Polytartrate composition
The invention provides a polytartrate composition for pulsatile release of a pharmaceutically active material that is in the form of a compressed tablet, and a process for preparing such a composition.
1 . A pharmaceutical composition comprising a polytartrate polymer and at least one pharmaceutically active material characterised in that the composition is capable of releasing the pharmaceutically active material in a pulsatile manner and is obtainable by forming the tablet with a compression force between 10 and 65 kN/cm 2 .
2 . The composition according to claim 1 characterised in that the composition is formed at a compression force between 20 and 50 kN/cm 2 .
3 . The composition according to claim 1 characterised in that the polytartrate polymer forms degradation products that increase the pressure inside the composition.
4 . The composition according to claim 3 characterised in that the polytartrate polymer forms during degradation a C1 to C4 alcohol, aldehyde or ester or acetone.
5 . The composition according to claim 4 characterised that the polytartrate polymer forms during degradation methanol, ethanol, propanol, isopropanol or acetone.
6 . The composition according to claim 1 characterised in that the polytartrate polymer is selected from the group of polycondensates of dimethyl tartrate, diethyl tartrate, diisopropyl tartrate or copolymers thereof and 2,3-O-alkylidenetartaric acid derivatives.
7 . The composition according to claim 6 characterised in that the polytartrate polymer is 2′3′-(1′,4′-diethyl)-L-tartryl poly-(2,3-O-isopropylidene)-L-tartrate.
8 . The composition according to the claim 1 characterised in that the polytartrate polymer has a glass transition temperature that is greater than 40° C.
9 . The composition according to claim 1 characterised in that the pharmaceutically active material is selected from one or more of antigens, antibodies or pharmaceutical substances.
10 . The composition according to claim 9 characterised in that the pharmaceutically active material is a GnRH agonist.
11 . The composition according to claim 10 characterised in that the pharmaceutically active material is buserelin.
12 . The composition according to claim 11 characterised in that the pharmaceutically active material is azagly nafarelin.
13 . The composition according to claim 1 characterised in that the composition additionally comprises one or more of pharmaceutically acceptable excipients or adjuvants.
14 . Process for the preparation of a polytartrate composition according to claim 1 involving the steps of
a) mixing an effective amount of a pharmaceutically active material with the polytartrate polymer,
b) shaping the mixture by a tabletting equipment to form compressed tablets by applying a compression force between 10 and 65 kN/cm 2 .
15 . according to claim 14 characterised in that the pharmaceutically active material and the polytartrate polymer are mixed in a powdered form.
16 . The process according to claim 14 characterised in that the mixture is sieved and optionally additional tabletting excipients are added to the mixture.
17 . A method of administering a pulsatile pharmaceutically active material to a body comprising the step of administering the composition of claim 1 to the body.
18 . The method of claim 17 wherein the body is selected from an animal body and a human body.
19 . A method of administering a pharmaceutically active material to a body comprising the steps of:
administering a composition of claim 1 to the body wherein the pharmaceutically is released in at least two phases comprising an initial burst and a second burst.
20 . The method of claim 19 wherein the initial burst and the second burst is separated by a lag phase.