Indonesian Journal of Pharmacy
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Co-crystallization of Sofosbuvir with Sugars for Enhanced Dissolution Rate
Get PDFSofosbuvir is one of the direct acting antiviral agents which is approved in the treatment of chronic HCV in combination with other agents. The low aqueous solubility of sofosbuvir resulted in slow dissolution which is supposed to be responsible for its low and variable bioavailability after oral administration. Accordingly, the objective of this work was to investigate the effect of co-crystallization of sofosbuvir with hydrophilic sugars on its crystalline structure and dissolution rate. Mixtures of sofosbuvir with hydrophilic sugars at various molar ratios were prepared by ethanol assisted kneading followed by drying. The dry products were then characterized by attenuated total reflectance fourier transform infrared spectroscopy (ATR FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (XRD) and in vitro dissolution studies. Combined instrumental analysis reflected development of new crystalline species of co-crystal type. This was evidenced by the existence of hydrogen bonding as shown from FTIR spectra, change in the thermal behaviour and appearance of new diffraction peaks in the diffractograms recorded by XRD. The co-crystallization was associated by weakening of intermolecular bonds which resulted in significant increase in the dissolution rate of sofosbuvir. The study introduced hydrophilic sugars as co-crystal co-formers for enhanced dissolution of sofosbuvir
A Retrospective Study of Body Weight Changes in Patients Receiving Cyproheptadine in A Hospital-Based Outpatient Setting in Thailand
Get PDFCyproheptadine has been used as an appetite stimulant to increase body weight in various population. This study aimed to determine the effect of cyproheptadine on weight changes in Thai patients. A retrospective longitudinal study was conducted in adult patients who were prescribed with cyproheptadine, having body weight records at 2 times consecutively during 12-month period at the medical outpatient department, the Police General Hospital, Thailand. Of 125 participants, 69.6% were females and the mean age was 78.38 (SD ± 11.68) years. Hypertension, dyslipidemia and diabetes mellitus were the most common underlying conditions. The mean body mass index (BMI) at 1st visit was 21.16 (SD ± 3.64) kg/m2. The mean body weight at 1st and 2nd visit were 52.46 (SD ± 11.11) kg, and 52.61 (SD ± 10.98) kg, respectively. Overall, there was no significant change in body weight between two visits. In underweight patients (BMI < 18.5 kg/m2), the mean BMI decreased significantly in the 2nd visit compared to 1st visit (p = 0.044). At the 2nd visit, older age and high-density lipoprotein cholesterol levels were negatively associated with body weight (p < 0.05). The polypharmacy (odds ratio (OR), 0.778; 95% confidence interval (CI), 0.616 – 0.982), the presence of hypertension (OR, 0.022; 95%. CI, 0.001 – 0.390) and low-density lipoprotein cholesterol levels (OR, 0.969; 95% CI, 0.942 – 0.996) were also negatively associated with abnormal BMI. Cyproheptadine might not improve the body weight of patients in this population. The factors associated with lower body weight in this study may be helpful in further research
Ciplukan (Physalis Angulata Linn.) Extract Compounds Potential on High-Fat Diet Induced Nonalcoholic Fatty Liver Disease (NAFLD) for Liver Anti-Fibrotic Drug Development
No full textAn increasing percentage of people have or are at risk to develop the non-alcoholic fatty liver disease (NAFLD) worldwide. Fibrosis has also been identified as the most important predictor of prognosis in patients with NAFLD. Ciplukan (Physalis angulata Linn.) was reported to have antifibrotic potency in CCl4-induced liver fibrotic rats. This study was conducted to evaluate the antifibrotic effect of ciplukan extract through repairing the liver function, anti-inflammatory, and lowering cholesterol. The liver fibrosis model using 20% margarine was injected subcutaneously 8 times with a frequency of twice a week for 4 weeks in 35 male and 35 female Wistar strains which were divided into 7 groups. Furthermore, the rats were given Ciplukan extract (CPL) orally starting the 6th week of treatment with 2 different doses, namely 13.5 mg (CPL-1) and 27 mg (CPL-2) every day for 4 weeks. The histopathological changes of liver fibrosis was analyzed using Haematoxylin Eosin (HE) staining. Determination of serum IL-6 and TGF-β1 levels was carried out by the ELISA method. ALT and cholesterol levels were tested using a diagnostic kit. Single and multiple doses of ciplukan extract with or without standard therapy (Vitamin E) can reduce fibrotic scores up to 1.30±0.95 (p=0.001), TGF-β1 levels up to 24.20±2.02 ng/mL (p = 0.000), IL-6 levels up to 1.68±0.52 pg/mL (p=0.156), ALT levels up to 104.57±2.02 U/mL (p=0.001), and cholesterol levels up to 81, 07±2.02 mg/dL (p=0.000). Ciplukan herb ethanol extract was proven to have liver antifibrotic activity, which means it has potential as a liver fibrotic drug. The liver antifibrotic effect of Ciplukan herb was shown by a histopathological decrease in liver fibrosis scores accompanied by a decrease in TGF-β1, IL-6, ALT, and cholesterol levels.
