.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 4,526,777

« Back to Dashboard

Details for Patent: 4,526,777

Title: Pharmaceutical combination composition and associated method
Abstract:A novel combination pharmaceutical composition is described, together with a method for making the same, wherein the pharmaceutically active ingredients are separately milled and then formed into separate granules, and only thereafter blended together to form the combination composition. The method for achieving this novel combination composition is also described. In particular, a novel combination composition of triamterene and hydrochlorothiazide having improved bioavialability and novel effectiveness to prevent or eliminate hypokalemic side effects is also described.
Inventor(s): Blume; Cheryl D. (Morgantown, WV), Bonner; Paul H. (Morgantown, WV)
Assignee: Mylan Pharmaceuticals Inc. (Morgantown, WV)
Filing Date:Feb 17, 1984
Application Number:06/581,412
Claims:1. A method for enhancing the bioavailability of pharmaceutical combination compositions in solid unit dosage form and composed of at least two solid pharmaceutically-active ingredients of respectively different hydrophilic characteristics, at least one of which is sparingly soluble in physiological fluids, which method consists essentially in

(1) separately providing each of said active ingredients in finely divided particulate solid form;

(2) separately mixing each of said finely divided active ingredients with respective non-toxic pharmaceutically-acceptable inert carrier materials, in finely-divided particulate form,

of the class including wicking agents, surfactants, lubricants, disintegrants and at least one agent functionally capable of aiding in compacting operations

(3) separately compacting said respective active ingredients with said respective carrier materials to form separate compactions thereof

(4) thereafter separately comminuting said separate compactions to form respectively separate granules of said respective active ingredients

each of such respective granules being composed of a large number of said respective individual finely divided active ingredient particles admixed with said finely divided particulate carrier materials

(5) thereafter mechanically blending said respective granules together in desired optimum pharmaceutically effective proportions to form a granularly heterogeneous blended combination and whereby said respective active ingredients particles are substantially retained within said respective granules

whereafter said thus-blended composition is formulated into unit dosage entities.

2. A method according to claim 1 wherein said unit dosage entities are in capsule form containing said thus-blended composition.

3. A method according to claim 1 wherein said unit dosage entity is a solid tablet, containing in addition to said thus-blended composition a lubricant ingredient blended therewith to aid in the processing of the granules.

4. A method according to claim 3 wherein said tablet further contains a coloring additive.

5. A method according to claim 1 wherein said finely-divided active ingredients will be such that at least 95% thereof will pass through a 100 mesh screen.

6. A method according to claim 1 wherein said granules have a size range from not more than 5% larger than 2 mm to not more than 20% being smaller than 0.075 mm.

7. A pharmaceutical combination composition having at least first and second pharmaceutically-active ingredients,

at least one of which ingredients is sparingly soluble in an aqueous physiological fluid, and which ingredients are of respectively different hydrophobic or hydrophilic characteristics,

and composed of a granularly heterogeneous but substantially homogeneous blend of said ingredients

said respective first and second ingredients being present in finely divided particulate form and having been first separately compacted and then separately comminuted into respectively separate granules, whereby

one set of said respective granules contains substantially only said first active ingredient in admixture with a first set of non-toxic pharmaceutically-acceptable inert carrier materials of the class including

wicking agents, disintegrants, surfactants,

lubricants and compacting aids, and

a second set of respective granules contains said second active ingredient in separate admixture with a second set of non-toxic pharmaceutically-acceptable inert carrier materials of the class including

wicking agents, disintegrants, surfactants, lubricants and compacting aids,

said respective first and second sets of carrier materials being respectively compatible with said first and second active ingredients and functionally capable of aiding disintegration of said repective granules and dissolution of said respective ingredient particles upon exposure of said granules to said physiological fluid,

whereby said composition exhibits enhanced bioavailability of at least one of said ingredients, relative to the bioavailability thereof in a combination of homogenous granules containing both of said respective finely divided ingredient particles in intimate admixture with each other.

8. A composition according to claim 7 formulated in a capsule unit dosage.

9. A composition according to claim 7 formulated as a tablet, and containing a lubricant blended with said respective first and second sets of granules in said tablet.

10. A composition according to claim 7 wherein said finely-divided particulate form has a size range such that at least 95% will pass through a 100 mesh screen.

11. A composition according to claim 7 wherein said granules have a size range such that not more than 5% is larger than 2 mm, to not more than 20% being larger than 0.075 mm.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc