Active Pharmacological Ingredients Research Articles

Advancements and Challenges of Nanostructured Lipid Carriers for Wound Healing Applications.

The current treatments for wound healing still exhibit drawbacks due to limited availability at the action sites, susceptibility to degradation, and immediate drug release, all of which are detrimental in chronic conditions. Nano-modification strategies, offering various advantages that can enhance the physicochemical properties of drugs, have been employed in efforts to maximize the efficacy of wound healing medications. Nowadays, nanostructured lipid carriers (NLCs) provide drug delivery capabilities that can safeguard active compounds from environmental influences and enable controlled release profiles. Consequently, NLCs are considered an alternative therapy to address the challenges encountered in wound treatment. This review delves into the application of NLCs in drug delivery for wound healing, encompassing discussions on their composition, preparation methods, and their impact on treatment effectiveness. The modification of drugs into the NLC model can be facilitated using relatively straightforward technologies such as pressure-based processes, emulsification techniques, solvent utilization methods, or phase inversion. Moreover, NLC production with minimal material compositions can accommodate both single and combination drug delivery. Through in vitro, in vivo, and clinical studies, it has been substantiated that NLCs can enhance the therapeutic potential of various drug types in wound healing treatments. NLCs enhance efficacy by reducing the active substance particle size, increasing solubility and bioavailability, and prolonging drug release, ensuring sustained dosage at the wound site for chronic wounds. In summary, NLCs represent an effective nanocarrier system for optimizing the bioavailability of active pharmacological ingredients in the context of wound healing.

Magnetic materials as adsorbents for the pre-concentration and separation of active ingredients from herbal medicine.

Herbal medicine (HM) is crucial in disease management and contains complex compounds with few active pharmacological ingredients, presenting challenges in quality control of raw materials and formulations. Effective separation, identification, and analysis of active components are vital for HM efficacy. Traditional methods like liquid-liquid extraction and solid-phase extraction are time-consuming and environmentally concerning, with limitations such as sorbent issues, pressure, and clogging. Magnetic solid-phase extraction uses magnetic sorbents for targeted analyte separation and enrichment, offering rapid, pressure-free separation. However, inorganic magnetic particles' aggregation and oxidation, as well as lack of selectivity, have led to the use of various coatings and modifications to enhance specificity and selectivity for complex herbal samples. This review delves into magnetic composites in HM pretreatment, specifically focusing on encapsulated or modified magnetic nanoparticles and materials like silica, ionic liquids, graphene family derivatives, carbon nanotubes, metal-organic frameworks, covalent organic frameworks, and molecularly imprinted polymers.

AN ANALYSIS OF ANTIMICROBIAL AND ANTIDIABETIC FIXED DOSE COMBINATIONS BANNED IN INDIA

Objective: National regulatory authority reviewed various fixed-dose combinations (FDCs) in view of doubtful rationality status and subsequently 349 FDCs were banned in 2018. This study was conducted to analyze the antimicrobial and antidiabetic FDCs banned by the Central Drugs Standard Control Organization in India. Methods: Data were collected from the report of drugs technical advisory board subcommittee. Banned antimicrobial and antidiabetic FDCs were assessed for the following parameters – number of active pharmacological ingredients, routes of administration and dosage forms, indications for marketing, reasons for banning, and pharmacological group of FDCs. Results: Seventy antimicrobial and 25 antidiabetic FDCs were analyzed. These FDCs contained 2–7 drugs, available mostly as tablets (51.42%, 100%) in antimicrobial and antidiabetic groups, respectively. Antimicrobial FDCs were marketed most for respiratory tract infections and infection and inflammatory conditions of the skin (17, 24.28% each) while antidiabetic FDCs were marketed for Type 2 diabetes mellitus (14, 56%). The reasons for ban were pharmacodynamic (68.57%, 16%) and pharmacokinetic (20%, 40%) mismatches, lack of evidence of efficacy (7.14%, 36%), and safety concerns (4.28%, 8%) in antimicrobial and antidiabetic groups, respectively. In antimicrobial FDCs, the most common combination was that of an antibacterial with other miscellaneous drugs (like zinc, Vitamin E, serratiopeptidase, etc.) (19, 27.14%) whereas antidiabetic FDCs most commonly had biguanide with thiazolidinedione and sulfonylurea (7, 28%). Conclusion: There is a need for scrutiny of other FDCs in larger interests of patient care and prescribers should be made aware about recently banned FDCs to promote rational pharmacotherapy.

