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3. Left 3.08: 10.3886/Icpsr23782v3 USOO84.81560B2 (12) United States Patent (10) Patent No.: US 8.481,560 B2 Stinchcomb et al. (45) Date of Patent: Jul. 9, 2013 (54) ABUSE DETERRENT TRANSDERMAL 2002/011 1377 A1 8, 2002 Stinchcomb FORMULATIONS OF OPIATEAGONSTS 38.86% A. 1398. SincesCCO) ea. AND AGONSTANTAGONSTS 2008/0076789 A1 3/2008 Stinchcomb et al. ......... 514,282 2008/0233.178 A1* 9/2008 Reidenberg et al. .......... 424/449 (75) Inventors: Audra Lynn Stinchcomb, Lexington, 2009.0017102 A1 1/2009 Stinchcomb et al. KY (US); Guohua Li, Lexington, KY 2009.0036523 A1 2/2009 Stinchcomb et al. (US); Stan Lee Banks, Frankfort, KY 3.s: A. ck 238 CCO)betal." ea. 514,646 (S), effey Lynn Howard Richmond, 2009/0246265 A1 * 10, 2009 Stinchcomb et al. ......... 424/449 SY (US); y Jerzy Golinski, 2010/0249045 A1 9, 2010 Babul ........................... 514,214 eX1ngton, OTHER PUBLICATIONS (73) Assignee: Alltranz Inc., Lexington, KY (US) U.S. Appl. No. 61/320,514, filed Apr. 2, 2010, Stinchcomb, et al. c - r U.S. Appl. No. 61/320,522, filed Apr. 2, 2010 Stinchcomb, et al. (*) Notice: St. tO E. site th still Nalluri, et al., “In Vitro Release Studies on Matrix TypeTransdermal p ls: e 22.d justed under Drug Delivery Systems of Naltrexone and Its Acetyl Prodrug”. Drug M YW- (b) by ayS. Development and Industrial Pharmacy, vol. 31, 2005, pp. 871-877. Satas, D., “15. Acrylic Adhesives'. Handbook of pressure sensitive (21) Appl. No.: 13/079,758 adhesive technology, (2" ed.), Satas D., ed., 1989 New York, NY: 1-1. Nostrand Reinhold. pp. 396-456. (22) Filed: Apr. 4, 2011 Sobieski., L.A. et al., "18. Silicone Pressure Sensitive Adhesives', O O Silicone Pressure Sensitive Adhesives, Handbook of pressure sensi (65) Prior Publication Data tive adhesive technology. (2" ed.), Satas. D., Ed. 1989, New York, US 2011/0245783 A1 Oct. 6, 2011 NY. Van Reinhold, pp. 508-517. Thong, et al., “Percutaneous Penetration Enhancers: An Overview”. Related U.S. Application Data Skin Pharmacology and Physiology, 2007, vol. 20, No. 6, pp. 272 AV 282. (60) Provisional application No. 61/320,526, filed on Apr. United States Department of Health and Human Services, Substance 2, 2010. Abuse and Mental Health Services Administration Office of Applied s Studies, National Survey on Drug Use and Health, 2007. (51) Int. Cl ICPSR23782-v3. Ann Arbor, MI: Inter-university Consortium for 3. we left 3.08: Political10.3886/ICPSR23782v3. and Social Research distributor, Jan. 4, 2013. doi: (52) U.S. Cl. * cited by examiner USPC ............................ 514/282: 514/279: 424/449 (58) Field of Classification Search Primary Examiner — Raymond Henley, III USPC ................................... 514/282, 278; 424/449 (74) Attorney, Agent, or Firm — Foley & Lardner LLP See application file for complete search history. (57) ABSTRACT (56) References Cited Described herein are abuse-resistant multi-layer transdermal patches comprising opioids and opioid prodrugs having a U.S. PATENT DOCUMENTS barrier layer located between the layer containing opioid or 4.584,355 A 4, 1986 Blizzard et al. 4,585,836 A 4, 1986 Homan et al. opioid prodrug and a layer containing an opioid antagonist or 4,591,622 A 5, 1986 Blizzard et al. opioid antagonist prodrug. 4,655,767 A 4, 1987 Woodard et al. 7,867,986 B2 1/2011 Houze 30 Claims, 4 Drawing Sheets U.S. Patent Jul. 9, 2013 Sheet 1 of 4 US 8.481,560 B2 ZZZZZYZZ YNYYYYY F.G. 4 U.S. Patent Jul. 9, 2013 Sheet 2 of 4 US 8.481,560 B2 E 0.5 S. 5 0.4 am Naitrexone sa 0.3 mas Total bupremorphine S0.2 O.1 O - -- ; -------- O 5 10 15 20 25 30 35 Time (min.) Figure 5. Release of NTX and total buprenorphine from buprenorphine prodrugnaltrexone patch (13% NTX-EC/HPC film, 5% BUPPD) in ethanol. mm Naltrexone --Total buprenorphine O 5 15 20 2S 30 Time (min.) Figure 6. Release of NTX and total buprenorphine from buprenorphine prodrugnaltrexone patch (13% NTX-EC/HPC film, 5% BUPPD) in water. U.S. Patent Jul. 9, 2013 Sheet 3 of 4 US 8.481,560 B2 -- Naloxote trial 1 -- Naloxone triad2 1.2 -- Total buprenorphinet trial 1 -o-Total bupremorphine trial 2 i is 4 l O. 8 OO O. 2 -------------------------------------------------------------, O 20 40 60 80 100 12O 140 Time (min.) Figure 7. Release of NLX and total buprenorphine from buprenorphine prodrug:naloxone patch (10% NLX-EC/HPC film, 7% BUPPD) in ethanol. --Naloxone triai 1. -- Naloxone trial 2 -iro Total buprenorphine trial 1 -- Total buprenorphine trial 2 0.07 - ---------------------------- - - - - O 2O 40 60 8O 100 2 140 Time (min.) Figure 8. Release of NLX and total buprenorphine from buprenorphine prodruginaloxone patch (10% NLX-EC/HPC film, 7% BUPPD) in water. U.S. Patent Jul. 9, 2013 Sheet 4 of 4 US 8.481,560 B2 accine NTX (EVA film) trial ram NTX (EVA film) trial 2 O.2 - “ gro. NTX (HPC film) trial 1 ne-NTX (HPC film) trial 2 Time (min.) Figure 9. Release kinetics in ethanol from a 5% NTX ethylcellulose film using an ethylene vinyl acetate (EVA) membrane (3MTM CotranTM 9728) or a prepared hydroxypropylcellulose membrane to separate the bi-layer system. US 8,481,560 B2 1. 