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Abuse resistant opioid drug-ion exchange resin complexes having hybrid coatings

a technology of opioid drug and resin complex, which is applied in the direction of drug composition, dispersed delivery, microcapsules, etc., can solve the problems of particular abuse of opioid drugs, inability to easily extract opioid drugs, and at times associated side effects of opioid drugs, etc., and achieves favorable abuse resistance properties

Active Publication Date: 2012-05-31
TRIS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0013]Advantageously, the combination of sustained release provided by the complexation of the opioid drug with the ion exchange resin and the hybrid layer coating comprising the barrier coating component and the enteric coating component, provide a desired modified release profile while also providing favorable abuse resistance properties.

Problems solved by technology

However, opioid drugs are at times associated with side effects including, e.g., stomach upset and other gastrointestinal effects.
Further, because of the sometimes addictive properties of these drugs and the euphoria which can be associated with taking them, including through routes other than those prescribed, these opioid drugs are particular susceptible to abuse.
These antagonists cannot be easily extracted from the agonist and will cause an aversive effect in a physically dependent patient.
However, these antagonists may have other side effects which may be disadvantageous.
Further, there is no data in the '392 patent of prolonged release of the drug from the coated drug-ion exchange resin complex beyond about 12 hours.
There have been literature-reported drawbacks of using ethyl cellulose based aqueous dispersions as coatings for drug-ion exchange resin complexes.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Hybrid Coated Morphine Resin Complex

[0094]The following example describes the preparation of a hybrid coated morphine-ion exchange resin complex, in which the cation exchange resin utilized is the Amberlite IRP-69 brand cross-linked polysytrene resin. The formed morphine-ion exchange resin complex may be referred to as morphine polistyrex for convenience.

IngredientQuantityMorphine Resin ComplexMorphine Sulfate810gPurified Water13600gAMBERLITE IRP-69 RESIN1358gKOLLIDON K-30 polyvinylpyrrolidone180gPurified water421gCoated Morphine Resin ComplexKOLLICOAT SR-30D polymer system693.38g (208.0164 g solids)(30% dispersion)Triacetin10.37gSURETERIC 90G18507 White41.6gPolyvinylacetate phthalate polymersystemPurified Water554.65gMorphine Resin Complex600g

[0095]The following was performed at room temperature unless otherwise specified. The morphine resin complex was prepared by first dissolving 810 g of morphine sulfate in 13.6 liters of purified water, and then slowly adding 135...

example 2

Tabletting of Hybrid Coated Morphine-Resin Complex

[0099]

IngredientQuantityHybrid coated Morphine Ion Resin Complex266.84g(from example 1)Calcium silicate, (RXCIPIENT ™ FM1000)40.5gSilicon dioxide, (RXCIPIENT ™ GL100)4.5gMicrocrystalline cellulose, (AVICEL ® PH 101)127.74gCrospovidone, (KOLLIDON ™ CL-SF)18gLactose monohydrate, (FLOWLAC ™ 100)96.6gTalc (IMPERIAL ™ 500)9gMagnesium Stearate2.1gTOTAL565.28gHybrid Coated MorphineModified Release tabletsOPADRY ® WHITE YS-1-18202-A-PVAP20gPurified water80gHybrid Coated Morphine ER tablets200g

[0100]Hybrid coated Morphine Ion Resin Complex (266.84 g, from example 1), calcium silicate (RXCIPIENT™ FM1000) (40.5 g), silicon dioxide (RXCIPIENT™ GL100) (4.5 g), microcrystalline cellulose (AVICEL® PH 101) (127.74 g), crospovidone (KOLLIDON™ CL-SF) (18 g), lactose monohydrate (FLOWLAC™ 100) (96.6 g), and talc (IMPERIAL™500) (9 g) were passed through 40 mesh screen and mixed for 10 minutes using a cube blender (ERWEKA™ AR-402). Magnesium stearate (2....

example 3

Preparation of Hybrid Coated Morphine Modified Release Suspension

[0104]

IngredientQuantityPlacebo Suspension BaseCitric acid, anhydrous8gHigh Fructose Corn Syrup 421,200gSucrose600gStarch92gXanthan gum7.6gGlycerin400gMethylparaben7.2gPropylparaben0.8gStrawberry Banana Flavor44.88gPurified WaterQS 3484.91gHybrid Coated Morphine-Ion Exchange ResinComplex Modified Release SuspensionPurified Water200gSodium Metabisulfite1gPolysorbate 801gHybrid Coated Morphine Ion Exchange Resin18.59g(From Example 1)Placebo Suspension Base871.2gPurified WaterQS 1,000mL

[0105]A placebo suspension base was prepared by first dissolving 8 g of citric acid in an appropriate amount of purified water, followed by adding 600 g of sucrose and 1200 g of high fructose corn syrup to achieve complete solution. 92 g of starch was then slowly introduced to the main container under high shear mixing condition to achieve uniform dispersion. In another container, 400 g glycerin was added and heated to 45-50° C. followed by...

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Abstract

A sustained release formulation for opioid drugs is described. The formulation contains an opioid-ion exchange resin complex having a hybrid coating. The hybrid coating contains a cured polyvinylacetate polymer and a pH-dependent enteric coating layer mixed therein. Also provided are methods of making and using same.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001]This application claims the benefit under 35 USC 119(e) of U.S. Provisional Patent Application No. 60 / 941,169, filed May 31, 2007.BACKGROUND OF THE INVENTION [0002]Opioids are commonly prescribed because of their effective analgesic, or pain-relieving, properties. Medications that fall within this class, referred to as prescription narcotics, include morphine sulfate (e.g., Kadian®, Avinza™), codeine salts, oxycodone HCl (e.g., OxyContin™, Percodan™, Percocet™), and related drugs. For example, OxyContin™ tablets are presently commercially available in 10, 20, 40, 80, and 160 milligrams forms. Morphine, for example, is often used before and after surgical procedures to alleviate severe pain. Codeine, on the other hand, is often prescribed for mild pain. In addition to their pain-relieving properties, some of these drugs can be used to relieve coughs and diarrhea. Codeine and diphenoxylate (Lomotil™) are examples of such drugs. However, op...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/22A61P25/04
CPCA61K9/0095A61K9/10A61K47/4823A61K9/5026A61K47/48015A61K9/2081A61P25/04A61K47/585A61K47/52A61K47/61
Inventor MEHTA, KETANTU, YU-HSINGCHAUDHURI, ALIVIAPERUMAL, ASHOK
Owner TRIS PHARMA
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