Microparticular pharmaceutical compositions
AssigneeIsomed, Inc.
InventorYoung W. Cho
Life of this patent
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AssigneeIsomed, Inc.
InventorYoung W. Cho
Estimating the term…
A pharmaceutical composition comprises microparticles in micelle. The microparticles contain at least one pharmaceutically-active agent, at least one water soluble or miscible phospholipid, at least one lipid soluble or miscible phospholipid, at least one non-ionic surfactant having an HLB value of about 15 or greater, at least one non-ionic surfactant having an HLB value of about or less, and at least one water soluble or miscible sterol compound. The microparticles are suspended in at least one fatty acid having a chain length of C.sub.14 or less. The composition may optionally contain at least one fatty acid having a chain length of C.sub.16 or greater in a concentration of about 5 w/v % or less. The composition is prepared by admixing the pharmaceutically-active agent, phospholipids, surfactants, and sterol, micronizing the admixture to form microparticles, and suspending the microparticles in at least one fatty acid of chain length of C.sub.14 or less to form microparticles in micelle. The invention may be useful in the oral administration of drugs and other therapeutic agents, as well as for the trans-umbilico-dermal administration of such drugs and therapeutic agents.
A pharmaceutical composition prepared by the process comprising (a) admixing about 0.15-5 mg/l of at least one pharmaceutically-active agent, about 17.5-70 g/l of at least one phospholipid selected from the group consisting of glycerophosphatcs, glycerophosphorylcbolines, phosphorylcholines, glycerophosphorylethanolamines, phosphorylethanolamines, glycerophosporylserines, and glycerophosphorylglycerols, about 3.5-34.5 mg/l of at least one phospholipid selected from the group consisting of sn-1-acyl-3-glycerophosphate, sn-1,2-diacylglycerol, sn-1-acyl-3-glycerophosphorylcholine, sn-1-diacyl-3-glycerophosphatc, sn-1-diacyl-3-glycerophosphorylethanolamine, sn-1-,2-acyl-3-glycerophosphorylserine, sn-1,2-acyl-3-glycerophosphate, sn-1-acyl-3-glycerophosphoryl-glycerol, sn-1,2-diacylglycerophosphate, 1-myristoyl-sn-glycero-3-phosphocholine, 1-myristoyl-sn-glycero-3-phosphoetharnolarnine, 1-myristoyl-sn-glycero-3-phospho-(N,N-dimethyl)-ethanolarnine, 1-palmltoyl-sn-glycero-3-phosphocholine, 1-palmitoyl-rac-glycero-3-phosphocholine, 1-palmltoyl-sn-glycero-3-phospho-(N,N-dimethyl)-ethanolamine, 1-stearoyl-sn-glycero-3-phosphocholine, and mixtures thereof, about 0.05-20 w/v % of at least one non-ionic surfactant having an HLB value of about 15 or greater which is a polyoxyethylene compound having from 1-100 oxyethylene moieties selected from the group consisting of polyoxyethylene-lauryl ether, polyoxyethylene-hydrogenated castor oil, polyoxyethylene-sorbitan monooleate, polyoxyethylene-monostearate, and polyoxyethylene-lauryl ether, about 0.5-5 w/v % of at least one non-ionic surfactant having an HLB value of about 6 or less selected from the group consisting of sorbitan-monocaprylate, sorbitan-monopalimitate, sorbitan-monostcaratc, sorbitan-sesquisterate, sorbitan-trioleate, sorbitan-monooleate, sorbitan-sesquioleate, sorbitan-dioleate, glyceryl-monostearate, glyceryl-monoleate, glycerol-dioleate, decaglyceryl-monstearate, decaglyceryl-pentastearate, decaglyceryl-monlinolate, decaglyceryl-monolaurate, and decaglyceryl-monomyristate, and about 9.75-39 g/l of at least one sterol selected from the group consisting of polyoxyethanyl-cholesterol adipate, cholesterol, cholesterol esters, cholesteryl-17-bromohepta-decanoate, cholesterol oleate, cholesterol palmitate, cholesterol sulfate, cholesterol monohydrate, and mixtures thereof, and micronizing the admixture to form microparticles;
A method of preparing a pharmaceutical composition comprising:
Dependencies are inferred from the claim text.