Evaluation of Three Chitin Metal Silicate Co-Precipitates as a Potential Multifunctional Single Excipient in Tablet Formulations

Abstract

The performance of the novel chitin metal silicate (CMS) co-precipitates as a single multifunctional excipient in tablet formulation using direct compression and wet granulation methods is evaluated. The neutral, acidic, and basic drugs Spironolactone (SPL), ibuprofen (IBU) and metronidazole (MET), respectively, were used as model drugs. Commercial Aldactone®, Fleximex® and Dumazole® tablets containing SPL, IBU and MET, respectively, and tablets made using Avicel® 200, were used in the study for comparison purposes. Tablets of acceptable crushing strength (>40 N) were obtained using CMS. The friability values for all tablets were well below the maximum 1% USP tolerance limit. CMS produced superdisintegrating tablets (disintegration time < 1 min) with the three model drugs. Regarding the dissolution rate, the sequence was as follow: CMS > Fleximex® > Avicel® 200, CMS > Avicel® 200 > Dumazole® and Aldactone® > Avicel® 200 > CMS for IBU, MET and SPL, respectively. Compressional properties of formulations were analyzed using density measurements and the compression Kawakita equation as assessment parameters. On the basis of DSC results, CMS co precipitates were found to be compatible with the tested drugs. Conclusively, the CMS co-precipitates have the potential to be used as filler, binder, and superdisintegrant, all-in-one, in the design of tablets by the direct compression as well as wet granulation methods.

Compaction and tableting properties of composite particles of microcrystalline cellulose and crospovidone engineered for direct compression

“…Each tablet was prepared by manual filling of powder weighing~80 mg into the die cavity measuring 5 mm and compressed at a speed of 120 mm/min at compression loads ranging from 100 to 500 kg (50-250MPa). For each pressure, a minimum of five tablets were compressed for reproducibility [13].…”

Poriferan Chitin as a Versatile Template for Extreme Biomimetics

“…Analysis of FTIR and Raman spectra suggest that the chitin scaffold interacts with silica by hydrogen bond formation; especially at the C(6) position [157,161,186]. The results of the hydrothermal silicification of chitin open new possibilities for synthesis of chitin-silica composites, which gain particular interest in the development of bone substitutes for tissue engineering [77,187]; waste water treatment [188], and drug delivery systems [189].…”

Chitin and Chitosan as Direct Compression Excipients in Pharmaceutical Applications

“…In the search for new multifunctional excipients with strong binding, good flow, and fast disintegration characteristics, there has been a focus on silicon derivatives. Initially, silicon dioxide was co-precipitated onto chitosan and chitin at a 1:1 mass ratio [ 10 , 50 , 51 , 119 ]. In addition to enhanced binding and disintegration properties, the compressibility improved in comparison to their initial properties.…”

“…The DA and molecular weight (MW) are important parameters to be examined because they affect the physical and chemical properties of chitin and chitosan [ 8 , 10 ]. The acetylated units prevail in chitin (DA typically > 90%), while chitosan has a typical DA of less than 35%.…”