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(12) Patent Application Publication (10) Pub. No.: US 2016/0317530 A1 Sandhu Et Al US 20160317530A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2016/0317530 A1 Sandhu et al. (43) Pub. Date: Nov. 3, 2016 (54) ABUSE-RESISTANT DRUG FORMULATIONS Publication Classification (71) Applicant: KASHIV PHARMA, LLC, (51) Int. Cl. Bridgewater, NJ (US) A63L/485 (2006.01) A63L/35 (2006.01) (72) Inventors: Harpreet Kaur Sandhu, West Orange, A6II 47/22 (2006.01) NJ (US); Siva Ram Kiran Vaka, A6II 47/8 (2006.01) Piscataway, NJ (US); Ashish Chatterji, A6II 47/10 (2006.01) East Brunswick, NJ (US); Dipen Desai, A6II 47/4 (2006.01) Whippany, NJ (US); Wantanee A6II 47/02 (2006.01) Phuapradit, Montville, NJ (US); A6II 47/44 (2006.01) Navnit H. Shah, Clifton, NJ (US) A6II 3/167 (2006.01) A6II 47/20 (2006.01) (52) U.S. Cl. (73) Assignee: Kashiv Pharma, LLC, Bridgewater, NJ CPC ........... A61K 31/485 (2013.01); A61K 3 1/167 (US) (2013.01); A61K 31/135 (2013.01); A61 K 47/22 (2013.01); A61K 47/20 (2013.01); A61 K (21) Appl. No.: 15/108,157 47/10 (2013.01); A61K 47/14 (2013.01); A61 K 47/02 (2013.01); A61K 47/44 (2013.01); A61 K (22) PCT Fed: Dec. 31, 2014 47/18 (2013.01) (86) PCT No.: PCT/US2O14/072968 (57) ABSTRACT Disclosed are abuse resistant oral pharmaceutical composi S 371 (c)(1), tions that reduce the likelihood of improper administration (2) Date: Jun. 24, 2016 of drugs that are susceptible to abuse. The oral pharmaceu tical formulations contain abuse deterrent agents that cause discomfort to the user when administered in an improper Related U.S. Application Data manner and make the extraction of an active ingredient more (60) Provisional application No. 61/922,158, filed on Dec. difficult. Methods of making and using the compositions are 31, 2013. also disclosed. Patent Application Publication Nov. 3, 2016 US 2016/0317530 A1 Release of drug from single unit capsule in Water 120 x.Dissolution of lipid Based Formulation in DeWater, 500ml 50 rpm &SSSSSSSSSNNNNNNx ys SS S SS coorooooooooooooooooooS S SS & 1.6A 6 O S $ x&s17A S Fig. 1 US 2016/0317530 A1 Nov. 3, 2016 ABUSE-RESISTANT DRUG FORMULATIONS crushing, breaking, and dissolution, and also to form a Viscous hydrogel in aqueous media that inhibits passage of CROSS-REFERENCE FOR PRIORITY an extract through a needle. APPLICATIONS 0011. In general, abusers of opioid drugs will not simply ingest more than a typical therapeutic dose, since the con 0001. The present application claims the benefit of the trolled-release formulations do not provide bursts of drug filing date of U.S. Provisional Application No. 61/922,158, bioavailability to create the desired euphoric sensations. filed Dec. 31, 2013, entitled ABUSE-RESISTANT DRUG Rather, abuse tends to involve some physical manipulation FORMULATIONS, the disclosure of which is hereby incor of a dosage form, so that larger amounts of immediately porated herein by reference. available drug can be taken orally, nasally, or by intravenous injection. For this reason, the OxyContin R tablets are BACKGROUND OF THE INVENTION formed from a partially molten mixture that contains a high 0002 Governmental reports state that prescription drug molecular weight polyethylene oxide excipient; the result is abuse is the fastest growing drug problem in the United a tablet that is not easily powdered and cannot readily be States, and a Survey indicated that nearly one-third of people treated to form a solution that is capable of being injected. age 12 and above who used drugs illicitly for the first time The very high hardness of this product, however, would not in 2009 began by the non-medical use of a prescription drug. permit reproducible splitting of a dosage form to administer The problem is considered to have been exacerbated by the a reduced dose or improve the administration for those introduction of controlled-release opioid products that con having difficulty in Swallowing. tain higher amounts of their active ingredients, beginning 0012 Despite the availability of a few products with with an oxycodone product that was approved for marketing abuse deterrent properties, the abuse of prescription medi in 1995. Reports of overdosing and death from prescription cine is still on rise and the serious abusers can bypass the pain products, especially the controlled-release oxycodone deterrent mechanism to extract the drug by more Sophisti product, began to rise sharply in the early 2000s. A need cated manipulation. Novel technologies are needed so that clearly exists to improve the safety of opioid drug products, these important classes of medicines can be made available by making the products less Susceptible for misuse. to the patients while lowering the risk of abuse and diversion 0003. In January 2013, the U.S. Food and Drug Admin for these products. In particular, new formulations are istration published a draft guidance document for the evalu needed which can be used with immediate release pharma ation and labeling of abuse-resistant opioid products. The ceutical products. guidance states that opioid analgesics can be abused by: 0013 New formulations, while having abuse-resistant Swallowing whole in excessive quantities; crushing and properties, must also allow for the active pharmaceutical Swallowing: crushing and inhaling nasally ('snorting); ingredient to be soluble in the gastrointestinal tract and have crushing and Smoking; or crushing, dissolving, and inject the desired pharmacological activity. In the case of opioids, ing. Categories of abuse-resistant formulations were the pharmacological activity would be an analgesic effect. described as: BRIEF SUMMARY OF THE INVENTION 0004. 