Borneo Journal of Pharmacy
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Stability Evaluation on Diminazene Diaceturate and Phenazone in Bulk and Combined Formulations using Validated Chromatographic Method
No full textThe combined therapy of diminazene aceturate (DMZ) and phenazone (PHENZ) is widely used in veterinary medicine to combat trypanosomiasis and babesiosis. This study presents a novel, validated HPLC method for accurately quantifying DMZ and PHENZ in various pharmaceutical formulations, including bulk powders, sachets, vials, and injectables. The chromatographic separation was achieved using a C18 column (150 x 4.6 mm, 5 μm particle size) with a mobile phase composed of phosphate buffer (pH 3.0) and methanol (70:30 v/v) at a flow rate of 1 mL/minute. UV detection was set at 250 nm. The method demonstrated linearity over a concentration range of 20-100 μg/mL for DMZ and 25-125 μg/mL for PHENZ, with correlation coefficients exceeding 0.999. Forced degradation studies were conducted under various stress conditions to assess the method's stability-indicating power. DMZ exhibited first-order degradation under acidic pH conditions. While slight degradation (2.4-3.1%) was observed under alkaline, UV, and indoor room light conditions, PHENZ remained stable. The validated HPLC method effectively quantified DMZ and PHENZ in the presence of their degradation products and impurities, demonstrating its suitability for quality control and stability studies of these combined drug formulations
An Initial Investigation of the Potential of Robusta Coffee, Arabica Coffee, and Caffeine in Asthma Treatment through the Evaluation of 5-Lipoxygenase Inhibition Activity
No full textNumerous studies have documented the potential of coffee to aid in asthma prevention. Nevertheless, research into how coffee influences asthma management has not been available. One known mechanism by which asthma medications work involves inhibiting 5-lipoxygenase (5-LOX) activity. This study aims to determine the potency of Coffea canephora var. Robusta extract (CRE), Coffea arabica extract (CAE), and caffeine are the primary isolates against 5-LOX activity. Extraction was performed by a reflux procedure using 96% ethanol with a sample-total solvent ratio of 1 : 10, an extraction time of 1 hour, and the extraction was conducted in triplicate. Fractionation was carried out by liquid-liquid partition using a chloroform-water system. Caffeine further purification was performed by the sublimation method, and the inhibition of 5-LOX activity was evaluated using the spectrophotometric method at λ = 234 nm. Apigenin was used as a positive control. From the experiment conducted, the IC50 of the CRE, CAE, caffeine, and apigenin against 5-LOX was 32.2 ± 1.4, 42.1 ± 2.3, 14.3 ± 1.6, and 7.4 ± 1.7 µg/mL, respectively. Continued efforts to isolate bioactive compounds from coffee extract led to the discovery of caffeine, which exhibited a more potent inhibitory effect on 5-LOX. The inhibition of 5-LOX activity by caffeine occurs in a non-competitive manner
Isolation and Identification of Marine Bacteria in Raja Ampat Islands West Papua Producing Antibacterial Against Salmonella typhi and Staphylococcus aureus
No full textIndonesia's vast archipelago harbors a wealth of natural resources, including marine bacteria with potential antibacterial properties. Given the increasing prevalence of antibiotic resistance, particularly against Salmonella typhi and Staphylococcus aureus, there is a pressing need to explore alternative antimicrobial agents. This study aimed to isolate and characterize marine bacteria with antibacterial activity and evaluate their efficacy against S. typhi and S. aureus. Isolation of marine bacteria was conducted using the spread plate method. Antibacterial activity screening of the secondary metabolites was performed using the well diffusion method. Minimum inhibitory concentration (MIC) was determined using the dilution method, while minimum bactericidal concentration (MBC) was determined using the spread plate method. Seven bacterial isolates were obtained, all identified as Gram-negative bacilli. The secondary metabolites of these marine bacteria demonstrated antibacterial activity against both S. typhi and S. aureus, with inhibition zones of 8.50 mm and 8.46 mm, respectively. The MIC for both bacteria was determined to be 1500 μg/mL. Statistical analysis revealed a significant difference in antibacterial activity between the isolates (Kruskal-Wallis Test, p-value = 0.007) and between S. typhi and S. aureus (Mann-Whitney Test, p-value = 0.025). While the secondary metabolites exhibited antibacterial activity against both bacteria, they did not demonstrate bactericidal activity as measured by the MBC test
