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Abuse deterrent compositions and methods of use

Inactive Publication Date: 2014-09-18
OHEMO LIFE SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides pharmaceutical compositions that can be used to treat various conditions. These compositions can also reduce the feeling of being "high" or "euphoric" associated with them, and decrease the potential for abuse in individuals who take opioid or stimulant-containing compositions. Overall, the invention provides new ways to formulate drugs that are safer and more effective in treating various medical conditions.

Problems solved by technology

With these general types of drugs, there is the potential of abuse and improper administration that may result in drug overdose, addiction, suboptimal efficacy, and / or death.
Central nervous stimulants are often used to increase mental alertness, and they can results in feelings of exhilaration and energy.
While pain medications, medications to reduce or eliminate anxiety attacks (psychotherapeutic drugs), stimulants and sleeping pills can be safe, effective, and therapeutically useful when administered properly, such drugs are susceptible to abuse.
Individuals seeking to abuse these drugs will often tamper with oral dosage forms containing the drugs to achieve this “high.” For example, a large amount of tablets can be placed in a liquid to form a solution, and abusers either consume the liquid or more often filter and inject the solution.
Nasal insufflation, which is another term for the inhalation of substances through the nose, is a common and harmful practice among abusers.
Long-term practice of nasal insufflation can result in permanent damage to nasal tissue and increased incidence of toxicity and overdose.

Method used

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  • Abuse deterrent compositions and methods of use

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0111]The following formulations were tested:

mg / tab(approximate amounts)IngredientTest ATest BPresent inBinder(s)300300Tablet CoreFiller(s)5050Tablet CoreGlidant55Tablet CoreLubricant1010Tablet CoreEudragit NE 30D67671st CoatingFiller25251st CoatingSurfactant0.250.251st CoatingGlidant551st CoatingEudragit NE30D12.512.52nd CoatingEudragit NM30D12.512.52nd CoatingOxycodone30302nd CoatinghydrochlorideSurfactant112nd CoatingGlidant222nd CoatingEUDRAGIT ® E100103rd CoatingETHOCEL ® 4533rd Coating(ethylcellulose)Plasticizer23rd CoatingLubricant53rd CoatingOpadry II film-coating10104th CoatingTOTAL TABLETabout 550 mgabout 530 mgWEIGHT

[0112]The following tables show the dissolution profile of TEST A tablets, which are tablets of the present invention; TEST B tablets and ROXICODONE® tablets, which are comparative tablets.

[0113]TABLE 1 shows the dissolution profile in acidic conditions (0.1 N Hydrochloric acid).

TABLE 1Comparative Dissolution Profile in 0.1N Hydrochloride acid; 500 mL;Paddles,...

example 2

[0115]The following coating formulations were tested, both in acidic medium (HCl) and neutral pH medium (deionized water):

Amount in mgIngredientsCoating 1Coating 2Coating 3Coating 4Coating 5Coating 6EUDRAGIT ® E10010.020.010.010.00.010.0DBS1.53.01.51.51.51.5Magnesium Stearate3.57.03.53.53.53.5ETHOCEL ® 450.00.02.03.03.05.0*Ethanol13527015316272180Total weight gain15.030.017.018.08.020.0Release in HClAcceptableAcceptableAcceptableAcceptableAcceptableNotacceptable;NLT 75%requiredafter 45minutesRelease In DI WaterVery fast; Very fast;ReleaseAcceptableVery fast; Acceptablenotnotmore thannotacceptableacceptable10% afteracceptable60 minutes;notacceptable*Evaporated during the process

Dissolution Data for the Above Examples in 0.1 N HCl and DI Water

[0116]

% Released for the above examples in 0.1N HCl and DI WaterTimeCoating 1Coating 2Coating 3Coating 4Coating 5Coating 6(min) HClWaterHClWater HClWaterHClWater HClWater HClWater5494057585322105051201075697975834641767513015918492929989229189260...

example 3

[0117]The following study was conducted to determine the relative bioavailability and abuse potential of equivalent doses of a crushed and intact formulation. The study was a randomized, double-blind study, wherein 26 subjects were tested. The following formulation was tested:

[0118]An extended release tablet formulation of the present invention containing 60 mg of morphine sulfate pentahydrate was tested.

[0119]The following mean exposures (AUC0-t) were observed after oral administration of a 60 mg intact tablet and intranasal administration of a ground 60 mg tablet.

MORPHINEM6GAUC (ng · h / mL)AUC (ng · h / mL)intranasaloralintranasaloraladministration ofadministrationadministration ofadministration ofground tabletof intact tabletground tabletintact tabletCmax24.0317.7249.41106.98AUC 0-t158.3132.86385.58830.12AUC 0-0.52.531.760.481.84AUC 0-110.176.963.8417.33AUC 0-231.421.530.8995.04AUC 0-8109.9685.64233.64537.79AUC 0-12130.18101.14294.23649.01AUC 0-24162.78132.92398.2830.29

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Abstract

Orally administrable pharmaceutical compositions, methods of administration, and methods of making the same are provided. The pharmaceutical compositions provide abuse deterrent properties.

Description

CROSS REFERENCE TO RELATED APPLICATION[0001]This application claims the benefit of U.S. Patent Provisional Application No. 61 / 799,096, filed on Mar. 15, 2013, which is incorporated herein by reference.FIELD OF THE INVENTION[0002]The present invention provides orally administrable pharmaceutical compositions, methods of administration, and methods of making the same.BACKGROUND OF THE INVENTION[0003]The present invention relates to orally administrable pharmaceutical compositions, and specifically relates to compositions that are designed to reduce the potential for improper administration of medications and their use in a non-indicated or non-prescribed manner. The present invention can comprise any drug, and it is especially useful with medications that are subject to abuse, such as drugs affecting the central nervous system. For example, the present invention is particularly useful for pain medications, medications to reduce or eliminate anxiety attacks, stimulants and sleeping pil...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61K31/485A61K9/20
CPCA61K9/2086A61K31/485A61K9/2846A61K9/5073A61K45/06
Inventor SHAH, MANISH S.DIFALCO, RAY J.AIGNER, STEFAN
Owner OHEMO LIFE SCI INC
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