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Sodium bicarbonate in situ conversion driven transdermal delivery of amine drug

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

AI Technical Summary

Benefits of technology

The patent text describes a study that measured the amount of memantine that can be delivered through different types of transdermal devices. The results showed that some formulations worked better than others, and that certain techniques could improve the efficiency of memantine delivery. Overall, the study provides a valuable tool for researchers to develop better ways of delivering memantine through the skin.

Problems solved by technology

There are a several significant drawbacks, however, in using the free base form in a transdermal formulation for many drugs.
For example, it is often difficult to solubilize a sufficient amount of free base in a drug-in-polymer matrix because the free base often has low solubility in the polymer matrix and tends to recrystallize into solid crystals during processing or during storage prior to use.
Further, certain liquid free base drugs are volatile, and a significant amount of the drug can be lost during processing due to evaporation.
Additionally, drug flux is often difficult to control and deliver for multiple days at a constant rate when a drug is very permeable through the skin.
Finally, drugs are often more unstable in the free base form than in the salt form.
In those prior attempts, the basic inorganic salts had a higher pKa value than the conjugated acid salt form of the amine drug, and as such, the converted free base was not soluble in the matrix and recrystallized into solid crystals, leading to decreased skin permeation.

Method used

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  • Sodium bicarbonate in situ conversion driven transdermal delivery of amine drug
  • Sodium bicarbonate in situ conversion driven transdermal delivery of amine drug
  • Sodium bicarbonate in situ conversion driven transdermal delivery of amine drug

Examples

Experimental program
Comparison scheme
Effect test

example 1

Donepezil Salt Transdermal Formulation with Sodium Bicarbonate

Preparation of Drug-in-Adhesive

[0117]An amount of 1.20 g of SPAN® 20 was dissolved in 6.00 g of triethyl citrate, and the solution was mixed with 1.80 g of lauryl lactate and 89.69 g of ethyl acetate. To the solution was added 6.00 g of glycerine and was mixed well. To the mixture, 9.00 g of donepezil hydrochloride and 1.82 g of sodium bicarbonate were dispersed. After addition of 12.00 g of KOLLIDON® CL-M to the drug dispersed solution, the mixture was homogenized by a Silverson mixer homogenizer. To the homogenized drug dispersion, 43.93 g of DURO-TAK® 387-2287 (solid content 50.5%) was added and mixed well. The wet adhesive formulation was coated on a release liner and dried using a Werner Mathis lab coater to get a dry coat weight of 12 mg / cm2.

Preparation of Contact Adhesive

[0118]An amount of 0.60 g of sorbitan monolaurate (SPAN® 20) was dissolved in 3.00 g of triethyl citrate, and mixed with 0.9 g of lauryl lactate, ...

example 2

Memantine Salt Transdermal Formulation with Sodium Bicarbonate

Preparation of Drug-in-Adhesive

[0123]An amount of 2.0 g of glycerine and 2.0 g of octyl dodecanol were mixed with a mixture of 29.35 g of ethyl acetate and 1.86 g of isopropyl alcohol. In the solution, 5.0 g of memantine hydrochloride and 1.95 g of sodium bicarbonate were dispersed by stirring. To the dispersion, 3.0 g of crosslinked polyvinylpyrrolidone (KOLLIDON® CL-M) was added and homogenized using a Silverson mixer homogenizer. To the homogenized drug dispersion, 11.99 g of acrylate copolymer (DURO-TAK® 387-2287, solid content 50.5%) was added and mixed well. The wet adhesive formulation was coated on a release liner and dried using a Werner Mathis coater to get a dry coat weight of 15 mg / cm2.

Preparation of Contact Adhesive

[0124]An amount of 2.0 g of octyl dodecanol was mixed with 20.67 g of n-heptane. After addition of 4.00 g of crosslinked polyvinylpyrrolidone (KOLLIDON® CL-M) to the solution, the mixture was homog...

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Abstract

Compositions, devices, and methods for transdermal administration of active agents provided in their salt form instead of neutral form are provided.

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 / 444,763, filed Jan. 10, 2017; U.S. Provisional Application No. 62 / 444,745, filed Jan. 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 herein incorporated by reference in its entirety.TECHNICAL FIELD[0002]The subject matter described herein relates to compositions, devices, and methods for transdermal administration of amine active agents provided in their salt form instead of neutral form.BACKGROUND[0003]Amine drugs exist in two forms, a free base and a salt. The salt form is the conjugated acid salt (i.e.,...

Claims

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Application Information

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IPC IPC(8): A61K47/02A61K31/00C08K5/00A61K9/70
CPCA61K47/02C08K5/0016A61K31/00A61K9/7023A61K9/7092A61K9/7038A61K47/12A61K47/10A61K45/00A61K9/7061A61K31/13A61K31/137A61K31/18A61K31/27A61K31/445A61K9/7084A61P13/00A61P13/02A61P13/08A61P25/00A61P25/02A61P25/04A61P25/14A61P25/16A61P25/22A61P25/24A61P25/26A61P25/28A61P25/36A61P35/00A61K47/32A61K9/7053A61K31/045
Inventor LEE, EUN SOOSINGH, PARMINDERSAGI, APPALAJAIN, AMIT K.
Owner CORIUM LLC