Contrast media containing liposomes as carriers

• US 4,192,859 A
• Filed: 09/29/1978
• Issued: 03/11/1980
• Est. Priority Date: 09/29/1978
• Status: Expired due to Term

• Current Assignee: Bracco International B.V. (Bracco SPA)
• Original Assignee: E R Squibb & Sons Incorporated
• Inventors: Mackaness, George B., Hou, Joseph P.
• Primary Examiner(s): Waddell, Frederick E.
• Application Number:
  US05/946,976
• Time in Patent Office: 529 Days
• Field of Search: 424/4, 424/5
• US Class Current: 424/9.45
• CPC Class Codes: A61K 49/0466 Liposomes, lipoprotein vesicles, e.g. HDL or LDL lipoproteins, phospholipidic or polymeric micelles
• CPC Class Codes: Y10S 424/90 In vivo diagnostic or in vivo test agent which contains an additional ingredient to reduce the toxicity or side effects of the active ingredient

Abstract

X-Ray contrast media are provided containing an X-ray contrast agent such as N,N'"'"'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide, sodium diatrizoate, meglumine diatrizoate, sodium iodipamide, meglumine iodipamide and the like, and a liposome as a carrier therefor.

Claims

1. An X-ray contrast medium comprising an X-ray contrast agent and a liposome as a carrier therefor, said liposome comprising a lecithin and a sterol, said X-ray contrast agent being present in an amount within the range of from about 20 to about 60% by weight of said contrast medium.

2. The X-ray contrast medium as defined in claim 1 wherein said X-ray contrast agent is selected from the group consisting of N,N'"'"'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide, metrizamide, diatrizoic acid, sodium diatrizoate, meglumine diatrizoate, acetrizoic acid and its soluble cationic salts, meglumine iocarmate, sodium iodipamide meglumine iodipamide, iodamide, iodohippuric acid and its soluble salts, diprotrizoic acid and its salts, iodomethamic acid, 3,5-diiodo-4-pyridone-N-acetic acid (iodopyracet), 3,5-diiodo-4-pyridone-N-acetic acid diethanolamine salt, iodo-2-pyridone-N-acetic acid and its amine salts, ioglycamic acid, iothalamic acid and its soluble salts, methanesulfonic acid, metrizoic acid, sodium metrizoate, sodium ipodate, ethiodized oil, iocetamic acid, iopanoic acid, tyropanoate sodium, iopydol, iophenoxic acid, and iophendylate, and mixtures thereof.

3. The X-ray contrast medium as defined in claim 2 wherein said X-ray contrast agent is N,N'"'"'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide.

4. The X-ray contrast medium as defined in claim 2 wherein said X-ray contrast agent is sodium diatrizoate.

5. The X-ray contrast medium as defined in claim 2 wherein said X-ray contrast agent is meglumine diatrizoate.

6. The X-ray contrast medium as defined in claim 2 wherein said X-ray contrast agent is meglumine iodipamide.

7. The X-ray contrast medium as defined in claim 1 wherein said lecithin comprises egg or soy lecithin.

8. The X-ray contrast medium as defined in claim 7 wherein said sterol is selected from the group consisting of cholesterol, phytosterol, sitosterol, sitosterol pyroglutamate, 7-dehydrocholesterol, lanosterol and mixtures thereof.

9. The X-ray contrast medium as defined in claim 7 wherein said sterol is cholesterol.

10. The X-ray contrast medium as defined in claim 7 wherein said liposome further includes dicetyl phosphate.

11. The X-ray contrast medium as defined in claim 7 wherein said liposome further includes hexadecylamine.

12. A method for the X-ray visualization of body cavities and organs, which comprises administering to the body of the test object an effective contrast producing amount of an X-ray contrast medium as defined in claim 1.

13. The method as defined in claim 11 wherein the liver is visualized.

14. The method as defined in claim 11 wherein the spleen is visualized.

15. The method as defined in claim 11 wherein the gall bladder is visualized.

16. The method as defined in claim 11 wherein the spinal cord is visualized.

17. A method as defined in claim 11 wherein the X-ray contrast agent employed is N,N'"'"'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide.

18. The method for the X-ray visualization of lymphatic channels, which comprises administering to the body of the test object an effective contrast producing amount of an X-ray contrast medium as defined in claim 1.

19. A method as defined in claim 14 wherein the X-ray contrast agent is N,N'"'"'-bis-[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide.

20. A method for the radiographic examination of the gastrointestinal tract, which comprises administering to the body of the test object an effective contrast producing amount of an X-ray contrast medium as defined in claim 1.

21. The X-ray contrast medium as defined in claim 1 where in said liposome carrier, said lecithin is present in an amount of from about 50 to about 85% by weight and said sterol is present in an amount of from about 10 to about 35% by weight.

22. The X-ray contrast medium as defined in claim 21 wherein said liposome carrier further includes dicetyl phosphate present in an amount of from 0 to about 30% by weight of said liposome carrier.