CONTENT


FARMACIA Nr.4, 2007:

  1. ANALOGUES OF GONADORELIN. NEW THERAPEUTIC VALENCES IN BONE METASTASATED PROSTATE ADENOCARCINOMA.
    ROXANA LUCACIU, LUCIA DICAN, CORINA IONESCU, M. BOJITĂ
    Abstract


  2. DISTRIBUTION PROFILES OF DRUGS WITH ACTIVE METABOLITES BY COMPARTMENTAL ANALYSIS.
    F. RĂDULESCU, DALIA MIRON, C.MIRCIOIU, V.A.VOICU
    Abstract


  3. MOLECULAR MECHANISM OF CYCLOSPORINE A - INDUCED HEPATOTOXICITY.
    DAMASCHIN C., HERTZOG D., HERTZOG R., PATRANICHI B., NICULINA MITREA
    Abstract


  4. FORMULATION AND CHARACTERIZATION OF TOPICAL LIPOSOME GEL BEARING PIROXICAM.
    L. HÎNCU, D. LUPULEASA, A. ANDRIES
    Abstract


  5. EXPERIMENTAL RESEARCHES CONCERNING THE SYNTHESIS AND PHYSICO-CHEMICAL CHARACTERISATION OF SOME NEW THIOUREIDES OF 2-THIOPHENE-CARBOXYLIC ACID.
    CARMELLINA DANIELA BĂDICEANU, AL. MISSIR
    Abstract


  6. THE EFFICIENCY OF ANTI-TOBACCO THERAPY WITH BUPROPION IN PATIENTS WITH CORONARY ARTERY DISEASE AND NICOTINIC DEPENDENCE.
    DANIELA IONESCU, S. DRAGAN, S. FUNAR-TIMOFEI, M MARC, C. CRISTESCU
    Abstract


  7. INFLUENCE OF HYPERICI HERBA ON THE BLOOD PARAMETERS OF THE RATS.NOTE I. COMPLETE BLOOD CELL (CBC) COUNT.
    CLAUDIA-CRINA TOMA, V. CUCUIU, MIRELA VOICU,G. D. MOGOSANU, H. POPESCU
    Abstract


  8. STUDIES REGARDING A NEW ANTIDOTE FOR Pb2+ INTOXICATION. I. PHYTOBIOLOGICAL TESTING OF THE QUERCETOL- Pb2+ COMPLEX.
    FLORENTINA RONCEA, VIORICA ISTUDOR, LAURA BUCUR, ELENA DOROFTEI, MARIANA ARCUS
    Abstract


  9. IN VITRO STUDIES ON ANTIOXIDANT EFFECT OF MELATONIN ON RAT ASTROCYTES.
    ADINA BECHEANU, DANIELA GRĂDINARU, NICULINA MITREA
    Abstract


  10. IN VITRO RELEASE OF DICLOFENAC SODIUM FROM TOPIC HYDROGELS.
    MARCELA ACHIM, DIANA FILIP, L.VLASE, I.TOMUTA, S.E.LEUCUTA
    Abstract


  11. ANALYSIS OF OLIGOELEMENTS IN THE AERIAL PARTS OF PIG CHESTNUT (AESCULUS HIPPOCASTANUM L.) USING ATOMIC ABSORPTION SPECTROMETRY.
    TÜNDE HORVATH, ELENA CUREA, ILDIKO SZABO
    Abstract




ABSTRACTS:

1. ANALOGUES OF GONADORELIN. NEW THERAPEUTIC VALENCES IN BONE METASTASATED PROSTATE ADENOCARCINOMA.
ROXANA LUCACIU1, LUCIA DICAN2, CORINA IONESCU1, M. BOJITĂ3

University of Medicine and Pharmacy "Iuliu Hațieganu" Cluj-Napoca, Pasteur 4/6
1Departament of Pharmaceutical Biochemistry and Clinical Laboratory
2Departament of Medical Biochemistry
3Departament of Drug Analysis


- Abstract -

In metastated prostate adenocarcinoma androgen ablation is usually first line treatment, although ultimately most tumours become hormone refractory, requiring second or third line treatments. Physicians and patients need to take an active role in the decision making, and weigh the risk of side effects versus benefits of the alternative treatment options. The introduction of the analogues of Gonadorelin (GnRH agonists) in therapy revolutionized the treatment of metastasated prostate cancer because no surgery is required. Therefore, they are usually preferred to chirurgical orchidectomy or oestrogens therapy. Still, it has to be emphasized that GnRH analogues represent a palliative treatment, do not cure prostate cancer.


