Influence of base on the release of antibiotics from officinal ointments

Backgraund. Officinal basis for the antibiotic ointments according to the 4th Yugoslav Pharmacopoeia is a hydrophobic base containing only aliphatic hydrocarbons. The fact that antibiotics are predominantly not lipophylic raises the question about the suitability of that particular type of the base for the manufacturing of antibiotic ointments. Recent studies of the lipid analysis of the skin corneal layer indicated that lipids had shown the bilamellar organization in the skin intercorneal space. Such structural organization could be seen in the ambiphylic bases whose structure was based on carefully selected emulsifier couple, consisting of the lyotropic and thermotropic liquid crystals. The aim of this study was to test the velocity of antibiotics (klindamycin hydrochloride, erythromycin base and chloramphenicol) release from the hydrophobic ointment-type bases, and from ambiphylic bases of anionic and non-ionic types. Methods. Membrane-free agar diffusion test as the basic method for testing the release velocity in vitro and Staphylococcus aureus as the strain highly susceptible to the chosen antibiotics were used. All the analyzed samples were manufactured as the suspension-type ointments. Results. The highest growth inhibition zone of the Staphylococcus aureus strain for all three analyzed antibiotics was achieved from the non-ionogenic ambiphylic base; the clear growth inhibition zone area for Staphylococcus aureus strain in the preparations containing anionic ambiphylic base was smaller by 10-31.28%, and in the preparations containing aliphatic hydrocarbon-type base, the decrease was 11.46-31.28%, compared to the results achieved with the non-ionogenic ambiphylic base. Conclusion. The optimal release velocity for the analyzed antibiotics was achieved from the non-ionic ambiphylic base.

Effect of Erythromycin on Orocecal Transit Time in Normal Healthy Male Subjects: A Double-Blind, Placebo Controlled Study

OBJECTIVE: To investigate the effect of erythromycin on orocecal transit time (OCTT) in 17 healthy male subjects in a double-blind, placebo controlled crossover trial.SUBJECTS AND METHODS: After an overnight fast, each subject received 250 mg erythromycin base, 500 mg erythromycin base or placebo on three different days. A standardized breakfast meal plus 20 g lactulose was administered 30 mins after ingestion of the test dose. Exhaled breath was collected and hydrogen concentration was assessed over 4 h. Hydrogen concentrations over time for each session were analyzed by a generalized logistic function generating a sigmoidal curve. The ‘front’ transit time (T1) was taken as the time when a sustained rise in breath hydrogen concentration was first observed. The midpoint from baseline to peak hydrogen concentration was denoted T2and represented the time when approximately half of the test meal had reached the cecum.RESULTS: There was no effect of erythromycin on OCTT. The T1(mean ± SEM) was 103.2±11.2, 103.3± 15.3 and 70.9±15.9 mins for placebo, 250 mg erythromycin base and 500 mg erythromycin base, respectively (P>0.05). Similarly, the T2was 113.3±11.3, 113.9± 16.5 and 99.3±15.3 mins for the three regimens.CONCLUSIONS: Oral administration of erythromycin does not alter OCTT in healthy male subjects.

Erythromycin Base-Induced Rash and Liver Function Disturbances

OBJECTIVE: To report a case of erythromycin base-induced rash and liver function disturbances. CASE SUMMARY: A patient with erythema nodosum and high antistreptolysin-O titers was treated with erythromycin on the assumption that occult streptococcal infection was the cause of the erythema nodosum. Forty-eight hours after the initiation of therapy the patient developed fever, severe generalized rash, pruritus, and cholestatic and hepatocellular liver function disturbances. Extensive evaluation to determine the cause of liver function disturbances was unrevealing. Marked improvement was noticed within days after cessation of erythromycin. DISCUSSION: Case reports in the literature on the adverse effects of erythromycin and its derivatives were reviewed. The possible immunologic mechanism involved is postulated. CONCLUSIONS: Erythromycin base must be added to the list of erythromycin derivatives that can cause rash and liver function disturbances. The concomitant appearance of fever, rash, jaundice, and liver function disturbances raises the possibility of hypersensitivity as the mechanism for the liver disturbances.

Acute Pancreatitis in a 12-Year-Old Girl After an Erythromycin Overdose

A variety of drugs including certain antibiotics have been implicated in causing acute pancreatitis.1 So far, there have been three reported cases in adults in which erythromycin was identified as a possible cause of acute pancreatitis.2-4 We report the first case of erythromycin-induced acute pancreatitis in childhood. We suggest a possible pathophysiological mechanism based on the known motilin agonist properties of erythromycin. CASE REPORT A 12-year-old girl was brought to the Emergency and Trauma Unit, with acute, crampy abdominal pain and vomiting. These symptoms had started 1 hour earlier, approximately 30 minutes after the deliberate ingestion of 20 tablets of erythromycin (Erythromycin Base Filmtab, 250 mg, Abbot Laboratories, Pharmaceutical Products Division, North Chicago, IL) after an argument with her parents and her boyfriend.

Comparison of Two Oral Forms of Erythromycin in the Treatment of Acute Respiratory Tract Infections. A Multicentre General Practice Study

A total of 1244 patients with acute upper or lower respiratory tract infection were randomized to receive, twice daily for 7 days, either capsules of enteric-coated pellets of erythromycin base at a dose of 1 g/day or erythromycin ethylsuccinate tablets at a dose of 2 g/day in a single-blind, multicentre study. The efficacy of each formulation was similar, with about 90% of patients who had completed at least 5 days of treatment being reported as either cured or improved. Gastro-intestinal symptoms were the most commonly reported side-effects, being significantly more frequent in patients receiving erythromycin base. Gastro-intestinal intolerance was also the main reason for discontinuing either treatment, although it was a significantly more frequent reason in patients given erythromycin base. This study indicates that both formulations of erythromycin are highly effective for routine, empirical treatment of acute respiratory tract infections. Erythromycin base, however, appears to be less well tolerated than erythromycin ethylsuccinate.