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Merck

Evaluation of dibutyrylchitin as new excipient for sustained drug release.

Drug development and industrial pharmacy (2011-11-30)
Luca Casettari, Marco Cespi, Enzo Castagnino
RESUMEN

Dibutyrylchitin (DBC), a lipophilic chitin diester, has been synthesized from chitin and butyric anhydride with methanesulfonic acid as catalyst. Exhaustive esterification of free alcoholic groups of chitin was assessed by FT-IR and (1)H-NMR spectroscopy. High degree of alkyl substitution allowed DBC to acquire an almost completely lipophilic character. Tablets of paracetamol and metformin employing DBC as major excipient, in comparison with starch, microcrystalline cellulose, lactose and polyvinylpyrrolidone, were prepared and rates of drug release were checked by dissolution test assays. DBC released drug at a lower rate than that of the other tested materials. A comparison study of rate release of metformin from DBC tablets and from metformin-hydroxypropyl methylcellulose prolonged release oral formulation available on the market has been also curried out. Under the same conditions and in the presence of the same amount of loaded drug, DBC released 64% of metformin whereas hypromellose-based tablets released 87%.

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Sodium methanesulfonate, 98%
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Methanesulfonic acid, ≥99.0%
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Potassium methanesulfonate, ≥98.0% (dry substance, T)
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Silver methanesulfonate
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Methanesulfonic acid solution, 70 wt. % in H2O
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Supelco
Methanesulfonic acid solution, 0.1 M CH3SO3H in water (0.1N), eluent concentrate for IC
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Butyric anhydride, purum, ≥97.0% (NT)
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Methanesulfonic acid solution, 4 M (with 0.2% (w/v) tryptamine)
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