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    FORMULATION DEVELOPMENT AND CHARACTERIZATION OF TEA TREE OIL LOADED ETHOSOMES

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    To prepare ethosomes containing tea tree oil by hot homogenization method and to evaluate its physical characters and in-vitro release pattern.  the preformulation studies were carried out by standard procedure. The morphology of globule was studied by optical microscopy. The globule size and zeta potential was determined by Zetasizer, respectively and in-vitro study was done by diffusion method and the drug content was analyzed by HPTLC method. The release kinetics was also studied by fitting into few mathematical models.  All the formulations were showed spherical and unilamellar shape with globule size of 931 to 975 nm, the zeta potential in the range of – 40 to -52 mV and entrapment efficiency was 57 to 65 %. Finally the invitro release studies showed the drug release from the ethosomal vesicles was burst release at initial time followed by sustained release over throughout the study. From the above consideration of evaluation studies, the tea tree oil loaded ethosomal formulation F5 shows best globule size, zeta potential and entrapment efficiency. The sustained action was confirmed by invitro release studies. All the formulations are followed zero order drug release and diffusion type of mechanism of drug releases with Fickian model. Ethosome loaded tea tree oil could be the best choice for topical application

    CYP1A1 and GST expression of hepatocytes induced by 7,12-dimethylbenz(a)anthracene and the influence of ethanolic extract of Gynura procumbens

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    The cytochrome P-450 (CYP) and glutathione S-transferase (GST) enzyme systems may influence the biological effects of carcinogens. As such, these enzymes may predict the developmental risk of breast cancer, as well as be potential targets for chemoprevention. The purpose of this study was to compare the expression of CYP1A1 and GSTµ between treatment groups. Expression of CYP1A1 and GSTµ was quantified in liver tissue from 18 female Sprague Dawley rats aged 40 days, which randomly divided into six treatment groups. Those are base line group (without DMBA and ethanolic extract treatment), DMBA induced cancer group, the other two groups was administrated by DMBA after treated by ethanolic extract in two different doses, 300 mg /kg BW and 750 mg/kg BW.  The last two groups were given two doses of extract ethanolic only, without initiated of DMBA. The ingestion of the extract was carried for three weeks and the ingestion of DMBA was performed twice in the third week. The expression CYP1A1 and GST was quantified by immunohistochemistry. CYP1A1 expression was significantly higher (P < 0.05) in cancer group (DMBA) as compared with other groups. On the other hand, GST expression was lower in cancer group (P < 0.05). Result of this study demonstrated that ethanolic extract leaves of  G. procumbens in 300 mg/kg BW dose could  inhibit CYP1A1 stronger than are other and induced GSTµ level. Has effect on ethanolic extract leaves of G. procumbens has ability in played role of as blocking agent in preventing initiation stage of carsinogenesis, therefore it should be taken into account for chemopreventing agent in mammary carsinogenesis.Key words : Gynura procumbens, breast cancer,  hemopreventive, CYP1A1, GST

    Potency of use ferrous sulphate from iron waste workshop bubut for raw material pharmacy

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    Iron Deficieny Anemia (IDA) representing one of especial micronutrient deficiency that happened in Indonesia. IDA suffered by Indonesia resident about 100 million soul. One of effort of handling IDA is supplementation by ferro sulphate. To serve the purpose of raw material pharmacy have to be up to standard quality of set in Pharmacopoeia of Indonesia Edition IV.This Research aimed to make, to purify and characterization ferro sulphate from iron waste. The produce with reacted iron waste and acid sulphate 25% during 2 day. Crystal dissociated and purified by recrystalization, and then characterization with SEM-EDS.Result of research showed that ferro sulphate from iron waste of workshop bubut fulfill the standard quality of in Indonesia Pharmacopoeia Edition IV.Key words : iron waste, ferrous sulfate, recrystalization, characterization

    Assay method validation of triamcinolone acetonide (TA) to support the investigation of TA-loaded nanoparticles

