Compositions and dosage forms for enhanced absorption

• US 20060094782A9
• Filed: 10/29/2004
• Published: 05/04/2006
• Est. Priority Date: 10/31/2003
• Status: Abandoned Application

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Wong, Patrick S.L., Yan, Dong, Guittard, George V.
• Application Number:
  US10/978,139
• Publication Number:
  US 20050165102A1
• Time in Patent Office: Days
• US Class Current: 514/553
• 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 31/155 Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
• CPC Class Codes: A61K 31/185 Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids hydroxamic acids A61K31/16; peroxy acids A61K31/327
• CPC Class Codes: A61K 31/195 having an amino group
• CPC Class Codes: A61K 31/197 the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid carnitine A61K31/205
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/20 having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
• CPC Class Codes: A61K 31/295 Iron group metal compounds
• CPC Class Codes: A61K 31/66 Phosphorus compounds
• CPC Class Codes: A61K 31/662 Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
• CPC Class Codes: A61K 33/26 Iron; Compounds thereof
• CPC Class Codes: A61K 47/541 Organic ions forming an ion pair complex with the pharmacologically or therapeutically active agent
• CPC Class Codes: A61K 47/585 Ion exchange resins, e.g. polystyrene sulfonic acid resin
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/06 : Antianaemics

Abstract

Disclosed is controlled delivery of pharmaceutical agents and methods, dosage forms and devices therefore. In particular, formulation, dosage forms, methods and devices for enhanced absorption and controlled delivery drug compounds are disclosed.

Claims

1. A substance comprising:

a complex that comprises a drug moiety, and a transport moiety.

2. The substance of claim 1, wherein the transport moiety comprises an acidic, a basic, or a zwitterionic structural element;

or an acidic, a basic, or a zwitterionic residual structural element paired with an ion to form a salt.

3. The substance of claim 2, wherein the transport moiety comprises fatty acids or its salts, benzenesulfonic acid or its salts, benzoic acid or its salts, fumaric acid or its salts, or salicylic acid or its salts.

4. The substance of claim 3, wherein the fatty acids or its salts comprises a C6-C18 fatty acid or its salt.

5. The substance of claim 4, wherein the C6-C18 fatty acid or its salt comprises a C12 fatty acid or its salt.

6. The substance of claim 2, wherein the transport moiety comprises an alkyl sulfate or its salt.

7. The substance of claim 6, wherein the alkyl sulfate or its salt comprises a C6-C18 sodium alkyl sulfate or its salt.

8. The substance of claim 7, wherein the C6-C18 sodium alkyl sulfate or its salt comprises sodium lauryl sulfate.

9. The substance of claim 2, wherein the transport moiety comprises a pharmaceutically acceptable primary, secondary, or tertiary amine, or salts thereof.

10. The substance of claim 1, wherein the drug moiety comprises an acidic, a basic, or a zwitterionic structural element;

or an acidic, a basic, or a zwitterionic residual structural element paired with an ion to form a salt.

11. A composition comprising the substance of claim 1 and an inactive ingredient.

12. A dosage form comprising the composition of claim 11.

13. A method of treating a disease or condition comprising:

administering the substance of claim 1 to a patient need thereof.

14. The method of claim 13, wherein the substance is administered via an oral, intravenous, subcutaneous, intramuscular, transdermal, intraarterial, intraarticular, or intradermal route.

15. A method of making a composition comprising:

providing a drug moiety in an ionic form;

providing a transport moiety in an ionic form;

combining the drug moiety and the transport moiety, in the presence of a solvent having a dielectric constant less than that of water, to form a complex; and

separating the complex from the solvent.

16. The method of claim 15, wherein the transport moiety comprises an acidic, a basic, or a zwitterionic structural element;

or an acidic, a basic, or a zwitterionic residual structural element paired with an ion to form a salt.

17. The method of claim 15, wherein the drug moiety comprises an acidic, a basic, or a zwitterionic structural element;

or an acidic, a basic, or a zwitterionic residual structural element paired with an ion to form a salt.

18. The method of claim 17, wherein the drug moiety comprises an acidic structural element or an acidic residual structural element;

and the drug moiety is processed to obtain the acid form of the drug moiety.

19. The method of claim 17, wherein the drug moiety comprises a basic structural element or a basic residual structural element;

and the drug moiety is processed to obtain the basic form of the drug moiety.

20. The method of claim 15, wherein the drug moiety comprises a zwitterionic structural element or zwitterionic residual structural element;

and a non-bonding structural element or residual structural element of the zwitterionic structural element or zwitterionic residual structural element is blocked before reacting the drug moiety and the transport moiety.

21. A method of treatment comprising:

providing a drug moiety in an ionic form;

providing a transport moiety in an ionic form;

combining the drug moiety and the transport moiety, in the presence of a solvent having a dielectric constant less than that of water, to form a complex;

separating the complex from the solvent; and

administering the separated complex to a patient in need thereof.

22. The method of claim 21, wherein the transport moiety comprises an acidic, a basic, or a zwitterionic structural element;

or an acidic, a basic, or a zwitterionic residual structural element paired with an ion to form a salt.

23. The method of claim 21, wherein the drug moiety comprises an acidic, a basic, or a zwitterionic structural element;

or an acidic, a basic, or a zwitterionic residual structural element paired with an ion to form a salt.

24. The method of claim 23, wherein the drug moiety comprises an acidic structural element or an acidic residual structural element;

and the drug moiety is processed to obtain the acid form of the drug moiety.

25. The method of claim 23, wherein the drug moiety comprises a basic structural element or a basic residual structural element;

and the drug moiety is processed to obtain the basic form of the drug moiety.

26. The method of claim 23, wherein the drug moiety comprises a zwitterionic structural element or zwitterionic residual structural element;

and a non-bonding structural element or residual structural element of the zwitterionic structural element or zwitterionic residual structural element is blocked before reacting the drug moiety and the transport moiety.

27. The method of claim 21, wherein the complex is administered via an oral, intravenous, subcutaneous, intramuscular, transdermal, intraarterial, intraarticular, or intradermal route.

28. A method of improving absorption of a drug moiety comprising:

providing a complex of the drug moiety and a transport moiety; and

administering the complex to a patient in need thereof.

29. The method of claim 28, wherein the complex is administered orally, and the improved absorption comprises improved oral absorption.

30. The method of claim 29, wherein the improved oral absorption comprises improved lower gastrointestinal tract absorption.

31. The method of claim 29, wherein the improved oral absorption comprises improved upper gastrointestinal tract absorption.

32. The method of claim 28, wherein the complex is administered transdermally, and the improved absorption is improved transdermal absorption.

33. The method of claim 28, wherein the complex is administered subcutaneously, and the improved absorption is improved subcutaneous absorption.