Background: Cyclodextrins are widely used as complexing agents to increase the solubility of poorly water-soluble drugs, to improve their bioavailability and stability, to reduce or prevent gastrointestinal or ocular irritation, to reduce or eliminate unpleasant smells or tastes and to prevent drug-drug or drug-additive interactions. In recent years, cyclodextrins have been proven to be effective as host compounds in molecular recognition and chiral separation.
Aim: To evaluate the complexation role of cyclodextrins toward fluoroquinolones (FQ) in an attempt to assess their potential as new formulation additives for more efficient fluoroquinolone delivery and as chiral selectors in case of racemic mixture compounds.
Material and methods: Guest-host interactions of three second generation quinolones, ciprofloxacin, ofloxacin and norfloxacin with two parent cyclodextrins, beta-cyclodextrin (b-CD), gamma-cyclodextrin (g-CD) and a beta-cyclodextrin derivative, 2-hydroxypropyl beta-cyclodextrin (HP-b -CD), were tested. Computer aided molecular modelling (ChemBio3D Ultra 12.0) was utilized to predict the preferred orientation of fluoroquinolones in the cyclodextrin cavity and the main structural features responsible for the enhancement of their solubility and photostability. Ciprofloxacin/b-cyclodextrin complex was prepared and the formation of inclusion complex was
demostrated by IR spectroscopy.
Results: Our studies show that the orientation with the piperazinyl group included in the CD cavity is energetically more favorable.
Conclusions: The CDs act as complexing agents with the three FQ derivatives, which enter inside the CD torus, and interact with the hydroxyl groups of CD by Van der Waals, electrostatic forces ang hydrogen bonding. Our results suggest the 1:1 stoichiometry in the complex formation.
Category Archives: Number
Surgical Strategies in the Differentiated Cancers of the Thyroid
Introduction: Amongst all epithelial cancers of the thyroid, the papillary and folicular types are usually histologically differentiated and have a more favourable outcome compared to the undifferentiated tumours. The aim of our study is to evaluate the surgical treatment of differentiated thyroid neoplasms both in terms of surgical indication and type of surgery.
Material and method: The study was conducted on 1349 patients suffering from different thyroid diseases that requested surgery between 2005–2009, within the First and Second Department of Surgery Tg-Mures.
Result: There have been taken into account data regarding the demographic aspecs, the pre- and postoperative diagnosis, surgical indication and the type of surgical procedure according to the histological type.
Conclusions: Surgery has proven to be the most efficient therapy in the differentiated forms of thyroid cancer including different types of total/near-totally thyroidectomies, and partial thyroidectomy comes into question only in exceptional cases.
Physical and Chemical Study of Simvastatin Inclusion Complexes
Background: Simvastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia.
Aim: To enhance his bioavailability through inclusion complexation, as host molecule hydroxypropyl-b-cyclodextrin had been used. The objective of this study is to present our results of the study of some simvastatin and hydroxypropil-b-cyclodextrin (HPbCD) inclusion complexes. We analyzed the products by phase solubility study, dissolution test and Fourier-transformed Infrared Spectroscopy (FT-IR).
Methods: Complexes were prepared by kneading molecular ratios of 1:1 and 1:2 and compared also with physical mixtures. Solubility studies were performed in the presence of various HPbCD concentrations and the stability constant was calculated. The inclusion complexation was evaluated by dissolution and Fourier transformed infrared spectroscopy.
Results: When compared with the pure drug, the dissolution of simvastatin is improved in the presence of b-cyclodextrin derivates, depending on the complex preparation method.
Conclusions: The solubility of simvastatin increases as a function of HPbCD concentration. FT-IR study suggests the presence of intermolecular hydrogen bonds between simvastatin and HPbCD in inclusion complex.
Improvements of Amoxicillin Stability in Acidic Environment
Background: Helicobacter pylori is a gram negative bacteria responsible for a series of gastrointestinal diseases: gastric and gastroduodenal ulcers. Usually used in combinations with other drugs, amoxicillin is effective against this germ. Amoxicillin has better stability than other penicillins in solutions with pH between 4 and 7, but stability is decreased at low pH values (gastric acidity).
