Sustained-release microencapsulated delivery system

Abstract

Disclosed is a process for producing sustained-release powders that is fast, efficient, and economical. The process involves melting a naturally derived oil with a melting point above 110° F. in specially designed mixer through either the work energy input of the mixer shaft itself, or a specially fitted plow type mixer equipped with a heating tank, cooling unit, jacket for hot water circulation, and heated lines with nozzles for atomizing the hot oil to be sprayed on. The entire manufacturing process can be completed in about 5-30 minutes, and results in small, sustained-release particles that are free flowing and solid at room temperature. The preferred oil is a hydrogenated soy oil with a melting point range of 145° F. to 160° F. which is applied at about a 1% level by weight in a high shear mixer. Also included are sustained-release compositions for therapeutic agents such as drugs, botanicals, biological agents, fungicides, and fertilizers.

1 . A microencapsulation process comprising: 
 a) adding a core material and a naturally derived oil having a melting point above 110° F. into a high shear mixer,    b) mixing the core material and the naturally derived oil until microencapsulated particles are formed in the high shear mixer, said microencapsulated particles comprising the core material and the naturally derived oil and being formed without dissolving or dispersing the core material or naturally derived oil with solvent; and    c) collecting the microencapsulated particles as a powder directly from the high shear mixer.    
   
   
       2 . The process of  claim 1 , wherein no classification step is performed during the microencapsulation process.  
   
   
       3 . The process of  claim 1 , wherein the naturally derived oil is an plant oil, vegetable oil, animal oil, combinations thereof.  
   
   
       4 . The process of  claim 1 , wherein the naturally derived oil is a non-hydrogenated oil.  
   
   
       5 . The process of  claim 1 , wherein the core material comprises ace-inhibitors, anti-anginal drugs, anti-arrhythmias, anti-asthmatics, anti-cholesterolemics, anti-convulsants, anti-depressants, anti-diarrhea preparations, anti-histamines, anti-hypertensive drugs, anti-infectives, anti-inflammatory agents, anti-lipid agents, anti-manics, anti-nauseants, anti-stroke agents, anti-thyroid preparations, anti-tumor drugs, anti-tussives, anti-uricernic drugs, anti-viral agents, acne drugs, alkaloids, amino acid preparations, anabolic drugs, analgesics, anesthetics, angiogenesis inhibitors, antacids, antiarthritics, antibiotics, anticoagulants, antiemetics, antiobesity drugs, antiparasitics, antipsychotics, antipyretics, antispasmodics, antithrombotic drugs, anxiolytic agents, appetite stimulants, appetite suppressants, beta blocking agents, bronchodilators, cardiovascular agents, cerebral dilators, chelating agents, cholecystokinin antagonists, chemotherapeutic agents, cognition activators, contraceptives, coronary dilators, cough suppressants, decongestants, deodorants, dermatological agents, diabetes agents, diuretics, emollients, enzymes, erythropoietic drugs, expectorants, fertility agents, fungicides, gastro-intestinal agents, growth regulators, hormone replacement agents, hyperglycemic agents, hypnotics, hypoglycernic agents, laxatives, migrain treatments, mineral supplements, mucolytics, narcotics, neuroleptics, neuromuscular drugs, NSAIDS, nutritional additives, peripheral vaso-dilators, polypeptides, prostaglandins, psychotropics, renin inhibitors, respiratory stimulants, steroids, stimulants, sympatholytics, thyroid preparations, tranquilizers, uterine relaxants, vaginal preparations, vaso-constrictors, vago-dilators, vertigo agents, vitamins, wound healing agents, botanical substances, fungicides, or fertilizers.  
   
   
       6 . The process of  claim 1 , wherein the animal or vegetable oil is a vegetable oil with a melting point from 110° F. and 200° F.  
   
   
       7 . The process of  claim 1 , wherein the animal or vegetable oil is a vegetable oil with a melting point from 135° F. to 165° F.  
   
   
       8 . The process of  claim 1 , wherein the oil is present in the microencapsulated particles at from 0.25% to 50% by weight.  
   
   
       9 . The process of  claim 1 , wherein the oil is present in the microencapsulated particles at from 0.25% to 3% by weight.  
   
