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Robust sustained release formulations

A sustained-release preparation and sustained-release technology, applied in the field of sustained-release pharmaceutical preparations, can solve the problems of low oral bioavailability and short duration of action of immediate-release oxymorphone

Inactive Publication Date: 2009-11-11
PENWEST PHARMA CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, evidence from past clinical trials and clinical experience suggest that immediate-release oxymorphone has a short duration of action and may require dosing every 4 hours to maintain optimal levels of analgesics in patients with chronic pain
Also, because oxymorphone is extensively metabolized in the liver, the oral bioavailability of immediate-release oxymorphone is low

Method used

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Examples

Experimental program
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other Embodiment approach

[0177] Other embodiments provide a drug comprising about 1-200 mg of oxymorphone hydrochloride, or about 5-80 mg of oxymorphone hydrochloride; and about 80-200 mg of an extended release delivery system, or about 120-200 mg of an extended release delivery system, or about 160 A robust sustained release solid dosage form formulation of a milligram sustained release delivery system; wherein the sustained release delivery system comprises about 8.3-41.7% locust bean gum, or about 25% locust bean gum; at least about 30% of the xanthan gum particles are capable of About 25-41.7% xanthan gum that passes through a #270 mesh sieve, or about 25% xanthan gum that at least about 30% of the particles are able to pass through a #270 mesh sieve; about 20-55% dextrose, or about 35% dextrose sugar; about 5-20% calcium sulfate dihydrate, or about 10% calcium sulfate dihydrate; and about 2-10% ethylcellulose, or about 5% ethylcellulose.

[0178] Some embodiments provide a drug comprising about 1...

other Embodiment approach

[0179] Other embodiments provide a drug comprising about 1-200 mg oxymorphone hydrochloride, or about 5-80 mg oxymorphone hydrochloride; and about 200-420 mg sustained release delivery system, or about 300-420 mg sustained release delivery system, or about 360 mg A robust sustained release solid dosage form formulation of a milligram sustained release delivery system; wherein the sustained release delivery system comprises about 8.3-41.7% locust bean gum, or about 25% locust bean gum; at least about 30% of the xanthan gum particles are capable of About 8.3-41.7% xanthan gum that passes through #270 mesh, or about 25% xanthan gum that at least about 30% of the particles are able to pass through #270 mesh; about 20-55% dextrose, or about 35% dextrose sugar; about 5-20% calcium sulfate dihydrate, or about 10% calcium sulfate dihydrate; and about 2-10% ethylcellulose, or about 5% ethylcellulose.

[0180] When administered orally, the patient's robust sustained-release formulations...

Embodiment 1

[0211] Prepare TIMERx- Sustained Release Delivery System

[0212] Batches of TIMERx- Sustained release delivery system.

[0213]Batches of xanthan gum (Jungbunzlauer, Perhoven, Austria or CP Kelco, Chicago, IL) were tested for particle size using a series of mesh screens. These mesh screens include #270 mesh screens which allow particles less than 53 microns in diameter to pass through (fines). The weight fraction of xanthan gum particles passing through the mesh sieve (ie fraction of xanthan gum fines) was determined. Batches with known xanthan fines weight fractions were then prepared. Dry blend the necessary amounts of xanthan gum, locust bean gum, calcium sulfate and dextrose in a high speed mixer / granulator for 3 minutes to prepare TIMERx- A hydrophobic polymer (ethylcellulose) slurry was prepared by dissolving ethylcellulose in ethanol. The slurry was added to the above dry blend mixture and the material was pelletized for 4 minutes with the chopper / impeller run...

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Abstract

Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these fopnulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.

Description

1. Field of invention [0001] The present invention provides robust sustained release pharmaceutical formulations and methods of making and using them. The formulations of the invention saturate at least one drug and the sustained release delivery system. 2. Background of the invention [0002] Extended-release drug formulations often contain more drug than immediate-release formulations. The functionality and safety of sustained release formulations is based on the known controlled rate of drug release from the formulation over an extended period of time (eg, 8-24 hours) after administration. The drug release profile of the formulation often depends on the chemical environment of the sustained release formulation, such as pH, ionic strength, and the presence of solvents such as ethanol. [0003] In some instances, the presence of relatively large amounts of drug in a sustained release formulation may be harmful to the patient if the drug is released from the formulation fa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/137A61K31/485A61P25/04
CPCA61K9/2054A61K9/2018A61K9/205A61P25/04A61P25/30A61P25/32A61P25/36A61P29/00A61K9/20A61K31/485A61K47/36
Inventor A·R·拜奇沃K·菲茨莫里斯S·拉布齐斯基
Owner PENWEST PHARMA CO
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