US2002197320A1PendingUtilityA1

Composition and method for rectal delivery of a lincosamide antibiotic drug

Priority: Aug 6, 1999Filed: Feb 5, 2002Published: Dec 26, 2002

Est. expiryAug 6, 2019(expired)· nominal 20-yr term from priority

Inventors:Lorraine Pena Phil Bryan Bowman Robert S. Chao Carolyn Pesheck Clayton Jacobsen

A61P 31/04A61K 31/7056A61K 9/02

PatentIndex Score

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References

Claims

Abstract

A suppository composition and method for rectal administration of a lincosamide antibacterial drug, such as clindamycin, lincomycin, or pirlimycin, is disclosed. The composition is a rectal suppository containing an antimicrobially effective amount of the lincosamide in particulate form dispersed in a Hard Fat suppository base, preferably a Hard Fat NF suppository base. The most preferred suppository compositions of the present invention have long term storage stability, while maintaining effectiveness against bacterial infections.

Claims

exact text as granted — not AI-modified

We claim:

1 . A suppository composition for rectal administration of a lincosamide antibacterial drug, comprising an antimicrobially effective amount of the lincosamide dispersed in a Hard Fat suppository base, wherein the lincosamide is in the form of solid particles.

2 . The composition of claim 1 , wherein the lincosamide is present in a form selected from the group consisting of a lincosamide salt and a lincosamide ester.

3 . The composition of claim 1 , wherein the lincosamide is present in the form of a lincosamide phosphate.

4 . The composition of claim 1 wherein the lincosamide is present in said composition in an amount from about 0.1% by weight of the entire composition to about 60% by weight of the entire composition.

5 . The composition of claim 1 wherein the lincosamide is selected from the group consisting of pirlimycin and lincomycin.

6 . The composition of claim 1 wherein the lincosamide is clindamycin.

7 . The composition of claim 6 wherein said composition contains 50 to 150 mg of the clindamycin is present in said composition in an amount from about 1.5% by weight of the entire composition to about 7.5% by weight of the entire composition.

8 . The composition of claim 1 wherein said Hard Fat has a β polymorphic form which has a flow point in the range from 30° C. to 40° C.

9 . The composition of claim 1 wherein said Hard Fat has a β polymorphic form which has a flow point of 37° C. or less.

10 . The composition of claim 1 wherein the Hard Fat is a mixture of glyceride esters of vegetable C 12 -C 18 saturated fatty acids containing at least about 50% triglyceride esters.

11 . The composition of claim 1 wherein the particles of lincosamide have particle size of 10 μm or less.

12 . The composition of claim 1 wherein the Hard Fat base is a Hard Fat NF suppository base having the following properties:

Open-tube melting point:
31.0-33.0° C. (α polymorphic form)

Solidification point:
30.0-32.5° C. (α polymorphic form)

Hydroxyl value
max. 3 mg potassium hydroxide/g

Saponification value:
240-250 mg potassium hydroxide/g

Diglycerides
max. 15% by weight

Monoglycerides
max 1% by weight.

13 . A method of rectally administering a lincosamide to a subject, comprising the steps of:
a) providing a suppository comprising an antimicrobially effective amount of the lincosamide, dispersed in a Hard Fat suppository base, wherein the lincosamide is in the form of particles, wherein the suppository is sufficiently small to pass through the anus of the subject; and b) inserting the rectal suppository into the rectum of the subject, through the anus.

14 . The method of claim 13 , wherein the subject is a mammal.

15 . The method of claim 14 , wherein the mammal is selected from the group consisting of a dog, a cat, a sheep, a cow, a steer, a goat, and a horse.

16 . The method of claim 14 , wherein the mammal is a human being.

17 . The method of claim 13 wherein the lincosamide is selected from the group consisting of lincomycin and pirlimycin.

18 . The method of claim 13 wherein the lincosamide is a clindamycin.

19 . The method of claim 13 , wherein the lincosamide is present in a form selected from the group consisting of a lincosamide salt and a lincosamide ester.

20 . The method of claim 13 , wherein the lincosamide is present in the form of a lincosamide phosphate.

21 . The method of claim 13 , wherein the lincosamide is present in the suppository in an amount from about 0.1% by weight to about 60% by weight of the entire composition.

22 . The method of claim 13 wherein said Hard Fat has a β polymorphic form which has a flow point in the range from 30° C. to 40° C.

23 . The method of claim 13 wherein said Hard Fat has a β polymorphic form which has a flow point of about 37° C. or less.

24 . The method of claim 13 wherein the Hard Fat is a mixture of glyceride esters of vegetable C 12 -C 18 saturated fatty acids containing at least about 50% triglyceride esters.

25 . The method of claim 13 wherein the lincosamide has a particle size of 10 μm or less.

26 . The method of claim 13 wherein the Hard Fat base is a Hard Fat NF suppository base having the following properties:

Open-tube melting point:
31.0-33.0° C. (α polymorphic form)

Solidification point:
30.0-32.5° C. (α polymorphic form)

Hydroxyl value
max. 3 mg potassium hydroxide/g

Saponification value:
240-250 mg potassium hydroxide/g

Diglycerides
max. 15% by weight

Monoglycerides
max 1% by weight.

27 . A method of treating a mammalian subject infected with at least one gram-positive, comprising the steps of:
a) providing a suppository comprising an antimicrobially effective amount of the lincosamide, dispersed in a Hard Fat suppository base, wherein the lincosamide is in the form of particles, wherein the suppository is sufficiently small to pass through the anus of the subject; b) inserting the rectal suppository into the rectum of the subject, through the anus; and c) repeating step (b) until the subject is cured of the infection.

28 . The method of claim 27 , wherein the mammal is a human being.

29 . The method of claim 27 wherein the lincosamide is selected from the group consisting of lincomycin and pirlimycin.

30 . The method of claim 27 wherein the lincosamide is a clindamycin.

31 . The method of claim 27 , wherein the lincosamide is present in a form selected from the group consisting of a lincosamide salt and a lincosamide ester.

32 . The method of claim 27 , wherein the lincosamide is present in the form of a lincosamide phosphate.

33 . The method of claim 27 wherein the Hard Fat has a β polymorphic form which has a flow point in the range from 30° C. to 40° C.

34 . The method of claim 27 wherein the Hard Fat is a mixture of glyceride esters of vegetable C 12 -C 18 saturated fatty acids containing at least about 50% triglyceride esters.

35 . The method of claim 27 wherein the lincosamide has a particle size of 10 μm or less.

36 . The method of claim 27 wherein the Hard Fat base is a Hard Fat NF suppository base having the following properties:

Open-tube melting point:
31.0-33.0° C. (α polymorphic form)

Solidification point:
30.0-32.5° C. (α polymorphic form)

Hydroxyl value
max. 3 mg potassium hydroxide/g

Saponification value:
240-250 mg potassium hydroxide/g

Diglycerides
max. 15% by weight

Monoglycerides
max 1% by weight.

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