Pharmaceutical compositions comprising rifaximin

Patent metadata

Field	Value
Publication number	US-11224591-B2
Application number	US-201716341333-A
Country	US
Kind code	B2
Filing date	Oct 13, 2017
Priority date	Oct 14, 2016
Publication date	Jan 18, 2022
Grant date	Jan 18, 2022

Abstract

A pharmaceutical composition is provided for the treatment of systemic infections as well as colonic diseases. The composition comprises a therapeutically effective amount of rifaximin and a therapeutically effective amount of at least one alkaloid or derivative thereof. Methods and kits are also provided.

First claim

We claim:

1. A pharmaceutical composition comprising a therapeutically effective amount of rifaximin and a therapeutically effective amount of at least one bioavailability enhancing agent comprising at least one piperine alkaloid selected from the group consisting of: piperine, tetrahydropiperine, cis-trans piperine, trans,cis-piperine, cis,cis-piperine, and a combination thereof:
wherein the rifaximin is present in an amount of from about 5 mg to about 1000 mg, and
wherein the piperine alkaloid is present in an amount from about 0.5 mg to about 400 mg.

2. The pharmaceutical composition of claim 1 , further comprising one or more pharmaceutically acceptable excipients comprising carriers, diluents, fillers, binders, lubricants, glidants, disintegrants, bulking agents, flavorants or any combination thereof.

3. The pharmaceutical composition of claim 2 , wherein the composition is in the form of a tablet, mini-tablet, granules, sprinkles, capsules, sachets, powders, pellets, disintegrating tablets, dispersible tablets, solution, suspension, emulsion, lyophilized powder or in the form of a kit.

4. The pharmaceutical composition of claim 2 , wherein the pharmaceutical composition is formulated for use in the treating systemic infections and colonic diseases.

5. A kit for treating disease caused by caused by Clostridium difficile infection and infections caused by Gram-positive and Gram-negative bacteria, the kit comprising
a therapeutically effective amount of rifaximin and
a therapeutically effective amount of at least one bioavailability enhancing agent comprising at least one piperine alkaloid selected from the group consisting of: piperine, tetrahydropiperine, cis-trans piperine, trans,cis-piperine, cis,cis-piperine, and a combination thereof,
wherein the rifaximin is in a separate composition from the at least one piperine alkaloid.

6. A method of treating systemic infections as well as colonic diseases in a patient in need of such treatment, the method comprising: administering a pharmaceutical composition comprising
(i) a therapeutically effective amount of rifaximin;
(ii) a therapeutically effective amount of at least one bioavailability enhancing agent comprising at least one piperine alkaloid selected from the group consisting of: piperine, tetrahydropiperine, cis-trans piperine, trans,cis-piperine, cis,cis-piperine, and a combination thereof; and
(iii) one or more pharmaceutically acceptable excipients comprising carriers, diluents, fillers, binders, lubricants, glidants, disintegrants, bulking agents, flavorants or any combination thereof.

7. The method according to claim 6 , wherein the diseases are caused by Clostridium difficile infection and infections caused by Gram-positive and Gram-negative bacteria.

8. A method of making a pharmaceutical composition that enhances the bioavailability of rifaximin, the method comprising:
mixing a therapeutically effective amount of rifaximin and a therapeutically effective amount of at least one bioavailability enhancing agent comprising at least one piperine alkaloid selected from the group consisting of: piperine, tetrahydropiperine, cis-trans piperine, trans,cis-piperine, cis,cis-piperine, and a combination thereof with one or more pharmaceutically acceptable excipients to make the pharmaceutical composition.

9. A method of enhancing the bioavailability of rifaximin, the method comprising:
providing a therapeutically effective amount of rifaximin and providing a therapeutically effective amount of at least one bioavailability enhancing agent comprising at least one piperine alkaloid selected from the group consisting of: piperine, tetrahydropiperine, cis-trans piperine, trans,cis-piperine, cis,cis-piperine, and a combination thereof.

10. The method of claim 9 , wherein (i) the rifaximin is in a first composition and the at least one piperine alkaloid thereof is in a second composition; or (ii) rifaximin and the at least one piperine alkaloid thereof is combined in one composition.

Assignees

• Cipla Ltd

Inventors

• Malhotra Geena
• Joshi Kalpana
• Ghosalkar Jeevan

Classifications

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title

• A61K9/4858

  Organic compounds · CPC title

• A61K9/0095

  Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006) · CPC title

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K31/437 Primary

  the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline · CPC title