Muscone restores anoikis sensitivity in TMZ-resistant glioblastoma cells by suppressing TOP2A via the EGFR/Integrin β1/FAK signaling pathway

BackgroundTemozolomide (TMZ) resistance is the main obstacle faced by glioblastoma multiforme (GBM) treatment. Muscone, one of the primary active pharmacological ingredients of Shexiang (Moschus), can cross the blood-brain barrier (BBB) and is being investigated as an antineoplastic medication. However, muscone treatment for GBM has received little research, and its possible mechanisms are still unclear. PurposeThis study aims to evaluate the effect and the potential molecular mechanism of muscone on TMZ-resistant GBM cells. MethodsThe differentially expressed genes (DEGs) between TMZ-resistant GBM cells and TMZ-sensitive GBM cells were screened using GEO2R. By progressively raising the TMZ concentration, a relatively stable TMZ-resistant human GBM cell line was established. The drug-resistance traits of U251-TR cells were assessed via the CCK-8 assay and Western Blot analysis of MGMT and TOP2A expression. Cell viability, cell proliferation, cell migration ability, and drug synergism were detected by the CCK-8 assay, colony formation assay, wound healing assay, and drug interaction relationship test, respectively. Anoikis was quantified by Calcein-AM/EthD-1 staining, MTT assay, and flow cytometry. Measurements of cell cycle arrest, apoptosis, mitochondrial membrane potential (MMP), and reactive oxygen species (ROS) were performed using cell cycle staining, Annexin V-FITC/PI labeling, JC-1 assay, and ROS assay, respectively. DNA damage was measured by TUNEL assay, alkaline comet assay, and γ-H2AX foci assay. GEPIA was used to investigate the link between the anoikis marker (FAK)/drug resistance gene and critical proteins in the EGFR/Integrin β1 signaling pathway. Molecular docking was used to anticipate the probable targets of muscone. The intracellular co-localization and expression of EGFR and FAK were shown using immunofluorescence. The U251-TR cell line stably overexpressing EGFR was constructed using lentiviral transduction to assess the involvement of EGFR-related signaling in anoikis resistance. Western Blot was employed to detect the expression of migration-related proteins, cyclins, anoikis-related proteins, DNA damage/repair-related proteins, and associated pathway proteins. ResultsDEGs analysis identified 97 deregulated chemotherapy-resistant genes and 3779 upregulated genes in TMZ-resistant GBM cells. Subsequent experiments verified TMZ resistance and the hyper-expression of DNA repair-related genes (TOP2A and MGMT) in continuously low-dose TMZ-induced U251-TR cells. Muscone exhibited dose-dependent inhibition of U251-TR cell migration and proliferation, and its co-administration with TMZ showed the potential for enhanced therapeutic efficacy. By downregulating FAK, muscone reduced anoikis resistance in anchorage-independent U251-TR cells. It also caused cell cycle arrest in the G2/M phase by upregulating p21 and downregulating CDK1, CDK2, and Cyclin E1. Muscone-induced anoikis was accompanied by mitochondrial membrane potential collapse, ROS production, an increase in the BAX/Bcl-2 ratio, as well as elevated levels of Cytochrome c (Cyt c), cleaved caspase-9, and cleaved caspase-3. These findings indicated that muscone might trigger mitochondrial-dependent anoikis via ROS generation. Moreover, significant DNA damage, DNA double-strand breaks (DSBs), the formation of γ-H2AX foci, and a reduction in TOP2A expression are also associated with muscone-induced anoikis. Overexpression of EGFR in U251-TR cells boosted the expression of Integrin β1, FAK, β-Catenin, and TOP2A, whereas muscone suppressed the expression levels of EGFR, Integrin β1, β-Catenin, FAK, and TOP2A. Muscone may influence the expression of the key DNA repair enzyme, TOP2A, by suppressing the EGFR/Integrin β1/FAK pathway. ConclusionWe first demonstrated that muscone suppressed TOP2A expression through the EGFR/Integrin β1/FAK pathway, hence restoring anoikis sensitivity in TMZ-resistant GBM cells. These data suggest that muscone may be a promising co-therapeutic agent for enhancing GBM treatment, particularly in cases of TMZ-resistant GBM with elevated TOP2A expression.

