Pharmaceutical formulations containing microparticles or nanoparticles of a delivery agent
This invention relates to microparticles and/or nanoparticles containing a delivery agent and/or an active agent. This invention also relates to pharmaceutical formulations and solid dosage forms, including controlled release solid dosage forms of active agent and a delivery agent.
1 .- 77 . (canceled)
78 . A solid pharmaceutical composition suitable for the oral delivery of a pharmacologically active agent comprising
a. a therapeutically effective amount of a pharmacologically active agent;
b. pharmaceutically acceptable inactive excipients, and
c. a delivery agent for the pharmacologically active agent, wherein the delivery agent is in micronized form.
79 . A composition according to claim 78 , wherein the active agent is a peptide.
80 . A composition according to claim 79 , wherein the peptide is a calcitonin.
81 . A composition according to claim 80 , wherein the calcitonin is salmon calcitonin.
82 . A composition according to claim 78 wherein the inactive excipients are selected from the group consisting of crospovidone and povidone.
83 . A composition according to claim 78 , wherein the delivery agent is selected from the group consisting of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, N-(10-[2-hydroxybenzoyl]-amino)decanoic acid, and N-(8-[2-hydroxybenzoyl]amino)caprylic acid.
84 . A composition according to claim 78 , wherein the delivery agent is selected from the group consisting of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, N-(10-[2-hydroxybenzoyl]-amino)decanoic acid, N-(8-[2-hydroxybenzoyl]amino)caprylic acid, and pharmaceutically acceptable salts thereof.
85 . A composition according to claim 78 , wherein the delivery agent is selected from the group consisting of a disodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, a disodium salt of N-(10-[2-hydroxybenzoyl]-amino)decanoic acid, and a disodium salt of N-(8-[2-hydroxybenzoyl]amino)caprylic acid.
86 . A composition according to claim 78 , which additionally includes a diluent.
87 . A composition according to claim 86 , wherein the diluent is microcrystalline cellulose.
88 . A composition according to claim 78 , which additionally includes a lubricant.
89 . A composition according to claim 88 , wherein the lubricant is magnesium stearate.
90 . A method for enhancing the oral bioavailability of a pharmacologically active agent, the method comprising administering to a patient in need of a pharmacologically active agent, an effective amount of a pharmaceutical composition according to claim 78 .
91 . A method of treatment of bone related diseases and calcium disorders comprising administering to a patient in need of such treatment a therapeutically effective amount of a composition according to claim 78 , wherein the pharmacologically active agent is a bone active agent.
92 . A method according to claim 91 , wherein the pharmacologically active agent is calcitonin.
93 . A method according to claim 92 wherein said calcitonin is salmon calcitonin.
94 . The use of a pharmaceutical composition according to claim 78 in the manufacture of a medicament for the treatment of bone related diseases, said pharmaceutical composition comprises an active agent which is a bone active agent.