The clinical usefulness of injectable biapenem (BIPM) was examined for various infectious diseases in thefields of internal medicine, urology, surgery, orthopedics, obstetrics and gynecology, otorhinolaryngology, ophthalmology, dermatology, oral surgery, and plastic surgery. BIPM was administered by intravenous dripinfusion at a dose of 150,300, or 600 mg twice a day. The concentrations in various body fluid and tissueswere also examined.
1. In the total enrollment of 256 cases, the numbers subjected to the analyses forclinical efficacy, bacteriologicalefficacy, side effects and abnormal laboratory findings were 214, 170, 252 and 251 cases, respectively.
2. The clinical efficacy rate was 85.5%(183/214 cases) as a whole, being 2/2 for sepsis, 6/8 for cellulitisand lymphangitis, 76.2%(16/21) for traumatic, operative wound and burn infections, 4/6 for osteomyelitis and arthritis, 92.9%(13/14) for peritonsillar abscess and peritonsillitis, 83.3%(15/18) for chronic lower respiratorytract infection, 7/7 for pneumonia, 83.3%(30/36) for complicated urinary tract infection, 100%(14/14) forcholecystitis and cholangitis, 88.2%(15/17) for peritonitis, 86.5%(32/37) for internal genital infection, 8/9 forpelvic peritonitis, 2/4 for corneal ulcer, orbital infection and panophthalmitis, 1/2 for otitis media, 4/4 forsinustitis, 93.3%(14/15) for osteitis of jaw and cellulitis of mouth floor. The efficacy rate in the poor respondersto the pretreatment by other antibiotics was 86.4%(70/81).
3. 300 strains of causative organisms were isolated from 170 cases which containedpolymicrobialinfections. The elimination rate of causative organisms was 85.3%(256/300 strains), in terms of bacteriologicalefficacy.
4. Side effects were noted in 11 of 252 cases (4.4%) with 11 events. The signs andsymptoms were the skinsymptoms (5 cases), gastro-intestinal symptoms (3 cases), interstitial pneumonia (2 cases), and feeling bad (1case), all of which disappeared during treatment or after the discontinuation of treatment. The abnormal laboratoryfindings were observed in 31 of 251 cases (12.4%) with 50 events, and major ones were an increase ineosinophils, and elevations of AST, ALT, y-GTP and Al-p.
5. The concentrations of BIPM in body fluid and tissues were determined in 46 cases (212 samples) most ofwhich were administered 300 mg of BIPM by intravenous drip infusion for 60 minutes. The concentrations in thesputum within 6 hours after administration were 0.1-2.5γg/g. The maximum concentrations in body fluid andtissues were 0.2-1.8γg/g or ml in the bile, middle ear mucosa, tonsillar tissue, aqueous humor and bone tissuesand were 2.0-5.7, ug/g or ml in the gallbladder, maxillary sinus mucous membrane, ethmoidal sinus mucousmembrane, oral tissues, skin, woman genitals, synovia, joint tissue, and the eschar. The concentrations in theuterine arterial plasma and retroperitoneal fluid were almost similar to those in the cubital vein plasma.
From the above-mentioned results of clinical efficacy, bacteriological efficacy, and safety, injectable BIPM was confirmed to be useful in the treatment of moderate, severe and/or refractory infections in various fields.

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The levels of levofloxacin (LVFX) in the serum, sputum and lung tissue were measured by a high-performanceliquid chromatography method, and the penetration ratio of LVFX into respiratory tissue was investigated.The subjects of this study were 23 patients under pulmonectomy or brochoscopy.
LVFX at the dose of 200 mg was given orally and specimens were collected as follows; serum at 2, 3 and 5hours after, sputum at 2 hours after, and lung tissue at 3 and 5 hours after the administration, respectively.The mean level of LVFX in lung tissue at 3 hours was 3.91±2.33 μg/g, and those in sputum and in serum at2 hours were 0.711±0.63 and 2.08±1.01μg/ml, respectively. A very strong correlation was demonstrated betweenthe level of LVFX in lung tissue and that in serum (p<0.0001), but correlation between those in sputum and inserum was not significant. The penetration ratio of LVFX into lung tissue was 217.2% and that into sputum was4.05%. Based on the results of this study, the breakpoints (BPs) of LVFX for pneumonia and chronic respiratorytract infections were calculated to be 4μg/ml and 1μg/ml, respectively.
It was concluded that penetration of LVFX into lung tissue was satisfactory, and the tissue level of LVFXexceeded greatly the MIC₉₀s against the typical pathogenic bacteria of respiratory tract infections. Taking theexcellent BP for pneumonia, 4μg/ml, into consideration, it was thought that LVFX is an effective antibacterial agent against pneumonia and other respiratory tract infections.

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Antibacterial activities of four carbapenems, imipenem, panipenem, meropenem, and biapenem, were determinedusing 353 strains belonging to 18 bacterial species which were isolated from clinical materials at Ehime University Hospital. The MIC values of these carbapenems against MRSA were widely distributed between 0.1 and 100μg/ml, and MIC₉₀ values of these 4 carbapenems were 25-50μg/ml.Any of these carbapenems prevented the bacterial growth of enterobacteriaceae of 8 bacterial speciesexcluding S. marcescens at concentrations of 1μg/ml or less.The MIC values against P. aeruginosa showed relatively wide distribution, being 0.39-25μg/ml forimipenem, 0.2-25μg/ml for panipenem, 0.1-12.5μg/ml for meropenem, and 0.2-12.5μg/ml for biapenem.From those results, it was confirmed that any of the carbapenems tested had a wide antibacterial spectrum and strong antibacterial activities.

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