Method for preparing powder exhibiting low susceptibility to electrification

• US 20070009444A1
• Filed: 06/02/2004
• Published: 01/11/2007
• Est. Priority Date: 06/04/2003
• Status: Abandoned Application

• Current Assignee: Shionogi & Co., Ltd.
• Original Assignee: Shionogi & Co., Ltd.
• Inventors: Yamaguchi, Hiroshi
• Application Number:
  US10/556,891
• Publication Number:
  US 20070009444A1
• Time in Patent Office: Days
• US Class Current: 424/46
• CPC Class Codes: A61K 31/216 of acids having aromatic rings, e.g. benactizyne, clofibrate
• CPC Class Codes: A61K 9/1641 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 13/12 of the kidneys
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• 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 method of producing lowly-charged powder comprising drying a liquid composition containing a highly-charged compound and polyethyleneglycol.

Claims

1. A method of producing lowly-charged powder comprising drying a liquid composition containing a highly-charged compound and polyethyleneglycol.

3. The method according to claim 1 or 2, wherein an average electric charge of the lowly-charged powder is −

2 q/m or higher.

4. The method according to any one of claims 1 to 3, wherein an average electric charge of the highly-charged compound is less than −

2 q/m.

5. The method according to any one of claims 1 to 4, wherein an absolute value of average electric charge of the lowly-charged powder is not more than one-fourth of an absolute value of average electric charge of the highly-charged compound.

6. The method according to any one of claims 1 to 5, wherein an average electric charge is measured by a particle charge distribution measuring device (voltage 500 V) using a sample mixture of a compound to be measured and iron powder at a ratio of 1:

9.

7. The method according to any one of claims 1 to 6, wherein a bulk density of a lowly-charged powder obtained by drying a liquid composition containing a highly-charged compound and polyethyleneglycol is not less than 1.5 times that of the highly-charged compound.

8. The method according to any one of claims 1 to 7, wherein a weight-average molecular weight of polyethyleneglycol is in the range of 350 to 10500.

9. The method according to any one of claims 1 to 8, wherein a coagulation point of polyethyleneglycol is not less than 4°

C.

10. The method according to any one of claims 1 to 9, wherein the polyethyleneglycol is one or a mixture of two or more selected from a group of polyethyleneglycol 400, polyethyleneglycol 4000 and polyethyleneglycol 600.

11. The method according to any one of claims 1 to 10, wherein an adding amount of the polyethyleneglycol is 0.01 mg to 0.5 mg, relative to 1 mg of the highly-charged compound.

12. The method according to any one of claims 1 to 11, wherein the highly-charged compound is a pharmaceutically active compound.

13. The method according to any one of claims 1 to 12, wherein the drying is spray drying.

15. Powder obtained by the method according to any one of claims 1 to 14.

2. A method of suppressing charge of obtainable powder comprising drying a liquid composition containing a highly-charged compound and polyethyleneglycol.

14. A method of producing powder with reduced charge compared to powder obtained by drying a liquid composition containing a pharmaceutically active compound, by drying a liquid composition containing a pharmaceutically active compound and polyethyleneglycol.

16. Powder containing a compound represented by Formula (I):

wherein R¹ is hydrogen or a metabolic ester residue, R² is hydrogen or -R³-R⁴, provided that R³ is SO₃, CH₂COO, COCOO or COR⁵COO, R⁵ is lower alkylene or lower alkenylene, and R⁴ is hydrogen or a metabolic ester residue, or its pharmaceutically acceptable salt or a solvate thereof, and polyethyleneglycol.

17. Lowly-charged powder obtained by drying a liquid composition containing a compound represented by Formula (I) described in claim 16 or its pharmaceutically acceptable salt or a solvate thereof.

18. A pharmaceutical composition containing powder of claim 16 or 17.

19. A method of producing powder with reduced adhesivity to an apparatus or a vessel by drying a liquid composition containing a highly-charged compound and polyethyleneglycol.

20. Powder with reduced adhesivity to an apparatus or a vessel, produced by drying a liquid composition containing a highly-charged compound and polyethyleneglycol.

21. Powder with reduced adhesivity to an apparatus or a vessel, produced by adding polyethyleneglycol to a compound represented by Formula (I):

wherein R¹ is hydrogen or a metabolic ester residue, R² is hydrogen or -R³-R⁴, provided that R³ is SO₃, CH₂COO, COCOO or COR⁵COO, R⁵ is lower alkylene or lower alkenylene, and R⁴ is hydrogen or a metabolic ester residue, or its pharmaceutically acceptable salt or a solvate thereof.

22. A method of producing a dry composition with suppressed charge by drying a liquid composition containing a pharmaceutically active compound and polyethyleneglycol.

24. The method according to claim 22 or 23, wherein the drying is spray drying.

23. A method of suppressing charge of an obtained dry composition by drying a liquid composition containing a pharmaceutically active compound and polyethyleneglycol.