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SECONDARY BIOACTIVE METABOLITE GENE CLUSTERS IDENTIFICATION OF ANTICANDIDA-PRODUCING Streptomyces Sp. GMR22 ISOLATED FROM WANAGAMA FOREST AS REVEALED BY GENOME MINING APPROACH
Full text linkStreptomyces are a group of Gram-positive bacteria belonging to the Actinobacteria class, which are among the most important bacteria for producing secondary bioactive metabolites such as antibiotics, chemotherapeutics, insecticides and other high-value chemicals. Genome mining of gene clusters that encode the biosynthetic pathways for these metabolites has become a key methodology for novel compound discovery. Recently, we have isolated the Streptomyces sp. GMR22 from Cajuput rhizospheric soil at Wanagama Forest, Indonesia. GMR22 produced secondary metabolite that inhibited Candida albicans with IC50 of 62,5 μg/mL. The objective of this work was to reveal the novel secondary metabolites from GMR22 by genome mining approach. The antiSMASH 3.0 was used to predict gene clusters that encode the biosynthetic pathways of secondary metabolites in the genome of GMR22, and their core chemical structures. The pylogenomic analysis showed that GMR22 was closely related to Streptomyces bingchenggensis BCW1, as well as to the large genome size (9.5-12.7Mbp) groups of Streptomyces. AntiSMASH 3.0 analysis revealed that the genome of Streptomyces sp. GMR22 harbored at least 63 gene clusters that encode the biosynthetic pathways of secondary metabolites. It was the highest number of gene clusters had been observed among the members of Streptomyces groups, with PKS was predicted as the major groups of the identified gene cluster products. The results suggested that GMR22 could be a strong potential candidate of secondary bioactive metabolites source
The Effect of Medication Reminder Chart on Level Adherence in diabetes mellitus type 2 patients at RSUD Sleman Yogyakarta
Full text linkPatient adherence is a key factor that determines the outcome of diabetes mellitus therapy. This study was conducted to determine the effect of a medication reminder chart on level adherence and clinical outcome in patients with Type 2 diabetes mellitus. The experimental study used pretest-posttest design with control group was conducted during February until April of 2016 at Sleman Hospital in Yogyakarta. Patients were categorized into two groups of different subjects, who received of medication reminder chart tools were 40 patients (Code A) and the other 40 patients were assigned to control group (Code B). Morisky Medication Adherence Scale of 8-item (MMAS-8) was used to measure adherence. Clinical outcome were measured based on FBG decrease (mg/dl). Two independent sample t-test was using to determine the mean differences of the average score of the adherence level before and after using the medication reminder chart. The results of this study showed that Medication Reminder Chart compared control groups improved adherence (p=0.000) but did not improve clinical outcome (p=0.411). The pharmacist might use The Medication Reminder Chart to improve medication adherence for chronic disease
Estimation of total phenolic, total flavonoid content and evaluation of anti-inflammatory and antioxidant activity of Ixora coccinea Linn. stems
Full text linkIxora coccinea Linn. (Rubiaceae) has mentioned in Ayurveda as Paranti and traditionally stems used in inflammatory diseases like sprains, eczema, contusions and boils. Present study deals with evaluation of anti-inflammatory and antioxidant activity of extracts of I.coccinea stem. Anti-inflammatory activity was studied in vivo by carrageenan-induced paw edema in rat and in vitro by human red blood cell membrane stabilization method. Total tannin and flavonoid content of extracts was determined by using the Folin- Ciocalteu method and aluminum chloride method, respectively. Antioxidant activity was evaluated by in vitro assay involving nitric oxide scavenging, hydrogen peroxide scavenging, 2,2- diphenylpicrylhydrazyl (DPPH) radical scavenging, and ion chelating activity. Chloroform extract showed significant reduction in carrageenan induced rat paw edema (p<0.05) and protection of HRBC in hypotonic solution. Methanol extract contain more total tannin and flavonoid content as compared with petroleum ether and chloroform extract. All extracts showed concentration dependant free radical scavenging activity. Methanol extract and chloroform extract have shown better antioxidant activity and due to this antioxidant nature might be responsible for its anti-inflammatory activity. These activity supports to use of I.coccinea extract in traditional used in treatment of various inflammatory disaeses
