Zinc compositions for coated microneedle arrays

Abstract

A medical device comprising a composition comprising a therapeutically active amount of active agent, a zinc compound, and an array of microneedles. The zinc compound may be selected from the group consisting of zinc, pharmaceutically acceptable salts of zinc, and mixtures thereof. At least a portion of the composition is present as a coating on at least a portion of the microneedles. Methods of delivering a therapeutically active agent to a mammal using compositions of the disclosure are also included.

1 - 16 . (canceled) 
     
     
         17 . A medical device comprising:
 a composition comprising a therapeutically active amount of an active agent;   a zinc compound selected from the group consisting of zinc, pharmaceutically acceptable salts of zinc, and mixtures thereof; and   an array of microneedles,   wherein at least a portion of the composition is present as a coating on at least a portion of the microneedles; and   wherein the molar ratio of zinc compound to active agent is greater than 0.1.   
     
     
         18 . A medical device according to  claim 17 , wherein the zinc compound comprises an inorganic salt of zinc. 
     
     
         19 . A medical device according to  claim 17 , wherein the zinc compound comprises a divalent salt of zinc. 
     
     
         20 . A medical device according to  claim 19 , wherein the zinc compound comprises zinc chloride or zinc acetate. 
     
     
         21 . A medical device according to  claim 17 , wherein the molar ratio of zinc compound to active is 0.1 to 2.0. 
     
     
         22 . A medical device according to  claim 21 , wherein the molar ratio of zinc compound to active is 0.2 to 1.5. 
     
     
         23 . A medical device according to  claim 22 , wherein the molar ratio of zinc compound to active is 0.25 to 1.0. 
     
     
         24 . A medical device according to  claim 17 , wherein the active agent is a protein or peptide. 
     
     
         25 . A medical device according to  claim 17 , wherein the active agent is selected from the group consisting of human growth hormone (hGH), tissue plasminogen activator (TPA), calcitonin gene related peptide (CGRP), leutinizing hormone releasing hormone (LHRH), goserelin, leuprolide, buserelin, triptorelin, gonadorelin, napfarelin, menotropins, follicle stimulating hormone (FSH), leutinizing hormone (LH)), human menopausal goanadotropins (hMG), human chorionic gonadotropin (hCG), vasopressin, desmopressin, insulin, adrenocortiocotropic hormone (ACTH), ACTH (1-24), calcitonin, parathyroid hormone (PTH), parathyroid hormone antagonists, parathyroid hormone-related protein (PTHrP), oxytocin, deamino [Val4, D-Arg8] arginine vasopressin, interferon alpha, interferon beta, interferon gamma, tumor necrosis factor (TNF), erythropoietin (EPO), granulocyte macrophage colony stimulating factor (GM-CSF), granulocyte colony stimulating factor (G-CSF), interleukins, interleukin-2 (IL-2), interleukin-10 (IL-10), glucagon, and growth hormone releasing factor (GRF). 
     
     
         26 . A medical device according to  claim 17 , wherein more than 50% by weight of the composition is present as a coating on the microneedles. 
     
     
         27 . A medical device according to  claim 26 , wherein more than 75% by weight of the composition is present as a coating on the microneedles. 
     
     
         28 . A medical device according to  claim 17 , wherein more than 90% by weight of the composition is present as a coating on the microneedles. 
     
     
         29 . A medical device according to  claim 17 , wherein the active agent is not a PTHrP analogue. 
     
     
         30 . A medical device according to  claim 17 , wherein the amount of zinc compound is 0.5% to 10% of the total weight of the composition. 
     
     
         31 . A medical device according to  claim 30 , wherein the amount of zinc compound is 1% to 8% of the total weight of the composition. 
     
     
         32 . A medical device according to  claim 31 , wherein the amount of zinc compound is 2% to 6% of the total weight of the composition. 
     
     
         33 . A medical device according to  claim 17 , wherein the molar ratio of zinc compound to active agent is greater than 0.2. 
     
     
         34 . A medical device according to  claim 17 , wherein the molar ratio of zinc compound to active agent is greater than 0.25. 
     
     
         35 . A method of delivering a therapeutically active agent to a mammal, comprising:
 applying a device according to  claim 17  to a skin surface of the mammal;   allowing the device to remain in contact with the skin for a period of time to allow a portion of the active agent to be transferred into the skin of the mammal; and   subsequently removing the device from the mammal.   
     
     
         36 . A method of delivering a therapeutically active agent to a mammal according to  claim 35 , wherein the Cmax attained in the mammal is greater than the Cmax that would be attained if a like device with a composition lacking zinc compound were applied to the mammal for the period of time. 
     
     
         37 . A method of delivering a therapeutically active agent to a mammal according to  claim 36 , wherein the AUC attained in the mammal is greater than the AUC that would be attained if a like device with a composition lacking zinc compound were applied to the mammal for the period of time. 
     
     
         38 . A method according to  claim 37 , wherein the active agent is not a PTHrP analogue.