Review on Herbal Excipients

The fact that herbal or natural excipients are non-toxic, inexpensive, and readily available gives them a significant advantage over their synthetic analogues. The pharmaceutical industries are becoming more inclined toward using these herbal excipients, which are mainly polymers of natural origin, in formulation development as awareness of these excipients grows. The plant-derived gums and mucilages from natural sources, such as tragacanth, carrageenan, thaumatin, lard, storax, and agar, meet many of the specifications for pharmaceutical excipients. These can be chosen over their synthetic counterparts for formulation development since they are more stable and come with less regulatory concerns. They are a powerful and affordable method of administering active pharmacological ingredients because they can be easily changed to match the demands of each individual patient. In view of their biocompatibility and capacity to provide additional nutrition to the established dosage form, natural excipients have the potential to be utilised as diluents, binder, disintegrants, and lubricants in a variety of formulations.

Phytochemical Screening of Ginger (Zingiber officinale), a Medicinal Plant

Ginger has potent values as a medicinal plant which originated from China and India. Currently there is a renewed interest in ginger because of its various active pharmacological ingredients including gingerols, beta-carotene, capsaicin, caffeic acid, curcumin, and salicylate making it a potential source of research to use as a drug. The present study was aimed at extraction of ginger root extract in acetone and methanol solvents by Soxhlet extraction method, screening of phytochemical constituents of ginger extract in acetone and methanol and evaluation of its antimicrobial activity against known pathogenic microorganism. The qualitative analysis of phytochemicals revealed the presence of saponins, alkaloids, flavonoids, and steroids in the extracts of ginger. Results of antimicrobial activity showed that ginger in acetone was having highest activity against Escherichia coli MTCC 334 with 24 mm of clear zone and lowest activity with ginger in methanol against Bacillus subtilis MTCC 441 with 10 mm of clear zone.

Encapsulating melittin from animal venom by finely tuned charge compensation with polymer carriers

Due to their wide availability, polypeptide/protein venoms produced by certain insects are of high interest as potential active pharmacological ingredients; however, the number of clinical studies on these venoms remains poor. In this paper, we describe an extremely efficient platform to form polyplexes from cationic amphiphilic animal venoms, such as the hemolytic poison melittin. The idea is based on supramolecular melittin cationic charge compensation with nanoparticles (micelles composed of hydrophobic glassy polystyrene core and hydrophilic poly(meth)acrylic acid corona, PMA and PAA acid homopolymers) with high anion charge density at physiological pH. An instant “mix and go” process and efficient melittin complexation with nanoparticles at concentrations down to micrograms per milliliter of PBS solution was achieved and proven by inhibition of melittin-induced hemolysis. We studied in detail how the structural features of the nanoparticles influence their potency; we found that the most important parameter is the number of carboxylates in the polyanion chain (proportional to the molecular weight and length of the anionic poly(meth)acrylic acid block). The poly(meth)acrylic acid-based polymer nanoparticles may be useful as melittin (and possibly other cationic amphiphilic animal venoms) antidotes but also as models for constructing future delivery systems to apply the venoms therapeutically.

Mechanism Research and Application for Ginsenosides in the Treatment of Hepatocellular Carcinoma.

