| CPC A61K 9/2054 (2013.01) [A61K 9/0053 (2013.01); A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2095 (2013.01); A61K 9/2846 (2013.01); A61K 9/2893 (2013.01); A61K 33/36 (2013.01)] | 27 Claims |
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1. A pharmaceutical composition suitable for oral administration comprising:
(a) a solid core comprising sodium meta-arsenite or potassium meta-arsenite, wherein the amount of sodium meta-arsenite or potassium meta-arsenite in the solid core is from about 0.1 to 5.0% w/w of the solid core, and the following pharmaceutically acceptable excipients:
(i) a filler or diluent in a range of from about 5 to 95% w/w of the solid core, wherein the filler or diluent is selected from dibasic calcium phosphate anhydrous, partially pregelatinised starch, silicified microcrystalline cellulose, or a mixture thereof;
(ii) a disintegrant in a range of from about 10 to 90% w/w of the solid core, wherein the disintegrant is selected from L-hydroxypropyl cellulose, partially pregelatinised starch, and sodium starch glycolate;
(iii) a glidant in a range of from about 0.1 to 5% w/w of the solid core, wherein the glidant is colloidal silicon dioxide;
(iv) a lubricant in a range of from about 0.1 to 5% w/w of the solid core, wherein the lubricant is sodium stearyl fumarate; and
(v) a binder in a range of up to about 30% w/w of the solid core; wherein the binder is selected from silicified microcrystalline cellulose, partially pregelatinised starch, L-hydroxypropyl cellulose (low substituted hydroxypropylcellulose), and hydroxypropyl cellulose;
and
(b) an enteric coating comprising an enteric polymer, wherein the enteric polymer is selected from:
copolymers of two or more of acrylic acids, esters of acrylic acids, methacrylic acids, or esters of methacrylic acids;
cellulose acetate phthalate polymers;
hydroxypropyl methylcellulose phthalate polymers;
hydroxypropyl methylcellulose acetate succinate;
polyvinyl acetate phthalate;
cellulose acetate trimellitate; and
combinations thereof;
wherein the pharmaceutically acceptable excipients are selected such that oxidation of meta-arsenite to meta-arsenate is minimised,
wherein the enteric coating provides a weight gain of from about 9.5% w/w of the solid core to a weight gain of about 14% w/w of the solid core,
wherein the coating thickness is from about 6.5% to about 15% of the thickness of the pharmaceutical composition, and
wherein the pharmaceutical composition is in the form of an enteric coated tablet; and
wherein the solid core is selected from the following:
(A) a solid core comprising: (i) sodium meta-arsenite or potassium meta-arsenite, and (ii) the following pharmaceutically acceptable excipients: dibasic calcium phosphate anhydrous, L-hydroxypropyl cellulose, hydroxypropyl cellulose, colloidal silicon dioxide, and sodium stearyl fumarate;
(B) a solid core comprising: (i) sodium meta-arsenite or potassium meta-arsenite, and (ii) the following pharmaceutically acceptable excipients: dibasic calcium phosphate anhydrous powder, dibasic calcium phosphate anhydrous granules, L-hydroxypropyl cellulose, sodium starch glycolate, colloidal silicon dioxide, and sodium stearyl fumarate;
(C) a solid core comprising: (i) sodium meta-arsenite or potassium meta-arsenite, and (ii) the following pharmaceutically acceptable excipients: dibasic calcium phosphate anhydrous, L-hydroxypropyl cellulose, sodium starch glycolate, colloidal silicon dioxide, and sodium stearyl fumarate; and
(D) a solid core comprising: (i) sodium meta-arsenite or potassium meta-arsenite, and (ii) the following pharmaceutically acceptable excipients: dibasic calcium phosphate anhydrous, silicified microcrystalline cellulose, sodium starch glycolate, colloidal silicon dioxide, and sodium stearyl fumarate.
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