Displaying publications 221 - 240 of 525 in total

Abstract:
Sort:
  1. Wong HS, Morad Z
    Transplant Proc, 2003 Feb;35(1):230-1.
    PMID: 12591376
    Matched MeSH terms: Immunosuppressive Agents/pharmacokinetics*; Cyclosporine/pharmacokinetics*
  2. Syed MA, Arshad JH, Mat S
    J Environ Sci Health B, 1992 Aug;27(4):347-54.
    PMID: 1527358
    Paddy (unmilled rice), milled rice and maize-bound 14C residues were prepared using 14C-succinate-labelled malathion at 10 and 152 ppm. After 3 months, the bound residues accounted for 12%, 6.5% and 17.7% of the applied dose in paddy, milled rice and maize respectively in the grains treated at 10 ppm. The corresponding values for the 152 ppm were 16.6%, 8.5% and 18.8%. Rats fed milled rice - bound 14C-residues eliminated 61% of the 14C in the faeces and 28% in the urine. The corresponding percentages for paddy and maize were 72%, 9% and 53%, 41% respectively; indicating that bound residues from milled rice and maize were moderately bioavailable. When rice-bound malathion residues (0.65 ppm in feed) were administered to rats in a 5 week feeding study, no signs of toxicity were observed. Plasma and RBC cholinesterase activities were slightly inhibited: blood urea nitrogen was significantly elevated in the test animals. Other parameters examined showed no or marginal changes.
    Matched MeSH terms: Malathion/pharmacokinetics*; Pesticide Residues/pharmacokinetics*
  3. Chin GS, Todo H, Kadhum WR, Hamid MA, Sugibayashi K
    Chem Pharm Bull (Tokyo), 2016;64(12):1666-1673.
    PMID: 27904075
    The current investigation evaluated the potential of proniosome as a carrier to enhance skin permeation and skin retention of a highly lipophilic compound, α-mangostin. α-Mangostin proniosomes were prepared using the coacervation phase seperation method. Upon hydration, α-mangostin loaded niosomes were characterized for size, polydispersity index (PDI), entrapment efficiency (EE) and ζ-potential. The in vitro permeation experiments with dermis-split Yucatan Micropig (YMP) skin revealed that proniosomes composed of Spans, soya lecithin and cholesterol were able to enhance the skin permeation of α-mangostin with a factor range from 1.8- to 8.0-fold as compared to the control suspension. Furthermore, incorporation of soya lecithin in the proniosomal formulation significantly enhanced the viable epidermis/dermis (VED) concentration of α-mangostin. All the proniosomal formulations (except for S20L) had significantly (p<0.05) enhanced deposition of α-mangostin in the VED layer with a factor range from 2.5- to 2.9-fold as compared to the control suspension. Since addition of Spans and soya lecithin in water improved the solubility of α-mangostin, this would be related to the enhancement of skin permeation and skin concentration of α-mangostin. The choice of non-ionic surfactant in proniosomes is an important factor governing the skin permeation and skin retention of α-mangostin. These results suggested that proniosomes can be utilized as a carrier for highly lipophilic compound like α-mangostin for topical application.
    Matched MeSH terms: Liposomes/pharmacokinetics*; Xanthones/pharmacokinetics*
  4. Gan SH, Ismail R
    J Chromatogr B Biomed Sci Appl, 2001 Aug 15;759(2):325-35.
    PMID: 11499486
    An HPLC system using solid-phase extraction and HPLC with UV detection has been validated in order to determine tramadol and o-desmethyltramadol (M1) concentrations in human plasma. The method developed was selective and linear for concentrations ranging from 50 to 3,500 ng/ml (tramadol) and 50 to 500 ng/ml (M1) with mean recoveries of 94.36 +/- 12.53% and 93.52 +/- 7.88%, respectively. Limit of quantitation (LOQ) was 50 ng/ml. For tramadol, the intra-day accuracy ranged from 95.48 to 114.64% and the inter-day accuracy, 97.21 to 103.24%. Good precision (0.51 and 18.32% for intra- and inter-day, respectively) was obtained at LOQ. The system has been applied to determine tramadol concentrations in human plasma samples for a pharmacokinetic study.
