Susceptibility of 29 bacterial strains including Pseudomonas aeruginosa, Ps. cepacia and Serratia marcescens, which were isolated recently from the flange of sink at various clinical divisions in Yamagata University Hospital, to 4 disinfectants, Chlorhexidine gluconate (CHG), Benzalkonium chloride (BAC), Saponated cresol (SAC) and Povidone iodine (PVP-I), was examined at the concentration recommended for disinfection of hands.
1. Although all of the isolates tested were sensitive to SAC and PVP-I, susceptibility to CHG and BAC varied from species to species and also from strain to strain. 2. Eighteen strains of Ps. aeruginosa tested were sensitive to CHG and BAC. 3. Three strains of Ps. cepacia tested were resistant to CHG. 4. Five of eight strains of Se. marcescens tested were resistant to CHG and BAC. 5. Two strains of Se. marcescens isolated from hands of doctors had the same biochemical properties and the susceptibility to disinfectants and antibiotics as those of the isolates from clinical divisions.
These results indicate that the resistant strains of Ps. cepacia and Se. marcescens against CHG and BAC at the concentration recommended for disinfection of hands are present in hospital, and that these strains may cause nosocomial infection through medical treatments.

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A pharmacokinetic model including the drug release process was proposed to simulate kinetically some complicated plasma concentration profiles of theophylline after single oral dose (300mg) of the 3 commercial sustained-release theophylline preparations (Theolong^®, Theodur^®, Slo-bid^®) on separate occasions into 4 healthy adult volunteers on empty stomach. In this model, the two step release process consisting of zero-order and first-order rate was assumed, which was connected to the one-compartment model with first-order elimination process.
The parameters in drug release process were estimated by fittings of plasma concentration data to the mathematical model and individual plasma concentration data of the 3 different slow release products could be appropriately simulated by the same mathematical model. The drug release-time profiles, calculated by using the estimated parameters, were compared between subjects and between products.From the present single oral dose studies on empty stomach, the marked differences in release rate between products were observed and Theodur^® tablets seemed to be more adequate formulations for a twice daily dosage regimen.

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Brompton mixture has been widely used for cancer patients to control pain.This mixture originally consists of morphine HCl, cocaine HCl, simple syrup, ethyl alcohol, chloroform and water.In Japan, chloroform is omitted and ethyl alcohol is occasionally removed from the original prescription.Because this mixture is a medicine for cancer patients, great attention should be paid to microbial contamination.But it has not been investigated on the preservative efficacy of Brompton mixture, yet. Thus, the preservative efficacy of Brompton mixture was studied.
Brompton mixtures with various compositions were challenged with 1×10⁶ cells/ml each of Staphylococcus aureus, Escherichia coli or Pseudomonas aeruginosa or 1×10⁵ cells/ml of Candida albicans or 1×10⁵ spores/ml of Aspergillus niger. Samples were taken on day 1, 2, 7, 14 and 28 during storage at 25°C for determining viable counts of the organisms.The preservative efficacy of Brompton mixture was assessed by a slightly modified British Pharmacopoeia (B. P.) standard;The number of S. aureus, E.coli and P. aeruginosa recovered per ml is reduced by less than 10³ within forty-eight hours of challenge, and there is no increase thereafter. The number of C. albicans recovered per ml is reduced by less than 10² within fourteen days of challenge, and there is no increase thereafter. In the case of A.niger, there is no budding of spores during twenty-eight days of challenge.
The modified B. P. standard was achieved by Brompton mixtures containing ethyl alcohol at concentrations above 8%, but not by mixtures containing no or less than 5% of ethyl alcohol. Then, the effect of preservative agents, parahydroxybenzoates on these inadequately preserved mixtures was studied.The modified B.P.standard was achieved by mixtures with 0.06% methylparaben, 0.03% ethylparaben and 0.01% propylparaben, but not 0.05% ethylparaben or 0.09% methylparaben and 0.01% propylparaben.
It is desire that Brompton mixtures containing no or less than 5% ethyl alcohol should include 0.06% methylparaben, 0.03% ethylparaben and 0.01% propylparaben for protecting microbial contamination.

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For an attempt to evaluate the usefulness of newly developed microultrafiltration devices (Ultrafree C3LGC, Molcut II LGC, Minicent-30, Minicent-10 and Airpress-30), free fractions (FF) of phenytoin, carbamazepine, valproic acid, and disopyramide separated by these devices were compared with those obtained by a commercially available devices, MPS-1.The present study clearly showed that the correct FF of a drug could not be obtained by using an ultrafiltration device.The protein leakage through the membrane and the adsorption to the instruments may result in their differences between the FFs.The adsorption degree of these drugs seems to depend on their hydrophilicity, since the adsorption had a tendency to increase with the hydrophilic properties of the drugs.
From these findings, it is recommended that a new device should be chosen by considering factors such as hydrophilicity of drugs and protein leakage through the membrane.

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This study discusses the possibility that human serum albumin (HSA) preparation has equal binding efficiency with drug to normal serum albumin. The binding percentage with theophylline (TH) in vitro was 61-64% in normal serum albumin, 32% in HSA preparation, and 65% in dialyskl HSA preparation.This suggests that the fall of the binding percentage with TH in HSA preparation results not from the heat treatment but from the stabilizers.
In addition, the influence of the change of pH value on the binding efficiency was equal in both normal albumin and HSA preparation, which suggests that the binding state of HSA preparation with TH is similar to that of normal serum albumin.

