Granulate containing cannabinoid, method for its manufacture and oral dosage unit comprising such granulate

Abstract

The present invention relates to a granulate comprising granules made up of 40-99 wt. % of lactose particles and 1-60 wt. % of a binding component that holds together the lactose particles within the granules. Said granules have a mass weighted average diameter of 50-500 μm and said binding component is a solid dispersion or a solid solution of 10-75 wt. % of a cannabinoid in 25-80 wt. % of a lipophilic matrix. The lipophilic matrix contains at least 80 wt. % sucrose fatty acid mono-ester, the fatty acid residue being selected from C 8 -C 18 fatty acids. The aforementioned granulate can be processed into oral dosage units in the form of tablets for oral delivery. The invention further provides a method for the manufacture of the granulate.

1 - 15 . (canceled) 
     
     
         16 . A granulate comprising granules comprising 40-99 wt. % lactose particles and 1-60 wt. % of a binding component, the granules having a mass weighted average diameter of 50-500 μm and the binding component being a solid dispersion or a solid solution of 10-75 wt. % of cannabinoid in 25-80 wt. % of a lipophilic matrix comprising at least 80 wt. % sucrose fatty acid mono-ester, wherein the fatty acid residue is a C 8 -C 18  fatty acid. 
     
     
         17 . The granulate according to  claim 16 , wherein the granules comprise 60-95 wt. % of lactose particles and 5-40 wt. % of the binding component. 
     
     
         18 . The granulate according to  claim 16 , wherein the fatty acid residue is a saturated C 10 -C 18  fatty acid. 
     
     
         19 . The granulate according to  claim 18 , wherein the sucrose fatty acid mono-ester is sucrose monolaurate. 
     
     
         20 . The granulate according to  claim 16 , wherein the cannabinoid has a water solubility of less than 1 mg/ml at a temperature of 25° C. 
     
     
         21 . The granulate according to  claim 16 , wherein the cannabinoid and the sucrose fatty acid mono-ester together represent at least 80 wt. % of the binding matrix. 
     
     
         22 . The granulate according to  claim 16 , wherein the binding component is a solid dispersion comprising dispersed particles comprising the cannabinoid, wherein the particles have a volume weighted mean diameter between 2 nm and 1 μm. 
     
     
         23 . The granulate according to  claim 16 , wherein at least 80 wt. % of the granules in the granulate have a diameter in the range of 50-500 μm. 
     
     
         24 . An oral dosage unit comprising between 10 and 98.8 wt. % of a granulate according to  claim 16 . 
     
     
         25 . The oral dosage unit according to  claim 24 , wherein the oral dosage unit is a compressed tablet or a capsule. 
     
     
         26 . A method of treating psychiatric disorders, behavioural disorders, schizophrenia, anxiety, epilepsy, movement disorders, eating disorders, Alzheimer, stroke, multiple sclerosis, spinal cord injury, peripheral neuropathy, neurogenic pain, nociceptive pain or nausea, the method comprising orally administering the dosage unit according to  claim 24 . 
     
     
         27 . A method of preparing a granulate according to  claim 16 , comprising:
 (a) providing a lactose powder having a mass weighted average diameter of 32-250 μm;   (b) granulating the lactose powder by combining the powder with a granulation liquid comprising a solution of a cannabinoid and sucrose fatty acid mono-ester in an organic solvent; and   (c) removing the organic solvent by evaporation.   
     
     
         28 . The method according to claim  12 , wherein the organic solvent is C 1 -C 3  alcohol. 
     
     
         29 . The method according to claim  12 , wherein the granulation liquid has the following composition:
 (a) 40-55 wt. % C 1 -C 3  alcohol;   (b) 15-20 wt. % of the cannabinoid; and   (c) 30-40 wt. % of the sucrose fatty acid mono-ester.