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Effervescent Compositions Of Metformin And Processes For Preparation Thereof

Abstract: The present invention relates to effervescent compositions of Metformin and optionally other anti-diabetic agents and processes for preparation thereof. More particularly provides an effervescent composition comprising Metformin an acid and a base such that the composition is free of affirmatively added binders and granulating solvents. The effervescent composition of the present invention has retained carbon dioxide content of at least 90% of the input blend.

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Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
25 June 2018
Publication Number
27/2018
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
email@obhans.com
Parent Application
Patent Number
Legal Status
Grant Date
2022-02-07
Renewal Date

Applicants

STEERLIFE INDIA PRIVATE LIMITED
290, 4th Main, 4th Phase Peenya Industrial Area Karnataka Bengaluru 560058

Inventors

1. BHUSHAN, Indu
c/o Steer Engineering Pvt. Ltd. No. 290, 4th Main, 4th Phase, Peenya Industrial Area, Karnataka Bengaluru 560058
2. KULKARNI, Vijay
c/o Steer Engineering Pvt. Ltd. No. 290, 4th Main, 4th Phase, Peenya Industrial Area, Karnataka Bengaluru 560058
3. SHETTY, Rakshith
c/o Steer Engineering Pvt. Ltd. No. 290, 4th Main, 4th Phase, Peenya Industrial Area, Karnataka Bengaluru 560058

Specification

CLAIMS
1. An effervescent composition comprising Metformin, an acid, a base and optionally, one or more anti-diabetic agents or one or more pharmaceutically acceptable excipients, wherein the composition has a retained carbon dioxide content of at least 90% of the input blend.
2. The effervescent composition according to claim 1, wherein the composition is free of affirmatively added binders and granulating solvents.
3. The effervescent composition according to claim 1, wherein the process for preparation of the composition involves the use of a twin screw processor.
4. The effervescent composition according to claim 1 wherein the acid is selected from
citric acid, tartaric acid, fumaric acid, malic acid, adipic acid, succinic acid, lactic acid,
glycolic acid, alpha hydroxy acid, ascorbic acid, amino acid or mixtures thereof.
5. The effervescent composition according to claim 1 wherein the base is selected from carbonate, sesquicarbonate or bicarbonate salts of potassium, lithium, sodium, calcium, or ammonium; L-lysine carbonate; arginine carbonate; sodium glycine carbonate; or sodium amino acid carbonate or mixtures thereof.
6. The effervescent composition according to claim 1 wherein the pharmaceutically acceptable excipient is selected from fillers, disintegrants, surfactants, taste modifiers, soluble or insoluble lubricants, flavoring substances, coloring agents, sweeteners or mixtures thereof.
7. The effervescent composition according to claim 1, wherein the acid and base are present in a weight ratio ranging from 3:1 to 1:5.
8. The effervescent composition according to claim 1 or 2, wherein the acid and base are anhydrous.

9. The effervescent composition according to claim 1 or 2, wherein the anti-diabetic agent
is selected from Rosiglitazone Maleate, Glyburide, Pioglitazone Hydrochloride,
Glipizide, Glimepiride, Repaglinide, Sitagliptin Phosphate, Canagliflozin, Linagliptin,
Alogliptin Benzoate, Empagliflozin, Saxagliptin Hydrochloride, Vildagliptin,
Teneligliptin, Pioglitazone Hydrochloride and Dapagliflozin Propanediol or their
derivatives or alternative salts thereof.
10. The effervescent composition according to claim 2, wherein the composition has a
disintegration time of less than 3 minutes.
i
11. The effervescent composition according to claim 2, wherein the composition has a disintegration time of less than 2 minutes.
12. A process for preparation of an effervescent Metformin composition comprising the steps of:

a) Processing an acid and a base through a twin screw processor; or
b) Processing an acid, a base and Metformin or atleast one pharmaceutically acceptable salt thereof, optionally with at least one other anti-diabetic agent through a twin screw processor;
i c) Mixing the product of step a) with Metformin or atleast one pharmaceutically acceptable salt thereof, and optionally at least one other anti-diabetic agent, and optionally at least one excipient followed, by compressing into tablets or filling into capsules or sachets; or
d) Compressing the product of step b) into tablets or filling it into capsules or sachets; after optionally mixing with at least one other anti-diabetic agent or at least one excipient; wherein only a portion of acid is melted in Step (a) or Step (b) to serve as an in-situ granulating agent and the said process being free of affirmatively added binders and granulating solvents.
i 13. The process according to claim 12, wherein the acid is selected from citric acid, tartaric acid, fumaric acid, malic acid, adipic acid, succinic acid, lactic acid, glycolic acid, alpha hydroxy acid, ascorbic acid, amino acid or mixtures thereof; and the base is selected

