Non-Absorbable Oral Gentamicin Sulphate: Biopharmaceutical and Dosage Form Evaluation

Dozie C. Nwakile; O.C. Dozie-Nwakile; E.I. Okoye; C.E. Umeyor; E.C. Uronnachi; I.K. Uchendu; A.A. Attama; V.C. Okore

doi:10.2478/afpuc-2020-0016

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Non-Absorbable Oral Gentamicin Sulphate: Biopharmaceutical and Dosage Form Evaluation

European Pharmaceutical Journal

Volume 68 (2021): Issue 2 (December 2021)

By: Dozie C. Nwakile, O.C. Dozie-Nwakile, E.I. Okoye, C.E. Umeyor, E.C. Uronnachi, I.K. Uchendu, A.A. Attama and V.C. Okore

Open Access

|Apr 2021

Figures & Tables

Calibration curve of Gentamicin Sulphate using S. aureus,

Concentration time curve of gentamicin sulphate capsule in normal saline.

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	400500	0.0±0.00.0±0.0	0.0±0.00.0±0.0	0.0±0.08.0±0.0	0.0±0.08.7±0.6	0.0±0.08.0±0.0
Drug/PEG 4000	400/30500/30	0.0±0.00.0±0.0	0.0±0.06.7±0.6	0.0±0.07.6±0.6	0.0±0.06.7±0.6	0.0±0.06.7±0.6
Drug/Tween^® 80	400/15500/15	0.0±0.00.0±0.0	0.0±0.06.7±0.6	0.0±0.06.7±0.6	0.0±0.06.7±0.6	0.0±0.07.0±1.0
Drug/Kolliphor^® 188	400/1.0500/1.0	0.0±0.00.0±0.0	0.0±0.08.7±0.6	0.0±0.08.7±0.6	0.0±0.09.0±0.0	0.0±0.09.0±0.0
Drug/Glycerine	400/1.5500/1.5	0.0±0.00.0±0.0	0.0±0.07.7±0.6	0.0±0.08.3±0.6	0.0±0.08.0±0.0	0.0±0.07.0±1.0
Drug/SLS	400/2500/2	0.0±0.00.0±0.0	0.0±0.00.0±0.0	0.0±0.09.0±0.0	0.0±0.01 0.0±0.0	0.0±0.09.3±0.6
Drug/Citric acid	400/2500/2	0.0±0.00.0±0.0	0.0±0.09.0±0.0	0.0±0.08.7±0.6	0.0±0.08.3±0.6	0.0±0.08.3±0.6
Drug/Oleic acid	400/2500/2	0.0±0.00.0±0.0	0.0±0.07.7±0.6	0.0±0.08.0±0.0	0.0±0.07.3±0.6	0.0±0.06.3±0.6
^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
8^b	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

References

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DOI: https://doi.org/10.2478/afpuc-2020-0016 | Journal eISSN: 2453-6725

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Language: English

Page range: 8 - 15

Submitted on: Jul 20, 2020

Accepted on: Feb 7, 2021

Published on: Apr 2, 2021

Published by: Comenius University in Bratislava, Faculty of Pharmacy

In partnership with: Paradigm Publishing Services

Publication frequency: 2 issues per year

Keywords:

Oral dosage form,

gentamicin sulphate,

enterobacteria,

permeation enhancers,

Related subjects:

© 2021 Dozie C. Nwakile, O.C. Dozie-Nwakile, E.I. Okoye, C.E. Umeyor, E.C. Uronnachi, I.K. Uchendu, A.A. Attama, V.C. Okore, published by Comenius University in Bratislava, Faculty of Pharmacy
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Volume 68 (2021): Issue 2 (December 2021)

Non-Absorbable Oral Gentamicin Sulphate: Biopharmaceutical and Dosage Form Evaluation

Figures & Tables

Figure 1

Figure 2

Formula for the production of different batches of gentamicin sulphate oral capsules_

Inhibition zone diameters (IZDs) of some bacteria for selection for the in vitro permeability study_

Average inhibition zone diameter (IZD) (mm) of gentamicin sulphate after 6 h of oral administration at different concentrations_

Baseline gentamicin sulphate dose level using inhibition zone diameter (IZDs) (mm) produced by serum drug level of oral gentamicin sulphate against Staphylococcus aureus_

Inhibition zone diameter (IZDs) (mm) produced by serum drug level of orally co-administered gentamicin sulphate with permeation enhancers against Staphylococcus aureus_

Duration of GIT local activity of orally administered gentamicin sulphate_

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