Ginsenosides, the main active pharmacological ingredients of ginseng, have been widely used for the treatment of numerous carcinomas. Hepatocellular carcinoma (HCC) is 3rd leading malignant tumor in terms of mortality worldwide. Accumulating evidence indicates that ginsenosides play a vital role in the prevention and treatment of HCC. Ginsenosides can significantly improve the symptoms of HCC, and their anticancer activity is mainly involved in inhibiting proliferation and migration, inducing cell cycle arrest at the G0/G1 phase, promoting caspase-3 and 8-mediated apoptosis, regulating autophagy related to Atg5, Atg7, Atg12, LC3-II, and PI3K/Akt pathways, and lowering invasion and metastasis associated with decreased nuclear translocation of NF-κB p65 and MMP-2/9, increasing IL-2 and IFN-γ levels to enhance immune function, as well as regulating the gut-liver axis. In addition, ginsenosides can be used as an adjuvant to conventional cancer therapies, enhancing sensitivity to chemotherapy drugs, and improving efficacy and/or reducing adverse reactions through synergistic effects. Therefore, the current manuscript discusses the mechanism and application of ginsenosides in HCC. It is hoped to provide theoretical basis for the treatment of HCC with ginsenosides.

Evaluation of rationality of fixed dose combinations of antimicrobials available in Indian market

Background: The antimicrobial resistance is alarming at present. One of the important factors for resistance is use of irrational fixed dose combinations. Thus, objective was to critically analyze the rationality of FDCs of antimicrobial agents currently available in India.Methods: The FDCs of AMAs enlisted in Indian Drug Review 2019 were analyzed by 8 point criteria tool. Analysis includes number of active pharmacological ingredients, approval by central drug standard control organization, listing in world health organization model list of essential medicines (2019) or Government of India national list of essential medicines (2015). Literature search was used for assessing efficacy, safety, pharmacokinetic and pharmacodynamic interactions and advantages of each FDC. Each criterion was assigned score one, if positive and minus one, if negative leading to total score of 12. FDC with score of ≥7 was considered as rational. Results: The FDCs of AMA available in Indian market were 116 while FDCs included in WHO model list, 2019 were 24. Majority of FDCs available were irrational that include combination of antibacterial with bromhexine, carbocisteine, ambroxol, serratiopeptidase, antiamoebic and antifungal etc. Most of the rational FDCs belong to antiretroviral, antitubercular and antimalarial drugs. Conclusions: Most of the FDCs of AMAs available in Indian market are irrational. These needs educating the prescribers including resident doctors. There is need to critically review such FDCs by drug regulators with strict action regarding manufacturing and marketing.

AN ANALYSIS OF BANNED FIXED-DOSE COMBINATIONS IN INDIA

Objective: The objective of the study was to analyze the nonsteroidal anti-inflammatory drugs (NSAIDs) and respiratory fixed-dose combinations (FDCs) recently banned in India.
 Methods: This observational study was conducted at the Department of Pharmacology, B. J. Medical College, Ahmedabad, Gujarat. The data were collected from the report on the banned FDCs submitted by the drug technical advisory board subcommittee. Total 195 FDCs belonging to NSAIDs (33) and respiratory group (162) were assessed for class, number of active pharmacological ingredients, formulations, indications, and reasons for banning.
 Results: The mean number of drugs in FDCs of NSAIDs was 2.6, while in respiratory FDCs, it was 3.6. The most common NSAID formulation was uncoated tablet (15, 30%) while it was syrup in respiratory (49, 30%). The most common reasons for banning these FDCs were safety concerns (153, 78.4%), followed by mismatched pharmacodynamics in respiratory FDCs and mismatched pharmacokinetics in NSAIDs FDCs. The NSAIDs FDCs were marketed for pain (70%) while respiratory FDCs were marketed for cough and cold (62%). Most common NSAIDs FDCs contained NSAID with NSAID (18%), while in respiratory FDCs combinations of a cough suppressant, expectorant, and soothing agents (10%) were present.
 Conclusion: Evaluation of FDCs is essential to prevent the marketing of irrational FDCs.

