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US 2022/0023222 A1Published application
Method of producing a delayed release drug formulation
AssigneeTillotts Pharma AG
InventorsFelipe Varum, Laetitia Von Rochow, Carsten Markus Füller, Roberto Carlos Bravo González
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Abstract
A method produces a coatable core for a delayed release drug formulation for oral administration, to deliver a drug to the colon. The method involves forming a core containing a drug. An outer layer coating preparation is formed by combining a first aqueous preparation of an enzymatically degradable polymer, which is degradable by colonic bacterial enzymes; a second aqueous preparation of a film-forming enteric polymer having a pH threshold of about pH 6 or above; and an organic anti-tack agent. The core is then coated with the outer layer coating preparation to form an outer layer coated core.
Claims18
1:
- A method of producing a delayed release drug formulation for oral administration to deliver a drug to the colon, said method comprising:
- forming a core comprising a drug;
- combining a first aqueous preparation of an enzymatically degradable polymer which is degradable by colonic bacterial enzymes;
- a second aqueous preparation of a film forming enteric polymer having a pH threshold of about pH 6 or above;
- and an organic anti-tack agent, to form an outer layer coating preparation;
- and
- coating the core with the outer layer coating preparation to form an outer layer coated core.
4 more elements
2:
- The method as claimed in claim 1, wherein the second aqueous preparation is formed by suspending the enteric polymer in water under stirring to form a suspension, and partially neutralising the suspension with a base.
3:
- The method as claimed in claim 2, wherein the base is added to the suspension in an amount sufficient to neutralise from about 10% to about 30% of carboxylic acid groups in the enteric polymer.
4:
- The method as claimed in claim 2, wherein the suspension is partially neutralised using aqueous ammonia.
5:
- The method as claimed in claim 4, wherein the aqueous ammonia has a concentration from about 0.5 N to about 2 N.
6:
- The method as claimed claim 1, wherein the organic anti-tack agent is in the form of an aqueous dispersion.
7:
- The method as claimed in claim 6, wherein the aqueous dispersion comprises a surfactant.
8:
- The method as claimed in claim 7, wherein the surfactant is non-ionic.
9:
- The method as claimed in claim 7, wherein the surfactant is hydrophilic.
10:
- The method as claimed in claim 1, wherein the organic anti-tack agent is glyceryl monostearate (GMS) or stearic acid.
11:
- The method as claimed in claim 1, wherein the core is pre-coated with an isolation layer comprising a film-forming non-ionic polymer that is soluble in gastrointestinal fluid, an inner layer comprising a polymeric material which is soluble in intestinal or gastrointestinal fluid, or both the isolation layer and the inner layer;
- wherein said polymeric material is selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer,
- provided that, where said polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.
12:
- The method as claimed in claim 11, wherein the inner layer, when present, comprises a buffer agent and a base.
13:
- The method as claimed in claim 1, wherein the outer layer coating preparation comprises no more than about 5% v/v organic solvent.
14:
- A delayed release drug formulation for oral administration to deliver a drug to the colon, said formulation comprising:
- a core comprising a drug, and
- an outer coating layer for the core, the outer coating layer comprising a mixture of an enzymatically degradable polysaccharide which is degradable by colonic bacterial enzymes, a film-forming enteric polymer having a pH threshold at about pH 6 or above, and an organic anti-tack agent;
- wherein the outer coating layer comprises no more than about 5000 ppm residual free organic solvent;
- and/or
- wherein the outer coating layer comprises at least 10% by weight of at east one plasticizer based on the weight of the film-forming enteric polymer.
3 more elements
15:
- The delayed release drug formulation according to claim 14, comprising an inner layer located between said core and said outer coating layer, wherein said inner layer comprises a film-forming non-ionic polymer that is soluble in gastrointestinal fluid, a buffer agent, and a base.
16:
- The delayed release drug formulation according to claim 14, comprising an isolation layer located on the surface of the core, said isolation layer comprising a film-forming ionic polymer that is soluble in gastrointestinal fluid.
17:
- The method as claimed in claim 3, wherein the base is added to the suspension in an amount sufficient to neutralise from about 15% to 20% of carboxylic acid groups in the enteric polymer.
18:
- The method as claimed in claim 5, wherein the aqueous ammonia has a concentration of about 1 N.