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Understanding Brain Delivery
Published in Carla Vitorino, Andreia Jorge, Alberto Pais, Nanoparticles for Brain Drug Delivery, 2021
Joana Bicker, Ana Fortuna, Gilberto Alves, Amílcar Falcäo
Peripheral selectivity can be achieved by developing compounds with a low rate of passive permeability, acidic functional groups or affinity to efflux transporters at the blood-brain barrier (BBB) [3]. These molecules display unbound brain-to-plasma concentration ratios (Kpuu) below 1, such as second-generation histamine-Hl receptor antagonists (e.g. (S)-cetirizine: Kpuu = 0.22) which have better tolerability profiles than first-generation antagonists, due to a more restricted access to the CNS [4]. Designing dual efflux substrates is an efficient strategy to minimise CNS penetration [3] since the lower Kp,uu is, the higher will be the dose necessary to obtain active concentrations in the CNS, maintaining an unaltered potency [5]. Estimates of brain exposure should always consider potency, since efflux substrates can still be centrally active, provided there is sufficient potency [6].
Composition of Proprietary Products Approved in the United States
Published in Sarfaraz K. Niazi, Handbook of Pharmaceutical Manufacturing Formulations, Third Edition, 2019
ZYRTEC-D 12 HOUR™ (cetirizine hydrochloride [5 mg] and pseudoephedrine hydrochloride [120 mg]) extended-release tablets for oral administration contain 5 mg of cetirizine hydrochloride for immediate release and 120 mg of pseudoephedrine hydrochloride for extended release in a bilayer tablet. Tablets also contain as inactive ingredients colloidal silicon dioxide, croscarmellose sodium, hypromellose, lactose monohydrate, magnesium stearate, and microcrystalline cellulose.
Tribo-electrification of pharmaceutical powder blends
Published in Particulate Science and Technology, 2019
Antonella Rescaglio, Frederic De Smet, Luc Aerts, Geoffoy Lumay
Levocetirizine and Cetirizine are Cetirizine dihydrochloride (racemic mixture of (±)-[2-[4-[(4-chlorophenyl)phenylmethyl]-1- piperazinyl]ethoxy]acetic acid), sold under the brand name Zyrtec® among others, is a second generation antihistamine used in the treatment of hay fever, allergies, angioedema, and urticaria, Baltes, De Lannoy, and Rodriguez (1985).