Spray-dried high-amylose sodium carboxymethyl starch: impact of α-amylase on drug-release profile.
Drug Dev Ind Pharm
; 42(11): 1887-93, 2016 Nov.
Article
in En
| MEDLINE
| ID: mdl-27109692
ABSTRACT
Spray-dried high-amylose sodium carboxymethyl starch (SD HASCA) is a promising pharmaceutical excipient for sustained-release (SR) matrix tablets produced by direct compression. The presence of α-amylase in the gastrointestinal tract and the variations of the gastric residence time of non-disintegrating dosage forms may affect the presystemic metabolism of this excipient and, consequently, the drug-release profile from formulations produced with SD HASCA. In this study, the influence of α-amylase and the residence time in acidic conditions on the drug-release profile was evaluated for a once-daily acetaminophen formulation (Acetaminophen SR) and a once-daily tramadol hydrochloride formulation (Tramadol SR). Both formulations were based on SD HASCA. α-Amylase concentrations ranging from 0 IU/L to 20000 IU/L did not significantly affect the drug-release profiles of acetaminophen and tramadol hydrochloride from SD HASCA tablets (f2 > 50) for all but only one of the studied conditions (f2 = 47). Moreover, the drug-release properties from both SD HASCA formulations were not significantly different when the residence time in acidic medium was 1 h or 3 h. An increase in α-amylase concentration led to an increase in the importance of polymer erosion as the main mechanism of drug-release instead of drug diffusion, for both formulations and both residence times, even if release profiles remained comparable. As such, it is expected that α-amylase concentration and residence time in the stomach will not clinically affect the performance of both SD HASCA SR formulations, even if the mechanism of release itself may be affected.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Starch
/
Tablets
/
Drug Carriers
/
Alpha-Amylases
/
Amylose
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Acetaminophen
Language:
En
Journal:
Drug Dev Ind Pharm
Year:
2016
Type:
Article
Affiliation country:
Canada