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(12) Patent Application Publication (10) Pub. No.: US 2005/0163856A1 Maloney Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2005/0163856A1 Maloney Et Al US 2005O163856A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0163856A1 Maloney et al. (43) Pub. Date: Jul. 28, 2005 (54) ABUSE-RESISTANTSUSTAINED-RELEASE Related U.S. Application Data OPOD FORMULATION (63) Continuation of application No. 10/264,020, filed on Oct. 3, 2002, which is a continuation-in-part of appli (75) Inventors: Ann Maloney, Dublin, OH (US); cation No. 10/085,597, filed on Feb. 27, 2002, now Debra Marie Murwin, Orient, OH abandoned, and which is a continuation of application (US); Michael Jay Schobelock, Grove No. 09/626,584, filed on Jul. 27, 2000, now aban City, OH (US) doned. (60) Provisional application No. 60/146,298, filed on Jul. Correspondence Address: 29, 1999. MICHAEL P. MORRIS Publication Classification BOEHRINGER INGELHEM CORPORATION 900 RIDGEBURY ROAD (51) Int. CI.7. ... A61K 31/485; A61K 9/14 PO BOX 368 (52) U.S. Cl. ............................................ 424/486; 514/282 RIDGEFIELD, CT 06877-0368 (US) (57) ABSTRACT (73) Assignee: Roxane Laboratories, Inc., Columbus, A method for reducing the abuse potential of an oral dosage OH form of an opioid extractable by commonly available house hold Solvents Said method comprising combining a thera (21) Appl. No.: 11/087,154 peutically effective amount of the opioid compound, or a Salt thereof, a matrix-forming polymer and an ionic exchange (22) Filed: Mar. 23, 2005 resin. US 2005/0163856 A1 Jul. 28, 2005 ABUSE-RESISTANTSUSTAINED-RELEASE after repeated administration of the drug, a given dose of the OPOD FORMULATION drug produces a decreased effect, or conversely, when increasingly larger doses of the drug must be administered RELATED APPLICATIONS to obtain effects observed with the original dose. “Physical dependence” references an altered physiological State pro 0001. This application is a continuation-in-part applica duced by the repeated administration of the drug that neces tion of patent application Ser. No. 10/085,597 filed Feb. 27, sitates the continued administration of the drug to prevent 2002, which was a continuation of patent application Ser. the appearance of a Stereotypical Syndrome, the withdrawal No. 09/626,584, filed Jul. 27, 2000, which claims, as the or abstinence Syndrome. A perSon may also develop “psy present application, priority to Provisional Patent Applica chological dependence' which is characterized by a drug tion Ser. No. 60/146,298, filed Jul. 29, 1999, the disclosures Seeking behavior directed towards achieving euphoria and of all of which are incorporated herein in their entirety. escape from daily life. BACKGROUND OF THE INVENTION 0008 Tolerance does not develop uniformly to all of the actions of opioid drugs. Typically, however, tolerance will 0002) 1. Field of Invention develop to the euphorigenic and other CNS depressant 0003. The present invention relates to a controlled-re effects. Tolerance to a number of opioid drugs can develop lease opioid delivery composition that is resistant to extrac with remarkable rapidity. However, the rate at which toler tion of the opioid with commonly-available solvents. More ance develops depends on the pattern of use. It is known that particularly, the present invention is directed to a controlled it is possible to obtain desired analgesic and Sedative effects release opioid formulation, capable of providing Sustained, of most opioids from doses in the therapeutic range for prolonged, repeat and/or delayed release, which provides nearly an indefinite period of time. However, when there is resistance to extraction of the opioid using commonly more or less continuous drug action, tolerance may develop. available Solvents. Such formulations are useful for decreas Thus in the addict who primarily seeks to get a “rush” or ing the potential for abuse. The formulation employs an ion maintain a State of dreamy indifference (a "high”), the dose eXchange resin in conjunction with a hydrophilic matrix and of the opioid to reach Such a State must be constantly the opioid. increased. In general, there appears to be a high degree of cross-tolerance between drugs with morphine-like actions, 0004 2. Background of the Related Art although cross-tolerance may not be seen when the opioids 0005 Opioids comprise a diverse group of drugs, natural act through different opioid receptors. Tolerance to opioids and Synthetic, that have, in varying degrees, opium- or largely disappears when a user undergoes “withdrawal' morphine-like properties and bind to one of Several Subspe from the drug. cies of opioid receptors. These drugs produce their major 0009. The time required to produce physical dependence effects on the central nervous system and bowel. Effects of on any opioid depends on a number