SOFT GELATIN CAPSULES WITH pH-INDEPENDENT RELEASE

• US 20180353432A1
• Filed: 11/25/2016
• Published: 12/13/2018
• Est. Priority Date: 12/09/2015
• Status: Active Grant

• Current Assignee: Altergon SA
• Original Assignee: Altergon SA
• Inventors: Carucci, Simone, Marchiorri, Maurizio, Pontiggia, Marco, Fossati, Tiziano
• Granted Patent: US 11,304,910 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• 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 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/40 Cyclodextrins; Derivatives thereof
• CPC Class Codes: A61K 9/4825 Proteins, e.g. gelatin gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds

Abstract

Disclosed are soft gelatin capsules comprising a gelatin shell, a plasticiser, water, and optionally a calcium salt and a filling containing a dispersed or solubilised medicament comprising gelatin with gelling power, hydrolysed gelatin, glycerol, water, pectin and gellan gum. The formulations according to the invention allow gradual release of the active ingredient, regardless of pH.

Claims

1. Soft gelatin capsules comprising a gelatin shell, a plasticiser, water and optionally a calcium salt and a filling containing a dispersed or solubilised medicament comprising gelatin having gelling power, hydrolysed gelatin, glycerol, water, pectin and gellan gum.

2. A capsule according to claim 1 wherein the active ingredient can be dispersed or solubilised by means of ethanol or other hydrophilic or lipophilic solvents, and/or complexed with cyclodextrin.

3. A capsule according to claim 1 wherein the shell contains calcium chloride.

4. A capsule according to claim 1 wherein the gelatin in the hydrophilic filling has Bloom values ranging from 60 to 150.

5. A capsule according to claim 1 wherein the active ingredients are selected from non-steroidal anti-inflammatory drugs, thyroid hormones, statins, bronchodilators, antihistamines, steroids and derivatives thereof, narcotic analgesics, antibacterials/antivirals, vitamins, oils of various kinds, glycosaminoglycans, antimycotics, proton pump inhibitors, fertility hormones, corticosteroids, erectile dysfunction medicaments, and anticoagulants.

6. A capsule according to claim 1 wherein the shell contains from 20 to 45% of gelatin having a Bloom value ranging from 110 to 300, plasticiser from 15 to 30%, water from 30 to 40% and optionally a calcium salt, the percentages being on the total shell weight.

7. A capsule according to claim 6 wherein the calcium salt is calcium chloride.

8. A capsule according to claim 7 wherein calcium chloride is present in percentages by weight ranging from 0.5 to 5% on the total shell weight.

9. A capsule according to claim 1 wherein the plasticiser is selected from glycerol, sorbitol, sorbitol/sorbitan mixtures, 1,2 propylene glycol, macrogol 200-600 and mixtures thereof.

10. A capsule according to claim 9 wherein the plasticiser is anhydrous glycerol.

11. A capsule according to claim 1 wherein the filling contains gelatin having a Bloom value ranging from 60 to 150 in percentages ranging from 1 to 5%, hydrolysed gelatin from 10 to 30%, 85% glycerol from 10 to 30%, pectin from 1 to 5%, gellan gum up to 5% and water from 20 to 60%, the percentages are expressed by weight, on the total filling weight.