Characterization of a crosslinked high amylose starch excipient.
A controlled release excipient based on sodium trimetaphosphate (STMP) crosslinked high amylose starch has been examined by 13C CP/MAS NMR. The dry excipient powder is pressed to a hard tablet whose volume increase in H2O runs parallel to the STMP concentration used. The known polymorph resonances of single helix 'V' starch (hydrated) and double helix 'B' starch (hydrated) both contribute to the spectrum corresponding to the swollen tablet. The wet tablet when loaded with a pharmaceutical agent provides a near zero-order release profile for up to 20 h. The swelling and drug release behaviour is explained in terms of self-assembly of the STMP treated starch nanomolecular particles. These particles are drawn together by "self-assembly" due to formation of amylose double helices as water penetrates the tablet. An optimum level of chemical crosslinking ensures the integrity of the swollen tablet whose sponge-like structure enclosed by a membranous surface is responsible for sustained release.
Le Bail
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McGill University, Department of Chemistry, Montreal, Que., Canada.
Morin
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FG
Marchessault
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RH
D000688:Amylose / Q000737:chemistry; D003432:Cross-Linking Reagents / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008855:Microscopy, Electron, Scanning; D011122:Polyphosphates / Q000737:chemistry*; D013213:Starch / Q000737:chemistry*; D014961:X-Ray Diffraction
D003432:Cross-Linking Reagents; D011122:Polyphosphates; D013213:Starch; D000688:Amylose; C009293:trimetaphosphoric acid