Sign In to Follow Application
View All Documents & Correspondence

Processes For Preparation Of Amorphous Form And Amorphous Solid Dispersion Of Mirabegron

Abstract: Aspects of the present invention relate to amorphous form of mirabegron amorphous solid dispersion of mirabegron process for its preparation processes for preparation of a form crystal and ß form crystal of mirabegron and pharmaceutical composition thereof.

Get Free WhatsApp Updates!
Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
05 December 2013
Publication Number
27/2015
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application
Patent Number
Legal Status
Grant Date
2019-09-28
Renewal Date

Applicants

DR. REDDYS LABORATORIES LIMITED
8 2 337 Road No. 3 Banjara Hills Andhara Pradesh Hyderabad 500 034

Inventors

1. PEDDY Vishweshwar
Plot No.341 Vasavi Colony Green Hills Road No.1 Saroornagar Post Andhra Pradesh Hyderabad 500 035
2. BOGE Rajesham
H.No. 1 56/1/B Road No.1 Jawahar Colony Chandanagar Andhra Pradesh Hyderabad 500 050

Specification

1. An amorphous mirabegron.
2. A process for preparing amorphous mirabegron of claim 1, comprising:

a) providing a solution of mirabegron in a solvent or mixture of solvents;
b) removing solvent from the solution obtained in step a), and
c) isolating an amorphous form of mirabegron

3. An amorphous solid dispersion of mirabegron together with one or more pharmaceutically acceptable carriers.
4. The amorphous solid dispersion of mirabegron of claim 3, wherein the pharmaceutically acceptable carrier is at least one selected from gelatines, ovalbumin, soybean proteins, gum arabic, non-sucrose fatty acid esters, starches, modified starches, cellulose, methylcellulose (MC), ethylcellulose (EC), hydroxy ethylcellulose (HEC), hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC), polycarbophil, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene derivatives, polymethacrylates, polyvinyl pyrrolidone (PVP, povidone), polyvinyl acetate (PVAc), PVP-vinylacetate-copolymer (PVP-VA), Kollidon VA 64 (a vinylpyrrolidone- vinyl acetate copolymer), lactose, sorbitol, mannitol, maltitol, saccharose, Isomalt, cyclodextrins such as a-cyclodextrins, P-cyclodextrins, y-cyclodextrins and hydroxyl-propyl-P-cyclodextrins, sodiumcarboxymethylcellulose, sodium alginate, xantham gum, caavageenan, locust bean gum (ceratonia), chitosan, guar gum, cross-linkedhighamylase starch, and cross-linked polyacrylic acid (carbopol).
5. An amorphous solid dispersion of mirabegron of claim 3, wherein the pharmaceutically acceptable carrier is povidone.
6. The amorphous solid dispersion of mirabegron of claim 3 to 5, wherein the ratio of at least one pharmaceutically carrier to the mirabegron is at least about 1:2 (w/w) to about (2:1) (w/w).
7. A process for preparing the amorphous solid dispersion of mirabegron of any of claims 3 to 6, comprising:

a) providing a solution of mirabegron in combination with one or more pharmaceutically acceptable carriers in a solvent or mixture of solvents;
b) removing the solvent from the solution or suspension obtained in step a) or combining the solution obtained in step a) with an anti-solvent, and
c) isolating solid dispersion of amorphous mirabegron together with one or more pharmaceutically acceptable carrier.

