U.S. patent application number 13/882953 was filed with the patent office on 2013-08-29 for combination composition.
This patent application is currently assigned to AFT Pharmaceuticals Limited. The applicant listed for this patent is Hartley Campbell Atkinson. Invention is credited to Hartley Campbell Atkinson.
Application Number | 20130225685 13/882953 |
Document ID | / |
Family ID | 46024668 |
Filed Date | 2013-08-29 |
United States Patent
Application |
20130225685 |
Kind Code |
A1 |
Atkinson; Hartley Campbell |
August 29, 2013 |
COMBINATION COMPOSITION
Abstract
An intravenous composition for providing relief for pain and/or
inflammation, the composition having ibuprofen and paracetamol in
combination for delivering to a human at each dose: a)
approximately 125 mg to approximately 175 mg ibuprofen in
combination with approximately 475 mg to approximately 525 mg
paracetamol; or b) approximately 275 mg to approximately 325 mg
ibuprofen in combination with approximately 975 mg to approximately
1,025 mg paracetamol.
Inventors: |
Atkinson; Hartley Campbell;
(Takapuna, NZ) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
Atkinson; Hartley Campbell |
Takapuna |
|
NZ |
|
|
Assignee: |
AFT Pharmaceuticals Limited
Takapuna, Auckland
NZ
|
Family ID: |
46024668 |
Appl. No.: |
13/882953 |
Filed: |
October 26, 2011 |
PCT Filed: |
October 26, 2011 |
PCT NO: |
PCT/NZ2011/000226 |
371 Date: |
May 1, 2013 |
Current U.S.
Class: |
514/570 |
Current CPC
Class: |
A61K 31/167 20130101;
A61P 43/00 20180101; A61P 25/04 20180101; A61K 9/08 20130101; A61K
31/192 20130101; A61P 25/20 20180101; A61P 29/00 20180101; A61K
9/0019 20130101; A61K 47/183 20130101; A61K 31/192 20130101; A61K
2300/00 20130101; A61K 31/167 20130101; A61K 2300/00 20130101 |
Class at
Publication: |
514/570 |
International
Class: |
A61K 9/00 20060101
A61K009/00; A61K 31/167 20060101 A61K031/167; A61K 31/192 20060101
A61K031/192 |
Foreign Application Data
Date |
Code |
Application Number |
Nov 4, 2010 |
NZ |
589011 |
Claims
1. An intravenous composition for providing relief for pain and/or
inflammation, the composition having ibuprofen and paracetamol in
combination for delivering to a human at each dose: a)
approximately 125 mg to approximately 175 mg ibuprofen in
combination with approximately 475 mg to approximately 525 mg
paracetamol; or b) approximately 275 mg to approximately 325 mg
ibuprofen in combination with approximately 975 mg to approximately
1,025 mg paracetamol.
2. The composition according to claim 1, for dosing on
approximately a 6 hourly basis.
3. The composition according to claim 1, comprising: a)
approximately 150 mg ibuprofen in combination with approximately
500 mg paracetamol; or b) approximately 300 mg ibuprofen in
combination with approximately 1,000 mg paracetamol.
4. The composition according to claim 1, in the form of a
solution.
5. A method for manufacturing an intravenous medicament for
treating pain and/or inflammation in a human wherein the medicament
comprises, on a per dose basis: a) approximately 125 mg to
approximately 175 mg ibuprofen in combination with approximately
475 mg to approximately 525 mg paracetamol; or b) approximately 275
mg to approximately 325 mg ibuprofen in combination with
approximately 975 mg to approximately 1,025 mg paracetamol;
comprising mixing ibuprofen and paracetamol in the aforementioned
amounts with an excipient.
6. The use according to claim 5, wherein the composition is for
dosing on approximately a 6 hourly basis
7. The use according to claim 5, wherein the composition comprises:
a) approximately 150 mg ibuprofen in combination with approximately
500 mg paracetamol; or b) approximately 300 mg ibuprofen in
combination with approximately 1,000 mg paracetamol.
