Formulations and methods of manufacturing formulations for use in colonic evacuation

• US 10,166,219 B2
• Filed: 07/26/2013
• Issued: 01/01/2019
• Est. Priority Date: 07/27/2012
• Status: Active Grant

• Current Assignee: RedHill Biopharma Ltd.
• Original Assignee: RedHill Biopharma Ltd.
• Inventors: Fathi, Reza, McLean, Patrick Laughlin
• Primary Examiner(s): Cohen, Michael P
• Application Number:
  US14/417,172
• Publication Number:
  US 20150272937A1
• Time in Patent Office: 1,985 Days
• Field of Search: None
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/185 Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids hydroxamic acids A61K31/16; peroxy acids A61K31/327
• CPC Class Codes: A61K 31/375 Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/4402 only substituted in position 2, e.g. pheniramine, bisacodyl
• CPC Class Codes: A61K 33/08 Oxides; Hydroxides
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• 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
• CPC Class Codes: A61K 9/28 Dragees; Coated pills or tablets , e.g. with film or compression coating A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209
• CPC Class Codes: A61K 9/2893 Tablet coating processes mechanical aspects A61J3/06
• CPC Class Codes: A61P 1/10 Laxatives

Abstract

Formulations and methods of manufacturing formulations for use in colonic evacuation are disclosed herein, in an embodiment, a solid dosage formulation includes an intra-granular fraction intermingled with an extra-granular fraction, wherein the intra-granular fraction includes granules comprising at least one osmotic evacuant agent, at least one antacid, and a first pharmaceutically acceptable excipient component, and wherein the extra-granular fraction includes one or more organic acids, a non-metallic lubricating element, and a second pharmaceutically acceptable excipient component.

Claims

1. A coated tablet, comprising:

an intra-granular fraction combined with an extra-granular fraction, and a coating layer,

wherein the intra-granular fraction includes granules comprising micronized sodium picosulfate, microcrystalline cellulose, magnesium oxide, and crospovidone, and wherein the intra-granular fractions excludes sodium starch glycolate,

wherein the extra-granular fraction includes one or more organic acids, microcrystalline cellulose, and crospovidone, and wherein the extra-granular fraction excludes sodium starch glycolate and magnesium stearate,

wherein the organic acid is one of ascorbic acid, citric acid, tartaric acid, or combinations thereof, and

wherein the coating layer delays dissolution beyond the mouth of a patient.

2. The coated tablet of claim 1 wherein the intra-granular fraction comprises about 50% of the total weight of the formulation, and wherein the extra-granular fraction comprises about 50% of the total weight of the formulation.

3. The coated tablet of claim 1 wherein the at least one organic acid is ascorbic acid.

4. The coated tablet of claim 1, wherein the coated tablet shows no signs of degradation at 16 weeks.

5. The coated tablet of claim 1, further comprising silicon dioxide.