5'-Deoxy-5-Fluorouridine (5'-DFUR) ointment was prepared for local chemotherapy application to inoperable breast cancer. Polyethyleneglycol-4000, ammoniumpolyacrylate and hydroxypropylcellulose-H ...were employed to prepare the ointment base. 1-Dodecylazacycloheptan-2-one (Azone) was added to 5'-DFUR ointment as an absorption promoter. The spreadability of the ointment was only slightly changed by Azone addition. Azone was dispersed well in the ointment when the concentration was 1%. 5'-DFUR in mouse skin and intestine were analyzed after the application of ointment and oral administration of 5'-DFUR solution. The AUC0-6 value observed with 5'-DFUR ointment containing 1% Azone was seven times greater than without Azone. Application of Azone-5'-DFUR ointment significantly lowered the levels of 5'-DFUR in plasma and intestinal tissues over those of the oral administration of 5'-DFUR solution. Furthermore, no change occurred in histopathological findings of mouse skin following ointment application. These results suggest that the addition of Azone in 5'-DFUR ointment may provide a better therapeutic effect in the local chemotherapy treatment of breast cancer.
A 34-yr-old female patient with juvenile onset diabetes developed atony and dilatation of both the bulb and loop of the duodenum, i.e. megaduodenum. She showed various symptoms of diabetic ...gastroenteropathy including constipation, nocturnal diarrhea and recurrent attacks of nausea and vomiting. Neurological examinations revealed diminished or absent reflexes and a sense of vibration of the extremities. The evoked EMG requision showed a low voltage and low duration. The ECG R-R interval requision revealed cardiac denervation. These findings suggested that she had peripheral diabetic neuropathy and autonomic neuropathy. X-ray examination of the upper gastrointestinal (GI) tract on her first admission revealed gastric atony, gastric retention, and disturbance of expulsion of the gastric contents without evidence of organic obstruction, i.e. functional pylorus stenosis. After 18 months, the upper GI series showed atony and dilatation of the duodenal bulb. Further, 5 years later, the X-ray findings for the duodenum revealed atony and dilatation of the duodenal loop in addition to the above findings. The patient was given ambenonium chloride (10 mg per day) as treatment for the atony and dilatation of the stomach and duodenum. An improvement of subjective symptoms was obtained, but no change was noted in the X-ray findings of the upper GI tract. Although no clear explanation of the pathogenesis of diabetic gastroenteropathy has yet been made, it seems likely that a close relation exists between gastrointestinal atony and diabetic neuropathy. It was thought of interest to report the present diabetic case with atony and dilatation of the duodenal loop, due to the rarity of this condition.
Increased activities of intestinal alkaline phosphatase (ALP) have been found in the sera of blood group 0 or B secretors and this is augmented by fatty meals. The frequency of demonstration of high ...intestinal ALP activities is greatest in liver cirrhosis and significantly high in diabetes mellitus. It is not known, however, whether the increased activity in diabetics is due to the diabetes mellitus per se or to hepatic injury associated with it. We experienced a case of juvenile-onset diabetes mellitus with markedly elevated intestinal ALP. Detailed studies were made on this case with respect to the above point. The patient was a 21-year-old male of blood group B secretor. the initial fasting blood glucose level was 240 mg/dl with strongly positive urine glucose and weakly positive urine ketone bodies. Serum ALP was markedly elevated to 17.2 B-L u with slightly increased GOT (88 u) and GPT (100 u). The ALP was mostly of the β-migrating intestinal type upon agar-gel electrophoresis with more than 50 % inhibition by 5 mM L-phenylalanine. The increase in intestinal ALP was enhanced after a fatty meal. The ALP level decreased following insulin treatment and rose after its cessation, indicating the presence of a close correlation between them. No such relation was found with the blood glucose level, GOT or GPT activities. Involvement of liver injury was discounted by peritoneoscopy and liver biopsy. The above results suggest that a direct relationship may exist between elevation of intestinal ALP and insulin insufficiency.
