Saltar al contenido
Merck

Mechanistic study of carvacrol processing and stabilization as glassy solid solution and microcapsule.

International journal of pharmaceutics (2014-12-17)
Markus W Tackenberg, Carola Geisthövel, Andreas Marmann, Heike P Schuchmann, Peter Kleinebudde, Markus Thommes
RESUMEN

Essential oils and other liquid active pharmaceutical ingredients (APIs) are frequently microencapsulated to improve shelf life, handling, and for tailoring release. A glassy solid solution (GSS), a single-phase system, where the excipient is plasticized by the API, could be an alternative formulation system. Thus this study focuses on the investigation of two formulation strategies using carvacrol as a model compound, namely a microcapsule (MC) and a glassy solid solution (GSS). Applying the solubility parameter approach, polyvinylpyrrolidone (PVP) was chosen as a suitable matrix material for a GSS system, whereas maltodextrin and sucrose served as excipients for a microcapsule (MC) system. Differential scanning calorimetry (DSC) measurements of the excipients' glass transition temperatures and the melting point of carvacrol verified plasticizing properties of carvacrol on PVP. Batch mixing processes, as preliminary experiments for future extrusion processes, were performed to prepare GSSs and MCs with various amounts of carvacrol, followed by crushing and sieving. Maximally 4.5% carvacrol was encapsulated in the carbohydrate material, whereas up to 16.3% were stabilized as GSS, which is an outstanding amount. However, grinding of the samples led to a loss of up to 30% of carvacrol.

MATERIALES
Referencia del producto
Marca
Descripción del producto

Sigma-Aldrich
Metanol, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Diclorometano, suitable for HPLC, ≥99.8%, contains amylene as stabilizer
Sigma-Aldrich
Metanol, ACS reagent, ≥99.8%
Sigma-Aldrich
Diclorometano, contains 40-150 ppm amylene as stabilizer, ACS reagent, ≥99.5%
Sigma-Aldrich
Hidróxido de sodio, ACS reagent, ≥97.0%, pellets
Sigma-Aldrich
Hidróxido de sodio, reagent grade, ≥98%, pellets (anhydrous)
Sigma-Aldrich
Hidróxido de sodio solution, 50% in H2O
Sigma-Aldrich
Metanol, HPLC Plus, ≥99.9%
Sigma-Aldrich
Diclorometano, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%, contains 50-150 ppm amylene as stabilizer
Sigma-Aldrich
Formamida, ReagentPlus®, ≥99.0% (GC)
Sigma-Aldrich
Hidróxido de sodio solution, BioUltra, for molecular biology, 10 M in H2O
Sigma-Aldrich
Metanol, suitable for HPLC, gradient grade, suitable as ACS-grade LC reagent, ≥99.9%
Sigma-Aldrich
Hidróxido de sodio, BioXtra, ≥98% (acidimetric), pellets (anhydrous)
Sigma-Aldrich
Hidróxido de sodio solution, 1.0 N, BioReagent, suitable for cell culture
Sigma-Aldrich
Hidróxido de sodio, puriss., meets analytical specification of Ph. Eur., BP, NF, E524, 98-100.5%, pellets
Sigma-Aldrich
Hidróxido de sodio, reagent grade, 97%, powder
Sigma-Aldrich
Diclorometano, ACS reagent, ≥99.5%, contains 40-150 ppm amylene as stabilizer
Sigma-Aldrich
Metanol, Laboratory Reagent, ≥99.6%
Sigma-Aldrich
Formamida, BioReagent, ≥99.5% (GC), for molecular biology
Sigma-Aldrich
Hidróxido de sodio, pellets, semiconductor grade, 99.99% trace metals basis
Sigma-Aldrich
Metanol, BioReagent, ≥99.93%
Sigma-Aldrich
Formamida, BioUltra, for molecular biology, ≥99.5% (T)
Sigma-Aldrich
Metanol, Absolute - Acetone free
Sigma-Aldrich
Metanol, ACS spectrophotometric grade, ≥99.9%
Sigma-Aldrich
Hidróxido de sodio solution, 5.0 M
Sigma-Aldrich
L-Lysine monohydrochloride, from non-animal source, meets EP, JP, USP testing specifications, suitable for cell culture, 98.5-101.0%
Sigma-Aldrich
Metanol, ACS reagent, ≥99.8%
Sigma-Aldrich
Hidróxido de sodio, beads, 16-60 mesh, reagent grade, 97%
USP
Metanol, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
N,N′-Disuccinimidyl carbonate, ≥95%