Hyperlipidemia is a pathological condition due to lipid metabolism abnormalities. Increased and oxidized LDL in hyperlipidemia will trigger an inflammatory response and produce proinflammatory cytokines, such as vascular cell adhesion molecule-1 (VCAM-1) and Interleukin-6 (IL-6). Curcumin can be used as antioxidants, anti-inflammatory and antihyperlipidemia, but as it is practically insoluble in water, formulation of curcumin nanosuspension is made to improve the effects of curcumin therapy. This study was conducted to determine the activities of nanocurcumin preparation as preventive measures for rats induced with hyperlipidemia. The test animals used were 49 male Wistar rats divided into 7 test groups: normal control group, negative control group, 80mg/kg BW/day curcumin control group, and nanosuspension curcumin dose of 80mg/kg BW/day, nanoemulsion curcumin dose of 80mg/kg BW/day, SNEDDS curcumin dose of 80mg/kg BW/day and solid lipid nanoparticles dose of 80mg/kg BW/day. Provision of preventive measure was performed on days 1-67. On day 11-67, the induction of lard and egg yolk (1:1) was administered with a volume of 2mL/200g of rat BW. On the 68 th day, blood samples were taken for the determination of VCAM-1 and IL-6 parameters using Biotin-Streptavidin-Amplified Enzyme-Linked Immuno-sorbent Assay method. Data analysis of VCAM-1 and IL-6 levels between test groups were conducted by means of normality test and One-way ANOVA (p<0.05). Based on the data of VCAM-1 and IL-6 levels, nanocurcumin dose of 80mg/kg BW preparation was able to significantly improve the preventive activity of curcumin compared to curcumin suspension dose of 80mg/kg BW by reducing VCAM-1 levels in SNEDDS (53.260%), nanoemulsion (52.737%), nanosuspension (52.325%) and solid lipid nanoparticles (51.444%) and decreasing IL-6 levels in SNEDDS (33.030%), nanoemulsion (31.568%), nanosuspension (29.898%), and solid lipid nanoparticles (28.875%).
Backround: Glibenclamide is an oral antidiabetic drug which is practically insoluble in water. Formation of β-cyclodextrin inclusion complex was able to increase glibenclamide solubility. Objective: Aims of this study are to characterize, formulate and evaluate inclusion complex tablets of glibenclamide to meet the requirements in Pharmacopeia. Methods: Inclusion complex was prepared in a 1: 1 and 1: 2 molar ratio by spray drying method. Characterization were performed by using Fourier Transform Infrared (FTIR) spectroscopy and Scanning Electron Microscope (SEM). Further, it was formulated into tablets by direct compression technique using primojel and crospovidone as disintegrants. Uniformity weight, hardness, friability, disintegration, and tablets were evaluated include dissolution. Dissolution studies of inclusion complex were performed by using United States Pharmacopeia (USP) II apparatus. Drug concentration dissolution was determined with high pressure liquid chromatography (HPLC). Result: Result of FTIR and SEM provided evidence of glibenclamide and β-cyclodextrin complex formation after using spray drying methods. The tablet evaluation with primojel and crospovidone as disintegrant showed that increase concentration of disintegrant would increase disintegration time of the tablets. All of the formulas meet the requirements in the Pharmacopoeia. Conclusion:The inclusion complex of glibenclamide-β cyclodextrin successfully used for enhancing the solubility of glibenclamide. The tablets meet the requirements in Pharmacopeia.Latar Belakang: Glibenklamid merupakan obat antidiabetes oral yang sukar larut dalam air. Pembentukan komplek inklusi dengan β-siklodekstrin diharapkan mampu meningkatkan kelarutan glibenklamid. Tujuan Penelitian: Penelitian ini bertujuan untuk mengkarakterisasi, memformulasi dan mengevaluasi tablet hasil komplek inklusi glibenklamid supaya memenuhi persyaratan Farmakope. Metode: Komplek inklusi dibuat dengan perbandingan rasio molar glibenklamid dan β-siklodekstrin 1 : 1 dan 1 : 2 dengan menggunakan metode spray drying. Hasil komplek inklusi dikarakterisasi meliputi spektroskopi FTIR dan SEM. Selanjutnya kompleks tersebut diformulasi menjadi tablet dengan teknik kempa langsung menggunakan primojel dan crospovidon sebagai disintegran. Tablet yang dihasilkan dievaluasi keseragaman bobot, kekerasan, kerapuhan, waktu hancur dan disolusi. Uji disolusi tablet hasil
BACKGROUND: Genetic variations in ABCB1 gene that encodes P-glycoprotein, the main transporter in the efflux of carbamazepine (CBZ) from the brain cells, can lead to pharmacodynamic and pharmacokinetic variability. Polymorphism of C3435T is widely known to cause protein overexpression that contributes to an increased risk of CBZ resistance. AIM: This study determined the allele frequency distribution of ABCB1 C3435T gene in healthy subjects of the Javanese population as a major ethnic group in Indonesia. METHODS: This cross-sectional study involved 100 healthy volunteers who fulfilled the inclusion criteria. The genotype analysis to detect polymorphism in the targets employed the polymerase chain reaction-restriction fragment length polymorphism method with 5’-TGCTGGTCCTGAAGTTGATCTGTGAAC-3’ as the forward primer and 5’-ACATTAGGCAGTGACTCGATGAAGGCA-3’ as the reverse primer. RESULTS: The frequency of subjects with C allele in ABCB1 C3435T gene reached 53%, higher than that with T allele. CONCLUSION: This finding was nearly the same as that in studies of the populations in China, Turkey, and four countries in the South European continent. It is recommended to conduct further research on the correlation between C3435T polymorphism and CBZ dose variability to provide a comprehensive approach to epilepsy management in patients receiving CBZ.
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