    Matched MeSH terms: Analgesics, Opioid/pharmacokinetics; Tramadol/pharmacokinetics
  5. Tan S, Yuen KH, Chan KL
    Planta Med, 2002 Apr;68(4):355-8.
    PMID: 11988862 DOI: 10.1055/s-2002-26751
    A new and simple HPLC method using fluorescence detection was developed to determine 9-methoxycanthin-6-one, an active compound of Eurycoma longifolia Jack in rat and human plasma. The method entailed direct injection of plasma sample after deproteinization using acetonitrile. The mobile phase comprised acetonitrile and distilled water (55 : 45, v/v). Analysis was run at a flow rate of 1.0 ml/min with the detector operating at an excitation wavelength of 371 nm and emission wavelength of 504 nm. The method was specific and sensitive with a detection limit of 0.6 ng/ml and a quantification limit of approximately 1.6 ng/ml. The method was applied in a pilot pharmacokinetic/bioavailability study of the compound in rats. Less than 1 % of the compound was found to be absorbed orally.
    Matched MeSH terms: Oleanolic Acid/pharmacokinetics*; Plant Extracts/pharmacokinetics*
  6. Moshikur RM, Ali MK, Wakabayashi R, Moniruzzaman M, Goto M
    Mol Pharm, 2021 08 02;18(8):3108-3115.
    PMID: 34250805 DOI: 10.1021/acs.molpharmaceut.1c00324
    Coronavirus disease 2019 (COVID-19) has spread across the world, and no specific antiviral drugs have yet been approved to combat this disease. Favipiravir (FAV) is an antiviral drug that is currently in clinical trials for use against COVID-19. However, the delivery of FAV is challenging because of its limited solubility, and its formulation is difficult with common organic solvents and water. To address these issues, four FAV ionic liquids (FAV-ILs) were synthesized as potent antiviral prodrugs and were fully characterized by nuclear magnetic resonance (NMR) spectroscopy, Fourier-transform infrared (FT-IR) spectrometry, powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), derivative thermogravimetry (DTG), and differential scanning calorimetry (DSC). The aqueous solubility and in vivo pharmacokinetic properties of the FAV-ILs were also evaluated. The FAV-ILs exhibited improved aqueous solubility by 78 to 125 orders of magnitude when compared with that of free FAV. Upon oral dosing in mice, the absolute bioavailability of the β-alanine ethyl ester FAV formulation was increased 1.9-fold compared with that of the control FAV formulation. The peak blood concentration, elimination half-life, and mean absorption time of FAV were also increased by 1.5-, 2.0-, and 1.5-fold, respectively, compared with the control. Furthermore, the FAV in the FAV-ILs exhibited significantly different biodistribution compared with the control FAV formulation. Interestingly, drug accumulation in the lungs and liver was improved 1.5-fold and 1.3-fold, respectively, compared with the control FAV formulation. These results indicate that the use of ILs exhibits potential as a simple, scalable strategy to improve the solubility and oral absorption of hydrophobic drugs, such as FAV.
    Matched MeSH terms: Amides/pharmacokinetics; Pyrazines/pharmacokinetics
  7. Akhtar N, Ilyas N, Yasmin H, Sayyed RZ, Hasnain Z, A Elsayed E, et al.
    Molecules, 2021 Mar 12;26(6).
