PHARMACEUTICAL COMPOSITIONS COMPRISING 40 - O - ( 2 - HYDROXY) ETHYL - RAPAMYCIN
First Claim
1. An extended release pharmaceutical formulation for oral administration in form of a multiparticulate comprising a) 40-O-(2-hydroxy)ethyl-rapamycin and b) at least one extended release coating which comprises i) a water insoluble coating forming polymer and ii) optionally a pore former.
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Accused Products
Abstract
The invention relates to extended release pharmaceutical formulations in form of multiparticulates comprising 40-O-(2-hydroxy)ethyl-rapamycin, to dosage forms which comprise said pharmaceutical formulations, to methods of preparing said pharmaceutical formulations and said dosage forms, to uses of said pharmaceutical formulations and said dosage for the manufacture of a medicament for the treatment or prevention of diseases or conditions responsive to inhibition of mTOR signaling pathway, such as for instance proliferative diseases or immunosuppression.
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Citations
34 Claims
- 1. An extended release pharmaceutical formulation for oral administration in form of a multiparticulate comprising a) 40-O-(2-hydroxy)ethyl-rapamycin and b) at least one extended release coating which comprises i) a water insoluble coating forming polymer and ii) optionally a pore former.
- 16. An extended release pharmaceutical formulation for oral administration in form of a multiparticulate comprising 40-O-(2-hydroxy)ethyl-rapamycin in a carrier matrix comprising hydrophilic matrix formers enabling diffusion controlled release of 40-O-(2-hydroxy)ethyl-rapamycin or lipophilic matrix formers enabling erosion controlled release of 40-O-(2-hydroxy)ethyl-rapamycin and optionally further functional layers and/or coatings.
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19. An extended release pharmaceutical formulation for oral administration in form of a multiparticulate comprising 40-O-(2-hydroxy)ethyl-rapamycin, wherein less than 45% of the active ingredient is released from said pharmaceutical composition after 30 min as determined by a dissolution assay in 900 mL phosphate buffer pH 6.8 containing sodium dodecyl sulfate 0.2% at 37°
- C. and the dissolution is performed using a paddle method at 75 rpm according to Ph.Eur. monograph 2.9.3.
- View Dependent Claims (20, 21, 22, 23)
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33. A method of reducing everolimus Cmax to Cmin ratio in a patient comprising administering an extended release pharmaceutical formulation for oral administration in form of a multiparticulates comprising a) 40-O-(2-hydroxy)ethyl-rapamycin and b) at least one extended release coating which comprises i) a water insoluble coating forming polymer and optionally a pore former or c) carrier matrix comprising hydrophilic matrix formers enabling diffusion or a lipophilic matrix enabling erosion controlled release.
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34. An extended release pharmaceutical formulation for oral administration in form of a multiparticulate comprising a) 40-O-(2-hydroxy)ethyl-rapamycin and b) at least one diffusion controlled extended release coating and/or c) carrier matrix comprising hydrophilic matrix formers enabling diffusion or erosion controlled release wherein Cmax to Cmin ratio of the formulation is <
- 5 at steady state.
Specification