Methods for targeting drug delivery to the upper and/or lower gastrointestinal tract
AssigneeElan Pharma International Limited
InventorsGary G. Liversidge, W. Mark Eickhoff, Kathleen J. Illig, Pramod Sarpotdar, Stephen B. Ruddy
Life of this patent
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Abstract
Particulate crystalline therapeutic substances are formulated with stabilizers to enhance contact between the crystalline therapeutic substances and the mucosal membranes to provide extended therapeutic effect.
Claims27
A method for targeting delivery of a pharmaceutical composition to the mucosal surface of the lower gastrointestinal tract (GIT) of a mammal comprising administering to a mammal a pharmaceutical composition comprising:
- (a) from about 0.1 to about 45% w/v of particles of an poorly water soluble crystalline therapeutic or diagnostic agent having an average particle size of less than about 2000 nm;
- (b) from about 0.1 to about 10% w/v of a polymer, wherein (i) the polymer is adsorbed on the surface of the therapeutic agent, and (ii) the polymer is selected from the group consisting of polyvinyl alcohol and poloxamer 407;
- and
- (c) water to make 100% w/v,
- wherein the administration results in the drug being predominantly delivered to the lower GIT of the mammal.
A method for targeting delivery of a pharmaceutical composition to the mucosal surface of the upper gastrointestinal tract (GIT) of a mammal comprising administering to a mammal a pharmaceutical composition comprising:
- (a) from about 0.1 to about 45% w/v of particles of a poorly water soluble crystalline therapeutic or diagnostic agent having an average particle size of less than about 2000 nm;
- (b) from about 0.1 to about 10% w/v of a polymer, wherein (i) the polymer is adsorbed on the surface of the therapeutic agent, and (ii) the polymer is selected from the group consisting of poloxamer 238, a combination of poloxamer 188 and dioctyl sodium sulfosuccinate, poloxamer 288, and poloxamer 338;
- and
- (c) water to make 100% w/v,
- wherein the administration results in the drug being predominantly delivered to the upper GIT of the mammal.
A method for delivering a pharmaceutical composition homogeneously to the mucosal surface of both the upper and lower gastrointestinal tract (GIT) of a mammal comprising administering to a mammal a pharmaceutical composition comprising:
- (a) from about 0.1 to about 45% w/v particles of a poorly water soluble crystalline therapeutic or diagnostic agent having an average particle size of less than about 2000 nm;
- (b) from about 0.1 to about 10% w/v of a polymer, wherein (i) the polymer is adsorbed on the surface of the therapeutic agent, and (ii) the polymer is selected from the group consisting of:
- (i) a mixture of poloxamer 217 and dioctyl sodium sulfosuccinate,
- (ii) poloxamer 237;
- (iii) a mixture of poloxamer 238 and dioctyl sodium sulfosuccinate;
- (iv) a mixture of poloxamer 237 and dioctyl sodium sulfosuccinate;
- (v) tyloxapol;
- (vi) a mixture of tyloxapol and dioctyl sodium sulfosuccinate,
- (vii) hydroxypropylmethyl cellulose,
- (viii) polyvinylpyrrolidone,
- (ix) dioctyl sodium sulfosuccinate, and
- (x) polyoxyethylene (20) sorbitan monooleate;
- and
- (c) water to make 100% w/v,
- wherein the administration results in the drug being homogeneously delivered to the lower end upper GIT of the mammal.
Dependencies are inferred from the claim text.