Effect of Lipid Ratio of Stearic Acid and Oleic Acid on Characteristics of Nanostructure Lipid Carrier (NLC) System of Diethylammonium Diclofenac
Full text linkThe aim of this study was to determine the effect of lipid ratio of stearic acid and oleic acid on the physical characteristics as well as the entrapment efficiency of diethylammonium diclofenac with Nanostructure Lipid Carrier (NLC) system. Diethylammonium diclofenac (DETA) is Non-Steroid Anti-Inflamatory Drugs (NSAIDs) that has been widely used in the treatment of osteoarthritis and rheumatoid arthritis. In the formulation of NLC-DETA, three different lipid ratios were used, which the ratio of stearic acid:oleic acid were 60:40, 70:30, and 80:20, respectively. In this NLC system, DETA served as the active drug, stearic acid as solid lipid, oleic acid as liquid lipid, and Tween 80 as surfactant components. NLC were characterized for organoleptic characteristics, pH, viscosity, particle morphology, particle size and polydispersity index (PI), profiles of Fourier Transform Infra-Red (FTIR) and Differential Thermal Analysis (DTA), and drug entrapment efficiency. The particle shape and morphology were determined by Transmission Electron Microscopy (TEM). The results showed that the different ratios of oleic acid lipids and stearic acid had no significant effects on the viscosity and entrapment efficiency of NLC-DETA. On the other hand, it affected the pH of all formulas, which were significantly different. Increasing the amount of liquid lipid in the formulations reduced the size of NLC-DETA particles.
FORMULA OPTIMIZATION OF ORALLY DISINTEGRATING TABLET CONTAINING MELOXICAM NANOPARTICLES
Full text linkMeloxicam is one of oxicams anti-inflamatory drugs that are effective to relieve toothaches, arthritis, dysmenorrhea, and fever. Meloxicam in this study was milled with High Energy Milling (HEM) method to obtain its nano size and then direct compression method was used to produce Orally Disintegrating Tablet (ODT). ODT is designed to be rapidly dissolved on the tongue within a minute. It can be administered without water or chewing and may improve the bioavailability and effectiveness of the drug, and increase the patient’s adherence. The present study aimed to understand the effects of Ac-Di-Sol and Kollidon CL as superdisintegrants, that were used separately or in combination, on the characteristics of nanoparticles meloxicam ODT. It was also to obtain the best proportion of combination between Ac-Di-Sol and Kollidon CL that can produce the optimum formula of meloxicam ODT. The effects of single or combined superdisintegrants were evaluated using Simplex Lattice Design (SLD). Ac-Di-Sol (X1) and Kollidon CL (X2) were the independent variables, while the dependent variables were friability (Y1), disintegrating time (Y2), wetting time (Y3), and percent meloxicam release after 60 seconds (Y4). Optimization of five nanoparticle meloxicam ODT formulas was conducted using Design Expert 7.1.5. The combination of Ac-Di-Sol 4.05mg (X1) and Kollidon CL 10.95mg (X2) in 150mg nanoparticles meloxicam ODT can produce optimal ODT characteristics. After verification there was no difference between predicted value and observed value with p value > 0.05
NOVEL CHRONOTHERAPEUTIC MULTIPARTICULATE DRUG DELIVERY SYSTEM OF FELODIPINE: AN EFFECTIVE TREATMENT FOR CARDIAC ARRHYTHMIA
