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

A technology for compositions and medicines, which can be used in pharmaceutical formulations, powder delivery, pill delivery, etc., and can solve problems such as the ability to trouble the final amount

Inactive Publication Date: 2009-10-14
创塞伯特制药公司
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  • 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

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  • 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

[0255] Example 2. Zolpidem Chewing Gum Composition

[0256] This example illustrates the zolpidem chewing gum composition of the present invention.

[0257] 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.

[0258] 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

[0266] Example 3. Zolpidem Tablet Composition

[0267] This example illustrates slow-dissolving, fast-dissolving, and chewable zolpidem tablet compositions of the present invention.

[0268] 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. e...

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Abstract

The present invention provides novel compositions for the delivery of hypnotics across the oral mucosa. Specifically, the buffer system in the compositions of the present invention raises the pH of saliva to a pH of greater than about 7.8, thereby promoting substantially complete conversion of the hypnotic agent from its ionized form to its unionized form. As a result, doses of hypnotics are rapidly and efficiently absorbed by the oral mucosa with surprisingly low inter-individual variability. Additionally, delivery of hypnotics across the oral mucosa advantageously avoids hepatic first-pass metabolism of the drug and avoids enzymatic degradation of the drug within the gastrointestinal tract. The invention also provides methods of treating sleep disorders such as insomnia using the compositions of the invention.

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 As short-, medium-, or long-acting hypnotic drugs, it has been proved to be useful in the treatment of insomnia. These benzodiazepines thought to bind benzodiazepines non-selectively 1(ω1) and benzodiazepines 2 (ω2) receptors. These non-selective combinations can cause benzodiazepines Some potential problems associated with compounds as sleeping pills. For example, some benzodiazepines Thought to inte...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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
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