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2. DISTRIBUTION PROFILES OF DRUGS WITH ACTIVE METABOLITES BY COMPARTMENTAL ANALYSIS.
F. RĂDULESCU, DALIA MIRON, C.MIRCIOIU, V.A.VOICU

University of Medicine and Pharmacy "Carol Davila", Faculty of Pharmacy, 6 Traian Vuia street, Bucharest, Romania

- Abstract -

The problem of the determination of active metabolites in bioequivalence studies and decision criteria in such cases remains a disputed problem. It is largely accepted that the evaluation of bioequivalence using data for parent drugs is preferable since metabolites are less sensitive to formulation effects, but the basis for this believe were not systematically studied.
The paper evaluated model fitting of the parent drug and active metabolites pharmacokinetic profile, in a series of bioequivalence studies, comparatively analyzing the physiological and metabolic significance of results.
Despite of the fact that pharmacokinetics of metabolites is more complex than that of parent drug, modeling of data in the case of initial entity, put in evidence a more simple behavior.

- compartmental analysis
- diltiazem
- loratadine
- tramadol
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3. MOLECULAR MECHANISM OF CYCLOSPORINE A - INDUCED HEPATOTOXICITY.
DAMASCHIN C1, HERTZOG D2, HERTZOG R3, PATRANICHI B3, NICULINA MITREA4

1Central Military Hospital Bucharest
2UMF Craiova, Pharmacology Department
3Army Center of Medical Research Bucharest
4UMF Carol Davila Bucharest, Faculty of Pharmacy, Biochemistry Department; biochimiebucuresti@yahoo.com


- Abstract -

Cyclosporine A (CsA) induces hepatotoxicity by blocking the ATP-dependent membrane transporters, mainly BSEP pumps (bile salt export proteins) that export bile acids into the biliary canaliculi, OATP (organic anions transport proteins) that transport organic anions across the basolaterale membrane and glycoproteins (gp) that eject the drugs from cells. This blocking is caused by increased level of reactive oxygen species (ROS) that oxidize membrane phospholipids and change the fluidity of membranes, affecting the membrane transport and, in consequency, the elimination of bile acids, generating cholestasis. We suggest that a high level of ROS is the result of decreased level of glutathione and superoxide-dismutase activity, the crucial cellular anti-oxidant systems. The interaction between CsA and reduced glutathione which forms an adduct could determine a diminution of intracellular concentration of glutathione. Also, CsA can interact with other ubiquitar intracellular proteins.

- Cyclosporine A
- Hepatotoxicity
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4. FORMULATION AND CHARACTERIZATION OF TOPICAL LIPOSOME GEL BEARING PIROXICAM.
L. HÎNCU1, D. LUPULEASA2, A. ANDRIES1

University of Medicine and Pharmacy "Carol Davila", Faculty of Pharmacy, 6 Traian Vuia street , Bucharest
1Departament of Industrial Drugs and Pharmaceutical Biotechnology
2Departament of Pharmaceutical Technology


