Solid Oral Dosage Form Containing An Enhancer
AssigneeMerrion Research III Limited
InventorThomas W. Leonard
Life of this patent
Estimating the term…
Abstract
The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.
Claims100
A pharmaceutical composition which is effective in delivering a therapeutically effective amounts of a drug and an enhancer, each as defined below, to an intestine, said composition comprising a bisphosphonate and an enhancer wherein the enhancer comprises a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms and is solid at room temperature.
A pharmaceutical composition which is effective in delivering therapeutically effective amounts of a bisphosphonate and an enhancer to an intestine, said composition comprising a bisphosphonate and an enhancer, wherein the enhancer comprises:
- (i) a salt of a medium chain fatty acid having a carbon chain length of from 6 to 20 carbon atoms;
- (ii) a medium chain fatty acid halide derivative, a medium chain fatty acid anhydride derivative, or a medium chain fatty acid glyceride derivative, each of said derivatives having a carbon chain length of from 6 to 20 carbon atoms;
- (iii) the fatty acid salt of clause (i) having, at the end opposite the fatty acid salt, an acid halide, acid anhydride, or glyceride moiety;
- (iv) an acid halide derivative of clause (ii) above having, at the end opposite of the halide portion, an acid halide, acid anhydride, or glyceride moiety;
- (v) an anhydride derivative of clause (ii) above having, at the end opposite of the anhydride, an acid anhydride, acid halide, or glyceride moiety;
- or
- (vi) a glyceride derivative of clause (ii) above having, at the end opposite of the glyceride portion, a glyceride, acid halide, or acid anhydride moiety;
- and wherein the enhancer is solid at room temperature.
A pharmaceutical composition which is effective in delivering therapeutically effective amounts of a bisphosphonate and an enhancer to an intestine, said composition comprising a bisphosphonate and an enhancer, wherein the enhancer:
- (1) comprises a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 Carbon atoms;
- (2) is the only enhancer present in the composition;
- and (3) enhances intestinal delivery of the bisphosphonate to the underlying circulation.
A process for the manufacture of a dosage form comprising the steps of:
- a) providing a blend comprising a bisphosphonate and an enhancer which is solid at room temperature and enhances intestinal delivery of the bisphosphonate to the underlying circulation, wherein the enhancer comprises:
- (i) a salt of a medium chain fatty acid having a carbon chain length of from 6 to 20 carbon atoms;
- (ii) a medium chain fatty acid halide derivative, a medium chain fatty acid anhydride derivative, or a medium chain fatty acid glyceride derivative, each of said derivatives having a carbon chain length of from 6 to 20 carbon atoms;
- (iii) the fatty acid salt of clause (i) having, at the end opposite the fatty acid salt, an acid halide, an acid anhydride, or glyceride moiety;
- (iv) an acid halide derivative of clause (ii) above having, at the end opposite of the halide portion, an acid halide, acid anhydride, or glyceride moiety;
- (v) an anhydride derivative of clause (ii) above having, at the end opposite of the anhydride, an acid anhydride, acid halide, or glyceride moiety;
- or
- (vi) a glyceride derivative of clause (ii) above having, at the end opposite of the glyceride portion, a glyceride, an acid halide, or acid anhydride moiety;
- and
- b) forming the solid oral dosage form from the blend.
A pharmaceutical composition comprising a bisphosphonate and an enhancer, wherein the enhancer enhances intestinal delivery of the bisphosphonate to the underlying circulation, and wherein the composition delivers a therapeutically effective amount of the bisphosphonate when administered to a patient within thirty minutes prior to the patient consuming food, medications, or beverages other than water.
A pharmaceutical composition comprising a bisphosphonate and an enhancer, wherein the enhancer enhances intestinal delivery of the bisphosphonate to the underlying circulation, and wherein the composition delivers a therapeutically effective amount of the bisphosphonate when administered to a patient at a time of day other than the morning.
A pharmaceutical composition comprising a bisphosphonate and an enhancer, wherein the enhancer enhances intestinal delivery of the bisphosphonate to the underlying circulation, and wherein the composition delivers a therapeutically effective amount of the bisphosphonate when administered to a patient within 30 minutes prior to the patient lying down.
A pharmaceutical composition comprising a bisphosphonate and an enhancer, wherein the enhancer enhances intestinal delivery of the bisphosphonate to the underlying circulation, and wherein the composition delivers a therapeutically effective amount of the bisphosphonate when administered to a patient within six hours after consuming food, medications, or beverages other than water.
A pharmaceutical composition for oral administration which is effective in delivering therapeutically effective amounts of a drug and an enhancer to an intestine, said composition comprising alendronate and an enhancer, wherein the composition delivers a therapeutically effective amount of the alendronate when administered to a patient at bedtime.
A pharmaceutical composition for oral administration which is effective in delivering a therapeutically effective amounts of a drug and an enhancer to an intestine, said composition comprising alendronate and an enhancer, wherein the composition is effective in the prevention of osteoporosis with a weekly dose of about 1 to about 10 mg, a daily dose of about 0.1 to about 2 mg, or a monthly dose of about 3 to about 45 mg.
A pharmaceutical composition for oral administration which is effective in delivering therapeutically effective amounts of a drug and an enhancer to an intestine, said composition comprising alendronate and an enhancer, wherein the composition delivers a therapeutically effective amount of the alendronate when administered to a patient within six hours after consuming food, medications, or beverages other than water.
A pharmaceutical composition for oral administration which is effective in delivering therapeutically effective amounts of a drug and an enhancer to an intestine, said composition comprising alendronate and an enhancer, and wherein the composition is effective in the treatment of osteoporosis with a weekly dose of about 2 to 20 mg, a daily dose of about 0.2 to about 4 mg, or a monthly dose of about 6 to about 90 mg.
A pharmaceutical composition for oral administration which is effective in delivering therapeutically effective amounts of a drug and an enhancer to an intestine, said composition comprising zoledronic acid and an enhancer.
Dependencies are inferred from the claim text.