DOSAGE UNIT FOR SUBLINGUAL, BUCCAL OR ORAL ADMINISTRATION OF WATER-INSOLUBLE PHARMACEUTICALLY ACTIVE SUBSTANCES
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Abstract
One aspect of the invention relates to a pharmaceutical dosage unit for sublingual, buccal, pulmonary or oral administration, said dosage unit having a weight of 20-500 mg and comprising 1-80 Wt. % of a microgranulate that is distributed throughout a solid hydrophilic matrix; said microgranulate being characterised in that it: has a volume weighted average diameter of 5-100 m; contains at least 0.01 wt. %, preferably at least 0.1 wt. % of one or more water-insoluble pharmaceutically active substances; contains at least 10 wt. %, preferably at least 20 wt. % of an emulsifier component; and is capable of forming a micro-emulsion upon contact with saliva or water. The dosage units of the present invention achieve the inherent benefits of oral delivery whilst at the same time realising a high transmucosal absorption rate of the cannabinoids contained therein. Other aspects of the present invention relate to the use of the aforementioned dosage units in the therapeutic or prophylactic treatment and to a process for the manufacture of said dosage units.
79 Citations
34 Claims
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1-17. -17. (canceled)
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18. A pharmaceutical dosage unit for oral administration, said dosage unit having a weight of 20-500 mg and comprising 1-80 wt. % of a microgranulate distributed throughout a solid hydrophilic matrix, said microgranulate comprising:
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(a) a volume weighted average diameter of 5-100 μ
m;(b) at least 0.01 wt. % of one or more water-insoluble pharmaceutically active substances having a solubility in demineralised water of 37°
C. (neutral pH) of less than 200 mg/l, wherein the pharmaceutically active substance is selected from the group consisting of cannabinoids, alkaloids, steroids and combinations thereof; and(c) at least 10 wt. % of an emulsifier component with an HLB of more than 7 selected from the group consisting of sugar fatty acid esters, mono-glycerides, di-glycerides, diacetyl tartaric acid ester of monoglyceride, polyglycerol esters, diacetyl tartaric acid ester of diglyceride, calcium stearoyl lactylate, sodium stearoyl lactylate and combinations thereof; wherein the pharmaceutical dosage unit is capable of forming a micro-emulsion upon contact with saliva or water. - View Dependent Claims (19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33)
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34. A method of manufacturing a pharmaceutical dosage unit having a weight of 20-500 mg and comprising 5-80 wt. % of a microgranulate that is distributed throughout a solid hydrophilic matrix, said process comprising:
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(A) mixing thoroughly; (i) 5 to 80 parts by weight of a microgranulate having a volume weighted average diameter of 5-100 μ
m and comprising;(a) at least 0.1 wt. % of one or more water-insoluble pharmaceutically active substances having a solubility in demineralised water of 37°
C. (neutral pH) of less than 200 mg/l, said pharmaceutically active substances being selected from the group consisting of cannabinoids, alkaloids, steroids and combinations thereof; and(b) at least 10 wt. % of an emulsifier component with an HLB of more than 7, said emulsifier component being selected from the group consisting of sugar fatty acid esters, mono-glycerides, di-glycerides, diacetyl tartaric acid ester of monoglyceride, polyglycerol esters, diacetyl tartaric acid ester of diglyceride, calcium stearoyl lactylate, sodium stearoyl lactylate and combinations thereof, with (ii) 20-95 parts of matrix-forming components; and (B) shaping the resulting mixture so as to obtain the dosage unit.
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Specification