Indonesian Journal of Pharmacy
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The Characterization of Fructose-Based High-Fat Diet and Low-Dose Streptozotocin in A Type 2 Diabetes Mellitus Rat Model
Get PDFAnimal models with valuable information on biochemical profiles are essential for preclinical trials of new antidiabetic agents. This study was to optimize and characterize of high-fat, high-fructose diet (HFFD) and low-dose streptozotocin (STZ) induced type 2 diabetes mellitus (type 2 DM). Wistar rats were fed with HFFD for 2, 4, and 6 weeks, followed by STZ (35 mg/kg BW), thus measuring the biochemical parameters. Non-induction HFFD and STZ were used as a normal control group. HFFD and low-dose STZ-induced rats demonstrated an elevation in the body weight, fasting blood glucose, triglyceride, triglyceride/ glucose index, necrosis score, and the insulin-negative cells. Moreover, this induction also reduced the number of insulin-positive cells and the percentage of insulin-positive cells. The findings imply that feeding Wistar rat HFFD for two weeks, followed by a single dose of STZ at 35 mg/kg BW will result in a reliable and stable diabetic rat model that closely resembles the biochemical characteristics of type 2 DM
Attenuation of TNF-α and Iron Levels in Renal Hemosiderosis by Phaleria macrocarpa (Scheff.) Boerl Extract in a Rat Iron Overload Model
Get PDFRegular blood transfusions are typically used to treat the genetic anemia known as thalassemia, which can lead to an increase in the body's total iron levels. The condition of excess iron can be toxic to the body due to the formation of free radicals that are harmful and can damage cells and tissues. So the availability of free iron will form the basis of iron toxicity because it accelerates the Fenton reaction to produce an increase in the amount of ROS that cannot be suppressed so that saturation of the antioxidant system can occur. Excess iron has been known to be a risk factor for organ dysfunction and damage that results in various organ diseases such as liver, heart and kidney, diabetes mellitus, and neurodegenerative diseases. Mangiferin is an active compound has been shown to act as an iron chelating agent by forming complexes with iron. The complex formed can reduce iron accumulation in thalassemia patients who receive blood transfusions on a regular basis. Mahkota Dewa (Phaleria macrocarpa) is a well-known medicinal plant native to Papua, Indonesia, and it also includes the active ingredient mangiferin. This study aims to determine the effectiveness of the ethanolic extract of Phaleria macrocarpa fruit as an iron chelating agent observed in the kidneys in a rat model of excess iro
LC-HRMS Metabolite Profiling of Lunasia amara Stem Bark and In Silico Study in Breast Cancer Receptors
Get PDFL. amara is a medicinal plant used as an aphrodisiac. Several studies show it has a compound with biological activities such as inhibition of cell proliferation, one of the mechanisms leading to anticancer activities. This study aimed to profile the metabolites and predict activity against two breast cancer receptors (ERα (3ERT) and HER2 (3PPO)) with an in silico approach. Metabolite profiling of water and 80% ethanol extract was analyzed by UHPLC-Q-Orbitrap-HRMS. Also, we performed a radical scavenging activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH). Putative identification of metabolite in L. amara showed the 46 metabolites (4 unknown) were identified and predominantly as quinoline alkaloids. Some of the compounds from glycosides and phenol groups were also identified. From the antioxidant capacity test results, the 80% ethanol extract had a higher radical scavenging capacity than the aqueous extract. Based on the molecular docking results, the highest affinity for the ERα receptor was found in the tested compound tetrahydropapaveroline and exceeded the native 4-OHT ligand. For the HER2 receptor, graveolinine has the highest affinity but is still below the native lapatinib ligand. Ligand interactions with the amino acids Leu 387 and Glu 419 on the active site of the ERα receptor and Phe1004 on the HER2 receptor are thought to play an important role in increasing the energy affinity. Overall, all compounds showed higher affinity for HER2 receptors than ERα. Alkaloids demonstrated anticancer activity. Further research should be conducted to determine the in vitro activity of these compounds on breast cancer cells
Apium graveolens Herbs Ethanolic-Extract Improve Acetic Acid–Induced Colitis Condition in Rats
Get PDFColitis is a growing gastrointestinal inflammation condition that affect individual all around the globe. No specific treatment for colitis condition is available at the moment and this disease can develop into colorectal cancer. Phytochemical in Apium graveolens (AG) are potential as anti-inflammation and antioxidant. This study aimed to investigate the potency of AG ethanolic-extract (EES) in improving acetic acid (AA) – induced colitis in rats.
Rats with colitis induced by acetic acid were treated with 5-ASA and several concentrations (100, 300, and 900 mg/kg) of EES. Colitis severity was determined by scoring of macroscopic condition including body weight, colon, and faeces condition. In addition, colon tissues conditions were observed with haematoxylin-eosin staining. Colon permeability is determined by measuring urine glucose level. The observation of the change in Enterobacteriaceae population is investigated using PCR.
