Abstract：
:The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct = 226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compared with HCO-60 micellar and plasma solutions of sudan II, the blood concentration of sudan II was markedly elevated by administration as a lipid emulsion. However, the distribution of sudan II to the liver, lungs, spleen, and adipose tissue was not altered, and that to the brain, heart, kidneys, muscle, and tumor was slightly decreased. To understand these results, pharmacokinetic analysis was performed using a newly derived compartmental model, and moreover, the organ distribution clearance was analyzed. It was suggested that the oil particles deliver the incorporated drug selectively to the liver, lungs, and spleen, and the speed of delivery could be surpressed by using HCO-60. However, in the case of sudan II, its rapid release from the oil particles after i.v. injection prevented a drastic alteration in the distribution of sudan II. The simulation studies suggested that a considerable decrease in the release rate or an increase in partition coefficient (experimentally more than 10(8) would be required for delivery.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Sakaeda T,Takahashi K,Nishihara Y,Hirano Kdoi
10.1248/bpb.17.1490subject
Has Abstractpub_date
1994-11-01 00:00:00pages
1490-5issue
11eissn
0918-6158issn
1347-5215journal_volume
17pub_type
杂志文章abstract：:Microvessels are composed of endothelial cells that cover the luminal surface and pericytes that wrap around and along endothelial cells. In the present study, we investigated the regulation of fibrinolysis in cultured human brain microvascular pericytes and endothelial cells after exposure to thrombin. It was found t...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.208
更新日期：2005-02-01 00:00:00
abstract：:It is therapeutically important to elucidate the factors involved in the radiation resistance of tumors. We previously showed that ATP is released from mouse melanoma B16 cells in response to γ-irradiation, but the role of adenosine, a metabolite of ATP, is still unclear. Here, we show that the adenosine A2B receptor ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b19-00976
更新日期：2020-03-01 00:00:00
abstract：:Glucocorticoids are effective drugs for the treatment of allergic skin diseases. In the present study, we observed the effects of prednisolone on the cutaneous reaction and skin barrier function in mice treated with a hapten, 2,4-dinitrofluorobenzene. Repeated hapten application onto the mouse ear resulted in a potent...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.26.618
更新日期：2003-05-01 00:00:00
abstract：:Two acidic polysaccharides, called ginsenan S-IA and ginsenan S-IIA, were isolated from the root of Panax ginseng C. A. Meyer. They were homogeneous on electrophoresis and gel chromatography, and their molecular masses were estimated to be 5.6 x 10(4) and 1.0 x 10(5), respectively. Ginsenan S-IA is composed of L-arabi...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.16.1087
更新日期：1993-11-01 00:00:00
abstract：:Plant phenolic compounds isolated from a 70% aqueous acetone extract of the leaves of Malus doumeri A. CHEV. var. formosana (KAWAK. & KOIDZ.) S. S. YING, a type of Taiwanese indigenous plant, were evaluated for potential application in the field of skin care. A phytochemical investigation of the active fractions resul...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.29.740
更新日期：2006-04-01 00:00:00
abstract：:Metronidazole (MTZ) ointment has been used widely as a hospital preparation against cancerous malodor. Although cancerous tissue with ulcer-like symptoms is likely to have a higher capacity to absorb drugs than normal skin, the extent to which MTZ is absorbed when a topical preparation is applied to cancerous tissue r...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b12-00687
更新日期：2013-01-01 00:00:00
abstract：:Physiological cell death is an essential event in normal development and maintenance of homeostasis. Recently, the morphological and pharmacological characteristics of programmed cell death, which are distinct from those of apoptosis under physiological and pathological conditions, have been reported. However, the mol...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.34.1589
更新日期：2011-01-01 00:00:00
abstract：:It has been recently reported that the consumption of a high-fat diet during pregnancy exerts various effects on fetuses and newborn mice. The purpose of this study was to determine the effects of a high-fat diet during pregnancy on the expression of cytochrome P450 (CYP) in the livers of offspring. Mouse dams were fe...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b12-01017