    PMID: 33809305 DOI: 10.3390/molecules26061569
    Plant growth-promoting rhizobacteria (PGPR) mediate heavy metal tolerance and improve phytoextraction potential in plants. The present research was conducted to find the potential of bacterial strains in improving the growth and phytoextraction abilities of Brassica nigra (L.) K. Koch. in chromium contaminated soil. In this study, a total of 15 bacterial strains were isolated from heavy metal polluted soil and were screened for their heavy metal tolerance and plant growth promotion potential. The most efficient strain was identified by 16S rRNA gene sequencing and was identified as Bacillus cereus. The isolate also showed the potential to solubilize phosphate and synthesize siderophore, phytohormones (indole acetic acid, cytokinin, and abscisic acid), and osmolyte (proline and sugar) in chromium (Cr+3) supplemented medium. The results of the present study showed that chromium stress has negative effects on seed germination and plant growth in B. nigra while inoculation of B. cereus improved plant growth and reduced chromium toxicity. The increase in seed germination percentage, shoot length, and root length was 28.07%, 35.86%, 19.11% while the fresh and dry biomass of the plant increased by 48.00% and 62.16%, respectively, as compared to the uninoculated/control plants. The photosynthetic pigments were also improved by bacterial inoculation as compared to untreated stress-exposed plants, i.e., increase in chlorophyll a, chlorophyll b, chlorophyll a + b, and carotenoid was d 25.94%, 10.65%, 20.35%, and 44.30%, respectively. Bacterial inoculation also resulted in osmotic adjustment (proline 8.76% and sugar 28.71%) and maintained the membrane stability (51.39%) which was also indicated by reduced malondialdehyde content (59.53% decrease). The antioxidant enzyme activities were also improved to 35.90% (superoxide dismutase), 59.61% (peroxide), and 33.33% (catalase) in inoculated stress-exposed plants as compared to the control plants. B. cereus inoculation also improved the uptake, bioaccumulation, and translocation of Cr in the plant. Data showed that B. cereus also increased Cr content in the root (2.71-fold) and shoot (4.01-fold), its bioaccumulation (2.71-fold in root and 4.03-fold in the shoot) and translocation (40%) was also high in B. nigra. The data revealed that B. cereus is a multifarious PGPR that efficiently tolerates heavy metal ions (Cr+3) and it can be used to enhance the growth and phytoextraction potential of B. nigra in heavy metal contaminated soil.
    Matched MeSH terms: Chromium/pharmacokinetics*; Soil Pollutants/pharmacokinetics*
  8. Chung WJ, Chan KL, Lee CY
    J Pharm Pharmacol, 2021 Mar 04;73(2):161-168.
    PMID: 33793798 DOI: 10.1093/jpp/rgaa026
    OBJECTIVES: The quassinoids eurycomanone (EN) and 13α,21-dihydroeurycomanone (DHY) of Eurycoma longifolia Jack are reported to enhance spermatogenesis. This study aims to profile the pharmacokinetics of DHY, a minor and hitherto unstudied constituent, evaluate its spermatogenesis enhancement property and compare these attributes with that of the predominant EN.

    METHODS: Crude Eurycoma longifolia extract was chromatographed into a DHY-enriched extract (DHY-F) and an EN-enriched extract (EN-F). Male Sprague-Dawley rats were administered intravenously and orally with both extracts and their plasma levels of both quassinoids were determined. The extracts were then tested for their spermatogenesis augmentation ability in normal rats and an andrographolide-induced oligospermia model.

    KEY FINDINGS: Chromatographic enrichment resulted in a 28-fold increase of DHY in DHY-F and a 5-fold increase of EN in EN-F compared with non-chromatographed crude extracts. DHY showed better oral bioavailability (1.04 ± 0.58%) than EN (0.31 ± 0.19%). At 5 mg/kg, EN exhibited higher efficacy in spermatogenesis enhancement in normal rats and restoration of oligospermia to normal sperm profile versus DHY.

    CONCLUSIONS: Despite the better pharmacokinetic profile of DHY, EN remains the main chemical contributor to plant bioactivity. DHY-F and EN-F represent improvements in developing Eurycoma longifolia as a potential phytomedicine for male infertility particularly oligospermia.

    Matched MeSH terms: Plant Extracts/pharmacokinetics*; Quassins/pharmacokinetics*
  9. Ali MK, Moshikur RM, Wakabayashi R, Moniruzzaman M, Goto M
    ACS Appl Mater Interfaces, 2021 May 05;13(17):19745-19755.