1. Physical barriers to prevent chewing, crushing, cutting, grating or grinding, and chemical barriers to resist 0014. The present invention is directed to immediate extraction of the active ingredient with common solvents release oral dosage forms of pharmaceutically active agents Such as water, alcohol, and organic liquids. that are susceptible to abuse, and which due to abuse 0005 2. Agonist/antagonist combinations that interfere deterrent agents contained therein, decrease the potential for with, reduce, or defeat the euphoria associated with abuse. or inhibit abuse of the pharmaceutically active agent. 00.15 Aspects of the present invention provide formula 0006 3. Aversion agents, by incorporating a substance tions of drugs that resist attempts to administer the active that produces an unpleasant effect when the dosage form is ingredients by unintended routes and/or in unintended large altered before ingestion, or is ingested in a high dose. doses. The inventive formulations contain a plurality of 0007 4. Delivery systems that provide abuse resistance abuse deterrent agents that cause discomfort to the user through release characteristic design or a mode of adminis when administered in an improper manner, make the extrac tration. tion of the active ingredient from the formulation more 0008 5. Prodrugs that lack opioid activity until acted difficult, and therefore prevent or at least significantly reduce upon in the gastrointestinal system. the potential for abuse, while allowing the pharmaceutical 0009. 6. Combinations of two or more of the foregoing. formulation to release the active pharmaceutical ingredient 0010. The FDA describes the science of abuse deterrence in the gastrointestinal tract upon ingestion at the recom as relatively new and rapidly evolving. A few abuse-resistant mended dose to allow for the desired pharmacological effect. opioid products are currently approved for marketing. Some 0016 A first aspect of the present invention is directed to of these products are OxyContin R (oxycodone hydrochlo an abuse-resistant, immediate-release liquid pharmaceutical ride extended-release tablets), Targiniq(R) (oxycodone HCL+ composition, comprising a mixture of an effective amount at naloxone HCL), and Embeda R. (morphine sulfate and nal least one pharmaceutically active agent Susceptible to abuse, trexone hydrochloride). Other products such as Suboxone(R) an organic vehicle, a Surfactant, a co-solvent, and optionally and Opana ER(R) (oxymorphone) also purport to have abuse a viscosity-building polymer; wherein said organic vehicle, deterrent properties but do not have a formal claim on the Surfactant, and co-solvent co-elute with the pharmaceuti label. The mechanism for abuse deterrence range from cally active agent when exposed to a solvent, and wherein physical barriers to the use of antagonists or abuse deterrent the Viscosity-building polymer is present in an amount that agents. For example, the OxycontinR product sold by Pur slows the release of the pharmaceutically active agent if due Pharma is formulated to have a high hardness to resist multiple unit doses of the composition are administered. US 2016/0317530 A1 Nov. 3, 2016 0017. Another aspect of the present invention is directed not limited to, salts, Solvates, hydrates, complexes with one to a method of rendering abuse resistant an active pharma or more molecules, prodrugs, active metabolites, lipophilic ceutical agent that is susceptible to abuse, comprising pre derivatives, analogs, and the like. paring an immediate-release liquid pharmaceutical compo 0024. The term “immediate release” as used herein sition, by mixing an effective amount of at least one means that the bulk of the drug is released from the dosage pharmaceutically active agent Susceptible to abuse, an form in which it is administered in the stomach. By “bulk.” organic vehicle, a Surfactant, a co-solvent, and optionally, a it is meant that at least about 50% of the drug should be Viscosity-building polymer; wherein said organic vehicle, released in the stomach. In many cases, that release will be Surfactant, and co-solvent co-elute with the pharmaceuti as quickly as practicable, i.e., dissolution will be as close to cally active agent when exposed to a solvent, and wherein that resulting from administering an equal amount of fine the Viscosity-building polymer is present in an amount that loose powder.” slows the release of the pharmaceutically active agent if 0025.
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