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-11590127-B2
Publication Date
2023-02-28
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, where 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, and the enteric polymer and non-enteric polymer are present in a ratio of 6:1 to 1:1. The composition releases posaconazole in the intestine and meets defined release amounts after exposure in 0.01 M HCl followed by pH 6.8 conditions.
The disclosed enteric polymer options include hypromellose derivatives such as HPMCP and HPMCAS, and polymethacrylic acid derivatives such as poly(methacrylic acid/methyl methacrylate) and poly(methacrylic acid/ethyl acrylate), as well as polymethacrylic acid/ethyl acrylate copolymers. Non-enteric polymer options include polyvinylpyrrolidone, copovidone, poly(vinylpyrrolidone/vinyl acetate), and graft copolymers including polyvinylcaprolactam/polyvinyl acetate/PEG graft copolymer, polyethylene glycol/polyvinyl alcohol graft copolymer, and poly(ethylene oxide/propylene oxide).
Optional formulation components include antioxidants, monomeric plasticizers, and sugar alcohols to support stability and processability of the molecularly dispersed posaconazole. The dosage forms described include granules optionally enteric-coated, and the composition can be filled in capsules or compressed into tablets. Stability testing under accelerated conditions and reported total impurity levels are described as supporting maintenance of the gastro-resistant composition performance during storage.
Claims Coverage
The partial content includes two independent claims covering a gastro-resistant pharmaceutical composition with molecularly dispersed posaconazole in an enteric/non-enteric polymer mixture prepared by hot-melt extrusion. The main inventive features are the molecularly dispersed formulation structure, the polymer mixture ratio range, and quantified gastro-resistant release constraints under defined acid and pH conditions.
Molecularly dispersed posaconazole in an enteric and non-enteric polymer mixture
Posaconazole is molecularly dispersed in a mixture containing an enteric polymer and a non-enteric polymer.
Hot-melt extrusion preparation of the polymer mixture
The enteric polymer and non-enteric polymer mixture containing the molecularly dispersed posaconazole is prepared by hot-melt extrusion.
Enteric-to-non-enteric polymer ratio 6:1 to 1:1
The enteric polymer and non-enteric polymer are present in a ratio of 6:1 to 1:1.
Intestinal release performance after 0.01 M HCl and pH 6.8
The gastro-resistant pharmaceutical composition releases ≥10% of the posaconazole after two hours in 0.01 M HCl and releases at least 80% of the posaconazole after the two hours in 0.01 M HCl followed by 45 minutes at pH 6.8.
Stomach and combined stomach+intestine release performance
The gastro-resistant pharmaceutical composition releases ≤10% of the posaconazole in the stomach and at least 80% of the posaconazole is released in stomach and intestine combined.
Overall, the independent claims cover gastro-resistant posaconazole compositions in which posaconazole is molecularly dispersed in an enteric/non-enteric polymer mixture prepared by hot-melt extrusion at an enteric:non-enteric ratio of 6:1 to 1:1, with quantified release targets in stomach and/or intestine under defined conditions.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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