Claims for Patent: 11,020,387

Summary for Patent: 11,020,387

Title:	Abuse-resistant pharmaceutical composition for the treatment of opioid dependence
Abstract:	There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain.
Inventor(s):	Fischer; Andreas (Uppsala, SE)
Assignee:	OREXO AB (Uppsala, SE)
Application Number:	17/032,934
Patent Claims:	1. A pharmaceutical composition in the form of a compressed tablet suitable for sublingual administration, which comprises: (i) buprenorphine or a pharmaceutically-acceptable salt thereof provided in the form of microparticles in a dosage amount (calculated as the free base) that is 11.4 mg (.+-.2%), 8.6 mg (.+-.2%), or 5.7 mg (.+-.2%); (ii) naloxone or a pharmaceutically-acceptable salt thereof provided in the form of particles in an amount (calculated as the free base) that is about 1/4 of the above doses of buprenorphine or salt thereof; (iii) particles comprising a weak acid; and (iv) a disintegrant, wherein the tablet weighs no more than about 250 mg and has a hardness that is in the range of about 10N to about 100N, as measured by the US Pharmacopoeia method <1217>. 2. The composition as claimed in claim 1, wherein the disintegrant is selected from the group croscarmellose sodium, sodium starch glycolate, crosslinked polyvinylpyrrolidone, and mixtures thereof. 3. The composition as claimed in claim 1, wherein the weak acid is citric acid. 4. The composition as claimed in claim 1, wherein the tablet further comprises a binder, carrier particles, particles comprising sodium citrate or any combination of these. 5. The composition as claimed in claim 4, wherein the weak acid is citric acid, and the particles comprising citric acid and the particles comprising sodium citrate are separate particles. 6. The composition as claimed in claim 1, wherein the tablet has a hardness that is in the range of about 15N to about 50N. 7. A method of treatment of a patient for opioid dependency and/or addiction, or for pain, which method comprises administering to said patient a pharmaceutical composition according to claim 1. 8. A pharmaceutical composition in the form of a compressed tablet suitable for sublingual administration, which comprises: (i) buprenorphine or a pharmaceutically-acceptable salt thereof provided in the form of microparticles in a dosage amount (calculated as the free base) that is 2.9 mg (.+-.2%); (ii) naloxone or a pharmaceutically-acceptable salt thereof provided in the form of particles in a dosage amount (calculated as the free base) that is about 1/4 of the above dose of buprenorphine or salt thereof; (iii) particles comprising a weak acid; and (iv) a disintegrant, wherein the tablet weighs no more than about 100 mg and has a hardness that is in the range of about 10N to about 100N, as measured by the US Pharmacopoeia method <1217>. 9. The composition as claimed in claim 8, wherein the disintegrant is selected from the group croscarmellose sodium, sodium starch glycolate, crosslinked polyvinylpyrrolidone, and mixtures thereof. 10. The composition as claimed in claim 8, wherein the weak acid is citric acid. 11. The composition as claimed in claim 8, wherein the tablet further comprises a binder, carrier particles, particles comprising sodium citrate or any combination of these. 12. The composition as claimed in claim 11, wherein the weak acid is citric acid, and the particles comprising citric acid and the particles comprising sodium citrate are separate particles. 13. The composition as claimed in claim 8, wherein the tablet has a hardness that is in the range of about 15N to about 50N. 14. A method of treatment of a patient for opioid dependency and/or addiction, or for pain, which method comprises administering to said patient a pharmaceutical composition according to claim 8.