Delivery of siRNA and Chloroquine Through an Aspherical, Nanostructured Microparticle for Passive Targeting of Alveolar Macrophages and Inhibition of Local TNF-α Secretion
Elena Haettig, Aaron Haben, Ralf Kautenburger
et al.
<b>Background/Objectives</b>: Alveolar macrophages represent the main path of defense in the peripheral pulmonary tissue, though their role in chronic inflammatory lung diseases shows that their protective function can turn pathological. This study focused on developing a system to passively target the release of the pro-inflammatory cytokine TNF-α through the local delivery of siRNA. <b>Methods</b>: An inhalable aspherical microparticle made up of mesoporous silica nanoparticles, crosslinked by an electrostatic LbL-system embedding the siRNA, was developed. <b>Results</b>: Through testing with the NGI, adequate aerodynamic properties with an MMAD as low as 3.37 µm could be determined, with a GSD as low as 1.46, suggesting a relatively small size distribution even during inhalation. To further understand the interaction of the microrods with the lung parenchyma and the resident cells, the disintegration of the rods in different simulant body fluids, their toxicity, and the cell uptake through dTHP-1 and A549 were observed. This showed slow but continuous disintegration, no toxicity in A549 cells, and high microrod uptake by dTHP-1 cells. To demonstrate the effect of the delivered siRNA on the release of TNF-α, ELISAs were carried out, establishing an inhibitory effect of the siRNA-carrying microcarrier system compared to those without siRNA or loaded with scrambled siRNA. To increase the efficacy of the siRNA, chloroquine as an endosomal escape-enhancing compound was loaded onto the mesoporous silica nanoparticles. This resulted in a significant improvement in siRNA inhibition. <b>Conclusions</b>: The developed formulation is able to reach the targeted structure and inhibit the secretion of TNF-α, with CQ increasing the inhibitory effect of the siRNA.
Pharmacy and materia medica
Integrated <i>In Vitro</i> and <i>In Silico</i> Profiling of Piperazinyl Thiosemicarbazone Derivatives Against <i>Trypanosoma cruzi</i>: Stage-Specific Activity and Enzyme Inhibition
Héctor A. Baldoni, María L. Sbaraglini, Darío E. Balcazar
et al.
<b>Background:</b> <i>Trypanosoma cruzi</i>, the causative agent of Chagas disease, remains a major public health concern, and there is a continued need for new antitrypanosomal agents. Thiosemicarbazone (TSC) derivatives have emerged as a promising class of compounds with potential antiparasitic activity. <b>Objectives:</b> This study aimed to report the synthesis, characterization, and biological profiling of a novel series of thiosemicarbazone derivatives as antitrypanosomal agents against <i>Trypanosoma cruzi</i>. <b>Methods:</b> Fourteen new compounds and six previously described analogues were prepared and characterized by <sup>1</sup>H/<sup>13</sup>C nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry (MS). As a preliminary <i>in vitro</i> screen, activity was assessed by direct parasite counting in epimastigote and bloodstream trypomastigote forms, as tractable models of replicative and infective stages sharing core metabolic targets with intracellular amastigotes. Epimastigote potency was quantified as half-maximal effective concentrations (EC<sub>50</sub>) derived from dose–response curves, whereas trypomastigote response was evaluated as percent viability after treatment at a fixed concentration of 20 µM. Mechanistic profiling included inhibition assays against the cysteine protease cruzipain (CZP) and selected redox defense enzymes, complemented by <i>in silico</i> similarity clustering and binding-pose affinity scoring. <b>Results:</b> A nitro-methoxy-substituted TSC showed potent CZP inhibition but limited trypomastigote efficacy, whereas brominated analogues displayed dual-stage activity independent of CZP inhibition. Tanimoto similarity analysis identified distinct structure–activity clusters, linking nitro-methoxy substitution to epimastigote selectivity and brominated scaffolds to broader antiparasitic profiles, with hydrophobicity and steric complementarity as key determinants. Enzymatic assays revealed no significant inhibition of cytosolic tryparedoxin peroxidase (cTXNPx) or glutathione peroxidase type I (TcGPx-I), suggesting redox disruption is not a primary mode of action. <i>In vitro</i> and <i>in silico</i> analyses showed low or no non-specific cytotoxicity under the tested conditions, supporting further optimization of these derivatives as antitrypanosomal preliminary hits. Key hits included derivative <b>3e</b> (epimastigote EC<sub>50</sub> = 0.36 ± 0.02 µM) and brominated analogues <b>2c</b> and <b>2e</b> (epimastigote EC<sub>50</sub> = 3.92 ± 0.13 and 4.36 ± 0.10 µM, respectively), while docking supported favorable binding-pose affinity (e.g., ΔG<i><sub>S</sub></i><sub>-pose</sub> = −20.78 ± 2.47 kcal/mol for <b>3e</b>). <b>Conclusions</b>: These results support further optimization of the identified thiosemicarbazone derivatives as preliminary antitrypanosomal hits and provide insight into structure–activity relationships and potential mechanisms of action.
