EP0778775B1
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EP
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Cosolvent parenteral formulation of tirilazad
Assignee: Pharmacia and Upjohn Co
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Filing: 1995-08-29
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Granted: 1999-01-20
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Expires: 2015-08-29
Abstract
Abstract PCT No. PCT/US95/10730 Sec. 371 Date Jan. 4, 1997 Sec. 102(e) Date Jan. 4, 1997 PCT Filed Aug. 29, 1995 PCT Pub. No. WO96/06618 PCT Pub. Date Mar. 7, 1996The invention is a cosolvent parenteral pharmaceutical formulation of a lazaroid and its pharmaceutically acceptable salts.
Inventors
- 👤 Ching-Chiang Su
- 👤 David S. Baker
- 👤 Susan M. Machkovech
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-01 05:37
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K31/00; A61K31/56; A61K31/58; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12; A61P; A61P25/00; A61P25/28
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
60 words
A sterile aqueous pharmaceutical composition for
parenteral administration, which comprises: (1) 0.9 to 90 mg/ml of a lazaroid or a
pharmaceutically-acceptable salt thereof, (2) 0.002 to 2.0 M citrate, (3) up to 80% of a cosolvent selected from
propylene glycol, polyethylene glycol, glycerol, ethanol,
DMSO, DMAC, dimethyl isosorbide and M-PYROL, and (4) water at a pH of 2.4 to 3.5.
Claim 2
Dependent Claim
18 words
A composition according to claim 1, where the lazaroid
is selected from tirilazad, 5α-tirilazad, 5β-tirilazad,
6α-hydroxytirilazad and 6β-hydroxytirilazad.
Claim 3
Dependent Claim
11 words
A composition according to claim 2, where the lazaroid
is tirilazad.
Claim 4
Dependent Claim
36 words
A composition according to any preceding claim, where
the pharmaceutically-acceptable acid addition salt is
selected from hydrochloride, hydrobromide, hydroiodide,
sulfate, phosphate, acetate, lactate, citrate, succinate,
benzoate, salicylate, pamoate, cyclohexanesulfamate,
methanesulfonate, naphthalenesulfonate, p-toluenesulfonate,
maleate, fumarate and oxalate.
Claim 5
Dependent Claim
14 words
A composition according to claim 4, where the
pharmaceutically-acceptable acid addition salt is
methanesulfonate.
Claim 6
Dependent Claim
12 words
A composition according to claim 1, where the lazaroid
is tirilazad mesylate.
Claim 7
Dependent Claim
17 words
A composition according to any preceding claim, which
comprises from 20 to 40 mg/ml of the lazaroid.
Claim 8
Dependent Claim
15 words
A composition according to any preceding claim, which
comprises from 0.25 to 0.4 M citrate.
Claim 9
Dependent Claim
20 words
A composition according to any preceding claim, where
the cosolvent is selected from propylene glycol,
polyethylene glycol, glycerol and ethanol.
Claim 10
Dependent Claim
12 words
A composition according to claim 9, where the
cosolvent is propylene glycol.
Claim 11
Dependent Claim
16 words
A composition according to any preceding claim, which
comprises from 1 to 80% of the cosolvent.
Claim 12
Dependent Claim
15 words
A composition according to claim 11, which comprises
from 20 to 60% of the cosolvent.
Claim 13
Dependent Claim
15 words
A composition according to any preceding claim, where
the pH is from 2.7 to 3.1.
Claim 14
Dependent Claim
10 words
A composition according to any preceding claim, which
is isotonic.
Claim 15
Dependent Claim
22 words
A composition according to any preceding claim, where
the molar ratio of total citrate buffer to lazaroid is from
4.3:1 to 14.5:1.
Claim 16
Dependent Claim
34 words
A sterile aqueous pharmaceutical composition for
parenteral administration, which comprises: (1) 25 mg/ml of 21-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]-1-piperazinyl]-16α-methylpregna-1,4,9(11)-triene-3,20-dione mesylate, (2) 0.25 M citrate, (3) 40% propylene glycol, and (4) water at a pH of 2.7 to 3.1.
References Cited (Backward Citations)
No citation records indexed.
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