Influence of pH Modifiers and HPMC Viscosity Grades on Nicotine-Magnesium Aluminum Silicate Complex-Loaded Buccal Matrix Tablets.
Summary of "Influence of pH Modifiers and HPMC Viscosity Grades on Nicotine-Magnesium Aluminum Silicate Complex-Loaded Buccal Matrix Tablets."
Hydroxypropyl methylcellulose (HPMC) tablets containing nicotine-magnesium aluminum silicate (NCT-MAS) complex particles and pH modifiers, namely, sodium chloride, citric acid, and magnesium hydroxide, were prepared using the direct compression method. The effects of HPMC viscosity grades and pH modifiers on NCT release and permeation of the matrix tablets were examined. The results showed that the higher the viscosity grade of HPMC that was used in the tablets, the lower was the unidirectional NCT release rate found. The unidirectional NCT permeation was not affected by the viscosity grade of HPMC because the NCT diffusion through the mucosal membrane was the rate-limiting step of the permeation. Incorporation of magnesium hydroxide could retard NCT release, whereas the enhancement of unidirectional NCT release was found in the tablets containing citric acid. Citric acid could inhibit NCT permeation due to the formation of protonated NCT in the swollen tablets at an acidic pH. Conversely, the NCT permeation rate increased with the use of magnesium hydroxide as a result of the neutral NCT that formed at a basic microenvironmental pH. The swollen HPMC tablets, with or without pH modifiers, gave sufficient adhesion to the mucosal membrane. Furthermore, the addition of magnesium hydroxide to the matrix tablets was the major factor in controlling buccal delivery of NCT. This study suggests that the NCT-MAS complex-loaded HPMC tablets, which contained magnesium hydroxide, are potential buccal delivery systems of NCT.
Affiliation
Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, 40002, Thailand, thaned@kku.ac.th.
Journal Details
This article was published in the following journal.
Name: AAPS PharmSciTech
ISSN: 1530-9932
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/22552930
- DOI: http://dx.doi.org/10.1208/s12249-012-9790-7
Medical and Biotech [MESH] Definitions
Blood Viscosity
The internal resistance of the BLOOD to shear forces. The in vitro measure of whole blood viscosity is of limited clinical utility because it bears little relationship to the actual viscosity within the circulation, but an increase in the viscosity of circulating blood can contribute to morbidity in patients suffering from disorders such as SICKLE CELL ANEMIA and POLYCYTHEMIA.
Nicotine
Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.
Magnesium Chloride
Magnesium chloride. An inorganic compound consisting of one magnesium and two chloride ions. The compound is used in medicine as a source of magnesium ions, which are essential for many cellular activities. It has also been used as a cathartic and in alloys.
Aluminum Compounds
Inorganic compounds that contain aluminum as an integral part of the molecule.
Magnesium Oxide
Magnesium oxide (MgO). An inorganic compound that occurs in nature as the mineral periclase. In aqueous media combines quickly with water to form magnesium hydroxide. It is used as an antacid and mild laxative and has many nonmedicinal uses.
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