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Summary for Patent: 4,366,310
|Title:||Controlled release compositions|
|Abstract:||Molecular coordination complexes are formed between a cellulose polymer and a non-polar solid aliphatic alcohol containing 8 to 18 carbon atoms optionally substituted with an aliphatic group containing 8 to 18 carbon atoms by solvating the polymer with a volatile polar solvent and reacting the solvated cellulose polymer directly with the aliphatic alcohol, preferably as a melt. The resulting composition may be dried. This constitutes the complex. The composition has utility as a matrix in controlled release formulations since it has a uniform porosity which may be varied.|
|Inventor(s):||Leslie; Stewart T. (Aberdeen, GB6)|
|Assignee:||Euroceltique, S.A. (LU)|
1. A molecular coordination complex of a cellulose polymer and a solid aliphatic alcohol selected from the group consisting of unsubstituted solid aliphatic alcohols of 8-18 carbon atoms
and solid aliphatic alcohols of 8-18 carbon atoms substituted by an aliphatic group of 8-18 carbon atoms.
2. Molecular coordination complex of claim 1 wherein said cellulose polymer is a hydroxy alkyl cellulose.
3. Molecular coordination complex according to claim 1 wherein the number of carbon atoms of the solid aliphatic alcohol is between 10 and 18 carbon atoms.
4. Molecular coordination complex according to claim 1 wherein said cellulose polymer is hydroxymethyl cellulose, hydroxyethyl cellulose or hydroxypropyl cellulose and wherein the aliphatic alcohol is lauryl, myristyl, cetyl, stearyl or cetostearyl alcohol.
5. Controlled release pharmaceutical composition comprising an active pharmaceutical agent distributed in the molecular coordination complex of claim 1.
6. Composition according to claim 5 wherein the amount of said molecular coordination complex is more than 20% of the weight of the composition.
7. Method of producing the molecular coordination complex of claim 1, which comprises solvating the cellulose polymer with a volatile polar solvent therefor to form a solvated cellulose polymer and reacting the thus solvated cellulose polymer with said solid aliphatic alcohol, thereby forming said molecular coordination complex.
8. Method according to claim 7 wherein said solvated cellulose polymer is introduced into a melt of said solid aliphatic alcohol so as to cause reaction therebetween, cooling the thus formed reaction mass and drying the same to remove any residual volatile polar solvent.
9. Method according to claim 8 wherein 1-6 parts by weight of said volatile polar solvent are used per each part of said cellulose polymer.
10. Method according to claim 8 wherein one part of aliphatic alcohol is used per each part of said volatile polar solvent.
11. The molecular coordination complex of claim 1 wherein said complex is porous.
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