Chitinosans as tableting excipients for modified release delivery systems.
The term 'chitinosans' embraces the spectrum of acetylated poly(N-glucosamines) ranging from chitin to chitosan. Chitinosans (I), at acidic pH, have protonated amines which can interact with oppositely charged drug ions and, thereby, modify drug release from drug delivery systems. Tablets were compressed from a physical mixture containing salicylic acid (II) as the model drug, I, and magnesium stearate. Five commercial I compounds, varying in degree of deacetylation and molecular weight, were selected. Tablets were compressed at 5000, 10 000, and 15 000 psig using a Carver and a single punch tablet press. The differential scanning calorimetry thermograms provided evidence of I-II interaction in the powder blend. Analysis of variance (ANOVA) indicated that the compression pressure did not significantly affect the crushing strength (CS) or the release profile of II from the I-matrix tablets (P?0.05). Furthermore, the ANOVA also indicated that the tablet press used during manufacture did not affect the above properties (P?0.05); however, the chitinosans significantly affected the CS as well as the release profile of II from I-matrix tablets (P<0.05). This study provides further evidence for the use of commercial I compounds as excipients for use in modified release drug delivery systems.
Rege
P R
PR
Department of Medicinal Chemistry and Pharmaceutics, 437 Mellon Hall of Science, School of Pharmacy, Duquesne University, Pittsburgh, PA 15282, USA.
Shukla
D J
DJ
Block
L H
LH
D000107:Acetylation; D000117:Acetylglucosamine / Q000031:analogs & derivatives / Q000737:chemistry; D000704:Analysis of Variance; D002240:Carbohydrate Sequence; D002686:Chitin / Q000031:analogs & derivatives* / Q000737:chemistry*; D019245:Compressive Strength; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D008969:Molecular Sequence Data; D008970:Molecular Weight; D020156:Salicylic Acid / Q000737:chemistry; D013607:Tablets
D003692:Delayed-Action Preparations; D005079:Excipients; D013607:Tablets; D002686:Chitin; D020156:Salicylic Acid; D000117:Acetylglucosamine