Volume 37,
Issue 10,
2009
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ORIGINAL ARTICLES
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薬理と治療 37巻10号, 805-812 (2009);
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Cilostazol orally disintegrated tablets(ODT)are a newly developed formulation for easierswallowing by patients with swallowing disorders that make it difficult for them to take tabletswith water. The bioequivalence of one cilostazol 100−mg ODT ingested with or withoutwater and one cilostazol 100−mg conventional tablet ingested with water was evaluated inhealthy adult male subjects in an open−label, randomized, 2−formulation, 2−treatment, 3−period crossover study.Thirty six subjects were enrolled, and 32 subjects completed the study. The differencesin the mean log−transformed AUC60h and Cmax values between the ODT without water andthe conventional tablet(ODT without water−conventional tablet, point estimates)were bothlog(0.94), with respective 90% confidence intervals of log(0.88)to log(1.00)and log(0.87)to log(1.02). The differences in the mean log−transformed AUC60h and Cmax valuesbetween the ODT with water and the conventional tablet(ODT with water−conventionaltablet, point estimates)were both log(0.98), with respective 90% confidence intervals of log(0.92)to log(1.04)and log(0.91)to log(1.06). All values were within the range of the equivalencejudgment criteria of log(0.8)to log(1.25)specified in the guideline for bioequivalencestudies.Based on the above results, one cilostazol 100−mg ODT, when administered either withor without water, was judged to be bioequivalent to one cilostazol 100−mg conventional tablet.All adverse events observed in all groups were mild or moderate in severity and wereresolved. Deaths or other serious adverse events or clinically significant adverse events didnot occur.(Jpn Pharmacol Ther 2009;37:805−12)KEY WORDS Cilostazol, Antithrombotic drug, Healthy adult male subjects, Orally disintegratedtablets, Bioequivalence
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Source:
薬理と治療 37巻10号, 813-819 (2009);
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Cilostazol orally disintegrated tablets(ODT)are a newly developed formulation for easierswallowing by patients with swallowing disorders that make it difficult for them to take tabletswith water. The buccal absorption of cilostazol ODT was evaluated in an open−label, randomized,2−treatment, 2−period crossover study in 14 healthy adult male subjects by comparisonof when one cilostazol ODT was disintegrated in the mouth and swallowed and whenit was held in the mouth for 3 minutes without swallowing and then spit out.The mean ratios of the AUC60h and Cmax for non−swallowing administration to those forswallowing administration were respectively 0.99% and 1.28%, both being lower than 5%,the judgment criteria for buccal absorption, and the recovery of cilostazol in the saliva andrinsing water collected from non−swallowing administration was 101.00%, being higher thanthe criteria of 95%.As the ratios of the AUC60h and Cmax for non−swallowing administration to those for swallowingadministration met the judgment criteria, it was concluded that buccal absorption ofcilostazol does not contribute to bioavailability when cilostazol ODT are orally administered.(Jpn Pharmacol Ther 2009;37:813−9)KEY WORDS Cilostazol, Antithrombotic drug, Healthy adult male subjects, Orally disintegratedtablets, Buccal absorption
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薬理と治療 37巻10号, 829-845 (2009);
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Background and Aim With the approval of Pariet_10 mg tablet for the maintenance treatmentof recurring/relapsing reflux esophagitis(RE)in July, 2003, the safety and efficacy ofthe tablet in long−term treatment were evaluated by the post−marketing survaillance.Methods Pariet_10 mg tablet once daily was administrated in patients with recurring/relapsing RE, whose RE had been healed endoscopically before survey. The duration ofadministration was between 6 and 24 months. The survey was implemented by the centralregistration system between Oct. 1, 2003 and Sep.20, 2006.Results 1443 subjects for safety and 898 subjects for efficacy were analyzed. Adverse reactionswere reported in 92 cases(6.38%, 1017 events). Based on patient background, significantdifferences were observed in 6 items i. e. complication of RE, pretreatment endoscopicfinding, history of RE treatment, history of RE, history of allergy and concomitant drug.Among 621 cases with endoscopic assessment, non−recurrent rates were 89.9% after52 weeks and 74.7% after 104 weeks in Kaplan−Meier method. In non−recurrent rate, significantdifferences were observed in two items(complication of RE and pretreatment endoscopicfinding)after 52 weeks and in 4 items(complication of RE, pretreatment endoscopicfindings, posttreatment endoscopic findings and history of GI tract surgery)after 104 weeks.Conclusion Pariet_10 mg tablet showed high tolerability for maintenance treatment ofrecurring/replacing RE and proved excellent preventive effect of RE. Incidence of adversereaction in two−year treatment was 6.38%. Non−recurrent rates were 89.9% and 74.4%after 52 and 104 weeks respectively.(Jpn Pharmacol Ther 2009;37:829−45)KEY WORDS Rabeprazole, Proton pump inhibitor, Maintenance treatment for reflux esophagitis,Long−term treatment, Special post−marketing surveillance
