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Administration of benzodiazepine compositions

Inactive Publication Date: 2009-10-15
NEURELIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0018]In some embodiments, the composition comprises at least one additional ingredient selected from the group consisting of: active pharmaceutical ingredients; enhancers; excipients; and agents used to adjust the pH, buffer the composition, prevent degradation, and improve appearance, odor, or taste.
[0027]In some embodiments, the composition comprises at least one additional ingredient selected from the group consisting of: active pharmaceutical ingredients; enhancers; excipients; and agents used to adjust the pH, buffer the composition, prevent degradation, and improve appearance, odor, or taste.

Problems solved by technology

This completely or substantially reduces the ability of the neuron to carry an action potential.
The ability to utilize these and other types of formulations has been significantly limited due, in many cases, to solubility challenges.
For example, the amount of time required for an orally administered benzodiazepine drug to reach therapeutically relevant concentrations in blood plasma may be rather long, such as an hour or more.
Moreover, as benzodiazepine drugs pass through the liver a significant amount may be metabolized.
Thus, it may require large doses to achieve therapeutic plasma levels.
Furthermore, due to the nature of seizures and muscle spasms, it can be extremely difficult for either a patient or a care-giver to administer the benzodiazepine drug orally.
However intravenous administration is generally limited to trained health care professionals in tightly controlled clinical settings.
Furthermore, administering any drug intravenously can be painful and is likely impractical for patients suffering from a phobia of needles.
However, the inconvenience of suppositories is an obvious impediment to their being administered by anyone outside a very small group of the patient's intimate acquaintances and the patient's professional medical caretakers.

Method used

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  • Administration of benzodiazepine compositions
  • Administration of benzodiazepine compositions
  • Administration of benzodiazepine compositions

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0196]A pharmaceutical composition comprising diazepam is prepared. It is formulated as a solution to be delivered via a nasal delivery device. The composition is used to treat or prevent seizures associated with epilepsy in adults. Treatment is administered either before or after a seizure has begun. If the patient is seizing, it is administered as 1 puff from any nasal delivery device (1 puff at 5.0 mg / puff (5.0 mg / 0.1 mL and 0.1 mL / puff)) every 5 minutes until cessation of the seizure. However, it can be given as 1 puff per nostril in each nostril (2 puffs at 2.5 mg / puff (5.0 mg / 0.1 mL and 0.05 mL / puff)) every 5 minutes until cessation of the seizure. The composition according to this example is set forth in the following table.

TABLE 1-15.0 mg / 0.1 mLDiazepam70.0 mgα-tocopherol  0.1 mLethanol (qs ad to 0.1 mL)

example 2

[0197]A pharmaceutical composition comprising diazepam is prepared. It is formulated as a solution to be delivered via a nasal delivery device. The composition is used to treat or prevent seizures associated with epilepsy in children. Treatment is administered either before or after a seizure has begun. If the patient is seizing, it is administered as 1 puff from any nasal delivery device (1 puff at 2.0 mg / puff (2.0 mg / 0.1 mL and 0.1 mL / puff)). If the seizure fails to stop another dose may be administered after 5 minutes. However, it can be given as 1 puff per nostril in each nostril (2 puffs at 1.0 mg / puff (2.0 mg / 0.1 mL and 0.05 mL / puff)). If the seizure fails to stop another dose may be administered after 5 minutes. The composition according to this example is set forth in the following table.

TABLE 2-12.0 mg / 0.1 mLDiazepam70.0 mgα-tocopherol  0.1 mLethanol (qs ad to 0.1 mL)

example 3

Formulation of Diazepam Solutions

[0198]In general, benzodiazepine solutions may be formulated by combining one or more natural or synthetic tocopherols or tocotrienols and one or more lower alcohols or glycols and mixing until a homogeneous mixture is formed, adding the benzodiazepine drug to the homogeneous mixture, heating and mixing the ingredients until the benzodiazepine is fully dissolved in the homogeneous mixture, cooling the mixture, and bringing the mixture to its final mass or volume with lower alcohol or glycol.

[0199]Two different diazepam solutions were formulated by the foregoing process. Vitamin E USP and dehydrated ethanol USP were combined in the amounts set forth in the following table and mixed to form a homogeneous mixture. Diazepam in the amounts set forth in the following table was then added to the homogeneous mixture. The ingredients were heated to 40-45° C. with mixing until the diazepam was fully dissolved, thereby forming a solution. The solution was coole...

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Abstract

The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.

Description

[0001]This application claims priority under 35 U.S.C. § 119(e) from U.S. provisional patent application No. 61 / 040,558, which was filed on Mar. 28, 2008, and which is incorporated herein in its entirety.FIELD OF THE INVENTION[0002]This application relates to the nasal administration of benzodiazepine drugs and combinations thereof.BACKGROUND OF THE INVENTION[0003]By way of non-limiting example, the benzodiazepine family consists of drugs such as diazepam, lorazepam, and medazepam. The drugs in this family have been observed as possessing sedative, tranquilizing and muscle relaxing properties. They are frequently classified as an anxiolytic and skeletal muscle relaxants. They are thought to be useful in preventing, treating, or ameliorating the symptoms of anxiety, insomnia, agitation, seizures (such as those caused by epilepsy), muscle spasms and rigidity (which can be caused by tetanus), the symptoms of drug withdrawal associated with the continuous abuse of central nervous system...

Claims

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Application Information

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IPC IPC(8): A61K31/5513
CPCA61K9/0043A61K31/5513A61K31/355A61K9/008A61P25/08A61P25/22
Inventor CARTT, STEVEMEDEIROS, DAVIDGWOZDZ, GARY THOMASLOXLEY, ANDREWMITCHNICK, MARKHALE, DAVID F.
Owner NEURELIS INC
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