Skip to Content
Merck
  • Mechanistic study of carvacrol processing and stabilization as glassy solid solution and microcapsule.

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
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Supelco
Sodium hydroxide concentrate, 0.1 M NaOH in water (0.1N), Eluent concentrate for IC
Sigma-Aldrich
Methanol, NMR reference standard
Sigma-Aldrich
Sodium hydroxide, BioUltra, for luminescence, ≥98.0% (T), pellets
Sigma-Aldrich
Sodium hydroxide solution, BioUltra, for molecular biology, 10 M in H2O
Sigma-Aldrich
Formamide, BioUltra, for molecular biology, ≥99.5% (T)
Supelco
Sodium hydroxide solution, 49-51% in water, eluent for IC
Supelco
Methanol, analytical standard
Sigma-Aldrich
Methanol, anhydrous, 99.8%
Sigma-Aldrich
Methanol, low water for titration
Sigma-Aldrich
Methanol, HPLC Plus, ≥99.9%, poly-coated bottles
Sigma-Aldrich
Sodium hydroxide, BioXtra, ≥98% (acidimetric), pellets (anhydrous)
Sigma-Aldrich
Sodium hydroxide solution, 1.0 N, BioReagent, suitable for cell culture
Sigma-Aldrich
Formamide, BioReagent, ≥99.5% (GC), for molecular biology
Sigma-Aldrich
N,N′-Disuccinimidyl carbonate, purum, ≥95.0% (NMR)
Sigma-Aldrich
Methanol, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Formamide, ReagentPlus®, ≥99.0% (GC)
Sigma-Aldrich
3-Ethyl-2,4-pentanedione, mixture of tautomers, 98%
Sigma-Aldrich
N,N′-Disuccinimidyl carbonate, ≥95%
Sigma-Aldrich
Methanol, AR, ≥99.5%
Sigma-Aldrich
Sodium hydroxide, anhydrous, free-flowing, Redi-Dri, reagent grade, ≥98%, pellets
Sigma-Aldrich
Sodium hydroxide solution, 0.1 N
Supelco
Methanol, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Methanol, LR, ≥99%
Sigma-Aldrich
Methanol, anhydrous, ≥99.5%
Sigma-Aldrich
Sodium hydroxide, AR, pellets, ≥98.5%
Sigma-Aldrich
Sodium hydroxide, LR, flakes, ≥96%
Sigma-Aldrich
Methanol, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Sodium hydroxide, puriss. p.a., ACS reagent, reag. Ph. Eur., K ≤0.02%, ≥98%, pellets
Sigma-Aldrich
Sodium hydroxide, pellets, semiconductor grade, 99.99% trace metals basis
Sigma-Aldrich
Sodium hydroxide, ACS reagent, ≥97.0%, pellets