Medicine, Pharmacy and materia medica
Long-Term Outcomes of Periodontal Interventions in Children with Leukemia: A Retrospective Analysis
Anuj Singh Parihar, Bhawna Gupta, Parth Shailesh Bhatt
et al.
Background:
Leukemia and its treatment compromise oral health, increasing periodontal disease risk in children. This study evaluated the long-term effects of periodontal interventions in children with leukemia.
Methods:
We reviewed records of 85 children with leukemia receiving periodontal treatment at People’s Dental Academy (2010–2020). Data included demographics, leukemia subtype (Acute Lymphoblastic Leukemia [ALL], Acute Myeloid Leukemia [AML], others), chemotherapy, Hematopoietic Stem Cell Transplantation [HSCT] history, periodontal diagnosis (gingivitis, periodontitis), interventions (scaling/root planing, surgery), and clinical parameters (Pocket Depth [PD], Clinical Attachment Level [CAL], Bleeding on Probing [BOP], radiographic bone loss) at baseline, one, three, and five years. Patients with ≥ three-year follow-up were included. Data were analyzed using descriptive statistics and repeated measures analysis of variance (ANOVA).
Results:
The cohort comprised 45 ALL, 30 AML, and 10 other leukemia subtypes. At baseline, 70% had gingivitis, 30% periodontitis. Scaling/root planing was most common. At one year, PD (3.2 mm to 2.5 mm, P < 0.001) and BOP (60% to 25%, P < 0.001) significantly decreased. Improvements were maintained at three years (PD 2.2 mm, P < 0.01 vs 1 year) and five years. HSCT patients showed similar improvements. No significant differences existed between leukemia subtypes. One patient experienced minor gingival recession post-surgery.
Conclusions:
Even after chemotherapy or HSCT, periodontal interventions sustain long-term periodontal health in children with leukemia. The importance of maintaining, as well as comprehensive oral health care and periodontal therapy stares at us from the five-year follow-up data. These results also illustrate the scant literature available on the long-term periodontal effects on these patients, pertaining to integrated dental practices. Further longitudinal research is warranted to confirm these results and identify additional risk factors.
Pharmacy and materia medica, Analytical chemistry
Historical Highlights of Ozone Therapy
Satya Lakshmi Komarraju, D. Sathyanath, Mandala Sathwik
et al.
Ozone therapy evolved from a chemically intriguing 18th-century observation to an increasingly standardized medical modality globally. Initially recognized for its powerful antimicrobial function, ozone was introduced into industrial water treatment and subsequently into many clinical uses, including wound healing, infections, and adjuvant cancer therapy. Early innovators Christian Friedrich Schönbein, Nikola Tesla, and Dr. Joachim Hänsler opened up the way for therapeutic applications, which led to inventions like ozone generators and autohemotherapy. Formal attempts at 20th-century development of ozone therapy as associations, academic publications, and research work followed. Major highlights include wartime application, dental and surgical procedure integration, and publication of landmark works. For the 21st century, establishment of the International Scientific Committee of Ozone Therapy (ISCO3) and the Madrid Declaration have marked progress in global standardization and ethical regulation. India’s latest steps, like including ozone therapy in the education and government-sanctioned training programs of naturopathy, are in line with its increasing legitimacy. The known antioxidant, anti-inflammatory, and immunomodulatory effects of the therapy have widened its scope in integrative and complementary medicine. A background check on ozone therapy shows a transition from experimental fringes to evidence-based, internationally used modality with sustainable use in modern healthcare.
