WO2017078647A1 - Pharmaceutical compositions of imatinib - Google Patents
Pharmaceutical compositions of imatinib Download PDFInfo
- Publication number
- WO2017078647A1 WO2017078647A1 PCT/TR2016/050424 TR2016050424W WO2017078647A1 WO 2017078647 A1 WO2017078647 A1 WO 2017078647A1 TR 2016050424 W TR2016050424 W TR 2016050424W WO 2017078647 A1 WO2017078647 A1 WO 2017078647A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- imatinib
- amount
- composition
- pharmaceutically acceptable
- pharmaceutical composition
- Prior art date
Links
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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Definitions
- the present invention relates to compositions comprising imatinib or a pharmaceutically acceptable salt thereof, characterized in that imatinib is present in an amount of about 24.5 – 29% of the total composition and the corresponding imatinib mesylate is present in an amount of about 29. 5- 34% of the total composition.
- Imatinib mesylate is chemically 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methy-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate.
- Imatinib is a protein-tyrosine kinase inhibitor and used to treat chronic mylogenous leukemia, gastrointestinal stromal tumors and other type of cancers.
- Imatinib inhibits the bcr-abl tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic mylogenous leukemia. Imatinib inhibits proliferation and induces apoptosis in bcr-abl positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia.
- imatinib mesylate also shows polymorphism that are reported in the following international patent application Nos. WO 99/03854, WO 2005/077933, WO 2005/095379, WO 2004/106326, WO 2006/054314, WO 2006/024863, WO 2006/ 048890, US 2006/0030568, WO 07/023182, WO 2007/136510 and US Pat. No 6894051.
- PCT application WO 01/47507 tells a pharmaceutical tablet composition containing about 22% w/w imatinib mesylate.
- PCT application IN 2010/000202 describes a film coated tablet comprising imatinib or pharmaceutically acceptable salts thereof in an amount of more than 80% based on the total weight of the coated tablet.
- PCT application WO 03/090720 describes a tablet formulation containing 30-80% w/w imatinib based on the total weight of the composition. These tablets were prepared by using wet granulation and described as being high loaded small size tablets which are easy to swallow. Because of high drug loaded composition the tablets shows high friability and limited flexibility.
- the present invention relates to compositions comprising imatinib or a pharmaceutically acceptable salt thereof characterized in that imatinib is present in an amount of from about 24.5 – 29% in weight based on the total composition and the corresponding imatinib mesylate is present in an amount of about 29.5 – 34% of the total composition.
- the present invention relates to compositions comprising imatinib or a pharmaceutically acceptable salt thereof characterized in that imatinib is present in an amount of from about 24.5 – 29% e.g. at least 24.5, 25, 26, 27, 28 or 29% and the corresponding imatinib mesylate is present in an amount of about 29.5 – 34%, e.g. at least 29.5, 30, 31, 32, 33 or 34% in weight based on the total composition.
- the present invention provides a composition comprising
- the amount of imatinib, calculated as the percentage of the content in weight based on the total weight of tablet is from about 24.5 – 29% e.g. at least about 24, 5, 25, 26, 27, 28 or 29% and the corresponding imatinib mesylate is from about 29.5 – 34%, e.g. at least about 29.5, 30, 31, 32, 33 or 34% in weight based on the total weight of the tablets.
- compositions according to the present invention comprises imatinib or a pharmaceutically acceptable salt of imatinib as the active ingredient, preferably the pharmaceutically acceptable salt of imatinib is imatinib mesylate.
- compositions according to the present invention comprises one or more pharmaceutically acceptable excipients e.g. at least one pharmaceutically acceptable binder, at least one pharmaceutically acceptable disintegrant, at least one pharmaceutically acceptable glidant and at least one pharmaceutically acceptable lubricant.
- pharmaceutically acceptable excipients e.g. at least one pharmaceutically acceptable binder, at least one pharmaceutically acceptable disintegrant, at least one pharmaceutically acceptable glidant and at least one pharmaceutically acceptable lubricant.
- Present invention discloses pharmaceutical compositions, preferably tablets, comprising imatinib or imatinib mesylate salt and at least one pharmaceutically acceptable excipient.
- compositions according to the present invention comprising imatinib or imatinib mesylate salt are preferably in tablet form, more preferably in film coated tablet form.
