Abstract: The present invention relates to a novel crystalline fonn of Gefitinib and a process for its Preparation thereof. Gefitinib is 4-(31-chloro-41-fluoro anilino)- 7-methoxy-6- (3-morpholino propoxy) quinazoline and has the structural formula-I The present invention is to provide a stable novel crystalline fonn of Gefitinib designated by us as Fonm-6, and a process for the preparation of the same. Gefitinib is useful in the treatment of a variety of solid tumors, especially non-small cell lung cancer and hematological malignancies.
1. A novel stable crystalline Gefitinib Form-6 having the characteristics given below:
XRPD: having typical characteristic peaks at about 7.05, 9.36, 12.3, 14.8, 16.8, 18.60,20.68, 24.72 on the 29 scale as shown in Fig 1 of the drawing accompanying this specification
DSC: having a typical first endotherm with a peak at approximately 66.4 to 82.4°C and a second endotherm with a peak at approximately 193.3 to 195.3°C as shown in Fig 2
K.F. value of 3.70%-3.95% w/w, preferably 3.75-3.85% w/w equivalent to monohydrate.
2. A process for the preparation of a novel crystalline form of Gefitinib, designated as Form-6 as
claimed in claim 1, which comprises mixing anhydrous Gefitinib of the formula-I,
I with water, stirring the resulting slurry at a temperature in the range of 25-30 °C for a period
ranging from 18 to about 20 hrs, filtering and air-drying the resultant Form-6 of Gefitinib
formed.
3. The process as claimed in claim 2 where in the stirring of anhydrous Gefitinib and the water
is effected for a period in the range of 15-25 hours, preferably between 18^20 hours.
1. A pharmaceutical composition comprising the novel stable crystalline Form-6 of Gefitinib as claimed in claim 1 and a pharmaceutically acceptable carrier.
>. A process for the preparation of a novel crystalline form of Gefitinib, designated as Form-6 laving the above mentioned characteristics, as claimed in claim 1 of Gefitinib of the formula-I ubstantially as herein described with reference to Example 1.
| # | Name | Date |
|---|---|---|
| 1 | 150-che-2005 correspondence others-25-06-2009.pdf | 2009-06-25 |
| 1 | 150-CHE-2005-Form 27_Statement of Working_05-10-2021.pdf | 2021-10-05 |
| 2 | 150-che-2005 description (complete)-13-07-2009.pdf | 2009-07-13 |
| 2 | 150-CHE-2005-RELEVANT DOCUMENTS [30-09-2021(online)].pdf | 2021-09-30 |
| 3 | 150-CHE-2005-Form27_Statement of working_18-03-2020.pdf | 2020-03-18 |
| 3 | 150-che-2005 correspondence others-13-07-2009.pdf | 2009-07-13 |
| 4 | 150-CHE-2005-RELEVANT DOCUMENTS [16-03-2020(online)].pdf | 2020-03-16 |
| 4 | 150-che-2005 claims-13-07-2009.pdf | 2009-07-13 |
| 5 | Form 27_Licence_01-04-2019.pdf | 2019-04-01 |
| 5 | 150-che-2005 abstract-13-07-2009.pdf | 2009-07-13 |
| 6 | 150-CHE-2005-RELEVANT DOCUMENTS [29-03-2019(online)].pdf | 2019-03-29 |
| 6 | 150-CHE-2005 EXAMINATION REPORT REPLY RECEIVED 22-12-2009.pdf | 2009-12-22 |
| 7 | Correspondence by Applicant_Form27_26-03-2018.pdf | 2018-03-26 |
| 7 | 150-CHE-2005 AMANDED CLAIMS 22-12-2009.pdf | 2009-12-22 |
| 8 | 150-CHE-2005-RELEVANT DOCUMENTS [20-03-2018(online)].pdf | 2018-03-20 |
| 8 | 150-CHE-2005 AMANDED PAGES OF SPECIFICATION 22-12-2009.pdf | 2009-12-22 |
| 9 | 150-CHE-2005 CORRESPONDENCE OTHERS 18-03-2010.pdf | 2010-03-18 |
| 9 | Correspondence By Agent_Form27_27-03-2017.pdf | 2017-03-27 |
| 10 | 150-che-2005 pct search report.pdf | 2011-09-02 |
| 10 | 150.jpg | 2011-09-02 |
| 11 | 150-che-2005 pct.pdf | 2011-09-02 |
| 12 | 150-che-2005 pct search report.pdf | 2011-09-02 |
| 12 | 150.jpg | 2011-09-02 |
| 13 | 150-CHE-2005 CORRESPONDENCE OTHERS 18-03-2010.pdf | 2010-03-18 |
| 13 | Correspondence By Agent_Form27_27-03-2017.pdf | 2017-03-27 |
| 14 | 150-CHE-2005 AMANDED PAGES OF SPECIFICATION 22-12-2009.pdf | 2009-12-22 |
| 14 | 150-CHE-2005-RELEVANT DOCUMENTS [20-03-2018(online)].pdf | 2018-03-20 |
| 15 | 150-CHE-2005 AMANDED CLAIMS 22-12-2009.pdf | 2009-12-22 |
| 15 | Correspondence by Applicant_Form27_26-03-2018.pdf | 2018-03-26 |
| 16 | 150-CHE-2005 EXAMINATION REPORT REPLY RECEIVED 22-12-2009.pdf | 2009-12-22 |
| 16 | 150-CHE-2005-RELEVANT DOCUMENTS [29-03-2019(online)].pdf | 2019-03-29 |
| 17 | 150-che-2005 abstract-13-07-2009.pdf | 2009-07-13 |
| 17 | Form 27_Licence_01-04-2019.pdf | 2019-04-01 |
| 18 | 150-che-2005 claims-13-07-2009.pdf | 2009-07-13 |
| 18 | 150-CHE-2005-RELEVANT DOCUMENTS [16-03-2020(online)].pdf | 2020-03-16 |
| 19 | 150-CHE-2005-Form27_Statement of working_18-03-2020.pdf | 2020-03-18 |
| 19 | 150-che-2005 correspondence others-13-07-2009.pdf | 2009-07-13 |
| 20 | 150-CHE-2005-RELEVANT DOCUMENTS [30-09-2021(online)].pdf | 2021-09-30 |
| 20 | 150-che-2005 description (complete)-13-07-2009.pdf | 2009-07-13 |
| 21 | 150-CHE-2005-Form 27_Statement of Working_05-10-2021.pdf | 2021-10-05 |
| 21 | 150-che-2005 correspondence others-25-06-2009.pdf | 2009-06-25 |