- Abstract -

Liposome gels, bearing piroxicam, intended for topical application were prepared and evaluated.
Liposomes composed of Soya lecithin and cholesterol, with lidocaine hydrochloride entrapped in the inner water compartment, were prepared by the simple mechanical method vortexing the phospholipid dispersion in water.
Topical liposome gels were prepared by incorporation of liposomes into a structured vehicle (1.5, 1.75 and 2 % Carbopol gel base). Also, corresponding hydrogels were prepared and drug release properties were investigated.
High percentage of encapsulated drug into liposomes was obtained (over 72 %). Liposome gels provided a prolonged drug release rate. The concentration of the gelling agent affected the release rate slightly. Also, embedding liposomes into a structured vehicle of Carbopol resulted in significantly slower drug release than hydrogels. Exponential dependence of the amount of drug released on time was evidenced; the diffusion exponents were superior to 0.5, indicating atipical Fickian diffusion, generally due to the swelling of the system in the solvent before the release took place. The mathematical processing of drug release data showed that after the 3rd hour liposomes acted as reservoir systems for continuous delivery of encapsulated drug.
Proposed formulations provided a stable percentage of encapsulated drug and drug release within an examination period of 3 weeks.

- Liposomes
- Piroxicam
- Carbopol gel
- Drug release
- Stability
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5. EXPERIMENTAL RESEARCHES CONCERNING THE SYNTHESIS AND PHYSICO-CHEMICAL CHARACTERISATION OF SOME NEW THIOUREIDES OF 2-THIOPHENE-CARBOXYLIC ACID.
CARMELLINA DANIELA BĂDICEANU, AL. MISSIR

University of Medicine and Pharmacy "Carol Davila", Faculty of Pharmacy Traian Vuia 6, Sect. 2, Bucharest Departament of Pharmaceutical Chemistry
*corresponding author: bcarmellina@yahoo.com


- Abstract -

The study continues our previous research regarding the chemical modeling of thioureides, with the aim of obtaining new compounds with potential pharmacological activity [2].
The biological activities of thiourea derivatives have been successfully screened for various biological actions: antidepressant, anticonvulsant, anthelmintic (nematodes), antispasmodic, antihistaminic, anesthetic (local), antipruritic, antitussive, analgesic etc [1,3].
For the new compounds synthesized from the 2-thiophenecarboxylic acid, we established the optimal reaction conditions to synthesize the new thioureides with high purity and yields and with potential pharmacological properties.

- thiourea derivatives
- thioureides
- 2-thiophenecarboxylic acid derivatives
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6. THE EFFICIENCY OF ANTI-TOBACCO THERAPY WITH BUPROPION IN PATIENTS WITH CORONARY ARTERY DISEASE AND NICOTINIC DEPENDENCE.
DANIELA IONESCU1*, S. DRAGAN2 , S. FUNAR-TIMOFEI3, M MARC4, C. CRISTESCU5

1Department of Toxicology, Victor Babes University of Medecine and Pharmacy, 2 Eftimie Murgu Square, 300411 Timisoara, Romania;
2Department of Cardiovascular Rehabilitation, of the Institute of Cardiovascular Diseases Timisoara Victor Babes University of Medecine and Pharmacy
3C. Dragulescu" Institute of Chemistry, Romanian Academy
4Preventive Antitobacco Centre of Timisoara
5Department of Clinical Pharmacy and Pharmacology, Victor Babes University of Medecine and Pharmacy
*corresponding author: daniela_ionescu2002@yahoo.com


- Abstract -

We aimed to evaluate the efficacy of Bupropion sustained release (Bupropion SR) in promoting abstinence from smoking in the case of patients with cardiovascular diseases and especially with coronary artery disease. 205 patients were diagnosed with cardiovascular diseases and nicotinic dependence within 2002-2003. Only the subjects with inclusion criteria were randomised in two groups: (A) 61 patients with Bupropion SR therapy and (B) 58 subjects with placebo conditions. Continous smoking abstinence rate in the 12th, 26th and 52nd week was evaluated. The prevalence of abstinence was significantly higher for the patients Bupropion SR compared with placebo. The study indicated that treatment with Bupropion SR can improve the rate of smoking abstinence over placebo in a population of smokers with cardiovascular diseases and especially coronary heart troubles.