Pharmacy and materia medica, Analytical chemistry
Effect of Polydopamine Nanoparticle-Induced Surface Modification on Demineralized Dentin for Enhanced Functional Remineralization
Manavalan Madhana Madhubala, Sekar Mahalaxmi
Background:
Development of biomimetic nanomaterials for remineralization therapy is an important strategy in minimally invasive dentistry. The size of the therapeutic agent has a great influence on bioavailability, penetration ability, and larger surface area for interaction in hard tissue remineralization through the nonclassical crystallization pathway. This study aimed to comparatively evaluate the remineralization-inducing potential of polydopamine (PDA) and polydopamine nanoparticles (nPDs) on artificially demineralized dentin.
Methodology:
nPDs were prepared using commercially procured dopamine hydrochloride by the wet precipitation method. Obtained particles were characterized using scanning electron microscopy–energy-dispersive X-ray spectroscopy (SEM-EDX), transmission electron microscopy, particle size analysis and zeta potential determination via dynamic light scattering with a laser particle analyser, X-ray diffraction, X-ray photoelectron spectroscopy, and attenuated total reflectance Fourier transform infrared spectroscopy. The cytocompatibility of nPD and PDA was assessed by (3-(4,5-dimethythiazol-2-yl) 2,5-diphenyl tetrazolium bromide) assay on human dental pulpal stem cell lines. A total of 66 demineralized dentin slabs of 3 mm × 3 mm × 1 mm dimension were immersed in 2 mg/ml of freshly prepared PDA and nPD solutions for 12 hours, followed by reimmersion in calcium and phosphate solution at 37°C days for 10 days. Samples immersed in deionized water were used as a control group. All the specimens were subjected to various remineralization testing methods using SEM-EDX, Vicker’s microhardness, and micro-Raman spectroscopic analysis. The Shapiro–Wilk test was used to assess the normality of the distribution, followed by one-way ANOVA for intergroup analysis and post hoc Tukey’s test for multiple comparisons within groups.
Results:
nPD exhibited a nanospherical morphology with positive zeta potential. nPD revealed the polymeric amorphous nature with characteristic functional groups and exhibited >80% relative cell viability. nPD promoted superior remineralization ability by the formation of hydroxyapatite closely mirroring the Ca/P ratio of natural dentin with a hardness value significantly closer to the baseline, which was further evidenced by higher-intensity peaks of phosphate, amide, and proline on micro-Raman spectroscopic analysis.
Conclusion:
Dentin remineralization is more strongly facilitated by nanometric PDA than PDA, which has an enhanced functional remineralization effect.
Pharmacy and materia medica, Analytical chemistry
Exploring molecular interactions and ADMET profiles of novel MAO-B inhibitors: toward effective therapeutic strategies for neurodegenerative disorders
Amir Raza, Jitendra Chaudhary, Azmat Ali Khan
et al.