8. A solid pharmaceutical formulation comprising the amorphous mirabegron or solid dispersion of amorphous mirabegron of any of claims 1 to 7 and one or more pharmaceutically acceptable carrier.
9. Use of amorphous mirabegron or amorphous solid dispersion of mirabegron according to any of claims 1 to 7 together with at least one pharmaceutically acceptable carrier, for the tre atment of a disease associated with overactive bladder.
10. A process for the preparation of a-form crystal of mirabegron comprising:

a) dissolving mirabegron in a solvent selected from methanol, ethanol, tetrahydrofuran, ethyl acetate, toluene or mixtures thereof to provide a solution;
b) cooling the solution obtained in step a), and
c) isolating a-form crystal of mirabegron.
11. A process for the preparation of a-form crystal of mirabegron comprising:
a) dissolving mirabegron in a mixture of methanol and water to provide a solution;
b) cooling the solution obtained in step a), and
c) isolating a-form crystal of mirabegron.
12. A process for the preparation of a-form crystal of mirabegron comprising:
a) providing a solution of mirabegron in a solvent selected from
tetrahydrofuran, methanol, ethanol, acetone, acetonitrile,l,4-dioxane, methyl isobutyl ketone, chlorobenzene or mixtures thereof;

b) adding an anti-solvent to the solution of step a), selected from cyclohexane, methylcyclohexane, n-heptane, diisopropyl ether, methyl tertiary butyl ether, toluene, water, provided that when methanol is used as a solvent then anti-solvent is other than water; and
c) isolating a-form crystal of mirabegron.
13. A process for the preparation of a-form crystal of mirabegron comprising:
a) dissolving mirabegron in acetone to provide a solution;
b) adding the solution obtained from step a) to methylcyclohexane, and
c) isolating a-form crystal of mirabegron.

14. A solid pharmaceutical formulation comprising a-form crystal of mirabegron obtained according to any of claims 10 to 13 and one or more pharmaceutically acceptable carrier.
15. Use of a-form crystal of mirabegron obtained according to any of claims 10 to 13 together with at least one pharmaceutically acceptable carrier for the treatment of a disease associated with overactive bladder.

1. A process for preparing amorphous mirabegron comprising:
c) providing a solution of mirabegron in a solvent or mixture of solvents;
d) removing solvent from the solution obtained in step a), and
e) isolating an amorphous form of mirabegron.
2. A process for preparing amorphous solid dispersion of mirabegron comprising:
d) providing a solution of mirabegron in combination with pharmaceutically acceptable carriers in a solvent or mixture of solvents;
e) removing the solvent from the solution or suspension obtained in step a) or combining the solution obtained in step a) with an anti-solvent, and
f) isolating solid dispersion of amorphous mirabegron together with one or more pharmaceutically acceptable carrier.
3. A process as claimed in claim 2, wherein the pharmaceutically acceptable carriers
in step a) is selected from gelatines, ovalbumin, soybean proteins, gum arabic,
non-sucrose fatty acid esters, starches, modified starches, cellulose,
methylcellulose (MC), ethylcellulose (EC), hydroxy ethylcellulose (HEC),
hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC),
polycarbophil, polyethylene glycol (PEG), polyethylene oxides, polyoxyalkylene
derivatives, polymethacrylates, polyvinyl pyrrolidone (PVP, povidone), polyvinyl
acetate (PVAc), PVP-vinylacetate-copolymer (PVP-VA), Kollidon VA 64 (a
vinylpyrrolidone- vinyl acetate copolymer), lactose, sorbitol, mannitol, maltitol,
saccharose, Isomalt, cyclodextrins like a-cyclodextrins, p-cyclodextrins, y-
cyclodextrins and hydroxyl-propyl-(3-cyclodextrins,
sodiumcarboxymethylcellulose, sodium alginate, xantham gum, caavageenan,
locust bean gum (ceratonia), chitosan, guar gum, cross-linkedhighamylase starch,
and cross-linked polyacrylic acid (carbopol).

4. A process as claimed in claim 2, wherein the pharmaceutical^ acceptable carrier is povidone.
5. A process as claimed in claim 2, wherein the ratio of pharmaceutically carrier to the mirabegron is in the range of 1:2 (w/w) to (2:1) (w/w).

