Bisphosphonate Formulation

Abstract

A bisphosphonate is formulated with an agent to reduce surface tension and/or reduce foaming in the stomach, leading to reduced reflux and oesophageal irritation in use and increased patient compliance.

1 - 22 . (canceled) 
     
     
         23 . A method of reducing oesophageal irritation in a patient in response to administration of a bisphosphonate-containing composition, comprising administering to the patient the bisphosphonate-containing composition in combination with an amount of an antifoaming agent effective to reduce foam formation in the patient's stomach, thereby reducing irritation in the patient's oesophagus. 
     
     
         24 . The method of  claim 23 , wherein the amount of antifoaming agent is in the range of 20 mg to 150 mg. 
     
     
         25 . The method of  claim 23 , wherein the amount of antifoaming agent is in the range of 35 mg to 125 mg. 
     
     
         26 . The method of  claim 23 , wherein the amount of antifoaming agent is in the range of 3% to 40% by weight of the bisphosphonate-containing composition. 
     
     
         27 . The method of  claim 23 , wherein the amount of antifoaming agent is in the range of 5% to 30% by weight of the bisphosphonate-containing composition. 
     
     
         28 . The method of  claim 23 , wherein the antifoaming agent is one or more polydimethylsiloxanes. 
     
     
         29 . The method of  claims 28  wherein the antifoaming agent comprises dimethicone BP. 
     
     
         30 . The method of  claim 28  wherein the antifoaming agent comprises simethicone BP. 
     
     
         31 . The method of  claim 23  wherein the bisphosphonate-containing composition additionally includes an antacid. 
     
     
         32 . The method of  claim 23  wherein the bisphosphonate is selected from alendronic acid, disodium etidronate, disodium pamidronate, ibandronic acid, risedronate sodium, sodium clodronate, strontium ranelate, tiludronic acid and zoledronic acid. 
     
     
         33 . The method of  claim 23  wherein the bisphosphonate-containing composition additionally comprises (i) a vitamin D derivative, (ii) a calcium supplement or (iii) both (i) and (ii). 
     
     
         34 . The method of  claim 23  wherein the bisphosphonate-containing composition additionally comprises a pharmaceutically acceptable carrier selected from one or more of microcrystalline cellulose, lactose, croscarmellose sodium, colloidal anhydrous silica, magnesium stearate, calcium carbonate, povidone, sucrose, stearic acid, sodium starch glycollate, talc, maize starch, mannitol, pregelatinized starch, low-substituted hydroxypropyl cellulose, silicon dioxide, sodium stearyl fumarate, gelatin and crospovidone. 
     
     
         35 . A method of reducing oesophageal irritation in a patient in response to administration of a bisphosphonate-containing composition, comprising administering to the patient the bisphosphonate-containing composition in combination with an amount of an antifoaming agent selected from simethicone, dimethicone and mixtures thereof in the range of from 5% to 30% by weight of the bisphosphonate-containing composition, thereby reducing irritation in the patient's oesophagus. 
     
     
         36 . The method of  claim 35 , comprising administering to the patient the bisphosphonate-containing composition in combination with from 35 mg to 125 mg of the antifoaming agent. 
     
     
         37 . The method of  claim 35  wherein the bisphosphonate is selected from alendronic acid, disodium etidronate, disodium pamidronate, ibandronic acid, risedronate sodium, sodium clodronate, strontium ranelate, tiludronic acid and zoledronic acid. 
     
     
         38 . The method of  claim 35  wherein the bisphosphonate-containing composition additionally comprises (i) a vitamin D derivative, (ii) a calcium supplement or (iii) both (i) and (ii). 
     
     
         39 . The method of  claim 35  wherein the antifoaming agent is administered in the range of from 7% to 18% by weight of the bisphosphonate-containing composition. 
     
     
         40 . The method of  claim 35  wherein the bisphosphonate-containing composition additionally comprises a pharmaceutically acceptable carrier selected from the group consisting of one or more of microcrystalline cellulose, lactose, croscarmellose sodium, colloidal anhydrous silica, magnesium stearate, calcium carbonate, povidone, sucrose, stearic acid, sodium starch glycollate, talc, maize starch, mannitol, pregelatinized starch, low-substituted hydroxypropyl cellulose, silicon dioxide, sodium stearyl fumarate, gelatin and crospovidone.