PT. ETFLIN Scientific Society (Sciences of Phytochemistry)
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Quality and Potency of Government-subsidized Antibiotics in Hospitals Across Jakarta, Indonesia
Full text linkSeveral pharmaceutical companies have long complained that the price of medicines that win the e-catalogue tender is too low, in some cases even below the cost of production. However, it should not be a concern that only pharmaceutical products with regulation of Indonesian food and drug (BPOM) distribution licenses are eligible for the price tender, as they are of good quality. This study aims to determine the quality and potency of three antibiotic drugs based on their highest utilization (DU 90%) in pneumonia patients at two hospitals, A (ceftriaxone, azithromycin tablet) and B (ceftriaxone, levofloxacin infusion) compared to brand name. The quality of the samples was evaluated following the Indonesian Pharmacopoeia 6th Edition (FI-VI). Antibiotic potency was assessed using the Plate-Cylinder Method with K. pneumonia from human and S. pneumonia ATCC 10015 as the test bacteria evaluated following CLSI. All samples meet the criteria of FI-VI antibiotic content, weight uniformity, dissolution. Antibiotic potency all samples test S.pneumonia and K.pneumonia were sensitive but ceftriaxone test with K.pneumonia was resistance. All antibiotic tablets and injections studied met the requirements of the Indonesian Pharmacopoeia Edition 6 for active medicinal ingredient content, dosage weight uniformity, and dissolution. All drugs from hospitals (INN) have lower antibiotic potency than branded drugs. This highlight the importance of conducting microbiological testing on antibiotic preparations
Phytoconstituents and In Vitro Free Radical Scavenging Potential of n-Hexane and Aqueous Fractions of Cucurbita maxima and Leptadenia hastata
Full text linkThe present study explored the phytoconstituents and radical scavenging activity of the respective n-hexane and aqueous fractions of Cucurbita maxima (CMHF and CMAF) and Leptadenia hastata (LHHF and LHAF) for potential application in oxidative stress-related ailments. The phytoconstituents were qualitatively determined and characterized using Fourier-transform Infrared (FTIR), while the antioxidant activity was determined in vitro. Alkaloids were present in only the aqueous fractions of C. maxima and L. hastata, while saponins, steroids, and flavonoids were detected in all the fractions. The FTIR revealed the presence of functional groups, including alcohols, sulfonates, alkenes, alkanes, amines, and aromatics in both plant fractions. The LHHF (35.53 ±2.11 ascorbic acid (AA) equivalent µg/mL) exhibited a significantly (p<0.05) higher total reducing power (TRP) than all the other fractions. The CMHF (69.11 ±2.56 AAE µg/mL) demonstrated a significantly (p<0.05) higher total antioxidant capacity (TAC) than all the other fractions. For the ferric thiocyanate (FTC) assay, the highest inhibition was exhibited by LHHF (79.78 ± 3.24%), significantly (p<0.05) higher than AA (26.46 ± 2.12%), CMHF (69.77 ± 3.16%), and CMAF (43.80 ± 2.12%). In the thiobarbituric acid assay, the lowest MDA concentration was exhibited by the CMHF (0.07 ±0.01 nmol/mL), significantly (p<0.05) lower than all the other fractions and ascorbic acid. Conclusively, the n-hexane fraction of both plants presents potential sources of novel antioxidant compounds with significant free radical scavenging and anti-lipid peroxidation activities, applicable in ailments linked to oxidative stress
Druggability of Pharmaceutical Compounds Using Lipinski Rules with Machine Learning
Full text linkIn the field of pharmaceutical research, identifying promising pharmaceutical compounds is a critical challenge. The observance of Lipinski's Rule of Five (RO5) is a fundamental criterion, but evaluating many compounds manually requires significant resources and time. However, the integration of computational techniques in drug discovery in its early stages has significantly transformed the pharmaceutical industry, enabling further efficient screening and selection of possible drug candidates. Therefore, this study explores RO5 using algorithms of Machine Learning (ML), offering a comprehensive method to predict the druggability of pharmaceutical compounds. The study developed, evaluated, and validated the performance metrics of multiple supervised machine learning models. The best model was used to build an application that can predict and classify potential drug candidates. The findings revealed promising capabilities across all models for drug classification. Among all the explored models, Random Forest (RF), Extreme Gradient Boost (XGBoost), and Decision Tree (DT) classifiers demonstrated exceptional performance, achieving near-perfect accuracy of 99.94%, 99.81% and 99.87% respectively. This highlights the robustness of ensemble learning methods in classifying compounds based on RO5 adherence. The comparative analysis of these models underscores the importance of considering balanced accuracy, precision, F1-score, recall, and Receiver Operating Characteristics-Area Under the Curve (ROC-AUC) score, interpretability, and computational efficiency when choosing between ML algorithms in drug discovery. The DrugCheckMaster application was subsequently developed using the most predictive model and is now available on Render (https://capstone-project-dc7w.onrender.com/)