Rationality of Fixed Dose Combinations of Central Nervous System Drugs in a Tertiary Care Hospital

Objectives: To analyze the rationality of central nervous system fixed dose combinations used in a tertiary care hospital. Methodology: The study was an hospital based observational study. The data was collected from an annual drug compendium entitled “Hospital Drug List”. Fixed dose combinations (FDCs) enlisted in central nervous system (CNS) sections were selected for the study purpose. The active pharmacological ingredients (APIs) in FDC was checked for approval by Drug Control General of India (DCGI), World Health Organization (WHO) and essential medicine (EML)/national essential medicine list (NEML),both or none and all the ingredients (molecule, excipients) present in the FDC was checked whether banned or under any controversies in India as well as worldwide. Efficacy and safety of the individual active pharmacological ingredients (APIs) and their combination were searched. Details of each drug were collected [Generic name, Pharmacokinetics, Interaction affected, Pharmacodynamics, and Advantages of FDCs]. The data collected was analyzed by a tool to assess the rationality of fixed dose combinations which is pre-tested and validated by Shah et al., based on WHO guidelines. Result and Discussion: A total of 25 CNS FDCs were taken, on assessment of CNS FDCs 21 (84%) were found to be rational and 4 (16%) were found to be irrational with the mean rationality score of 7.2. By winding up, state of nonbeing, absenteeism of legality and effectiveness of the formulations appeared in to a peculiar combinations and inadequate practice. The approval process of these combinations by various committees should be robust. Keywords: Rationality; Fixed Dose Combinations; CNS Drugs; Safety and Efficacy.

Development of the UHPLC-DAD method for simultaneous determination of four active pharmacological ingredients in cannabinoid plant material

Development of the UHPLC-DAD method for simultaneous determination of four active pharmacological ingredients in cannabinoid plant material

Searching for synergistic calcium antagonists and novel therapeutic regimens for coronary heart disease therapy from a Traditional Chinese Medicine, Suxiao Jiuxin Pill

Coronary heart disease is a vital cause of morbidity and mortality worldwide, and calcium channel blockers (CCBs) are important drugs that can be used to treat cardiovascular diseases. Suxiao Jiuxin Pill (SX), a traditional Chinese medicine, is widely used as an emergency drug for coronary heart disease therapy. However, understanding its potential mechanism in intracellular calcium concentration ([Ca2+]i) modulation remains a challenge. To identify the active pharmacological ingredients (APIs) and reveal a novel combination therapy for ameliorating cardiovascular diseases, the ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF MS) combined with a dual-luciferase reporter [Ca2+]i assay system was applied. Ligustrazine, ferulic acid, senkyunolide I, senkyunolide A and ligustilide were identified as potential calcium antagonists in SX, and the combination of ligustrazine and senkyunolide A showed synergetic calcium antagonistic activity. Additionally, the synergetic mechanism was further investigated by live-imaging analysis with the Ca2+ indicator fluo-4/AM by monitoring fluorescence changes. Our results indicated that ligustrazine can block voltage-operated Ca2+ channels (VDCCs) effectively and senkyunolide A can exert an inhibition effect mostly on ryanodine receptors (RYRs) and partly on VDCCs. Finally, an arterial ring assay showed that the combination of ligustrazine and senkyunolide A exerted a better vasodilatation function than using any components alone. In this study, we first revealed that a pair of natural APIs in combination acting on VDCCs and RYRs was more effective on vasodilatation by regulating [Ca2+]i.

Nanoemulsions and dermatological diseases: contributions and therapeutic advances.

Skin disease is one of the most common human diseases and affects between 30% and 70% of individuals, which requires a lot of attention to their treatments. The delivery of active pharmacological ingredients at the topical level is a challenge because of the difficulties in overcoming the mechanical barrier created by the skin and reaching greater depths, since delivery specificities are decisive for the degree of effectiveness. In this way, the nanoemulsions emerge as a potential system for the incorporation of active substances in the cells and for the controlled release of active principles. The present article intends to review the main treatments for which the nanoemulsions were used in the field of dermatology. In addition, it discusses the results and advantages over the other dermatological therapies that are being used. The results showed that the particle size in nanoemulsions increased the contact surface area, resulting in increased drug efficacy, even in comparison with other existing pharmaceutical formulations. In conclusion, it has been shown that nanoemulsions have a better performance in efficacy, safety, permeability profile, and bioavailability compared with other formulations studied.

