Publications by authors named "Alina Panainte"

8 Publications

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New nitric oxide-releasing indomethacin derivatives with 1,3-thiazolidine-4-one scaffold: Design, synthesis, in silico and in vitro studies.

Biomed Pharmacother 2021 Jul 6;139:111678. Epub 2021 May 6.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, "Grigore T. Popa" University of Medicine and Pharmacy of Iași, 16 University Street, Iasi, Romania. Electronic address:

In this study we present design and synthesis of nineteen new nitric oxide-releasing indomethacin derivatives with 1,3-thiazolidine-4-one scaffold (NO-IND-TZDs) (6a-s), as a new safer and efficient multi-targets strategy for inflammatory diseases. The chemical structure of all synthesized derivatives (intermediaries and finals) was proved by NMR and mass spectroscopic analysis. In order to study the selectivity of NO-IND-TZDs for COX isoenzymes (COX-1 and COX-2) a molecular docking study was performed using AutoDock 4.2.6 software. Based on docking results, COX-2 inhibitors were designed and 6o appears as the most selective derivative which showed an improved selective index compared with indomethacin (IND) and diclofenac (DCF), used as reference drugs. The biological evaluation of 6a-s, using in vitro assays has included the anti-inflammatory and antioxidant effects as well as the nitric oxide (NO) release. Referring to the anti-inflammatory effects, the most active compound was 6i, which was more active than IND and aspirin (ASP) in term of denaturation effect, on bovine serum albumin (BSA), as indirect assay to predict the anti-inflammatory effect. An appreciable anti-inflammatory effect, in reference with IND and ASP, was also showed by 6k, 6c, 6q, 6o, 6j, 6d. The antioxidant assay revealed the compound 6n as the most active, being 100 times more active than IND. The compound 6n showed also the most increase capacity to release NO, which means is safer in terms of gastro-intestinal side effects. The ADME-Tox study revealed also that the NO-IND-TZDs are generally proper for oral administration, having optimal physico-chemical and ADME properties. We can conclude that the compounds 6i and 6n are promising agents and could be included in further investigations to study in more detail their pharmaco-toxicological profile.
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http://dx.doi.org/10.1016/j.biopha.2021.111678DOI Listing
July 2021

In Vitro Dissolution Studies of Amiodarone Hydrochloride From Hydroxy-Propyl-β-Cyclodextrin/Amiodarone Inclusion Complex Formulated Into Modified-Release Tablets.

Rev Med Chir Soc Med Nat Iasi 2016 Jul-Sep;120(3):715-9

Aim: Drug release from modified-release matrix tablets made of Kollidon® SR and Chitosan is dependent on its degree of solubility in the dissolution medium as well as on the matrix forming polymer. By complexing hydrochloride amiodarone with hydroxypropyl-β-cyclodextrin, an inclusion complex was obtained, which showed an increase in solubility by more than 200%. The complex was used to obtain modified-release matrix tablets based on Kollidon® SR and Chitosan.

Materials And Methods: Matrix tablets were obtained through direct compression method of non-complexed amiodarone and inclusion complex, and they were marked F1 and F10, respectively. The two formulations were studied comparatively in terms of release kinetics of the active substance through in vitro drug release tests. Those tests were conducted using a paddle apparatus II for 12 hours and two gastrointestinal simulation liquids with different pH values relevant for oral administration - 2 hours at pH 1.2 and 10 hours at pH 6.8. The release of hydrochloride amiodarone was quantified using a validated HPLC method. Two factors were calculated to assess the release profile of amiodarone: the similarity factor f1 and difference factor f2.

Results: The increase in Kollidon® SR concentration resulted in a slower release of amiodarone at both pH values. The use of Chitosan resulted in a decrease of AMD release only at pH 6.8.

Conclusions: The similarities between the two release profiles of AMD were confirmed by the values of the similarity factor (f1 = 43.697) and difference factor f2 (f2 = 68.263).
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November 2018

A NEW SPECTROPHOTOMETRIC METHOD FOR THE ASSAY OF LISINOPRIL.

Rev Med Chir Soc Med Nat Iasi 2015 Oct-Dec;119(4):1199-204

Aim: A new spectrophotometric method for the assay of lisinopril using 2,4-dinitrophenol as reagent is described.

Material And Methods: The method involved the addition of 2,4-dinitrophenol to lisinopril in methanol followed by absorbance measurement at 400 nm. Experimental conditions that provide wide linear range, maximum sensitivity, selectivity, accuracy and precisions were optimized.

Results And Discussions: Beer's law was obeyed in the concentration range 2.0-14.0 μg/mL. Linear regression equation of calibration graph was A = 0.005 + 0.045 x concentration, with a regression coefficient (r) of 0.9995 (n = 8). The limits of detection (LOD) and quantification (LOQ) calculated according to the ICH guidelines were 0.42 and 1.42 μg/mL, respectively. Accuracy and precision of the assays were determined by computing the intra-day and inter-day variations at three different lisinopril concentrations; the intra-day and inter-day RSD was < 1.43% and accuracy was better than 1.72%.

Conclusions: The proposed method is simple, easy to perform, sensitive, linear, precise, accurate and robust.
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March 2016

ANTINFLAMMATORY ACTIVITY OF AN N, N'-DISALICYLIDENEMETHYLENDIAMINE-DERIVED SCHIFF BIS BASE AND ITS COPPER(II) COMPLEX.

