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Abuse resistant drug formulationAbuse resistant drug formulation description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20080069891, Abuse resistant drug formulation. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001]This application claims the benefit of the filing date of U.S. Provisional Patent Application Nos. 60/845,128 filed Sep. 15, 2006, 60/845,127 filed Sep. 15, 2006, 60/845,126 filed Sep. 15, 2006, 60/845,151 filed Sep. 15, 2006, and 60/850,456 filed Oct. 10, 2006, the disclosures of which are hereby incorporated herein by reference. BACKGROUND OF THE INVENTION [0002]Some prescription drugs provide a controlled release of the active pharmaceutical ingredient ("API") that they are intended to deliver. Controlled release can be a delayed release such as an enteric release in the intestines. It can be an extended release where release begins immediately or shortly after ingestion and continues, either at a constant rate or in some pattern, over an extended period of time, usually from about 6 to about 24 hours. Often this is accomplished using a controlled release coating. Not only are controlled release dosage forms, and especially extended release dosage forms, convenient for the patients as they can take fewer doses throughout the day, but they also help prevent patients from being exposed to too much of the API thereby potentially suffering side effects. However, drug abusers may be at any one time or over a short period of time frustrated by such coatings for that same reason: they may prevent one from obtaining high initial blood concentrations which can cause the very effect--the "high," that the abuser is seeking to obtain. [0003]Indeed, opioids such as oxycodone, are sometimes available as extended release dosage forms for oral administration. One such product is OXCONTIN.RTM. from Purdue Pharma L.P. Once swallowed, these types of tablets slowly release their dose of active ingredient over an extended period, often over 6-24 hours. Such an extended release might be accomplished using a coating of some type over the individual particles of the opioid. [0004]However, people can abuse such tablets, using them as recreational drugs, by circumventing the extended release substructure or feature, in this example, the extended release coating. Indeed, a person can compromise this or some other extended release feature by crushing the dosage form through chewing or other means. This can crush any coating or other controlled release feature thereby allowing the release of a relatively large amount of the opioid sooner than intended into their systems once ingested. [0005]Ways of making a dosage form more crush resistant/abuse resistant include those disclosed in U.S. Patent App. Pub. No. 2006/0104909 and 2006/0193914. Coating pharmaceuticals with various materials to achieve other objectives, such as taste-masking, extended release, easier swallowing, etc. are also known. See, for example, U.S. Pat. Nos. 5,178,878; 5,607,697; 6,024,981; 6,280,770; 6,368,625; 6,692,771; 6,740,341; and 2003/0180362. [0006]Another way to circumvent controlled release coatings is to attempt to dissolve the dosage form in a solvent such as water or ethanol. The latter can be particularly dangerous as many prescription drugs should not be taken with alcohol. Depending upon the coating material used, the ethanol or water may act as a solvent, dissolving or eroding the coating and circumventing the intended controlled release. The resulting material can then be administered generally, orally, or in a syringe by a drug abuser. [0007]There are several techniques which have been developed to deter this type of solvent abuse. One abuse deterrent system for oral opioid compounds is described in U.S. Published Application No. 2006/0177380. This disclosure describes a composition containing a gel forming polymer forming an obstacle to syringe uptake, and nasal/mucosal irritant that causes discomfort when excessive amounts of the active compound are inhaled. Such abuse-deterring systems are designed for the nasal or parenteral abuse routes. See also U.S. Patent App. Pub. Nos. 2006/0193914, 2006/0188447, 2006/0193782, 2006/0204573, 2002/0110595, WO2007/087452A2, U.S. Pat. Nos. 6,607,751 and 7,090,867. SUMMARY OF THE INVENTION [0008]The present invention can be used in any number of contexts including improving manufacturing, storage, and use of dosage forms. However, one particular benefit that can inure from the use of the present invention is rendering an active pharmaceutical ingredient ("API")-containing particle, a coated particle or a dosage form less capable of being crushed, dissolved, injected or otherwise abused. [0009]Certain drugs, such as, for example, the opioid oxycodone, are administered to patients to reduce pain. Successful pain management in many of these patients requires maintenance of certain blood levels of the opioid throughout the day. One way of obtaining acceptable blood levels, used commonly in the pharmaceutical industry, is providing a dose which contains far more drug than is necessary to obtain the desired blood level. Blood levels shortly after the tablet is ingested reach a maximum or C.sub.max in a relatively short time, often within hours of ingestion (T.sub.max) and thereafter, as the body uses, processes and excretes drug from the blood system, the blood level drops. If the C.sub.max attained is sufficiently high, and the body's clearance of the drug is sufficiently slow, the blood levels may not fall to subtherapeutic levels for 4-12 hours or even longer. However, with drugs like oxycodone and indeed for many other drugs, this is an impractical and inefficient dosing system. In addition, there is a risk to the patient in that such high initial API levels can