Toxicity and Safety Analysis of Polyhexamethylene Guanidine: A Comprehensive Systematic Review
Full text linkPolyhexamethylene guanidine (PHMG) is a commonly used disinfectant, but safety concerns have arisen due to poisoning cases. This systematic review assesses the toxicity and safety of PHMG by inhalation, oral administration, skin contact, and ocular contact to determine its potential medical applications and acceptable concentration limits. Searches in PubMed, ScienceDirect, CENTRAL, and CyberLeninka up to January 2024 identified 11 in vitro studies with human cell lines, 28 animal studies, and 10 articles involving patients and healthy volunteers. The review found that inhalation of PHMG leads to pulmonary fibrosis and malignant neoplasms, making aerosol forms unacceptable. PHMG can also affect liver function and have adverse effects on the heart, kidneys, and hematopoietic system. For dermal use, PHMG appears to be safe at concentrations up to 3%, although practical use may limit this to 1% due to potential discomfort. Still, it is important to consider possible sensitization, especially in patients with pre-existing skin conditions. In oral hygiene, 1% PHMG-P has been used safely in periodontal treatment, suggesting its potential in dentistry. For ophthalmic use, concentrations should be carefully monitored. PHMG-P solutions below 0.13% appear to be safe for human corneal epithelium, however lower concentrations still pose a risk of corneal fibrosis, as shown in animal studies. Physicians should prefer lower concentrations and consider alternatives or formulations with reduced toxicity for sensitive applications such as eye drops. Overall, although PHMG and its derivatives show promise in a variety of medical applications, their use should be reasonable, with careful consideration of the associated risks
Effect of Combination of Porang and Moringa Flour on Blood Glucose Levels and Body Weight in Rats
Full text linkPorang tuber is rich in fiber and low in calories of carbohydrates. Moringa oleifera leaf has a high protein and a low content of lipids. Obesity and diabetes mellitus are the risk factors of cardiovascular disease, also known as cardiovascular disease risk factors. Combining of porang and moringa as feed can increase nutrition without causing weight gain. This study aims to determine these two materials as antidiabetic and antiobesity agents. The samples are porang tuber, a combination of porang tuber and M. oleifera leaves, a combination of M. oleifera leaves and wheat flour, wheat flour, and standard feed of mice. The parameters tested in this study are analysis of macronutrients of feed, loss of weight of mice, average consuming feed in 28 days, and reduction of blood glucose with a glucometer. The results obtained are a combination of porang tuber and moringa had a low contain carbohydrates and a high contain lipids and protein, can reduction in body weight of 21%, the lowest consumption of feed, and the lowest fasting and postprandial blood glucose levels compared to the other feeds. A combination of porang and moringa can be an antidiabetic and antiobesity agent
Sterility of Ophthalmic Solutions as a Factor in the Evolution of Primary Packaging for Eye Drops: A Literature Review
Full text linkPreservatives in eye drops, while not always necessary, can lead to undesirable effects. Developing preservative-free solutions demands special measures for sterility, utilizing multidose or monodose primary packaging. This review explores the merits and drawbacks of these packaging types. A literature search on PubMed, Google Scholar, and EMBASE until December 2023, using MESH terms, yielded 28 studies on multidose ampoules and 24 on monodose packaging. Heterogeneous data revealed advantages and disadvantages concerning patient use and manufacturing. Chronologically presenting the development of eye drop packaging, this study finds Droptainer® simple but unable to maintain sterility. Comod®, 3K®, ABAK®, Novelia®, and Ophthalmic Squeeze Dispenser show high sterility probability, with Comod® and ABAK® having a contamination risk. Novelia® excels with long-term sterility and better control. Ophthalmic Squeeze Dispenser, FDA-approved, boasts a smaller carbon footprint. Unit-dose systems preserve sterility and offer design flexibility. Proposing an alternative, blister technology maintains sterility, is convenient and safe, and holds promise for recycling. This comprehensive assessment aids in understanding the evolving landscape of eye drop packaging, emphasizing the importance of sterility, convenience, and environmental impact
Phytochemical Analysis, In-vitro, and In-silico Antibacterial Activity of Stembark Extract of Anogeissus leiocarpus (DC) Guill and Perr
