Experimental data of co-crystals of Etravirine and L-tartaric acid

Abstract

Etravirine is a drug used alongside other medication in the treatment of HIV and is a non-nucleoside reverse transcriptase inhibitor. It is a BCS class IV drug, having low solubility and high permeability (Drugbank, https://www.drugbank.ca/drugs/DB06414) [1]. As a result, large doses of the drug are required for treatment. Two pills have to be taken twice a day, making it a “pill burden” (Intelence, http://www.intelence.com/hcp/dosing/administration-options) [2]. Therefore, attempts of co-crystallizing Etravirine are attractive as the solubility of the drug tends to increase in this solid form (Schultheiss and Newman, 2009) [3].In this study Etravirine co-crystals were synthesized in the molar ratios 1:1, 1:2 and 2:1 with L-tartaric acid as the co-former. Both slow evaporation and physical mixture was performed to mix the components. DSC values of final products are presented as well as FTIR spectra to observe the altered intermolecular interactions. A chemical stability test was performed after seven days using area under curve data from an HPLC instrument.

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Thymosin alpha 1: A comprehensive review of the literature

“…Thymalfasin is contraindicated in patients with hypersensitivity to thymosin alpha 1 or any of the components of the injection. Due to the immunomodulatory action of thymalfasin, it is also contraindicated in immu-nosuppressed patients, such as organ transplant recipients, unless the benefits of the treatment exceed the risks[ 35 ].…”

State of the Art of Pharmaceutical Solid Forms: from Crystal Property Issues to Nanocrystals Formulation

“…[7] However,i ns ome cases, the oral administration route can still be chosen for such BCS class IV APIs as etravirine, by modifying their physicochemical properties. [9,10] Indeed, al ist of mainly orally administered drugs according to the BCS has been compiled by Lindenberg et al [11] The solid state of ad rug can be adapted to optimize its pharmaceutical properties. Selecting the suitable physicalf orm of ad rugp rovides as trategic alternative for optimizing physicochemical properties such as chemical and physical stability, solubility,d issolution rate, and bioavailability.T hose strategies are mainly applied for drugs with low solubility such as BCS class II drugs.…”

“…administration is more convenient [7] . However, in some cases, the oral administration route can still be chosen for such BCS class IV APIs as etravirine, by modifying their physicochemical properties [9, 10] . Indeed, a list of mainly orally administered drugs according to the BCS has been compiled by Lindenberg et al [11] …”