Publication

Design, Synthesis and in vitro Controlled Release of New Adamantanodiarylketone Antimycobacterials

Résumé

In the present investigation, the synthesis, the biology and the development of matrix tablet formulations for the in vitro controlled release of new adamantane diarylketone antimycobacterial derivatives, is presented. In the skeleton of the new compounds, a diarylketone, functionalized by a 2-hydroxypropylenoxy-3-butylamine, a 2-hydroxypropylenoxy-3-hexylamine and a 1-(2-hydroxyoctyl)piperidin-4-yl moiety, is incorporated at the C-1 adamantane position. The new derivatives were tested against the H37Rv Mycobacterium tuberculosis strain and exhibited satisfactory activity. In view of their lipophilic character, it was intriguing to examine their in vitro dissolution profile in buffer solutions simulating the gastric and intestinal environments. To this end, matrix tablets of the most active compound, {4-[(adamantan-1-yl)phenyl-4-(3-(butylamino)-2-hydroxypropoxy)]phenyl}methanone (A), incorporating the appropriate excipients, were prepared using the direct compression method. The preliminary test results show that its dissolution profile is in alignment with the desired pattern for the per os administration of tuberculocidal agents.

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Concepts associés (23)
Pharmaceutical formulation
Pharmaceutical formulation, in pharmaceutics, is the process in which different chemical substances, including the active drug, are combined to produce a final medicinal product. The word formulation is often used in a way that includes dosage form. Formulation studies involve developing a preparation of the drug which is both stable and acceptable to the patients. For orally administered drugs, this usually involves incorporating the drug into a tablet or a capsule.
Modified-release dosage
Modified-release dosage is a mechanism that (in contrast to immediate-release dosage) delivers a drug with a delay after its administration (delayed-release dosage) or for a prolonged period of time (extended-release [ER, XR, XL] dosage) or to a specific target in the body (targeted-release dosage). Sustained-release dosage forms are dosage forms designed to release (liberate) a drug at a predetermined rate in order to maintain a constant drug concentration for a specific period of time with minimum side effects.
Voie buccale
La voie buccale est la voie d'administration de médicaments par laquelle le principe actif est administré dans la bouche. L’action des médicaments pris par voie buccale peut être locale ou générale (systémique). Dans ce second cas, la voie d'administration est entérale : le principe actif diffuse à travers la muqueuse buccale (tissus qui tapissent la bouche) et entre directement dans la circulation sanguine.
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