Levothyroxine formulations for oral use
The present invention relates to novel oral spray formulations of Levothyroxine. Further the invention also describes process for preparing such formulations.
1. A spray formulation of Levothyroxine comprising:
(i) levothyroxine sodium in a concentration of 0.0025-5% by weight of the total formulation;
(ii) buffering agents or pH adjusting agents selected from arginine or alanine in a concentration of 0.0015-0.5% by weight of the total formulation;
(iii) one or more solvents, wherein the solvents are selected from one or more of propylene glycol, glycerol, polyethylene glycol (PEG), and water;
(iv) sulfobutylether-β-cyclodextrin (SBECD); and
(v) one or more pharmaceutically acceptable excipients, wherein the pH of the formulation is between 5.5 and 6.5.
2. A spray formulation of Levothyroxine according to claim 1 further comprising buffering agents selected from phosphate, citrate, sodium carbonate, sodium bicarbonate, tartarate, benzoate, lactate, acetate, glutaric, malic, succinic acid, carbonic acid, Tris, and meglumine.
3. A spray formulation of Levothyroxine according to claim 1 further comprising sodium hydroxide, potassium hydroxide, ammonium carbonate, hydrochloric acid, citric acid, lactic acid, phosphoric acid, or sulfuric acid.
4. The spray formulation of claim 1 , wherein the pharmaceutically acceptable excipients are selected from sweetening agents, flavoring agents, preservatives, penetration enhancers and stabilizers.
5. The formulation of claim 1 , wherein the concentration of SBECD ranges from 10-40% by weight of the total formulation.
6. A spray formulation of levothyroxine comprising:
(i) levothyroxine sodium in a concentration of 0.0025-5% by weight of the total formulation;
(ii) arginine in a concentration of 0.0015-0.5% by weight of the total formulation;
(iii) propylene glycol in a concentration of 0.002-0.05% by weight of the total formulation;
(iv) sulfobutylether-β-cyclodextrin (SBECD) in a concentration of 10-40% by weight of the total formulation; and
(v) one or more pharmaceutically acceptable excipients, wherein the pH of the formulation is between 5.5 and 6.5.