Aim: Our goal was to improve amoxicillin’s stability by using auxiliary substances such b-cyclodextrin (b-CD), 2-hydroxypropil-bcyclodextrin (2-HP-b-CD), magnesium glutamate and magnesium aspartate.
Methods: Influence of these excipients on amoxicillin stability was assessed at pH value of 1.2 and also in weakly alkaline environment. High pressure liquid chromatography and thin layer chromatography were used to quantitate these influences.
Results: All the studied excipients improved the stability of amoxicillin, best results being recorded when amoxicillin was associated with cyclodextrins in a mole ratio of 1:5.
Conclusions: Poor stability of amoxicillin in acidic environments can be overcome by using cyclodextrins and magnesium salts of glutamic and aspartic acids.
Medical Versus Revascularization Therapy in the Management of Stable Angina Pectoris
Background: In patients with stable coronary artery disease, there are very few studies that compare the value of optimal medical therapy with revascularization therapy in reducing the risk of cardiovascular events.
Aim: To compare three therapeutic options for stable angina pectoris: percutaneous coronary intervention (PCI), coronary artery bypass grafting (CABG) and medication alone.
Methods: We studied 98 randomized patients with stable angina pectoris who underwent coronarography and had objective evidence of significant coronary disease. We assigned 36 patients to undergo PCI, 28 patients to undergo CABG, both subgroups with optimal medical therapy, and 34 patients with optimal medical therapy alone. Primary outcomes were cardiac death and non fatal myocardial infarction, during a follow-up period of 3 years.
Results: There were 3 primary events in the medical-therapy group, 1 event in the CABG group and 1 event in the PCI group. The 3-year cumulative primary-event rates were 2.8% in the PCI group, 3.6% in the CABG group and 11.8% in the medical-therapy group (P = 0.16).
Conclusion: In patients with disabling stable angina pectoris without high-risk criteria, the revascularization has the advantage of improving the long-term quality of life. In some patients with high-risk criteria, the percutaneous coronary intervention using drug-eluting stents can be a viable alternative to surgical revascularization.
General Characteristics of the Romanian Medical Webscape
Background: Although the percentage of Romanians who use the Internet to find health information is 16% and the proportion of Romanians looking for health information on the web has tripled from 2006 to 2009, no attempt has been made so far to assess the quality of information in the Romanian medical webscape.
Aim: The present study aimed to evaluate some general characteristics of the Romanian health related websites.
Methods: We investigated a sample of 317 medical sites randomly selected from the largest Romanian web directory. Two of the authors collected independently data about the number of unique visitors/month, medical specialty, site ownership, main purpose of the site and target audience. Disagreements were identified and a final common decision was taken by the evaluators through consensus.
Results: Our results suggest that the Romanian medical webscape represents a relatively small portion of the Romanian webscape. In terms of number of sites, we found that the most prominent categories were the complementary and alternative medicine sites and multispecialty sites ranking first and second respectively. With more then 80% of the total traffic recorded by the medical websites, multispecialty sites clearly dominate the virtual health space. A very small number of medical websites have a real potential to influence health
information seeking Internet users, since almost 90% of the medical websites draw an insignificant number of visitors.
Conclusions: The results of our study might be representative beyond its statistical population to the general Romanian webscape but this has yet to be verified.
Studies Concerning the Synthesis and Characterization of Hydroxyapatite Powder
Introduction: Recently, a special attention was given to the growth of some biomaterials with the goal of renewal and/or reconstruction of bone tissue. Of these biomaterials, hydroxyapatite (HA) presents a series of properties such as biocompatibility and bioactivity, being frequently used for bone grafts realization and to cover some metallic components of some prosthesis used in orthopedics. Although HA is available on the market as synthetic material for more than 15 years, being used for ceramic implants for more than 10 years, new solutions are looked for the inclusion in its structure of some anionic or cationic substitutes in order to bring its composition closer to the biologic apatite.
Aim: The aim of this study was to synthetise and characterize hydroxyapatite powder.
Method: Of the synthesis methods of HA, we used the wet-precipitation method. The obtained compound using this method was characterized by X-ray diffraction (XRD), FTIR microspectroscopy and laser difractometry.
