ORAL DOSAGE FORMS
The present invention relates generally to encapsulated pharmaceutical compositions enabling improved oral delivery and methods of using such compositions.
1 .- 102 . (canceled)
103 . An oral dosage form comprising a capsule comprising a therapeutic agent, wherein the capsule is coated with a first coating comprising polyvinyl alcohol, and a second coating on top of the first coating comprising a methacrylic acid and ethyl acrylate copolymer dispersion.
104 . The oral dosage form of claim 103 , wherein the ratio of methacrylic acid to ethyl acrylate in the copolymer is 1.4:1 to 1:1.4.
105 . The oral dosage form of claim 103 , wherein the polyvinyl alcohol is partially hydrolysed.
106 . The oral dosage form of claim 103 , wherein the polyvinyl alcohol has an average molecular weight between 20,000-35,000 Da.
107 . The oral dosage form of claim 103 , wherein the methacrylic acid and ethyl acrylate copolymer has an average molecular weight between 30,000 and 40,000 Da.
108 . The oral dosage form of claim 103 , further comprising a third coating on top of the second coating, wherein the third coating comprises talc.
109 . The oral dosage form of claim 103 , wherein the capsule consists of i) gelatin or ii) HPMC.
110 . The oral dosage form of claim 103 , wherein the second coating further comprises sodium lauryl sulfate and polysorbate 80.
111 . The oral dosage form of claim 103 , wherein the second coating does not comprise sodium bicarbonate or titanium dioxide.
112 . The oral dosage form of claim 103 , wherein the first coating further comprises talc, glycerol monocaprylocaprate type 1 and sodium lauryl sulfate.
113 . The oral dosage form of claim 103 , wherein the second coating comprises sodium lauryl sulfate and polysorbate 80.
114 . The oral dosage form of claim 103 , wherein the therapeutic agent is a polypeptide.
115 . The oral dosage form of claim 114 , wherein the polypeptide is terlipressin or an analog thereof or octreotide or an analog thereof.
116 . The oral dosage form of claim 114 , wherein the polypeptide is octreotide or salt thereof.
117 . The oral dosage form of claim 115 , wherein the oral dosage form comprises 5-50 mg of terlipressin.
118 . The oral dosage form of claim 115 , wherein the oral dosage form comprises 5-50 mg of octreotide.
119 . A method of treating a subject suffering from acromegaly or a neuroendocrine tumor, comprising administering to the subject a therapeutically effective amount of the oral dosage form of claim 116 .
120 . The oral dosage form of claim 103 , wherein the first coating comprises 40-80% (wt %) of polyvinyl alcohol, 20-55% (wt %) of talc, 1-20% (wt %) of glycerol monocaprylate and 1-5% (wt %) of sodium lauryl sulfate and the second coating comprises 80-99.0% (wt %) of the methacrylic acid and ethyl acrylate copolymer, 0.1%-2% (wt %) of sodium lauryl sulfate, 0.5-4% (wt %) of polysorbate and triethyl citrate.
121 . The oral dosage form of claim 120 , wherein the second coating comprises 5-30% (wt %) of triethyl citrate.
122 . A method of producing an enteric-coated capsule comprising a therapeutic agent, wherein the method comprises:
applying to the capsule a first coating which comprises polyvinyl alcohol, talc, glycerol monocaprylate and sodium lauryl sulfate, and
applying a second coating on top of the first coating wherein the second coating comprises a methacrylic acid and ethyl acrylate copolymer dispersion, sodium lauryl sulfate, polysorbate and triethyl citrate.
123 . An oral dosage form comprising a capsule, wherein the capsule comprises a formulation comprising a therapeutic agent, wherein the capsule is coated with a first coating comprising hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC) or shellac and a second coating on top of the first coating comprising a methacrylic acid and ethyl acrylate copolymer dispersion.
124 . The oral dosage form of claim 123 , wherein the therapeutic agent is a polypeptide.
125 . The oral dosage form of claim 124 , wherein the polypeptide is octreotide or terlipressin.
126 . The oral dosage form of claim 123 , wherein the formulation comprises a medium chain fatty acid salt and polyvinylpyrrolidone (PVP).
127 . An oral dosage form comprising a capsule and a suspension, wherein the suspension comprises an admixture of a hydrophobic oily medium and a solid form wherein the solid form comprises a therapeutically effective amount of a polypeptide and at least one salt of a medium chain fatty acid in an amount of at least 10% by weight and polyvinylpyrrolidone (PVP) in an amount of at least 3% by weight, wherein the capsule is coated with a coating comprising methacrylic acid and ethyl acrylate copolymer dispersion.
128 . The oral dosage form of claim 127 , wherein the ratio of methacrylic acid to ethyl acrylate in the copolymer is 1.4:1 to 1:1.4.
129 . The oral dosage form of claim 127 , wherein methacrylic acid and ethyl acrylate copolymer has an average molecular weight between 30,000 and 40,000 Da.
130 . The oral dosage form of claim 127 , wherein the coating further comprises sodium lauryl sulfate and polysorbate 80.
131 . The oral dosage form of claim 127 , wherein the therapeutic agent is a polypeptide.