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    Theaim of this study was to develop the valid analytical method which used for the assay of triamcinolone acetonide (TA) in the investigation of TA loaded nanoparticle formulations. High Performance Liquid Chromatography(HPLC) method was applied in  his study by using an Econosil column,C1810 m, 250x 4.6mm (Alltech Associates Inc, PA,USA )as the stationary phase. Themobile phase consisted of a composition of acetonitrile (ACN) and 20mM phosphate buffer solution (pH 4.2) in the proportion of 50:50 v/v. The HPLCassay of TA was validated for selectivity, linearity, precision, ecovery (accuracy),sensitivity and stability of TA during the assay. Results showed that the concentration of TA in the sample scan be determined against the standard in the concentration range of calibration curve. The system precision and level of recovery were considered to be acceptable, and the method was selective and sensitive.Key words:triamcinoloneacetonide,assay,validatio

    OPTIMIZING STRUCTURE-BASED VIRTUAL SCREENING PROTOCOL TO IDENTIFY PHYTOCHEMICALS AS CYCLOOXYGENASE-2 INHIBITORS

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    By employing Databases of Useful Decoys (DUD) and its enhanced version (DUD-E), several attempts to construct validated Structure-based Virtual Screening (SBVS) protocols to identify cyclooxygenase-2 (COX-2) inhibitors have been performed. Both databases tagged active COX-2 inhibitors for compounds with IC50 values < 1mM. In the search for phytochemicals as natural COX-2 inhibitors, however, most of their IC50 values are in the micromolar range, which will likely be identified as non-inhibitors for COX-2 by the available SBVS protocols. In this article, validation of an SBVS protocol by adding marginal active COX-2 inhibitors from DUD-E as active compounds is presented. Binary quantitative-structure activity relationship analysis by using recursive partition and regression tree method was performed subsequently to optimize the predictive ability of the protocol. The enrichment factor and the F-measure values of the optimized protocol could reach 44.78 and 0.47, respectively. The optimized protocol could identify 1 out of 9 phytochemicals as COX-2 inhibitors

    The effects of PGV-1 and PGV-2 on the b-hexosaminidase release from intraceluller calcium ion-induced mast cells

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    PGV-1 or 2,5-bis(4'-hydroxy-3',5'-dimethylbenzylidene)cyclopentanone and PGV-2 or 2,5-bis(4'-hydroxy-3',5'-diethylbenzylidene)cyclopentanone are two benzylidene cyclopentanone analogues of curcumin. In our study, weinvestigated the effects of these compounds on the b-hexoaminidase enzyme release from mast cell culture (RBL-2H3 cell line). Thapsigargin and ionomycin were used as intracellular calcium ion stimulants for inducing b-hexoaminidase enzyme release from mast cells. The release of b-hexoaminidase enzyme was determined by colorimetric methods with substrate, p-nitrophenyl-2-acetamido-2-deoxy-b-D-glucopyranocide, and a microplate reader at 405 nm. In present study, treatment of 0.5 mM thapsigargin or 1 mM ionomycin could stimulate therelease of b-hexoaminidase enzyme from RBL-2H3 cells by 43.91 ± 1.30 % dan 52.93 ± 2.07 %, respectively. PGV-1 and PGV-2 showed inhibitory effects on the b-hexoaminidase enzyme release from RBL-2H3 cells induced by the increase of intraceluller calcium ion in dose-dependent manner. At the dose of 100 mM, PGV-1 and PGV-2, respectively, inhibited the b-hexoaminidase enzyme release by 73.51 ± 8.69 % and 66.42 ± 8.63 % on thapsigargin experiments; and by 89.73 ± 3.23 % and 38.57 ± 5.32 % on ionomycin experiments. The IC50 values of their effects on the b-hexoaminidase enzyme release from RBL-2H3 cells, respectively, were 22.20 mM and 22.27 mM on thapsigargin experiment; and 22.77 mM and >100 mM on ionomycin experiment. Based on the results, the inhibitory effect of PGV-1 and PGV-2 on the b-hexoaminidase enzyme release from RBL-2H3 cells involving mechanisms related to the alteration on activationprocesses of intracellular calcium ion on mast cells.Key words : Curcumin, PGV-1, PGV-2, mast cells, b-hexoaminidase enzym

