scholarly journals Controlled Release Imatinib Mesylate Tablet Formulation: Using Hydrophilic Matrix System

2015 ◽  
Vol 21 (3) ◽  
pp. 157-166 ◽  
Author(s):  
Ehsan Mohajeri ◽  
Mehdi Ansari ◽  
Abbas Pardakhty
2013 ◽  
Vol 241 ◽  
pp. 252-262 ◽  
Author(s):  
Loreana Gallo ◽  
Juliana Piña ◽  
Verónica Bucalá ◽  
Daniel Allemandi ◽  
María Verónica Ramírez-Rigo

2018 ◽  
Vol 19 (5) ◽  
pp. 2144-2154 ◽  
Author(s):  
Jinheng Huang ◽  
Huaqing Lin ◽  
Bingxin Peng ◽  
Qianfeng Huang ◽  
Fangzhou Shuai ◽  
...  

2018 ◽  
Vol 287 ◽  
pp. 247-256 ◽  
Author(s):  
Matteo Cerea ◽  
Alessandra Maroni ◽  
Luca Palugan ◽  
Marco Bellini ◽  
Anastasia Foppoli ◽  
...  

2019 ◽  
Vol 16 (3) ◽  
pp. 347-352 ◽  
Author(s):  
M. Vlachou ◽  
G. Stavrou ◽  
A. Siamidi ◽  
S. Flitouri ◽  
V. Ioannidou ◽  
...  

Background: N-Acetylserotonin (NAS, N-acetyl-5-hydroxytryptamine) is the immediate precursor of the neurohormone melatonin (MT, N-acetyl-5-methoxytryptamine), which regulates sleep and wake cycles. NAS is produced by the N-acetylation of serotonin and is converted to melatonin via the action of Acetylserotonin O-methyltransferase (ASMT). Like melatonin, NAS acts as an agonist on the melatonin receptors MT1, MT2, and MT3. However, as NAS is abundant in specific brain areas, separate from serotonin and melatonin, it may also have discrete central effects. Indicatively, it has been reported that NAS may play a role in the antidepressant effects of Selective Serotonin Reuptake Inhibitors (SSRIs) and Monoamine Oxidase Inhibitors (MAOIs). </P><P> Objective: To decipher the controlled release characteristics of the active substances (NAS and MT) in a quick initial pace, aiming at a satisfactory sleep-onset related anti-depressive profile and prolonged release, thereafter, targeting at coping with poor sleep quality problems. </P><P> Methods: A series of hydrophilic matrix tablets involving as excipients, hydroxypropylmethylcellulose (HPMC) K15M, low viscosity sodium alginate, lactose monohydrate, and polyvinylpyrrolidone (PVP) M.W.: 10.000 and 55.000) was developed and tested at two dissolution media (pH 1.2 and 7.4). </P><P> Results: The results showed that commonly used excipients with different physicochemical properties govern the controlled release of NAS and MT from solid matrix systems. </P><P> Conclusions: We have demonstrated how broadly used excipients affect the in vitro controlled release of NAS and MT from solid pharmaceutical formulations. Currently, we extend our studies on the controlled release of these drugs using various other biopolymers/formulants of different physicochemical characteristics, which will help to highlight the discrete release profiles of NAS and MT.


2011 ◽  
Vol 65 (1-2) ◽  
pp. 71-81
Author(s):  
Irena Homsek ◽  
Dragica Popadic ◽  
Slobodanka Simic ◽  
Slavica Ristic ◽  
Katarina Vucicevic ◽  
...  

Controlled-release (CR) pharmaceutical formulations offer several advantages over the conventional, immediate release dosage forms of the same drug, including reduced dosing frequency, decreased incidence and/or intensity of adverse effects, greater selectivity of pharmacological activity, reduced drug plasma fluctuation, and better compliance. After a drug product has been registered, and is already on market, minor changes in formulation might be needed. At the same time, the product has to remain effective and safe for patients that could be confirmed via plasma drug concentrations and pharmacokinetic characteristics. It is challenging to predict human absorption and pharmacokinetic characteristics of a drug based on the in vitro dissolution test and the animal pharmacokinetic data. Therefore, the objective of this study was to establish correlation of the pharmacokinetic parameters of carbamazepine (CBZ) CR tablet formulation between the rabbit and the human model, and to establish in vitro in vivo correlation (IVIVC) based on the predicted fractions of absorbed CBZ. Although differences in mean plasma concentration profiles were notified, the data concerning the predicted fraction of drug absorbed were almost superimposable. Accordingly, it can be concluded that rabbits may be representative as an in vivo model for predicting the pharmacokinetics of the CR formulation of CBZ in humans.


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