Complexation of Amlodipine Besylate with β-Cyclodextrin.
نویسندگان
چکیده
In this paper the procedure for the preparation of inclusion compounds of bioactive substance 2-[(2-aminoetoxy)-methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridine dicarboxylic acid 3-ethyl-5-methyl esterbenzene sulfonate, called amlodipine besylate with β-cyclodextrin (β-CD) and their structural characterization was described. Molecular inclusion compound of amlodipine besylate is obtained by different preparation method: kneading, co-precipitation and freeze-drying. The so obtained compounds were investigated by FTIR spectroscopy, X-ray diffraction method and differential scanning calorimetric measurements (DSC) to evidence their formation. Molecular modeling (using DFT theoretical computations) shows the spatial architecture of the inclusion compound in good agreement with FTIR experimental data: the drug is included with dihydropyridine dicarboxylate part inside β-cyclodextrin cavity. The inclusion of amlodipine besylate in β-cyclodextrin increases the stability and bioavailability of the drug.
منابع مشابه
Simultaneous estimation of amlodipine besylate and nebivolol hydrochloride in pharmaceutical tablets formulation by RP-HPLC using PDA detector
Background: The present work was undertaken with the aim to develop and validate a rapid and consistent RP-HPLC method in which the peaks will be appear with short period of time as per ICH Guidelines. Materials and Methods: The separation was achieved on a a stainless steel analytical column, Eclipse XDB plus C18 column (4.6 X 150 mm; 5 μm) in an isocratic mode. The mobile phase w...
متن کاملAripiprazole-Cyclodextrin Binary Systems for Dissolution Enhancement: Effect of Preparation Technique, Cyclodextrin Type and Molar Ratio
Objective(s): The aim of this work was to investigate the effect of the natural and the chemically modified form of cyclodextrins namely; β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) respectively on the solubility and dissolution rate of aripiprazole; an antipsychotic medication showing poor aqueous solubility. Materials and Methods: Phase solubility of ar...
متن کاملThe Effect of Water Soluble Polymers on Felodipine Aqueous Solubility and Complexing Abilities with Natural and Modified β-Cyclodextrin
Purpose of this study was to investigate the effect of the presence of the water soluble polymers viz HPMC, PVP and PEG 6000 on aqueous solubility and complexation abilities of felodipine with or without presence of β-cyclodextrin (βCD) and HPβCD by phase solubility studies. The data revealed the initial increase in drug solubility followed by plateau in t...
متن کاملSolubility of Cyproterone Derivatives in the Presence of Hydroxypropyl-β-Cyclodextrin: Experimental and Molecular Modeling Studies
This study presents the influence of hydroxypropyl-β-cyclodextrin (HPBCD) on the aqueous solubility of acyl esters of cyproterone. First, a number of esters of cyproterone were synthesized. Then the phase solubility analysis of the compounds in the presence of HPBCD was investigated in phosphate buffer solution at a pH of 7.4. To gain a better understanding of the complexation mechanism, ...
متن کاملAmlodipine besylate-excipients interaction in solid dosage form.
This article studies the compatibility of amlodipine besylate in its solid formulations with various drug excipients. The various factors affecting amlodipine besylate stability were studied using high-performance liquid chromatography (HPLC). It has been found that binary 1:1 mixtures of amlodipine besylate and an excipient are stable at 65 degrees C and 40 degrees C/75% RH. Further investigat...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Acta chimica Slovenica
دوره 59 1 شماره
صفحات -
تاریخ انتشار 2012