Compositions and methods for administering therapeutically active compounds

• US 5,070,085 A
• Filed: 04/06/1990
• Issued: 12/03/1991
• Est. Priority Date: 04/10/1987
• Status: Expired due to Term

• Current Assignee: The Ester C Co.
• Original Assignee: Oxycal Laboratories, Inc. (TOLMAR Holding, Inc.)
• Inventors: Markham, Richard G.
• Primary Examiner(s): Waddell, Frederick E.
• Assistant Examiner(s): Henley, III., Raymond J.
• Application Number:
  US07/459,806
• Time in Patent Office: 606 Days
• Field of Search: 514/165, 514/226.5, 514/473, 514/946, 514/161, 514/784, 514/785, 514/77
• US Class Current: 514/161
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/365 Lactones
• CPC Class Codes: A61K 31/375 Ascorbic acid, i.e. vitamin C; Salts thereof

Abstract

A composition useful for administering therapeutically active compounds to improve the body absorption and/or retention thereof comprising a composition includes a therapeutically active compound having a molecular weight below about 5,000, having an acidic functional group and a pKa of ≦6 at pH 7.4 normally eliminated unmetabolized from the body via the renal tubular secretion pathway for organic anions, for example, Vitamin C, and at least one compound selected from the class consisting of L-threonic, L-xylonic and L-lyxonic acids, and the edible salts, aldono-lactones and aldono-lactides thereof.

A method for establishing and maintaining body levels of a therapeutically active compound includes the step of administering a therapeutically effective dose of this composition.

Claims

1. A therapeutic composition, said composition comprising:

(a) an effective amount of a therapeutically active compound, said compound having

(i) a molecular weight below about 5,000,

(ii) an acidic functional group and a pKa of ≦

6 at physiological pH=7.4, and

(iii) which is normally eliminated unmetabolized via the renal tubular secretion pathway for organic anions;

and

(b) at least one compound selected from the group consisting of L-threonic, L-xylonic and L-lyxonic acids, and the edible non-toxic salts, aldono-lactones and aldono-lactides thereof, in an amount effective to increase the body absorption rate of said active compound.

2. The composition of claim 1 wherein said active compound is piroxicam.

3. The composition of claim 1 in which said active compound is aspirin.

4. The composition of claim 1 in which said compound of subparagraph (b) is present in an amount effective to reduce the body elimination rate of said active compound.

12. A treatment method for improving the effectiveness of a therapeutically active compound, said compound having

a molecular weight below about 5,000,

an acidic functional group and a pKa of ≦

6 at physiological pH=7.4, and

which is normally eliminated unmetabolized via the renal tubular secretion pathway for organic anions,

said method comprising, in sequence, the step of;

(a) administering to a subject at least one compound selected from the group consisting of L-threonic, L-xylonic and L-lyxonic acids, and the edible non-toxic salts, aldono-lactones and aldono-lactides thereof to establish a concentration thereof in the subject in an amount sufficient to improve the effectiveness of said active compound; and

(b) thereafter administering to said subject the composition of claim 1.

13. The method of claim 12 in which said active compound is piroxicam.

14. The method of claim 12 in which the compound of subparagraph (a) is administered in an amount to establish a concentration thereof in the subject effective to reduce the body elimination rate of said active compound.

5. A Vitamin C composition, said composition comprising:

(a) an effective amount of a compound having Vitamin C activity, selected from the group consisting of (i) dehydroascorbic acid, (ii) L-ascorbic acid and the edible salts thereof;

and

(b) at least one compound selected from the group consisting of the aldono-lactones of L-threonic acid, L-xylonic acid, L-lyxonic acid and the edible salts of L-threonic acid, L-xyonic acid and L-lyxonic acids, in an amount effective to increase the human body absorption rate of said Vitamin C compound.

6. The composition of claim 5 in which the amount of aldonic compound is effective to increase the absorption rate of said Vitamin C compound.

7. The composition of claim 5 in which the amount of aldonic compound is effective to decrease the excretion rate of said Vitamin C compound.

15. A method for establishing high Vitamin C levels in the human body which comprise the step of orally administering to a subject an effective amount of the composition of claim 5.

16. The method of claim 15 in which the amount of aldonic compound is affective to increase the absorption rate of said Vitamin C compound.

17. The method of claim 15 in which the amount of aldonic compound is effective to decrease the excretion rate of said Vitamin C compound.

8. A method for improving the effectiveness of a therapeutically active compound, said compound having

a molecular weight below about 5,000,

an acid functional group and a pKa of ≦

6 at physiological pH=7.4, and

which is normally eliminated unmetabolized via the renal tubular secretion pathway for organic anions,

said method consisting of the step of administering to a subject an effective dose of a composition comprising;

(a) an effective amount of a therapeutically active compound;

and

(b) at least one compound selected from the group consisting of L-threonic acid, L-lyxonic acids, and the edible non-toxic salts, aldono-lactones and aldono-lactides thereat, in an amount effective to increase the body absorption rate of said active compound.

9. The method of claim 8 in which said active compound is piroxicam.

10. The method of claim 8 in which said active compound is aspirin.

11. The method of claim 8 in which the compound of subparagraph (b) is present in an amount effective to reduce the body elimination rate of said active compound.

18. A method of suppressing the excretion of organic anions via the renal tubular secretion pathway comprising the step of establishing an effective blood concentration of a compound selected from the group consisting of L-threonic, L-xylonic and L-lyxonic acids, and the edible non-toxic salts, aldono-lactones and aldono-lactides thereof.

19. A method of improving the absorption of organic anions in body tissue comprising the step of establishing an effective blood concentration of a compound selected from the groups consisting of L-threonic, L-xylonic and L-lyxonic acids, and the edible non-toxic salts, aldon-lactones and aldon-lactides thereof.