Abstract
Hydroxypropyl methylcellulose (hypromellose) is a widely known excipient commonly used in the preparation of drug formulations. It can interact with some active pharmaceutical ingredients (APIs), thereby contributing to a reduction in crystallinity, serve as a solvent for API or form stable dispersion with no tendency to aggregation. The aim of the present study was to investigate the effect of hypromellose on the solubility, miscibility and amorphization of paracetamol in mixture with this polymer. Homogenized mixtures of paracetamol with hypromellose were studied using differential scanning calorimetry (DSC), hot-stage microscopy (HSM), Fourier transform infrared (FT-IR) and Raman methods to obtain a deeper insight into the interactions between ingredients in solid state including phase diagram construction for crystalline API and amorphous polymer. A DSC study revealed potential interaction between ingredients resulting in reduced paracetamol crystallinity. This was proved using heating-cooling-heating test to confirm paracetamol amorphization. FT-IR and Raman investigations excluded chemical reaction and hydrogen bonding between ingredients. The phase diagram developed facilitates predictions on the solubility of API in polymer, on the mutual miscibility of ingredients and on the temperature of mixture glass transition.
Highlights
Hydroxypropyl methylcellulose is a widely known excipient used in the pharmaceutical industry for preparing oral, ophthalmic, nasal and topical formulations (Rowe et al, 2009)
Because hypromellose is commonly used as an important excipient in the fabrication of paracetamol drug formulations, the current study was carried out to assess potential interactions between ingredients mixed at differing mass ratios
differential scanning calorimetry (DSC) curves for mixtures prepared using a pestle (Figure 2B, curves b-f) did not display the melting peak of paracetamol for mixtures containing
Summary
Hydroxypropyl methylcellulose (hypromellose, HPMC, MHPC) is a widely known excipient used in the pharmaceutical industry for preparing oral, ophthalmic, nasal and topical formulations (Rowe et al, 2009). As a non-toxic, biodegradable and hydrophilic polymer, hypromellose has recently been used for the development of new formulations such as the sustained-release mucosa adhesive, controlled-release pellets, microcapsules and variety of matrix, multilayers and coating sustained-release and controlled-release formulations (Rowe et al, 2009). It is characterized by high swellability, which significantly effects the release kinetics of incorporated API (Siepmann and Peppas, 2001).
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
