Abstract:
:The bioavailability of morphine after rectal administration using three types of suppositories containing morphine hydrochloride (10 mg) in different added forms was evaluated in rabbits. Three types of suppositories were constructed with a base material (Witepsol H-15): a conventional suppository containing morphine hydrochloride mixed with a base material, a hollow-type suppository containing morphine in an aqueous solution in its cavity, and a hollow-type suppository containing morphine as a powder (hydrochloride salt) in its cavity. The plasma concentrations of morphine and its metabolites, morphine-3-glucuronide (M-3-G) and morphine-6-glucuronide (M-6-G), were determined. The mean AUC0-6 of morphine after rectal administration of the hollow-type suppository containing powdered morphine was significantly higher than that after the administration of a conventional suppository, whereas the mean AUC0-6 of M-3-G was lower than that after administration of a conventional suppository. The mean AUC0-6 of M-6-G by a hollow-type suppository containing powdered morphine was higher than that by a conventional suppository. Although the mean AUC0-6 ratio of M-3-G to morphine after administration of a conventional suppository was three times larger than that of a hollow-type suppository containing powdered morphine, the mean AUC0-6 ratios of M-6-G to morphine after use of the three types of suppositories were all approximately 1.0. This study demonstrates that the hollow-type suppository containing powdered morphine is a more effective rectal dosage vehicle than the conventional suppository.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Matsumoto Y,Watanabe Y,Yamamoto I,Matsumoto Mdoi
10.1248/bpb.16.150subject
Has Abstractpub_date
1993-02-01 00:00:00pages
150-3issue
2eissn
0918-6158issn
1347-5215journal_volume
16pub_type
杂志文章abstract::Tumor necrosis factor alpha (TNFalpha) generates a potent cytotoxic effect, however many cancer cells are resistant to TNFalpha-mediated killing and the cause of the differential sensitivity remains to be elucidated. In this study, we demonstrated that TNFalpha induced cell death in four different human colon cancer c...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.23.420
更新日期:2000-04-01 00:00:00
abstract::The constituents of the leaves of Garcinia intermedia and heartwood of Calophyllum brasiliense were investigated based on their trypanocidal activity against epimastigotes of Trypanosoma cruzi, the etiologic agent of Chagas' disease. As the active components, the polyisoprenylated benzophenone derivative guttiferone A...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.27.141
更新日期:2004-01-01 00:00:00
abstract::The roles of OmpC and OmpF in acidic resistance (AR) were examined. When ompC and ompF were deleted, AR was decreased. The decreased level of AR seen in the mutant that was deficient in ompC and ompF was elevated by the addition of glutamate, but not by the addition of arginine or lysine. The expression levels of adiA...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.34.330
更新日期:2011-01-01 00:00:00
abstract::Our previous study using apoptosis analysis suggested that Ca(2+) release through inositol 1,4,5-trisphosphate (IP3) receptors and the subsequent Ca(2+) influx through store-operated channels (SOCs) constitute a triggering signal for H2O2-induced β-cell apoptosis. In the present study, we further examined the obligato...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00396
更新日期:2015-01-01 00:00:00
abstract::The permeability of insulin across Xenopus pulmonary membrane and the effects of various absorption enhancers on insulin permeability were examined using an in vitro Ussing chamber technique. Absorption enhancers used in this study were sodium caprate (NaCap), sodium glycocholate (NaGC), sodium salicylate (NaSal) and ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.24.385
更新日期:2001-04-01 00:00:00
abstract::Meiosis activating sterol (MAS), the intermediate of cholesterol biosynthesis, is an important substance to stimulate oocytes maturation in FSH-induced signal transduction pathway. Lanosterol 14alpha-demethylase (CYP51) converts lanosterol to MAS. Although MAS is firstly isolated from bovine testis, the information ab...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.430
更新日期:2006-03-01 00:00:00
abstract::Compound C is a widely used chemical inhibitor that down-regulates AMP-activated protein kinase (AMPK) activity. However, it has been suggested that compound C exerts AMPK-independent effects in various cells. Here, we investigated whether compound C induces Sestrin2 (SESN2), an antioxidant enzyme induced by diverse s...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00938
