|Title:||Polyol esters, their preparation and use in depot forms of pharmacologically active agents|
|Abstract:||This invention provides a polyester of a polyol, said polyol containing at least 3 hydroxyl groups and having a molecular weight of up to 20,000 at least 1 hydroxyl group in said polyol being in the form of an ester, with a poly- or co-poly-lactic acid residue, each having a molecular weight of at least 5,000. These are useful for parenteral depot formulations.|
|Inventor(s):||Brich; Zdenek (Binningen, CH), Kissel; Thomas (Ehrenkirchen, DE)|
|Assignee:||Novartis AG (Basel, CH)|
1. A polyol ester having a molecular weight of 20,000 to 200,000, said polyol ester consisting essentially of:
1) 0.06% to 10% by weight of a polyol residue selected from the group consisting of
i) a cyclic structure having 1 to 8 glucose units containing 4 to 30 hydroxyl groups and
ii) a linear structure of mannitol containing 3 to 6 hydroxyl groups; and
2) a polylactic or co-poly-lactic residue having a molecular weight of 5,000 to 85,000, said polyol ester having at least 3 of said hydroxyl groups in esterified form and having a star-shaped polymer structure, wherein said polyol residue forms a central part surrounded by said polylactic or co-poly-lactic acid residue, and said co-poly-lactic residue comprises glycolic acid.
2. A polyol ester of claim 1 having a molecular weight of about 20,000 to about 80,000.
3. A polyol ester of claim 1 wherein said co-poly-lactic acid residue comprises about 30 to 70 mole % glycolic acid.
4. A depot formulation comprising a matrix of a polyol ester of claim 1 and a therapeutically effective amount of a pharmacologically active agent.
5. A depot formulation of claim 4 wherein said active agent is selected from the group consisting of bromocriptine, ketotifen and co-dergocrine.
6. A depot formulation of claim 4 wherein said formulation is in implant form.
7. A depot formulation of claim 4 wherein said formulation is in microcapsule form.
8. A polyol ester of claim 1 comprising from 0.2% to 1% by weight of said polyol residue.