Solid preparation having improved solubility

• US 8,133,513 B2
• Filed: 03/20/2007
• Issued: 03/13/2012
• Est. Priority Date: 03/23/2006
• Status: Expired due to Fees

• Current Assignee: Shionogi & Co., Ltd.
• Original Assignee: Shionogi & Co., Ltd.
• Inventors: Hayashi, Takashi, Takakura, Asako
• Primary Examiner(s): Wax, Robert A
• Assistant Examiner(s): AL-AWADI, DANAH J
• Application Number:
  US12/294,036
• Publication Number:
  US 20090105312A1
• Time in Patent Office: 1,820 Days
• Field of Search: None
• US Class Current: 424/488
• CPC Class Codes: A61K 31/4422 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• 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: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives

Abstract

A preparation which can improve the dissolution property of a poorly water soluble drug even when the drug is contained in the preparation at a high content is provided.

When an addition amount of nicotinic acid amide and/or urea is 0.1 to 10% by weight in a solid preparation containing a poorly water soluble drug, and a water-soluble polymer, even a poorly water soluble drug, particularly a drug having a high content can be dissolved out from the preparation by an almost all amount.

Claims

1. A solid preparation comprising 20 to 50% by weight of a drug, 0.1 to 10% by weight of nicotinic acid amide and/or urea, and a water-soluble polymer.

2. The solid preparation according to claim 1, wherein the content of nicotinic acid amide and/or urea is 2 to 7% by weight.

3. The solid preparation according to claim 1, wherein solubility in water of the drug is not more than 100 μ

g/mL.

4. The solid preparation according to claim 1, wherein the water-soluble polymer is one or more selected from the group consisting of polyvinylpyrrolidone, water-soluble cellulose, polyvinyl alcohol, polyvinyl acetate, gelatin, agar, sodium alginate, pectin, pullulan, gum xanthan, gum arabic, chondroitin sulfate, hyaluronic acid and carrageenan.

5. The solid preparation according to claim 4, wherein the water-soluble cellulose is one or more selected from the group consisting of hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate and carboxymethylcellulose sodium.

6. The solid preparation according to claim 4, wherein the water-soluble polymer is polyvinylpyrrolidone and/or hydroxypropylmethylcellulose acetate succinate.

8. The solid preparation according to claim 1, wherein the water-soluble polymer is polyvinylpyrrolidone.

9. The solid preparation according to claim 2, wherein the water-soluble polymer is polyvinylpyrrolidone.

12. The solid preparation according to claim 1 that comprises nicotinic acid amide.

13. The solid preparation according to claim 8 that comprises nicotinic acid amide.

7. A method for improving solubility of a drug comprising preparing a solid composition comprising 20 to 50% by weight of the drug, 0.1 to 10% by weight of nicotinic acid amide and/or urea, and a water-soluble polymer.

10. A solid preparation comprising about 30% by weight of a drug, 63 to 68% by weight of a water-soluble polymer, and 2 to 7% by weight of nicotinic acid amide.

11. The solid preparation according to claim 10, wherein the water-soluble polymer is polyvinylpyrrolidone.