   
       10 . The process of  claim 1 , wherein the oil is present in the microencapsulated particles at from 0.25% to 20% by weight.  
   
   
       11 . The process of  claim 1 , wherein a high shear mixer includes a heated jacket, and wherein said heated jacket heats the mixer sufficiently to melt the naturally derived oil.  
   
   
       12 . The process of  claim 1 , wherein a sugar or mineral is mixed with the core material and the naturally derived oil in the high shear mixer.  
   
   
       13 . The process of  claim 12 , wherein the sugar is present in the microencapsulated particles at from 1% to 30% by weight.  
   
   
       14 . The process of  claim 12 , wherein the sugar is present in the microencapsulated particles at from 5% to 20% by weight.  
   
   
       15 . The process of  claim 12 , wherein the sugar is selected from the group consisting of sucrose, dextrose, lactose, polydextrose, maltodextrin, and maltose.  
   
   
       16 . The process of  claim 12 , wherein the mineral is present in the microencapsulated particles at from 1% to 20% by weight.  
   
   
       17 . The process of  claim 12 , wherein the mineral is present in the microencapsulated particles at from 5% to 10% by weight.  
   
   
       18 . The process of  claim 12 , wherein the mineral is calcium carbonate.  
   
   
       19 . A solid sustained-release pharmaceutical composition, comprising a microencapsulated core material that is microencapsulated by a naturally derived oil having a melting point above 110° F., and wherein the naturally derived oil is present in an amount of 0.25% to 50% by weight of the microencapsulated particles, said composition being free of processing solvent.  
   
   
       20 . The composition of  claim 19 , wherein the composition is in an oral dosage form.  
   
   
       21 . The composition of  claim 19 , wherein naturally derived oil in the microencapsulated particles present at from 0.25% to 3% by weight.  
   
   
       22 . The composition of  claim 19 , wherein naturally derived oil in the microencapsulated particles present at from 0.25% to 20% by weight.  
   
   
       23 . The composition of  claim 19 , wherein the naturally derived oil has a melting point between 110° F. to 200° F.  
   
   
       24 . The composition of  claim 19 , wherein the naturally derived oil has a melting point from 120° F. to 180° F.  
   
   
       25 . The composition of  claim 19 , wherein the naturally derived oil has a melting point of about 160° F.  
   
   
       26 . The composition of  claim 19 , wherein the naturally derived oil is a vegetable oil.  
   
   
       27 . The composition of  claim 19 , wherein the naturally derived oil is a non-hydrogenated palm oil with a melting point range from 140° F. to 160° F.  
   
   
       28 . The composition of  claim 19 , wherein the core material is selected from the group consisting of a drug, a nutritional agent, a botanical substance, a biological substance, a fungicide, a fertilizer, and mixtures thereof.  
   
   
       29 . The composition of  claim 19 , wherein the core material comprises ace-inhibitors, anti-anginal drugs anti-arrhythmias, anti-asthmatics, anti-cholesterolemics, anti-convulsants, anti-depressants, anti-diarrhea preparations, anti-histamines, anti-hypertensive drugs, anti-infectives, anti-inflammatory agents, anti-lipid agents, anti-manics, anti-nauseants, anti-stroke agents, anti-thyroid preparations, anti-tumor drugs, anti-tussives, anti-uricernic drugs, anti-viral agents, acne drugs, alkaloids, amino acid preparations, anabolic drugs, analgesics, anesthetics, angiogenesis inhibitors, antacids, antiarthritics, antibiotics, anticoagulants, antiemetics, antiobesity drugs, antiparasitics, antipsychotics, antipyretics, antispasmodics, antithrombotic drugs, anxiolytic agents, appetite stimulants, appetite suppressants, beta blocking agents, bronchodilators, cardiovascular agents, cerebral dilators, chelating agents, cholecystokinin antagonists, chemotherapeutic agents, cognition activators, contraceptives, coronary dilators, cough suppressants, decongestants, deodorants, dermatological agents, diabetes agents, diuretics, emollients, enzymes, erythropoietic drugs, expectorants, fertility agents, fungicides, gastro-intestinal agents, growth regulators, hormone replacement agents, hyperglycemic agents, hypnotics, hypoglycernic agents, laxatives, migrain treatments, mineral supplements, mucolytics, narcotics, neuroleptics, neuromuscular drugs, NSAIDS, nutritional additives, peripheral vaso-dilators, polypeptides, prostaglandins, psychotropics, renin inhibitors, respiratory stimulants, steroids, stimulants, sympatholytics, thyroid preparations, tranquilizers, uterine relaxants, vaginal preparations, vaso-constrictors, vago-dilators, vertigo agents, vitamins, or wound healing agents.  
   
