A new inclusion complex of amlodipine besylate and soluble β-cyclodextrin polymer: preparation, characterization and dissolution profile

Abstract

Amlodipine besylate (AML) has become the most popular blood pressure medication for hypertensive pets. It belongs to the class I (high solubility and high permeability) according to BCS and is marketed in Europe only as white tablets equivalent to 2.5, 5.0 and 10.0 mg of amlodipine for oral administration. Unfortunately, oral AML dosage for cats and dogs is in the range 0.1–0.2 and 0.625–0.125 mg/kg/die respectively. Moreover, AML shows a slight solubility in water according to Ph. Eur. 7°. According to these considerations, the aim of this work was the complexation between soluble β-cyclodextrin polymer (CD) and AML using the solubilization/freeze-dried method to obtain powders easily dosable and soluble in water for the treatment of hypertension in pets. The complex in solution was evaluated by phase solubility studies that indicated the optimal 2:1 drug/CD ratio to form a stable complex. UV–Vis absorption and circular dichroism showed the formation of a complex with a weak bond such as confirmed by differential scanning calorimetry, infrared spectroscopy and fluorescence microscopy. In vitro dissolution/release tests were performed in water to investigate the influence of formulative parameters on drug dissolution/release properties. The inclusion of AML in CD increased its wettability, dissolution rate and solubility in water. This method could be a suitable approach for the administration of an extemporaneous solution of the antihypertensive drug to guarantee a correct dose to pets increasing the compliance

Evidence of the Disassembly of α-Cyclodextrin-octylamine Inclusion Compounds Conjugated to Gold Nanoparticles via Thermal and Photothermal Effects

“…CD ICs have been extensively studied using different techniques, including differential scanning calorimetry (DSC). This technique corroborates IC formations by comparing the thermal profiles of the isolated precursors with those of the conjugate systems [6,7,8]. However, thermal studies that provide information on CD IC topotactic processes have not been studied.…”

Design and Evaluation of Orally Dispersible Tablets Containing Amlodipine Inclusion Complexes in Hydroxypropyl-β-cyclodextrin and Methyl-β-cyclodextrin

“…Several studies that investigated AML inclusion in different β-CDs cavities had already been performed and published, and they served as starting points for the present study. Lauro et al [ 12 ] proved, with phase solubility studies, that the optimal molar ratio to form a stable complex is 2:1 drug/CD. Meantime, Malakzadeh et al [ 29 ] calculated the formation constant and found that a 1:1 molar ratio leads to the encapsulation of AML in β-CDs.…”

“…Two forms of amlodipine are reported: S-enantiomer, which is more active, and R-enantiomer [ 10 , 11 ]. Amlodipine besylate (AML), the besylate salt of amlodipine, has become the most used blood pressure medication [ 12 ] and the most widespread cardiovascular drug [ 13 ]. The different polymorph forms of amlodipine besylate (hydrated or solvated forms) can affect pharmaceutical properties like morphology, stability, solubility, dissolution rate, and also the final performance of solid dosage tablets.…”

Development and In Vitro Evaluation of an Innovative “Dietary Flavonoid Supplement” on Osteoarthritis Process

“…Thermograms were recorded by placing accurately given quantities (1-2 mg weighed with a microbalance MTS Mettler Toledo, OH, USA) of each sample in a 40 μ L aluminium pan which was sealed and pierced. The sample was scanned (10°C/min) between 25 and 350°C [ 27 ]. Melting temperature ( T m ) and heat of fusion (Δ H m ) were measured.…”