Pharmaceutical development of complex wound-healing ointment for the needs of military medicine

This article presents experimentally proved scientific-practical methods of developing modern vulnerary medical preparations in the form of an ointment with antibacterial, anti-inflammatory and anesthetic properties for the purposes of military medicine. In pursuit of the designated goals, the authors used modern methods of research: pharmacological-technological, physical-chemical, structural-mechanical and biological methods – for proving the compound of the combined ointment including ofloxacin, nimesulide and lidocaine. On the basis of the research conducted, we proved the content and rational technique of the complex antimicrobial ointment with anti-inflammatory and anesthetic effect using ofloxacin (0.05 g), nimesulide (1.0 g) and lidocaine (4.0 g). We experimentally established the optimal content of the main component of the ointment: emulsive base of mixture of Polyethylene Oxide-400 and Polyethylene Oxide-1500 (1 : 4) and a complex of emulsifiers of the first and the second generations – cetostearylic alcohol – 3%, monoglyceryl stearate – 5% at the constant concentration of paraffin oil – 20%, which involves a certain temperature regime during preparation, a sequence of introducing active pharmacological ingredients and adjuvants to the water and oil phases, frequency and duration of mixing. Physical-chemical tests of the ointment base determined the optimum concentration of glycerine as 5%, which encourages elimination of purulent discharge from damaged tissues, causing an anti-inflammatory effect and providing a prolonged, but milder dehydrating effect. The relation between physical-chemical, rheological, biopharmaceutical properties of the developed preparation and the concentration and method of introduction of the active pharmaceutical ingredients was theoretically and experimentally proven. We conducted pre-clinical studies (in vivo) for defining the therapeutic efficiency of the ofloxacin-nimesulide composition in the compound of the developed ointment for complex treatment of the wound process. We studied the specific activity (anti-alternative – model of standard tissue wounds in rats), which allowed us to establish the optimum concentration of nimesulide, which is 1%. Biopharmaceutical studies (in vitro method) determined the optimum method of introducing ofloxacin, nimesulide and lidocaine in the ointment base as a solution in dimethyl sulfoxide. To select an anesthetic substance for the ointment, the authors conducted a comparative study on the anesthetic effect of the anesthetics most widely available in Ukraine: novocaine, dicainum, lidocaine, trimecainum and pyromecainum. The research conducted on the time it took for the anesthetic effect to occur and on the duration and extent of the effect enabled us to select a 4% concentration of lidocaine anesthetic for the preparation. The choice of the temperature regime for the ointment’s preparation was proved. The in vitro method and rheological studies determined that the optimum temperature regime for the technological process of preparing the ointment on the emulsive base is 25–30 ºС. The development and introduction of the new combined ointment on a contemporary hydrophilic ointment base into practical pharmacy would lead to an enlargement in the nomenclature of the medical preparations used for local treatment of the purulent – necrotic phase of the wound process, which is relevant for pharmaceutical technology and global medical science and practice.

Mahuannin B an adenylate cyclase inhibitor attenuates hyperhidrosis via suppressing β2-adrenoceptor/cAMP signaling pathway

BackgroundBased on the traditional application of traditional Chinese Medicines (TCMs), Ephedra Herba (EH) is used to cure cold fever by inducing sweating, whereas Ephedra Radix (ER) is used to treat hyperhidrosis. Although they come from the same plant, Ephedra sinica Stapf, but have play opposing roles in clinical applications. EH is known to contain ephedrine alkaloids, which is the driver of the physiological changes in sweating, heart rate and blood pressure. However, the active pharmacological ingredients (APIs) of ER and the mechanisms by which it restricts sweating remain unknown. PurposeThe current work aims to discover the hidroschesis APIs from ER, as well as to establish its action mechanism. MethodsUPLC-Q/TOF-MS, PCA, and heat map were utilized for identifying the differences between EH and ER. HPLC integrated with a β2-adrenoceptor (β2-AR) activity luciferase reporter assay system was used to screen active inhibitors; molecular docking and a series of biological assays centered on β2-AR-related signaling pathways were evaluated to understand the roles of APIs. ResultsThe opposite effect on sweating of EH and ER can be attributed to the APIs of amphetamine-type alkaloids and flavonoid derivatives. Mahuannin B is an effective anti-hydrotic agent, inhibiting the production of cAMP via suppression of adenylate cyclase (AC) activity. ConclusionThe effects of EH and ER on sweat and β2-AR-related signaling pathway are opposite due to different alkaloids and flavonoids of APIs in EH and ER. The present work not only sheds light on the hidroschesis action of mahuannin B, but also presents a potential target of AC in the treatment of hyperhidrosis.

