Method of preparing stable drug nanoparticles
AssigneeNanoSystems L.L.C.
InventorLan De Castro
Life of this patent
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Abstract
Stable dispersible particles consisting essentially of a crystalline drug substance having a surface modifier adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 400 nm are prepared by providing a drug substance, depyrogenating grinding media, mixing the drug substance, grinding media and autoclaving and adding a surface modifier either during autoclaving or after autoclaving and subsequently wet milling. Pharmaceutical compositions containing the particles exhibit unexpected bioavailability and are useful in methods of treating mammals.
Claims14
A method of preparing sterilized nanoparticulate crystalline drug particles comprising the steps of:
- 1) providing a drug substance having a solubility in water of less than 10 mg/ml
- 2) depyrogenating rigid grinding media having an average particle size less than 3 mm at from 200.degree. C. to 300.degree. C. for from 6 to 20 hours
- 3) mixing the drug substance and rigid grinding media and autoclaving it from 100.degree. C. to 150.degree. C. for 10 to 50 minutes and
- 4) adding a surface modifier to the autoclaved drug substance and rigid grinding media to a dispersion medium and wet grinding the drug substance sufficiently to maintain an effective average particle size of less than 400 nm.
The method of claim wherein the drug substance is selected from the group consisting of analgesics, anti-inflammatory agents, anthelmintics, antiarrhythmic agents, antibiotics, anticoagulants, antidepressants, antidiabetic agents, antiepileptics, antihistamines, antihypertensive agents, antimuscarinic agents, antimycobacterial agents, antineoplastic agents, immunosuppressants, antithyroid agents, antiviral agents, anxiolytic sedatives (hypnotics and neuroleptics), astringents, beta-adrenoceptor blocking agents, blood products and substitutes, cardia inotropic agents, contrast media, corticosteroids, cough suppressants (expectorants and mucolytics), diagnostic agents, diagnostic imaging agents, diuretics, dopaminergics (antiparkinsonian agents), haemostatics, immunological agents, lipid regulating agents, muscle relaxants, parasympathomimetics, parathyroid calcitonin and bisphosphonates, prostaglandins, radio-pharmaceuticals, sex hormones, anti-allergic agents, stimulants and anoretics, sympathomimetics, thyroid agents, vasodilators and xanthines.
Dependencies are inferred from the claim text.