Apium graveolens ethanolic-extract shows highest improvement of colitis condition at concentration of 900 mg/kg, based on macroscopic observation and disease severity index. At this dose, no blood existed on the faeces and the faeces consistency is solid. Group receiving lower dose of EES still shows blood existence and less solid faeces. The EES dose dependently return the population of Enterobacteriaceae which increase upon AA treatment. Apium graveolens is potential to be use as preventive or treatment for colitis
Simultaneous Quantification of Ramipril and Ramiprilat in Drug Formulations: A Clinical LC-MS/MS Study
Get PDFRamipril is a drug controlling hypertension. Two drugs were studied in 36 healthy adults. The drugs are the test (Atb®) and the reference (Tritace®). This concept is crucial in the pharmaceutical industry during the development process. The maximum concentration (Cmax) of Ramipril and its metabolite (Ramiprilat) were determined throughout drug administration in healthy subjects. All analysis was performed using LC-MS/MS. The method was validated over a range of 0.200 – 25.000 ng/mL in which linearity (R2) was 0.9983, accuracy was 99.9%, precision (CV) was less than 20%, and the Lower Limit of Quantitation was 0.200 ng/mL. Stability and other parameters were discussed. The time needed to reach this concentration (Tmax) and the time-drug concentration area under the curve (AUC) were most agreed upon. The two drugs were proven to be interchangeable. Both have similar pharmacokinetics and bioequivalence profiles. Consequently, the drugs are bioequivalent and considered alternatives to one another pharmaceutically. For example, 90% confidence intervals (C.I.) for the in-tra-individual ratios (test/reference) for pharmacokinetic parameters were Cmax, and AUC0-t for total exposure C.I. Log – transformed Values were 80-125 %
Comparative Cellular and In Vivo Anti-cancer studies of Doxorubicin Liposomes Prepared with Different Types of Phospholipids
Get PDFThe selection of lipid components of membrane bilayer determines the rigidity of liposomes affecting drug efficacy, especially for cancer drug delivery. The present study evaluated liposomes with different rigidity for delivering doxorubicin (DOX). In this work, liposomes composed of rigid lipid, hydrogenated soybean phosphatidylcholine (HSPC), were totally or partially substituted with 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) or 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE). The liposomes are composed of phosphatidylcholine (HSPC, POPC), with and without combination with DOPE, cholesterol, and DSPE-mPEG2000 with a molar ratio of 57: 38: 5, respectively. Liposomes were prepared using a thin layer hydration method. Then, in vitro cytotoxicity and in vivo antitumor activity of these liposomes were evaluated. Substitution of HSPC with POPC resulted in similar cytotoxicities profiles similar to the DOX solution on C26 colon cancer cells and LLC cells. The DOPE addition to DOX liposomes reduced the antitumor activity. In conclusion, the lipid substitution of HSPC with POPC or DOPE reduced liposome rigidity; however, it lowered the in vivo antitumor activity
Clinical Decision Support Systems to Identify Drug-Related Problems in Diabetes Mellitus Patients: A Systematic Review
Get PDFClinical Decision Support Systems (CDSSs) has been developed for utilization to provide rational therapy to Diabetes Mellitus (DM) patients including preventing Drug-related Problems (DRPs) such as the effect of drug treatment being not optimal, untreated indications and symptoms, unnecessary therapy, and adverse drug reactions. This study aims to summarize the available evidence on the intervention of CDSSs, key outputs, and impact of the user in DM patients. This study was a systematic review using PubMed, Scopus database, and by manually searching the bibliographies of articles that have been found. We included studies reporting on evaluated CDSSs that had been implemented in medication prescription, reducing medication errors, adverse drug events, drug-allergy checking, drug dosing support, and so on. A total of 8 studies were selected among 855 studies. CDSSs are used in hospitals and primary care settings to identify potential drug interactions, correct therapy regimens, monitor therapy, blood glucose documentation, ensure patients receive medication according to the guideline, provide nutritional advice, and schedule physical activity. The usage of CDSSs improves blood glucose levels, detects possible drug interactions, reduces face-to-face consultations, improves documentation, assists in identifying dose, and promotes prescribing in line with the guideline. The use of CDSSs can help to reduce the risk of errors in management therapy
Zinc Sulfate and α-tocopherol Supplementation Enhance Reproductive Performance in Male Albino Rats (Rattus norvegicus) With Lead Acetate Toxicity
