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Last Updated: November 25, 2020

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Claims for Patent: 9,439,906

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Summary for Patent: 9,439,906
Title:Dosing regimen associated with long acting injectable paliperidone esters
Abstract: The present invention provides a method of treating patients in need of treatment with long acting injectable paliperidone palmitate formulations.
Inventor(s): Vermeulen; An (Beerse, BE), Wouters; Alfons (Beerse, BE)
Assignee: Janssen Pharmaceutica NV (BE)
Application Number:12/337,144
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,439,906
Patent Claims: 1. A dosing regimen for administering paliperidone palmitate to a psychiatric patient in need of treatment for schizophrenia, schizoaffective disorder, or schizophreniform disorder comprising (1) administering intramuscularly in the deltoid of a patient in need of treatment a first loading dose of about 150 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the first day of treatment; (2) administering intramuscularly in the deltoid muscle of the patient in need of treatment a second loading dose of about 100 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the 6.sup.th to about 10th day of treatment; and (3) administering intramuscularly in the deltoid or gluteal muscle of the patient in need of treatment a first maintenance dose of about 25 mg-eq. to about 150 mg-eq. of paliperidone as paliperidone palmitate in a sustained release formulation a month (.+-.7 days) after the second loading dose.

2. The dosing regimen of claim 1 wherein after administration of the first maintenance dose, subsequent maintenance doses of from about 25 mg-eq. to 150 mg-eq. are administered in the deltoid or gluteal muscle of the psychiatric patient in need of treatment at monthly (.+-.7 days) intervals.

3. The dosing regimen of claim 1 wherein the sustained release formulation is an aqueous nanoparticle suspension.

4. A dosing regimen for administering paliperidone palmitate to a psychiatric patient in need of treatment for psychotic disorder comprising (a) administering intramuscularly in the deltoid of a patient in need of treatment a first loading dose of about 150 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the first day of treatment; (b) administering intramuscularly in the deltoid muscle of the patient in need of treatment a second loading dose of about 100 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the eighth day of treatment; and (c) administering intramuscularly in the deltoid or gluteal muscle of the patient in need of treatment a first maintenance dose of about 25 mg-eq. to about 150 mg-eq. of paliperidone as paliperidone palmitate in a sustained release formulation a month (.+-.7 days) after the second loading dose.

5. The dosing regimen of claim 4 wherein the sustained release formulation is an aqueous nanoparticle suspension.

6. The dosing regimen of claim 4 wherein the psychiatric patient is in need of treatment for psychotic disorder wherein the psychotic disorder is schizophrenia.

7. The dosing regimen of claim 4 wherein the psychiatric patient is in need of treatment for a psychotic disorder wherein the psychotic disorder is schizoaffective disorder.

8. A dosing regimen for administering paliperidone palmitate to a renally impaired psychiatric patient in need of treatment for schizophrenia, schizoaffective disorder, or schizophreniform disorder comprising (a) administering intramuscularly in the deltoid of a renally impaired psychiatric patient in need of treatment a first loading dose of from about 75 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the first day of treatment; (b) administering intramuscularly in the deltoid muscle of the patient in need of treatment a second loading dose of from about 75 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the 6.sup.th to about 10th day of treatment; and (c) administering intramuscularly in the deltoid or gluteal muscle of the patient in need of treatment a first maintenance dose of about 25 mg-eq. to about 75 mg-eq. of paliperidone as paliperidone palmitate in a sustained release formulation a month (.+-.7 days) after the second loading dose.

9. The dosing regimen of claim 8 wherein after the first maintenance dose, subsequent maintenance doses of from about 25 mg-eg. to 150 mg-eg. are administered in the deltoid or gluteal muscle of the psychiatric patient in need of treatment of monthly (.+-.7) intervals.

10. The dosing regimen of claim 8 wherein the sustained release formulation is an aqueous nanoparticle suspension.

11. A dosing regimen for administering paliperidone palmitate to a renally impaired psychiatric patient in need of treatment for psychotic disorder comprising (a) administering intramuscularly in the deltoid of a renally impaired psychiatric patient in need of treatment a first loading dose of from about 75 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the first day of treatment; (b) administering intramuscularly in the deltoid muscle of the patient in need of treatment a second loading dose of from about 75 mg-eq. of paliperidone as paliperidone palmitate formulated in a sustained release formulation on the eighth day of treatment; and (c) administering intramuscularly in the deltoid or gluteal muscle of the patient in need of treatment a first maintenance dose of about 25 mg-eq. to about 50 mg-eq. of paliperidone as paliperidone palmitate in a sustained release formulation a month (.+-.7 days) after the second loading dose.

12. The dosing regimen of claim 11 wherein the sustained release formulation is an aqueous nanoparticle suspension.

13. The dosing regimen of claim 11 wherein the psychiatric patient is in need of treatment for of a psychotic disorder wherein the psychotic disorder is schizophrenia.

14. The dosing regimen of claim 11 wherein the psychiatric patient is in need of treatment for a psychotic disorder wherein the psychotic disorder is schizoaffective disorder.

15. The dosing regimen of claim 4 wherein after administration of the first maintenance dose, subsequent maintenance doses of from about 25 mg-eq. to 150 mg-eq. are administered in the deltoid or gluteal muscle of the psychiatric patient in need of treatment at monthly (.+-.7 days) intervals.

16. The dosing regimen of claim 11 wherein after administration of the first maintenance dose, subsequent maintenance doses of from about 25 mg-eq. to 150 mg-eq. are administered in the deltoid or gluteal muscle of the psychiatric patient in need of treatment at monthly (.+-.7 days) intervals.

17. The dosing regimen of claim 1, 4, 8 or 11 wherein the formulation is an aqueous nanoparticle suspension comprises (a) from 3 to 20% (w/v) of the paliperidone palmitate having an average particle size (d50) of from about 1600 nm to about 900 nm; (b) from 0.5 to 3% (w/v) of a wetting agent wherein the wetting agent is polysorbate 20; (c) one or more buffering agents sufficient to render the composition neutral to very slightly basic (pH 8.5); (d) from 0.5 to 3% (w/v) of a suspending agent wherein the suspending agent is polyethylene glycol 4000; and (e) up to 2% (w/v) preservatives; and (f) water q.s. ad 100%.

18. The dosage regimen of claim 17 wherein the concentration of paliperidone palmitate is 156 mg/ml in the aqueous nanoparticle suspension.

19. The dosing regimen of claims 1, 4, 8 or 11 wherein the sustained release depot formulation is an aqueous nanoparticle suspension consists essentially of (a) 156 mg/ml of the paliperidone palmitate having an average particle size (d50) of from about 1600 nm to about 900 nm; (b) 12 mg/ml of polysorbate 20; (c) one or more buffering agents sufficient to render the composition neutral to very slightly basic (pH 8.5); (d) 30 mg/ml of a suspending agent wherein the suspending agent is polyethylene glycol 4000; and (f) water q.s. ad 100%.

20. The dosage regimen of claim 19 wherein in the buffering agents contained in the aqueous nanoparticle suspension are citric acid monohydrate, disodium hydrogen phosphate anhydrous, sodium dihydrogen phosphate monohydrate, sodium hydroxide.

21. The dosage regimen of claim 19 wherein in the pH of the aqueous nanoparticle suspension is in the range of pH 7 to 7.5.

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