    PMID: 33891816 DOI: 10.1021/acsami.1c03111
    Chemotherapeutic cytotoxic agents such as paclitaxel (PTX) are considered essential for the treatment of various cancers. However, PTX injection is associated with severe systemic side effects and high rates of patient noncompliance. Micelle formulations (MFs) are nano-drug delivery systems that offer a solution to these problems. Herein, we report an advantageous carrier for the transdermal delivery of PTX comprising a new MF that consists of two biocompatible surfactants: cholinium oleate ([Cho][Ole]), which is a surface-active ionic liquid (SAIL), and sorbitan monolaurate (Span-20). A solubility assessment confirmed that PTX was readily solubilized in the SAIL-based micelles via multipoint hydrogen bonding and cation-π and π-π interactions between PTX and SAIL[Cho][Ole]. Dynamic light scattering (DLS) and transmission electron microscopy revealed that in the presence of PTX, the MF formed spherical PTX-loaded micelles that were well-distributed in the range 8.7-25.3 nm. According to DLS, the sizes and size distributions of the micelle droplets did not change significantly over the entire storage period, attesting to their physical stability. In vitro transdermal assessments using a Franz diffusion cell revealed that the MF absorbed PTX 4 times more effectively than a Tween 80-based formulation and 6 times more effectively than an ethanol-based formulation. In vitro and in vivo skin irritation tests revealed that the new carrier had a negligible toxicity profile compared with a conventional ionic liquid-based carrier. Based on these findings, we believe that the SAIL[Cho][Ole]-based MF has potential as a biocompatible nanocarrier for the effective transdermal delivery of poorly soluble chemotherapeutics such as PTX.
    Matched MeSH terms: Antineoplastic Agents, Phytogenic/pharmacokinetics; Paclitaxel/pharmacokinetics
  10. Mohd Sazlly Lim S, Heffernan AJ, Zowawi HM, Roberts JA, Sime FB
    Eur J Clin Microbiol Infect Dis, 2021 Sep;40(9):1943-1952.
    PMID: 33884516 DOI: 10.1007/s10096-021-04252-z
    Due to limited treatment options for carbapenem-resistant Acinetobacter baumannii (CR-AB) infections, antibiotic combinations are commonly used. In this study, we explored the potential efficacy of meropenem-sulbactam combination (MEM/SUL) against CR-AB. The checkerboard method was used to screen for synergistic activity of MEM/SUL against 50 clinical CR-AB isolates. Subsequently, time-kill studies against two CR-AB isolates were performed. Time-kill data were described using a semi-mechanistic pharmacokinetic/pharmacodynamic (PK/PD) model. Subsequently, Monte Carlo simulations were performed to estimate the probability of 2-log kill, 1-log kill or stasis at 24-h following combination therapy. The MEM/SUL demonstrated synergy against 28/50 isolates. No antagonism was observed. The MIC50 and MIC90 of MEM/SUL were decreased fourfold, compared to the monotherapy MIC. In the time-kill studies, the combination displayed synergistic killing against both isolates at the highest clinically achievable concentrations. At concentrations equal to the fractional inhibitory concentration, synergism was observed against one isolate. The PK/PD model adequately delineated the data and the interaction between meropenem and sulbactam. The effect of the combination was driven by sulbactam, with meropenem acting as a potentiator. The simulations of various dosing regimens revealed no activity for the monotherapies. At best, the MEM/SUL regimen of 2 g/4 g every 8 h demonstrated a probability of target attainment of 2-log10 kill at 24 h of 34%. The reduction in the MIC values and the achievement of a moderate PTA of a 2-log10 reduction in bacterial burden demonstrated that MEM/SUL may potentially be effective against some CR-AB infections.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacokinetics*; Sulbactam/pharmacokinetics*
  11. Wong TW
    Recent Pat Drug Deliv Formul, 2009 Jan;3(1):8-25.
    PMID: 19149726 DOI: 10.2174/187221109787158346
    The global burden of diabetes is estimated to escalate from about 171 million in 2000 to 366 million people in 2030. The routine of diabetes treatment by injection of insulin incurs pain and has been one major factor negating the quality of life of diabetic patients. The possibility of administering insulin via alternative routes such as oral and nasal pathways has been investigated over the years, but with insulin experiencing risks of enzymatic degradation and poor transmucosal absorption. This leads to the rising needs to develop new formulation strategies emphasizing on the assembly of insulin and excipients into a physical structure to maintain the stability and increase the bioavailability of insulin. Chitosan and its derivatives or salts have been widely investigated as functional excipients of delivering insulin via oral, nasal and transdermal routes. The overview of various recent patented strategies on non-injection insulin delivery denotes the significance of chitosan for its mucoadhesive and able to protect the insulin from enzymatic degradation, prolong the retention time of insulin, as well as, open the inter-epithelial tight junction to facilitate systemic insulin transport. The chitosan can be employed to strengthen the physicochemical stability of insulin and multi-particulate matrix. The introduction of chitosan coat or co-formulation of chitosan with cationic gelatin or electrolytes which provide solidified or partially crosslinked structures retain and/or enhance the positive charges of dosage form necessary to induce mucoadhesiveness. The chitosan is modifiable chemically to produce water-soluble low molecular weight polymer which renders insulin able to be processed under mild conditions, and sulphated chitosan which markedly opens the paracellular channels for insulin transport. Combination of chitosan and fatty acid as hydrophobic nanoparticles promotes the insulin absorption via lymphoid tissue. Attainment of optimized formulations with higher levels of pharmacological bioavailability is deemed possible in future through targeted delivery of insulin using chitosan with specific adhesiveness to the intended absorption mucosa.