Keywords: Physalis angulata Linn (Ciplukan), liver fibrosis, NAFLD, ALT, Cholesterol, IL-
Isolation and Characterization of Curcumenotone, a Sesquiterpene from Curcuma aeruginosa Roxb as Antioxidant
Get PDFAntioxidant compounds are necessary to block the initiation of oxidation chain reactions and inhibit the formation of ROS which are the cause of various diseases. Natural antioxidants can be isolated from various sources, one of them from Curcuma aeruginosa Roxb Rhizome. This study was aimed to isolate and identify antioxidant compounds from Curcuma aeruginosa Roxb rhizome. To isolate the active compound, the 2,2-diphenyl-1-picrylhidrazyl (DPPH) free radical scavenging activity guide was used. Initially the Curcuma aeruginosa Roxb rhizome powdered material macerated with ethanol 70% to give ethanol extract (EE). The EE was then fractionated gradually with increasing polarity solvents to give n-hexane (HF), ethyl acetate (EAF), ethanol (EF) and insoluble (IF) fractions. The EF was the active fraction, was fractionated into 6 fractions (EE.a-f) based on their TLC picture. Two compounds (EF.a1 and EF.a2) were isolated from active fraction (EF.a) by preparative TLC. The EF.a2 appeared as white crystals demonstrates better activity as anti radical DPPH, having 96.24% purity (HPLC). EF.a2 appeared as a single peak in GC (Rt 12,78), and having molecular weight at m/z 234. There were 2 absorbtion peaks at 226 nm and 260 nm in Uv-Vis spectrophotometer and absorption bands at 3364, 3314, 2905 and 1653 cm-1 on the FT-IR spectrum. Based on spectroscopic data (1H-,13C-NMR) and comparison with reported data, the EF.a2 was identified as sesquiterpene, curcumenotone (C15H22O2). The curcumenotone was shown potent antioxidant in DPPH radical scavenging assay had an IC50 53.24±1.51 µg/mL, ABTS radical scavenging assay had an IC50 41.33±3.15 µg/mL, and FRAP assay had an IC50 37,82±2.02 µg/mL
Assessing the Antimetabolite Activity of Anthocyanins in Cantigi Fruits from Two Conservation Sites in Indonesia
Get PDFThe objective of the current study was to evaluate the antimetabolite activity of anthocyanins in Cantigi fruits from two Indonesian conservation areas. Cantigi (Vaccinium varingiaefolium) is a native fruit species known for its rich anthocyanin content associated with various health benefits. However, more research needs to be conducted on the antimetabolite properties of these anthocyanins. This study collected Cantigi fruits from two conservation sites in Indonesia, Tangkuban Perahu (CTP) and Papandayan (CPP) Mountain, and the antimetabolite activity was evaluated using enzymatic assays. The results demonstrated significant antimetabolite activity of CTP, particularly in inhibiting α-Glucosidase (53.72±1,98 µg/ml), pancreatic lipase (110.48±2,13 µg/ml), and angiotensin-converting enzyme (27.32±1,24 µg/ml). Furthermore, our analysis using HRMS revealed the presence of three anthocyanin compounds, delphinidin, malvidin, and peonidin, which are believed to contribute to the observed antimetabolite activities of Cantigi. These findings provide valuable insights into the specific compounds responsible for the bioactivity of Cantigi and further support its potential as a natural source of bioactive substances. Future research should focus on elucidating the molecular mechanisms underlying the effects of these anthocyanins on the targeted enzymes and exploring their potential synergistic interactions
Educational Curriculum to Improve Clinical Outcomes in Diabetes Mellitus Patients: A Systematic Review