Abstract Background Neurodegenerative disorders (NDs), primarily affecting the elderly, are marked by complex pathophysiological processes and are projected to become the second leading cause of death. Parkinson’s disease (PD), one of the most common NDs, is characterized by motor impairments due to reduced dopamine levels in the substantia nigra (SN), a crucial midbrain region involved in motor control and reward mechanisms. PD also impacts cognitive functions, potentially leading to depression and sleep disturbances. Recent research highlights the importance of MAO-B inhibitors in PD management, as these enzymes play a critical role in regulating neurotransmitter levels by catalyzing the oxidative deamination of intracellular amines and monoamine neurotransmitters. Result Computational virtual screening of several quinoline-based ligands against the target protein MAO-B (PDB ID: 1OJA) was performed using molecular docking simulation and ADMET studies to identify promising inhibitors for neurodegenerative disease treatment. The most active hit, Compound PA001, exhibited a MolDock score of − 207.76 kcal/mol. Subsequent investigation of 6-methoxy-2-(4-phenylpiperazin-1-yl)quinoline (Compound PA001) using molecular dynamics (MD) simulations with GROMACS revealed potent inhibition and significant interactions at key active site residues. MD simulations confirmed the stability of the Compound PA001-MAO-B complex under physiological conditions. Additionally, ADMET analysis demonstrated that Compound PA001 possesses favorable drug-like properties, including absorption, distribution, metabolism, excretion, and toxicity profiles. These findings underscore 6-methoxy-2-(4-phenylpiperazin-1-yl)quinoline (Compound PA001) as a promising candidate for developing new MAO-B inhibitors to treat neurodegenerative diseases. Conclusion The research highlighted 6-methoxy-2-(4-phenylpiperazin-1-yl)quinoline (Compound PA001) as a promising MAO-B inhibitor, exhibiting strong binding affinity, stability, and desirable drug-like characteristics for the treatment of neurodegenerative diseases. Among the top ten molecules, Compound PA001 was selected for molecular dynamics (MD) simulation using GROMACS. The compound showed potent inhibition, significant interactions with key active site residues, and stable complex formation under physiological conditions. ADMET analysis further confirmed its favorable pharmacokinetic profile.
Therapeutics. Pharmacology, Pharmacy and materia medica
Non-Invasive Drug Delivery across the Blood–Brain Barrier: A Prospective Analysis
Sarfaraz K. Niazi
Non-invasive drug delivery across the blood–brain barrier (BBB) represents a significant advancement in treating neurological diseases. The BBB is a tightly packed layer of endothelial cells that shields the brain from harmful substances in the blood, allowing necessary nutrients to pass through. It is a highly selective barrier, which poses a challenge to delivering therapeutic agents into the brain. Several non-invasive procedures and devices have been developed or are currently being investigated to enhance drug delivery across the BBB. This paper presents a review and a prospective analysis of the art and science that address pharmacology, technology, delivery systems, regulatory approval, ethical concerns, and future possibilities.
Pharmacy and materia medica
Novel Fusidic Acid Cream Containing Metal Ions and Natural Products against Multidrug-Resistant Bacteria
Hani Naseef, Yousef Sahoury, Mohammad Farraj
et al.
Background: Drug design and development to overcome antimicrobial resistance continues to be an area of research due to the evolution of microbial resistance mechanisms and the necessity for new treatments. Natural products have been used since the dawn of medicine to heal skin infections. The antimicrobial properties of fusidic acid, zinc sulfate, and copper sulfate have been studied and are well known. Furthermore, these compounds have different mechanisms of action in targeting microorganisms, either by inhibiting protein synthesis or bacterial cell walls. Therefore, their combination is expected to have synergistic activity in killing bacteria. However, the synergistic antimicrobial activity has not been evaluated in a cream formulation. Therefore, the objectives of this in vitro study were to develop and evaluate the synergistic efficacy of fusidic acid in combinations with natural products, including oleuropein, thyme oil, zinc sulfate, and copper sulfate, as a cream to eradicate fusidic-acid-resistant microorganisms in skin infections. Methods: Three different cream formulations were developed, compared, and labeled F1, F2, and F3. The compounds were studied for their antibacterial activity. In addition, the stability of the cream was investigated at 25 °C and 40 °C in plastic jars over three months. Results: The F2 formula has adequate physicochemical properties. Furthermore, it displays stable and better results than the marketed trade product and has potential inhibition zones (ZOI). Interestingly, considerable numbers (9.5%) of fusidic-acid-resistant Staphylococcus aureus (FRSA) isolates possessed a high resistance pattern with MIC ≥ 128 μg/mL. In contrast, most tested FRSA isolates (90.5%) had a low resistance pattern with MIC ≤ 8 μg/mL. Conclusion: In conclusion, the F2 cream made with fusidic acid, oleuropein, thyme oil, zinc sulfate, and copper sulfate in the right amounts has stable physical and chemical properties and has potential against FRSA as an antimicrobial agent.
