions pharmaceutiques d'acide benzoquinolizine-2-carboxylique WO2008053295A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1782/MUM/2006 2006-10-30
IN1782MU2006 2006-10-30

Publications (2)

Publication Number Publication Date
WO2008053295A2 true WO2008053295A2 (fr) 2008-05-08
WO2008053295A3 WO2008053295A3 (fr) 2009-04-23

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2007/003115 WO2008053295A2 (fr) 2006-10-30 2007-10-18 Compositions pharmaceutiques d'acide benzoquinolizine-2-carboxylique

Country Status (1)

Country Link
WO (1) WO2008053295A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102470109A (zh) * 2009-07-02 2012-05-23 惠氏有限责任公司 3-氰基喹啉片剂制剂及其应用
WO2016181276A1 (fr) * 2015-05-08 2016-11-17 Wockhardt Limited Compositions pharmaceutiques stables comprenant un agent antibactérien
WO2020021575A1 (fr) * 2018-07-27 2020-01-30 Wockhardt Limited Compositions pharmaceutiques et procédés

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000068229A2 (fr) * 1999-05-07 2000-11-16 Wockhardt Limited Acides carboxyliques de benzoquinolizine antibacteriens optiquement purs, procedes, compositions et procedes de traitement

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000068229A2 (fr) * 1999-05-07 2000-11-16 Wockhardt Limited Acides carboxyliques de benzoquinolizine antibacteriens optiquement purs, procedes, compositions et procedes de traitement

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102470109A (zh) * 2009-07-02 2012-05-23 惠氏有限责任公司 3-氰基喹啉片剂制剂及其应用
WO2016181276A1 (fr) * 2015-05-08 2016-11-17 Wockhardt Limited Compositions pharmaceutiques stables comprenant un agent antibactérien
CN107580493A (zh) * 2015-05-08 2018-01-12 沃克哈特有限公司 包含抗细菌剂的稳定的药物组合物
JP2018510197A (ja) * 2015-05-08 2018-04-12 ウォックハート リミテッド 抗菌物質を含む安定な医薬組成物
WO2020021575A1 (fr) * 2018-07-27 2020-01-30 Wockhardt Limited Compositions pharmaceutiques et procédés

Also Published As

Publication number Publication date
WO2008053295A3 (fr) 2009-04-23

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