- the film coated tablet compositions comprising imatinib or imatinib mesylate according to the present invention can be prepared by a process of compressing the mixture of an inner phase and an outer phase and optionally coating the tablets.
- the pharmaceutically acceptable binders can be selected but not limited from the group consisting of microcrystalline cellulose, hydropropyl cellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose, hypromellose and polyvinylpyrrolidone.
- compositions comprising imatinib or imatinib mesylate prepared by the wet granulation process according to the present invention comprises a binder in a range of from 1 – 60%, preferably in a range of from 10 – 60% of the total composition.
- compositions comprising imatinib or imatinib mesylate prepared by the wet granulation process according to the present invention comprising of an inner phase and and outer phase wherein the inner phase comprises a binder in a range of from about 1 – 30% of the total composition while the outer phase comprises a binder in a range of from about 1 – 15% of the total composition.
- the pharmaceutically acceptable disintegrants can be selected but not limited from the group consisting of maize starch, CMC-Ca, CMC-Na, microcrystalline cellulose, cross-linked polyvinyl pyrolidone (crospovidone), alginic acid, sodium alginate and quar gum.
- the disintegrant used in the invention is in a range of from 4 – 30%, preferably in a range of form 10 – 30% of the total composition.
- the pharmaceutically acceptable glidants can be selected but not limited from the group consisting of silica, colloidal silicon dioxide, magnesium trisilicat, powdered cellulose, starch, talc and mixture thereof.
- the glidant used in the invention is in a range of from 0.2 – 5% of the total composition.
- the pharmaceutically acceptable lubricants can be selected but not limited from the group consisting of magnesium stearate, aluminum stearate, calcium stearate, PEG 4000, PEG 8000 and talc.
- the lubricant used in the invention is in a range of from 0.1 – 4% of the total composition.
- compositions according to the present invention comprises one or more pharmaceutically acceptable excipient, e.g. at least one pharmaceutically acceptable binder in a range of 1 – 60%, at least one pharmaceutically acceptable disintegrant in a range of 4 – 30% of the total composition, at least one pharmaceutically acceptable glidant in a range of 0.2 – 5% of the total composition and at least one pharmaceutically acceptable lubricant in a range of 0.1 – 4% of the total composition.
- pharmaceutically acceptable excipient e.g. at least one pharmaceutically acceptable binder in a range of 1 – 60%
- at least one pharmaceutically acceptable disintegrant in a range of 4 – 30% of the total composition
- at least one pharmaceutically acceptable glidant in a range of 0.2 – 5% of the total composition
- at least one pharmaceutically acceptable lubricant in a range of 0.1 – 4% of the total composition.
- the pharmaceutical composition of the invention comprises a dosage containing from about 50 mg to 500 mg, preferably from about 100 mg to 400 mg imatinib or a pharmaceutically acceptable salt thereof.
- the present invention also provides a process for preparing pharmaceutical composition, comprising imatinib in an amount of about 24.5 – 29% of total composition and corresponding imatinib mesylate in an amount of about 29.5 – 34% of the total composition.
- the tablet compositions comprising imatinib or imatinib mesylate salt according to the present invention may be prepared by direct compression, wet granulation or roll compaction.
- the film coated tablet compositions comprising imatinib or imatinib mesylate salt according to the present invention is prepared preferably by wet granulation.
- the wet granulation process of the film coated tablet compositions comprising imatinib or imatinib mesylate according to the present invention may be carried out using the solvent selected from water, ethyl alcohol, isopropyl alcohol and mixture thereof, preferably the solvent is ethyl alcohol.