2 ABUSE DETERRENT TRANSIDERMAL or intractable pain often also suffer from a lack of appetite, FORMULATIONS OF OPIATE AGONSTS nausea and/or frequent emesis. As such, oral and Sublingual AND AGONSTANTAGONSTS therapies for these patients are often either poorly tolerated or fail to provide an effective therapeutic dose. For these patients, transdermal administration can provide CROSS REFERENCES TO RELATED a favorable route of administration. Transdermal dosing pro APPLICATIONS vides the patient with a desirable systemic delivery profile which can minimize or eliminate any “highs' (dizziness and This application claims the benefit of U.S. Provisional drowsiness) associated with more rapid absorption and can Application Ser. No. 61/320,526, filed Apr. 2, 2010, which is reduce the side effects associated with oral administration of incorporated herein by reference in its entirety. 10 a drug, Such as abdominal pain, nausea and Vomiting. Addi tionally, transdermal administration avoids first-pass metabo FIELD lism which can allow for higher therapeutic concentrations to beachieved, and also offers a patient freedom from injections Described herein are opioid agonists, opioid agonist-an and Surgical implantations. Transdermal delivery can also tagonist or prodrugs of the foregoing in an abuse-resistant 15 improve patient compliance by reducing the dose frequency. formulation and dosage form for transdermal delivery of the A transdermal patch can offer Sustained release of a drug for opioid agonist, opioid agonist-antagonist or prodrugs of the an extended period (e.g., one week). foregoing. Because of the inherent potential for abuse, it is important that any pharmaceutical composition containing an opioid BACKGROUND agonist or opioid agonist-antagonist or prodrugs of either be made as abuse-resistant or abuse-deterrent as possible. This is Pain is the most frequently reported symptom and is a particularly true with extended release opioid products, common clinical problem confronting the clinician. Millions including transdermal applications. Illicit users often will of people in the United States suffer from severe pain that, attempt to circumvent the extended release properties of these according to numerous recent reports, is chronically under 25 dosage forms by injecting, chewing or otherwise misusing or treated or inappropriately managed. abusing the product in order to achieve an immediate release of the opioid agonist, opioid agonist-antagonist or prodrugs Opioids have long been recognized as one of the most of the foregoing. effective treatments of pain. However, they also have a high The Food and Drug Administration (“FDA) has recently potential of abuse. In fact, opioid and narcotic abuse are major emphasized the importance of reducing the risk of opioid worldwide problems connected with tremendous social and 30 abuse. In a Feb. 9, 2009 press release, the FDA publicly personal strife. As of 1992, the estimated United States eco announced a program in which it would meet with the manu nomic cost of drug and alcohol abuse was $246 billion. A facturers of extended release and transdermal opioids regard recent National Household Survey on Drug Abuse survey ing opioid misuse and abuse. Under the terms of the conducted by the Substance Abuse and Mental Health Ser announced program, the manufactures will be required to vices Administration reported in July 2007 that nearly one in 35 develop Risk Evaluation and Mitigations Strategies to ensure twelve full-time workers in the United States have serious proper opioid use. enough drug/alcohol problems to require medical treatment. Thus, it would be desirable to transdermally administer an Providing recovery assistance for drug addicts and alcoholics opioid agonist or agonist-antagonist, Such as buprenorphine, with pharmacological interventions has proven helpful. where the formulation or dosage form used to deliver the Certain opioids, such as buprenorphine (BUP), butorpha 40 opioid agonist or agonist-antagonist is resistant to possible nol, dezocine, meptazinol, nalbuphine and pentazocine, have abuse or other illicit diversion. both agonist and antagonist qualities. For example, the main agonist-antagonist effect of buprenorphine is through its SUMMARY binding to u-opioid and K-opioid receptors, acting clinically Some embodiments described herein, include an opioid as an agonist at lower doses and as an antagonist at higher 45 agonist, agonist-antagonist or prodrugs of the foregoing, in an doses. The dual agonist-antagonist activity of these opioids abuse resistant composition, formulation and dosage form make them effective at not only treating pain, but also at (e.g., a patch) for transdermal delivery of the opioid. reducing the severity of the withdrawal symptoms experi Other embodiments, objects, features and advantages will enced when a former abuser begins to eliminate opioid and/or be set forth in the detailed description of the embodiments alcohol.
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