Get PDFMetal toxicity from lead affects reproductive organ function by activating reactive oxygen species processes. This study aims to see how α-tocopherol and zinc sulfate (ZnSO4) affect gonads, liver, follicle-stimulating hormone, luteinizing hormone, spermatogenesis (the amount of spermatogonia, spermatocytes, and spermatids), and Leydig cells in male albino rats (Rattus norvegicus) exposed to lead acetate Pb(CH3COO)2. The samples used were 25 male Wistar rats aged 4 months, separated into five groups. For 30 days, all treatment groups were exposed to Pb(CH3COO)2 at a level of 50-mg/kg body weight (BW). The T1 group was given a dosage of 100-mg/kg BW of α-tocopherol. The ZnSO4 was given to the T2 group at a dose of 0.54-mg/kg BW. Meanwhile, the T3 group was given a mixture of ZnSO4 at 0.54-mg/kg BW and α-tocopherol at 100-mg/kg BW orally. ELISA test was carried out to determine the level of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in a blood plasma sample of 100 μl / 1 mg. Histopathological observations made on the liver included counting damaged cells and seminiferous tubules that included counting the amount of spermatogonia, spermatocytes, spermatids, Sertoli cells, and Leydig cells. Using SPSS 20 software, the collected data were analyzed using analysis of variance, followed by Duncan’s test with a 95% simultaneous confidence level. The highest average levels of FSH and LH in the T3 group were 3.6162 mIU/mL and 14.9658 mIU/mL. The finding showed that Pb(CH3COO)2 caused disruptions in the spermatogenesis and Leydig cell processes. Exogenous antioxidants in combination with ZnSO4 and α-tocopherol had significant effect on enhancing reproductive performance in animals exposed to Pb(CH3COO)2
Empirical Studies Assessing the Perceptions and Knowledge of Medicine in Mongolia: A Nationwide Population-Based Study
Get PDFThe availability and affordability of medicine is an essential issue in any population globally, and drug regulatory agencies need the information to prevent an unforeseen matter and take necessary decisions by relevant agencies so that medicine will be available at an affordable price. Moreover, it is also essential to assess the consumer perception of patterns and knowledge about medicine use, subject to perception bias and belief bias. The current study examines consumers’ perceptions of medicine availability, medicine spending, affordability of medicine, patterns and knowledge of medication use. A nationwide cross-sectional study was performed in Mongolia. The survey consists of nineteen closed-ended questionnaire items. The manuscript has presented according to The Strengthening the Reporting of Observational Studies in Epidemiology (STROBE) guidelines on the cross-sectional study. A total of seven thousand five hundred and thirty-two (n=7532) had participated in the study. 46.3% of the study population consider the quality during buying of medicine. The average spending of medicine per month in Mongolia is 4.00 USD-17.00 USD/= per month. A large percentage of the population (47.8%) has skipped buying prescription drugs due to affordability issues. 47.4% of the population believe that the price of the drug sold in the market is expensive. A surprisingly 56% of study population indicate that the pharmacy does not have enough type and stock of drug. The study population (40.4%) does not have enough awareness about falsified medicine, and 30.4% cannot buy discounted medicine covered by the health insurance fund. A considerable percentage of the population (74.2%) take medicine according to doctor instructions and is firmly in favour of the government to regulate the drug prices (79.9%). The current study showed consumers’ perception, pattern, knowledge and affordability about medicines. The results indicate a lack of education by the healthcare providers on falsified medicine, the financial burden of medicine on the population, and the unavailability of different medicine stock
The Abundance of Bioactive Compounds in Fingerroot Essential Oil Before and After Self Nanoemulsifying Drug Delivery System (SNEDDS) as a Potential Substitute for Synthetic Antibiotics in Livestock
No full textThis research focuses on optimizing and stabilizing the essential oil of fingerroot (Boesenbergia rotunda), a plant native to Indonesia, using self-nanoemulsifying drug delivery system (SNEDDS) technology. This essential oil possesses antimicrobial, anti-inflammatory, and antifungal properties, making it a potential alternative to synthetic antibiotics. However, its low bioavailability and volatility limit its usage. The study involved two stages: nanoemulsion creation using a D-optimization design expert and stability analysis of bioactive compounds through gas chromatography-mass spectrometry (GC-MS). The optimized formula consisted of fingerroot essential oil, virgin coconut oil (VCO), Tween 80, and Polyethylene Glycol (PEG) 400 in percentages of 12.61, 12.61, 53.65, and 21.12%, respectively. Prior to nanoemulsion, the essential oil contained 28.28% camphor and 27.13% 1,8-cineole as the highest bioactive compounds. After applying the SNEDDS technology, the camphor content decreased to 25.17%, while the 1,8-cineole content reduced to 12.14%. These findings enhance the effectiveness and stability of fingerroot essential oil, facilitating its potential application in pharmaceutical and therapeutic fields.