Purpose:
To develop sustained release matrix tablets of diltiazem
hydrochloride (DTZ) using karaya gum (K) alone or in
combination with locust bean gum (LB) and hydroxypropyl
methylcellulose (H).
Methods:
Matrix tablets of DTZ were prepared at different ratios
of drug:gum (1:1, 1:2, and 1:4) and of the gum blends
(K, K/LB, K/H and K/LB/H) by direct compression. The
matrix tablets were evaluated for hardness, friability,
in vitro release and drug content. The formulations were
also characterised by scanning electron microscopy (SEM),
Fourier transform infra-red spectroscopy (FTIR) and
differential scanning calorimetry (DSC). A commercial
diltiazem hydrochloride product Dilzem SR, was used as a
reference for comparison
Results:
Tablets with only K or K/H had the highest mean
dissolution time (MDT), the least dissolution efficiency
(DE, 12 %), and released drug by swelling, diffusion and
erosion mechanisms. Karaya gum or combinations with
locust bean gum sufficiently controlled drug release,
while combinations of KH and KLBH exhibited high and low
drug release efficiency, respectively. SEM images of the
tablets before and after dissolution showed
morphological changes on the tablet surface while FTIR
and DSC studies indicate that there was no chemical
interaction between the drug and the polymers. Three of
the formulations compared well with the reference (p <
0.05) in terms of release characteristics.
Conclusion:
The results of the study demonstrate that karaya gum
alone or in suitable combination with locust bean gum
and hydroxypropyl methylcellulose is suitable for
formulating sustained-release matrix tablets of
diltiazem.
Key words:
Karaya gum, Locust bean gum, Diltiazem hydrochloride,
Sustained release, Hydroxypropyl methylcellulose.