Solid oral dosage form containing an enhancer
First Claim
1. A solid oral dosage form which is effective in delivering a drug and an enhancer, each as defined below, to an intestine and which consists of a pharmaceutical composition consisting of:
- (A) a therapeutically effective amount of a hydrophilic or macromolecular drug;
(B) one or more absorption enhancers, each of which;
(i) is a solid at room temperature;
(ii) is a salt of a medium chain fatty acid having a carbon length of from 8 to 14 carbon atoms; and
(iii) is present in the dosage form such that the ratio of the drug to the one or more absorption enhancers is 1;
100,000 to 10;
1;
(C) one or more excipients selected from the group consisting of rate-controlling polymeric materials, diluents, lubricants, disintegrants, plasticizers, anti-tack agents, opacifying agents, pigments, and flavorings; and
optionally, a controlled release coating;
wherein the solid oral dosage form is a tablet, a multiparticulate compressible to form a tablet, or a capsule containing a multiparticulate compressible to form a tablet.
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Accused Products
Abstract
The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.
222 Citations
53 Claims
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1. A solid oral dosage form which is effective in delivering a drug and an enhancer, each as defined below, to an intestine and which consists of a pharmaceutical composition consisting of:
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(A) a therapeutically effective amount of a hydrophilic or macromolecular drug; (B) one or more absorption enhancers, each of which;
(i) is a solid at room temperature;
(ii) is a salt of a medium chain fatty acid having a carbon length of from 8 to 14 carbon atoms; and
(iii) is present in the dosage form such that the ratio of the drug to the one or more absorption enhancers is 1;
100,000 to 10;
1;(C) one or more excipients selected from the group consisting of rate-controlling polymeric materials, diluents, lubricants, disintegrants, plasticizers, anti-tack agents, opacifying agents, pigments, and flavorings; and optionally, a controlled release coating; wherein the solid oral dosage form is a tablet, a multiparticulate compressible to form a tablet, or a capsule containing a multiparticulate compressible to form a tablet. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51)
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52. A process for the manufacture of a solid oral dosage form consisting of a pharmaceutical composition consisting of:
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(A) a therapeutically effective amount of a hydrophilic or macromolecular drug; (B) one or more absorption enhancers, each of which;
(i) is a solid at room temperature;(ii) is a salt of a medium chain fatty acid having a carbon length of from 8 to 14 carbon atoms; and
(iii) is present in the dosage form such that the ratio of the drug to the one or more absorption enhancers is 1;
100,000 to 10;
1;(C) one or more excipients selected from the group consisting of rate-controlling polymeric materials, diluents, lubricants, disintegrants, plasticizers, anti-tack agents, opacifying agents, pigments, and flavorings; and optionally, a controlled release coating; the process comprising the steps of; a) blending a hydrophilic or macromolecular drug with one or more absorption enhancers, and optionally additional excipients, to form a blend;
wherein each of the absorption enhancers;
(i) is a solid at room temperature; and
(ii) is a salt of a medium chain fatty acid having a carbon length of from 8 to 14 carbon atoms in particulate form; andb) forming a solid oral dosage form from the blend by i) direct compression of the blend to form the solid oral dosage form, or ii) granulating the blend to form a granulate for incorporation into the solid oral dosage form, or iii) spray drying the blend to form a multiparticulate for incorporation into the solid oral dosage form; wherein the solid oral dosage form is a tablet, a multiparticulate compressible to form a tablet, or a capsule containing a multiparticulate compressible to form a tablet. - View Dependent Claims (53)
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Specification