Drug carrier pellet production process

Abstract

The invention provides a process for the production of drug carrier pellets comprising spray-dried pellets comprising spray-drying a solution of a physiologically tolerable cellulosic binder containing a physiologically tolerable inert particulate carrier having a particle size D (v.0.5) of less than 50 μm.

1 - 21 . (canceled) 
   
   
       22 . A process for the production of drug carrier pellets comprising spray-drying a solution of a physiologically tolerable cellulosic binder, containing a physiologically tolerable inert particulate carrier having a particulate size D(v, 0.5) of less than 50 μm, and a filler selected from lactose, lactose monohydrate, sucrose, fructose, a fructooligosaccharide, insulin, mannitol, sorbitol, xylitol, inositol, isomalt or maltodextrin, wherein said solution further contains an active drug substance selected from the group consisting of a peptide, protein, vaccine, nucleic acid, analgesic, antiinflammatory, tranquilizer, cardiac glycoside, narcotic antagonist, anti parkinsonism agent, antidepressant, antineoplastic agent, immunosuppressant, antiviral, antibiotic, antifungal, antimicrobial, appetite suppressant, antiemetic, antihistamine, antimigraine, vasodilator, antianginal, calcium channel blocker, hormonal agent, contraceptive, antithrombotic, diuretic, antihypertensive, anaesthetic, dependency drug, corticosteroid, vitamin, dermatological agent, ophthalmic agent, steroid, azole, nitro compound, amine, oxicam, mucopolysaccharide, opioid, prostaglandin, benzamide, xanthine, catecholamine, dihydropyridine, contrast agent, thiazide, sydnonimine, oligosaccharide, polysaccharide, diltiazem, and furosemide. 
   
   
       23 . The process of  claim 22  wherein the active drug substance is selected from the group consisting of growth factors, interferons, insulin, SOD, urokinase, EPO, DNA, buprenorphine, ibuprofen, diazepam, digoxin, naloxone, bromocriptine, imipramine, bleomycin, acyclovir, erythromycin, ketoconazole, tetracycline, fenfluramine, metoclopramide, chlorpheniramine, dihydroergotamine, nifedipine, glyceryl nitrate, verapamil, estradiol, norgestrel, warfarin, flunarizine, propranolol, lidocaine, methadone, betamethasone, nitrofurantoin, pilocarpine, progesterone, imidazoles, nitroglycerine, benzocaine, piroxicam thiomucase, morphine, PGA, PGB, PGE, PGF, enaprostil, metoclopramide, theophylline, salbutamol, hydrochlorothiazide, molsidomine, glycosaminoglycan, sulphated polysaccharide, heparin, and heparinoid. 
   
   
       24 . The process of  claim 22  wherein the active drug substance is diltiazem. 
   
   
       25 . The process of  claim 22  wherein the active drug substance is furosemide. 
   
   
       26 . The process of  claim 22  wherein the physiologically tolerable cellulosic binder is selected from the group consisting of alkyl cellulose, hydroxyalkylalkyl cellulose, hydroxyalkylcellulose, and carboxyalkyl cellulose. 
   
   
       27 . The process of  claim 26  wherein the physiologically tolerable cellulosic binder is selected from the group consisting of methylcellulose, ethylcellulose, hydroxypropylmethylcellulose, hydroxyethylmethyl-cellulose, hydroxypropylcellulose, carboxy C 1-5  alkyl cellulose, sodium carboxy methyl cellulose, powdered cellulose, cellulose acetate phthalate, Methocel, Avicel, Pharmacoat, Benecel, Culminal, and Walocels Pharmacoat. 
   
   
       28 . The process of  claim 27  wherein the physiologically tolerable cellulosic binder is Pharmacoat 603 or Surelease E-7-7050. 
   
   
       29 . The process of  claim 22  wherein the filler is maltodextrin. 
   
   
       30 . The process of  claim 22  wherein the active drug substance is diltiazem, the physiologically tolerable cellulosic binder is Pharmacoat 603 or Surelease E-7-7050, and the filler is maltodextrin. 
   
   
       31 . The process of  claim 22  wherein the active drug substance is furosemide, the physiologically tolerable cellulosic binder is Pharmacoat 603 or Surelease E-7-7050, and the filler is maltodextrin. 
   