    Matched MeSH terms: Hypoglycemic Agents/pharmacokinetics; Insulin/pharmacokinetics
  12. Lee CY, Sim SM, Cheng HM
    Nutr Res, 2008 Aug;28(8):555-63.
    PMID: 19083460 DOI: 10.1016/j.nutres.2008.05.001
    The use of a high quercetin dose to demonstrate its absorption and bioavailability does not reflect the real dietary situation because quercetin glycosides are usually present in small amounts in the human diet. This study aimed to demonstrate the absorption and bioavailability of quercetin in mulberry leaves that represents a more physiologic dietary situation. Mulberry leaf ethanol extract was prepared similar to tea infusion, which is the way the tea leaves are generally prepared for consumption. Accordingly, rats were fed by oral intubation the mulberry leaf ethanol extract (15 g%/rat per day) or pure rutin (135 microg/rat per day) for 2 weeks. The control group received a similar volume of the vehicle, 10% ethanol. There was a significant increase in total antioxidant activity (TAA) in the urine and feces of the antioxidants-fed rats. Phenylacetic acid, a microbial metabolite of quercetin, was detected in the urine of the test animals, and quercetin was present in the fecal samples. By using an in situ intestinal preparation, 3-hydroxyphenylacetic acid, another microbial metabolite of quercetin, was detected in the plasma when the duodenal segment was instilled with 2 mg of rutin. This microbial metabolite retained 50% of the TAA of quercetin. The results of this study indicate that in a more realistic dietary situation, an increase in TAA in the body after consumption of quercetin-containing foods is contributed mainly by the microbial metabolites.
    Matched MeSH terms: Plant Extracts/pharmacokinetics; Quercetin/pharmacokinetics
  13. Rasool AH, Rahman AR, Yuen KH, Wong AR
    Arch Pharm Res, 2008 Sep;31(9):1212-7.
    PMID: 18806966 DOI: 10.1007/s12272-001-1291-5
    The tocotrienol vitamin E has potent antioxidant property, however absorption is low due to high lipid solubility. A self emulsifying preparation of tocotrienol rich vitamin E (SF-TRE) had been reported to increase their bioavailability. This randomized, placebo controlled, blinded end point clinical study aimed to determine the effects of 50, 100 and 200 mg daily of SF-TRE and placebo for two months on arterial compliance and vitamin E blood levels. Assessment of arterial compliance by carotid femoral pulse wave velocity (PWV) and augmentation index (AI), plasma vitamin E, serum total cholesterol and low density lipoprotein cholesterol were taken before and after 2 months' treatment in 36 healthy males. Un-supplemented tocotrienol levels were low, after treatment, all SF-TRE treated groups had significantly higher plasma alpha, delta and delta tocotrienol concentrations compared to placebo. Augmentation index change from baseline to end of treatment for groups placebo, 50, 100, and 200 mg were 2.22+/-1.54, -6.59+/-2.84, -8.72+/-3.77, and -6.27+/-2.67% respectively (p=0.049, 0.049, and 0.047 respectively). Groups 100 and 200 mg showed significant improvement after treatment with pulse wave velocity reductions of 0.77 m/s and 0.65 m/s respectively (p=0.007 and p=0.002). There was no effect of SF-TRE on serum lipids. We conclude that there was a trend towards improvement in arterial compliance with 2 months' of SF-TRE.
    Matched MeSH terms: Antioxidants/pharmacokinetics; Tocotrienols/pharmacokinetics
  14. Saravanan M, Bhaskar K, Maharajan G, Pillai KS
    J Drug Target, 2011 Feb;19(2):96-103.