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薬理と治療 37巻10号, 849-856 (2009);
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We investigated the effects of the chewing gum containing phosphoryl oligosaccharidesof calcium(POs−Ca(+)gum)on recovery of mineral contents(remineralization)and crystalcontents(recrystallization)of early enamel lesion of bovine teeth in 8 adult volunteers. Theeffect of POs−Ca was assessed under double blind crossover design. The volunteers wereequally divided into two groups, and chewed the gum once a day, for 5 days. The durationtime of each chewing was 20 minutes, and whole saliva secreted from each volunteer wascollected. Then, the enamel slabs, which were demineralized in advance, were immersed inthe saliva. In this step, we designed each slab to have three regions:the sound, demineralized,and remineralized. The remineralization effect of POs−Ca was assessed from the mineralloss parameters from the transversal microradiography analyses after immersion of theslabs. In addition, the recrystallization effect of POs−Ca was assessed from the quantitativeanalyses of the hydroxyapatite crystals in the remineralized region with 6μm X−raymicrobeam. The recrystallization degree was scanned from the serial 5μm spots aligned fromthe enamel surface to dentin of each region of the enamel slabs. As a result, both the remineralizationand recrystallization effect on the bovine enamel of the POs−Ca(+)gum wasobserved significantly(p<0.05)in comparison with that of the POs−Ca(−)gum. Theseresults indicate that chewing of POs−Ca(+)gum could be one effective approach to facilitateboth remineralization and recrystallization of early−stage dental caries and thereby to maintainteeth sound and healthy.(Jpn Pharmacol Ther 2009;37:849−56)KEY WORDS POs−Ca, Enamel, Remineralization, Recrystallization, Chewing gum
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薬理と治療 37巻10号, 857-866 (2009);
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Objectives In order to examine the effect of black tea containing resistant maltodextrin onthe elevation of serum triglyceride and the safety of excessive or long term intake of the beverage,a double−blinded crossover study and open−labeled study were performed.Methods For assessment of the effect on postprandial serum triglyceride levels, 50 healthymale and female adults were loaded a diet containing about 40 g of lipid together with beveragecontaining 5 g(as dietary fiber)of resistant maltodextrin or not in a double−blind manner.Blood samples were taken before and 1, 2, 3, 4, 5, 6 hours after ingestion and serum triglyceridelevels were measured. For assessment of safety of excessive or long term intake of thebeverage, 18 male and female subjects were used in each trial, and the subjects were treatedwith triple regular amount of resistant maltodextrin for 4 weeks(excessive intake)or regularamount for 12 weeks(long term intake).Results Intake of resistant maltdextrin beverage significantly suppressed the elevation ofserum triglyceride levels at 3, 4 hours after diet ingestion as compare with those of controlbeverage(p<0.05). In the excessive and long term ingestion trials, no clinical problems wereobserved in the blood examinations and physical examinations.Conclusions The present results showed that black tea containing resistant maltodextrintaken together with diet had the inhibitory effect on the postprandial serum triglyceride elevationand possessed high safety for the excessive and long term ingestion.(Jpn Pharmacol Ther 2009;37:857−66)KEY WORDS Resistant maltodextrin, Postprandial serum triglyceride elevation,Remnant’like particle cholesterol, Black tea
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Source:
薬理と治療 37巻10号, 869-876 (2009);
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Objectives We compared an improvement effect of two shiitake hypha culture educt(L. E.M)component cosmetics(cream and granular)for a pigmentation of face skin and a crowfootaround eyes.Methods For Japanese woman 34 people having chloasma from 31 years old to 56 yearsold, we examined a utility for pigmentation and a crowfoot around eyes by a continuous usefor 12 weeks of L. E. M. The test sample applied to facial right and left respectively twice aday in morning and evening. Observation of skin condition by a dermatologist and the measurementof a skin parameter were performed clinical study start day and 4, 8, 12 weeks later.Final number of cases was 30 examples, and the average age was 45.7 years old.Results In cutaneous pigmentation, a significant rise of a skin−colored(L*)value and significantdecrease of melanin value and erythema value were observed. In addition, in replicaanalysis for a crowfoot around eyes, wrinkles area rate and the wrinkles number and wrinklestotal volume rate decreased significantly. Further, a water holding capacity of the stratumcorneum was increased, and that there was a moisturizing effect was observed. Forthese effects, the L. E. M cream and the L. E. M granule showed an approximately similareffect.Conclusions It was suggested that the L. E. M cream and the L. E. M granule showed asimilar whitening effect and a similar improvement effect for a slight wrinkle by drying.(Jpn Pharmacol Ther 2009;37:869−76)KEY WORDS Lentinus edodes mycelia(L. E. M),Wrinkle,Pigmentation,Whitening effect