Enzyme Delivery Systems and Methods of Preparation and Use

Abstract

This invention relates to coated digestive enzyme preparations and enzyme delivery systems and pharmaceutical compositions comprising the preparations. This invention further relates to methods of preparation and use of the systems, pharmaceutical compositions and preparations to treat persons having ADD, ADHD, autism, cystic fibrosis and other behavioral and neurological disorders.

1 - 59 . (canceled) 
     
     
         60 . A pancreatin pellet consisting of pancreatin, which pellet contains no auxiliary substances and binding agents. 
     
     
         61 . The pancreatin pellet according to  claim 60 , wherein the pellet is a micropellet. 
     
     
         62 . The pancreatin pellet according to  claim 60 , wherein the pancreatin is obtained from the pancreas of a mammal. 
     
     
         63 . A pancreatin pellet comprising a core and a coating, wherein the core consists of pancreatin. 
     
     
         64 . The pancreatin pellet according to  claim 63 , wherein the coating comprises pancreatin. 
     
     
         65 . The pancreatin pellet according to  claim 63 , wherein the coating comprises auxiliary substances and binding agents. 
     
     
         66 . The pancreatin pellet according to  claim 63 , wherein the coating has a first inner layer which surrounds the core consisting of pancreatin, and a second, outer layer. 
     
     
         67 . The pancreatin pellet according to  claim 66 , wherein the first layer comprises of auxiliary substances and binding agents. 
     
     
         68 . The pancreatin pellet according to  claim 66 , wherein the second layer comprises a material that is resistant to gastric juices, and wherein the pellet has a drop-like or spherical shape. 
     
     
         69 . The pancreatin pellet according to  claim 60 , wherein the pellet has a spherical, elliptical or drop-like shape, and wherein the diameter of the sphere or the shorter axis lies in the range of 0.4 to 0.8 mm. 
     
     
         70 . A pharmaceutical composition, comprising a pharmacologically active quantity of pancreatin pellets which consist of pancreatin, which pellets contain no auxiliary substances and binding agents. 
     
     
         71 . The pharmaceutical composition according to  claim 70 , in a dosage form that is suitable for oral administration. 
     
     
         72 . A method of producing a pellet and/or micropellet consisting of pancreatin, which pellet contains no auxiliary substances and binding agents, comprising the steps of: a.) comminuting the pancreases of pigs or cattle and conducting autolysis; b.) obtaining a sieved filtrate by filtration of the intermediate product obtained in step a); c.) precipitating the enzymes from the sieved filtrate; d.) filtering the mixtures obtained in step c) to obtain a filter cake; e.) grinding and vacuum-drying the filter cake until a residual moisture of 0.1 to 0.3% by weight is obtained, whereby the pancreatin product with 0.1 to 0.3% by weight of residual moisture constitutes the dried end product; whereas the extrudable filter cake mass contains more residual moisture and/or organic solvent residues, which are of the order of 50%; f.) thermally treating the filter cake at 80° C. or at a temperature below 80° C.; g.) extruding the thermally treated filter cake having sufficient plasticity and having no additives and/or binding agents in order to form strands; h.) spheronising the extrusion of step g) without additives and/or binding agents or auxiliary substances so as to obtain spherical, elliptical or drop-shaped pellets. 
     
     
         73 . A digestive enzyme particle consisting of pancreatin, wherein the particle contains no additives, extenders, colorants, dyes, or flow enhancers. 
     
     
         74 . The digestive enzyme particle according to  claim 73 , wherein the particle is about 105-425 μm in size. 
     
     
         75 . The digestive enzyme particle according to  claim 73 , wherein the pancreatin is obtained from the pancreas of a mammal. 
     
     
         76 . A digestive enzyme preparation comprising a core and a coating, wherein the core consists of pancreatin. 
     
     
         77 . The digestive enzyme preparation according to  claim 76 , wherein the coating comprises pancreatin. 
     
     
         78 . The digestive enzyme preparation according to  claim 76 , wherein the coating comprises hypromellose phthalate, dimethicone  1000 , and dibutyl phthalate, monoglycerides, or an emulsifiable lipid. 
     
     
         79 . The digestive enzyme preparation according to  claim 76 , wherein the coating has a first inner layer which surrounds the core consisting of pancreatin, and a second, outer layer. 
     
     
         80 . The digestive enzyme preparation according to  claim 79 , wherein the first layer comprises hypromellose phthalate, dimethicone  1000 , and dibutyl phthalate, monoglycerides, or an emulsifiable lipid. 
     
     
         81 . The digestive enzyme preparation according to  claim 79 , wherein the second layer comprises a material that is resistant to HCl present in the stomach, and wherein the digestive enzyme preparation has round surfaces and is free-flowing. 
     
     
         82 . The digestive enzyme particle according to  claim 73 , wherein the particle has a round surface, and wherein the particle is about 105-425 μm in size. 
     
     
         83 . A pharmaceutical composition, comprising a therapeutically effective amount of digestive enzyme particles which consist of pancreatin, wherein the particles contain no additives, extenders, colorants, dyes, or flow enhancers. 
     
     
         84 . The pharmaceutical composition according to  claim 83 , in a dosage form that is suitable for oral administration. 
     
     
         85 . A method of producing a digestive enzyme preparation comprising digestive enzyme particles, wherein the particles contains no additives, comprising the steps of: a.) obtaining unprocessed, raw enzyme preparation; b.) screening or filtering uncoated particles to obtain particles of suitable size; c.) obtaining sieved particles of suitable size and shape.