Numerous knockout mouse studies have revealed that P-glycoprotein (P-gp) significantly limits drug distribution across the blood-brain barrier (BBB). To determine importance of P-gp at human BBB, we developed a state-of-the-art, noninvasive, quantitative imaging technique to measure activity by use carbon 11-labeled verapamil as substrate and cyclosporine (INN, ciclosporin) inhibitor.In brief, 11C-verapamil (approximately 0.2 mCi/kg) was administered healthy volunteers (n = 12 [6 women 6...

The multiple-drug resistance (MDR) transporter P-glycoprotein (P-gp) is highly expressed at the human blood–brain barrier (BBB). P-gp actively effluxes a wide variety of drugs from central nervous system, including anticancer drugs. We have previously demonstrated activity BBB using PET ¹¹C-verapamil distribution into brain in absence and presence inhibitor cyclosporine-A (CsA). Here we extend initial noncompartmental analysis these data apply compartmental modeling to verapamil...

To predict the magnitude of P-glycoprotein (P-gp)-based drug interactions at human blood-brain barrier (BBB), rodent studies are routinely conducted where P-gp is chemically inhibited. For such to be predictive BBB, plasma concentration inhibitor must comparable with that observed in clinic. Therefore, we determined vivo EC₅₀ inhibition rat BBB using verapamil as a model substrate and cyclosporine A (CsA) inhibitor. Under isoflurane anesthesia, male Sprague-Dawley rats were...

Tamarind water extract has been shown to demonstrate an anti-obesity effect. In this research, long-term use of tamarind pulp safety was evaluated. extracted by reflux method, followed freeze-drying obtain dry extract. Wistar rats were divided into six groups, with 20 animals each sex per group. The control group and satellite received carboxymethylcellulose sodium (CMC-Na) 0.5% 1 mL/100 g bw (body weight) day. Treatment groups at doses 75, 200, 1000, 1000 mg/kg day for months. After months,...

Abstract Background Gut microbiota is pivotal in maintaining children's health and well-being. The ingestion of enteric pathogens dysbiosis lead to Environmental Enteric Dysfunction (EED), which essential stunting pathogenesis. roles gut microbiome infections have not been explored comprehensively relation childhood Indonesia. This study aimed determine the correlation between composition, infections, growth biomarker, Insulin-like Growth Factor 1 (IGF-1), stunted children from Pidie, Aceh,...

Aims To investigate uptake of fluconazole into the interstitial fluid human subcutaneous tissue using microdialysis and suction blister techniques. Methods A sterile probe (CMA/60) was inserted subcutaneously upper arm five healthy volunteers following an overnight fast. Blisters were induced on lower gentle prior to ingestion a single oral dose (200 mg). Microdialysate, blood sampled over 8 h. Fluconazole concentrations determined in each sample validated HPLC assay. In vivo recovery from...

The aim of this study was to investigate the acute and subchronic toxicity a film formulation that combines κ-Carrageenan konjac glucomannan for soft capsule application. For study, dose 2000 mg/kg body weight (bw) suspension administered orally rats. animals were observed toxic symptoms mortality daily 14 days. In suspension, at doses 10, 30 75 bw 28 days, After rats sacrificed hematological, biochemical histological examination. neither signs nor death among up days experimental period....

A simple and rapid high-performance liquid chromatography (HPLC) was developed to determine the plasma level of nifedipine in rats after its single administration combination with herbs. Nifedipine extracted acetonitrile precipitate protein from samples. The separation implemented on a C 18 column mobile phase acetonitrile: water (63:37, v/v). calibration curve displayed good linearity 30–1000 ng/mL range. lower limit quantification (LLOQ) 30 ng/mL. intraday interday assay accuracy precision...

The bioavailability of two 300 mg irbesartan (CAS 138402-11-6)/12.5 hydrochlorothiazide 58-93-5) tablet formulations was compared, using Co-Irvell® tablets as test formulation and the originator product reference formulation. Twenty-four subjects were included in this single-dose, open-label, randomized two-way crossover study following an overnight fasting. A two-week wash-out period applied. Blood samples drawn up to 48 h drug administrations. Irbesartan plasma concentrations determined by...

Abstract A simple and reliable high-performance liquid chromatography method for simultaneous quantitation of gliclazide ciprofloxacin in plasma sample has been developed validated. This implements protein precipitation, a practical pretreatment by the addition acetonitrile that gives clean supernatant. The separation was carried out system consisted C18 column with KH2PO4 (0.01 M, 0.1% v/v triethylamine, pH 2.7) as mobile phase gradient elution at total flow-rate 1 mL/min. Gliclazide were...

Ekstrak kunyit dan bawang putih telah diketahui mempunyai efek antidiabetik, tetapi mekanisme kerjanya belum diketahui. Penelitian ini mengamati tiga ekstrak rimpang (Curcuma longa L.) ( Allium sativum L.), yaitu heksan, etil asetat, etanol terhadap kadar glukosa darah dengan tes toleransi glukosa. Selanjutnya, yang paling efektif komponen aktifnya (kurkuminoid S-metil sistein) diuji insulin. Empat puluh ekor tikus galur Wistar dibagi menjadi 8 kelompok, kelompok normal, hanya diberi emulsi...

KELARUTAN DAN STABILITAS KIMIA KOMPLEKS DIDANOSIN DENGAN NIKOTINAMID ATAU L-ARGININ . Didanosin (DDI) adalah obat anti HIV yang bekerja dengan menghambat enzim reverse transkriptase bertanggung jawab dalam replikasi virus HIV. Ketersediaan hayati DDI pada pemberian secara oral sangat buruk akibat terhidrolisis suasana asam. Penelitian ini bertujuan untuk mengetahui pengaruh pembentukan kompleks antara NKT atau ARG terhadap kelarutan dan stabilitas kimia DDI. Kompleks DDI-NKT dibuat metode...

To compare the bioavailability of two dexamethasone (CAS 50-02-2) tablet formulations–4 mg Dexmethsone^® tablets as test formulation and 4 originator product reference formulation. The study was conducted according to an open-label, randomized two-way crossover design with a one-week washout period. Twenty-four volunteers received single dose different formulations. Blood samples for pharmacokinetic profiling were taken up 24 h after drug administration in fasting condition. Plasma...

Nigella sativa oil (NSO) has been used widely for its putative anti-hyperglycemic activity. However, little is known about potential effect on the pharmacokinetics and pharmacodynamics of antidiabetic drugs, including gliclazide. This study aimed to investigate herb-drug interactions between gliclazide NSO in rats. Plasma concentrations (single oral intravenous dose 33 26.4 mg/kg, respectively) presence absence co-administration with (52 mg/kg per oral) were quantified healthy insulin...