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Details for Patent: 4,361,545

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Details for Patent: 4,361,545

Title: Solid pharmaceutical formulations for slow, zero order release via controlled surface erosion
Abstract:A new class of solid pharmaceutical formulations enables the attainment of slow, zero order in vivo release of a wide range of pharmaceutically active ingredients upon oral administration. A broad range of release rates can be preselected by suitable adjustments of tablet properties. The formulations are based upon control of active ingredient release from the surface of the tablet via a controlled surface erosion mechanism. These compositions comprise: (a) an effective amount in the range of 10-90 wt % of a pharmacologically active compound having a water solubility (20.degree. C.) of 1/5-1/500 (w/w); (b) 1-40 wt % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20.degree. C.) of 1/1-1/40 (w/w); (c) 2-20 wt % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20.degree. C.) of 1/1-1/10 (w/w); (d) an amount in the range of 0.05-1.0 wt % of a disintegrating agent for pharmaceutical compositions, at which amount the compound is ineffective as a disintegrating agent; (e) 0.1-2.0 wt % of a surfactant which is pharmaceutically acceptable in oral compositions; and, if necessary for tablet manufacturing purposes, (f) 1-20 wt % of a binder which is pharmaceutically acceptable in oral compositions; or (g) 0.5-5.0 wt % of a die wall lubricant which is pharmaceutically acceptable in oral compositions.
Inventor(s): Powell; David R. (Baudette, MN), Patel; Vithal K. (Baudette, MN)
Assignee: Rowell Laboratories, Inc. (Baudette, MN)
Filing Date:Apr 27, 1981
Application Number:06/258,133
Claims:1. A solid, orally administrable pharmaceutical tablet composition from which the active ingredient has a slow, zero order release rate attained without layers, beads or enteric materials and without relatively insoluble polymers, waxes or gums when administered orally, said tablet being compressed to a hardness of about 5-20 kg, and being either shaped as a sphere, or else having a ratio of tablet thickness to tablet diameter effective to permit tablet erosion and penetration control sufficient for controlled surface erosion thereof, comprising an essentially homogeneous, granulated mixture of:

(a) an effective amount in the range of about 10-90 wt % of a pharmacologically active compound having a water solubility (20.degree. C.) of about 1/5-1/500 (w/w);

(b) about 1-40 wt % of a surface controlling compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20.degree. C.) of about 1/1-1/40 (w/w);

(c) about 2-20 wt % of an erosion controlling compound which is pharmaceutically acceptable in oral compositions and has a water solubility of about 1/1-1/10 (w/w);

(d) an amount in the range of about 0.05-1.0 wt %, of a surface activator which is a disintegrating agent for pharmaceutical compositions at which amount the compound is ineffective as a disintegrating agent;

(e) about 0.1-2.0 wt % of a surfactant which is pharmaceutically acceptable in oral compositions and,

as necessary for tablet manufacturing purposes;

(f) about 1-20 wt % of a binder which is pharmaceutically acceptable in oral compositions; or

(g) about 0.5-5.0 wt % of a die wall lubricant which is pharmaceutically acceptable in oral compositions;

the pharmacologically active ingredient thus having a slow, zero order release rate when administered orally, and the pharmacologically active compound not being a lithium compound, and not being penny shaped or pancake shaped wherein the ratio of thickness to diameter is too small for erosion and penetration control.

2. A pharmaceutical composition consisting essentially of all of ingredients (a)-(g).

3. A pharmaceutical composition of claim 1 wherein the amounts of ingredients are as follows:

(a) 50-90 wt %,

(b) 3-30 wt %,

(c) 3-10 wt %,

(d) 0.05-0.5 wt %,

(e) 0.15-1.0 wt %,

(f) 1-5 wt %, and

(g) 1-4 wt %.

4. A pharmaceutical composition of claim 1 wherein ingredient (a) has a water solubility (20.degree. C.) of 1/50-1/300; ingredient (b) has a water solubility (20.degree. C.) of 1/2-1/30; and ingredient (c) has a water solubility (20.degree. C.) of 1/1-1/5.

5. A pharmaceutical composition of claim 1 having a spherical shape or a ratio of tablet thickness to tablet diameter of about 0.5.+-.15%.

6. A pharmaceutical composition of claim 1 wherein all ingredients have a particle size distribution in the fine (U.S.P.) or very fine (U.S.P.) range.

7. A pharmaceutical composition of claim 1 further comprising, in place of a corresponding amount of active ingredient (a), 1-80 wt % of an inert bulking excipient (h), pharmaceutically acceptable in oral compositions and having a water solubility (20.degree. C.) of 1/5-1/500 (w/w).

8. A pharmaceutical composition of claim 1 wherein

(b) is a chloride, sulfate or phosphate of potassium, sodium or magnesium; calcium citrate, phosphate, lactate, gluconate or succinate; a mono- or di-saccharide or a corresponding polyhydric alcohol; a natural amino acid; or an organic carboxylic or sulfonic acid; and

(c) is a mono- or di-saccharide or a corresponding polyhydric alcohol; a natural amino acid; or an organic carboxylic or sulfonic acid.

9. A pharmaceutical composition of claim 8 wherein

(b) is an inorganic salt and

(c) is a mono- or di-saccharide or a corresponding polyhydric alcohol.

10. A pharmaceutical composition of claim 9 wherein

(b) is sodium chloride or calcium phosphate monobasic; and

(c) is mannitol, lactose or sorbitol.

11. A pharmaceutical composition of claim 10 wherein

(b) is sodium chloride or calcium phosphate monobasic;

(c) is mannitol, lactose or sorbitol;

(d) is sodium starch glycolate;

(e) is sodium lauryl sulfate;

(f) is polyvinylpyrrolidone; and

(g) is calcium stearate.

12. A pharmaceutical composition of claim 6 prepared by first wet granulating ingredients (a), (b) and (f) if present, to form a homogeneous granulate; drying the resultant granulate; dry blending the remaining ingredients with the dried granulate and compressing the blend obtained into tablets of a hardness of 5-20 kg.

13. A pharmaceutical composition of claim 1, 3 or 8 wherein active ingredient (a) is theophylline.

14. A pharmaceutical composition of claim 13 wherein (b) is sodium chloride; (c) is sorbitol; (d) is sodium starch glycolate; (e) is sodium lauryl sulfate; (f) is polyvinylpyrrolidone; and (g) is calcium stearate.

15. A pharmaceutical composition of claim 1, 3 or 8 wherein active ingredient (a) is quinidine sulfate.

16. A pharmaceutical composition of claim 15 wherein (b) is calcium phosphate monobasic; (c) is lactose or mannitol; (d) is sodium starch glycolate; (e) is sodium lauryl sulfate; (f) is polyvinylpyrrolidone; and (g) is calcium stearate.

17. A method of orally administering an active ingredient (a) as defined in claim 1 to a patient in need of treatment with (a), such that (a) is released in vivo with a slow, zero order release rate, comprising orally administering to such a patient a pharmaceutical composition of claim 1.
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