.

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

Claims for Patent: 5,880,106

« Back to Dashboard

Claims for Patent: 5,880,106

Title: Oral dosing formulations of dideoxy purine nucleosides
Abstract:Improved oral dosage formulations for acid-labile dideoxy purine nucleoside derivatives such as ddA, ddI, and ddG, have been developed by incorporating selected water-insoluble buffering systems in the formulation. These novel formulations provide reduced mass dosage units in the form of convenient, palatable chewable/dispersible tablets or a dry powder sachet. The reduced mass requirement, necessary to allow tablets of reasonable size, was achieved in part by an unexpected 20 to 25% increase in drug bioavailability resulting from use of the selected buffering systems comprised of an insoluble magnesium antacid agent and either dihydroxyaluminum sodium carbonate or calcium carbonate.
Inventor(s): Ullah; Ismat (Cranbury, NJ), Agharkar; Shreeram Narahari (Princeton, NJ), Wiley; Gary James (Jackson, NJ)
Assignee: Bristol-Myers Squibb Company (Princeton, NJ)
Application Number:08/942,660
Patent Claims: 1. A pharmaceutical composition for oral delivery of dideoxypurine nucleosides with improved bioavailability, the composition comprising;

from about 5 to 375 mg per dosing unit of a dideoxy purine nucleoside selected from the group consisting of 2',3'-dideoxyadenosine (ddA), 2',3'-dideoxyinosine (ddI), 2',3'-dideoxyguanosine (ddG), and individual pharmaceutically acceptable salts, prodrug esters, and hydrates thereof;

and about 800 to 2800 mg of a water-insoluble antacid buffering composition which contains a water insoluble antacid magnesium compound selected from the group consisting of magnesium carbonate, magnesium carbonate hydroxide, magnesium hydroxide, magnesium oxide, magnesium (tribasic) phosphate and magnesium trisilicate,

combined with a dihydroxyaluminum alkali metal carbonate or with calcium carbonate;

optionally containing a soluble citrate buffer;

and which optionally additionally contains binders, disintegrants, sweeteners, flavoring agents, and other pharmaceutically acceptable excipients;

with the proviso that the formulation does not act like a bulk laxative, cause constipation, or cause either physiological pH or electrolyte imbalances in the host following administration.

2. The pharmaceutical composition of claim 1 wherein the water-insoluble antacid buffering composition contains

one part of a water-insoluble antacid magnesium compound in combination with about 2 to 4 parts of a dihydroxyaluminum alkali metal carbonate or with about 1.5 to 3 parts of calcium carbonate.

3. A chewable oral tablet formulation that may chewed or dispersed in a liquid and swallowed, the tablet formulation containing the pharmaceutical composition of claim 1.

4. The composition of claim 1 containing a sweetening agent.

5. The composition of claim 4 wherein the sweetening agent is selected from the group consisting of aspartame, sorbitol and sucrose.

6. The composition of claim 1 containing a flavoring agent.

7. The composition of claim 1 containing a disintegrant.

8. The composition of claim 1 containing a binder.

9. The composition of claim 1 containing pharmaceutically acceptable excipients.

10. The composition of claim 1 wherein the dideoxy purine nucleoside is ddI.

11. The composition of claim 1 wherein the water-insoluble antacid buffering composition contains a dihydroxyaluminum alkali metal carbonate.

12. The composition of claim 11 wherein the water-insoluble antacid buffering composition contains dihydroxyaluminum sodium carbonate.

13. The composition of claim 1 wherein the water-insoluble antacid buffering composition contains calcium carbonate.

14. The composition of claim 1 wherein the water-insoluble antacid magnesium compound is magnesium hydroxide.

15. The composition of claim 1 containing -ddI, dihydroxyaluminum sodium carbonate, magnesium hydroxide, a soluble citrate antacid buffer, a sweetening agent, and a flavoring agent.

16. The composition of claim 1 containing -ddI, calcium carbonate, magnesium hydroxide, a sweetening agent, and a flavoring agent.

17. An oral tablet formulation containing the pharmaceutical composition of claim 15.

18. An oral tablet formulation containing the pharmaceutical composition of claim 16.

19. An oral powder formulation for dispersal in a liquid and containing the pharmaceutical composition of claim 1.

20. An oral powder formulation for dispersal in a liquid and containing the pharmaceutical composition of claim 15.

21. An oral powder formulation for dispersal in a liquid and containing the pharmaceutical composition of claim 16.

22. A chewable or dispersible tablet formulation comprising from about 5 to 375 mg of ddI; about 1.3 to 1.4 g of dihydroxyaluminum sodium carbonate; about 0.4 to 0.5 g of magnesium hydroxide; about 0.3 g of sodium citrate dihydrate; about 0.06 g aspartame and about 0.16 g sucrose; about 0.075 g tablet disintegrant, about 0.04 g silicon dioxide; about 0.02 g wintergreen flavor; about 0.05 g magnesium stearate; and sufficient microcrystalline cellulose to yield a tablet weighing about 3.0 g.

23. A chewable or dispersible tablet formulation comprising about 5 to 375 mg of ddI; about 0.5 to 0.6 g calcium carbonate; about 0.2 to 0.3 g magnesium hydroxide; about 0.06 g aspartame; about 0.08 g tablet disintegrant; about 0.02 g silicon dioxide; about 0.05 g orange flavor; about 0.02 g magnesium stearate and sufficient microcrystalline cellulose to yield a tablet weighing about 1.9 g.

24. A chewable or dispersible tablet formulation comprising about 5 to 375 mg of ddI; about 0.5 to 0.6 g calcium carbonate; about 0.2 to 0.3 g magnesium hydroxide; about 0.07 g aspartame; about 0.1 g tablet disintegrant; about 0.3 g sorbitol; about 0.05 g mandarin orange flavor; about 0.03 g magnesium stearate and sufficient microcrystalline cellulose to yield a tablet weighing about 2.1 g.
« 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