Results: The XRD spectra showed that the obtained material is HA and we managed to establish the optimum parameters for obtaining HA uncontaminated by impurities and crystalline.
Conclusions: Using a method of chemical synthesis through precipitation, we obtained a HA powder, crystalline and stoechiometric.
The Role of Sonoelastography in the Differential Diagnosis of Breast Lesions
Background: Tissue elasticity imaging technology is expected to be a new modality for breast diagnosis, based on hardness as a tissue characteristic that is affected by tissue disease such as cancer.
Aim: To assess the value of sonoelastography in the differential diagnosis of breast lesions.
Patients and method: We included in this prospective study 59 patients diagnosed with breast lesions between January 2009 and January 2010. All the patients were examined in the supine position and the B mode ultrasound image was displayed alongside the elastography strain image. An EUS Hitachi EUB 8500 ultrasound system with an embedded elastography module (Hitachi Medical Systems Europe Holding AG, Zug, Switzerland) and a 6.5-MHz linear probe was used to obtain the B mode and elastography strain images. The elastography strain images were scored according to the Tsukuba elasticity score.
Results: For assessment of sonoelastography role in differential diagnosis of breast lesions, we performed ROC analysis, and we obtained a sensitivity of 89.7%, and a specificity of 92.9% (area under the ROC curve = 0.924, 95% CI = 0.822–0.977 and p = 0.0001).
Conclusions: Elastography is a fast, simple method which can complement the conventional US. Elastography is promising, and with future improvements in the technology, this imaging modality will become an invaluable tool for the diagnosis of breast diseases in the clinical setting.
Depression and Quality of Life in Elderly Patients with Cluster C Personality Disorder
Introduction: Health-related quality of life (HRQoL) is an accepted outcome measure in patients with depression.
Aim: Our study aimed at assessing QoL in depressed elderly patients with cluster C PDs, admitted to Psychiatric Clinic No II Targu Mures. Cluster C PDs is the most frequent diagnosis on axis II for depression.
Material and method: A sample of thirty elderly in-patients with cluster C PDs and depression was studied. Mental disorders were assessed based on DSM IV criteria, Hamilton scale of depression and SCID II (structured clinical interview for DSM). QoL was assessed with the aid of the World Health Organization Quality of Life instrument (WHOQoL-Bref), and the Global Assessment of Functioning scale (GAF).
Results: We formed high co-morbidity among depression and cluster C PD, especially dependent PD, which was associated with poor QoL. The WHOQoL physical health and social functioning were significantly associated with GAF. Conclusion and Discussion: PD symptoms in elderly patients appear to operate as co-factor that amplify or exacerbate the impact of depression on long-term functioning and QoL. We conclude that if co-morbid personality disorder is not treated, patients will respond less well to treatment for depression than do those without PD.
Medico-legal and Social Aspects of Mechanic Asphyxias
Background: In the last years, in Mureş county there was ascertained a significant growth of deaths due to anoxias caused by violence.
Aim: This study is an assessment concerning the prevalence and incidence of mechanical asphyxia in Mures county over three years, from 2005 to 2007.
Methods: The study took place at the Forensic Medicine Institute, Tg. Mures, including the analysis of 1926 medico-legal necropsies, 434 cases being violent deaths caused by mechanical asphyxias like: hanging, drowning in water and asphyxia with food bolus.
Results: In the analyzed casuistry was found that there were prevalent the deaths caused by hanging (343 cases), these being followed by the drowning ones (84 cases) and then the mechanical asphyxias caused by food bolus (7 cases). Distribution by sex showed a predominance of deaths in males (352 cases) compared to females (82 cases). Depending on location, deaths in rural location were prevalent to the ones from the urban location.
Conclusions: Concerning mechanical asphyxias predominates the mechanical asphyxia by hanging, which also represents suicide method, the other 2 types of asphyxias (drowning in water and mechanical asphyxia caused by food bolus) being seldom. Death by drowning in water represents a rarer method of suicide and the accidental form is met more during the warm season. Asphyxia with food bolus is produced totally accidental in persons under alcohol influence or total edentate.