CONTROLLED RELEASE FORMULATIONS OF OCTREOTIDE
A formulation of octreotide or pharmaceutically acceptable salts thereof, which provides controlled release of a therapeutically effective amount of octreotide for a period of at least about two months. Methods of treating acromegaly, decreasing growth hormone, decreasing IGF-1, and treating conditions associated with carcinoid tumors and VIPomas by administering a controlled release formulation of octreotide are provided herein.
1 .- 23 . (canceled)
24 . A method of treating a patient suffering from a condition associated with carcinoid tumors or suffering from one or more symptoms associated with such condition, the method comprising:
implanting subcutaneously into a patient in need thereof at least one implant comprising a hydrophilic polymer and a pharmaceutical formulation comprising octreotide acetate, 0.5 to 20% w/w of hydroxypropylcellulose, and 0.5 to 5% w/w of magnesium stearate, wherein the at least one implant is implanted in a dry state;
wherein the hydrophilic polymer comprises a copolymer of at least two hydrophilic, ethylenically unsaturated monomers, wherein the at least two hydrophilic, ethylenically unsaturated monomers are 2-hydroxyethyl methacrylate and hydroxypropyl methacrylate, and wherein the copolymer comprises about 20% by weight of 2-hydroxyethyl methacrylate and about 80% by weight hydroxypropylmethacrylate;
wherein the pharmaceutical formulation is contained within the hydrophilic polymer;
wherein the pharmaceutical formulation contains between about 20 to about 150 milligrams of octreotide acetate; and
wherein the at least one implant releases a therapeutically effective amount of the octreotide acetate to the patient at a rate of about 30 to 300 μg/day to provide an in vivo average C ss in the patient of about 0.1 ng/ml to about 9 ng/ml of octreotide over a period of at least about two months to about two years.
25 . The method of claim 24 , wherein the pharmaceutical formulation contains from about 40 to about 90 milligrams of octreotide acetate.
26 . The method of claim 25 , wherein the pharmaceutical formulation contains about 50 milligrams of the octreotide acetate.
27 . The method of claim 25 , wherein the pharmaceutical formulation contains about 80 milligrams of the octreotide acetate.
28 . The method of claim 24 , wherein the effective amount of the octreotide provides an in vivo average C ss in the patient of about 1 ng/ml to about 2 ng/ml of octreotide.
29 . The method of claim 24 , wherein the at least one implant releases a therapeutically effective amount of the octreotide over about six months.
30 . The method of claim 24 , wherein the at least one implant is two or more implants.
31 . The method of claim 24 , wherein the at least one implant is implanted in a hydrated state.
32 . The method of claim 24 , wherein the at least one implant releases a therapeutically effective amount of the octreotide acetate to the patient at a rate of about 30 to 250 μg/day.
33 . The method of claim 24 , wherein the at least one implant releases a therapeutically effective amount of the octreotide acetate to the patient at a rate of about 100 μg/day.
34 . The method of claim 24 , wherein the at least one implant releases a therapeutically effective amount of the octreotide acetate to the patient at a rate of about 100 to 300 μg/day.