Polyethylene glycol coating for electrostatic dry deposition of pharmaceuticals

• US 20020102308A1
• Filed: 01/29/2002
• Published: 08/01/2002
• Est. Priority Date: 12/16/1998
• Status: Abandoned Application

• Current Assignee: Herling Uang, Shifeng Bill Wei
• Original Assignee: Herling Uang, Shifeng Bill Wei
• Inventors: Uang, Herling, Wei, Shifeng Bill
• Application Number:
  US10/059,635
• Publication Number:
  US 20020102308A1
• Time in Patent Office: Days
• US Class Current: 424/486
• CPC Class Codes: A61K 9/2086 Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat active cores with a complete drug-free outer coat A61K9/28
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00

Abstract

The invention relates to a substrate coating for the electrostatic deposition of dry powder medicaments for use in the manufacture of pharmaceutical dosage forms comprising micronized polyethylene glycol (PEG), with A molecular weight in the range of 1,000 to 20,000, and having a particle size of 1-100 μm. The invention also relates to pharmaceutical compositions having such a substrate coating, and processes for manufacturing such pharmaceutical compositions. The invention also relates to the technology of reversing negative charge of medicaments so that they can be electrostatically deposited on a negatively charged substrate.

Claims

1. A substrate coating for the electrostatic deposition of dry powder medicaments for use in the manufacture of pharmaceutical dosage forms comprising micronized polyethylene glycol (PEG), with molecular weight in the range of 1,000 to 20,000, and having a particle size of 1-100 μ

m.

2. The substrate coating of claim 1 having a melting point in the range of 50-63°

C.

3. The substrate coating of claim 1 wherein the PEG has a molecular weight in the range of 6,000-8,000.

4. The substrate coating of claim 1 also containing a plasticizer.

5. The substrate coating of claim 4 wherein the plasticizer is selected from castor oil, polyethylene glycol, propylene glycol or glycerine.

6. The substrate coating of claim 1 also containing one or more coloring, pacifying, flavoring and/or sweetening agents.

7. A pharmaceutical composition comprising an edible substrate having micronized drug substance with a particle size of 1-100 μ

m deposited on the surface of the substrate by electrostatic dry powder deposition, and a film coating on the substrate and drug substance consisting essentially of micronized polyethylene glycol (PEG), with molecular weight in the range of 1,000 to 20,000, and having a particle size of 1-100 μ

m.

8. The pharmaceutical composition of claim 7 wherein the film coating has a melting point in the range of 50-63°

C.

9. The pharmaceutical composition of claim 7 wherein the PEG has a molecular weight in the range of 6,000-8,000.

10. The pharmaceutical composition of claim 7 wherein the PEG film coating (dried) constitutes from about 1 to about 10, percent by weight of the total weight of the solid dosage form.

11. The pharmaceutical composition of claim 7 wherein the edible substrate is comprised of a tablet core.

12. The pharmaceutical composition of claim 8 wherein the tablet core is prepared by compressing a mixture of microcrystalline cellulose (99-99.5%) and magnesium stearate (0.5-1%).

13. The pharmaceutical composition of claim 7 wherein the drug substance is selected from one or more estrogens and/or progestins.

14. The pharmaceutical composition of claim 13 wherein the drug substance is a combination of norgestimate and ethinyl estradiol.

17. The method according to claim 16 wherein the PEG has a molecular weight in the range of 1,000 to 20,000 and a particle size of 1-100 μ

m.

18. The method according to claim 16 wherein the PEG has a melting point in the range of 50-63°

C.

19. The method according to claim 16 wherein the PEG has a molecular weight in the range of 6,000 to 8,000.

15. In a process for manufacturing pharmaceutical unit dosage forms by the electrostatic deposition of dry powder medicament to a substrate, the improvement comprising coating the substrate in place with dry micronized polyethylene glycol (PEG), melting the dry polyethylene glycol coating and allowing it to cool whereupon a protective coating is formed.

16. A method of depositing negatively charged dry powder medicament on a negatively charged substrate by an electrostatic dry powder deposition process, the method comprising reversing the charge of the medicament to a positive charge by mixing the negatively charged medicament with micronized polyethylene glycol (PEG), at the ratio of medicament to PEG of 1:

1 to 1;

60, and then depositing the mixture onto the negatively charged substrate.