- the tablet compositions comprising imatinib or imatinib mesylate prepared by the wet granulation process according to the present invention may be carried out by a process comprising the steps of;
- compositions comprising imatinib or imatinib mesylate salt according to the present invention may be carried out by a process comprising the steps of;
- imatinib or imatinib mesylate salt with one or more pharmaceutically acceptable binder, e.g. microcrystalline cellulose in a mixer,
- step (b) the mixture obtained from step (a) is wet granulated with a solvent selected from water, alcohol or mixture thereof,
- one or more pharmaceutically acceptable disintegrants e.g. crospovidone
- one or more pharmaceutically acceptable binders e.g. microcrystalline cellulose
- one or more pharmaceutically acceptable glidants e.g. colloidal silicon dioxide
- step (e) tableting the mixture obtained in step (e) by direct compression
- compositions comprising imatinib or imatinib mesylate salt according to the present invention may be carried out by a process comprising the steps of;
- imatinib or imatinib mesylate salt with one or more pharmaceutically acceptable binder, e.g. microcrystalline cellulose in an amount in the range of 1 – 30% in a mixer,
- step (b) the mixture obtained from step (a) is wet granulated with a solvent selected from water, alcohol or mixture thereof,
- one or more pharmaceutically acceptable binder e.g. microcrystalline cellulose in an amount in the range of 1 – 15% and/or one or more pharmaceutically acceptable disintegrant, e.g. crospovidone in an amount in the range of 4 – 30% and/or one or more pharmaceutically acceptable glidant, e.g. colloidal silicon dioxide in an amount in the range of 0.2 – 5% is mixed with the inner phase comprising imatinib or imatinib mesylate salt obtained from step (c) and the outer phase is obtained,
- step (e) tableting the mixture obtained in step (e) by compression
- the mixture of imatinib mesylate corresponding to 100 mg of imatinib as the active ingredient with microcrystalline cellulose, hydroxypropylmethylcellulose, crospovidone and colloidal silicon dioxide in amounts given above is wet granulated, the granules are compressed into tablets and coated with the coating materials.
- the coating process is performed at room temperature.
- the mixture of imatinib mesylate corresponding to 400 mg of imatinib as the active ingredient with microcrystalline cellulose, hydroxypropylmethylcellulose, crospovidone and colloidal silicon dioxide in amounts given above is wet granulated, the granules are compressed into tablets and coated with the coating materials. The coating process is performed at room temperature.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to compositions comprising imatinib or a pharmaceutically acceptable salt thereof, characterized in that imatinib is present in an amount of about 24.5-29% of the total composition and the corresponding imatinib mesylate is present in an amount of about 29. 5-34% of the total composition.
Description
The present invention relates to compositions
comprising imatinib or a pharmaceutically acceptable salt
thereof, characterized in that imatinib is present in an
amount of about 24.5 – 29% of the total composition and the
corresponding imatinib mesylate is present in an amount of
about 29. 5- 34% of the total composition.
Imatinib mesylate is chemically
4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methy-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide
methanesulfonate. Imatinib is a protein-tyrosine kinase
inhibitor and used to treat chronic mylogenous leukemia,
gastrointestinal stromal tumors and other type of cancers.
Imatinib inhibits the bcr-abl tyrosine kinase, the
constitutive abnormal tyrosine kinase created by the
Philadelphia chromosome abnormality in chronic mylogenous
leukemia. Imatinib inhibits proliferation and induces
apoptosis in bcr-abl positive cell lines as well as fresh
leukemic cells from Philadelphia chromosome positive chronic
myeloid leukemia.
As most of the pharmaceutical substances imatinib
mesylate also shows polymorphism that are reported in the
following international patent application Nos. WO 99/03854,
WO 2005/077933, WO 2005/095379, WO 2004/106326, WO
2006/054314, WO 2006/024863, WO 2006/ 048890, US
2006/0030568, WO 07/023182, WO 2007/136510 and US Pat. No 6894051.
PCT application WO 01/47507 tells a pharmaceutical
tablet composition containing about 22% w/w imatinib mesylate.
PCT application IN 2010/000202 describes a film
coated tablet comprising imatinib or pharmaceutically
acceptable salts thereof in an amount of more than 80% based
on the total weight of the coated tablet.
PCT application WO 03/090720 describes a tablet
formulation containing 30-80% w/w imatinib based on the
total weight of the composition. These tablets were prepared
by using wet granulation and described as being high loaded
small size tablets which are easy to swallow. Because of
high drug loaded composition the tablets shows high
friability and limited flexibility.
US patent application No 2009/0087489 reports a
pharmaceutical tablet compositions containing about 23 – 29%
w/w of imatinib mesylate which were prepared using dry
granulation or using direct compression.
The properties of the active ingredient, high
dosage administration to patients and problems arising
during the preparing tablets of imatinib with such low
excipients, there is still a need for commercially
acceptable composition of imatinib.