    Synthesis and gastric ulcer protective activity of chlorinated quercetin

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    Gastrointestinal toxicity due to non-steroid anti-inflammatory drugs can be inhibited by the compounds that have antioxidant activity. Quercetin is a flavonoid that has antioxidant activity and protection effect against gastric ulcer. Chlorination of quercetin enhanced the antioxidant activity. This study aims to obtain the chlorinated derivative of quercetin and examine the protection effect against acetosal-induced gastric ulcer. Chlorination was done by the addition of chlorine at room temperature. Ulcer induction was carried out on rats by oraladministration of acetosal. Incidences of gastric ulcer were determined by macroscopic and microscopic observation. Chlorination of quercetin with chlorine gas produced 6-chloroqueretin as major product. The protection effect against acetosal-induced gastric ulcer of this compound was higher than quercetin.Key words : quercetin, chlorination, gastric ulcer, NSAID

    FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF GRANISETRON HYDROCHLORIDE USING PLANTAGO OVATE AS NATURAL SUPERDISINTEGRANTS

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    The main objective of the study was to develop orodispersible tablets of Granisetron hydrochloride, a selective 5-HT3 receptor antagonist (an antivomiting agent) for improving patient compliance, especially those of paediatric & geriatric categories with difficulties in swallowing. In the wet granulation method orodispersible (ORD) tablets were prepared using natural super disintegrants  plantago ovate.The prepared batches of tablets were evaluated for weight variation, hardness, friability, wetting time, in vitro dispersion time, drug content and in vitro dissolution studies. The tablet formulation batch F4 was considered as the overall best formulation (with an in vitro drug release study of 99.11%).Short term stability studies (at 40±2ºC/75±5% RH) on the best formulation indicated that there no significant changes in drug content. From the Fourier Transform Infrared (FTIR) spectroscopy study indicated that there are no drug excipient interactions. Key words:  Granisetron hydrochloride, Orodispersible tablets, FTIR spectroscopy, in vitro drug release study

    DETERMINATION OF SIBUTRAMINE ADULTERATED IN HERBAL SLIMMING PRODUCTS USING TLC DENSITOMETRIC METHOD

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    Determination of sibutramine adulterated in herbal slimming product using thin layer chromatography (TLC) densitometric method with TLC silica gel 60 F254 aluminium plate as stationary phase and mixture of toluen-diethylamine (10:0.3) as mobile phase has been developed. The calibration curve in the concentration range of 0.50 to 5.00 µg/spot showed good linier relationship (r2 = 0.9986). The limit of detection and quantitation (LOD and LOQ) were 217.5 ng and 724.9 ng/spot, respectively. The method gave satisfactory specificity, linierity, precision and accuracy validation criteria and was applied for determination of sibutramine in herbal slimming products obtained from several drugstrores in Depok City, West Java, Indonesia. Results of the determination showed that six of seven samples analyzed were detected containing sibutramine HCl with the concentration of 2.45 - 26.24 mg in a single dosage of slimming herbal product

    NATIONAL HEALTH COVERAGE SYSTEM : PHARMACISTS AND JKN PARTICIPANT SATISFACTION IN PRIMARY HEALTH FACILITIES

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    National Health Insurance is a health protection system for participants to obtain health care benefits and protection to meet basic health needs that organized based on social insurance and equity principles. JKN in cooperation with the primary health facilities to provide comprehensive health services including pharmacy services. Pharmacist responsible for drug availability and affordability that affected by drug procurement process, drug distribution process, and drug cost claiming process.This research’s aim to determine relationship between national health insurances services to pharmacists satisfaction and to determine relationship between pharmacy services to outpatient satisfaction at primary health facilities. Data used in research are primary data that collected through questionnare and interview. The method used is purposive sampling which the data is analyzed using linear and multiple regresion and see significant value (p). The number of respondents was 40 pharmacists and 150 patients in health centers and primary clinics scattered in Sleman, Bantul, and Kota Yogyakarta. The results showed that the process of procurement and distribution of drugs have a relationship with a pharmacist satisfaction while drug costs not process claims with consecutive p 0.010, 0.002, and 0.261. Related to the satisfaction of the outpatient pharmacy services result there is a relationship of drug availability (p = 0.003), service time (p = 0.006), and get drug (p = 0.000) to the satisfaction of outpatients. The conclusion of this study is the process of procurement and distribution of drugs have a relationship with a pharmacist satisfaction. In addition, the availability of pharmacy services such as medication, a drug services, and the provision of drug information also has a significant relationship to the satisfaction of outpatients in health facilities first rate.Keywords: pharmacy services, pharmacists, patients, JK

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