Rev Med Chir Soc Med Nat Iasi 2015 Oct-Dec;119(4):1195-8

Aim: The cooper(II) complex combination of N, N'-disalicylidenemethylenediamine and the Schiff bis base were investigated for anti-inflammatory activity.

Material And Methods: In vivo, the anti-inflammatory activity of the metallic complex in comparison with the activity of the Schiff bis base was tested by the method of Winter and co-workers using the Levy technique.

Results And Discussions: Our study on the anti-inflammatory activity of a new Schiff bis base and its complex cooper(II) combination showed that the Schiff bis bases exhibited significant anti-inflammatory action in acute experimental inflammation when compared to the control group. The copper cation from the complex combination enhanced the anti-inflammatory effect of the Schiff bis base, the effect being stronger at doses of 10 mg/kg cooper(II) complex.

Conclusions: The Schiff bis base and its cooper(II) complex had an anti-inflammatory effect comparable to that of indomethacin.
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March 2016

IN VITRO TESTING OF XANTHAN/LIGNIN HYDROGELS AS CARRIERS FOR CONTROLLED DELIVERY OF BISOPROLOL FUMARATE.

Rev Med Chir Soc Med Nat Iasi 2015 Oct-Dec;119(4):1189-94

Aim: To develop sustained release matrix tablets based on xanthan as highly water-soluble, cost-effective, non-toxic, easily available, and suitable hydrophilic systems.

Material And Methods: Xanthan and lignin epoxy-modified resin (LER) mixture were crosslinked using epichlorohydrin as crosslinking agent leading to superabsorbent hydrogels with high swelling rate in aqueous mediums.

Results And Conclusions: These hydrogels were tested as carries by the loading/delivery behaviour of bisoprolol fumarate in physiological conditions and based on the obtained results these hydrogels may show interest for application in medical and pharmaceutical areas. The amount of drug loaded in polymer networks was found to be ranging between 14.4% and 19.2%. Drug release was retarded and the release mechanism of the active principle was found to depend on matrix composition.
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March 2016

OPTIMIZATION OF THE PREPARATION OF KOLLIDON SR-BASED AMIODARONE HYDROCHLORIDE TABLETS WITH SUSTAINED RELEASE.

Rev Med Chir Soc Med Nat Iasi 2015 Oct-Dec;119(4):1161-5

Aim: The formulation of sustained release tablets of AMD-HCl using KOLLIDON SR as matrix-forming agent. Chitosan, a natural polysaccharide with superior hydrating and absorbing properties was used in the formulation stage to optimize the release characteristics of those matrix tablets.

Material And Methods: Nine formulations of sustained release matrix tablets of AMD x HCl (200 mg/tablet) were prepared through direct compression. The concentrations of matrix forming agents were included as independent variables of a type 2(3) mixed factorial plan in order to develop formulations of AMD-HCl with optimal release characteristics. The dependent variables of that plan were the amount of AMD released from the tablets studied by using in vitro dissolution testing. The test was carried out in the paddle apparatus II for 12 hours in two pH media that were relevant to oral delivery: 2 hours at pH 1.2 and 10 hours at pH 6.8. The released AMD-HCl was quantitatively determined through a validated HPLC method.

Results: The increase in KOL concentration leads to a decrease in AMD release rate at both pH values. The use of CHT resulted in a decrease of AMD release only at pH 6.8 in formulations with the lowest concentration of KOL.

Conclusions: The retarding effect on the release of AMD-HCl in the tablets developed in this study was directly proportional to the KOL concentration in the formulation.
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March 2016

Spectrophotometric method for estimation of bisoprolol fumarate in tablets.

Rev Med Chir Soc Med Nat Iasi 2014 Apr-Jun;118(2):558-63

Unlabelled: Bisoprolol fumarate is prescribed for the treatment of hypertension and angina pectoris.

Aim: The purpose of this study was to develop a simple, sensitive, accurate, and reproducible method for estimation of bisoprolol fumarate in tablets.

Material And Methods: The proposed method was based on a yellow colored complex formed with tropaeolin 00, extractable in dichloromethane with maximum absorbance at 412 nm. The method was validated statistically.

Results: The linearity domain was observed in the concentration of 5-30 microg/ml. The recovery studies confirmed the accuracy of the proposed method.

Conclusions: The proposed method can be applied for the routine analysis of bisoprolol from formulations.
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October 2014

Spectrometric method for the assay of ramipril using molybdophosphoric acid.

Rev Med Chir Soc Med Nat Iasi 2012 Oct-Dec;116(4):1218-22

University of Medicine and Pharmacy Grigore T Popa lasi, Faculty of Pharmacy.

Unlabelled: Ramipril is a drug of the angiotensin converting enzyme inhibitor class.

Aim: A new molecular absorbance spectrometric method was developed for the assay of ramipril using molybdophosphoric acid in acidic medium.

Material And Methods: The reaction product showed a maximum absorbance at 361 nm. The optimum conditions of the reaction were established. The developed method was validated.

Results: The method showed a good linearity in the range of 8 - 36 microg/ml (correlation coefficient r = 0.9996). The detection limit (LD) was 0.86microg/ml and the quantification limit (LQ) 2.88 pg/ml. Precision and accuracy were determined (RSD = 1.15%); mean recovery was 98.90% in the 97.13-101.03% concentration range.

Conclusions: The proposed method is simple, easy to perform, sensitive, linear, precise, accurate and robust.
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August 2013