Full text linkBacterial infections subsequently leading to antibiotic resistance has been a leading cause of mortality and morbidity worldwide especially in developing countries with high poverty rate and poor healthcare system. Thus, prompting the prospect in alternative therapy such as medicinal plants. In the present study, we evaluated the antibacterial action of stem bark extract of Anogeissus leiocarpus (AL) Guill and Perr. as applied in folkloric medicine for antibacterial purposes. The phytochemicals present in the plant extract were identified and quantified, followed by the determination of the antibacterial effects of the extract against Escherichia coli and Staphylococcus aureus. Molecular docking study was carried out to ascertain the inhibitory effects of compounds from AL against bacterial enzymes. Alkaloids (7.17% ±0.60), saponins (11.33% ±3.18), and flavonoids (31.01% ±4.04) were detected. A maximum ZI was observed for E. coli compared to S. aureus at the highest extract concentration (100 mg/mL) with amoxicillin having superior ZI at 50 mg/mL concentration. The MIC against E. coli and S. aureus were 12.5 mg/mL and ≤ 6.25 mg/mL respectively while the MBC was>100 mg/mL and 100 mg/mL respectively. Among the identified compounds, IX exhibited the least binding affinity (BA) (7.2 kcal/mol) and inhibition constant (Ki) (5 µM) against UDP-N-acetylglucosamine Enolpyruvyl Transferase (Mur A) compared to all the other targets. AL demonstrated antibacterial activity evidenced by the bacterial growth inhibition, bactericidal potential, and in-silico study revealing high affinity of the bacterial enzymes for the identified compounds, thereby supporting the acclaimed antibacterial use of the plant in folkloric medicine
Central and Peripheral Analgesic Activities of Aqueous Extract of Centella Asiatica (AECA) Leaves in Rats and Mice
Full text linkThe demand of herbal based medicines are increasing all over the world and the focus on plant research has increased. Centella asiatica (CA) is a medicinal herb used in traditional medicine as remedy for a variety of diseases. It is widely used in Ayurvedic medicines. The present study evaluated the Analgesic Activity of Aqueous Extract of the leaves of Centella asiatica (AECA). Acute oral toxicity test was performed according to Organization for Economic Cooperation and Development, 2008 (OECD) guidelines. The tail flick method and glacial acetic acid-induced writhing tests were used to study the central and peripheral analgesic activities of AECA, respectively. AECA (200mg/kg) produced significant analgesia in both central and peripheral mechanisms compared to the control. The maximal analgesic effect was observed after 90 minutes of drug administration in the tail-flick method. In the glacial acetic acid-induced writhing test, AECA (200 mg/kg, p.o) produced a significant decrease (71.07%) in the number of writhes (p<0.01) when compared to the control. Therefore, CA can be a very promising herbal-based medicine for treatment of various painful conditions. Further investigations are needed to determine the precise mechanism and site of action of AECA
Novasome: Combining Ufasome and Niosome for Excellent Vesicular Drug Delivery System
Full text linkNovasome technology is a novel encapsulation-based drug delivery method that is more effective and efficient than standard liposome systems. It is composed of a mixture of surfactant, cholesterol, and free fatty acids, which produce superior vesicle characteristics for drug delivery. Various studies have investigated the optimal combination of surfactant type, free fatty acid type, and their ratio, as well as the formulation factors that can significantly affect the vesicle characteristics. The novasome technology has demonstrated its potential for delivering a range of substances, including terconazole, fenticonazole, zolmitriptan, and vaccines. Novasomes can be produced using various methods, such as the thin film hydration (TFH) method, injection method, and vortex method combined with a suitable size reduction method. Future research can focus on exploring the potential of novasome technology for delivering a wider range of drugs and vaccines and developing more efficient and effective methods for producing novasome vesicles
Comparison of Microsampling and Conventional Sampling Techniques for Quantification of Warfarin in Blood Samples: A Systematic Review
Full text linkWarfarin is a vitamin K antagonist (VKAs) anticoagulant associated with interindividual patients’ response to therapy, narrow therapeutic index, and serious adverse drug events. Monitoring ensures efficacy and safety by measuring drug concentration in the bloodstream, which demands blood or plasma samples from patients through conventional sampling. Conventional sampling often requires invasive methods that may be uncomfortable for patients. Microsampling offers an opportunity to reduce the burden of multiple blood sampling on patients and simplifies the process of sample transportation and storage. This systematic review describes conventional and microsampling techniques for quantifying warfarin in human blood samples and the bioanalytical method employed to perform the analysis. Related studies (537) were screened from several databases and narrowed down into 12 eligible articles, which were then used to fulfill the purpose of this review in a narrative form. It is concluded that while there are still limited studies regarding the application of microsampling for warfarin quantification in patients, there has been evidence of comparable plasma and micro samples results, highlighting the potential for future development of routine monitoring using the microsampling technique