cause significant side effects. [0010]Another method of administering drugs involves the use of an extended release mechanism. An extended release can be achieved in many different ways and there are many different release profiles that can be attained. For exemplification only, a granulate material can be produced with a material that when exposed to the digestive tract, swells with available fluids and either slowly erodes or slows the wetting and diffusion of API drug materials contained within the granulate, thus providing a much lower C.sub.max and often a much longer T.sub.max. Ideally, a zero order release is obtained whereby a constant release rate and a constant blood level is attained throughout an extended period of time often six hours or more, more preferably twelve hours or more, and most preferably over about 24 hours. Not only could this strategy reduce the number of doses that need to be taken in a day, it also may prevent one from being exposed to the side effects which can come from unnecessarily high initial blood levels. [0011]Those who seek to abuse these types of products to "get high" can be frustrated by such extended and indeed other controlled release strategies. These strategies actively prevent one from obtaining high blood levels of the drug which can cause the euphoria or other physiologic effects which they are actually seeking, but which normal patients would consider an undesirable or even dangerous side effect. Such prescription drug abusers have learned to circumvent controlled release mechanisms by various administrative abuse means including simply chewing extended release tablets or crushing them using a mortar and a pestle for injection or the like. This can cause the rupture or otherwise compromise the API particle and/or controlled release coating, exposing more of the API to digestion and absorption more quickly, allowing the abuser to achieve much higher blood levels. [0012]Such abuse can have rather far ranging consequences. First, it facilitates drug abuse by individuals which can lead to significant health consequences and even death for the abuser. The consequences of such abuse reach far beyond the abuser and his or her immediate family. Indeed, they can be societal as well. Useful drugs necessary for cancer patients, patients with post-operative or pre-operative pain, chronic pains from arthritis or back injuries need to have available products to allow them to cope. However, the potential for abuse is a constant concern to regulators and law enforcement as these often prescription drugs may be more freely obtainable than truly illegal illicit substances. There are also the societal problems relating to drug use, which includes the cost of their health care, the cost of their rehabilitation, the increase in crime which may come from supporting their drug habit and the like. [0013]In a first embodiment, the present invention may be a coated granulate, comprising a granulate including at least one active pharmaceutical ingredient susceptible to abuse by an individual in an amount between about 0.1 to about 90 percent by weight of the granulate mixed with at least two materials, a first material that is substantially water insoluble and at least partially alcohol soluble and is present in an amount between about 1 to about 90 percent by weight of the granulate and a second material that is substantially alcohol insoluble and at least partially water soluble and is present in an amount between about 1 and about 90 percent by weight of the granulate, the active pharmaceutical ingredient and the two materials are granulated in the presence of water and alcohol; and a coating on the granulate provided in an amount of between about 20 and about 75 percent by weight of the coated granulate exhibiting crush resistance, wherein the coating may be any material such as, for example, cellulose polymers, methacrylate ester copolymers, methacrylic acid copolymers and shellac, said material deposited on said granulate using an alcohol based solvent. [0014]In another embodiment, the present invention may be a pharmaceutical composition comprising a granulate including at least one active pharmaceutical ingredient susceptible to abuse by an individual in an amount between about 0.1 to about 90 percent by weight of the granulate mixed with at least two materials, a first material that is substantially water insoluble and at least partially alcohol soluble and is present in an amount between about 1 to about 90 percent by weight of the granulate and a second material that is substantially alcohol insoluble and at least partially water soluble and is present in an amount between about 1 and about 90 percent by weight of the granulate, the active pharmaceutical ingredient and the two materials are granulated in the presence of water and alcohol; and a coating on the granulate provided in an amount of between about 20 and about 75 percent by weight of the coated granulate exhibiting crush resistance, wherein the coating may be any material such as, for example, cellulose polymers, methacrylate ester copolymers, methacrylic acid copolymers and shellac, said material deposited on said granulate using an alcohol based solvent; and a fat/wax present in an amount between about 1 to about 50 percent by weight of the pharmaceutical composition. [0015]In yet another embodiment, the present invention may be a pharmaceutical dosage form comprising a granulate which may include an opiate in an amount between about 0.1 to about 90 percent by weight of the granulate mixed with an at least two materials, a first material comprising ethylcellulose present in an amount between about 10 to about 40 percent by weight of the granulate and a second material comprising hydroxypropylmethylcellulose present in an amount between about 