Evaluation Of Spheronized Pellets As Potential Matrix Sustained Release Dosage Form
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Date
1995-02
Authors
Bee Cheng, Lee
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Abstract
Satisfactory spherical pellets were successfully· prepared by the process of
extrusionlspheronization using the excipient microcrystalline cellulose (IvrCC) as
pellet-forming material. Nonetheless, the preparation of acceptable round spheres
is highly dependent upon the attainment of an optimal formulation suited for this
mcthod or proccssillg. The earlier part of the work has revealed that the MCe
pellet system containing the active ingredientdiclofenac sodium generally produced
strongly bonded spheroids which remained intact throughout the dissolution test. It
may thus be postulated that the pellets behaved as an inert matrix system.
The effecl of some excipients on the pellet quality and physical properties of
diclofenac sodium-containing pellets was investigated. Certain disintegrants used
,
were fot~d to have a marked influence on the quality of the pellets. In addition,
rapid pellet disintegration and dissolution were observed for the soybean oilformulated
pellets, suggesting the potential of soybean oil as a disintegrating agent
in pellet dosage form. However, when two other model drugs of varying aqueous
solubilities, namely paracetamol and artemisinin, were separately incorporated into
the soybean oil-containing formulations and compared, differences in the physical
characteristics of the pellets such as disintegration and in vitro drug release were
observed. The artemisinin-formulated pellets did not disintegrate and at the same
time showed a considerably slower dissolution release rate than the pellets
containing either diclofenac sodium or paracetamol, which are of higher aqueous
solubilities. Since the former preparation exhibited no disintegration and produced
an in vitro dissolution profile characteristic of sustained release products, it is
apparent that the incorporated soybean oil failed to act as a disintegrant in the
evident that both fast- and slow-release spherical pelleted products can be prepared
via the extrusion/spheronization technique.
In vivo evaluation of the artemisinin-containing preparation in five healthy human
subjects, produced relatively uniform plasma concentration versus time profiles that
were reflective of a slow and sustained rate of absorption. Moreover, the
preparation showed a comparable extent of absorption than that of the drug
administered as an aqueous suspension. Plasma concentrations of the drug wer~
determined using a developed HPLC method. A satisfactory correlation was
obtained between the in vitro dissolution rate measurements and its in' vivo
pharmacokinetic findings.
Description
Keywords
Spheronized Pellets , Dosage Form