Abstract: The present invention relates to an improved process for the preparation of Erythromycin Lactobionate (1) having purity more than 98.0%. It further relates to the preparation of crystalline hydrated forms of Erythromycin Lactobionate (1).
We Claim:
1. A process for the preparation of monohydrate form of Erythromycin
Lactobionate (1), comprising:
a) providing a solution of Erythromycin in a suitable solvent;
b) adding Lactobionic acid to the reaction mixture; and
c) isolating monohydrate form of Erythromycin Lactobionate (1).
2. The process according to claim 1, wherein the water content of Erythromycin Lactobionate (1) is less than 2.0% (w/w).
3. A process for the preparation of dihydrate form of Erythromycin Lactobionate (1), comprising:
a) providing a solution of Erythromycin in a suitable solvent;
b) adding Lactobionic acid to the reaction mixture; and
c) isolating dihydrate form of Erythromycin Lactobionate (1).
4. The process according to claim 3, wherein the water content of Erythromycin Lactobionate (1) is less than 3.0% (w/w).
5. The process according to claim 1 and claim 2, wherein, the suitable solvents is selected from a group comprising of methanol, ethanol, isopropyl alcohol (IPA), n-propanol, n-butanol, water, hexane, cyclohexane, toulene, xylene, tetrahydrofuran, acetone, acetonitrile, 1,4-dioxane, diethyl ether, dichloromethane, ethyl acetate, N, N-dimethylformamide, methyl tertiary butyl ether or mixtures thereof.
6. The process according to claim 1 and claim 2 , wherein the suitable technique used for isolating Erythromycin Lactobionate (1) is selected from a group comprising of, air tray dryer, vacuum tray dryer, fluidized bed dryer, agitated Nutsche filter dryers (ANFD), spin flash dryer or flash dryer.
7. The process according to claim 1 and claim 2, wherein the purity of
Erythromycin Lactobionate (1) is more than 95.0 % (w/w).
8. The process according claim 1 and claim 2 wherein, the, Erythromycin
Lactobionate (1) is having having purity greater than 95.0% by HPLC and
characterized by one or more of the following:
i. no greater than 2.0% (w/w) of impurity A;
ii. no greater than 2.0% (w/w). of impurity B;
iii. no greater than 3.0% (w/w) of impurity C;
iv. no greater than 1.0% (w/w). of impurity D;
v. no greater than 1.0% (w/w) of impurity E;
vi. no greater than 1.0% (w/w) of impurity F; vii. no greater than 0.5% (w/w) of impurity L; and viii. no greater than 2ppm of heavy metal content.
9. The process according to claim 1, wherein, the Erythromycin Lactobionate (1),
obtained in the present invention is characterized by X-ray powder diffraction
(XRPD) pattern as illustrated in figure 1.
| # | Name | Date |
|---|---|---|
| 1 | 201941031924-PROVISIONAL SPECIFICATION [07-08-2019(online)].pdf | 2019-08-07 |
| 2 | 201941031924-FORM 1 [07-08-2019(online)].pdf | 2019-08-07 |
| 3 | 201941031924-DRAWINGS [07-08-2019(online)].pdf | 2019-08-07 |
| 4 | Correspondence by Agent_Form 1_16-08-2019.pdf | 2019-08-16 |
| 5 | 201941031924-FORM 3 [07-08-2020(online)].pdf | 2020-08-07 |
| 6 | 201941031924-ENDORSEMENT BY INVENTORS [07-08-2020(online)].pdf | 2020-08-07 |
| 7 | 201941031924-DRAWING [07-08-2020(online)].pdf | 2020-08-07 |
| 8 | 201941031924-COMPLETE SPECIFICATION [07-08-2020(online)].pdf | 2020-08-07 |
| 9 | 201941031924-Correspondence-Form 2, Form 3, Form 5, Specification-03-09-2020.pdf | 2020-09-03 |