Get PDFThe success of controlling the current condition of Diabetes Mellitus (DM) is not only determined by the help of medicine. DM therapy management is strongly supported by the success of providing education to DM patients, so that patients comply with treatment, adopt a healthy lifestyle, and can prevent complications that can end in death. This systematic review aims to find out what curriculum or content of educational materials needs to be given to DM patients to improve the achievement of clinical outcomes. Sage, Scient direct, and Pubmed were searched for relevant articles published between 2012 and 2022 using multiple search terms. STROBE tools were used to conduct quality assessments. Following that, a narrative synthesis of the findings was performed yield 1619 citations. After de-duplicating and screening, 18 studies were eligible for inclusion giving results. Educational materials related to diet/nutrition (n=17), physical activity (n=15), DM treatment (n=14), complications and risk factors (n= 13), goal setting or Healthy Living with DM (n=13), monitoring blood glucose levels parameters (n=11), description of DM (n=7), mental health (n=5), and foot care DM (n= 4). The review was hampered by the poor quality of the included studies. However, the evidence presented shows that educational materials provided to DM patients can improve clinical outcomes. Overall, the evidence base for educating DM patients in the community is still limited, and further research is needed
A Narrative Review of Staphylococcus hominis Resistance Pattern: Multidrug- and Possible Extensively Drug-Resistance
Get PDFStaphylococcus hominis is the third most frequent opportunistic pathogen in neonates and immunosuppressed patients that cause bacteremia, septicemia, endophthalmitis, and endocarditis. The emergence of methicillin resistant Staphylococcus hominis (MRSHo) has been reported and is a growing concern. This review was intended to determine the susceptibility of Staphylococcus hominis to antibiotic agents with pharmacokinetics/pharmacodynamic approach. In addition, this review was determined the phenotypic criteria and antibiotic choice of Staphylococcus hominis infection. Four databases i.e., PubMed, PlosOne, ScienceDirect and Google Scholar were employed in searching process. Antibiotic resistance was identified using the minimum inhibitory concentration (MIC) and the percentage of resistance. The breakpoint value was based on The European Committee on Antimicrobial Susceptibility Testing (EUCAST) Breakpoint tables for interpretation of MIC and zone diameters Version 11.0. There were 876 articles identified, 35 duplications were removed. These gave a total of 841 articles were screened yet 820 articles were irrelevant. Eventually, 21 articles were reviewed in this report. This review found that Staphylococcus hominis is potentially had MDR activity and a possible XDR bacterium that resistant to some antibacterial agents. The susceptibility of antibiotic to bacteria is not identical, and the regional reported drug resistance varies commonly due to differences in environment and antibiotic use. The resistance profile of Staphylococcus hominis is a complex interaction that affected by multifactorial such as: pharmacokinetics/pharmacodynamics index, mutant prevention concentration (MPC), mutant selection window (MSW), and the capability to produce biofilm
The Effects of Duration of Fermentation on Total Phenolic Content, Antioxidant Activity, and Isoflavones of The Germinated Jack Bean Tempeh (Canavalia Ensiformis)
Get PDFTempeh is one of the food products from legumes often consumed by Indonesians as a side dish. Moreover, tempeh is a functional food that contains bioactive compounds, such as antioxidants and isoflavones. This study aims to determine the content of total phenolic compounds, antioxidant activity, and isoflavones content of germinated jack bean tempeh with a fermentation duration of 0-5 days. Isoflavones extract was obtained using the extraction method with 70% ethanol. The total content of phenolic compounds was measured using the method of Folin-Ciocalteau. Meanwhile, antioxidant activity was measured with