Surety is performing system maintenance this weekend. Electronic date stamps on new Prior Art Database disclosures may be delayed.
Browse Prior Art Database


IP.com Disclosure Number: IPCOM000238032D
Publication Date: 2014-Jul-28
Document File: 7 page(s) / 140K

Publishing Venue

The IP.com Prior Art Database

This text was extracted from a Microsoft Word document.
This is the abbreviated version, containing approximately 12% of the total text.


It is generally known that the human immunodeficiency virus (HIV) is a retrovirus that infects cells of the immune system, destroying or impairing their function. As the infection progresses, the immune system becomes weaker, and the person becomes more susceptible to infections. The most advanced stage of HIV infection is acquired immunodeficiency syndrome (AIDS). Standard antiretroviral therapy consists of the combination of at least three anti-retroviral drugs to maximally suppress the HIV virus and stop the progression of HIV disease. According to WHO data huge reductions have been seen in rates of death and suffering when use is made of a potent anti-retroviral regimen, particularly in early stages of the disease. Since 2013, WHO also recommends the use of anti-retroviral drugs for the prevention of HIV infection, particularly for pregnant women, young children, and key populations exposed to HIV risk.

Therefore, there exists a great need to prepare a combination composition to treat HIV infection. Thus, the present disclosure describes a pharmaceutical composition comprising different anti-retroviral active substances and the manufacturing process thereof. More particularly, the present disclosure relates to a pharmaceutical composition comprising at least two anti-retroviral drugs that may be selected from the group consisting of NNRTI such as for example dapivirine, efavirenz, etravirine, delavirdine, nevirapine, rilpivirine and NRTI such as for example emtricitabine, tenofovir and any of its ester and salts thereof and any mixture thereof. More preferably the pharmaceutical composition comprises emtricitabine, tenofovir and any of its ester and salts thereof and optionally efavirenz.

Efavirenz is an HIV-1 specific, non-nucleoside, reverse transcriptase inhibitor (NNRTI) with chemical name (S)-6-chloro-4(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. Efavirenz is a white to slightly pink crystalline powder that is soluble in various organic solvents but practically insoluble in water. Efavirenz has one chiral centre and is used as a single enantiomer (S). Efavirenz in combination with other antiretroviral agents is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. On the US market efavirenz is present in Sustiva® (Bristol  Myers  Squibb) and Atripla® (Gilead).

Efavirenz used in the pharmaceutical composition as disclosed in the present disclosure can be prepared by any method known from the state of the art such as for example from WO9403440, WO9520389, US5519021, WO9827073, WO200066571, WO2009095931.

Any known polymorphic form of efavirenz  may be used such as for example polymorphic forms disclosed in WO9833782, WO9964405, WO2006018853, WO2006030299, WO2006040643, IN1251DEL2006, IN1908CHE2007, WO2008108630,  WO2009095931, WO2009011567, WO02010073254, IPCOM0001531, WO2010032259 or prepared by...