Full text linkArrhythmia follows chronobiology, thus necessitating development of time-dependent formulation for its treatment. The aim of the current work was to develop a solubility-enhanced chronotherapeutic system of felodipine, a widely prescribed anti-arrhythmic. Systematically optimized hot-melt extrusion process was employed to formulate solubility-enhanced extrudates. Film-casting method was adopted for the selection of polymers. Drug released at 5, 15, 30min was taken as response variables in 32 face-centered cube design. Nearly 10-fold increase was observed in the solubility of the optimized extrudates in comparison to pure drug. Physical characterization of the extrudates depicted complete amorphization of drug. Sequential coating was performed on to the extrudates to enable a time-dependent release. In-vitro studies clearly demonstrated that 25% of drug was available rapidly within 10 min of administration. The remaining 75% of drug was available over a period of 4, 8 and 12h. Stability studies performed for 6 months at accelerated conditions depicted no significant change in the physicochemical characteristics of the optimized formulation. In-vivo pharmacokinetic studies conducted in beagle dogs ratified the results of in-vitro studies where a sequential time dependent absorption of felodipine was observed over a period of 12h. Concisely, the studies demonstrated successful development of solubility-enhanced chronotherapeutic system of felodipine
ROLE OF CHITOSAN, CARBOXY METHYL CELLULOS, POLYVINYL PYRROLIDONE, KYRON T134 AND PRIMOGEL TO DESIGN THE MOUTH DISINTEGRATING TELMISARTAN TABLET WITH EXTENDED RELEASE PROFILE
Full text linkThe Mouth Disintegrating Extended Release Telmisartan (MDERT) tablets are designed for adequate pharmacokinetic profile to avoid the unusual peaks and troughs. Although, there are extensive advance techniques used to deliver drugs. But oral route is still remains effective in most of the therapeutical situations. Thus we aimed this study to formulate a dosage form with dual character of orodispersion as well as extended effectiveness. MDERTS dosage form was prepared by direct compression method. The major components of this preparation were Telmisartan (TLM), Carboxy methyl cellulose polyvinyl Pyrrolidone, Chitosan, Talc, Mg-stearate, Lactose. The MDERTS dosage form was characterized with different determinants. While, the drug release curves of all 6 formulations upto 12h, DSC spectra of TLM, Kyron T134, Primogel, TLM+Kyron T134+Primogel, Chitosan, CMC and different excepients are presented as comprehensive scientific figures. DSC and FTIR spectroscopic studies indicate the compatibility of drugs with each other and with excipients. Moreover, the formulation F2 containing more than 10% of Kyron T had shown best results. Whereas, the overall results had shown that Kyron T containing tablets had best, in vitro dispersion time, wetting time and wetting volume, water absorption ratio. The order in which superdisintegrants and polymers had produced desirable effect is Kyron T134 > Kyron T134134 + primogel > primogel and for polymers chitosan> chitosan+CMC> chitosan +PVP> CMC> CMC+PVP> PVP. Thus, Kyron T is the best superdisintegrant of others which were used in present study and direct compression method is the best used to prepare extended release mouth disintegrating tablets.
PHARMACODYNAMICS STUDY OF ETHANOL EXTRACT OF CYCLEA BARBATA (MIERS.) LEAVES ON SRF AND COX-2 GASTRIC MICE WITH NSAID GASTROPATHY
Full text linkEpidemiology of NSAIDs gastropathy is increasing as increase number of usage. From arthritis to cardiovascular events and cancer prevention, the versatility of NSAIDs is not questioned. However, no dose of NSAIDs is safe. No matter low dose, or single use, NSAIDs will cause gastric damage upto 3-7 days after use. In inflammation and healing process of gastropathy there are various proteins involved, but treatment with COX-2 and SRF are associated with an immediate healing and better quality of gastric mucosa. Cyclea barbata (miers.) has been declared as functional food for preventing and treatment gastropathy yet, its mechanism of actions have not yet clearly discovered. Hence the aim of this study is to analyze the effects of Cyclea barbata (miers.) ethanol extract to COX-2 and SRF in gastric tissue, in time series basis. Laboratory mice was induced with aspirin to produce gastropathy and then treated with Cyclea barbata (miers.) extract for 1, 3, 7, 10 or 14 days. Gastric tissue then harvested and analysed with elisa procedure to determine tissue SRF and COX-2 level. Treatment was proven to increase COX-2 and SRF higher than control group. This concludes one of Cyclea barbata (miers.) mechanism for NSAIDs gastropathy is by increasing tissue COX-2 and SRF.
