Transdermal delivery systems with pharmacokinetics bioequivalent to oral delivery

Inactive Publication Date: 2018-02-01
CORIUM LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0028]In another embodiment, systems comprising (a) one or more of the aforementioned drug reservoirs; (b) a rate controlling membrane or a non-woven layer; and (c) a contact adhesive; and (d) optionally a permeation enhancer included in one or both of the drug reservoir and/or the contact adhesive are described. In embodiments, the rate controlling membrane is a microporous polypropylene membrane.
[0029]In another embodiment, systems comprising (a) one or more of the aforementioned drug reservoirs; (b) a rate controlling membrane or a non-woven layer; and (c) a contact adhesive comprising a higher alcohol and a biocompatible polymer, optionally together with a matrix modifier and further optionally dispersive silica are provided. In embodiments, the contact adhesive comprises the higher alcohol, the biocompatible polymer and the matrix modifier. In other embodiments, the contact adhesive comprises the higher alcohol, the biocompatible polymer and the dispersive silica.
[0030]In a related embodiment, systems comprising (a) one or more of the aforementioned drug reservoirs; (b) a rate controlling membrane or a non-woven layer; and (c) a contact adhesive comprising a higher alcohol selected from the group consisting of lauryl alcohol, isostearyl alcohol, octyldodecanol, and oleyl alcohol and a biocompatible polymer selected from polyisobutylene (PIB), silicone polymers, acrylate copolymers, butyl rubber, polybutylene, styrene-iosprene-styrene block copolymers, styrene-butadiene-styrene block copolymers, ethylene-vinyl acetate (EVA), or a mixture thereof or a copolymer thereof, optionally together with a matrix modifier selected from the group consisting of cross-linked polyvinylpyrrolidone (PVP), soluble PVP, cellulose derivatives, polyacrylamide, polyacrylic acid and clay and further optionally high purity amorphous anhydrous colloidal silicon dioxide are provided.
[0031]In one particular embodi

Problems solved by technology

Other limitations of the related art will become apparent to those of skill

Method used

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  • Transdermal delivery systems with pharmacokinetics bioequivalent to oral delivery
  • Transdermal delivery systems with pharmacokinetics bioequivalent to oral delivery
  • Transdermal delivery systems with pharmacokinetics bioequivalent to oral delivery

Examples

Experimental program
Comparison scheme
Effect test

example 1

Donepezil Transdermal Delivery System

[0172]A transdermal delivery system comprising donepezil was prepared as follows.

[0173]Preparation of Drug Reservoir:

[0174]1.20 grams of sorbitan monolaurate (SPAN® 20) was dissolved in 6.00 g of triethyl citrate and mixed with 1.80 grams of lauryl lactate and 89.69 grams of ethyl acetate. 6.00 grams of glycerin (glycerol) was added and mixed. 9.00 grams of donepezil hydrochloride and 1.82 grams of sodium bicarbonate were added and dispersed in the mixture. 12.00 grams of crosslinked, micronized polyvinylpyrrolidone (KOLLIDON® CL-M) was then added and the mixture was homogenized. To the homogenized drug dispersion, 43.93 grams of acrylic acid / vinyl acetate copolymer (DURO-TAK® 387-2287, solid content 50.5%) was added and well mixed. The wet adhesive formulation was coated on a release liner and dried using a lab coater (Werner Mathis) to yield a dry coat weight of 12 mg / cm2.

[0175]Preparation of Contact Adhesive:

[0176]0.60 grams of sorbitan monola...

example 2

In Vivo Administration of Donepezil from a Donepezil Transdermal Delivery System

[0180]Transdermal delivery systems comprising donepezil were prepared as described in Example 1. Twelve (12) human subjects were randomized into two groups for treatment with a transdermal delivery system (n=6) or with orally administered donepezil (ARICPET®), 5 mg taken on day one and on day 7 of the study. The transdermal delivery system was applied to the skin and worn for one week and then removed. Blood samples were taken daily from the subjects treated with the transdermal delivery system. Blood samples were taken at frequent hour intervals on day 1 and day 7 in the group treated with orally delivered donepezil, and again on days 8, 10, 12 and 14. Mean plasma concentration of donepezil in the treatment groups are shown in FIGS. 2A-2B.

example 3

Memantine Transdermal Delivery System

[0181]A transdermal delivery system comprising memantine was prepared as follows. 10 grams (g) of memantine base was dissolved in a mixture of 82.42 g ethyl acetate, 4.34 g isopropyl alcohol, 12 g of propylene glycol, and 6.48 g levulinic acid to form a clear solution. 7.0 g fumed silica (AEROSIL® 200P) was added and the mixture was homogenized. 127.8 g acrylic acid / vinyl acetate copolymer (DURO-TAK® 387-2287, solid content 50.5%) was added and mixed until the mixture become homogenous.

[0182]The adhesive formulation mixture was coated on a siliconized polyethylene terephthalate liner and dried in a Werner Mathis coater at 60° C. for 8 minutes to yield a dry adhesive layer with a coat weight of 90 gram per square meter. A transdermal delivery system was fabricated using two of the dry adhesive layers sandwiched together with a non-woven polyester fabric between the two adhesive layers. Then, coated polyethylene terephthalate liner was replaced wit...

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Abstract

A method for delivering a therapeutic agent to a subject from a transdermal delivery system is described, where the therapeutic agent (i) has a half-life in the blood when delivered orally of greater than about 48 hours and (ii) is for the treatment of a chronic condition. The transdermal delivery system achieves transdermal delivery of the therapeutic agent at steady state that is bioequivalent to administration of the therapeutic agent orally, wherein bioequivalency is established by (a) a 90% confidence interval of the relative mean Cmax and AUC of the therapeutic agent administered from the transdermal delivery system and via oral delivery between 0.70 and 1.43 or between 0.80 and 1.25, or (b) a 90% confidence interval of the ratios for AUC and Cmax of the therapeutic agent administered from the transdermal delivery system and via oral delivery between 0.70 and 1.43 or between 0.80 and 1.25.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application No. 62 / 504,408, filed May 10, 2017; U.S. Provisional Application No. 62 / 504,391, filed May 10, 2017; U.S. Provisional Application No. 62 / 457,794, filed Feb. 10, 2017; U.S. Provisional Application No. 62 / 423,133, filed Nov. 16, 2016; U.S. Provisional Application No. 62 / 367,542, filed Jul. 27, 2016; and U.S. Provisional Application No. 62 / 367,502, filed Jul. 27, 2016, each incorporated herein by reference in its entirety.TECHNICAL FIELD[0002]The subject matter described herein relates to transdermal delivery of a therapeutic agent from a system designed to provide pharmacokinetics bioequivalent to oral delivery of a similar dose of the therapeutic agent.BACKGROUND[0003]Transdermal delivery of a therapeutically active agent through the skin provides a means for a sustained, constant plasma level of the agent. It differs from conventional therapy via oral administration in th...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/10A61K9/00
CPCA61K9/7038A61K9/0014A61K47/38A61K31/56A61K47/10A61K9/7061A61K9/7092A61K31/13A61K31/137A61K9/7084A61K31/445A61P25/00A61P25/28A61K47/02A61K47/12A61K47/32
Inventor SINGH, PARMINDERLEE, EUN SOOJAIN, AMIT K.
Owner CORIUM LLC
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