US2016228386A1PendingUtilityA1

Pharmaceutical Formulation

Assignee: RECKITT BENCKISER LLCPriority: Feb 4, 2011Filed: Apr 19, 2016Published: Aug 11, 2016

Est. expiryFeb 4, 2031(~4.5 yrs left)· nominal 20-yr term from priority

Inventors:Nils Ahlgren Mark Nuttall Jeannie Chow Wong Venkatesh Balasubramanian Craig Belongie Ashfaq Khan Neil Campbell Muir

A61P 11/14A61P 11/00A61P 11/10A61P 11/02A61K 9/5047A61K 31/137A61K 31/09A61K 45/06A61K 9/4808A61K 31/485A61K 9/5026A61K 9/20A61K 9/2027A61K 9/2054A61K 9/209A61K 9/5042

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References

Claims

Abstract

A pharmaceutical composition in the form of a tablet including a first portion and a second portion, wherein the first portion includes guaifenesin having an immediate release profile and a second drug having a sustained release profile, and wherein the second portion includes guaifenesin having a sustained release profile. The second drug can be in the form of a drug-resin complex. The second drug can be either an anti-tussive or a decongestant. The drug-resin complex includes a drug complexed to an ion exchange resin. The ion exchange resin can be a polystyrene sulfonate resin, polacrilex resin, polacrilin potassium, cholestyramine resin, or a colestyramine resin. The drug-resin complex can be provided with a coating, the coating thickness being selected to obtain the desired release profile. The drug-resin complex can be provided with a coating level of from 5% to 50%. The coating level can be from 10% to 35%.

Claims

exact text as granted — not AI-modified

We claim:

1 . A pharmaceutical composition comprising:
a first portion; and a second portion; wherein the first portion comprises guaifenesin having an immediate release profile and a second drug having a sustained release profile; and wherein the second portion comprises guaifenesin having a sustained release profile.

2 . The pharmaceutical composition as claimed in claim 1 , wherein the second portion comprises a release-delaying matrix comprising a hydrophilic polymer and a water-insoluble polymer.

3 . The pharmaceutical composition as claimed in claim 1 , wherein the second drug comprises codeine.

4 . The pharmaceutical composition as claimed in claim 2 , wherein the hydrophilic polymer comprises hydroxypropyl methylcellulose.

5 . The pharmaceutical composition as claimed in claim 2 , wherein the water-insoluble polymer comprises a carbomer.

6 . The pharmaceutical composition as claimed in claim 1 , wherein the second drug is in the form of a coated drug-resin complex.

7 . The pharmaceutical composition as claimed in claim 1 , wherein the second drug is selected from the group consisting of an anti-tussive and a decongestant.

8 . The pharmaceutical composition as claimed in claim 1 , wherein the second drug is selected from the group consisting of codeine, pseudoephedrine, phenylephrine, dextromethorphan and hydrocodone.

9 . The pharmaceutical composition as claimed in claim 6 , wherein the coated drug-resin complex comprises an ion exchange resin.

10 . The pharmaceutical composition as claimed in claim 9 , wherein the ion exchange resin is selected from the group consisting of a polystyrene sulfonate resin, polacrilex resin, polacrilin potassium, cholestyramine resin, a colestyramine resin, and a sodium polystyrene sulfonate resin.

11 . The pharmaceutical composition as claimed in claim 6 , wherein the coating level of the coated drug-resin complex is from 5% to 50%.

12 . The pharmaceutical composition as claimed in claim 11 , wherein the coating level is from 10% to 35%.

13 . A pharmaceutical composition comprising:
a first portion; and a second portion; wherein the first portion comprises guaifenesin having an immediate release profile and a second drug in the form of a coated drug-resin complex having a sustained release profile; and wherein the second portion comprises guaifenesin having a sustained release profile.

14 . The pharmaceutical composition as claimed in claim 13 , wherein the coated drug-resin complex comprises a coated codeine polistirex complex.

15 . The pharmaceutical composition as claimed in claim 13 , wherein the coated drug resin complex has a coating level of 30% and has the following dissolution profile in USP apparatus 1 (baskets) at 50 rpm in 0.1N HCl at 37° C.:

Time (hours)
Average % Codeine released

1
18-48

2
27-57

6
42-72

12
51-81

16 . The pharmaceutical composition as claimed in claim 13 , wherein the coated drug resin complex has a coating level of 30% and has the following dissolution profile in USP apparatus 1 (baskets) at 50 rpm in 0.1N HCl at 37° C.:

Time (hours)
Average % Codeine released

1
33

2
42

6
57

12
66

17 . The pharmaceutical composition as claimed in claim 13 , wherein the coated drug resin complex has a coating level of 15% and has the following dissolution profile in USP apparatus 1 (baskets) at 50 rpm in 0.1N HCl at 37° C.:

Time (hours)
Average % Codeine released

1
30-60

2
43-73

6
64-94

12
at least 73

18 . The pharmaceutical composition as claimed in claim 13 , wherein the coated drug resin complex has a coating level of 15% and has the following dissolution profile in USP apparatus 1 (baskets) at 50 rpm in 0.1N HCl at 37° C.:

Time (hours)
Average % Codeine released

1
45

2
58

6
79

12
88

19 . A pharmaceutical composition comprising:
a first portion; and a second portion; wherein the first portion comprises guaifenesin having an immediate release profile and a second drug having a sustained release profile; wherein the second portion comprises guaifenesin having a sustained release profile; wherein the total amount of guaifenesin is between 500 mg and 1300 mg; wherein the total amount of the second drug is up to 100 mg; and wherein the ratio of the total quantity of guaifenesin to the second drug in the same portion is from 1:1 to 30:1 (by weight).

