Polyethylene glycol coating for electrostatic dry deposition of pharmaceuticals

• US 6,372,246 B1
• Filed: 12/16/1998
• Issued: 04/16/2002
• Est. Priority Date: 12/16/1998
• Status: Expired due to Term

• Current Assignee: Ortho-McNeil Pharmaceutical Incorporated (Johnson & Johnson)
• Original Assignee: Ortho-McNeil Pharmaceutical Incorporated (Johnson & Johnson)
• Inventors: Wei, Shifeng Bill, Uang, Herling
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Seidleck, Brian K.
• Application Number:
  US09/212,886
• Time in Patent Office: 1,217 Days
• Field of Search: 424/439, 424/441, 424/489, 424/464, 106/244, 427/2.14, 427/472
• US Class Current: 424/439
• 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 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 polyethylene glycol, wherein the film coating is applied by;

(a) coating the substrate in place by electrostatic dry powder deposition with dry micronized polyethylene glycol having a molecular weight in the range of 1,000 to 20,000 and having a particle size of 1-100 μ

m, and

(b) melting the dry polyethylene glycol coating and allowing it to cool whereupon a protective coating is formed.

2. The pharmaceutical composition of claim 1 wherein the film coating has a melting point in the range of 50-63°

C.

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

4. The pharmaceutical composition of claim 1 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.

5. The pharmaceutical composition of claim 1 wherein the edible substrate is comprised of a tablet core.

6. The pharmaceutical composition of claim 2 wherein the tablet core is prepared by compressing a mixture of microcrystalline cellulose (99-99.5%) and magnesium stearate (0.5-1%).

7. The pharmaceutical composition of claim 1 wherein the drug substance is selected from one or more estrogens and/or progestins.

8. The pharmaceutical composition of claim 7 wherein the drug substance is a combination of norgestimate and ethinyl estradiol.