Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Compositions for delivering hypnotic agents across the oral mucosa and methods of use thereof

A technology of oral mucosa and composition, applied in the field of composition and its usage for delivering hypnotic drugs through oral mucosa, capable of solving problems such as the trouble of the final amount

Inactive Publication Date: 2007-03-14
创塞伯特制药公司
View PDF5 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The variability of these rates between different users further complicates the ability to predict the final amount of drug entering the systemic circulation

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Compositions for delivering hypnotic agents across the oral mucosa and methods of use thereof
  • Compositions for delivering hypnotic agents across the oral mucosa and methods of use thereof
  • Compositions for delivering hypnotic agents across the oral mucosa and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0249] Embodiment 1. Zolpidem film test

[0250] This example illustrates the beneficial effect of pH adjustment on membrane permeation of zolpidem dosage forms.

[0251] Membrane assays can be used to show the effect of pH adjustment on the degree of ionization and thus on the degree of transmucosal penetration of therapeutic agents, see, e.g., Kansy et al., J. Med. Chem., 41:1007-1010 (1998); and Avdeef, Curr. Topics Med. Chem., 1:277-351 (2001). This test uses lipid-coated membranes to predict membrane penetration of lipidic mucosa. The membrane device consists of a dodecane membrane sandwiched between donor and recipient cells. The lipid-covered membrane is less porous than the oral mucosa. As such, the improvements seen in the membrane assay are likely to be amplified in vivo.

[0252] Membrane tests were performed using zolpidem tartrate solutions at pH conditions of 5.8, 6.8, and 7.8. Adjust the alkaline pH to 7.8 with freshly prepared 0.01 M sodium bicarbonate / sod...

Embodiment 2

[0254] Example 2. Zolpidem Chewing Gum Composition

[0255] This example illustrates the zolpidem chewing gum composition of the present invention.

[0256] Zolpidem can be formulated as a chewing gum composition as described above. In these embodiments, the unit dose or supply of chewing gum comprises from about 0.1 to about 100 milligrams (mg) of zolpidem (measured as its tartrate salt form), preferably from about 1 to about 50 mg, more preferably from about 2 to about 25 mg . In other embodiments, the unit dose comprises from about 2 to about 20 mg of zolpidem, preferably from about 5 to about 15 mg. Additional zolpidem may be added, such as up to about 10% to about 25% by weight, as an "overdose" or as an amount that is expected to be "washed out" and otherwise not released or absorbed during chewing.

[0257] In additional embodiments, the unit dose or supply of chewing gum comprises from about 0.81 to about 42 mg of the base form of zolpidem, more preferably from abou...

Embodiment 3

[0265] Example 3. Zolpidem Tablet Composition

[0266] This example illustrates slow-dissolving, fast-dissolving, and chewable zolpidem tablet compositions of the present invention.

[0267]Zolpidem can be formulated as a tablet composition as described above. In these embodiments, the unit dose or supply of tablets comprises from about 0.1 to about 100 milligrams (mg) of zolpidem (measured as its tartrate salt form), preferably from about 1 to about 50 mg, more preferably from about 2 to about 25 mg . In other embodiments, the unit dose comprises from about 2 to about 20 mg of zolpidem, preferably from about 2 to about 15 mg, more preferably from about 2 to about 10 mg, e.g., about 2, 3, 4, 5, 6, 7, 8 , 9, or 10 mg. In a particularly preferred embodiment, the unit dose comprises an amount of zolpidem that is less than the dose typically used in commercially available oral tablets, but which has comparable or greater bioavailability and efficacy of therapeutic activity. ef...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
The average particle sizeaaaaaaaaaa
Volumeaaaaaaaaaa
Login to View More

Abstract

The present invention provides novel compositions for the delivery of a hypnotic agent across the oral mucosa. In particular, the buffer system in the compositions of the present invention raises the pH of saliva to a pH greater than about 7.8, thereby facilitating the substantially complete conversion of the hypnotic agent from its ionized to its un-ionized form. As a result, the dose of hypnotic agent is rapidly and efficiently absorbed by the oral mucosa with surprisingly low inter-subject variability. Furthermore, delivery of the hypnotic agent across the oral mucosa advantageously bypasses hepatic first pass metabolism of the drug and avoids enzymatic degradation of the drug within the gastrointestinal tract. Methods for using the compositions of the present invention for treating sleep disorders such as insomnia are also provided.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Patent Application 10 / 783,118, filed February 17, 2004, which has become a U.S. Provisional Application, and U.S. Provisional Application 60 / 598,629, filed August 3, 2004, each of which is incorporated in its entirety incorporated herein by reference. Background of the invention [0003] Insomnia is a condition that affects a person's ability to fall asleep or stay asleep. It is the most common sleep disorder, affecting millions of Americans each year. Benzodiazepines have been shown to be useful in the treatment of insomnia as short-, medium-, or long-acting hypnotics. These benzodiazepines are thought to bind non-selectively to benzodiazepine 1 (ω1) and benzodiazepine 2 (ω2) receptors. These non-selective bindings can cause some potential problems associated with the use of benzodiazepines as hypnotics. For example, some benzodiazepines are thought to interfere with memory, ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/20A61K9/14A61K9/68A61K9/28
Inventor 尼基莱什·N·辛格
Owner 创塞伯特制药公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com