Stable multiparticulate pharmaceutical composition of rosuvastatin

Patent metadata

Field	Value
Publication number	US-12527792-B2
Application number	US-202117157047-A
Country	US
Kind code	B2
Filing date	Jan 25, 2021
Priority date	Sep 1, 2015
Publication date	Jan 20, 2026
Grant date	Jan 20, 2026

Abstract

A stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers.

First claim

The invention claimed is:

1 . A method of treating hyperlipidemia, mixed dyslipidemia, hypertriglyceridemia or other hypercholesterolemia, comprising administering to a patient in need thereof a stable capsule composition by opening the capsule, emptying contents of the capsule onto soft food; and consuming the soft food, the capsule having pellets or granules, the pellets or granules consisting essentially of
i) rosuvastatin or its pharmaceutically accepted salts, (ii) one or more osmotic release modifier selected from the group consisting of mannitol sucrose, lactose, fructose, lactitol, sodium citrate, sodium phosphate, sodium bicarbonate, sodium chloride, potassium sulfate and mixtures thereof, and (iii) one or more stabilizer which is magnesium oxide, wherein the composition when tested for dissolution in an acetate buffer at a pH of 4.5, releases at least 80% of the rosuvastatin or its pharmaceutically acceptable salts within 10 minutes, wherein the average particle size of the pellets or granules is in a range of about 0.4 mm to about 0.8 mm, wherein the pellets or granules when sprinkled on soft food do not release rosuvastatin or its pharmaceutically acceptable salts, and wherein the stable capsule composition when stored at accelerated conditions of 40/75% relative humidity, a rosuvastatin lactone impurity is less than 0.5% by weight of the composition after at least three months.

2 . The method of claim 1 , wherein the patient is a geriatric patient or a patient with dysphagia with trouble swallowing a capsule.

3 . The method of claim 1 , wherein the capsule is opened using a capsule opening device that opens the capsule and empties the contents directly onto the soft food.

4 . The method of claim 1 , wherein the capsule is substantially devoid of fine particles.

5 . The method of claim 1 , wherein the pellets or granules are surrounded by a taste masking coating.

6 . The method of claim 1 , wherein the pellets or granules are free of a water insoluble barrier coating.

7 . The method of claim 1 , wherein the pellets or granules have an aspect ratio of 1 to 2.

8 . The method of claim 1 , wherein the size of pellets or granules enables the escape of pellets or granules from chewing or mastication upon administration with the food.

9 . The method of claim 1 , wherein the pellets or granules consist of rosuvastatin or its pharmaceutically accepted salts, one or more osmotic release modifier, magnesium oxide and optionally a disintegrant, a diluent and a lubricant.

10 . The method of claim 1 , wherein the osmotic release modifier is present in an amount ranging from about 1% to about 20% by weight of the stable capsule composition.

11 . The method of claim 1 , wherein the magnesium oxide is present in an amount ranging from about 1% to about 20% by weight of the stable capsule composition.

Assignees

• Sun Pharma Advanced Res Co Ltd

Inventors

• Dharmadikari Nitin Bhalachandra
• Zala Yashoraj R
• GADKARI Ashwini

Classifications

• A61K9/5047

  Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose · CPC title

• A61K9/5042

  Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose · CPC title

• A61K9/5031

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide) · CPC title

• A61K9/4866

  Organic macromolecular compounds · CPC title

• A61K9/4858

  Organic compounds · CPC title