The present invention relates to compositions
comprising imatinib or a pharmaceutically acceptable salt
thereof characterized in that imatinib is present in an
amount of from about 24.5 – 29% in weight based on the total
composition and the corresponding imatinib mesylate is
present in an amount of about 29.5 – 34% of the total
composition.
Specifically, the present invention relates to
compositions comprising imatinib or a pharmaceutically
acceptable salt thereof characterized in that imatinib is
present in an amount of from about 24.5 – 29% e.g. at least
24.5, 25, 26, 27, 28 or 29% and the corresponding imatinib
mesylate is present in an amount of about 29.5 – 34%, e.g.
at least 29.5, 30, 31, 32, 33 or 34% in weight based on the
total composition.
More specifically, the present invention provides
a composition comprising
a-) a pharmaceutically effective amount of
imatinib or a pharmaceutically acceptable salt thereof, and
b-) at least one pharmaceutically acceptable
excipient suitable for the preparation of tablets wherein
the amount of imatinib, calculated as the percentage of the
content in weight based on the total weight of tablet is
from about 24.5 – 29% e.g. at least about 24, 5, 25, 26, 27,
28 or 29% and the corresponding imatinib mesylate is from
about 29.5 – 34%, e.g. at least about 29.5, 30, 31, 32, 33
or 34% in weight based on the total weight of the tablets.
The pharmaceutical compositions according to the
present invention comprises imatinib or a pharmaceutically
acceptable salt of imatinib as the active ingredient,
preferably the pharmaceutically acceptable salt of imatinib
is imatinib mesylate.
The pharmaceutical compositions according to the
present invention comprises one or more pharmaceutically
acceptable excipients e.g. at least one pharmaceutically
acceptable binder, at least one pharmaceutically acceptable
disintegrant, at least one pharmaceutically acceptable
glidant and at least one pharmaceutically acceptable lubricant.
Present invention discloses pharmaceutical
compositions, preferably tablets, comprising imatinib or
imatinib mesylate salt and at least one pharmaceutically
acceptable excipient.
The pharmaceutical compositions according to the
present invention comprising imatinib or imatinib mesylate
salt are preferably in tablet form, more preferably in film
coated tablet form.
The film coated tablet compositions comprising
imatinib or imatinib mesylate according to the present
invention can be prepared by a process of compressing the
mixture of an inner phase and an outer phase and optionally
coating the tablets.
The pharmaceutically acceptable binders can be
selected but not limited from the group consisting of
microcrystalline cellulose, hydropropyl cellulose,
hydroxyethyl cellulose, hydroxypropylmethyl cellulose,
hypromellose and polyvinylpyrrolidone.
The compositions comprising imatinib or imatinib
mesylate prepared by the wet granulation process according
to the present invention comprises a binder in a range of
from 1 – 60%, preferably in a range of from 10 – 60% of the
total composition.
Also, the compositions comprising imatinib or
imatinib mesylate prepared by the wet granulation process
according to the present invention comprising of an inner
phase and and outer phase wherein the inner phase comprises
a binder in a range of from about 1 – 30% of the total
composition while the outer phase comprises a binder in a
range of from about 1 – 15% of the total composition.
The pharmaceutically acceptable disintegrants can
be selected but not limited from the group consisting of
maize starch, CMC-Ca, CMC-Na, microcrystalline cellulose,
cross-linked polyvinyl pyrolidone (crospovidone), alginic
acid, sodium alginate and quar gum. The disintegrant used in
the invention is in a range of from 4 – 30%, preferably in a
range of form 10 – 30% of the total composition.
The pharmaceutically acceptable glidants can be
selected but not limited from the group consisting of
silica, colloidal silicon dioxide, magnesium trisilicat,
powdered cellulose, starch, talc and mixture thereof. The
glidant used in the invention is in a range of from 0.2 – 5%
of the total composition.
The pharmaceutically acceptable lubricants can be
selected but not limited from the group consisting of
magnesium stearate, aluminum stearate, calcium stearate, PEG
4000, PEG 8000 and talc. The lubricant used in the invention
is in a range of from 0.1 – 4% of the total composition.
