The dissolution step of practically insoluble drugs plays an important role in drug absorption. In this paper, the pharmaceutical properties of a ground mixture of nifedipine are described. A ground mixture of nifedipine was prepared by grinding with casein, magnesium silicate, and cellulose acetate phthalate in a vibrational ball mill. The X-ray powder diffraction patterns and differential scanning calorimetry data thereafter suggested that nifedipine was present in its amorphous form in the ground mixture. The wettability of the ground mixture was better than that of the physical mixture. The solubility of amorphous nifedipine in water was also better than that in crystalline. Both the dissolution rate and the bioavailability of amorphous nifedipine in the ground mixture were significantly greater than those of the physical mixture. The above results thus suggest that a mixture grinding method not only improves the solubility of nifedipine and the dissolution profile of its preparation but also enhances its bioavailability after oral administration.

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The pyrogenic activity of 10% inulin injections prepared at a hospital pharmacy was measured using the Pyrogen test in Japanese Pharmacopeia (JP), while the endotoxin concentration in the injections was determined by the, Limulus test, which were JP Endotoxin test and a turbidmetric kinetic assay. After the intravenous administration of 30 ml of inulin injections to a rabbit, the rectal temperature rose to 1.5° compared with that before administration. As a result, the endotoxin was found in all lots of the inulin injections tested, and their values were markedly beyond the limit of Water For Injections prescribed in JP (0.25 EU/ml). In addition, the endotoxin content varied between the various lots of inulin powder, and also between the manufacturers. The endotoxin in inulin injection was removed (less than the quantitative limit of 0.031 EU/ml) by adding activated carbon black to the injection or the filtration using a Posidyne^® Nylon 66 filter. No pyrogenic activity was observed in the inulin injections after the removal of endotoxin.
Based on these results, the adverse effects induced by inulin injections may thus be caused by endotoxin derived from inulin. This method using either adsorption or filtration is thus considered to be useful for the removal of endotoxin when preparing inulin injections.

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The pharmacokinetic parameters were estimated and the pharmacokinetic models of aprindine were evaluated in patients. Two pharmacokinetic models were used, comprising a linear elimination model and a non-linear elimination model, both one-compartment models in which first-order absorption is assumed. Twenty-two serum levels of patients in terms of TDM were measured and the pharmacokinetic parameters were estimated using the simple pool method. The pharmacokinetic parameters estimated using a linear model were ka= 0.244 (hr^-1), ke=0.020 (hr^-1) and Vd=1.778 (1/kg), while those using a non-linear model were ka=0.666 (hr-1), Km=2.022 (μg/ml), Vmax=0.106 (mg/hr/kg) and Vd=2.754 (1/kg).
The non-linear model was more suitable than the linear model for the AIC (linear model:-12.59, non-linear model:-19.61). The parameters estimated using the non-linear model were therefore more accurate and were found to have a smaller bias than those estimated using the linear model.

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The interaction between bezafibrate (BF) and cholestyramine (CT), an anionic exchange resin, was evaluated both in vitro and in vivo.
In an in vitro study, the incubation of 100 or 1000 μg/ml of BF solution with 200 mg of CT at various pH (2.0, 5.0 and 7.0) solutions was performed at 37° for 10 min in order to evaluate the binding ability of BF to CT. After incubation, 100 μg/ml of BF bound to CT by 85.41, 89.40 and 92.14% at pH 2, 5 and 7, respectively, and 1000 μg/m1 of BF bound to CT by 66.28 and 69.02%, at pH 5 and 7, respectively.
Next, the effect of CT on the pharmacokinetics and pharmacodynamics of BF was examined in experimentally induced hypercholesterolemic rats. When BF (50 mg/kg/day p. o.) and CT (600 mg/kg/day p.o.) were continuously administered to rats once a day for 7 days, CT caused a significant reduction in the cholesterol-lowering effect of BF in accordance with a significant decrease in the plasma level of BF, compared with the administration of BF alone. The decreased plasma BF level closely reflected the cholesterol-lowering effect of BF. Even when CT was given 3h after BF, the pharmacokinetics and pharmacodynamics of BF were not sufficient to achieve a full recovery of the BF level. The present observations thus suggest that CT should be used with extreme caution in patients receiving BF.

