Self-emulsifying compositions of cannabinoids

Abstract

The present invention provides self-emulsifying, high concentration and high dose cannabinoid compositions and formulations, to improve administration of cannabinoids and standardized marijuana extracts to patients.

1 - 50 . (canceled) 
     
     
         51 . A high concentration self-emulsifying composition, comprising:
 (i) from about 20% to about 90% by weight of a cannabinoid or a mixture of cannabinoids,   (ii) from about 5% to about 50% by weight of a terpene or a mixture of terpenes, and   (iii) from about 5% to about 50% by weight of an emulsifier or a mixture of emulsifiers,   wherein the composition is essentially free of triglycerides and liposomes and wherein the composition self-emulsifies in an aqueous medium to produce a plurality of particles having a mean particle size from about 20 microns to about 100 nm.   
     
     
         52 . The composition of  claim 51 , further comprising about 10% to about 25% by weight of a viscosity-modifying agent or a mixture of viscosity-modifying agents. 
     
     
         53 . The composition of  claim 51 , wherein the cannabinoid is selected from the group consisting of cannabidiol (CBD), cannabidiolic acid (CBDA), ttetrahydrocannabinol (THC), tetrahydrocannabinolic acid (THCA), cannabigerol (CBG), cannabichromene (CBC), cannabinol (CBN), cannabielsoin (CBE), iso-tetrahydrocannabinol (iso-THC), cannabicyclol (CBL), cannabicitran (CBT), cannabivarin (CBV), tetrahydrocannabivarin (THCV), cannabidivarin (CBDV), cannabichromevarin (CBCV), cannabigerovarin (CBGV), cannabigerol monomethylether (CBGM), salts thereof, derivatives thereof and mixtures thereof. 
     
     
         54 . The composition of  claim 51 , wherein the terpene is selected from the group consisting of bisabolol, bomeol, caryophyllene, carene, camphene, cineol, citronella, eucalyptol, geraniol, guaiol, humulene, isopropyltoluene, isopulegol, linalool, limonene, menthol, myrcene, nerolidol, ocimene, pinene, phytol, pulegone, terpinene, terpinolene, thymol, salts thereof, derivatives thereof, and mixtures thereof. 
     
     
         55 . The composition of  claim 51 , wherein the weight ratio between the cannabinoid and the terpene is from about 20:1 to about 0.5:1, from about 15:1 to about 1:1, from about 10:1 to about 1:1 or from about 5:1 to about 1:1. 
     
     
         56 . The composition of  claim 51 , comprising from about 5% to about 25% by weight or from about 25% to about 50% by weight of an emulsifier or a mixture of emulsifiers. 
     
     
         57 . The composition of  claim 51 , wherein the emulsifier is selected from the group consisting of polysorbate 80, oleoyl polyoxyl-6 glycerides, polyoxyl-35 hydrogenated castor oil, sucrose distearate, tocopherol polyethylene glycol 1000 succinate, lauryl polyoxyl-32 glycerides, sorbitan monooleate, polyglyceryl-3 dioleate, salts thereof, derivatives thereof and mixtures thereof. 
     
     
         58 . The composition of  claim 51 , wherein the composition self-emulsifies in presence of an aqueous medium to produce a plurality of particles, wherein at least 80% of the particles have a size of 30 microns or less or wherein at least 90% of the particles have a size of 10 microns or less, and wherein the mean particle size by number is below about 2 microns or below about 1 micron. 
     
     
         59 . The composition of  claim 51 , further comprising from about 1% to about 20% by weight or from about 5% to about 15% by weight of at least one release retarding agent or a mixture thereof, wherein formulated for slow release of a cannabinoid or a mixture of cannabinoids upon self-emulsification. 
     
     
         60 . A high strength oral dosage form comprising the composition of  claim 51 , formulated as a hard-shell capsule, a soft-shell capsule, a tablet, a liquid, a syrup, a dragee, wherein comprising 150 mg, 200 mg, 300 mg 400 mg, 500 mg 600 mg, 800 mg, 1000 mg or 1200 mg of a cannabinoid or mixture of cannabinoids per single unit dose. 
     
     
         61 . A method of treatment of a cannabinoid-responsive symptom, disease or disorder selected from graft versus host disease (GVHD), inflammatory bowel diseases (IBD), epilepsy, Parkinson's disease, Alzheimer's disease, multiple sclerosis, amyotrophic lateral sclerosis, arthritis, cancer, psoriasis, asthma, arthritis, atherosclerosis, geriatric syndrome, psychiatric indications selected from schizophrenia and borderline personality disorders (BPD) and opioid addiction withdrawal syndrome, comprising administering to a subject in need thereof a therapeutically effective dose of a dosage form of  claim 60 . 
     
     
         62 . The method of treatment of  claim 61 , wherein administering to the subject in need thereof is once or twice daily of one dosage form unit comprising 150 mg, 200 mg, 300 mg 400 mg, 500 mg 600 mg 800 mg 1000 mg or 1200 mg of a cannabinoid or mixture of cannabinoids per single unit dose. 
     
     
         63 . The method of treatment of  claim 61 , wherein the symptom, disease or disorder is borderline personality disorder (BPD) or a BPD-related symptom and the cannabinoid is an essentially non-psychoactive cannabinoid selected from cannabidiol (CBD), CBD isomers and CBD derivatives. 
     
     
         64 . The method of treatment of  claim 63 , wherein the treatment results in improvement in scores of one or more of the rating scales selected from the group consisting of Borderline Symptom List 23 (BSL-23); Borderline Symptom List 95 (BSL-95); Brief Psychiatric Rating Scale (BPRS); Hamilton Anxiety (HAM-A); Hamilton Depression (HAM-D); Barratt Impulsiveness Scale (BIS-11); Pittsburgh Sleep Quality Index (PSQI); Columbia-Suicide Severity Rating Scales (C-SSRS); Columbia Non-Suicidal Self-Injury Rating Scale; Sheehan Disability Scale (SDS); Fagerstrom test for nicotine dependence (FTND); Pain Catastrophizing symptoms questionnaire (PCS); and Zanarini Rating Scale for BPD (ZAN-BPD). 
     
     
         65 . The dosage form of  claim 60 , wherein the cannabinoid or mixture of cannabinoids comprises a cannabinoid selected from CBD, its derivatives and isomers. 
     
     
         66 . The dosage form of  claim 65 , further comprising one or more cannabinoids other than CBD, selected from the group consisting of cannabidiolic acid (CBDA), tetrahydrocannabinol (THC), tetrahydrocannabinolic acid (THCA), cannabigerol (CBG), cannabichromene (CBC), cannabinol (CBN), cannabielsoin (CBE), iso-tetrahydrocannabinol (iso-THC), cannabicyclol (CBL), cannabicitran (CBT), cannabivarin (CBV), tetrahydrocannabivarin (THCV), cannabidivarin (CBDV), cannabichromevarin (CBCV), cannabigerovarin (CBGV), cannabigerol monomethylether (CBGM), salts thereof, derivatives thereof and mixtures thereof. 
     
     
         67 . The composition or dosage form of  claim 66 , wherein the CBD to the cannabinoid other than CBD weight ratio is about 10:1, or about 15:1 or about 20:1.