Pharmacy and materia medica
Study of Antibodies to Influenza Neuraminidase N2
Yulia Desheva, Nadezhda Petkova, Tatiana Smolonogina
et al.
Humoral immunity to influenza neuraminidase (NA) was evaluated among different groups of people including patients with acute influenza infection and healthy people in different age groups using an enzyme linked lectin assay (ELLA). The amino acid composition of NA of seasonal influenza viruses A/Victoria/361/2011(H3N2) and A/Hong Kong/4801/2014(H3N2) differed by 2%, while cross-reacting neuraminidase-inhibiting (NI) antibodies to them in the same serum samples were detected in 10% of cases. Middle-aged patients born from 1977 to 2000 had a high level of hemagglutination-inhibiting (HI) antibodies to A/Hong Kong/4801/2014(H3N2), but almost no NI antibodies, which may indicate that in the case of a change in the hemagglutinin (HA) subtype, this age group will be susceptible to influenza A/H3N2 viruses. Therefore, it could mean there is a need for priority vaccination of this age group with a vaccine against the appropriate strain. It was shown that after intranasal administration of live influenza vaccine (LAIV) for the 2017–2018 season, serum antibody response was not lower compared to that during natural infection. In older people, antibodies to archival A/H2N2 viruses were detected more often than to modern A/H3N2. Since the conversion of antibodies to HA and NA often did not coincide, antibodies to NA can serve as an additional criterion for assessing the immunogenicity of influenza vaccines.
Medicine, Pharmacy and materia medica
Uncovering the biodiversity and biosynthetic potentials of rare actinomycetes
Chijioke E. Ezeobiora, Nwamaka H. Igbokwe, Dina H. Amin
et al.
Abstract Background Antibiotic resistance is on the rise, and new antibiotic research has slowed in recent years, necessitating the discovery of possibly novel microbial resources capable of producing bioactive compounds. Microbial infections are gaining resistance to existing antibiotics, emphasizing the need for novel medicinal molecules to be discovered as soon as possible. Because the possibilities of isolating undiscovered actinomycetes strains have decreased, the quest for novel products has shifted to rare actinomycetes genera from regular environments or the identification of new species identified in unusual habitats. Main body of the abstract The non-streptomyces actinobacteria are known as rare actinomycetes that are extremely difficult to cultivate. Rare actinomycetes are known to produce a variety of secondary metabolites with varying medicinal value. In this review, we reported the diversity of rare actinomycetes in several habitat including soil, plants, aquatic environment, caves, insects and extreme environments. We also reported some isolation methods to easily recover rare Actinobacteria from various sources guided with some procedures to identify the rare Actinobacteria isolates. Finally, we reported the biosynthetic potential of rare actinomycetes and its role in the production of unique secondary metabolites that could be used in medicine, agriculture, and industry. These microbial resources will be of interest to humanity, as antibiotics, insecticides, anticancer, antioxidants, to mention but a few. Short conclusion Rare actinomycetes are increasingly being investigated for new medicinal compounds that could help to address existing human health challenges such as newly emerging infectious illnesses, antibiotic resistance, and metabolic disorders. The bioactive secondary metabolites from uncommon actinomycetes are the subject of this review, which focuses on their diversity in different habitats, isolation, identification and biosynthetic potentials.