Efficacy and safety of ofloxacin (OFLX), a new quinolone antibacterial agent, were investigated in cases of sexually transmitted male urethritis and cervicitis. Chlamydial infections occupied a large ...part of the patients enrolled. This study was conducted in 29 institutions. A total of 1, 126 patients with gonococcal, chlamydial or non-gonococcal non-chlamydial infections were enrolled in the study. The general dosing regimen of oral OFLX was 100mg t. i. d. or 200mg t. i. d. for 14 consecutive days. Along with the clinical efficacy evaluated by doctors in charge, therapeutic and clinical efficacies were determined according to standardized evaluation criteria. The evaluation of therapeutic efficacy was based on bacterial eradication. On the other hand, clinical efficacy was determined upon the improvement in causative bacteria, WBC counts in smear (or initial urine) specimens and urethra/cervical discharges. Clinical efficacy was determined on 7 and 14 days after starting the medication, except for gonococcal infections for which the efficacy was determined on Day 3 and Day 7. The results obtained are summarized as follows. 1. Efficacy evaluation by standardized criteria Therapeutic efficacy rates in gonococcal infections were 97.9% (93/95) on Day 3 and 100% (119/119) on Day 7. In chlamydial infections, the rates were 77.7% (363/467) on Day 7 and 93.6% (392/419) on Day 14. Chlamydial urethritis rated 94.8% (239/252) and cervicitis 91.6% (153/167) on Day 14. Clinical efficacy rates in gonococcal infections were 63.2% (60/95) on Day 3 and 95.8% (114/119) on Day 7. In chlamydial infections, they were 70.0% (327/467) on Day 7 and 89.7% (376/419) on Day 14. Chlamydial urethritis rated 88.5% (223/252) and cervicitis 91.6% (153/167) on Day 14. Clinical efficacy rates in non-gonococcal non-chlamydial infections were 93.3% (97/104) for male urethritis and 65.9% (27/41) for cervicitis on Day 14. 2. Clinical efficacy determined by doctors in charge A total of 1,028 cases, 752 urethritis and 276 cervicitis cases, was evaluated by doctors in charge. Clinical efficacy rates were 90.3% for urethritis and 92.4% for cervicitis. 3. Safety Safety evaluations was conducted in 1,087 patients. Side effects were observed in 23 patients among them (2.12%). None of them were deemed serious. General laboratory examinations were conducted for 169 patients. Abnormal findings were seen in 11 patients (6.51%) or 13 cases, all of which were minor. The results of this multi-center clinical trial demonstrated that OFLX is effective and well tolerated in the treatment of sexually transmitted disease (STD), both gonococcal and chlamydial infections.
4,6-Dichloro-s-triazinyl Duolite A7 (CC-A7) as a carrier of immobilized enzymes was studied.
The reactivity of the second and the third organic chlorines of s-triazines attached to the carrier toward ...amino acids or proteins was investigated. The results show that CC-A7 can bind a large quantity of amino acids or proteins and these compounds seem to be bound covalently via the second organic chlorine of s-triazine of the carrier under the usual condition.
It is also shown that this carrier can bind a sufficient amount of protein and enzyme activity of aminoacylase and retains a high activity in column operation.
These results indicate that 4, 6-dichloro-s-triazinyl Duolite A7 is a convenient and useful carrier for the industrial application of immobilized enzyme.
Antibacterial activity of cefmenoxime (CMX, SCE-1365) was markedly strogner than that of cefazolin against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Indole (+) Proteus, Serratia ...marcescens, Enterobacter cloacae, Enterobacter aerogenes, Citrobacter freundii and Pseudomonas aeruginosa. To evaluate the clinical efficacy of cefmenoxime, . the treatment was made with the drug in 56 patients, including 22 with acute pneumonia, 1 with acute bronchitis, 1 with chronic bronchitis, 5 with acute cystitis, 16 with chronic cystitis. 8 with acute pyelonephritis and 3 with chronic pyelonephritis. Responses were excellent in 17 patients, good in 35 and poor in 4. The incidence of adverse side-effect was very low. Fever was occurred only in one case and elevation of serum GOT and GPT or GOT was observed in three cases. Cefmenoxime was considered to be a useful antibiotic for the treatment of infections.
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