8. The use according to claim 5, wherein the composition is in the
form of a solution.
9. A method of treating pain and/or inflammation by administering
to a human, intravenously, a medicament comprising: a)
approximately 125 mg to approximately 175 mg ibuprofen in
combination with approximately 475 mg to approximately 525 mg
paracetamol; or b) approximately 275 mg to approximately 325 mg
ibuprofen in combination with approximately 975 mg to approximately
1,025 mg paracetamol.
10. The method according to claim 9, wherein the composition is
administered on a 6 hourly basis.
11. The method according to claim 9, wherein the composition
comprises: a) approximately 150 mg ibuprofen in combination with
approximately 500 mg paracetamol; or b) approximately 300 mg
ibuprofen in combination with approximately 1,000 mg
paracetamol.
12. The composition according to claim 2, comprising: a)
approximately 150 mg ibuprofen in combination with approximately
500 mg paracetamol; or b) approximately 300 mg ibuprofen in
combination with approximately 1,000 mg paracetamol.
13. The composition according to claim 2, in the form of a
solution.
14. The composition according to claim 3, in the form of a
solution.
15. The use according to claim 6, wherein the composition is in the
form of a solution.
16. The use according to claim 7, wherein the composition is in the
form of a solution.
17. The use according to claim 6, wherein the composition
comprises: a) approximately 150 mg ibuprofen in combination with
approximately 500 mg paracetamol; or b) approximately 300 mg
ibuprofen in combination with approximately 1,000 mg
paracetamol.
18. The method according to claim 10, wherein the composition
comprises: a) approximately 150 mg ibuprofen in combination with
approximately 500 mg paracetamol; or b) approximately 300 mg
ibuprofen in combination with approximately 1,000 mg paracetamol.
Description
FIELD OF INVENTION
[0001] This invention relates to a combination composition
comprising paracetamol and ibuprofen. A particularly preferred
embodiment of the invention relates to a combination composition
containing these active ingredients for use in relieving pain
and/or inflammation.
BACKGROUND
[0002] Combinations of paracetamol and ibuprofen are known, for
example as relatively low dose tablets having 150 mg ibuprofen and
500 mg paracetamol. However there is a need for a medication,
particularly one which can be administered intravenously in a
hospital environment. It is an object of an embodiment of the
present invention to go at least some way towards facilitating
this.
Definitions
[0003] References in this specification to an adult mean a person
weighing 50 kg or more.
[0004] References in this specification to a child mean a person
weighing less than 50 kg.
[0005] While ibuprofen and paracetamol are specifically referred to
in this specification, suitable other pharmaceutically acceptable
forms of these two actives (eg salts, etc) may also be used and are
intended to be embraced in the claims by references to the actives
per se, with the weight amounts adjusted accordingly. For example,
when a salt form is used, sufficient quantity may be included to
meet the desired amount of the compound per se (eg, 513 mg
ibuprofen lysinate, or 553 mg ibuprofen arginine salt, corresponds
with 300 mg ibuprofen). Thus, for example, a reference to 300 mg
ibuprofen may be construed as sufficient to embrace the
therapeutically equivalent amount of ibuprofen lysinate or
ibuprofen arginine.
[0006] The term "comprising" and derivatives thereof, eg
"comprises", if and when used in relation to a combination of
features should not be taken to exclude the possibility of the
combination having further unspecified features.
SUMMARY OF INVENTION
[0007] According to one aspect of the invention there is provided
an intravenous composition for providing relief for pain and/or
inflammation, the composition having ibuprofen and paracetamol in
combination for delivering to a human at each dose: [0008] a)
approximately 125 mg to approximately 175 mg ibuprofen in
combination with approximately 475 mg to approximately 525 mg
paracetamol; or [0009] b) approximately 275 mg to approximately 325
mg ibuprofen in combination with approximately 975 mg to
approximately 1,025 mg paracetamol.