Therapeutics. Pharmacology, Pharmacy and materia medica
QbD Consideration for Developing a Double-Layered Tablet into a Single-Layered Tablet with Telmisartan and Amlodipine
Joo-Eun Kim, Young-Joon Park
The aim of this study was to develop a single-layered version of commercially available Twynstar<sup>®</sup> (Telmisartan + Amlodipine) double-layered tablets to improve the dosing convenience. A quality-by-design approach was applied to develop the single-layered version. To evaluate the range and cause of risks for a single-layered tablet in the formulation design research, we used the tools of the risk assessment, initial risk assessment of preliminary hazard analysis and main risk assessment of failure mode and effect analysis to determine the parameters affecting formulation, drug dissolution, and impurities. The critical material attributes were the stabilizer and disintegrant, and the critical process parameters were the wet granulation and tableting process. The optimal range of the design space was determined using the central composite design in the wet granulation and tablet compression processes. The stabilizer, kneading time, and disintegrant of the wet granulation were identified as X values affecting Y values. The compression force and turret speed in the tablet compression were identified as X values affecting Y values. After deciding on the design space with the deduced Y values, the single-layered tablets were formulated, and their dissolution patterns were compared with that of the double-layered tablet. The selected quality-by-design (QbD) approach single-layered tablet formulated using design space were found to be bioequivalent to the Twynstar<sup>®</sup> double-layered tablets. Hence, the development of single-layered tablets with two API using the QbD approach could improve the medication compliance of patients and could be used as a platform to overcome time-consuming and excessive costs and the technical and commercial limitations related to various multi-layered tablets.
Pharmacy and materia medica
Impacto econômico como resultado da atuação de uma comissão de farmácia e terapêutica: a experiência do Mato Grosso
Helder Cássio de Oliveira, Kelli Carneiro de Freitas Nakata, Luisa Daige Marques
Objetivo: Demonstrar o impacto econômico, sob a perspectiva da Secretaria Estadual da Saúde de Mato Grosso, das atividades desenvolvidas por uma Comissão Permanente de Farmácia e Terapêutica (CPFT-MT) com atuação transparente e fundamentada na avaliação de tecnologias em saúde. Métodos: Avaliou- -se o comportamento dos gastos com medicamentos não constantes nas listas de medicamentos essenciais do Sistema Único de Saúde durante e após a vigência de uma via administrativa planejada para dar acesso a população a esse tipo de medicamentos. Foram levantados os gastos com desembolsos diretos para aquisição de medicamentos destinados a atender a Portaria Estadual nº 172/2010 e ações judiciais com auxílio do Sistema Integrado de Planejamento, Contabilidade e Finanças (FIPLAN). Com a finalidade de trazer os valores gastos para os dias atuais, aplicou-se um ajuste inflacionário com base no Índice Nacional de Preços ao Consumidor Amplo (IPCA). Resultados: Os achados apontaram para gastos médios anuais expressivos e constantes com medicamentos não selecionados durante a vigência da via administrativa com consequente redução de gastos com ações judiciais a partir de sua revogação. Período este coincidente com a entrega de diversos trabalhos da CPFT-MT, especialmente a lista estadual de medicamentos e construção e atualização de protocolos clínicos estaduais, resultando em uma economia para o estado de R$ 6.222.196,90 (53,1%). Conclusão: Os resultados apontam para que uma comissão de farmácia e terapêutica capacitada e atuante, com apoio da gestão, pode contribuir para uma melhor utilização dos recursos financeiros e cooperar com uso racional de tecnologias em saúde.
Pharmacy and materia medica, Pharmaceutical industry
Lithium salts of Krebs cycle substrates as potential normothymic antioxidant agents
Evgenii Plotnikov, Elena Korotkova, Olesya Voronova
Objective: Aim of the present work was to study the antioxidant properties of lithium salts of Krebs cycle substrates and their influence on immune cells. Lithium is a well-known and widely used mood stabilizer. These lithium-based substances have a lot of potential properties because of the anionic component of the Krebs cycle substrates, which take part in basic intracellular biochemical process. Materials and Methods: Lithium salts of fumarate, pyruvate, malate, succinate, and citrate (as reference drug) were investigated in this study as antioxidants and immunomodulators. The antioxidant properties were studied by the voltammetry method, which evaluates oxygen radical scavenging capacity of lithium substances. Influence of the lithium compounds on the immune cells of human blood was indicated by the reaction of blast transformation of lymphocytes. Results: All tested substances and their mixes possessed antioxidant properties, more expressed in maximal therapeutic concentration. Lithium compounds showed no toxic influence on human blood immune cells and caused no significant changes in both spontaneous and stimulated proliferation. Conclusion: The results allow considering lithium salts of Krebs cycle substrates as potential normothymic agents (mood stabilizer) with antioxidant properties and low toxicity.