Appropriateness and Cost of Prophylaxis Stress Ulcer for Inpatient in the Internal Medicine Department in a Government Hospital: A Cross-Sectional Study
No full textGuidelines from the American Society of Health-System Pharmacists (ASHP) 1999 prohibit acid-suppressing therapy for stress ulcer prophylaxis (SUP) in patients who are not critically ill. Stress ulcer prophylaxis is not recommended in non-ICU patients with <2 risk factors. Inappropriate use of SUP can increase costs for patients. This study aims to evaluate the use and the cost of SUP. This research was a non-experimental observational study with a cross-sectional approach. Data was collected retrospectively using the consecutive sampling method with a random sampling technique on the medical records of inpatients in the internal medicine ward of Sleman Regional Public Hospital from January to December 2020, totaling 340 samples. The results showed that proton pump inhibitors were the most widely used acid-suppressing drugs, with 45.8%. Furthermore, the histamine-2 receptor antagonist was 42.6%, the sucralfate group was 7.4%, and the antacid group was 4.2%. Of 340 patients, 57 (16.8%) were in the proper indication based on the guidelines, and 283 (83.2%) were under the wrong indication for SUP. They were using SUP with the proper indication so that the therapy could save treatment costs by Rp. 19,933,582. There was a high prevalence of inappropriate SUP prescriptions among inpatients in the internal medicine department; if these drugs were given with the appropriate indications, they could save more on the prophylaxis cost. Clinician pharmacists should develop an effective intervention strategy to reduce inappropriate SUP drugs
Formulation of Nutraceutical Jelly Candy from a Combination of Cucurbita moschata Puree and Averrhoa carambola Juice as Antioxidant
No full textNutraceutical candy jellies are gaining popularity as a potential approach to deliver antioxidants in a palatable form. This study investigated the antioxidant activity of Cucurbita moschata puree combined with Averrhoa carambola juice, formulated into jelly candies. Design-Expert software V.13 was used to optimize the jelly candy base formula. The combined C. moschata puree and A. carambola juice exhibited strong antioxidant activity (IC50 = 29.580 ppm) at variation V1. The optimal base formula B3 consisted of 12% gelatin and 4% carrageenan. The formulated jelly candy possessed very strong antioxidant activity (IC50 = 44.771 ppm). These findings suggest the potential of C. moschata puree and A. carambola juice as ingredients in functional jelly candies
Total Flavonoid Levels in n-hexane and Ethyl Acetate Fractions of Rosmarinus officinalis L. Leaves and Their Antibacterial and Antioxidant Activities
No full textThe rosemary (Rosmarinus officinalis L.) is a plant of the Lamiaceae tribe that has not been widely studied regarding its pharmacological activity, known from previous studies to contain secondary metabolites of flavonoids. Flavonoids are phenol compounds with many pharmacological activities, including antibacterials and antioxidants. This study aims to determine the total flavonoid levels in R. officinalis leaves and their effect on antibacterial and antioxidant activities. This research began with the preparation of ethanol extract from R. officinalis leaves, then the fractionation of the extract produced n-hexane and ethyl acetate fractions. Total flavonoid levels were determined against both fractions by UV-Vis spectrophotometry. A test of the fraction’s antibacterial activity against Staphylococcus aureus was performed using the disc diffusion method. The antioxidant test is carried out by the DPPH method. The total flavonoid content of the ethyl acetate fraction is 47.437 ± 1.947%, higher than the n-hexane fraction. Test antibacterial and antioxidant activity showed more significant results in the ethyl acetate fraction than in the n-hexane fraction. In conclusion, the total flavonoid levels of ethyl acetate fraction are directly proportional to the antibacterial and antioxidant activities of R. officinalis leaves
Antisense Oligonucleotides: Concepts and Pharmaceutical Applications
No full textAntisense oligonucleotides are drugs whose mechanism is based on binding to RNA target sequences. For this purpose, they modify the protein expression through steric hindrance and exon omission. Its production involves several steps: synthesis, purification, and lyophilization. Usually, the most complicated procedure is synthesis due to the chemical reactions necessary to add the required oligonucleotide bases. BP1001, inotersen, nusinersen, eteplirsen, and golodirsen are a few antisense drugs developed for treating neurodegenerative and neuromuscular diseases. Although antisense oligonucleotides present off-target reactions, multiple studies are being performed. The following review shows information regarding the pharmaceutical characteristics for industrial production and the current state of applicability in clinical practice. In conclusion, some molecules have already been approved for commercialization (inotersen, nusinersen, ataluren, eteplirsen, and golodirsen), showing them as promising therapeutic solutions in the short and medium term for disorders developed by specific genetic factors