   
       32 . A spray-dried pellet comprising a physiologically tolerable cellulosic binder, a physiologically tolerable inert particulate carrier having a particle size D(v, 0.5) of less than 50 μm and a filler selected from lactose, lactose monohydrate, sucrose, fructose, fructooligosaccharides, insulin, mannitol, sorbitol, xylitol, inositol, isomalt and maltodextrin, and an active drug substance selected from the group consisting of a peptide, protein, vaccine, nucleic acid, analgesic, antiinflammatory, tranquilizer, cardiac glycoside, narcotic antagonist, anti parkinsonism agent, antidepressant, antineoplastic agent, immunosuppressant, antiviral, antibiotic, antifungal, antimicrobial, appetite suppressant, antiemetic, antihistamine, antimigraine, vasodilator, antianginal, calcium channel blocker, hormonal agent, contraceptive, antithrombotic, diuretic, antihypertensive, anaesthetic, dependency drug, corticosteroid, vitamin, dermatological agent, ophthalmic agent, steroid, azole, nitro compound, amine, oxicam, mucopolysaccharide, opioid, prostaglandin, benzamide, xanthine, catecholamine, dihydropyridine, contrast agent, thiazide, sydnonimine, oligosaccharide, polysaccharide, diltiazem, and furosemide. 
   
   
       33 . The spray-dried pellet of  claim 32  wherein the active drug substance is selected from the group consisting of growth factors, interferons, insulin, SOD, urokinase, EPO, DNA, buprenorphine, ibuprofen, diazepam, digoxin, naloxone, bromocriptine, imipramine, bleomycin, acyclovir, erythromycin, ketoconazole, tetracycline, fenfluramine, metoclopramide, chlorpheniramine, dihydroergotamine, nifedipine, glyceryl nitrate, verapamil, estradiol, norgestrel, warfarin, flunarizine, propranolol, lidocaine, methadone, betamethasone, nitrofurantoin, pilocarpine, progesterone, imidazoles, nitroglycerine, benzocaine, piroxicam thiomucase, morphine, PGA, PGB, PGE, PGF, enaprostil, metoclopramide, theophylline, salbutamol, hydrochlorothiazide, molsidomine, glycosaminoglycan, sulphated polysaccharide, heparin, and heparinoid. 
   
   
       34 . The spray-dried pellet of  claim 32  wherein the active drug substance is diltiazem. 
   
   
       35 . The spray-dried pellet of  claim 32  wherein the active drug substance is furosemide. 
   
   
       36 . The spray-dried pellet of  claim 32  wherein the physiologically tolerable cellulosic binder is selected from the group consisting of alkyl cellulose, hydroxyalkylalkyl cellulose, hydroxyalkylcellulose, and carboxyalkyl cellulose. 
   
   
       37 . The spray-dried pellet of  claim 36  wherein the physiologically tolerable cellulosic binder is selected from the group consisting of methylcellulose, ethylcellulose, hydroxypropylmethylcellulose, hydroxyethylmethyl-cellulose, hydroxypropylcellulose, carboxy C 1-5  alkyl cellulose, sodium carboxy methyl cellulose, powdered cellulose, cellulose acetate phthalate, Methocel, Avicel, Pharmacoat, Benecel, Culminal, and Walocels Pharmacoat. 
   
   
       38 . The spray-dried pellet of  claim 37  wherein the physiologically tolerable cellulosic binder is Pharmacoat 603 or Surelease E-7-7050. 
   
   
       39 . The spray-dried pellet of  claim 32  wherein the filler is maltodextrin. 
   
   
       40 . The spray-dried pellet of  claim 32  wherein the active drug substance is diltiazem, the physiologically tolerable cellulosic binder is Pharmacoat 603 or Surelease E-7-7050, and the filler is maltodextrin. 
   
   
       41 . The spray-dried pellet of  claim 32  wherein the active drug substance is furosemide, the physiologically tolerable cellulosic binder is Pharmacoat 603 or Surelease E-7-7050, and the filler is maltodextrin. 
   
   
       42 . A pharmaceutical composition comprising a spray-dried pellet of  claim 32  with at least one pharmaceutically acceptable carrier or excipient.