Pharmacy and materia medica, Analytical chemistry
A Case of Gorhams Syndrome: An anesthetic challenge
Supriya Lynette Dsouza, Adarsh Kulkarni, Hashim Sageer
et al.
Anesthesiology, Pharmacy and materia medica
Synergistic Effect of Potassium Clavulanate in Combination withCefamandol and Ceftazidime on ï¢- Lactamase, Extracted From Resistant E.coli
Siham S. Shaokat, Hamoudi A. Hameed
The aim of this study was to evaluate in-vitro activity of Cefamandol and Ceftazidime, in combination with potassium clavulanate against 10 uropathogenic E.coli isolated from patients with chronic complicated urinary tract infections (UTIs), these isolates were identified by the Api identification systems.The antimicrobial susceptibility tests were determined by Kirby-Bauer method and the minimum inhibitory concentrations of Cefamandol and Ceftazidime, were determined, by tube method. These isolates were resistant to Ampicillin (Amp), Amoxicillin (Amo), Carbenicillin (Cb), Ticarcillin (Tic), Amoxicillin\ Potassium Clavulanate {Augmentin}, (Amo\CA), Ticarcillin\ Potassium Clavulanate {Timentin} (Tic\CA), Cefamandol (Cfm) and Ceftazidime (Cfz), also resistant to other antibiotics, such as Tetracycline, Chloramphenicol, Trimethoprim and (50% of the isolates were resistant to Nalidixic acid and Rifampicin). Transfer of plasmids by direct conjugation experiments were performed by mating 10 strains with recipient strain E.coliK12C 600 Rif or Nal resistant, and cell free b- lactamases were prepared and detected by macro-iodometric method. The activities of each cell free b– lactamases extract against Cfm and Cfz were determined by disks diffusion method (microbiological Masuda method) and by macro-iodometric method. The activity of b- lactamases was inhibited by the addition of Potassium Clavulanate. Conclusion:
Good effectiveness of Cfm\ CA and Cfz\ CA was obtained against resistant strains of E.coli due to complicated urinary tract infection (UTIs).
Key words: b- lactamases, Cefamandol, Ceftazidime, Timentin and Augmentin .
Pharmacy and materia medica
Utilização de planejamento fatorial para a determinação da capacidade antioxidante e doseamento de flavonoides totais em Verbena minutiflora Briq. ex Moldenke (gervai)
K.E. PELOI, F. BOVO, I.J. MESSIAS-REASON
et al.
RESUMO Verbena minutiflora Briq. ex Moldenke (gervai) tem seu uso medicinal relatado popularmente para tratamento de doenças hepáticas, diarreia e outros problemas de saúde. Entretanto, pouco se conhece a respeito de seus componentes químicos e estudos que comprovem suas propriedades medicinais são escassos. O objetivo desse estudo foi avaliar a composição química dos extratos aquosos e etanólicos de flores de V. minutiflora e otimizar processos de obtenção de extratos com maiores capacidades antioxidantes e maiores concentrações de flavonoides. O método de extração foi desenhado por planejamento fatorial, onde as variáveis para a determinação da capacidade antioxidante foram: pH, extração líquida, método e tempo de extração. Para a determinação de flavonoides totais as variáveis avaliadas por planejamento fatorial foram: concentração de hexametilenotetramina, tipo de ácido, volume de ácido e tempo de aquecimento. Os resultados das análises químicas dos extratos mostraram: aminogrupos, taninos e ácidos fixos (extrato aquoso) aminogrupos, flavonoides, triterpenos, esteroides, alcaloides e cumarinas (extrado hidroetanólico). Os resultados dos planejamentos fatoriais mostraram que o melhor método de extração para a capacidade antioxidante foi o que usou vórtex, por 35 min, com água:etanol 50:50, com pH1, obtendo 0,1899± 5,8.10-3 mmol expressos em ácido ascórbico g-1 nos extratos de V. minutiflora. Enquanto, para as dosagens de flavonoides totais as variáveis significantes foram: tipo de ácido e volume de ácido. A melhor extração obtida foi: 6,748. 10-2± 2,085 10-3% expressos em quercetina. Os resultados mostraram que o planejamento fatorial é uma importante ferramenta para a otimização de extração de componentes químicos em produtos naturais.
