Thermal behaviour of procaine and benzocaine Part II: compatibility study with some pharmaceutical excipients used in solid dosage forms

Abstract

BackgroundThe compatibility study of active substances with excipients finds an important role in the domain of pharmaceutical research, being known the fact that final formulation is the one administered to the patient. In order to evaluate the compatibility between active substance and excipients, different analytical techniques can be used, based on their accuracy, reproducibility and fastness.ResultsCompatibility study of two well-known active substances, procaine and benzocaine, with four commonly used excipients, was carried out employing thermal analysis (TG/DTG/HF) and Fourier Transform Infrared Spectroscopy (UATR-FT-IR). The selected excipients were microcrystalline cellulose, lactose monohydrate, magnesium stearate and talc. Equal proportion of active substance and excipients (w/w) was utilized in the interaction study. The absolute value of the difference between the melting point peak of active substances and the one corresponding for the active substances in the analysed mixture, as well the absolute value of the difference between the enthalpy of the pure active ingredient melting peak and that of its melting peak in the different analysed mixtures were chosen as indexes of the drug-excipient interaction degree. All the results obtained through thermal analysis were also sustained by FT-IR spectroscopy.ConclusionsThe corroboration of data obtained by thermal analysis with the ones from FT-IR spectroscopy indicated that no interaction occurs between procaine and benzocaine, with microcrystalline cellulose and talc, as well for the benzocaine-lactose mixture. Interactions were confirmed between procaine and benzocaine respectively and magnesium stearate, and for procaine and lactose.

DSC kinetic study of the incompatibility of doxepin with dextrose

“…Any change in position or intensity, disappearance and appearance of an absorption band in IR spectra can refer to drug-excipient interactions [11,12].…”

Compatibility studies of hydrocortisone with excipients using thermogravimetric analysis supported by multivariate statistical analysis

“…Preformulation stage of solid dosage formulations includes detection of possible interactions of an active pharmaceutical ingredient (API) with excipients [1][2][3][4]. Chemical interactions result in reduction of API quantity in the formulation that can lower its absorption and therapeutic effect.…”

Sodium alendronate used in bone treatment

“…Therefore, by the following discussions, the HF signal of the binary mixtures studied will be analyzed in respect with the signal recorded for A at 270°C. Talc and SiO 2 are known as highly thermal and chemically stable compounds, and therefore they are used as ''inert standards'' in compatibility studies [15,16]. By investigating Figs.…”

“…According to [5] and some of our previous papers [11][12][13][14][15][16], the thermal behavior of these binary mixtures was studied under non-isothermal conditions in order to detect the thermally induced interactions.…”