Gastro-resistant formulation containing posaconazole
Inventors
PRATHAP, Vamshi Ramana • KALAMATA, Venkatasimhadri Naidu • RALLABANDI, Bala Ramesha Chary • KATAKAM, Vinay Kumar • Schlehahn, Hendrik
Assignees
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Publication Number
US-11058682-B2
Publication Date
2021-07-13
Expiration Date
Abstract
The present invention relates to a gastro-resistant pharmaceutical composition comprising a solid solution prepared by hot-melt extrusion, whereby the solid solution contains posaconazole, an enteric polymer and a non-enteric polymer. The composition is preferably a granulate material that can be filled into a capsule or compressed into a tablet.
Core Innovation
The invention relates to a gastro-resistant pharmaceutical composition comprising posaconazole. The posaconazole is molecularly dispersed in a mixture containing an enteric polymer and a non-enteric polymer, and the mixture is prepared by hot-melt extrusion.
The gastro-resistant composition is configured to release posaconazole in the intestine while limiting release in 0.1M HCl. A key aspect is the enteric polymer to non-enteric polymer ratio, which ranges from 6:1 to 1:1.
The disclosed polymer systems include hypromellose derivatives, cellulose derivatives, polyvinylacetate derivatives, or polymethacrylic acid derivatives for the enteric polymer, with polymethacrylic acid derivatives being preferred. The non-enteric polymer includes povidone/copolyvidone and polyethylene glycol.
The document further describes optional formulation components including antioxidants and antioxidant synergists, as well as optional plasticizers and sugar alcohols. The composition can be presented as granules, tablets, or capsules with optional enteric coating.
Claims Coverage
The partial claim set contains one independent claim that defines a gastro-resistant posaconazole composition with molecular dispersion in a hot-melt-extruded enteric/non-enteric polymer mixture, including a release profile requirement in 0.1M HCl and an enteric:non-enteric polymer ratio range of 6:1 to 1:1.
Molecularly dispersed posaconazole in an enteric and non-enteric polymer mixture prepared by hot-melt extrusion
A gastro-resistant pharmaceutical composition comprising posaconazole, wherein the posaconazole is molecularly dispersed in a mixture containing an enteric polymer and a non-enteric polymer, the mixture is prepared by hot-melt extrusion.
Enteric to non-enteric polymer ratio for gastro-resistant release
The enteric polymer and non-enteric polymer are present in a ratio of 6:1 to 1:1.
Intestine release with limited release in 0.1M HCl after two hours
The gastro-resistant pharmaceutical composition releases posaconazole in the intestine and releases ≤10% of the posaconazole in 0.1M HCl after two hours.
Overall claim coverage centers on posaconazole molecularly dispersed in a hot-melt-extruded mixture of an enteric polymer and a non-enteric polymer, using an enteric:non-enteric ratio of 6:1 to 1:1, and achieving intestine release with ≤10% release in 0.1M HCl after two hours.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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