[0010] Preferably the composition is for dosing on approximately a
6 hourly basis.
[0011] Preferably the composition comprises: [0012] a)
approximately 150 mg ibuprofen in combination with approximately
500 mg paracetamol; or [0013] b) approximately 300 mg ibuprofen in
combination with approximately 1,000 mg paracetamol.
[0014] Preferably the composition is in the form of a solution.
[0015] A further aspect of the invention comprises the use of
paracetamol and ibuprofen in the manufacture of an intravenous
medicament for treating pain and/or inflammation in a human wherein
the medicament comprises, on a per dose basis: [0016] a)
approximately 125 mg to approximately 175 mg ibuprofen in
combination with approximately 475 mg to approximately 525 mg
paracetamol; or [0017] b) approximately 275 mg to approximately 325
mg ibuprofen in combination with approximately 975 mg to
approximately 1,025 mg paracetamol.
[0018] Preferably the composition is for dosing on approximately a
6 hourly basis
[0019] Preferably the composition comprises: [0020] a)
approximately 150 mg ibuprofen in combination with approximately
500 mg paracetamol; or [0021] b) approximately 300 mg ibuprofen in
combination with approximately 1,000 mg paracetamol.
[0022] Preferably the composition is in the form of a solution.
[0023] A further aspect of the invention comprises a method of
treating pain and/or inflammation by administering to a human,
intravenously, a medicament comprising: [0024] a) approximately 125
mg to approximately 175 mg ibuprofen in combination with
approximately 475 mg to approximately 525 mg paracetamol; or [0025]
b) approximately 275 mg to approximately 325 mg ibuprofen in
combination with approximately 975 mg to approximately 1,025 mg
paracetamol.
[0026] Preferably the composition is administered on a 6 hourly
basis.
[0027] Preferably the composition comprises: [0028] a)
approximately 150 mg ibuprofen in combination with approximately
500 mg paracetamol; or [0029] b) approximately 300 mg ibuprofen in
combination with approximately 1,000 mg paracetamol.
[0030] Preferably the composition is in the form of a solution.
DETAILED DESCRIPTION
[0031] In a preferred embodiment of the invention an intravenous
solution is provided for use in treating pain or inflammation in
human patients. The solution is a combination medication comprising
ibuprofen, paracetamol and suitable excipients as will be known to
those with ordinary skills in the art of formulating intravenous
medicines. The excipients may include suitable antioxidants, pH
modulators, buffering agents isotonicity agents and purified
water.
[0032] The following examples illustrate preferred embodiments of
the invention in the form of intravenous infusion solutions.
TABLE-US-00001 Example 1 Example 2 Ingredient mg/100 ml vial mg/100
ml vial Ibuprofen 150 300 Paracetamol 500 1,000
[0033] For each of the above examples the two active ingredients
are mixed with suitable standard excipients to give the vial
volumes indicated above.
[0034] The infusion solutions are for delivery to a patient as a
full dose, for example in each case the patient receives the
complete vial contents as a 15 minute infusion every 6 hours.
Example 1 is a child's dose and Example 2 is an adult dose. In the
case of very young or small children only part of the vial contents
of Example 1 may be dosed on a body weight basis, commensurate with
instructions from the prescribing physician.
[0035] Paracetamol at 4,000 mg per 24 hour period, taken in 4 doses
of 1,000 mg every 6 hours, has long been considered sufficient for
relieving low level pain but for many patients suffering
significant pain, for example in some post operative situations, it
is not sufficient. However it is generally not advisable to dose
paracetamol at more than 1,000 mg per dose or at more than 4,000 mg
per 24 hour period, because to do so can lead to undesirable side
effects.