更新日期:2016-01-01 00:00:00
abstract::Permeation enhancement of ketoprofen (KP) from supersaturated systems and the effects of antinucleant polymers on both stability and permeation of supersaturated KP were investigated using silicone membrane as a skin model. The supersaturation was prepared by the cosolvent technique with water and propylene glycol (PG...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1684
更新日期:2005-09-01 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::Three antiinflammatory saponin components were isolated from the alkaline hydrolysate of a butanol-soluble portion of Kalopanax pictus bark extract through an in vivo activity-guided fractionation procedure. The hydrolysate showed inhibition of adjuvant induced arthritis in rats. After further fractionation, the ethyl...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.26.429
更新日期:2003-04-01 00:00:00
abstract::As one of the adverse effects of oxaliplatin, a key agent in colon cancer chemotherapy, a taste disorder is a severe issue in a clinical situation because it decreases the quality of life of patients. However, there is little information on the mechanism underlying the oxaliplatin-induced taste disorder. Here, we exam...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00935
更新日期:2016-01-01 00:00:00
abstract::Although hypokalemia is an adverse effect of Yokukansan preparation, especially in geriatric patients, its association with age is unclear. We investigated whether age is a risk factor for hypokalemia. This single-center retrospective cohort study, conducted at Tokyo Women's Medical University, Medical Center East bet...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b20-00476
更新日期:2020-01-01 00:00:00
abstract::Morinda citrifolia L., known as noni, originated from Indonesia exhibits various pharmacological activities including anti-inflammatory properties. However, the validity of noni fruit juice as a treatment for rheumatoid arthritis (RA), an autoimmune disorder, has not been confirmed yet. Therefore, the main purpose of ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b18-00480
更新日期:2019-01-01 00:00:00
abstract::In order to clarify that squalene monohydroperoxide (SQOOH) correlates with changes in morphology through cytotoxicity and establish in vitro evaluation of the cytotoxicity of lipid hydroperoxide, the effect of SQOOH on cytotoxicity and morphology in normal human epidermal keratinocytes (NHEK(B)) and the Gunze three-d...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.605
更新日期:2002-05-01 00:00:00
abstract::Curcumin, a bioactive component in tumeric, has been shown to exert antioxidant, anti-inflammatory, anticarcinogenic, hepatoprotective, and neuroprotective effects, but the effects of curcumin against manganese (Mn)-mediated neurotoxicity have not been studied. This study examined the protective effects of curcumin on...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b17-00160
更新日期:2017-08-01 00:00:00
abstract::Methylsulfonylmethane (MSM), also known as dimethyl sulfone and methyl sulfone, is an organic sulfur-containing compound that occurs naturally in a variety of fruits, vegetables, grains, and animals, including humans. In the present study, we demonstrated the anti-inflammatory effects of MSM in lipopolysaccharide (LPS...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.651
更新日期:2009-04-01 00:00:00
abstract::The in vitro percutaneous permeation of diclofenac from various vehicles was examined using rat abdominal skin as a model membrane. The oleaginous vehicles used in this study consisted of three components: i.e. fatty acid, fatty acid ester and nonpolar oil. The solubilities of sodium diclofenac in formulated vehicles ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.571
更新日期:1995-04-01 00:00:00
abstract::CCl(4) (0.5 ml/kg as CCl(4)) was orally administered to rats. Twelve hours after administration of CCl(4), plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels, indicators of liver necrosis, were significantly higher than those in the control group showing that active liver necrosis took p...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.707
更新日期:2010-01-01 00:00:00
abstract::The anti-herpes simplex virus type 1 (HSV-1) activity of 15 oleanan-type triterpenoides including glycyrrhizin and its sapogenol was examined and their structure-activity relationships were discussed. Although glycyrrhizin which exhibited in vivo efficacy against HSV-1 replication showed moderate in vitro anti-HSV-1 a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1779
