Delivery of oral drugs

Abstract

Disclosed is a system for delivery of a drug comprising a multiple unit dosing device comprising a chousing and an actuator, said device containing multiple doses of multiparticulates comprising drug particles, said device upon actuation delivering a unit dose of said multiparticulates, said drug particles having a mean diameter of greater than 10 μm to about 1 mm such that an effective dose of said drug cannot be delivered into the lower lung of a human patient. Also disclosed are novel methods, devices and dosage forms for delivering a drug.

1 - 73 . (canceled) 
   
   
       74 : A drug formulation for gastrointestinal deposition comprising a non-compressed free flowing plurality of particles comprising a drug and a pharmaceutically acceptable excipient, said drug particles having a mean diameter of greater than 10 μm to about 1 mm, said particles comprising at least about 80% drug. 
   
   
       75 : The drug formulation of  claim 74  wherein said particles comprise at least about 90% drug. 
   
   
       76 : The formulation of  claim 74  further comprising a facilitating agent which enhances the oral administrability of a unit dose of said formulation. 
   
   
       77 : The formulation of  claim 76  wherein said facilitating agent is selected from the group consisting of an absorbability enhancer, a texture modifier, a taste masking agent, a sweetener, a flavorant, a salivary stimulant, an effervescent compound or combinations thereof. 
   
   
       78 : The formulation of  claim 77  wherein said saliva stimulant is selected from the group consisting of citric acid, tartaric acid, malic acid, fumaric acid, adipic acid, succinic acid, acid anhydrides thereof, acid salts thereof and combinations thereof. 
   
   
       79 : The formulation of  claim 74  wherein said excipient comprises a sustained release material. 
   
   
       80 : The formulation of  claim 74 , wherein said particles are divisible into unit doses containing a therapeutically effective amount of said drug, wherein the amount of said drug is about 1 mg to about 500 mg. 
   
   
       81 : The formulation of  claim 74 , wherein said drug particles have a mean diameter of greater than about 50 μm. 
   
   
       82 : The formulation of  claim 74 , wherein 80% of the drug particles have a diameter of greater than 10 μm to about 1 mm. 
   
   
       83 : The formulation of  claim 74 , wherein 80% of the drug particles have a diameter of greater than about 50 μm to about 1 mm. 
   
   
       84 : A method of preparing a drug formulation for gastrointestinal deposition comprising preparing a non-compressed free flowing plurality of particles comprising a drug and a pharmaceutically acceptable excipient, said particles having a mean diameter of greater than 10 μm to about 1 mm, said particles comprising at least about 80% drug. 
   
   
       85 - 91 . (canceled) 
   
   
       92 : The drug formulation of  claim 74 , wherein the pharmaceutically acceptable excipient does not comprise more than 20% of the multiparticulates by weight. 
   
   
       93 : The drug formulation of  claim 92 , wherein the pharmaceutically acceptable excipient does not comprise more than 10% of the multiparticulates by weight. 
   
   
       94 : The drug formulation of  claim 74 , wherein the pharmaceutically acceptable excipient is coated with the drug. 
   
   
       95 : The drug formulation of  claim 74 , wherein the drug is coated with the pharmaceutically acceptable excipient. 
   
   
       96 : The drug formulation of  claim 74 , comprising a mixture of powders of the drug and the pharmaceutically acceptable excipient, each being greater than about 50 μm. 
   
   
       97 : The drug formulation of  claim 74 , wherein greater than 80% of the drug particles have a diameter from about 100 μm to about 1 mm. 
   
   
       98 : The drug formulation of  claim 74 , wherein the particles are of a size such that an effective dose cannot be delivered into the lower lung of a human patient. 
   
   
       99 : The drug formulation of  claim 74 , further comprising particles of 10 μm or less of the same or a different drug. 
   
   
       100 : The drug formulation of  claim 95 , wherein the pharmaceutically acceptable excipient is formulated to provide a sustained release of the drug over time in the gastro-intestinal tract. 
   
   
       101 : The drug formulation of  claim 95 , wherein the pharmaceutically acceptable excipient is formulated to provide a delayed release wherein the drug is released in the intestine. 
   
   
       102 : The drug formulation of  claim 74 , wherein the multiparticulates are formulated as controlled release powders. 
   
   
       103 : The method of  claim 84 , wherein the pharmaceutically acceptable excipient does not comprise more than 20% of the multiparticulates by weight. 
   
   
       104 : The method of  claim 103 , wherein the pharmaceutically acceptable excipient does not comprise more than 10% of the multiparticulates by weight.