    PMID: 20380621 DOI: 10.3109/10611861003733979
    We have previously reported on the targeting of diclofenac sodium in joint inflammation using gelatin magnetic microspheres. To overcome complications in the administration of magnetic microspheres and achieve higher targeting efficiency, the present work focuses on the formulation of gelatin microspheres for intra-articular administration. Drug-loaded microspheres were prepared by the emulsification/cross-linking method, characterized by drug loading, size distribution, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), gas chromatography, and in vitro release studies. The targeting efficiency of microspheres was studied in vivo in rabbits. The microspheres showed drug loading of 9.8, 18.3, and 26.7% w/w with an average size range of 37-46 µm, depending upon the drug-polymer ratio. They were spherical in nature and free from surface drug as evidenced by the SEM photographs. FT-IR, DSC, and XRD revealed the absence of drug-polymer interaction and amorphous nature of entrapped drug. Gas chromatography confirms the absences of residual glutaraldehyde. The formulated microspheres could prolong the drug release up to 30 days in vitro. About 81.2 and 43.7% of administered drug in the microspheres were recovered from the target joint after 1 and 7 days of postintra-articular injection, respectively, revealing good targeting efficiency.
    Matched MeSH terms: Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics; Diclofenac/pharmacokinetics
  15. Chik Z, Basu RC, Pendek R, Lee TC, Mohamed Z
    Clin Ther, 2010 Sep;32(10):1822-31.
    PMID: 21194606 DOI: 10.1016/j.clinthera.2010.09.006
    Rifampicin is a semisynthetic antibiotic derivative of rifamycin used worldwide for the treatment of various forms of tuberculosis.
    Matched MeSH terms: Antibiotics, Antitubercular/pharmacokinetics*; Rifampin/pharmacokinetics*
  16. Haron H, Shahar S, O'Brien KO, Ismail A, Kamaruddin N, Rahman SA
    Int J Food Sci Nutr, 2010 Mar;61(2):125-37.
    PMID: 19995131 DOI: 10.3109/09637480903348080
    Assessment of calcium bioavailability from non-dairy foods containing moderate amounts of calcium is especially important in populations that have habitually low dairy consumption. Absorption of calcium from milk and tempeh (a traditional fermented soy product) was compared in a sample of Malay subjects. A randomized, crossover design was utilized to assess calcium absorption in 20 postmenopausal women from either a glass of milk (114 g) or from a meal of tempeh (206 g); each containing 130 mg calcium. At each study of Phase 1 (mid-July) and Phase 2 (mid-August), intravenous (42)Ca and oral (44)Ca were administered and calcium absorption was measured in 24-h urine collections post-dosing; with a 1-month washout period between phases. Absorption of calcium from tempeh did not differ significantly from milk (36.9 +/- 10.6% vs. 34.3 +/- 8.6%, respectively). Due to differences in the calcium content of tempeh, four servings of this product would be needed to get the same amount of absorbed calcium as that obtained from a 4-ounce glass of milk. Tempeh may provide readily available calcium for this population of women at risk for low bone mass.
    Matched MeSH terms: Calcium/pharmacokinetics*; Calcium, Dietary/pharmacokinetics*
  17. Koh KH, Tan HH
    Med J Malaysia, 2006 Mar;61(1):109-11.
    PMID: 16708747 MyJurnal
    Acute severe intoxication with carbamazepine is associated with seizures, coma and respiratory depression. Traditionally, charcoal haemoperfusion is used to remove the drug. We present a case of carbamazepine intoxication, successfully treated with three hours of high-flux haemodialysis. Thus, haemodialysis using high-flux membranes is a feasible and effective therapeutic option for carbamazepine intoxication.
    Matched MeSH terms: Anticonvulsants/pharmacokinetics; Carbamazepine/pharmacokinetics
  18. Hong Ng C, Norman TR, Naing KO, Schweitzer I, Kong Wai Ho B, Fan A, et al.
    Int Clin Psychopharmacol, 2006 Mar;21(2):87-92.
