Delayed release carnitine

• US 20030170290A1
• Filed: 03/07/2003
• Published: 09/11/2003
• Est. Priority Date: 06/16/1993
• Status: Abandoned Application

• Current Assignee: Austin L. Shug, Carl E. Gulbrandsen
• Original Assignee: Austin L. Shug, Carl E. Gulbrandsen
• Inventors: Shug, Austin L., Gulbrandsen, Carl E.
• Application Number:
  US10/384,085
• Publication Number:
  US 20030170290A1
• Time in Patent Office: Days
• US Class Current: 424/428
• 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 31/205 Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/5026 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5042 Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose

Abstract

A sustained release, orally administered pharmaceutical composition comprising carnitine and an acceptable pharmaceutical excipient is described for the treatment of carnitine deficiency and other carnitine responsive conditions. The sustained release formulation avoids the characteristic problems of gastrointestinal invitation, dumping in the urine and bacterial degradation attendant previously known oral formulations of carnitine.

Claims

1. A sustained release oral medicament for administration to a human being, said human being having gastrointestinal fluid, said medicament comprising:

(a) a unitary dosage amount of carnitine;

(b) a means for slowly releasing said carnitine from said medicament upon exposure of said medicament to gastrointestinal fluid;

(c) an acceptable pharmaceutical excipient.

2. A sustained release oral medicament as claimed in claim 1, wherein said carnitine is slowly released over a period of time greater than two hours upon exposure to gastrointestinal fluid.

3. A sustained release oral medicament as claimed in claim 1, wherein said carnitine is L-carnitine.

4. A sustained release oral medicament as claimed in claim 1, wherein said carnitine is gamma-butyrobetaine.

5. A sustained release oral medicament as claimed in claim 1, wherein said means for slowly releasing said carnitine comprises a slowly water permeable polimerisation product which coats said carnitine.

6. A sustained release oral medicament for administration to a human being, said human being having gastrointestinal fluid, said medicament comprising:

(a) a unitary dosage amount of carnitine;

(b) a slowly water permeable polimerisation product coating said carnitine;

(c) an acceptable pharmaceutical excipient.

7. A sustained release oral medicament as claimed in claim 6, wherein said carnitine is released over a period of time greater than two hours upon exposure to gastrointestinal fluid.

8. A sustained release oral medicament as claimed in claim 6, wherein said carnitine is L-carnitine.

9. A sustained release oral medicament as claimed in claim 6, wherein said carnitine is gamma-butyrobetaine.

10. A sustained release oral medicament as claimed in claim 6, wherein said means for slowly releasing said carnitine comprises a slowly water permeable polimerisation product which coats said carnitine.

11. A sustained release oral medicament as claimed in claim 6, further comprising a unitary dosage amount of DHEA.

12. A method of preventing gastrointestinal irritation associated with oral administration of carnitine, comprising the steps of:

(a) granulating said carnitine;

(b) coating said granulated carnitine with a slowly water permeable polimerisation product so as to form coated carnitine;

(c) incorporating a unit dosage amount of said coated carnitine and an acceptable pharmaceutical excipient into an oral medicament;

(d) orally administering said medicament.

13. A method for treating and preventing osteoporosis, comprising the step of:

orally administering daily in a sustained release formulation an effective amount of L-carnitine and DHEAS along with an acceptable pharmaceutical excipient.

14. A method for treating and preventing osteoporosis as claimed in claim 13, wherein said sustained release formulation