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Publication Date: 2007-Feb-16
Document File: 4 page(s) / 35K

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The present disclosure provides a method of drying nelfinavir mesylate.

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Tarun Kant Sharma, Raghvendra Prasad, Anshul Agrawal

Ranbaxy Laboratories Limited, Plot 20, Sector 18, Udyog Vihar, Gurgaon -122001, Haryana, India


The present disclosure provides a method of drying nelfinavir mesylate.


Nelfinavir is chemically [3S-[2(2S*,3S*),3,4a,8a]]-N-(1,1-dimethylethyl)decahydro-2-[2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinoline carboxamide. It is commercially available in the form of its mono-methanesulfonate of Formula I.

       FORMULA I

Nelfinavir mesylate, in combination with other antiretroviral agents, is indicated for the treatment of HIV infection. Nelfinavir is a member of the group of drugs referred to as protease inhibitors (PIs). This class of drug combats viral replication of HIV by blocking HIV protease. This enzyme is used by HIV to break up large viral proteins into smaller particles from which new HIV particles can be formed. Protease inhibitors ensure that these new particles are immature and incapable of infecting new cells, thus inhibiting the HIV replication process.

Nelfinavir mesylate is marketed as a white to off-white amorphous powder. US Patent No 5,484,926 discloses a process for the preparation of amorphous nelfinavir mesylate, wherein the process involves cooling a suspension of nelfinavir mesylate in a freezer, followed by filtration at cold temperature and drying in a vacuum oven.

U.S. Patent No 6,303,786 provides a process for drying nelfinavir mesylate by spray drying, wherein the process involves pumping an alcoholic solution of nelfinavir mesylate into a Nitro Atomizer Portable Spray Dryer, which utilizes vane, co-current flow or countercurrent flow atomizer, and collecting the spray dried product.  The ‘786 patent discloses another method of drying nelfinavir mesylate, wherein the method involves drying a solid nelfinavir mesylate in rotocone drier under vacuum at 60o-65oC for 12-72 h. The drying process is accelerated in this method by milling the drier contents in a Fitzmill grinder.

The present inventors have developed a novel method for drying nelfinavir mesylate by using agitated thin film dryer (ATFD).  The present process provides dry free flowing nelfinavir mesylate in a single pass as a one-step process. The present process also eliminates thermal degradation of the product due to low residence time and indirect contact drying. The ATFD process also consumes comparatively low energy and thus improves process economics. The present process also provides nelfinavir mesylate in amorphous form.

The term “feeding” of the present disclosure includes loading, dozing, introducing, charging, filling, supplying, passing, pouring or heaping. The term “collecting” of the present...