Population-Based Approach to Analyze Sparse Sampling Data in Biopharmaceutics and Pharmacokinetics using Monolix and NONMEM
No full textAlthough it has been developed since 1972, the implementation of a population-based modeling approach in Indonesia, particularly to analyze biopharmaceutics and pharmacokinetics data is still very limited. This study was aimed to evaluate the performance of Monolix and NONMEM, two of the popular software packages in a population-based modeling approach, to analyze the limited data (sparse sampling data) of the time profiles of the simulated plasma drug concentration of a theoretical compound. and NONMEM were used to model the limited data (40 data points) as a results of the random selection from the 180 point data of simulated plasma drug concentration (Cp) on 20 subjects at 0.25; 0.5; 0.75; 1; 1.5; 3; 6; 12 and 18 hours after per-oral administration of a 100mg of a theoretical compound. Population values of the absorption rate constant (Ka), the elimination rate constant (Kel) and volume of distribution (Vd) were compared to the average Ka, Kel and Vd obtained by the conventional method (two stage approach) using PKSolver on the Cp data of all subjects. The calculation system of a nonlinear mixed effect model in Monolix and NONMEM, successfully describes the sparse data, based on the visual evaluation of the goodness of fit. Comparison of parameter estimates of population values in Monolix and NONMEM are in the range of 94 to 108% of the real values of the rich data analysed by PKSolver. A population-based modeling can adequately analyze limited or sparse data, demonstrating its capability as an important tool in clinical studies, involving patients
Hepatoprotective Activity of Ethyl Acetate Fraction of Senggugu’s Root Bark (Clerodendrum serratum L.Moon) on Rats Induced by CCl4
Full text linkSenggugu is a plant that has long been used to treat syphilis, typhoid, cancer, jaundice, and hypertension. The pharmacological activity of senggugu in Indonesia that have been reported include antifertility activity in leaves, mucolytic activity, anti-inflammatory and tracheospasmolytic, also antioxidant in its root bark. This study aims to determine the hepatoprotective effect of ethyl acetate extract fraction of senggugu’s root bark in rats induced by CCl4. The powder of senggugu’s root bark was extracted by terraced maceration method starts from n-hexane, ethyl acetate, to methanol, thus obtained ethyl acetate extract fraction of senggugu’s root bark (FEAKAS). The ethyl acetate extract fractions were then tested for hepatoproctective activity using doses of 25, 50, and 100 mg/Kg.BW on rats induced by CCl4. FEAKAS hepatoprotective activity was determined from the analysis of blood biochemical and oxidative stress parameters. The blood biochemical parameters included SGOT (serum glutamic oxaloacetic transaminase), SGPT (serum glutamic pyruvic transaminase), ALP (alkaline phosphatase), bilirubin, and total protein were measured with test kit. The oxidative stress parameters were measured from homogenates of liver tissue that were prepared by adding 500 mL of 50 nM Tris buffer (pH 7.4) containing 1 mM EDTA and 10 µg/mL leupeptin. The homogenates were centrifuged to obtain supernatants for measurement of oxidative stress parameters using spectrophotometer method, including MDA (malondialdehyde), GPx (glutathione peroxidase) and CAT (catalase). The results showed that the effect of FEAKAS against CCl4 induction for preventing lipid peroxidation, from both blood chemical and oxidative stress parameters, are shown at a dose of 100 mg/Kg.BW that significantly different compared to CCl4 control (ρ <0.05) on all blood chemical and oxidative stress parameters