- Bupropion
- Nicotinic dependence
- Cardiovascular and coronary artery disease
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7. INFLUENCE OF HYPERICI HERBA ON THE BLOOD PARAMETERS OF THE RATS. NOTE I. COMPLETE BLOOD CELL (CBC) COUNT.
CLAUDIA-CRINA TOMA1, V. CUCUIU2, MIRELA VOICU3, G. D. MOGOSANU4*, H. POPESCU4

1Department of Pharmacognosy & Phytotherapy
2Department of Pharmaceutical industry and Biotechnologies
3Department of Pharmacology "Victor Babes" University of Medicine and Pharmacy Timisoara, Faculty of Pharmacy, 2 Eftimie Murgu Street, 300041 Romania
4Department of Pharmacognosy & Phytotherapy University of Medicine and Pharmacy of Craiova, Faculty of Pharmacy, 2-4 Petru Rares Street, 200349 Romania
*Corresponding author: mogosanu@umfcv.ro


- Abstract -

Hypericum perforatum L. is a traditional folk remedy used for the treatment of superficial wounds, scars, burns, ulcers, myalgia, and moderate depression. Hypericin is a photodynamic active plant pigment, which may cause a severe photodermatitis called hypericism, when higher amounts of St. John's wort are orally ingested. The active principles from Hyperici herba correlated with UV-B light are responsible for the phototoxic effects with the variation of the complete blood cell (CBC) count of the rats: decreasing of the erythrocytes number, haemoglobin and hematocrit levels, and increasing of the thrombocytes and leukocytes number. The blood parameters MCV, MCH, MCHC, and RDW were in normal limits. Taking into account these toxic effects, it is recommended to avoid the direct exposing to the sun or to use some photoprotective creams with a high level of protection, during the treatment with medicinal products based on Hyperici herba.

- Hyperici herba
- rats
- complete blood cell (CBC) count
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8. STUDIES REGARDING A NEW ANTIDOTE FOR Pb2+ INTOXICATION. I. PHYTOBIOLOGICAL TESTING OF THE QUERCETOL- Pb2+ COMPLEX.
FLORENTINA RONCEA1, VIORICA ISTUDOR2, LAURA BUCUR1, ELENA DOROFTEI3, MARIANA ARCUS1

1"Ovidius" University, Dental Medicine and Pharmacy Faculty, Pharmacy Department, Constanta
2"Carol Davila" Medical and Pharmacy University, Pharmacy Faculty, Bucharest
3"Ovidius" University, Biology Faculty, Constanta
*Corresponding author: florentinaroncea@yahoo.com


- Abstract -

Our research used Constantinescu phytobiological method (Triticum test) and root development and potential changes of the mitotic film of the plant cell (biological reactant) were registered. The measurements were performed on Triticum vulgare Mill., wheat (Poaceae) caryopses using methanol solutions of quercetol-Pb2+ complex (referred to as Qcomplex) with concentrations ranging between 6,6x 10-5 and 1 x 10-3M, towards a control maintained in water.
The influences of these solutions on wheat root development were followed in 5 consecutive days as well as the potential influence over the mitotic film, after 6 and 24 hours respectively. The data were statistically evaluated using the Student "t" test. We determined that: none of the solutions inhibited the germination of the wheat caryopses, embryonic root development stimulation takes place between concentrations of 6.6 x 10-5 and 6,6 x 10-4M and development inhibition produced between 7,3x 10-4 and 1x 10-3 M. At macroscopic level, development of contorted, thickened and claw-like secondary roots were noted at samples with concentrations between 3,3x 10-4 M and 1 x 10-3 M. Regarding the root development we noticed significant variations among series, which determines us to think that these should be due rather to the plant tissues and not to the concentration of the quercetol- Pb2+ complex. Statistically significant are considered only 6 samples with p < 0.05, while other 8 samples with p > 0.05 were considered insignificant.
In comparison, the changes in the mitotic film revealed a cytotoxic effect expressed in plasmolysed cells, hypertrophied nuclei, heterochromatinization, degrading genetic material which demonstrates the cytotoxic character of the lead elimination product following treatment with quercetol (as antidote).

