Qualities of commercial products including benzalkonium chloride (BC) were evaluated. Amounts of C₁₂, C₁₄, and C₁₆ in the commercial BC products were 66.6 to 83.3%, 10.1 to 26.2 %, and 0.0 to 3.3%, respectively.BC with C₁₂ and C₁₄ alkyl group is known to adsorb to a cotton ball in the monomolecular adsorption manner following the Langmuir's adsorption isotherm. The adsorption rate of C₁₄ was larger than that of C₁₂.
These results suggested that the preparation containing a larger amount of C₁₂ was suitable for the clinical use.

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In the present study, according to the standardized methods, we tried to evaluate the quality and efficacy of oral kallidinogenase preparations, which were manufactured under the new quality standard, and the stabillity and purity tests by using HPLC-post-column analysis.Results obtained by the standardized methods showed that all of the specimens were in compliance with standards.The purity test by HPLC-post-column analysis revealed that many specimens were found to have enzyme activities other than kallidinogenase.The stability test showed that most specimens were stable enough under the storage conditions at 50°C for 2 months, but one particular specimen reduced to 30% of the labeled activity under the same conditions.These results suggest that although the products have been manufactured and marketed under the standardized criteria, the qualities of kallidinogenase preparations are found considerably different among manufactures.

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Acute renal failure developed in a 5 year-old girl during the fifth course of high dose methotrexate (MTX) treatment for osteosarcoma. She showed oliguria, and the serum MTX concentration, BUN and Scr were 461 μmoles/1, 50 mg/dl and 2.6 mg/dl, respectively, at 27 hr after infusion.Massive leucovorin calcium rescure, direct hemoperfusion, hemodialysis and plasma exchange therapies were successfully treated and she recovered gradually.Neither toxic bone marrow suppression nor side effect of massive leucovorin calcium appeared.The pharmacokinetic analysis of MTX during the renal failure and the dialysis treatment was investigated.

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Pharmacokinetics of MTX in seven osteosarcoma patients treated with 36 courses of high dose MTX therapy was investigated.Serum concentrations of MTX were well fitted to 3-compartment model.The slopes of γ phase were significantly correlated with the counts of leukocytes (r=0.65, p<0.001), and also the mean γ value in the patients suffering the adverse reactions was significantly smaller than that without any adverse reactions (p<0.05).

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The compatibility of Wintermin^® fine granules consisting of chlorpromazine phenolphthalinate and magnesium oxide was investigated by sensory test, and the residual amount of chlorpromazine was measured with high-performance liquid chromatography. Although the coloration to pink in the preparation was observed after preservation under medium (20°C, RH 75%) and severe (30°C, RH 92%) conditions, no change in the amount of chlorpromazine under any condition tested was noticed.
It was also found from the chromatogram that a slight amount of phenolphthalein was contaminated in Wintermin^®fine granules. Moreover, no change was detected in the compatibility test of chlorpromazine hydrochloride and magnesium oxide under the severe condition.It was, therefore, suggested that the interaction between phenolphthalein and magnesium oxide alkalized by moisture was responsible for the coloration in the preparation of Wintermin^®fine granules and magnesium oxide.

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For the topical application to the treatment for stomatitis, six oral cavity viscous fluids containing 0.1% sodium guaiazulene sulfonate (SGAS) were prepared with 4% methylcellulose, 2%sodium acrylate or 4% hydroxypropylcellulose (HPC) as viscous liquids, procaine or lidocaine as analgesics.Examination of the stabilities of SGAS in each preparation based on its absorbancy showed that SGAS was most stable in the preparation containing HPC and procaine, stored in light-resistant containers below 4° for 5weeks.Retaining of SGAS after gingivo-buccal application was examined.Concentration of SGAS in saliva was declined according to the first-order rate process.HPC was observed to provide adequate retainability to the preparation.Elimination constant was 4.8×10^-2/min, and half-life was 14.2 minutes. With these results it is concluded that the SGAS oral cavity viscous fluid consisting of HPC and procaine is most efficacious to the treatment for stomatitis and lichen planus among six preparations.The present preparation was very efficacious clinically.Some patient, having depended on intubation feeding, recuperated enough to eat food orally.

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Buprenorphine (BN) is a long-lasting, low-dependent and non-narcotic analgesic, which is effectively employed against various pains, such as cancer, myocardiac and postoperative pain. However, since BN was used only as an injection in Japan, we have planned to adapt it for suppository use for patients who cannot take oral drugs or for home therapy.A method of freeze-drying of the BN injection was chosen on the basis of its simplicity and reproducibility over other methods. With this method, we prepared both a water-soluble, polyethylene glycol based suppository (200.1 ± 1.51μg, n=5) and an oil-soluble, witepsol based suppository (200.8 ±1.70μg, n=5).The physical characteristics of each suppository were examined with regard to the pharmaceutical items of weight, BN content, hardness, melting point, liquefaction time and dissolution.In the clinical cross-over test, the rectal administration of both types of suppository showed equally good results.

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One-vial vitamins was added to 12 different formuras being prepared by mixing a basic solution of hyperalimentation with 4 kind of fat emulsions and 3 kind of amino acid injections. Stability of vitamins, change of pH and diameters of fat particles in the mixtures were examined at room temperature with non-blocked or blocked light and at a cool dark place.
In case of most of the mixtures without one-vial vitamins their particle size became above 10μm at room temperature after 24hrs or at the cool dark place after 96hrs.However, no change in diameters of the fat particles in many of the mixtures was noted when one-vial vitamins was added.As a result of vitamin analysis in the mixtures, residual rate of B₂, K₁ and A was found to be above 90% when the mixtures were kept at room temperature with nonblocked light (500Lux) for 24hrs.No decrease of B₁, B₆, FA and E contents was observed in the mixtures.

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In vitro combined effects of cefteram, an active metabolite of cefteram pivoxil, with ampicillin, cefaclor or minocycline against Escherichia coli NIHJJC-2, Staphylococcus aureus FDA 209P or Methicillin Resistant Staphylococcus aureus (MRSA) were examined by checkerboard dilution method.The combined use of cefteram and ampicillin showed an apparent synergistic antimicrobial action against eight strains in ten of MRSA.The combined use of cefteram and cefaclor also showed an apparent synergistic action against three strains in ten of MRSA and a partial synergistic action against six strains in ten of MRSA, while the combined use of cefteram and minocycline showed a partial synergism against nine strains in ten of MRSA.
The combined use of cefteram and ampicillin, cefaclor or minocycline observed a synergistic action against Staphylococcus aureus FDA 209P, but no synergistic action against Escherichia coli NIHJJC-2.

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