The compositions according to the present
invention comprises one or more pharmaceutically acceptable
excipient, e.g. at least one pharmaceutically acceptable
binder in a range of 1 – 60%, at least one pharmaceutically
acceptable disintegrant in a range of 4 – 30% of the total
composition, at least one pharmaceutically acceptable
glidant in a range of 0.2 – 5% of the total composition and
at least one pharmaceutically acceptable lubricant in a
range of 0.1 – 4% of the total composition.
The pharmaceutical composition of the invention
comprises a dosage containing from about 50 mg to 500 mg,
preferably from about 100 mg to 400 mg imatinib or a
pharmaceutically acceptable salt thereof.
The present invention also provides a process for
preparing pharmaceutical composition, comprising imatinib in
an amount of about 24.5 – 29% of total composition and
corresponding imatinib mesylate in an amount of about 29.5 –
34% of the total composition.
The tablet compositions comprising imatinib or
imatinib mesylate salt according to the present invention
may be prepared by direct compression, wet granulation or
roll compaction.
The film coated tablet compositions comprising
imatinib or imatinib mesylate salt according to the present
invention is prepared preferably by wet granulation.
The wet granulation process of the film coated
tablet compositions comprising imatinib or imatinib mesylate
according to the present invention may be carried out using
the solvent selected from water, ethyl alcohol, isopropyl
alcohol and mixture thereof, preferably the solvent is ethyl alcohol.
The tablet compositions comprising imatinib or
imatinib mesylate prepared by the wet granulation process
according to the present invention may be carried out by a
process comprising the steps of;
a) mixing imatinib or imatinib mesylate together
with one or more pharmaceutically acceptable excipients,
b) wet granulating the mixture obtained from step (a),
c) obtained inner phase is mixed with one or more
pharmaceutically acceptable excipients to obtain the outer phase,
d) forming the tablet by compressing the mixture
obtained in steps (a) – (c),
e)preferably the obtained tablets are coated.
Specifically the tablet compositions comprising
imatinib or imatinib mesylate salt according to the present
invention may be carried out by a process comprising the
steps of;
a) mixing imatinib or imatinib mesylate salt with
one or more pharmaceutically acceptable binder, e.g.
microcrystalline cellulose in a mixer,
b) the mixture obtained from step (a) is wet
granulated with a solvent selected from water, alcohol or
mixture thereof,
c) obtained granules are dried,
d) one or more pharmaceutically acceptable
disintegrants, e.g. crospovidone, one or more
pharmaceutically acceptable binders, e.g. microcrystalline
cellulose, one or more pharmaceutically acceptable glidants,
e.g. colloidal silicon dioxide is added to the granules
obtained from step (c) and mixed,
e) adding one or more pharmaceutically acceptable
lubricants, e.g. magnesium stearate to the mixture and
sieving,
f) tableting the mixture obtained in step (e) by
direct compression and
g) coating the tablets.
More specifically the tablet compositions
comprising imatinib or imatinib mesylate salt according to
the present invention may be carried out by a process
comprising the steps of;
a) mixing imatinib or imatinib mesylate salt with
one or more pharmaceutically acceptable binder, e.g.
microcrystalline cellulose in an amount in the range of 1 –
30% in a mixer,
b) the mixture obtained from step (a) is wet
granulated with a solvent selected from water, alcohol or
mixture thereof,
c) obtained granules are dried by a convenient
method known in the prior art,
d) one or more pharmaceutically acceptable binder,
e.g. microcrystalline cellulose in an amount in the range of
1 – 15% and/or one or more pharmaceutically acceptable
disintegrant, e.g. crospovidone in an amount in the range of
4 – 30% and/or one or more pharmaceutically acceptable
glidant, e.g. colloidal silicon dioxide in an amount in the
range of 0.2 – 5% is mixed with the inner phase comprising
imatinib or imatinib mesylate salt obtained from step (c)
and the outer phase is obtained,
e) adding one or more pharmaceutically acceptable
lubricants, e.g. magnesium stearate in an amount in the
range of 0.1 – 4% to the obtained mixture and sieving,
f) tableting the mixture obtained in step (e) by
compression and
g) preferably film coating the tablets.
The following examples are given for the purpose
of illustrating the invention and shall not be understood as
limiting the scope or spirit of the invention.
