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AssigneeHetero Labs Limited
InventorsBandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Adullla VENKAT NARSIMHA REDDY, Bandi VAMSI KRISHNA
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The present invention relates to a process for preparing amorphous form of Sacubitril/Valsartan sodium salt of Formula-II and pharmaceutical composition comprising thereof.
A pharmaceutical formulation comprising a therapeutically effective amount of amorphous Sacubitril/Valsartan trisodium salt of Formula-II.
A pharmaceutical formulation comprising a therapeutically effective amount of Amorphous Sacubitril/Valsartan trisodium salt of Formula-II prepared by a process comprising the steps of:
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Not condensed with other rings: five-membered rings
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having five-membered rings with two or more ring hetero atoms, at least…
Drugs for disorders of the cardiovascular system: inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
Heterocyclic compounds
Term end not estimated
The present invention relates to a process for preparing amorphous form of LCZ696 and pharmaceutical composition comprising thereof.
LCZ696 is known as Sacubitril/Valsartan trisodium hemipetahydrate and chemically known as 3-[N-[1(S)-(biphenyl-4-ylmethyl)-4-ethoxy-3(R)-methyl-4-oxobutyl]carbamoyl]propionic acid and N-pentanoyl-N-[2′-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-L-valine trisodium hemipentahydrate and has the following structure, wherein designated as Formula-I.
Sacubitril is a neprilysin inhibitor pro-drug (AHU-377) and has now been tested in hypertension. LCZ696 has been approved in US under the trade name Entresto® as a tablet having dosage strengths 24MG, 26MG; 49MG, 51MG and 97MG, 103MG for treating chronic heart failure.
FIG. 1 is a powder X-ray diffractogram pattern of Amorphous form of Sacubitril/Valsartan trisodium.
FIG. 2 is a powder X-ray diffractogram pattern of Crystalline Sacubitril triethanolamine salt.
FIG. 3 is a powder X-ray diffractogram pattern of Crystalline Sacubitril triethanolamine salt.
The present invention relates to a process for the preparation of amorphous form of Sacubitril/Valsartan sodium salt of Formula-II, which comprises reacting Sacubitril of Formula-III with Valsartan of Formula-IV in a solvent, wherein the solvent is selected from the group comprising of halogenated solvents, alcohols, ketonic solvents, ethers, esters hydrocarbons or mixture thereof, followed by adding a sodium source, wherein sodium source is selected from the group comprising of sodium hydroxide, sodium alkoxides, sodium 2-ethylhexanoate; thereafter removing the solvent.
In another embodiment of the present invention, after removing the solvent to the obtained reaction mass added organic solvent, selected from the group comprising of alcohol, ester and hydrocarbon or mixtures thereof and thereafter solvent is removed to isolate stable amorphous form of Sacubitril/Valsartan sodium salt of Formula-II.
In another embodiment of the present invention, the removal of the solvent is carried out by evaporation, fractional distillation, azeotropic distillation, rotavapour distillation, vacuum distillation and the like.