from carbonate, sesquicarbonate or bicarbonate salts of potassium, lithium, sodium, calcium, or ammonium; L-lysine carbonate; arginine carbonate; sodium glycine carbonate; or sodium amino acid carbonate or mixtures thereof; and wherein the effervescent Metformin composition has a retained carbon dioxide content of at least 90% of the input blend.
14. A method for treatment of Type-2 diabetes in a patient, comprising administering orally to the patient, the effervescent composition according to any one of the claims 1 toll.
15. The effervescent composition according to any one of the claims 1 to 11,for use in the treatment of Type-2 diabetes.

Documents

Application Documents

# Name Date
1 201847023657-STATEMENT OF UNDERTAKING (FORM 3) [25-06-2018(online)].pdf 2018-06-25
2 201847023657-PRIORITY DOCUMENTS [25-06-2018(online)].pdf 2018-06-25
3 201847023657-FORM 1 [25-06-2018(online)].pdf 2018-06-25
4 201847023657-DECLARATION OF INVENTORSHIP (FORM 5) [25-06-2018(online)].pdf 2018-06-25
5 201847023657-COMPLETE SPECIFICATION [25-06-2018(online)].pdf 2018-06-25
6 201847023657-FORM 3 [27-06-2018(online)].pdf 2018-06-27
7 201847023657-FORM-26 [17-07-2018(online)].pdf 2018-07-17
8 201847023657-Proof of Right (MANDATORY) [19-07-2018(online)].pdf 2018-07-19
9 Correspondence by Agent_Form 1, Power of Attorney_23-07-2018.pdf 2018-07-23
10 201847023657-FORM 3 [28-09-2018(online)].pdf 2018-09-28
11 201847023657-FORM 3 [08-05-2019(online)].pdf 2019-05-08
12 201847023657-FORM 18 [13-05-2019(online)].pdf 2019-05-13
13 201847023657-FORM 3 [08-11-2019(online)].pdf 2019-11-08
14 201847023657-FER.pdf 2020-02-25
15 201847023657-RELEVANT DOCUMENTS [17-03-2020(online)].pdf 2020-03-17
16 201847023657-FORM-26 [17-03-2020(online)].pdf 2020-03-17
17 201847023657-FORM 13 [17-03-2020(online)].pdf 2020-03-17
18 201847023657-OTHERS [24-08-2020(online)].pdf 2020-08-24
19 201847023657-FER_SER_REPLY [24-08-2020(online)].pdf 2020-08-24
20 201847023657-COMPLETE SPECIFICATION [24-08-2020(online)].pdf 2020-08-24
21 201847023657-CLAIMS [24-08-2020(online)].pdf 2020-08-24
22 201847023657-ABSTRACT [24-08-2020(online)].pdf 2020-08-24
23 201847023657-REQUEST FOR ADJOURNMENT OF HEARING UNDER RULE 129A [15-04-2021(online)].pdf 2021-04-15
24 201847023657-Correspondence to notify the Controller [14-05-2021(online)].pdf 2021-05-14
25 201847023657-PETITION UNDER RULE 138 [02-06-2021(online)].pdf 2021-06-02
26 201847023657-Written submissions and relevant documents [02-07-2021(online)].pdf 2021-07-02
27 201847023657-Information under section 8(2) [03-09-2021(online)].pdf 2021-09-03
28 201847023657-US(14)-HearingNotice-(HearingDate-20-04-2021).pdf 2021-10-17
29 201847023657-US(14)-ExtendedHearingNotice-(HearingDate-19-05-2021).pdf 2021-10-17
30 201847023657-PatentCertificate07-02-2022.pdf 2022-02-07
31 201847023657-IntimationOfGrant07-02-2022.pdf 2022-02-07
32 201847023657-RELEVANT DOCUMENTS [23-09-2023(online)].pdf 2023-09-23

Search Strategy

1 201847023657search_24-02-2020.pdf

ERegister / Renewals

3rd: 25 Mar 2022

From 12/12/2018 - To 12/12/2019

4th: 25 Mar 2022

From 12/12/2019 - To 12/12/2020

5th: 25 Mar 2022

From 12/12/2020 - To 12/12/2021

6th: 25 Mar 2022

From 12/12/2021 - To 12/12/2022

7th: 07 Dec 2022

From 12/12/2022 - To 12/12/2023

8th: 07 Dec 2023

From 12/12/2023 - To 12/12/2024

9th: 13 Nov 2024

From 12/12/2024 - To 12/12/2025