Figure 1
Figure 2
Formula for the production of different batches of gentamicin sulphate oral capsules_
| Quantity (mg) | |||
|---|---|---|---|
| Ingredients | Batch A | Batch B | Batch C |
| Gentamicin sulphate | 250 | 250 | 250 |
| Carb-o-sil® | 15 | 15 | 15 |
| N-starch | 30 | 30 | 30 |
| Ac-di-sol® | 5 | 5 | 5 |
| PEG 4000 | 50 | --- | --- |
| PVP | --- | 50 | --- |
| Gelatine powder | --- | --- | 50 |
Inhibition zone diameters (IZDs) of some bacteria for selection for the in vitro permeability study_
| Time (h) | ||||
|---|---|---|---|---|
| 0.5 | 1 | 2 | 3 | |
| Organism | IZD (mm) | |||
| B. subtilis | 13.3±0.6 | 7.0±0.0 | 10.0±0.0 | 3.6±0.6 |
| K. pneumonia | 8.0±0.0 | 5.0±0.0 | 2.0±0.0 | 0.0±0.0 |
| S. aureus* | 20.0±0.0 | 14.0±0.0 | 15.7±0.6 | 4.0±0.0 |
| E. coli | 6.0±0.0 | 4.0±0.0 | 3.3±0.6 | 0.0±0.0 |
| S. typhi | 8.0±0.0 | 3.0±0.0 | 3.0±0.0 | 0.0±0.0 |
Average inhibition zone diameter (IZD) (mm) of gentamicin sulphate after 6 h of oral administration at different concentrations_
| Dose (mg/kg) | |||||
|---|---|---|---|---|---|
| Microorganism | 500 | 14.28 | 10.71 | 7.14 | 3.57 |
| E. coli | 12.0±0.8 | 6.3±0.5 | 6.0±0.0 | 4.3±0.5 | 0.0±0.0 |
| S. typhi | 13.3±0.5 | 6.0±0.0 | 6.3±0.5 | 4.0±0.0 | 0.0±0.0 |
| K. pneumonia | 15.0±0.8 | 8.0±0.8 | 10.0±0.0 | 8.3±0.5 | 0.0±0.0 |
| S. aureus | 14.3±0.5 | 10.0±0.8 | 7.0±0.8 | 6.3±0.5 | 0.0±0.0 |
Baseline gentamicin sulphate dose level using inhibition zone diameter (IZDs) (mm) produced by serum drug level of oral gentamicin sulphate against Staphylococcus aureus_
| Dose (mg/kg) | |||
|---|---|---|---|
| Time (h) | 400 | 500 | 1,000 |
| 0.0 | 0.0 | 0.0 | 0.0 |
| 0.5 | 0.0 | 7.3±0.6 | 10.3±0.6 |
| 1.0 | 0.0 | 8.7±1.2 | 11.3±0.6 |
| 2.0 | 0.0 | 8.2±1.2 | 12.3±0.6 |
| 3.0 | 0.0 | 7.3±0.6 | 13.0±0.0 |
Inhibition zone diameter (IZDs) (mm) produced by serum drug level of orally co-administered gentamicin sulphate with permeation enhancers against Staphylococcus aureus_
| IZD | (mm) | |||||
|---|---|---|---|---|---|---|
| Drug/P. enhancera | ((mg/kg)/%) | 0 h | 0.5 h | 1 h | 2 h | 3 h |
| Drug | 400 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| Drug/PEG 4000 | 400/30 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| Drug/Tween® 80 | 400/15 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| Drug/Kolliphor® 188 | 400/1.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| Drug/Glycerine | 400/1.5 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| Drug/SLS | 400/2 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| Drug/Citric acid | 400/2 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| Drug/Oleic acid | 400/2 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| aP. enhancer = | Permeation | enhancer, | SLS = | Sodium | lauryl | sulphate |
Duration of GIT local activity of orally administered gentamicin sulphate_
| Time (h) | E. coli | S. typhi | K. pneumonia | S. aureus |
|---|---|---|---|---|
| 0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| 4 | 2.5±0.7 | 0.0±0.0 | 0.0±0.0 | 2.0±0.0 |
| 6 | 3.5±0.7 | 4.0±0.0 | 2.0±0.0 | 6.0±0.0 |
| 8b | 6.0±0.0 | 4.0±0.0 | 4.0±0.0 | 8.0±0.0 |
| 10 | 3.5±0.7 | 0.0±0.0 | 0.0±0.0 | 4.0±0.0 |
| 12 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| 14 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| 16 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |
| 18 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 | 0.0±0.0 |