of factors, including the opioids are remarkably diverse, including analgesia, dosage Schedule, route of administration, and the physi drowsiness, changes in mood and alterations of the endo ological profile of the opioid. The degree to which function crine and autonomic nervous Systems. Opioid analgesics in the CNS is altered by the drug, and the continuity of this comprise the major class of drugs used in the management alteration, appear to be very important in the development of of moderate to Severe pain. nervous Systems. Opioid anal physical dependence. gesics comprise the major class of drugs used in the man 0010. The development of clinically observable physical agement of moderate to Severe pain. dependence gives rise to the possibility of reinforcement of 0006. One of the effects of opioid administration is the drug abusive behavior based on administration of the drug ability of Such drugs in Some individuals to alter mood and operating to alleviate “withdrawal distress.” However, feeling in a manner So as to provide a desirable Sense of whether withdrawal symptoms are clinically observable “well-being dissociated from therapeutic ameliorative depends on Several factors including the criteria used for effects. This mood-altering effect is found by some indi withdrawal Symptoms, the Sensitivity of the technique used viduals to be extremely pleasurable, So much So, that Some to detect withdrawal, and the rate at which the drug is users after repeated administration develop a craving for removed from its site of action. Withdrawal symptoms from re-administration of the opioid. The intensity of this craving opioid agonist administration may be aggravated when may range from a mild desire to use the drug, to a preoc opioid antagonists are administered. For example, long cupation with its procurement and use, not for its therapeutic acting opioids, Such as methadone, produces withdrawal ameliorative effects, but rather for its mood-altering effects. Symptoms that are slow in onset and generally leSS Severe In the latter case, the opioid becomes the central fixation in than Short-acting opioids. However, when an antagonist is a State commonly referred to as "drug abuse,” a term used given to a perSon displaying dependence on a long-acting to describe the usage of any drug in a manner which deviates opioid, a Severe withdrawal Syndrome ensues. from approved medical or Social patterns within a given 0011. It is known that a protracted opioid abstinence culture. When the drug abuse involves overwhelming Syndrome may develop Subsequent to withdrawal of certain involvement with the use of the drug, Securing its Supply, opioids and the condition can last for weekS. Such Syndrome and a high tendency to relapse into drug use after its is characterized by physiological and psychological abnor withdrawal, an “addiction” is said to have developed. Often malities that give the perSon a Subjective Sense of “not being an addict will administer opioids in the face of Self-harm. quite right.” Such Syndrome may be alleviated by adminis 0007. A consequence of the repeated use of many opioids tration of an opioid, predisposing one to relapse by creating is the development of “tolerance' and, in Some cases “physi a period of increased Vulnerability during which the effects cal dependence.”Tolerance” refers to a phenomenon when of opioids are especially reinforcing. US 2005/0163856 A1 Jul. 28, 2005 0012 Common symptoms of opioid withdrawal include Visit numerous doctors, Sometimes in Several States, to abdominal cramps, anorexia, chills alternating with exces acquire large amounts of controlled Substances they abuse or Sive Sweating, goose flesh, hyperexcitability, hyperirritabil sell to others. ity, increased heart rate, lachrymation, nausea, pupillary 0018 Scheduling of opioid drugs has also had the unin dilation, muscle Spasms, and rhinorrhea. Withdrawal Symp tentional Side-effect of causing physicians, fearful of being toms may manifest gradually or precipitously, and typically accused of permitting drug abuse, to prescribe Sub-optimal begin to occur 24-48 hours after the last dose of the opioid. doses of opioids to patients in need of them, and to prescribe less effective drugs to patients that are not Similarly Sched 0013 The abuse potential of any particular opioid relates uled. This is particularly true with respect to the treatment of to a number of factors including the capacity of the drug to cancer patients who are frequently given Sub-optimal pain induce euphoria, patterns of Side-effects when the drug is control because of fears with respect to the “addictive used at Supra-therapeutic doses, the distreSS caused by nature' and "legal controls' Surrounding approved opioid withdrawal of the drug after dependence has developed, the drugs. There is a growing recognition in the medical
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