20 . The pharmaceutical composition as claimed in claim 19 , wherein the second portion comprises a release-delaying matrix comprising a hydrophilic polymer and a water-insoluble polymer.

21 . The pharmaceutical composition as claimed in claim 19 , wherein the second drug comprises codeine.

22 . The pharmaceutical composition as claimed in claim 20 , wherein the hydrophilic polymer comprises hydroxypropyl methylcellulose.

23 . The pharmaceutical composition as claimed in claim 20 , wherein the water-insoluble polymer comprises a carbomer.

24 . The pharmaceutical composition as claimed in claim 19 , wherein the second drug is in the form of a coated drug-resin complex.

25 . The pharmaceutical composition as claimed in claim 19 , wherein the second drug is selected from the group consisting of an anti-tussive and a decongestant.

26 . The pharmaceutical composition as claimed in claim 19 , wherein the second drug is selected from the group consisting of codeine, pseudoephedrine, phenylephrine, dextromethorphan and hydrocodone.

27 . The pharmaceutical composition as claimed in claim 24 , wherein the coated drug-resin complex comprises an ion exchange resin.

28 . The pharmaceutical composition as claimed in claim 27 , wherein the ion exchange resin is selected from the group consisting of a polystyrene sulfonate resin, polacrilex resin, polacrilin potassium, cholestyramine resin, a colestyramine resin, and a sodium polystyrene sulfonate resin.

29 . The pharmaceutical composition as claimed in claim 25 , wherein the coating level of the coated drug-resin complex is from 5% to 50%.

30 . The pharmaceutical composition as claimed in claim 29 , wherein the coating level is from 10% to 35%.

31 . The pharmaceutical composition as claimed in claim 19 , wherein the second drug is also the sustained release portion.

32 . The pharmaceutical composition as claimed in claim 20 , wherein the weight ratio of hydrophilic polymer to water-insoluble polymer is from 1:1 to 9:1.

33 . The pharmaceutical composition as claimed in claim 20 , wherein the weight ratio of hydrophilic polymer to water-insoluble polymer is from 3:2 to 6:1.

34 . The pharmaceutical composition as claimed in claim 20 , wherein the weight ratio of hydrophilic polymer to water-insoluble polymer is from 2:1 to 4:1.

35 . The pharmaceutical composition as claimed in claim 19 , wherein the total amount of guaifenesin is between 600 mg to 1200 mg.

36 . The pharmaceutical composition as claimed in claim 19 , wherein the formulation contains 1200 mg of guaifenesin.

37 . The pharmaceutical composition as claimed in claim 19 , wherein the formulation contains 600 mg of guaifenesin.

38 . The pharmaceutical composition as claimed in claim 19 , wherein the total amount of the second drug is between 20-80 mg.

39 . The pharmaceutical composition as claimed in claim 21 , wherein the composition contains an amount of codeine that is therapeutically equivalent to 60 mg of codeine phosphate.

40 . The pharmaceutical composition as claimed in claim 21 , wherein the composition contains an amount of codeine that is therapeutically equivalent to 30 mg of codeine phosphate.

41 . The pharmaceutical composition as claimed in claim 21 , wherein the composition comprises 600 mg of guaifenesin and an amount of codeine that is therapeutically equivalent to 30 mg of codeine phosphate.

42 . The pharmaceutical composition as claimed in claim 21 , wherein the composition comprises 600 mg of guaifenesin and an amount of codeine that is therapeutically equivalent to 30 mg of codeine phosphate.

43 . The pharmaceutical composition as claimed in claim 21 , wherein the immediate release portion comprises microcrystalline cellulose, crospovidone and magnesium stearate.

44 . The pharmaceutical composition as claimed in claim 21 , wherein ratio of the total quantity of guaifenesin to codeine in the same portion is from 1:1 to 25:1 (by weight).

45 . The pharmaceutical composition as claimed in claim 19 , wherein the ratio of the immediate release quantity of guaifenesin to the sustained release quantity of guaifenesin is from 1:1 to 1:15 (by weight).

46 . The pharmaceutical composition as claimed in claim 19 , wherein the ratio of the immediate release quantity of guaifenesin to the sustained release quantity of guaifenesin is from 2:3 to 1:11 (by weight).

47 . The pharmaceutical composition as claimed in claim 19 , wherein the at least 60% of guaifenesin particles used to make the pharmaceutical composition has a particle size in the range of from 25 μm to 2.0 mm.

48 . The pharmaceutical composition as claimed in claim 19 , wherein the formulation comprises immediate release and sustained release portions each comprising abutting planar layers which form a bi-layer tablet.

49 . The pharmaceutical composition as claimed in claim 19 , wherein the formulation comprises a capsule that contains discrete or associated immediate release and sustained release portions.

50 . The pharmaceutical composition as claimed in claim 19 , wherein the sustained release portion is coated by a layer of the immediate release portion.

51 . The pharmaceutical composition as claimed in claim 19 , wherein each drug in the formulation exhibits a therapeutic effect for a period of 12 hours.

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