Porous particles
AssigneeLucideon Limited
InventorsPhilip Robert Jackson, Mark Cresswell, Ian F. Campbell
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Abstract
Processes for preparing porous particles are disclosed, in which the resulting particles release an encapsulated active ingredient more readily in aqueous media than they do in alcoholic media. Also described are the particles themselves, as well as tamperproof, abuse-deterrent, dosage forms comprising the porous particles. The release characteristics of the porous particles make them useful for overcoming drug-abuse techniques, such as dose-dumping in alcoholic media.
Claims20
A sol-gel process for the preparation of a plurality of porous particles comprising at least one active ingredient present within the pores, wherein the at least one active ingredient is an opioid or opioid derivative and wherein the percentage release of the active ingredient from the pores of the particles into simulated intestinal fluid is greater than or equal to the percentage release of the active ingredient from the pores of the particles into 40% vol/vol ethanol in 0.1 M HCl,
- the process comprising the steps of:
- a) providing a mixture comprising water and HCl, said mixture having a pH of less than or equal to 2.5,
- b) adding to the mixture of step a) an inorganic porous particle monomer such that the molar ratio of water to the inorganic porous particle monomer is less than or equal to 12.5,
- c) adding to the mixture of step b) at least one active ingredient, wherein the at least one active ingredient comprises an opioid or opioid derivative,
- d) drying the mixture resulting from step c) at a temperature of greater than or equal to 60°C.,
- e) milling the material resulting from step d) to a particle size of 25-500 μm, and
- f) drying the resulting porous particles at a temperature of greater than or equal to 60°C.;
- wherein on addition of the at least one active ingredient to the mixture of step b), the mixture of step b) is a colloidal solution with a maximum viscosity at room temperature of 2.0 Pa·s;
- and drying steps d) and (f) are performed at a temperature of 60-90 °C.
A particle comprising a porous substrate and at least one active ingredient present within the pores, wherein the at least one active ingredient is an opioid or opioid derivative and the particle has a particle size of 25-500 μm and a moisture content of less than or equal to 6% by weight, and wherein
- i. the percentage release of the at least one active ingredient from the particle in an aqueous solution of pH 6.8 at 37°C. is 30-50 after 1 hour, 45-65 after 2 hours, 60-80 after 4hours and 85 or more after 10 hours, and
- ii. the percentage release of the at least one active ingredient from the particle in a solution of 40% vol/vol ethanol in 0.1 M HCl at 37°C. is 40 or less after 30 minutes, 50 or less after 1 hour and 65 or less after 2 hours.
Dependencies are inferred from the claim text.