EXAMPLE 1
Tablets containing in a range of 29.5 – 34%
imatinib mesylate corresponding to 100 mg imatinib prepared
by wet granulation
| Composition per unit (mg) | % | ||
| Imatinib mesylate | Active Ingredient | 119.50 | 33.7 |
| Microcrystalline Cellulose | Binder | 100.00 | 28.2 |
| Hydroxypropyl Methylcellulose | Binder | 15.00 | 4.2 |
| Microcrytallinecellulose | Binder | 25.00 | 7.06 |
| Crospovidone | Disintegrant | 80.00 | 22.6 |
| Colloidal silicon dioxide | Glidant | 3.00 | 0.85 |
| Magnesium stearate | Lubricant | 4.00 | 1.13 |
| Basic cooting premix yellow | Coating | 7.10 | 2.0 |
| Basic cooting premix red | Coating | 0.40 | 0.26 |
| Total tablet weight | 354.00 | 100 |
The mixture of imatinib mesylate corresponding to
100 mg of imatinib as the active ingredient with
microcrystalline cellulose, hydroxypropylmethylcellulose,
crospovidone and colloidal silicon dioxide in amounts given
above is wet granulated, the granules are compressed into
tablets and coated with the coating materials. The coating
process is performed at room temperature.
EXAMPLE 2
Tablets containing in a range of 29.5 – 34%
imatinib mesylate corresponding to 400 mg imatinib prepared
by wet granulation
| Composition per unit (mg) | % | ||
| Imatinib mesylate | Active Ingredient | 478.00 | 33.7 |
| Microcrystalline Cellulose | Binder | 400.00 | 28.2 |
| Hydroxypropyl Methylcellulose | Binder | 60.00 | 4.2 |
| Microcrytallinecellulose | Binder | 100.00 | 7.06 |
| Crospovidone | Disintegrant | 320.00 | 22.6 |
| Colloidal silicon dioxide | Glidant | 12.00 | 0.85 |
| Magnesium stearate | Lubricant | 16.00 | 1.13 |
| Basic cooting premix yellow | Coating | 28.40 | 2.0 |
| Basic cooting premix red | Coating | 1.60 | 0.26 |
| Total tablet weight | 1416.00 | 100 |
The mixture of imatinib mesylate corresponding to
400 mg of imatinib as the active ingredient with
microcrystalline cellulose, hydroxypropylmethylcellulose,
crospovidone and colloidal silicon dioxide in amounts given
above is wet granulated, the granules are compressed into
tablets and coated with the coating materials. The coating
process is performed at room temperature.
Claims (11)
- A pharmaceutical composition comprising imatinib or a pharmaceutically acceptable salt thereof characterized in that the amount of imatinib in the composition is in an amount of about 24.5 – 29% of the total composition and the corresponding imatinib mesylate in an amount of about 29.5 – 34% of the total composition.
- The pharmaceutical composition of claim 1 characterized in that imatinib mesylate is in an amount of about 29.5 – 34% of the total composition.
- The pharmaceutical composition of claims 1 and 2 characterized in that the composition is in the form of tablet.
- The pharmaceutical composition of claim 3 characterized in that the composition is in the form of film coated tablet.
- The pharmaceutical composition of claims 3 – 4 characterized in that the composition comprises a dosage of about 50 – 500 mg of imatinib.
- The pharmaceutical composition of claim 5 characterized in that the composition comprises a dosage of 100 – 400 mg of imatinib.
- The pharmaceutical composition according to any one of the preceding claims, characterized in that the composition comprises imatinib mesylate in an amount from 29.5 – 34%, binder in an amount from 1 – 60%, disintegrant in an amount from 4 – 30%, glidant in an amount from 0.2 – 5% and lubricant in an amount from 0.1 – 4%.
- The pharmaceutical composition of claim 7 characterized in that the binder is selected from microcrystalline cellulose, hydroxypropylmethyl cellulose or a mixture thereof.
- The pharmaceutical composition of claim 7 characterized in that the disintegrant is crospovidone.
- The pharmaceutical composition of claim 7 characterized in that the glidant is colloidal silicon dioxide.