Vocational training of dentistry students regarding knowledge of oral rinses with antiseptic

<p><strong>Objetivo</strong>: o uso indiscriminado dos enxaguatórios bucais com antissépticos por parte da população pode trazer riscos à saúde, uma vez que os princípios ativos e os demais componentes dessas formulações não são inócuos. Nessa perspectiva é essencial que se tenha o controle da formação profissional desde o ingresso dos estudantes nas universidades até a diplomação. O objetivo desse estudo foi avaliar o grau de conhecimento adquirido pelos acadêmicos de Odontologia formandos em 2014 sobre os enxaguatórios bucais com antissépticos, ao longo da formação universitária em 3 instituições públicas e 3 privadas. <strong>Metodologia</strong>: aplicação de um instrumento investigativo destinado à coleta de informações prestadas por estudantes concluintes em 2014 de seis cursos de Odontologia no estado da Bahia. <strong>Resultados</strong>: 56% dos acadêmicos procedentes de instituições privadas declaram ter estudado os enxaguatórios durante a graduação, enquanto que 67% com origem em instituições públicas se manifestaram contrariamente. Os entrevistados fizeram referência a um elenco variado de disciplinas que tratam deste tema. 53,1% dos concluintes das instituições públicas e 46,9% das privadas declararam fazer uso de enxaguatórios, sendo similares os percentuais de uso diário e o registro da preferência pelo Colgate (50,7%), Oral B (26,4%) e Listerine (16,4%). Com relação ao conhecimento sobre os princípios ativos, destaca-se 81% de respostas em branco, apesar do relativo conhecimento sobre os diluentes. <strong>Conclusão</strong>: muito embora o ensino do tema enxaguatório tenha sido considerado, o grau de conhecimento dos acadêmicos não é satisfatório, haja vista o elevado percentual de respostas em branco a respeito dos princípios ativos e suas indicações clínicas.</p>

An evaluation of knowledge, attitude and practices about prescribing fixed dose combinations among postgraduates of a rural tertiary health care teaching hospital

Background: Fixed dose combinations (FDCs) is a combination product of two or more active pharmacological ingredients (APIs) in a single dosage form. There is lot of debate over rationality and irrationality of FDCs presently. This study was focused on medical postgraduates to evaluate their knowledge, attitude and practices about prescribing fixed dose combinations as they are the physicians who are future practitioners and it is up to them to misuse it or use it judiciously by prescribing rationally. The objective of the study was to evaluate knowledge, attitude and practices about prescribing fixed dose combinations among postgraduate medical students. Methods: A cross-sectional questionnaire based study was conducted among postgraduate medical students of AIMS, B G Nagar, Nagamangala, Mandya, Karnataka, India. Results: Total respondents were 124. 81 participants (65.32%) were males and 43 participants (34.67%) were females. 73.38% of participants were aware of the term FDCs. Improvement in patient’s compliance (68.54%) and improved efficacy of individual drugs (62.09%) were the advantages of using FDCs and irrational prescription of FDCs leading to drug resistance (70.96%) and difficulty in dose adjustments of individual drugs (54.83%) were the disadvantages mentioned. Knowledge of banned FDCs was lacking. More than half (58%) of them were not able to mention a single banned FDC in India. Medical representatives (45.16%), Internet (27.41%), textbooks (15.32%) were the most common sources of information of FDCs. Amoxicillin with clavulanic acid was the most common prescribed FDC (60.2%). Conclusions: Majority of the postgraduates have the knowledge about general aspects of FDCs, their advantages and disadvantages. However, knowledge about rational or irrational drugs, banned FDCs and availability of essential list is lacking. It is required that the concepts of rational drug use should be implemented in undergraduate curriculum vigorously and to strengthen their knowledge and skills to prescribe rationally.

