US2012035162A1PendingUtilityA1
Process for preparation of high-purity meloxicam and meloxicam potassium salt
Est. expiryNov 18, 2024(expired)· nominal 20-yr term from priority
Inventors:Tibor MezeiGyula SimigEniko MolnarGyula LukacsMarta Porcs-MakkayBalazs VolkValéria Hofmanné FeketeKalman NagyNorbert MesterházyGyorgy KrasznaiGyörgyi Vereczkeyné DonáthGyuláné KörtvélyessyÉva Pécsi
A61P 43/00A61P 29/00A61P 27/00C07D 417/12
35
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Claims
Abstract
The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium salt monohydrate is produced. Said salt is subsequently treated with mineral or organic acid to yield high-purity meloxicam.
Claims
exact text as granted — not AI-modified1 - 13 . (canceled)
14 . Meloxicam potassium salt monohydrate of the Formula (I)
15 . Meloxicam potassium salt monohydrate of the Formula (I)
essentially free of 4-hydroxy-2-methyl-N-alkyl-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide of the Formula (V)
wherein R is methyl, ethyl or isopropyl.
16 . A pharmaceutical composition comprising a therapeutically effective amount of meloxicam potassium salt monohydrate of the Formula (I)
according to claim 14 and one or more pharmaceutically acceptable vehicles or auxiliary agents.
17 . A process for the preparation of 99.8% pure meloxicam potassium salt monohydrate of the Formula (I)
as defined in claim 14 , which comprises the steps of:
(a) reacting crude meloxicam of the Formula (II)
which also contains water-insoluble impurities including the compound of the Formula (V)
wherein R is methyl, ethyl or isopropyl with potassium hydroxide or potassium carbonate dissolved in water or in the mixture of water and an organic solvent,
(b) separating pure meloxicam potassium salt monohydrate from the water-insoluble impurities of the Formula (V) and if desired,
(c) crystallizing the pure meloxicam potassium salt monohydrate of the Formula (I) thus formed.
18 . Meloxicam of the Formula (II)
free of water-insoluble impurities of the compound of the Formula (V)
wherein R is methyl, ethyl or isopropyl,
prepared according to a process which comprises the following steps:
(a) dissolving meloxicam potassium salt monohydrate of the Formula (I)
with the water-insoluble impurities of the Formula (V), in water or in a mixture of water and an organic solvent,
(b) removing from the meloxicam potassium salt monohydrate, the water-insoluble impurities of the compound of the Formula (V); and
(c) treating the resulting solution with an organic or inorganic acid, and crystallizing 99.8% pure meloxicam
19 . Meloxicam of the Formula (II)
free of water-insoluble impurities of the compound of the Formula (V)
wherein R is methyl, ethyl or isopropyl,
prepared according to a process which comprises the following steps:
(a) transforming meloxicam raw product into crystalline meloxicam potassium salt monohydrate of the Formula (I)
with the water-insoluble impurities of the compound of the Formula (v),
(b) dissolving said meloxicam potassium salt monohydrate of the Formula (I) with the water-insoluble impurities of the Formula (V) in water or in a mixture of water and an organic solvent,
(c) removing from the meloxicam potassium salt monohydrate, the water-insoluble impurities of the compound of the Formula (V), and
(d) treating the dissolved potassium salt of meloxicam with an organic or inorganic acid, followed by crystallization of 99.8% pure meloxicam of the Formula (II).
20 . Meloxicam of the Formula (II)
free of water-insoluble impurities of the compound of the Formula (V)
wherein R is methyl, ethyl or isopropyl,
prepared according to a process which comprises the following steps:
(a) reacting a compound of the Formula (III)
wherein R is methyl, ethyl or isopropyl with 2-amino-5-methyl-thiazole of the Formula (IV)
to form a meloxicam raw product of the Formula (II);
(b) transforming the resulting meloxicam of the Formula (II) into its potassium monohydrate salt along with the water-insoluble impurities of the compound of the Formula (V),
(c) separating the water-insoluble impurities of the compound of the Formula (V) from an aqueous or aqueous-organic solution of said meloxicam potassium salt to form a solution of 99.8% pure meloxicam; and
(d) treating said solution with an organic or inorganic acid and crystallizing 99.8% pure meloxicam.Cited by (0)
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