Claims for Patent: 11,433,066

Summary for Patent: 11,433,066

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:	17/032,882
Patent Claims:	1. A method of treatment of opioid dependence in a subject, which method comprises: providing a sublingual tablet comprising (i) a dosage amount of buprenorphine or a pharmaceutically-acceptable salt thereof (calculated as the free base) that is 11.4 mg (.+-.2%), 8.6 mg (.+-.2%), 5.7 mg (.+-.2%), 2.9 mg (.+-.2%), or 1.4 mg (.+-.2%); (ii) a dosage amount of naloxone or a pharmaceutically-acceptable salt thereof (calculated as the free base) that is about 1/4 of the above doses of buprenorphine or salt thereof; and (iii) citric acid; and (iv) a disintegrant, which tablet is prepared according to a process comprising: (a) associatively admixing microparticles of buprenorphine or pharmaceutically-acceptable salt thereof with particles of citric acid by a process of simple mixing and/or granulation, to form an associative admixture between the microparticles of buprenorphine or salt thereof and the particles of citric acid; (b) mixing the associative admixture obtained in step (a) with particles comprising naloxone or pharmaceutically-acceptable salt thereof; and (c) compressing the mixture obtained in step (b) to produce said tablet; and sublingually administering the tablet to a subject in need of treatment of opioid dependence. 2. The method 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 method as claimed in claim 1, wherein the tablet further comprises sodium citrate. 4. The method as claimed in claim 1, wherein the tablet further comprises a binder, carrier particles, or both. 5. The method as claimed in claim 4, wherein the binder is a cellulose gum or microcrystalline cellulose. 6. The method as claimed in claim 1, wherein the associative admixture formed in step (a) is carried out by simple mixing. 7. The method as claimed in claim 1, wherein the associative admixture formed in step (a) is carried out by granulation. 8. The method as claimed in claim 7, wherein the granulation comprises dry granulation, wet granulation, melt granulation, thermoplastic pelletising, spray granulation or extrusion/spheronisation. 9. The method as claimed in claim 4, wherein the binder, carrier particles, or both, are associatively admixed in step (a) by granulation. 10. The method as claimed in claim 3, wherein the sodium citrate is in the form of particles, which are associatively admixed in step (a). 11. The method as claimed in claim 4, wherein the carrier particles are present in the tablet, and the carrier particles are associatively admixed in step (a).