- The pharmaceutical composition of claim 7 characterized in that the lubricant is magnesium stearate.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR201513856 | 2015-11-05 | ||
| TR2015/13856 | 2015-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2017078647A1 true WO2017078647A1 (en) | 2017-05-11 |
Family
ID=57680466
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/TR2016/050424 WO2017078647A1 (en) | 2015-11-05 | 2016-11-04 | Pharmaceutical compositions of imatinib |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2017078647A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11285152B2 (en) | 2017-07-20 | 2022-03-29 | Kashiv Biosciences, Llc | Stable oral pharmaceutical composition of imatinib |
Citations (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999003854A1 (en) | 1997-07-18 | 1999-01-28 | Novartis Ag | Crystal modification of a n-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use |
| WO2001047507A2 (en) | 1999-12-27 | 2001-07-05 | Novartis Ag | Combinations of receptor tyrosine kinase inhibitor with an a1-acidic glycoprotein binding compound |
| WO2003090720A1 (en) | 2002-04-23 | 2003-11-06 | Novartis Ag | High drug load tablet |
| WO2004106326A1 (en) | 2003-06-02 | 2004-12-09 | Hetero Drugs Limited | Novel polymorphs of imatinib mesylate |
| WO2005077933A1 (en) | 2004-02-11 | 2005-08-25 | Natco Pharma Limited | Novel polymorphic form of imatinib mesylate and a process for its preparation |
| WO2005095379A2 (en) | 2004-04-02 | 2005-10-13 | Instytut Farmaceutyczny | Crystalline methanesulfonic acid addition salts of imatinib |
| WO2006024863A1 (en) | 2004-09-02 | 2006-03-09 | Cipla Limited | Stable crystal form of imatinib mesylate and process for the preparation thereof |
| WO2006048890A1 (en) | 2004-11-04 | 2006-05-11 | Sun Pharmaceutical Industries Limited | Imatinib mesylate crystal form and process for preparation thereof |
| WO2006054314A1 (en) | 2004-11-17 | 2006-05-26 | Natco Pharma Limited | Polymorphic forms of imatinib mesylate |
| WO2007023182A1 (en) | 2005-08-26 | 2007-03-01 | Novartis Ag | Delta and epsilon crystal forms of imatinib mesylate |
| WO2007136510A2 (en) | 2006-04-27 | 2007-11-29 | Sicor Inc. | Polymorphic forms of imatinib mesylate and processes for their preparation as well as of amorphous imatinib mesylate and form alpha |
| US20090087489A1 (en) | 2007-09-25 | 2009-04-02 | Bella Gerber | Imatinib compositions |
| EP2604596A1 (en) * | 2011-12-16 | 2013-06-19 | Deva Holding Anonim Sirketi | Polymorphs of imatinib |
| EP2749269A1 (en) * | 2012-12-31 | 2014-07-02 | Deva Holding Anonim Sirketi | Process for the preparation of adsorbates of imatinib |
-
2016
- 2016-11-04 WO PCT/TR2016/050424 patent/WO2017078647A1/en active Application Filing
Patent Citations (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999003854A1 (en) | 1997-07-18 | 1999-01-28 | Novartis Ag | Crystal modification of a n-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use |
| US6894051B1 (en) | 1997-07-18 | 2005-05-17 | Novartis Ag | Crystal modification of a N-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use |
| US20060030568A1 (en) | 1997-07-18 | 2006-02-09 | Jurg Zimmermann | Crystal modificaion of a N-phenyl-2-pyrimidineamine derivative, processed for its manufacture and its use |
| WO2001047507A2 (en) | 1999-12-27 | 2001-07-05 | Novartis Ag | Combinations of receptor tyrosine kinase inhibitor with an a1-acidic glycoprotein binding compound |
| WO2003090720A1 (en) | 2002-04-23 | 2003-11-06 | Novartis Ag | High drug load tablet |
| WO2004106326A1 (en) | 2003-06-02 | 2004-12-09 | Hetero Drugs Limited | Novel polymorphs of imatinib mesylate |
| WO2005077933A1 (en) | 2004-02-11 | 2005-08-25 | Natco Pharma Limited | Novel polymorphic form of imatinib mesylate and a process for its preparation |
| WO2005095379A2 (en) | 2004-04-02 | 2005-10-13 | Instytut Farmaceutyczny | Crystalline methanesulfonic acid addition salts of imatinib |