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In the previous paper, we reported the evaluation method of patient compliance using the data obtained from the new eyedrop medication monitor numerically in the case of that patients were prescribed the number of administrations each day and medication time.In this study, We investigated the evaluation method of patient compliance in the case of that patients were prescribed only the number of administrations each day on the envelope.
The data from this monitor were evaluated by two methods, that is (1) the prescribed number of administrations, (2) the interval between administrations based on the results evaluated by 9 panelists (pharmacist).The mean value of compliance of 10 patients used this monitor was 77.2% by the total evaluation of the two methods.And the difference of compliance was significant between people over fifty years old and under fifty by a t test of p<0.01.

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Cyclosporin-A (cy-A) is used for an immunosuppressant, but its narrow therapeutic index of effective concentration requires careful blood level monitoring of cy-A. Recently fluorescence polarization immunoassay (FPIA) of cy-A detection system in human serum level was commercialized, we compared FPIA with radioimmunoassay (RIA) and high performance liquid chromatography (HPLC) method. The correlation coefficient was r=0.873 between FPIA and HPLC in 62 serum samples of renal transplantation patients. FPIA system detected cy-A metabolite like peaks which fractionized by HPLC analysis. Further cyclosporin-D of HPLC internal standard substance was assayed in cy-A at 80% concentration.
With respect to these results, it was indicated that the FPIA caused to cross reactivity against to cy-A derivatives because of its polyclonal antibody use, and it made the determained value by FPIA greater than that by HPLC. However, it is a relatively simple and rapid procedure, this assay system is useful to facilitate the analysis of a large number of samples and to decide the sufficient dosage of cy-A after organ transplanted patient.

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Homogeneous enzyme immunoassay method (Emit method) for the determination of tricyclic antidepressants, imipramine (IP), desipramine (DP), amitriptyline (AT) and nortriptyline (NT), in serum was evaluated.The within-run precision was determined by assaying 10 eluates of serum added antidepressants.The between-run precision was determined by assaying eluates from serum added antidepressants in 10 times during a two-week period.Each coefficient of variation value of within-run precision for each drug in serum was less than 7% and that of between-run precision was less than 9%.The serum drug concentrations by Emit method were compared with those by high-performance liquid chromatography (HPLC).There was a good correlation between HPLC and Emit method results, which correlation coefficients were more than 0.996.The cross-reactivities of six drugs in each IP, DP, AT and NT assay kit were found.No clinically significant interference was observed with hemolytic and lipetic samples at concentrations below 3g/dl hemoglobin, 400mg/dl cholesterol and 420mg/dl triglycerides. From these results, Emit method may be useful for serum drug-level monitoring of patients under the tricyclic antidepressants therapy.A lack of correlation between daily IP dose and serum IP concentration or between daily AT dose and serum AT concentration was obtained in out-patients.

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Serum cortisol level of kidney transplant patients treated with prednisolone as an immunosuppressive agent was determined by a combination of rapid-flow fractionation (RFF) and high performance liquid chromatograpy (HPLC). A 0.5ml serum was extracted with ether using RFF technique prior to HPLC to obtain cortisol fraction. The ether extract was analyzed by HPLC with normal phase silica gel column and organic solvent system as a mobile phase solvent. Detection limit of this method was as low as 500pg/ml of serum.The cortisol peak was not disturbed by concomitant drugs such as azathioprine or cyclosporin A.

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Teprenone fine granule has excellent feeling of tongue contact, but its marked dustability causes a pharmaceutical problem. We obtained a reformed preparation which aimed at improvement in pharmaceutical preparation while retaining its excellent feeling of tongue contact, and evaluated its pharmaceutical property.
As a result, the preparation has high granular uniformity and excellent pharmaceutical fitness, though slightly pales before the feeling of tongue contact. When evaluated from an overall viewpoint, the reformed preparation seems to be better than the control drugs.

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A patient offered that oral administered tablet excreted in stool in the unchanged form. We investigated this film-coated tablet, Perycit^® (Niceritrol), by the J.P.XI disintegration test.
Although it was broken completely in the J. P. XI first fluid (pH 1.2), it was not broken at all in the J.P.XI second fluid (pH 6.8) or water.We examined its disintegration test in various pH with Mcllvaine buffer solution, and the results were that the time prolonged extremely above pH 5.0.57 kinds of commercial film-coated tablets tested were broken rapidly in the J.P.XI second fluid and water except Perycit^®. Perycit^® seemed to be used in a peculiar film-coating material and may be not disintegrated in human gastrointestinal fluid because of the resistance of film-coating material to alkali and water.These results suggest that Perycit^® should be used carefully to patient with anacidity and such information must be given to users in detail.

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The radial partition fluorometric enzyme immunoassay (RPIA) was studied for determination of digoxin concentration in the serum.In 3 levels of digoxin added sample, the coefficients of variation (CV) values of within-run from 5 replicate assays were 1.58-12.2% in digoxin spiked samples at 3 levels.The mean recovery of digoxin by RPIA was 94.7-108.8% from 5 kinds of concentration known samples.The CV values obtained from a low level (0.5 ng/ml) of digoxin were greater than those from middle (1.0 ng/ml) and high (2.0 ng/ml) levels of the drug.The constituents in the blood such as proteins, triglycerides and hemoglobin had little influence on this analysis.There was a significant correlation between digoxin concentrations of 50 samples determined by both RPIA and fluorescence polarization immunoassay (FPIA), although the values determined by RPIA tended to be slightly higher than those by FPIA. RPIA seemed to be a reliable and useful technique for rapid determination of digoxin concentrations since the method is able to precisely determine digoxin in the serum even in the presence of hemolysis or chylomicronemia and moreover requires no pretreatment of deproteinization.

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