Drug microparticles
OwnerItzhak Lerner, Vered Rosenberger +3inventors
InventorsItzhak Lerner, Vered Rosenberger, Moshe Flashner-Barak, Anna Drabkin, Naomi Moldavski
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Abstract
Provided are microparticles of active pharmaceutical ingredients, drug delivery vehicles comprising same, and methods for making them.
Claims25
A pharmaceutical composition comprising microparticles of oxybutynin that are not mechanically micronized.
A pharmaceutical composition comprising microparticles of oxybutynin that have not been micronized by a mechanical process selected from high energy milling and high pressure homogenization, from which pharmaceutical composition about 75 weight-% of the oxybutynin of a sample of the composition comprising 100 mg of oxybutynin dissolves from the composition within about 180 minutes when dissolution is measured at 37° C. with an apparatus II dissolution tester as described in the United States Pharmacopoeia operating at about 50 RPM in a medium consisting essentially of 100 mL of 50 mM aqueous phosphate buffer, pH ˜6.8.
A pharmaceutical composition comprising microparticles of oxybutynin obtained by sublimation of a sublimable carrier from a solid solution of oxybutynin in the sublimable carrier.
A pharmaceutical composition comprising pharmaceutical carrier particles consisting essentially of a non-hydrosoluble material and, deposited thereon, microparticles of oxybutynin that are obtained by sublimation of a sublimable carrier from a solid solution of oxybutynin in the sublimable carrier, wherein at least about 75 weight-% of the oxybutynin of a sample of the composition comprising 100 mg of oxybutynin dissolves from the pharmaceutical composition within at most about 180 minutes when dissolution is measured at 37° C. with an apparatus II dissolution tester as described in the United States Pharmacopoeia operating at about 50 RPM in a medium consisting essentially of 100 mL of 50 mM aqueous phosphate buffer, pH ˜6.8.
A process for preparing an oxybutynin delivery vehicle comprising the steps of:
- a) forming a solid solution of oxybutynin and a sublimable carrier on the surface of a pharmaceutical carrier particle;
- and
- b) subliming the sublimable carrier from the solid solution to deposit microparticles of oxybutynin on the surface of the pharmaceutical carrier particle to obtain the oxybutynin delivery vehicle.
Dependencies are inferred from the claim text.