Aqueous gel formulation and method for inducing topical anesthesia

Abstract

Disclosed is a stable aqueous gel formulation suitable for topical use comprising water, an anesthetic (e.g., lidocaine hydrochloride), a viscoelastic polymer, and a tonicity modifier, wherein the aqueous gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile and has low particulate count. Also disclosed is a method of inducing topical anesthesia on a tissue or organ, e.g., the eye, of an animal comprising providing a stable aqueous gel formulation comprising water, an anesthetic, a viscoelastic polymer, and a tonicity modifier, wherein the aqueous gel formulation is free of preservatives and phosphate buffer, is isotonic with physiological fluids, and is sterile, and topically administering an effective amount of the aqueous gel formulation to the tissue or organ of the animal.

Description

CROSS-REFERENCE TO A RELATED APPLICATION[0001]This is a continuation-in-part of U.S. patent application Ser. No. 11 / 491,611, filed Jul. 24, 2006, the disclosure of which is incorporated by reference.BACKGROUND OF THE INVENTION[0002]Anesthesia is a process commonly used to block the perception of pain. The first public demonstration of administering an anesthetic agent occurred over 150 years ago when diethyl ether was utilized during a surgical operation to remove a tumor. Today, anesthetic agents are utilized in patient procedures across the medical specialties.[0003]Anesthetic agents are used in procedures carried out on various tissues and organs. For example, with regard to procedures performed on the eye, common anesthetic agents utilized include subconjunctival injections of aqueous lidocaine and tetracaine drops. However, subconjunctival injections of aqueous lidocaine are less than desirable as many patients suffer from anxiety caused by needle phobia and / or the physical pai...

AI Technical Summary

Benefits of technology

[0005]The foregoing need has been fulfilled to a great extent by the invention which provides an aqueous gel formulation comprising water, an anesthetic, a viscoelastic polymer, and a tonicity modifier. Specifically, the invention provides an aqueous gel formulation which comprises, consists essentially of, or consists of, water, an anesthetic, a viscoelastic polymer, and a tonicity modifier. The formulation may also contain a pH adjusting agent or a product produced as a result of pH adjustment. Advantageously, the gel formulation is free of preservatives and / or phosphate buffer. The aqueous gel formulation of the invention is targeted for application to various tissues or organs (internal or external) of an animal, particularly to the eye of a human. The invention also provides a method for inducing topical anesthesia to a tissue or organ of an animal. The administration of the topical formulation of the invention preferably avoids the need to administer a subsequent administration (e.g., topical or injection) of the anesthetic during a medical procedure.

[0006]The aqueous gel formulation of the invention is viscous and reduces the potential for systemic absorption through nasolacrimal system, thereby reducing the risk of systemic toxicity. The aqueous gel formulation is also free of preservatives that can cause allergic reactions that are associated with corneal toxicity. The aqueous gel formulation does not cause significant corneal epithelial defects or irregularities. The aqueous gel formulation is also associated with reduced corneal drying and epithelial decompensation. With its extended corneal contact and effective anesthesia at low concentrations, the aqueous gel formulation of the invention fulfills an unmet need in the ophthalmic pharmacopeia for a topical ocular anesthetic.

Problems solved by technology

However, subconjunctival injections of aqueous lidocaine are less than desirable as many patients suffer from anxiety caused by needle phobia and / or the physical pain caused by the actual injection.

However, there are some drawbacks with such drops.

Some of the drops administered to patient may miss the eye due to the shaking of the hand or the blinking of the eye.

Thus, the anesthetic efficacy of the tetracaine drops could become insufficient since both the onset of anesthesia is not rapid, and the duration of anesthetic activity is limited.

In addition, tetracaine may also be toxic to the cornea.