FORMULATION STUDIES OF ACACIA SIEBERIANA GUM IN CHOROQUINE AND METRONIDAZOLE MATRIX TABLETS
FORMULATION STUDIES OF ACACIA SIEBERIANA GUM IN CHOROQUINE AND METRONIDAZOLE MATRIX TABLETS
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Date
2006-11
Authors
OYETUNJI, Shittu Abiodun
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Abstract
The crude plant gum from African Acacia sieberiana was purified and investigated
for use as a matrix excipient for chloroquine phosphate and metronidazole tablet
formulations. The chromatographic analysis of the acid hydrolysed gum revealed
the presence of rhamnose, galactose, ribose, xylose and fructose. The viscosity was
found to increase with increase in concentration of the gum. Ten percent mucilage
had pH of 5 and pH change has no effect on the viscosity of the mucilage Both the
swelling and hydration capacity showed that water penetration and retention of the
gum were very high, as such it could not maintain slow release for a long period.
The various particle size fractions of the gum had good flow rate with angle of
repose less than 30o. The compressibility (densification) of the different particle
sizes was investigated and found to be highly compressible at low compression
pressure (1.8 to 3.1 x 105 N/m2 ). The compactibility studies revealed that radial
tensile strength of the gum increases with increase in compression pressure. The
compactness was found to increased with decrease in particle size, while the
dissolution rate decreased with decrease in particle size of the gum. The t90% for the
matrices made of >125-150 μm and >150-250 μm particle sizes were 2h 12 min
and 38 min respectively. The effects of concentration of the gum on compactness
and dissolution rate of compacts directly compressed revealed decrease in
compactness with decrease in concentration of gum. Increase in concentration of
gum was found to have profound effects on drug release rate from tablets
formulated by direct compression method. The chloroquine phosphate matrices containing 60 %,50 %, and 40 %, corresponding to batches 1, 2 and 3 respectively,
were subjected to dissolution test. The t90% s for the three batches were 3 h 30 min,
1 h 45 min and 1 h 40 min respectively. The dissolution efficiencies (DE) at 1 h for
the three batches were found to be 37 %, 71 % and 75 % respectively. The release
rate of chloroquine and metronidazole (wet granulation method) was evaluated
based on t90% and dissolution efficiency (DE) at 1 h. The DE ( 1 h ) for the batches
1 of test gum chloroquine matrix, test gum metronidazole matrix and standard
[Acacia Senegal] gum chloroquine matrix were: 98 %, 34 %, and 92 %
respectively. The USA,FDA similarity factor “f2 “value for the dissolution data
between test and standard gum was found to be >50, this signifies that, there is no
significant difference in dissolution. While the f2 value for the test gum matrices of
chloroquine and metronidazole dissolution data was <50, this indicate a significant
difference in dissolution between the two formulations. In conclusion, Acacia
sieberiana gum has been found to be directly compressible, a good material for wet
granulation, and a potential gum matrix excipient for delaying the release of drug,
particularly poorly soluble drugs.
Description
A THESIS SUBMITTED TO POST GRADUATE SCHOOL AHMADU BELLO
UNIVERSITY IN PARTIAL FULFILLMENT OF THE REQUIREMENT FOR THE
AWARD OF THE DEGREE OF MASTER OF SCIENCE IN PHARMACEUTICS
DEPARTMENT OF PHARMACEUTICSAND PHARMACEUTICAL MICROBIOLOGY,
FACULTY OF PHARMACEUTICAL SCIENCES,
AHMADU BELLO UNIVERSITY,
ZARIA, NIGERIA
Keywords
FORMULATION STUDIES,, ACACIA SIEBERIANA GUM,, CHOROQUINE,, METRONIDAZOLE MATRIX TABLETS.