Oral pharmaceutical delivery system with improved sustained release

Abstract

A solid orally ingested delivery system having at least one lipid, dry particles including at least one pharmaceutical, and at least one filler, where the dry particles are continuously coated by the lipid and form a homogeneous suspension with the lipid, and at least part of the pharmaceutical is microencapsulated with a polymer that releases in the pH range of about 5.0 to 7.0.

1 . A sustained release solid orally ingested delivery system comprising at least one lipid and dry particles having a particle size greater than about 50 microns, wherein the dry particles contain at least one pharmaceutical, 
 wherein the dry particles are continuously coated with the lipid and form a homogeneous suspension with the lipid;    wherein the suspension, when melted exhibits pseudoplastic and/or thixotropic properties;    wherein at least part of the pharmaceutical is encapsulated with a polymer that dissolves at a pH in the range of from about 4.0 to about 7.0, and the ratio of unencapsulated to encapsulated pharmaceutical is in the range of about 1:10 to 10:1; and    wherein the suspension is formed or shaped into the appropriate solid dosage form by molding or pouring the suspension when in a liquid or semi-liquid state.    
   
   
       2 . The delivery system of  claim 1  wherein the system contains a rupturing agent.  
   
   
       3 . The delivery system of  claim 1  wherein the system contains a surfactant.  
   
   
       4 . The delivery system of  claim 1  wherein ratio of unencapsulated to encapsulated is in the range of about 3:2 to 2:3.  
   
   
       5 . The delivery system of  claim 1  wherein the polymer dissolves at a pH in the range of about 5.0 to 7.0.  
   
   
       6 . The delivery system of  claim 1 , wherein the pharmaceutical is selected from the group consisting of analgesics, antibodies, anti-inflammatory agents, cardiovascular drugs, gastrointestinal medicines, hormones and laxatives.  
   
   
       7 . A sustained release solid orally ingested delivery system comprising at least one lipid and dry particles having a particle size greater than about 50 microns, wherein the dry particles contain at least one pharmaceutical, a surfactant and a rupturing agent, 
 wherein the dry particles are continuously coated with the lipid and form a homogeneous suspension with the lipid;    wherein the suspension, when melted exhibits pseudoplastic and/or thixotropic properties;    wherein at least part of the pharmaceutical is encapsulated with a polymer that dissolves at a pH in the range of from about 5.0 to about 7.0, and the ratio of unencapsulated to encapsulated pharmaceutical is in the range of about 2:3 to 3:2; and    wherein the suspension is formed or shaped into the appropriate solid dosage form by molding or pouring the suspension when in a liquid or semi-liquid state.    
   
   
       8 . The delivery system of  claim 7 , wherein the pharmaceutical is selected from the group consisting of analgesics, antibodies, anti-inflammatory agents, cardiovascular drugs, gastrointestinal medicines, hormones and laxatives.  
   
   
       9 . A method of preparing a sustained release solid orally ingested delivery system comprising melting at least one lipid, blending dry particles which include at least one pharmaceutical and at least one filler to form a suspension, and pouring or molding the suspension to provide a solid oral delivery system; 
 wherein the pharmaceutical is encapsulated and unencapsulated in a ratio of 1:10 to 10:1 encapsulated to unencapsulated;    wherein the pharmaceutical is encapsulated with a polymer that dissolves at a pH in the range of from 4.0 to 7.0; and    wherein the system, when melted, exhibits thixotropic and pseudoplastic flow properties.    
   
   
       10 . The method of  claim 9 , wherein the delivery system includes a rupturing agent.  
   
   
       11 . The method of  claim 9 , wherein the ratio of encapsulated to non-encapsulated is in the range of 2:3 to 3:2.  
   
   
       12 . The method of  claim 9 , wherein the microencapsulating film releases at a pH in the range of about 5.0 to 7.0.  
   
   
       13 . The method of  claim 9 , wherein the microencapsulating film releases at a pH in the range of about 5.5 to 7.0.  
   
   
       14 . The method of  claim 9 , wherein the delivery system includes a surfactant.  
   
   
       15 . A method of preparing a sustained release solid oral delivery system comprising 
 a) microencapsulating at least part of a pharmaceutical,    b) melting at least one lipid,    c) dry-mixing dry particles including the pharmaceutical, and at least one filler,    d) mixing the dry particle mixture with the melted lipid to form a suspension,    wherein the dry particles are continuously coated by the lipid and form a homogeneous suspension with the lipid;    wherein at least part of the pharmaceutical is encapsulated with a polymer that dissolves at a pH in the range of from about 4.0 to about 7.0, and the ratio of unencapsulated to encapsulated pharmaceutical is in the range of about 1:10 to 10:1;    wherein the suspension, when melted, exhibits thixotropic and/or pseudoplastic properties,    wherein the suspension is formed into the desired dose by molding or pouring the suspension when in a liquid or semi-liquid state.    
   
   
       16 . The method of  claim 15 , wherein said pharmaceutical is selected form the group consisting of analgesics, antibodies, anti-inflammatory agents, cardiovascular drugs, gastrointestinal medicines, hormones and laxatives.  
   
   
       17 . A method of administering a pharmaceutical to a human or animal comprising administering by oral ingestion to the human or animal a therapeutic amount of a delivery system comprising at least one lipid and dry particles having a particle size greater than about 50 microns, wherein the dry particles contain at least one pharmaceutical, 
 wherein the dry particles are continuously coated with the lipid and form a homogeneous suspension with the lipid;    wherein the suspension, when melted exhibits pseudoplastic and/or thixotropic properties;    wherein at least part of the pharmaceutical is encapsulated with a polymer that dissolves at a pH in the range of from about 4.0 to about 7.0, and the ratio of unencapsulated to encapsulated pharmaceutical is in the range of about 1:10 to 10:1; and    wherein the suspension is formed or shaped into the appropriate solid dosage form by molding or pouring the suspension when in a liquid or semi-liquid state.    
   
   
       18 . The delivery system of  claim 1  wherein the pharmaceutical is testosterone.  
   
   
       19 . The method of  claim 9 , wherein the pharmaceutical is testosterone.  
   
   
       20 . The method of  claim 17 , wherein the pharmaceutical is testosterone.