更新日期：2013-01-01 00:00:00
abstract：:The adsorption characteristics of eight adsorbents, cholestyramine, colestimide, aluminum silicate, sucralfate, aluminum hydroxide, calcium polystyrene sulfonate, carbon sphere and medicinal carbon, on the drugs such as methotrexate, antidepressants, mizoribine and ciprofloxacin hydrochloride were investigated in vitr...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.841
更新日期：2005-05-01 00:00:00
abstract：:Acute biliary pancreatitis (ABP) with a high mortality rate is an incurable digestive system disease induced by abnormal bile acid regurgitation due to the biliary obstruction. Dehydrocholic acid (DA) alleviates the severity of cholestatic hepatitis related to biliary inflammation, suggesting DA is potential to develo...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b20-00021
更新日期：2020-01-01 00:00:00
abstract：:We determined the in vivo and in vitro antitumor activities of gambogic acid (GA) and one of the possible mechanisms for its inhibitory activities. In vivo antitumor activity of GA was evaluated by the relative tumor growth ratio (T/C) in nude mice, and in vitro inhibition of SPC-A1 cells was measured by 3-(4,5-dimeth...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.1769
更新日期：2004-11-01 00:00:00
abstract：:Nonalcoholic steatohepatitis (NASH) is the most frequent cause of liver dysfunction and a common global problem. Gypenosides can decrease pathological modifications of high-fat diet-induced rat atherosclerosis; however, its effect and mechanism on NASH remain unclear. In this study, rats were randomly divided into nor...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b16-00942
更新日期：2017-01-01 00:00:00
abstract：:The overproduction of nitric oxide (NO) by inducible nitric oxide synthase (iNOS) switches the function of NO from a physiological neuromodulator to a neurotoxic effector in central nervous system (CNS) after brain injury. From the methanol extracts of Psoralea corylifolia, we purified two inhibitors of NO production ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.2253
更新日期：2005-12-01 00:00:00
abstract：:To develop a piroxicam-loaded gelatin microcapsule with enhanced bioavailability, a gelatin microcapsule encapsulated ethanol and piroxicam has been formulated by using gelatin as a water-soluble polymer shell. The aqueous solubility and bioavailability of piroxicam in piroxicam-loaded microcapsule in rats were then e...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.1284
更新日期：2008-06-01 00:00:00
abstract：:Ras, a small G-protein, physiologically directs cell proliferation and cell cycle via regulation of mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) signaling cascade. Dysregulation of Ras/MEK/ERK signaling has been reported to cause tumorigenesis and gliomas. Nobiletin, a citr...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b12-00824
更新日期：2013-01-01 00:00:00
abstract：:We recently suggested that the transferrin (Tf)-gallium-67 (67Ga) complex dissociated on the surface of the hepatocytes after partial hepatectomy and free 67Ga bound to heparan sulfate in the extracellular matrix. In the present study, we investigated whether the entering of indium-111 (111In) and iron-59 (59Fe) with ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.1193
更新日期：2004-08-01 00:00:00
abstract：:Digitalis has been used to treat congestive heart failure for more than 200 years, although the dual effects (proliferation and death) induced by digitalis on cell growth have been known for many years, the mechanisms by which digitalis causes the actions were not completely known. The aim of this work was to characte...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.30.247
更新日期：2007-02-01 00:00:00
abstract：:The improvement of diabetic complications such as lipid lowering and anti-oxidative potential of Hydrangea Dulcis Folium (HDF) was studied in streptozotocin-induced diabetic rats. Male Sprague-Dawley rats were divided into 3 groups after induction of streptozotocin (STZ)-diabetes: normal control; diabetic control; dia...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.32.153
更新日期：2009-01-01 00:00:00
abstract：:The effect of pulsed output ultrasound (1 MHz) with on/off ratios of 1:2, 1:4 and 1:9 on transdermal absorption of indomethacin from an ointment was studied in rats. Ultrasound energy was supplied for between 10 and 19 min at a range of intensities (1.0-2.5 W.cm-2), energy levels commonly used for therapeutic purposes...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.20.288
