Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1994-12-22
1996-07-09
Killos, Paul J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
424465, A61K 31155
Patent
active
055345514
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention is generally directed to pharmaceutical formulations comprising aminoguanidine for oral administration prepared with spray drying techniques to form direct compression tablets.
BACKGROUND OF THE INVENTION
Spray-drying techniques have been used in previous formulations, examples of which follow. However, spray-drying has not been reported in connection with aminoguanidine preparations.
U.S. Pat. No. 4,605,666 shows a preparation of vitamin powders by spray drying a slurry containing vitamin, binder, magnesium stearate and SiO.sub.2.
U.S. Pat. No. 4,710,519 shows a preparation of acetaminophen powder by spray drying slurry of acetaminophena and binder and adding magnesium stearate and SiO.sub.2.
U.S. Pat. No. 4,892,889 shows a preparation of vitamin powders by spray drying the mixture of vitamin, gelatin, carbohydrate, fatty acid monoglyceride, SiO.sub.2 and water.
U.S. Pat. No. 4,519,961 shows a preparation of free-flowing powders of oxidation sensitive materials. Colloid suspension of a substance and one or more saccharides. The spray adjuvant is silicic acid and a metal salt of a higher fatty acid.
U.S. Pat. No. 4,916,163 shows an anti-diabetic compound containing glyburide, and spray dried lactose. Other excipients include SiO.sub.2 and Magnesium Stearate.
JP Patent no. 03206034 shows a composition comprising aminoguanidine derivative and mannitol which can be in a tablet form.
SU Patent no. 1172920 shows the preparation of free-flowing cholin-chloride powder by spray drying.
U.S. Pat. No. 4,533,674 shows the preparation of vitamin C powder by spray drying a slurry of vitamin, binder and SiO.sub.2.
JP 50157517 shows the preparation of triglyceride tablets by spray-drying a suspension of compounds with casein, starch and dextrin.
EP 436373 shows the preparation of naproxen tablets by spray drying slurry of compound or its salt and excipients.
Various patent applications and patents on aminoguanidine include JP 75001255, JP 71016967, EP 339496, JP 01083059, JP 01056614, DE 2736064, NL 7317772, U.S. Pat. No. 3,659,016, U.S. Pat. No. 3,714,363, BE 748407 and U.S. Pat. No. 3,621,056.
SUMMARY OF THE INVENTION
A method of making a direct compression tablet suitable for commercial pharmaceutical use comprising between about 50% to about 99% aminoguanidine or pharmaceutically acceptable salt thereof by weight of the tablet comprising: acceptable salt thereof, a sufficient amount of an aqueous solution capable of substantially dissolving the aminoguanidine or pharmaceutically acceptable salt thereof, and a sufficient amount of a suitably compatible binder to produce an aminoguanidine solution; conditions sufficient to obtain a spray-dried powder suitable for direct compression into tablets; and for administration to a patient.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 shows a plot of tablet hardness versus compression force for various formulations made from aminoguanidine (AMG) and Avicel.RTM. (AV) (Microcrystalline Cellulose) and 0.25% Magnesium Stearate: the circle indicates 80% AMG/20% AV tablet with a total tablet weight of 750 mg; the diamond indicates 70% AMG/30% AV tablet with a total tablet weight of 857 mg; the square indicates 60% AMG/40% AV tablet with a total tablet weight of 1000 mg; and the triangle indicates 50% AMG/50% AV tablet with a total tablet weight of 1200 mg. The black square shows about 96% Aminoguanidine HCl tablet prepared by spray drying techniques in accordance with Example 1 of the present invention.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The development of a pharmaceutical formulation is often a laborious task. However, if the active ingredient has poor compressibility, compactibility and flow properties, the search for a large scale, economically efficient manufacturing process can be painstaking. Additionally, if the active ingredient is incompatible with excipients commonly used in pharmaceutical formulations, the task of developing the pharmaceutical formulation may require extensive experimentation. This task c
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Berman Jonathan
Minish Sharon K.
Page Phillip E.
Pence Janet M.
Hoechst Marion Roussel Inc.
Killos Paul J.
Moon Carolyn D.
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