- Pb2+ intoxication
- Quercetol- Pb2+ complex
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9. IN VITRO STUDIES ON ANTIOXIDANT EFFECT OF MELATONIN ON RAT ASTROCYTES.
ADINA BECHEANU, DANIELA GRĂDINARU*, NICULINA MITREA

Department of Biochemistry, Faculty of Pharmacy, University of Medicine and Pharmacy "Carol Davila", Bucharest
*corresponding author: biochimiebucuresti@yahoo.com


- Abstract -

Reactive oxygen species (ROS) produced during the normal metabolism and under conditions of oxidative stress, are though to be implicated in the etiology or progression of several neurodegenerative pathologies and in the normal brain aging. However, recent studies pointed out that ROS could initiate complex intracellular redox modulatory systems that regulate gene transcription and translation of many phase I and II drug metabolizing enzymes. By the use of primary cultures of rat astrocytes, this study aimed at following up the effects of an induced oxidative stress caused by the exposure to redox-cycling xenobiotics, on conjugation enzyme expression UDP-glucuronosyl transferases (UGT). We showed that after a 48-hours treatment with moderate concentrations of menadione, paraquat, UGT expression was significantly incresed. In the presence of the antioxidant melatonin in the culture medium, the induction of these detoxification enzymes was suppressed.

- astrocytes
- reactive oxygen species
- melatonin
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10. IN VITRO RELEASE OF DICLOFENAC SODIUM FROM TOPIC HYDROGELS.
MARCELA ACHIM, DIANA FILIP, L.VLASE, I.TOMUTA, S.E.LEUCUTA.

University of Medicine and Pharmacy "Iuliu Hatieganu", Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 13, Emil Isac Street, 400023, Cluj-Napoca, Romania

- Abstract -

The in vitro release of diclofenac sodium (DS) from commercial and original hydrogels was studied using a static diffusion cell. The original hydrogels were prepared on polyacrylic acid (Carbopol 940), sodium carboxymethylcellulose (NaCMC) and methylcellulose (MC). DS was incorporated by dissolution, the concentration being 1% (w/w). The assay of DS was made spectrophotometrically in UV at 275 nm. The release kinetics were determined by the use of two mechanistic mathematical models (Higuchi and Peppas).
The results showed that in vitro DS release from all commercial hydrogels was similar, while in the case of original hydrogels the release was slighly dependent on the nature of hydrogel forming agent. The release rate of DS from emulsion in hydrogel was lower than from simple commercial hydrogels. In the case of the original hydrogels the release rate decreased slightly in the order: NaCMC, Carbopol and MC. The release rate from original hydrogels was little lower than from commercial hydrogels.

- diclofenac sodium
- hydrogels
- in vitro release
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11. ANALYSIS OF OLIGOELEMENTS IN THE AERIAL PARTS OF PIG CHESTNUT (AESCULUS HIPPOCASTANUM L.) USING ATOMIC ABSORPTION SPECTROMETRY.
TÜNDE HORVATH1, ELENA CUREA2, ILDIKO SZABO1

1University of Oradea, Faculty of Medicine and Pharmacy, Pta 1 Decembrie nr. 10, cod 410073
2Faculty of Pharmacy, University of Medicine and Pharmacy "Iuliu Hațieganu", Cluj-Napoca


- Abstract -

The lack of oligoelements in organisms may constitute the cause of diseases whose symptoms become reversible by means of a nutrition based on these oligoelements. Vegetal products may constitute an important source of essential oligoelements.
Using atomic absorption in flame spectrometry (AASF) we evaluated the content of oligoelements such as: Cu, Zn, Mn, Cr, Ni, Cd, Pb in the aerial parts (leaves, flowers) of Aesculus hippocastanum L. (the pig chestnut).
Taking into account that the type and humidity of the soil, the atmospheric polution, the age of the plant and the morphologic properties influence the content of oligoelements, with this work we performed a comparative analytical study.

- Atomic absorption spectrometry
- Aesculus hippocastanum L.
- Oligoelements
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