Critical Analysis of Cardiovascular and Central Nervous System Fixed Dose Combinations Available in Indian Market.

Fixed Dose Combinations (FDCs) are being increasingly used to improve compliance and achieve greater benefits of the two or more active ingredients given together than the corresponding individual drug components given separately. To analyse the rationality of Cardiovascular (CV) and Central Nervous System (CNS) FDCs available in Indian market. CVS and CNS FDCs, enlisted in Indian Drug Review, 2014, were analysed by a pretested validated eight point criteria tool. Each FDC was assessed for number of active pharmacological ingredients, approval by regulatory authority, listing in WHO Essential Medicine List. While efficacy, safety, pharmacokinetic, pharmacodynamic interactions and advantages of each FDC were analysed by literature search. The total score of the tool was 12 and score ≥7 was considered rational. FDCs were divided in four groups as per rationality and DCGI approval. ANOVA was used for statistical analysis and p<0.05 was considering statistically significant. Out of 152 FDCs, 107 were CV and 45 belonged to CNS group and 40 had documented evidence of efficacy and safety. Majority of FDCs showed advantage of being convenient by reducing pill count and only 32 showed reducing adverse drug reactions. Out of 107 CV FDCs, 46 were rational and 61 were irrational with a mean rationality score of 6.72±2.82 (CI- 95 %, 3.90 - 9.54). While out of 45 CNS FDCs, 8 were rational and 37 were irrational with a mean rationality score of 6.22±2.08 (CI - 95 %, 4.14 - 8.30). A significant difference in mean rationality score of group A (DCGI approved + rational) was observed as compared to group B (DCGI approved + irrational) and group C (DCGI unapproved + rational) as compared to group D (DCGI unapproved + irrational) (p<0.05). The absence of watertight pre-requisite, critical analysis of the scientific validity of the formulations and 'convenience' category has resulted into proliferation of irrational FDCs. This calls for strict regulatory approval process to avoid miserable FDC scenario in the country.

Critical analysis of antimicrobial and respiratory fixed dose combinations available in Indian market

Objective: To analyze the rationality of antimicrobial (AM) and respiratory (RP) fixed dose combinations (FDCs) available in Indian market. Materials and Methods: Antimicrobial and RP FDCs enlisted in Indian Drug Review 2010 and 2013 respectively were analyzed by a pretested validated 8 point criteria tool. Each FDC was assessed for number of active pharmacological ingredients, approval by regulatory authority, listing in World Health Organization (WHO) essential medicine list (EML) or National List of Essential Medicine. While efficacy, safety, pharmacokinetic and pharmacodynamic interactions and advantages of each FDC were analyzed by evidence based literature search. Each criterion was scored one for positive and minus one for negative or unfavorable observation. The total score for the tool was 12 and score ≥7 was considered rational. Results: Of 209 FDCs, 108 were AMs and 101 were RPs. The mean rationality score was 5.41 ± 1.63 (95% CI, 2.15-8.67). Majority of FDCs were irrational (174) while 35 were rational, and only 12 of these were listed in WHO EML 2013. Out of 108 AM FDCs, 21 (19%) were rational while 87 (81%) were irrational. Out of 101 RP FDCs, 14 (14%) were rational while 87 (86%) were irrational and 24 (24%) with unfavorable pharmacodynamic interactions. Majority of the rational AM FDCs were antiretroviral (6) agents while RP FDCs were indicated for chronic obstructive pulmonary diseases. While majority of irrational FDCs were AM plus steroids, β 2 agonists plus antihistaminics/expectorants/anticholinergics/mast cell stabilizers/leukotriene receptor antagonists. Conclusion: Rationality assessment of AM and RP FDCs reveals that a substantial number of these FDCs in Indian market are irrational. This calls for a close scrutiny of marketed FDCs and educating prescribers to use them with great care and caution. This also indicates a serious review of the regulatory framework for drug manufacturing and marketing.