MICRONEEDLE DEVICES AND METHODS
A medical device, comprising: an array of microneedles, and a coating disposed on the microneedles, wherein the coating comprises: a local anesthetic selected from the group consisting of lidocaine, prilocaine, and a combination thereof; and a local anesthetic dose-extending component selected from the group consisting of tetracaine, ropivacaine, bupivacaine, procaine and a combination thereof; wherein the local anesthetic is present in an amount of at least 1 wt-% based upon total weight of solids in the coating, and wherein the local anesthetic and dose-extending component are in a non-eutectic weight ratio; a medical device, comprising an array of dissolvable microneedles, the microneedles comprising: a dissolvable matrix material; at least 1 wt-% of a local anesthetic selected from the group consisting of lidocaine, prilocaine, and a combination thereof; and a local anesthetic dose-extending component selected from the group consisting of tetracaine, ropivacaine, bupivacaine, procaine and a combination thereof; wherein the local anesthetic and dose-extending component are in a non-eutectic weight ratio, and wherein wt-% is based upon total weight of solids in all portions of the dissolvable microneedles which contain the local anesthetic; a method of extending a topically delivered local anesthetic dose in mammalian tissue using the devices; and methods of making the devices are provided.
1 - 15 . (canceled)
16 . A medical device, comprising:
an array of microneedles, and
a coating disposed on the microneedles,
wherein the coating comprises:
a local anesthetic selected from the group consisting of lidocaine, prilocaine, and a combination thereof, and
a local anesthetic dose-extending component selected from the group consisting of tetracaine, ropivacaine, bupivacaine, procaine and a combination thereof,
wherein the local anesthetic and the local anesthetic dose-extending component are in a non-eutectic weight ratio; and
wherein the dose-extending component/local anesthetic weight ratio is 0.1 to 0.9;
wherein the coating further comprising at least one excipient; and
wherein upon topically delivering the local anesthetic and the local anesthetic dose-extending component to mammalian tissue, a concentration of the local anesthetic in the mammalian tissue 30 minutes after delivery is about 31% to about 54% than a concentration of
17 . The device of claim 16 , wherein the coating comprises 10 to 75 wt-% of the at least one excipient, based upon total weight of solids in the coating.
18 . The device of claim 16 , wherein the excipient is selected from the group consisting of sucrose, dextrins, dextrans, hyroxyethyl cellulose (HEC), polyvinyl pyrrolidone (PVP), polyethylene glycols, amino acids, peptides, polysorbate, human serum albumin, saccharin sodium dehydrate, and a combination thereof.
19 . The device of claim 16 , wherein the at least one excipient is a saccharide.
20 . The device of claim 18 , wherein the saccharide is selected from the group consisting of dextran, sucrose, trehalose, and a combination thereof.
21 . The device of claim 16 , wherein the local anesthetic is present in an amount of 20 to 90 wt %, based upon total weight of solids in the coating.
22 . The device of claim 16 , wherein the dose-extending component is present in an amount of 2 to 48 wt %, based upon total weight of solids in the coating.
23 . The device of claim 16 , wherein the coating is present on the microneedles in an average amount of 0.01 to 2 micrograms per microneedle.
24 . The device of claim 16 , wherein the microneedles have a height of 200 to 1000 micrometers.
25 . The device of claim 23 , wherein at least 50% of the microneedles have the coating present on the microneedles near the tip and extending not more than 50 percent of the distance toward the base.
26 . A medical device, comprising an array of dissolvable microneedles, the microneedles comprising:
a dissolvable matrix material;
a local anesthetic selected from the group consisting of lidocaine, prilocaine, and a combination thereof, and
a local anesthetic dose-extending component selected from the group consisting of tetracaine, ropivacaine, bupivacaine, procaine and a combination thereof,
wherein the local anesthetic and the local anesthetic dose-extending component are in a non-eutectic weight ratio, and
wherein the dose-extending component/local anesthetic weight ratio is 0.1 to 0.9; and
wherein upon topically delivering the local anesthetic and the local anesthetic dose-extending component to mammalian tissue, a concentration of the local anesthetic in the mammalian tissue 30 minutes after delivery is about 31% to about 54% than a concentration of the local anesthetic in the mammalian tissue immediately after delivery.