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Particles containing an opioid receptor antagonist and methods of use

a technology of opioid receptor and opioid receptor, applied in the field of opioid receptor antagonists and drug delivery, can solve the problems of limited efficacy of common treatments of bulking agents and laxatives, affecting so as to improve the absorption of opioid receptor antagonists. , the effect of reducing the dose required

Inactive Publication Date: 2011-10-13
UNIVERSITY OF CHICAGO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]The present invention provides methods and compositions involving particles comprising an opioid receptor antagonist. In some embodiments, these particles allow for enhanced effects on opioid-induced bowel dysfunction and other indications. For example, particles of the present invention may result in improved absorption of the opioid receptor antagonist into the circulatory system compared to traditional formulations, thus resulting in a decrease in the dose required to reach therapeutic plasma levels. The particles may also be employed in preventative methods as well, such as to prevent opioid-induced side effects. Moreover, the opioid responsible for the opioid-induced effects may be an exogenously administered opioid, or an endogenous opioid that is produced by a patient in response to, for example, abdominal surgery. Chronic opioid users may also benefit from receiving particles of the present invention. Particles may comprise enteric coatings and / or time-release agents to assist in targeted or controlled absorption of the opioid receptor antagonist.

Problems solved by technology

However, their use is associated with a number of undesirable side effects.
Opioid-induced changes in gastrointestinal motility are almost universal when these drugs are used to treat pain, and at times may limit their use, leaving the patient in pain.
Common treatments of bulking agents and laxatives have limited efficacy and may be associated with side effects such as electrolyte imbalances.
However, high levels of MNTX in the plasma can lead to undesirable side effects such as orthostatic hypotension.

Method used

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  • Particles containing an opioid receptor antagonist and methods of use
  • Particles containing an opioid receptor antagonist and methods of use
  • Particles containing an opioid receptor antagonist and methods of use

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Particles Comprising Methylnaltrexone

[0138]A procedure developed by the Alonso lab from the School of Pharmacy, University of Santiago de Compostela, Spain was employed (Calvo et al., 1997; Fernandez-Urrusuno et al., 1999).

[0139]Methylnaltrexone (MNTX) (Mallinckrodt Chemicals, St. Louis, Mo.) was dissolved in water and then incorporated in an aqueous pentasodium tripolyphosphate (TPP) solution. Under high-speed magnetic stirring of an aqueous chitosan solution, the MNTX-containing TPP solution was slowly added into the chitosan solution. Nanoparticles containing MNTX were then formed. The final ratio of chitosan:TPP:MNTX was approximately 5 / 1.8 / 3.2 (w / w / w). MNTX nanoparticles were collected by centrifugation, supernatants were discarded and the remaining nanoparticles were lyophilized.

example 2

Preparation of Enterically Coated Particles Comprising Methylnaltrexone

[0140]Enterically coated MNTX nanoparticles were prepared by encapsulating the nanoparticles of Example 1 with a Eudagrit® L100 and Myvacet® 9-45 mixture. See, e.g., U.S. Pat. No. 6,608,075 and Yuan et al., 2000, each of which is incorporated herein by reference in its entirety. The final substance was the 30-80 mesh fraction which was 60% MNTX nanoparticles by weight. It was shown to decrease release of the drug at gastric pH by 90% based on the methods of the United States Pharmacopoeia / National Formulary (The United States Pharmacopeia, 1995). See also U.S. Pat. No. 6,608,075 and Yuan et al., 2000.

example 3

Preparation of a Heteroparticulate Particle Comprising Methylnaltrexone

[0141]Methodology as described by Beck et al., 2004 was followed. To prepare the outer particles, a lipophilic solution consisting of Epikuron 170® (0.1532 g), a polymer (poly(caprolactone) (PCL) (MW=60,000 g / mol) or Eudragit® 5100) (1.0 g) and acetone (267.0 ml) was used. This organic phase was added to an aqueous solution (533.0 ml) containing Tween 80® (0.1532 g) under moderate magnetic stirring. The solution was concentrated by evaporation under reduced pressure, and then the final volume was adjusted to 100 ml using acetone, corresponding to a polymer concentration of 10 mg / ml.

[0142]To prepare the inner particle, an MNTX solution (17 mM, 50 mL) was added to Aerosil® 200 (1.50 g). The mixture was fed into a mini-spray-dryer to produce particles having an MNTX core (feed rate: 3.0 ml / min; air flow rate: 500 NL / hr; atomizing air pressure: 200 kPa; inlet temperature: 170±4° C.; outlet temperature: 110±4° C.; noz...

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Abstract

Particles comprising an opioid receptor antagonist as well as methods of their use and methods of their preparation are provided herein. Such particles may be used for treating and preventing opioid-induced side effects in patients, and may be provided to chronic opioid users as well.

Description

[0001]The present application claims the benefit of priority to U.S. Provisional Application No. 61 / 077,242, filed Jul. 1, 2008 the entire contents of this application being incorporated by reference.BACKGROUND OF THE INVENTION[0002]1. Field of the Invention[0003]The present invention relates to the fields of opioid receptor antagonists and drug delivery. In general, particles comprising an opioid receptor antagonist are described along with methods of their use.[0004]2. Description of Related Art[0005]Opioids are effective analgesics. However, their use is associated with a number of undesirable side effects. One such effect is constipation. Opioid-induced changes in gastrointestinal motility are almost universal when these drugs are used to treat pain, and at times may limit their use, leaving the patient in pain. Common treatments of bulking agents and laxatives have limited efficacy and may be associated with side effects such as electrolyte imbalances.[0006]One treatment for op...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61P1/00A61K9/50A61K31/485B82Y5/00
CPCA61K9/5138A61K31/485A61K31/00A61K9/5161A61P1/00A61P1/04A61P1/08A61P1/10A61P1/16A61P1/18A61P7/06A61P9/00A61P9/10A61P9/14A61P13/02A61P17/00A61P17/04A61P25/04A61P25/22A61P27/02A61P29/00A61P35/00A61P37/06A61P43/00
Inventor YUAN, CHUN-SU
Owner UNIVERSITY OF CHICAGO
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