Delivery of a bioactive material
View Patent ↗A solid pharmaceutical composition comprising a water-soluble bioactive material and an encapsulating material which is present in the composition in the form of continuous solid phase, and in which solid particles of the bioactive material are dispersed and encapsulated in the continuous solid phase of the encapsulating material, wherein each of the bioactive material and the encapsulating material is normally a solid at room temperature and the melting point of the encapsulating material is lower than the melting point of the bioactive material, the bioactive material being preferably a bisphosphonate, most preferably alendronate, and the encapsulating material includes an enhancer, preferably a mono- or di-glyceride, or an encapsulating surfactant, preferably, a polyoxyethylene/polyoxypropylene block copolymer having surface active properties, and a process for preparing the composition in which solid particles of the bioactive material are mixed with and dispersed in the encapsulating material which is in molten (liquid) form; and cooling the molten form of the encapsulating material to form a solid pharmaceutical composition having the solid particles of the bioactive material dispersed and encapsulated in a continuous solid phase of the encapsulating material.
1. A solid oral pharmaceutical composition which consists essentially of: (A) about 0.0005 to about 70 wt. % of a pharmaceutically effective amount of solid particles of a water-soluble bioactive material which is a bisphosphonate and which has a low bioavailability in the gastrointestinal tract of an animal and which is a solid at room temperature and which has a predetermined melting point; (B) about 5 to about 80 wt. % of a glyceride enhancer which is normally a solid at room temperature and which has a melting point lower than the melting point of the bioactive material and which is present in an amount that increases the bioavailability of the bioactive material when it is present within the gastrointestinal tract of an animal; (C) about 10 to about 50 wt. % of a polyoxyethylene/polyoxypropylene block copolymer surfactant; and optionally (D) about 0.01 to about 20 wt. % of another surfactant which has an HLB of about 9 to about 20 and/or about 0.1 to about 50 wt. % of a biocompatible oil; wherein the enhancer is present in the composition in the form of a continuous solid phase in which the solid particles of bioactive material are dispersed uniformly and encapsulated in the composition, wherein the composition is stable, and wherein the solid particles have a mean particle size of about 1 nm to about 1 mm.
2. The composition according to claim 1 including also about 0.01 to about 20 wt. % of another surfactant which has an HLB of about 9 to about 20.
3. The composition according to claim 1 including also about 0.1 to about 50 wt. % of a biocompatible oil.
4. The composition according to claim 1 wherein said glyceride enhancer consists essentially of a mono- or di-glyceride of capric acid, a mono- or di-glyceride of caprylic acid, or a mixture of mono- and di-glycerides of caprylic and capric acids, or a mixture of two or more thereof, and said block copolymer has a molecular weight of about 6000 to about 15,000 and an HLB value of at least about 13.
5. The composition according to claim 1 , wherein the solid particles have a mean particle size of about 50 nm to about 0.5 mm.