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A method for comparing the dividing and packing accuracy of four powder dividing machines;(A), (B), (C) and (D), were devised. The working time defined as the time from the start of dividing to the end of packing the powders was measured. Ten % phenytoin powder (10% Aleviatin^® powder, repose angle: 41°, 50% particle size: 123 pm), magnemagnesium oxide (repose angle: 31°, 50% particle size: 320 μm), pancreatin powder (repose angle: 40°, 50% particle size: 75 pm), and 50% aspirin granule (Minimax^®, repose angle: 41°, 50 % particle size: 250μm) were all used for the test. The maximum division errors were found to be significantly related to the coefficients of variation (CV) of packed powder's weights. This indicated that the CV values of the packed powder below 5 % represented the maximum devision errors below 10 %. We next compared the performance of the powder dividing machines by evaluating the working time to achieve a CV value of below 5 %. For dividing and packing the phenytoin powder, (A), (B), and (C) had an equal ability, however, (D) was somewhat inferior. In the case of magnesium oxide, (A) showed the best dividing performance of the four machines. In the case of pancreatin powder, (A), (C), and (D) had a excellent dividing performance. For the 50 % aspirin granules, all machines achieved a fast and accurate division, and the difference between the machines was small. These results thus indicate that this newly developed method for comparing dividing machines appears to be useful.

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The effect of grapefruit juice on the urinary 6β-hydroxycortisolicortisol ratio was investigated in healthy volunteers. The urinary concentration of cortisol was virtually unaffected by the administration of grapefruit juice whereas the concetration of 6β-hydroxycortisol in the urine decreased when grapefruit juice was given every 3 hours. The administration of grapefruit juice was thus considered to result in a decrease in the urinary 6β-hydroxycortisol/cortisol ratio. In addition, both diurnal and individual differences were also observed in the extent of the inhibitory effect of grapefruit juice.

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The effect of the patients understanding of the prescribed drugs regarding medication compliance were studied in 425 in-patients based on an objective assessment of their understanding of drug therapy and their compliance.
Each objective subject was assessed by three grades at initial and final drug consultation by pharmacists. The group who showed an improvement in their overall understanding of drug therapy also showed an improved medication compliance. The other group who showed an insignificant improvement in drug therapy, in contrast, showed a poor medication compliance.
These results suggested that the patient's level of influences of drug therapy thus understanding medication compliance, and, as a result, an improvement in the patients understanding of drug therapy based on consultation with pharmacists can therefore help to improve their medication compliance.

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The effects of drug consultation with pharmacists on medication compliance in patients with acute myocardial infarction (AMI) or angina pectoris (AP) were studied. The objective knowledge regarding medication and the drug action of the AMI group were lower than that for the AP group at the initial drug consultation, which may be due to differences in their past disease history. However, an objective assessment of both groups showed similar values for the above factors at the time of at discharge.

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The ratios of the number of MRSA cases isolated in out patients and admitted-patients were 9.4 and 93.5%, respectively. Out of the total of MRSA isolated, approximately 50% were mixed-infections. An analysis using the Spearman's Rank Correlation suggested no significant correlation between MRSA-infection and the third generation cephems utilized at the hospital. The sensitivity of MRSA to antibiotics other than VCM and MINO also decreased annually during the period analyzed. The present analysis thus suggests that more care should be taken to prevent the spread of MRSA in hospitalized patients.

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In curing diabetes mellitus, both the education and motivation provided by the medical staff is important for the patients achieving self-control.
We sent out a questionnaire (20 questions) regarding pharmacotherapy for diabetes mellitus to 164 NIDDM hospitalized patients in order to evaluate their level of knowledge of pharmacotherapy. The number of correct answers was 10.8±6.4 (mean±SD) when entering the hospital and 15.8±4.5 when leaving the hospital, which thus showed an improvement in the level of understanding.
The number of correct answers by patients their third or mare hospital stay was almost equal to that of the patients in either their first or second hospital stay. Some patients, however, entered the hospital without controling their blood sugar levels in spite of possessing sufficient knowledge about diabetes mellitus.
It is therefore important to properly educate and counsel patients in order to help them achieve a cure.

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We developed a drug information database using a method that employs the commercial application software called “KIRI”, and also designed a support system for both pharmaceutical management and counseling services.
This new method is considered to improve both the quality of patient care services and rational use of medication, regarding pharmaceutical management and counseling services.

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A hospital formulary designed for desk top publising (DTP) was published according to the online database system UMIN. In addition to the revision of the textual content, some illustrations and drawings were also inserted in the previous format of our formulary and the publication of the DTP-directed formulary was established in this edition. The database according to this new system at our hospital which has been maintained using a relational database software, was found to be useful for developing additional materials, such as worksheets as well as for insertings structural drawing objects on the drug tables each time. Using the local network system (LAN) by the Windows NT Server, it was possible to perform benefitial data conversions between different OS which thus led to the effective edition of our work. Electric publication of the formurary is suggested to be an excellent method provide the most up-to-date contents of all drug information and to satisfy the need to constantly update the informationl contents.

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