| WO2006024863A1 (en) | 2004-09-02 | 2006-03-09 | Cipla Limited | Stable crystal form of imatinib mesylate and process for the preparation thereof |
| WO2006048890A1 (en) | 2004-11-04 | 2006-05-11 | Sun Pharmaceutical Industries Limited | Imatinib mesylate crystal form and process for preparation thereof |
| WO2006054314A1 (en) | 2004-11-17 | 2006-05-26 | Natco Pharma Limited | Polymorphic forms of imatinib mesylate |
| WO2007023182A1 (en) | 2005-08-26 | 2007-03-01 | Novartis Ag | Delta and epsilon crystal forms of imatinib mesylate |
| WO2007136510A2 (en) | 2006-04-27 | 2007-11-29 | Sicor Inc. | Polymorphic forms of imatinib mesylate and processes for their preparation as well as of amorphous imatinib mesylate and form alpha |
| US20090087489A1 (en) | 2007-09-25 | 2009-04-02 | Bella Gerber | Imatinib compositions |
| EP2604596A1 (en) * | 2011-12-16 | 2013-06-19 | Deva Holding Anonim Sirketi | Polymorphs of imatinib |
| EP2749269A1 (en) * | 2012-12-31 | 2014-07-02 | Deva Holding Anonim Sirketi | Process for the preparation of adsorbates of imatinib |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11285152B2 (en) | 2017-07-20 | 2022-03-29 | Kashiv Biosciences, Llc | Stable oral pharmaceutical composition of imatinib |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP2582362A1 (en) | Pharmaceutical compositions comprising imatinib or pharmaceutically acceptable salt thereof and processes for the manufacture thereof | |
| EP3606511B1 (en) | Pharmaceutical composition comprising lenvatinib mesylate | |
| EP2468361A1 (en) | Vildagliptin Formulations | |
| JP2017088609A (en) | Solid pharmaceutical composition containing compound having angiotensin ii antagonism | |
| JP2023175743A (en) | Pharmaceutical composition containing poorly soluble basic drug | |
| TW201717937A (en) | Pharmaceutical composition containing aryl alkyl amine compound | |
| US11000523B2 (en) | Ceritinib formulation | |
| CN106913529B (en) | Preparation method of pharmaceutical composition of neratinib or pharmaceutically acceptable salt thereof | |
| WO2019020706A1 (en) | Pharmaceutical composition comprising sacubitril and valsartan | |
| EP3860606B1 (en) | Pharmaceutical composition comprising lenvatinib esylate or tosylate | |
| US20130085145A1 (en) | Imatinib mesilate pharmaceutical tablet | |
| US9750700B2 (en) | Imatinib mesylate oral pharmaceutical composition and process for preparation thereof | |
| WO2017078647A1 (en) | Pharmaceutical compositions of imatinib | |
| WO2013008253A2 (en) | Imatinib formulations | |
| RU2735807C2 (en) | Method for preparing a pharmaceutical composition comprising a quinoline derivative or salt thereof | |
| WO2014115082A1 (en) | Pharmaceutical formulations of imatinib | |
| AU2013309686B2 (en) | Bilayered composite tablet formulation comprising atorvastatin, irbesartan and magnesium carbonate | |
| EP2803353B1 (en) | Compositions of Imatinib | |
| EP4260848A1 (en) | Pharmaceutical composition for solid dosage form containing nilotinib and process for its preparation | |
| KR102444073B1 (en) | Pharmaceutical formulation containing methylergometrine maleate with improved stability and method preparing the same | |
| TW201726135A (en) | A pharmaceutical composition comprising quinoline derivatives or salt thereof | |
| DK3166596T3 (en) | Pharmaceutical dosage forms | |
| JP5827428B1 (en) | Telmisartan-containing tablets | |
| CN111888476A (en) | Modified release pharmaceutical composition of trimetazidine dihydrochloride | |
| JP2021066715A (en) | Method for producing particle containing imidafenacin and use thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 121 | Ep: the epo has been informed by wipo that ep was designated in this application |
Ref document number: 16819697 Country of ref document: EP Kind code of ref document: A1 |
|
| NENP | Non-entry into the national phase |
Ref country code: DE |
|
| 122 | Ep: pct application non-entry in european phase |
Ref document number: 16819697 Country of ref document: EP Kind code of ref document: A1 |