Cytotoxic Activity of Ethyl Acetate Extract from Voacanga foetida (Bl.) Rolfe Leaves Against T47D Breast Cancer Cells
No full textThe cytotoxicity of ethyl acetate extract from Tampa badak (Voacanga foetida (Bl.) Rolfe) leaves against Artemia salina leach larvae was determined using the brine shrimp lethality test (BSLT) method and was evaluated against T47D breast cancer cells using MTT assay method. The result of BSLT showed a consistent result with MTT assay, which is the result obtained that ethyl acetate extract is very toxic against A. salina Leach larvae with LC50 value of 8.61 µg/mL and very cytotoxic against T47D breast cancer cells with IC50 values of 0.87; 0.66; and 0.95 µg/mL at the 24, 48 and 72 hours of incubation times, respectively. The MTT assay data were analyzed using a two-way ANOVA statistical method to see the effect of the dependent variable (concentration and time) on the independent variable (% viability). Based on the statistical test result, there is a difference in % viability between concentrations of 0.1; 1; and 10 µg/mL (p <0.05), but the length of incubation does not affect % viability (p >0.05)
Chemical Screening and Antioxidant Activity of Ethyl Acetate Fraction and Residue from Lansium domesticum Ethanolic Extract
No full textLangsat (Lansium domesticum) is a plant that thrives in the tropics. The search for photoprotective compounds derived from natural ingredients has been intensively conducted to develop cosmetic formulations to obtain safe and protective products against UV rays. This study aims to identify chemical compounds in the ethyl acetate fraction and residues of ethanol extract from L. domesticum bark using tube and gas chromatography-mass spectrophotometry tests. At the same time, the antioxidant activity and SPF values were assessed with the DPPH and FRAP methods. The qualitative GC-MS test obtained the percentage peak value and molecular weight. Furthermore, the antioxidant activity was tested using the compound DPPH measured with an ELISA reader at a wavelength of 515.5 nm with UV/vis spectrophotometer and FRAP method using FeCl3 and TPTZ compounds at 615 nm. The SPF value was assessed using Mansur's formula with UV/Vis spectrophotometer at 290 to 320 nm. The results obtained in the ethyl acetate fraction showed terpenoids, while the residue contains phenolics, flavonoids, tannins, and saponins. The GC-MS tests found that the ethyl acetate fraction had 47 types of chemical compounds, including terpenoids and fatty acids group; in the residue, four classes were found, with terpenoid and fatty acid groups being more predominant. Based on the results, the ethyl acetate fraction has an IC50 value of 341.25±26.45 µg/ml and 436.3±10.8 µg/ml; the residue was 94.72±34.22 µg/ml and 2602.79±11.8 µg/ml. Additionally, the SPF values for both were 2.87 and 3.9
Ointment Formulation of Tapak Dara (Catharanthus roseus (L.) G. Don) Flower Ethanol Extract and its Activity in Burn-Healing
No full textTreatment done on burn wounds is intended to provide local therapy to heal as quickly as possible. The content of secondary metabolites in the tapak dara (Catharanthus roseus (L.) G. Don) flower can help the healing process of burns, namely alkaloids, saponins, tannins, and flavonoids. Alkaloids act as antibacterial; saponins can trigger collagen formation; tannins as astringents that cause shrinkage of skin pores and stop minor bleeding in wounds; and flavonoids have anti-inflammatory effects. This study aimed to formulate an ointment of C. roseus flower ethanol extract and determine its physical characteristics such as organoleptic test, homogeneity, pH value, dispersion, and stability test of the preparation and examine the activity as a burn healer in white male rats. The research data were analyzed statistically using the ANOVA method, followed by the LSD test (least significant difference) to see how the ointment-containing extract reduced the diameter and percentage of the burn wounds. The results show that all ethanol extracts of C. roseus flower ointments met the requirements for its physical characteristic tests. It offers a good activity as a burn healer in white male rats. The most effective concentration is an ointment containing 15% of ethanol extract from C. roseus flower (F3 group), which shows a significant difference (p <0.05) from the blank and the other group formula in burn wound healing