Documents

Orders

Section Controller Decision Date

Application Documents

# Name Date
1 9704-CHENP-2013-RELEVANT DOCUMENTS [30-03-2022(online)].pdf 2022-03-30
1 IN NP draft filed online.pdf 2013-12-05
2 9704-CHENP-2013-RELEVANT DOCUMENTS [03-03-2021(online)].pdf 2021-03-03
2 FORM-5.pdf 2013-12-05
3 FORM 3.pdf 2013-12-05
3 9704-CHENP-2013-RELEVANT DOCUMENTS [05-03-2020(online)].pdf 2020-03-05
4 9704-CHENP-2013.pdf 2014-03-21
4 9704-CHENP-2013-IntimationOfGrant28-09-2019.pdf 2019-09-28
5 9704-CHENP-2013-PatentCertificate28-09-2019.pdf 2019-09-28
5 9704-CHENP-2013-FER.pdf 2018-03-21
6 Abstract_Granted 321858_28-09-2019.pdf 2019-09-28
6 9704-chenp-2013-OTHERS [20-09-2018(online)].pdf 2018-09-20
7 Claims_Granted 321858_28-09-2019.pdf 2019-09-28
7 9704-chenp-2013-FER_SER_REPLY [20-09-2018(online)].pdf 2018-09-20
8 Description_Granted 321858_28-09-2019.pdf 2019-09-28
8 9704-chenp-2013-CORRESPONDENCE [20-09-2018(online)].pdf 2018-09-20
9 9704-chenp-2013-COMPLETE SPECIFICATION [20-09-2018(online)].pdf 2018-09-20
9 Drawings_Granted 321858_28-09-2019.pdf 2019-09-28
10 9704-chenp-2013-CLAIMS [20-09-2018(online)].pdf 2018-09-20
10 Marked up Claims_Granted 321858_28-09-2019.pdf 2019-09-28
11 9704-chenp-2013-ABSTRACT [20-09-2018(online)].pdf 2018-09-20
11 Correspondence by Agent_Proof of Right-Form1_25-09-2019.pdf 2019-09-25
12 Form 1_Proof of Right_25-09-2019.pdf 2019-09-25
12 Form2 Title Page_Complete_31-12-2018.pdf 2018-12-31
13 9704-CHENP-2013-Annexure [13-09-2019(online)].pdf 2019-09-13
13 Form 5_FER Reply_31-12-2018.pdf 2018-12-31
14 9704-CHENP-2013-PETITION UNDER RULE 137 [13-09-2019(online)]-1.pdf 2019-09-13
14 Form 3_FER Reply_31-12-2018.pdf 2018-12-31
15 9704-CHENP-2013-PETITION UNDER RULE 137 [13-09-2019(online)].pdf 2019-09-13
15 Form 1_FER Reply_31-12-2018.pdf 2018-12-31
16 9704-CHENP-2013-RELEVANT DOCUMENTS [13-09-2019(online)]-1.pdf 2019-09-13
16 Drawings_FER Reply_31-12-2018.pdf 2018-12-31
17 Correspondence by Applicant_Form 18_31-12-2018.pdf 2018-12-31
17 9704-CHENP-2013-RELEVANT DOCUMENTS [13-09-2019(online)].pdf 2019-09-13
18 9704-CHENP-2013-Written submissions and relevant documents (MANDATORY) [13-09-2019(online)].pdf 2019-09-13
18 Claims_FER Reply_31-12-2018.pdf 2018-12-31
19 9704-CHENP-2013-HearingNoticeLetter04-09-2019.pdf 2019-09-04
19 Amended Pages of Specification_FER Reply_31-12-2018.pdf 2018-12-31
20 9704-CHENP-2013-HearingNoticeLetter04-09-2019.pdf 2019-09-04
20 Amended Pages of Specification_FER Reply_31-12-2018.pdf 2018-12-31
21 9704-CHENP-2013-Written submissions and relevant documents (MANDATORY) [13-09-2019(online)].pdf 2019-09-13