    PMID: 16421459
    This prospective 6-week study examined the differences in dosage and steady state plasma concentrations of sertraline in Chinese versus Caucasian depressed patients. Two groups of Chinese patients from different geographical sites and a group of Caucasian patients were evaluated with clinical measures during an initial dose of 50 mg/day, with subsequent doses adjusted clinically. The results of 17 Australian Chinese (ACHI), 13 Malaysian Chinese (MCHI) and 15 Australian Caucasians (AC) were analysed. Despite controlling for weight, the AC subjects received a significantly higher dose than both the ACHI (P = 0.002) and the MCHI groups (P = 0.012). However, the mean sertraline concentration to dose ratios at weeks 1 and 6 were not significantly different between the three groups. Sertraline was effective and well tolerated in both ethnic groups with few adverse events. Although there was a lack of difference between groups in the pharmacokinetic results, Chinese depressed patients appeared to require lower dosages with consequently lower plasma concentrations of sertraline compared to Caucasian patients to achieve clinical efficacy. Further studies of the dosages, kinetics and adverse effects of selective serotonin reuptake inhibitors linked with genotyping are necessary.
    Matched MeSH terms: Antidepressive Agents/pharmacokinetics*; Sertraline/pharmacokinetics*
  19. Das B, Sarkar C, Biswas R, Pandey S
    Pak J Pharm Sci, 2008 Jan;21(1):78-87.
    PMID: 18166524
    Glycopeptide antibiotics represent an important class of microbial compounds produced by several genera of actinomycetes. The emergence of resistance to glycopeptides among enterococci and staphylococci has prompted the search for second-generation drugs of this class and semi-synthetic derivatives are currently under clinical trials. Antimicrobial resistance among gram-positive organisms has been increasing steadily during the past several decades. Dalbavancin, a novel lipoglycopeptide, has a mechanism of action similar to that of other glycopeptides. It has in vitro activity against a variety of Gram-positive organisms specially multidrug resistant Staphylococcus aureus, but no activity against Gram-negative or vancomycin-resistant enterococci that possess vanA gene. Due to its prolonged half-life (6-10 days), dalbavancin can be administered intravenously once weekly. In Phase II and III clinical trials, dalbavancin was effective and well-tolerated for the treatment of skin and soft-tissue infections, catheter-related bloodstream infections, and skin and skin-structure infections. To date, adverse events have been mild and limited; the most common being pyrexia, headache, diarrhea. Dalbavancin appears to be a promising antimicrobial agent for the treatment of Gram-positive infections. Additional clinical data are required to fully assess its use. Despite the remarkable and favorable pharmacokinetic and pharmacodynamic properties, the use of this potent agent should be restricted to severe infections due to multidrug resistant organisms to limit the risk of selection of resistance. It is active against Gram-positive aerobes and anerobes, including resistant pathogens, with the exception of strains producing vanA-mediated resistance. Its approval by the FDA is expected soon. The extent to which dalbavancin will supplant vancomycin and whether it will be preferred over other newer agents such as linezolid in the next decade remains to be seen.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacokinetics; Teicoplanin/pharmacokinetics
  20. Ling SS, Magosso E, Khan NA, Yuen KH, Barker SA
    Drug Dev Ind Pharm, 2006 Mar;32(3):335-45.
    PMID: 16556538
    A liposome system was evaluated for oral delivery of a poorly bioavailable hydrophilic drug. The system was prepared from proliposome, which consisted of negatively charged phosphatidylcholine, whereas cefotaxime was chosen as the model drug. An in vivo study was carried out on nine rats according to a three-way crossover design to compare the oral bioavailability of cefotaxime from the liposomal formulation with that of an aqueous drug solution and a physical mixture of cefotaxime with blank liposomes. The results indicated that the extent of bioavailability of cefotaxime was increased approximately 2.7 and 2.3 times compared with that of the aqueous solution and the physical mixture, respectively. In a separate study, simultaneous determination of cefotaxime in intestinal lymph (collected from the mesenteric lymph duct) and in plasma (collected from the tail vein) revealed that its concentration was consistently higher in the lymph than in the plasma when administered via the liposomal formulation, whereas the reverse was observed with the aqueous solution. Thus, the results indicated that the liposomes system has the potential of increasing the oral bioavailability of poorly bioavailable hydrophilic drugs and also promote their lymphatic transport in the intestinal lymph.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacokinetics*; Cefotaxime/pharmacokinetics*
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links