[0036] It is known to treat severe pain with ibuprofen in doses of
800 mg every 8 hours. However. doses as high as 800 mg can lead to
undesirable side effects, for example adverse cardio renal
conditions, renal problems, thrombotic risks and gastrointestinal
bleeding. Reducing the amount of ibuprofen at each dosing event may
reduce the risk of side effects but at the same time may provide
substantially less pain relief.
[0037] Surprisingly, an intravenous medicine comprising 150 mg or
300 mg ibuprofen, plus 500 mg or 1,000 mg paracetamol,
respectively, for use every 6 hours, provides adequate pain relief
for some patients that would otherwise need to take, respectively,
400 mg or 800 mg every 8 hours. The lower dose of ibuprofen reduces
the risk of undesirable side effects in some patients but the
effectiveness of the medication for such patients is not
compromised due to the presence of the paracetamol. This is
unexpected because for many patients one would not predict the
presence of paracetamol to assist to any significant degree. The
combination is counterintuitive because, for example, 400 mg
ibuprofen for relief of pain is generally seen as an 8 hourly
medicament, and 1,000 mg paracetamol is generally seen as a 6
hourly medicament. The normal dosage regimens for these active
ingredients are out of step with one another, ie 8 hourly versus 6
hourly, and thus to the normally skilled artesian they would not,
at the doses of the present invention, be seen as suitable for a
combination medication.
[0038] Similar considerations apply in the case of 150 mg
ibuprofen, in combination with 500 mg paracetamol, for treating
children suffering from pain. In this regard, surprisingly, some
children that would normally be given 200 mg ibuprofen for pain can
be given, as an alternative, 150 mg ibuprofen in combination with
500 mg paracetamol.
[0039] Administering an intravenous combination solution comprising
300 mg ibuprofen plus 1,000 mg paracetamol to an adult, or an
intravenous combination solution comprising 150 mg ibuprofen plus
500 mg paracetamol to a child, on an ongoing basis, for example
every 6 hours, provides a surprising level of pain relief compared
to administering the same doses orally, for example by way of a
tablet. The intravenous administration reduces the need for rescue
pain relief in at least some patients recovering from surgical
procedures. The intravenous administration may for example be by
way of injection or infusion.
Example 3
[0040] In a particular embodiment of the invention an intravenous
solution may be prepared by mixing the following active ingredients
and excipients:
TABLE-US-00002 AMOUNT ACTIVE INGREDIENTS Paracetamol 1000 mg
Ibuprofen arginine 553 mg EXCIPIENTS Reduced glutathione (as
antioxidant) 20 mg Sodium hydroxide or hydrochloric sufficient to
give a pH of 5-6 acid (as a pH modulator) Sodium citrate (as a
buffering agent) 10 mg Sodium chloride (as an isotonicity
sufficient to impart isotonicity agent) Purified water Sufficient
to bring the composition to 100 ml
[0041] The solution is for administration to an adult as a single
intravenous dose and further equivalent doses may be repeated every
6 hours if need be, commensurate with instructions from the
prescribing physician.
Example 4
[0042] In a further embodiment of the invention an intravenous
solution may be prepared by mixing the following active ingredients
and excipients:
TABLE-US-00003 AMOUNT ACTIVE INGREDIENTS Paracetamol 500 mg
Ibuprofen arginine 276.5 mg EXCIPIENTS Reduced glutathione (as
antioxidant) 10 mg Sodium hydroxide or hydrochloric sufficient to
give a pH of 5-6 acid (as a pH modulator) Sodium citrate (as a
buffering agent) 5 mg Sodium chloride (as an isotonicity sufficient
to impart isotonicity agent) Purified water Sufficient to bring the
composition to 100 ml
[0043] The solution is for administration to a child as a single
intravenous dose and further equivalent doses may be repeated every
6 hours if need be, commensurate with instructions from the
prescribing physician.
[0044] While some preferred forms of the invention have been
described by way of example it should be appreciated that
modifications and improvements can occur without departing from the
scope of the following claims.
* * * * *