更新日期：1997-03-01 00:00:00
abstract：:The present study describes the activity of Ca(2+)-ATPase in liver plasma membrane and cytosolic-free Ca2+ concentration ([Ca2+]i) in an individual vital cell in mouse liver 18 h after endotoxin administration. Ca(2+)-ATPase activity in liver plasma membrane in the poisoned mice was markedly decreased to 28% of that i...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.16.808
更新日期：1993-08-01 00:00:00
abstract：:Costunolide is an active compound isolated from the root of Saussurea lappa Clarks, a Chinese medicinal herb, and is considered a therapeutic candidate for various types of cancers. Nevertheless, the pharmacological pathways of costunolide are still unknown. In this study, we investigate the effects of costunolide on ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.24.303
更新日期：2001-03-01 00:00:00
abstract：:It has been identified that skeletal muscle is an endocrine tissue. Since skeletal muscle aging affects not only to muscle strength and function but to systemic aging and lifespan, myokines secreted from skeletal muscle may be crucial factors for intertissue communication during aging. In the present study, we investi...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b17-00969
更新日期：2018-01-01 00:00:00
abstract：:The purpose of this study was to investigate the absorption behavior of an ophthalmic drug injected in rabbit periocular tissues. After intracapsular, retrobulbar and palpebral conjunctival injections of 150 microl and 50 microl fluorescein isothiocyanate dextran (FITC-dextran, average molecular weight 11000), leakage...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.22.956
更新日期：1999-09-01 00:00:00
abstract：:Escherichia coli BM2506 produced macrolide 2'-phosphotransferase II [MPH (2') II]. A gene for MPH (2') II, designated mphB, is located on plasmids pTZ3721 and pTZ3723 in E. coli BM2506. In the present study, we determined the nucleotide sequence of the 6.5-kb EcoRI-PstI fragment containing mphB on pTZ3721. The DNA reg...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.22.227
更新日期：1999-02-01 00:00:00
abstract：:In order to treat a hyperammonemic patient with adult-onset type-II citrullinemia (CTLN2), sodium phenylacetate powder was prepared from chemical reagent grade phenylacetic acid in Gunma University Hospital. After purification by recrystalization, phenylacetic acid was neutralized with sodium carbonate and dried at 70...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.25.1244
更新日期：2002-09-01 00:00:00
abstract：:Mouse brain microsomes contain an amidase that catalyzes the hydrolysis of N-arachidonylethanolamide to arachidonic acid and ethanolamine. The enzymatic activity is dependent on the protein concentration of the microsomes and observed over a wide range of pH, 7.4 to 9.5. Kinetic analysis indicated that K(m) (microM) a...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.19.1109
更新日期：1996-08-01 00:00:00
abstract：:The aim of the present study was to evaluate the effect of the aqueous extract of seeds of two varieties, namely a country and hybrid variety of Momordica charantia (MCSEt1 and MCSEt2) on oxidative stress in plasma and pancreas of streptozotocin (STZ) induced diabetic rats. Oral administration of each of the seed extr...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.978
更新日期：2005-06-01 00:00:00
abstract：:The effects of the plant isoflavones, daidzin and genistin, on bone loss in ovariectomized (ovx) rats fed a calcium-deficient diet were investigated. Daidzin and genistin were orally administered to ovx rats for 4 weeks. The femurs of these rats showed significantly lower density, strength (breaking forces), ash weigh...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.21.62
更新日期：1998-01-01 00:00:00
abstract：:Schizophyllan (SPG) is used to treat cervical cancer in combination with irradiation to enhance the immunological surveillance system. Dectin-1 is a cell surface receptor for 1,3-beta-glucan. In this study, we prepared two anti-Dectin-1 monoclonal antibodies, 4B2 and SC30 having a K(D) of 7.04 x 10(-8) M and 1.55 x 10...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.30.1384
更新日期：2007-08-01 00:00:00
abstract：:The in vitro antimalarial activity against human malaria parasite (Plasmodium falciparum, FCR-3 strain) was examined using 59 triterpenoids obtained during studies on the triterpenic constituents of Cimicifuga spp. The 50% effective concentration values (EC50) of 25 active triterpenoids were 1.0-3.0 microM, and 19 of ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.21.823
更新日期：1998-08-01 00:00:00