20 and about 50 percent by weight of the granulate, wherein the active pharmaceutical ingredient and the two materials are granulated in the presence of water and alcohol, said granulate present in an amount sufficient to provide an effective amount of said opiate; a coating on said granulate provided in an amount of between about 40 and about 60 percent by weight of the coated granulate exhibiting crush resistance, wherein the coating comprises a material selected from the group consisting of cellulose polymers, methacrylate ester copolymers, methacrylic acid copolymers and shellac, said material deposited on said granulate using an alcohol based solvent; a fat/wax present in an amount between about 5 to about 25 percent by weight of the final dosage form; and at least one excipient. [0016]In a further embodiment, the present invention may be a method of making a coated granulate which may include combining an at least one active pharmaceutical ingredient susceptible to abuse by an individual in an amount between about 0.1 to about 90 percent by weight of the granulate mixed with an at least two materials, a first material that is substantially water insoluble and at least partially alcohol soluble and is present in an amount between about 1 to about 90 percent by weight of the granulate and a second material that is substantially alcohol insoluble and at least partially water soluble and is present in an amount between about 1 and about 90 percent by weight of the granulate, wherein the active pharmaceutical ingredient and the two materials are granulated in the presence of water and alcohol, forming a wet granulate; milling and drying the wet granulate to form a granulate comprising an average particle size of about 50 to about 700 um; depositing a coating on said granulate provided in an amount of between about 20 and about 75 percent by weight of the coated granulate exhibiting crush resistance, wherein the coating comprises a material selected from the group consisting of cellulose polymers, methacrylate ester copolymers, methacrylic acid copolymers and shellac, said material deposited on said granulate using an alcohol based solvent; and allowing the coating to dry. [0017]In another embodiment, the present invention may be a method of treating a patient having pain which may include administering a pharmaceutical dosage form such a granulate which may include an opiate in an amount between about 0.1 to about 90 percent by weight of the granulate mixed with an at least two materials, a first material comprising ethylcellulose present in an amount between about 10 to about 40 percent by weight of the granulate and a second material comprising hydroxypropylmethylcellulose present in an amount between about 20 and about 50 percent by weight of the granulate, wherein the active pharmaceutical ingredient and the two materials are granulated in the presence of water and alcohol, said granulate present in an amount sufficient to provide an effective amount of said opiate; a coating on said granulate provided in an amount of between about 40 and about 60 percent by weight of the coated granulate exhibiting crush resistance, wherein the coating comprises a material selected from the group consisting of cellulose polymers, methacrylate ester copolymers, methacrylic acid copolymers and shellac, said material deposited on said granulate using an alcohol based solvent; a fat/wax present in an amount between about 5 to about 25 percent by weight of the final dosage form; and at least one excipient. [0018]In still a further embodiment, the present invention may be a pharmaceutical composition comprising at least one coated first particle comprising at least one API susceptible to administration abuse by an individual mixed with an at least two polymers: a first polymer that is substantially water insoluble and at least partially alcohol soluble and a second polymer that is substantially alcohol insoluble and at least partially water soluble. The coating exhibiting crush resistance may be ethylcellulose deposited from an alcohol containing solvent. The composition exhibits resistance to administration abuse by an individual. Moreover, the composition of this embodiment may further comprise a second particle which may be a fat/wax. [0019]In another embodiment, the present invention may be a pharmaceutical composition comprising at least one coated particle comprising an API susceptible to administration abuse by an individual mixed with at least one polymer dispersed or dissolved in an aqueous alcoholic solvent. The coating, which exhibits crush resistance, is deposited from an alcohol containing solvent. [0020]In a further embodiment, the present invention may be a pharmaceutical composition comprising two particles. The first particle comprises an API on a pharmaceutically effective amount wherein the first particle is coated with a polymer. The second particle comprises a fat/wax material present in an amount sufficient to inhibit administration abuse of the API from the first particle. [0021]In another embodiment, the present invention may be a method of making a pharmaceutically active coated particle. At least the API is combined with an aqueous alcoholic solvent to form a wet granulate. The wet granulate is milled and dried to form a granulate which may have a particle size of about 50 to about 700 um. The granulate may then be coated with one or more coating materials from an alcohol containing solvent. The coating may then be dried. Continue reading about Abuse resistant drug formulation... Full patent description for Abuse resistant drug formulation Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Abuse resistant drug formulation patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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