更新日期:2005-09-01 00:00:00
abstract::A liposomal formulation of UCN-01 was studied to prevent binding of drug to human alpha1-acid glycoprotein (hAGP). The release of drug from liposomes added to various media was investigated by monitoring the concentration of UCN-01 in different fractions. Protein bound UCN-01 was separated from liposomal UCN-01 and fr...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1259
更新日期:2005-07-01 00:00:00
abstract::Fraxinellone and sauchinone, isolated from natural substance, are known to have an anti-inflammatory effect in inflammatory conditions. However, the anti-inflammatory actions of these compounds have been insufficiently demonstrated in viral-induced neuroinflammation. A viral component (double-stranded (ds)RNA) trigger...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.1870
更新日期:2009-11-01 00:00:00
abstract::The present study was designed to determine the effect of delta(9)-tetrahydrocannabinol (THC) on susceptibility to stress. We reported that THC significantly prolonged the immobility time during the forced swim-stress. The selective cannabinoid CB(1) receptor antagonist O-2050 significantly reduced the enhancement of ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.2065
更新日期:2009-12-01 00:00:00
abstract::In Parkinson's disease, while dopamine (DA) replacement therapy, such as with L-DOPA (levodopa), improves the symptoms, it does not inhibit the degeneration of DA neurons in the substantia nigra. Numerous studies have suggested that both endogenous and environmental neurotoxins and oxidative stress may participate in ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.25.284
更新日期:2002-03-01 00:00:00
abstract::The emulsion prepared with β-cyclodextrin as an emulsifier (βCDE) is considered to be a Pickering emulsion. We examined the characteristics of βCDEs using captopril (CP) as a model drug, and studied the in vitro skin permeation of CP from βCDEs through hairless mouse skin. The stability of βCDE was increased with incr...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b18-00711
更新日期:2019-01-01 00:00:00
abstract::We have found a new compound from thermophile extracts which inhibits antigen presentation on mouse macrophages. The substance inhibits the expression of the class II major histocompatibility molecule (Ia). It was extracted from Bacillus stearothermophilus UBT8038 and purified by silica gel column chromatography. The ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.889
更新日期:1994-07-01 00:00:00
abstract::Lysosomal trapping was investigated in the retinal capillary endothelial cells that are responsible for the inner blood-retinal barrier (BRB) using LysoTracker(®) Red (LTR). Using confocal microscopy on TR-iBRB2 cells, an in vitro model of the inner BRB, the presence of lysosomal trapping in retinal capillary endothel...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b16-00140
更新日期:2016-01-01 00:00:00
abstract::A rat model of early sepsis induced by lipopolysaccharide (LPS) combined with interleukin-2 (IL-2) was developed. The primary aim was to assess the pharmacokinetics of gentamicin and sepsis-induced pathophysiological changes. Moreover, the effects on the glomerular filtration rate and tubular function were studied in ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b12-00205
更新日期:2012-01-01 00:00:00
abstract::The physiological correlation between casein kinase I (CK-I) and an isoform eta of protein kinase C (C-kinase eta) was investigated in vitro, since it has been reported that (i) cholesterol-3-sulfate (CH-3S) effectively activates C-kinase eta rather than the other isoforms (C-kinase epsilon and C-kinase delta) in vitr...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.27.109
更新日期:2004-01-01 00:00:00
abstract::Butylbenzyl phthalate (BBzP) is used as a plasticizer to import flexibility to polyvinylchloride plastics. In this study, hydrolysis of BBzP to monobutyl phthalate (MBP) and monobenzyl phthalate (MBzP) in liver microsomes of humans, monkeys, dogs, rats and mice was examined. The kinetics for MBP formation by human, do...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b14-00002
更新日期:2014-01-01 00:00:00
abstract::Most malignant tumors are derived from epithelium, and pathologic microorganisms often invade the body through the mucosal epithelium. Thus epithelial tissues are potent targets for drug delivery. The tight junction (TJ) is the intercellular seal in epithelial cell sheets. Claudins (CLs) are a family of tetratransmemb...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.b13-00014
更新日期:2013-01-01 00:00:00