Oral controlled release liquid suspension pharmaceutical...

A - Human Necessities – 61 – K

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A61K 47/30 (2006.01) A61K 9/10 (2006.01)

Patent

CA 2143070

A controlled release oral formulation for use with a variety of drugs, e.g. anti-Parkinsonian, cardiovascular and anti-epileptic drugs are formed in liquid suspension form. The ingredients in the suspension are water, an edible oil and a stabilizer for the liquid suspension, at least one pharmaceutically active ingredient, at least two water soluble biodegradable polymers, and optionally with at least one antioxidant to prevent degradation and oxidation of the pharmaceutically active ingredients. Suitable polymers are polysucrose, copolymer of sucrose and epichlorohydrin, hydroxyethyl cellulose hydroxypropyl- ethyl cellulose, hydoxypropyl-methyl cellulose, gelatine, starch, modified crosslinked starch, polyethyleneimine, methoxypolyethylene glycol, polyethylene oxide, cellulose acetate, polyvinyl alcohol, sodium alginate, N,N-diethylaminoacetate, block copolymers of polyoxyethylene, block copolymers of polyoxypropylene, a mixture of hydroxyethyl cellulose and sodium carboxymethyl cellulose, and combinations thereof. Suitable edible oils are mineral oil, soyabean oil, coconut oil, vegetable oil and sunflower oil and combinations thereof. Suitable stabilizers are oleic acid, cholic acid, deoxycholic acid, pharmaceutically acceptable salts thereof and combinations thereof. Suitable antioxidants are tocopherol, deteroxime mesylate, methyl paraben and ascorbic acid. A typical teaspoon dose of anti-Parkinson liquid suspension contains 15-150 mg carbidopa, 50-1500 mg -23- levodopa, 100-300 mg of a combination of polyvinyl alcohol and polysucrose, 10-50 mg oil, 5-15 mg antioxidant, e.g. vitamin E, 5-20 mg stabilizer, 10-15 mg colorants, 10-15 mg natural flavouring agents and 5 ml water.

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