Novel Method

• US 20140066516A1
• Filed: 11/06/2013
• Published: 03/06/2014
• Est. Priority Date: 07/30/2008
• Status: Abandoned Application

• Current Assignee: GlaxoSmithKline LLC (GlaxoSmithKline PLC)
• Original Assignee: GlaxoSmithKline LLC (GlaxoSmithKline PLC)
• Inventors: Clarke, Geoffrey Douglas, Grattan, Timothy James, Burnett, Ian
• Application Number:
  US14/073,038
• Publication Number:
  US 20140066516A1
• Time in Patent Office: Days
• US Class Current: 514/629
• 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 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention is directed to a novel method for reducing intrapatient variability in pharmaceutically active agent which is suitably not absorbed in the stomach, such as paracetamol, containing formulations in patients having gastric dysmotility, or a method of improving analgesia in a diabetic patient, or improving absorption of an active agent is a patient with gastric dysmotility, which methods comprises administering orally to said patient in need thereof a pharmaceutical dosage form comprising a first active agent, calcium carbonate, at least one first binding agent, and at least one disintegrating agent as intragranular components in the form of a granulate, and as an extragranular component at least one hydrophilic colloid, an optionally a second binding agent, calcium carbonate, a super disintegrant, and a second active agent.

Claims

1. A method for improving analgesia in a diabetic comprising administering to said patient in need thereof an orally administered pharmaceutical dosage comprising a first active agent which is paracetamol present in an amount of about 60 to about 80% by weight, calcium carbonate present in an amount of about 5 to about 20% by weight, at least one first binding agent, and at least one disintegrating agent as intragranular components in the form of a granulate, and as an extragranular component at least one hydrophilic colloid.

2. A method for improving absorption of paracetamol in a patient with gastric dysmotility comprising administering to said patient in need thereof an orally administered pharmaceutical dosage comprising a first active agent which is paracetamol present in an amount of about 60 to about 80% by weight, calcium carbonate present in an amount of about 5 to about 20% by weight, at least one first binding agent, and at least one disintegrating agent as intragranular components in the form of a granulate, and as an extragranular component at least one hydrophilic colloid, an optionally a second binding agent, calcium carbonate, super disintegrant, and a second active agent.

3. A method for improving analgesia in a diabetic comprising administering to said patient in need thereof an orally administered pharmaceutical dosage comprising

a) paracetamol;

b) at least one agent which contributes to dissolution selected from sodium carbonate, ammonium carbonate, sodium bicarbonate, potassium bicarbonate, calcium carbonate, magnesium carbonate, disodium glycine carbonate, sodium glycine carbonate, lysine carbonate, arginine carbonate, or combinations of two or more of the above;

c) at least one water uptake agent selected from cross-linked polyvinylpyrrolidone (crospovidone), croscarmellose sodium, sodium starch glycolate, povidone, starch, starch derivatives, low substituted hydroxypropylcellulose, hydroxypropylcellulose, alginic acid, sodium alginate, calcium sulfate, calcium carboxymethylcellulose, microcrystalline cellulose, powdered cellulose, colloidal silicon dioxide, docusate sodium, guar gum, magnesium aluminum silicate, methylcellulose, polacrilin potassium, silicified microcrystalline cellulose, magnesium oxide, tragacanth, mannitol, sorbitol, xylitol, sucrose, lactose, fructose, maltose, polyethylene glycol, amino acids, cyclodextrin, urea and/or polyvinylpyrrolidone; and

wherein at least 70 of the paracetamol is dissolved from the formulation within 180 seconds in USP dissolution apparatus 2 with 900 ml of 0.05 N hydrochloric acid at 30 rpm and 37°

C.