You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: May 15, 2024

Claims for Patent: 10,098,882


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 10,098,882
Title:Risperidone sustained release microsphere composition
Abstract:A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.
Inventor(s):Sun Kaoxiang, Liang Rongcai, Wang Qilin, Wang Wenyan, Liu Wanhui, Li Youxin
Assignee:
Application Number:US15347365
Patent Claims: 1. Microspheres for sustained release of an active agent comprising:an active component selected from the group consisting of risperidone, 9-hydroxy risperidone, a salt of risperidone, and a salt of 9-hydroxy risperidone; anda polymer blend consisting essentially of a first uncapped poly(lactide-co-glycolide) and a second uncapped poly(lactide-co-glycolide),wherein the first uncapped poly(lactide-co-glycolide) has an intrinsic viscosity of 0.4-0.9 dl/g and a molar ratio of lactide to glycolide of 65:35 to 90:10; andwherein the second uncapped poly(lactide-co-glycolide) has an intrinsic viscosity of 0.1-0.35 dl/g and a molar ratio of lactide to glycolide of 50:50 to 75:25.2. The microspheres of claim 1 ,wherein the molar ratio of lactide to glycolide in the first uncapped poly(lactide-co-glycolide) is 75:25; andwherein the molar ratio of lactide to glycolide in the second uncapped poly(lactide-co-glycolide) is 50:50.3. The microspheres of claim 1 ,wherein a weight ratio of the first uncapped poly(lactide-co-glycolide) to the second uncapped poly(lactide-co-glycolide) is in a range from 50:50 to 95:5.4. The microspheres of claim 1 ,wherein the first uncapped poly(lactide-co-glycolide) has a molecular weight from 50,000 to 145,000; andwherein the second uncapped poly(lactide-co-glycolide) has a molecular weight from 4,000 to 45,000.5. The microspheres of claim 1 ,wherein the active agent is in an amount of from 10% to 60% based on a total weight of the microspheres.6. Microspheres for sustained release of an active agent comprising:an active agent selected from the group consisting of risperidone, 9-hydroxy risperidone, a salt of risperidone, and a salt of 9-hydroxy risperidone; anda polymer blend consisting essentially of a first uncapped poly(lactide-co-glycolide) and a second uncapped poly(lactide-co-glycolide);wherein the first uncapped poly(lactide-co-glycolide) has a molecular weight from 50,000 to 145,000 and a molar ratio of lactide to glycolide in a range from 65:35 to 90:10;wherein the second uncapped poly(lactide-co-glycolide) has a molecular weight from 4,000 to 45,000 and a molar ratio of lactide to glycolide in a range from 50:50 to 75:25.7. The microspheres of claim 6 ,wherein the first uncapped poly(lactide-co-glycolide) has a molecular weight from 55,000 to 110,000; andwherein the second uncapped poly(lactide-co-glycolide) has a molecular weight from 15,000 to 35,000.8. The microspheres of claim 6 ,wherein the molar ratio of lactide to glycolide in the first uncapped poly(lactide-co-glycolide) is 75:25; andwherein the molar ratio of lactide to glycolide in the second uncapped poly(lactide-co-glycolide) is 50:50.9. The microspheres of claim 6 ,wherein a weight ratio of the first uncapped poly(lactide-co-glycolide) to the second uncapped poly(lactide-co-glycolide) is in a range from 50:50 to 95:5.10. The microspheres of claim 6 ,wherein the first uncapped poly(lactide-co-glycolide) has an intrinsic viscosity of 0.4-0.9 dl/g; andwherein the second uncapped poly(lactide-co-glycolide) has an intrinsic viscosity of 0.1-0.35 dl/g.11. The microspheres of claim 6 ,wherein the active agent is in an amount of from 10% to 60% based on a total weight of the microspheres.12. Microspheres for sustained release of an active agent comprising:an active agent selected from the group consisting of risperidone, 9-hydroxy risperidone, a salt of risperidone, and a salt of 9-hydroxy risperidone; anda polymer blend comprising a first uncapped poly(lactide-co-glycolide) and a second uncapped poly(lactide-co-glycolide);wherein the first uncapped poly(lactide-co-glycolide) has a molecular weight from 55,000 to 110,000, an intrinsic viscosity of 0.4-0.9 dl/g, and a molar ratio of lactide to glycolide in a range from 65:35 to 90:10;wherein the second uncapped poly(lactide-co-glycolide) has a molecular weight from 15,000 to 35,000, an intrinsic viscosity of 0.1-0.35 dl/g, and a molar ratio of lactide to glycolide in a range from 50:50 to 75:25; andwherein a weight ratio of the first uncapped poly(lactide-co-glycolide) to the second uncapped poly(lactide-co-glycolide) is in a range from 50:50 to 95:5, such that lactide is a major monomer component compared to glycolide of the polymer blend.13. The microspheres of claim 12 ,wherein the active agent is in an amount of from 10% to 60% based on a total weight of the microspheres.14. The microspheres of claim 13 ,wherein no crystals of the active agent are precipitated on the surfaces of the microspheres.15. A pharmaceutical formulation for injection into a patient in need claim 1 , comprising: the microspheres of .16. A method of treating a psychosis comprising: administering parenterally a therapeutically effective amount of the pharmaceutical formulation of to a patient in need.17. The method of claim 16 , wherein the administrating method is intramuscular injection claim 16 , subcutaneous injection claim 16 , intradermal injection claim 16 , or intraperitoneal injection.18. The method of claim 16 , wherein each administration dose provides 12.5 to 150 mg of risperidone.19. The method of claim 16 , wherein the therapeutically effective amount is 0.2 to 2.5 mg risperidone per kg of body weight.20. The method of claim 16 , wherein the therapeutically effective amount is 0.4 to 1.7 mg risperidone per kg of body weight.22. The method of wherein the plurality of microspheres comprise 10% - 60% of the active component based on the total weight of the microspheres.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.