Evaluation of Pharmaceutical Compatibility between Acarbose and Common Excipients Used in the Development of Controlled Release Formulations

Abstract

Background: Excipients are used in the formulation of pharmaceutical dosage forms, but mayinteract with active pharmaceutical ingredients (APIs). Some of these interactions could alterthe physicochemical properties of the APIs which can affect the therapeutic efficacy and safety.Acarbose is an anti-diabetic drug used in this study as an API to investigate its compatibility withcommon excipients in order to development of pharmaceutical controlled release formulations. Methods: For this purpose, 15 different excipients were selected. Binary mixtures of drug witheach of the excipients (1:1 mass ratio) were prepared. Mixtures were analyzed immediately aftermixing and also after incubation at stress conditions (adding 20% water and incubated at 40°Cfor 2 months). The thermal analytical investigation like differential scanning calorimetry (DSC),Fourier transform infra-red spectroscopy (FTIR) and high-performance liquid chromatography(HPLC) were employed for physicochemical evaluations of the possible incompatibility.Photodiode-array (PDA) and mass studies were performed to ensure the peak purity of theHPLC peaks of API in stressed samples. Results: Incompatible excipients with acarbose were determined as EC (ethyl cellulose),Carbopol 934, Hydroxypropyl cellulose, PEG2000 (Polyethylene Glycol 2000), Mg Stearate, NaAlginate and Poloxamer. Conclusion: Results of this study would be used for the development of controlled releaseformulation of acarbose. It is recommended to avoid the use of incompatible excipients.

Assessment of Binary Agarose–Carbopol Buccal Gels for Mucoadhesive Drug Delivery: Ex Vivo and In Vivo Characterization

“…It demonstrated an absorption peak at approximately 768 cm −1 , corresponding to the 3,6-anhydro galactose bending of agarose polymer [ 43 ]. The presence of O-H stretching vibration of CP in the mixture was evident in the region of 1440 cm −1 , which corresponded to similar findings from literature [ 16 , 44 ]. The shift in the -OH vibration to lower values (~3417 cm −1 ) as reported in the literature corresponds to the hydrogen bonding of CP with the hydrophilic groups of AG [ 45 ].…”

Evaluating Novel Agarose-Based Buccal Gels Scaffold: Mucoadhesive and Pharmacokinetic Profiling in Healthy Volunteers

“…Owing to the specific energy absorption by functional groups in the molecule, FTIR interpretation is a simple procedure to identify the specific absorption regions. The FTIR spectral analysis on CP depicted prominent stretching vibration of the carbonyl group (C=O) between 1750 and 1700 cm −1 , whereas the peak in the region of 1450-1400 cm −1 showed the C-O or O-H stretching of the molecule [32] as seen in Figure 5. The band spectrum ~1250-1200 reflected the C-O-C of the acrylate derivative [29].…”

“…Owing to the specific energy absorption by functional groups in the m interpretation is a simple procedure to identify the specific absorption regi spectral analysis on CP depicted prominent stretching vibration of the ca (C=O) between 1750 and 1700 cm −1 , whereas the peak in the region of 1 showed the C-O or O-H stretching of the molecule [32] as seen in Figur spectrum ~1250-1200 reflected the C-O-C of the acrylate derivative [29]. Th was shown by the peak around 1164 cm −1 indicating its stretching vibrat between the 850 and 800 cm −1 represented the C-H out of the plane ben bomers [33].…”