DPPH, and isoflavones content was determined using high-performance liquid chromatography (HPLC). The total content of phenolic compounds (TPC), antioxidant activity, and isoflavones were analyzed using the ANOVA, and differences between treatments were compared to the Smallest Real Difference test with a significance level of 5%. The total phenolic compound content and the highest antioxidant activity during the tempeh fermentation process were obtained on the fifth day of the fermentation period of 10.70±0.31 (mg GAE/g) for the total phenolic and 457.04±151.91(%) for IC50 values. The intergroup test results show significant differences. The highest isoflavones deposits for all isoflavones, such as daidzein, glycitein, genistein, and factor-2, were also obtained at day 5 of tempeh fermentation duration. This study has discovered significant differences between treatment groups. The isoflavones content is 4.63±1.74 µg/g of daidzein, 5.45±2.29 µg/g of glycitein, 0.92±0.33 µg/g of genistein, and 0.46±0.21µg/g of factor-2. This study has discovered that the germination and fermentation process of jack bean tempeh changes the content of total phenolic compounds and antioxidant activity as well as increases and influences the isoflavones profile
Influence of Polymer Combınatıon Concentratıon on The Characterıstıcs, In Vıtro Release And In Vıvo Lung Deposıtıon of Algınate-Carrageenan Mıcrospheres Encapsulatıng Cıprofloxacın HCl
Get PDFInhalation Ciprofloxacin HCl microspheres were formulated with combination of alginate and kappa carrageenan with a total of 1% (F1), 1.5% (F2), and 2% (F3). Aim of this research is to examine effect of polymer concentration on characteristics, release, and lung deposition of microspheres. Microspheres were characterized including loading, efficiency, yield, size, moisture content, mucoadhesivity, and release. Deposition was studied by fluorescence microscopy. Results showed spherical and smooth with size ofless than 2 µm. Loading showed about 18.55% to 29.65%. Entrapment efficiency was 52.86-76.29%. Yield was 49.83-70.72%. Swelling index was less than 10. For moisture content, all formulas demonstrated less than 6.5%. For mucoadhesivity, F1, F2, and F3 showed 0.0090 kg, 0.0217 kg, and 0.0329 kg respectively. It was found that increasing polymer concentration did not affect size, loading, efficiency, and yield of microspheres. Cumulative release at F1, F2, and F3 was 72.64%, 59.25%, and 47.66% respectively in 10 minutes at PBS pH 7.4 with burst release profile. In vivo showed that all formulas were able to deposit on rat lungs and it was found that the intensity were decreased at the 4th hour due to increase of polymer. Remaining intensity indicated that microspheres were able to maintain the drugs loaded
Antioxidant Activity and Irritation Potency of Face Tonic Formulation from Ethanol Fraction of Sappan Wood (Caesalpinia sappan L.)
Get PDFSappan wood is a medicinal plant that contains phenolic compounds such as brazilin. It can be used to treat photoaging due to oxidative stress. Face tonic is one type of facial skin care cosmetic that has this purpose. The research aims to determine the formula, IC50 value, and irritation potency of face tonic from the ethanol fraction of sappan wood. The ethanol fraction of sappan wood was formulated into a face tonic preparation using glycerin and propylene glycol as cosolvents. The evaluation of face tonic involved antioxidant activity using the DPPH method. Meanwhile, the irritation-potential test was conducted using the HET-CAM method. The results showed that face tonic formulas had an antioxidant activity with IC50 values of 639.904 ppm (FI) and 620.365 ppm (FII). The irritation score of each formula was 0 (non-irritant) and 5.44 (moderate irritant). Face tonic with glycerin as a cosolvent has antioxidant activity and is safe to use.