   
       30 . The composition of  claim 19 , wherein the core material is selected from the group consisting of niacin, L-arginine, creatine monohydrate, L-camitine, aspirin, loratidine, lovastatin, vitamin C, garlic powder, grape polyphenols, tocotrienol, co-enzyme Q-10 and mixtures thereof.  
   
   
       31 . A solid sustained-release pharmaceutical composition, comprising a microencapsulated core material that is microencapsulated by a naturally derived oil having a melting point above 110° F., and wherein the naturally derived oil is present in an amount of 0.25% to 3% by weight of the microencapsulated particles.  
   
   
       32 . The composition of  claim 31 , wherein the composition is in an oral dosage form.  
   
   
       33 . The composition of  claim 31 , wherein the naturally derived oil has a melting point between 110° F. to 200° F.  
   
   
       34 . The composition of  claim 31 , wherein the naturally derived oil has a melting point from 120° F. to 180° F.  
   
   
       35 . The composition of  claim 31 , wherein the naturally derived oil has a melting point of about 160° F.  
   
   
       36 . The composition of  claim 31 , wherein the naturally derived oil is a vegetable oil.  
   
   
       37 . The composition of  claim 31 , wherein the naturally derived oil is a non-hydrogenated palm oil with a melting point range from 140° F. to 160° F.  
   
   
       38 . The composition of  claim 31 , wherein the core material is selected from the group consisting of a drug, a nutritional agent, a botanical substance, a biological substance, a fungicide, a fertilizer, and mixtures thereof.  
   
   
       39 . The composition of  claim 31 , wherein the core material comprises ace-inhibitors, anti-anginal drugs anti-arrhythmias, anti-asthmatics, anti-cholesterolemics, anti-convulsants, anti-depressants, anti-diarrhea preparations, anti-histamines, anti-hypertensive drugs, anti-infectives, anti-inflammatory agents, anti-lipid agents, anti-manics, anti-nauseants, anti-stroke agents, anti-thyroid preparations, anti-tumor drugs, anti-tussives, anti-uricernic drugs, anti-viral agents, acne drugs, alkaloids, amino acid preparations, anabolic drugs, analgesics, anesthetics, angiogenesis inhibitors, antacids, antiarthritics, antibiotics, anticoagulants, antiemetics, antiobesity drugs, antiparasitics, antipsychotics, antipyretics, antispasmodics, antithrombotic drugs, anxiolytic agents, appetite stimulants, appetite suppressants, beta blocking agents, bronchodilators, cardiovascular agents, cerebral dilators, chelating agents, cholecystokinin antagonists, chemotherapeutic agents, cognition activators, contraceptives, coronary dilators, cough suppressants, decongestants, deodorants, dermatological agents, diabetes agents, diuretics, emollients, enzymes, erythropoietic drugs, expectorants, fertility agents, fungicides, gastro-intestinal agents, growth regulators, hormone replacement agents, hyperglycemic agents, hypnotics, hypoglycernic agents, laxatives, migrain treatments, mineral supplements, mucolytics, narcotics, neuroleptics, neuromuscular drugs, NSAIDS, nutritional additives, peripheral vaso-dilators, polypeptides, prostaglandins, psychotropics, renin inhibitors, respiratory stimulants, steroids, stimulants, sympatholytics, thyroid preparations, tranquilizers, uterine relaxants, vaginal preparations, vaso-constrictors, vago-dilators, vertigo agents, vitamins, or wound healing agents.  
   
   
       40 . The composition of  claim 31 , wherein the core material is selected from the group consisting of niacin, L-arginine, creatine monohydrate, L-carnitine, aspirin, loratidine, lovastatin, vitamin C, garlic powder, grape polyphenols, tocotrienol, co-enzyme Q-10 and mixtures thereof.