21 Claims_FER Reply_31-12-2018.pdf 2018-12-31
22 9704-CHENP-2013-RELEVANT DOCUMENTS [13-09-2019(online)].pdf 2019-09-13
22 Correspondence by Applicant_Form 18_31-12-2018.pdf 2018-12-31
23 9704-CHENP-2013-RELEVANT DOCUMENTS [13-09-2019(online)]-1.pdf 2019-09-13
23 Drawings_FER Reply_31-12-2018.pdf 2018-12-31
24 Form 1_FER Reply_31-12-2018.pdf 2018-12-31
24 9704-CHENP-2013-PETITION UNDER RULE 137 [13-09-2019(online)].pdf 2019-09-13
25 9704-CHENP-2013-PETITION UNDER RULE 137 [13-09-2019(online)]-1.pdf 2019-09-13
25 Form 3_FER Reply_31-12-2018.pdf 2018-12-31
26 9704-CHENP-2013-Annexure [13-09-2019(online)].pdf 2019-09-13
26 Form 5_FER Reply_31-12-2018.pdf 2018-12-31
27 Form 1_Proof of Right_25-09-2019.pdf 2019-09-25
27 Form2 Title Page_Complete_31-12-2018.pdf 2018-12-31
28 9704-chenp-2013-ABSTRACT [20-09-2018(online)].pdf 2018-09-20
28 Correspondence by Agent_Proof of Right-Form1_25-09-2019.pdf 2019-09-25
29 9704-chenp-2013-CLAIMS [20-09-2018(online)].pdf 2018-09-20
29 Marked up Claims_Granted 321858_28-09-2019.pdf 2019-09-28
30 9704-chenp-2013-COMPLETE SPECIFICATION [20-09-2018(online)].pdf 2018-09-20
30 Drawings_Granted 321858_28-09-2019.pdf 2019-09-28
31 Description_Granted 321858_28-09-2019.pdf 2019-09-28
31 9704-chenp-2013-CORRESPONDENCE [20-09-2018(online)].pdf 2018-09-20
32 Claims_Granted 321858_28-09-2019.pdf 2019-09-28
32 9704-chenp-2013-FER_SER_REPLY [20-09-2018(online)].pdf 2018-09-20
33 Abstract_Granted 321858_28-09-2019.pdf 2019-09-28
33 9704-chenp-2013-OTHERS [20-09-2018(online)].pdf 2018-09-20
34 9704-CHENP-2013-PatentCertificate28-09-2019.pdf 2019-09-28
34 9704-CHENP-2013-FER.pdf 2018-03-21
35 9704-CHENP-2013.pdf 2014-03-21
35 9704-CHENP-2013-IntimationOfGrant28-09-2019.pdf 2019-09-28
36 FORM 3.pdf 2013-12-05
36 9704-CHENP-2013-RELEVANT DOCUMENTS [05-03-2020(online)].pdf 2020-03-05
37 9704-CHENP-2013-RELEVANT DOCUMENTS [03-03-2021(online)].pdf 2021-03-03
37 FORM-5.pdf 2013-12-05
38 9704-CHENP-2013-RELEVANT DOCUMENTS [30-03-2022(online)].pdf 2022-03-30
38 IN NP draft filed online.pdf 2013-12-05

Search Strategy

1 searchstrategy_07-02-2018.pdf

ERegister / Renewals

3rd: 27 Nov 2019

From 17/05/2014 - To 17/05/2015

4th: 27 Nov 2019

From 17/05/2015 - To 17/05/2016

5th: 27 Nov 2019

From 17/05/2016 - To 17/05/2017

6th: 27 Nov 2019

From 17/05/2017 - To 17/05/2018

7th: 27 Nov 2019

From 17/05/2018 - To 17/05/2019

8th: 27 Nov 2019

From 17/05/2019 - To 17/05/2020

9th: 04 Jun 2020

From 17/05/2020 - To 17/05/2021

10th: 26 Jul 2021

From 17/05/2021 - To 17/05/2022