Pharmacy and materia medica, Botany
Análise de prescrições médicas para tratamento de câncer de mama em um hospital universitário do estado de São Paulo
Luís Felipe Beloni Bózoli, Camila Milani Ribeiro, Polyana Lara de Mello Zoccal
et al.
Este artigo centra-se na análise de prescrições médicas para o tratamento de câncer de mama em pacientes em seguimento em um hospital universitário do estado de São Paulo, Foram analisadas 408 prescrições médicas entre setembro e dezembro de 2012, sendo 201 na Central de Quimioterapia e 207 na Farmácia de Quimioterapia Ambulatorial deste hospital de ensino, Os principais resultados foram: (a) das 201 prescrições analisadas na Central de Quimioterapia, apenas 123 (61,2%) apresentaram o peso, 89 (44,3%) a altura e 113 (56,2%) a superfície corpórea do paciente, (b) 100% das prescrições na Central e 48,3% na Farmácia de Quimioterapia apresentaram abreviaturas, (c) o nome comercial dos medicamentos esteve presente em 54,7% das prescrições na Central de Quimioterapia, (d) altos índices de ausência de informação quanto à forma farmacêutica do medicamento, (e) 05 (1,2%) prescrições com nome ilegível do paciente e 04 (1%) prescrições com nome ilegível do medicamento, A análise dos dados mostra a ausência da informação completa necessária para o uso seguro dos medicamentos antineoplásicos, evidenciando o não cumprimento da legislação vigente, Assim, destaca-se a necessidade de constante treinamento dos prescritores relacionado à importância de uma prescrição médica correta, contendo todas as informações de forma clara, como também maior participação do farmacêutico clínico e sugere-se, ainda, a implantação da prescrição médica eletrônica, Essas ações podem melhorar a qualidade das prescrições e promover o uso seguro e racional de medicamentos.
Pharmaceutical industry, Pharmacy and materia medica
Development of a Survey to Assess the Acceptability of an Innovative Contraception Practice among Rural Pharmacists
Michael Wong, Judith A. Soon, Peter J. Zed
et al.
Improved access to effective contraceptive methods is needed in Canada, particularly in rural areas, where unintended pregnancy rates are high and specific sexual health services may be further away. A rural pharmacist may be the most accessible health care professional. Pharmacy practice increasingly incorporates cognitive services. In Canada many provinces allow pharmacists to independently prescribe for some indications, but not for hormonal contraception. To assess the acceptability for the implementation of this innovative practice in Canada, we developed and piloted a survey instrument. We chose questions to address the components for adoption and change described in Rogers’ “diffusion of innovations” theory. The proposed instrument was iteratively reviewed by 12 experts, then focus group tested among eight pharmacists or students to improve the instrument for face validity, readability, consistency and relevancy to community pharmacists in the Canadian context. We then pilot tested the survey among urban and rural pharmacies. 4% of urban and 35% of rural pharmacies returned pilot surveys. Internal consistency on repeated re-phrased questions was high (Cronbach’s Alpha = 0.901). We present our process for the development of a survey instrument to assess the acceptability and feasibility among Canadian community pharmacists for the innovative practice of the independent prescribing of hormonal contraception.
Pharmacy and materia medica
Improving access to health commodities by strengthening the supply chain Management workforce: the case of Namibia
Erin Hasselberg, Lazarus Indongo, Tonata Ngulu
et al.
Therapeutics. Pharmacology, Pharmacy and materia medica
Study on the Treatment of Rheumatoid Arthritis with Xinfeng Capsule based on the Xin'an Medical Theory
L. Jia