Effects of Hydrophilic Excipients and Compression Pressure on Physical Properties and Release Behavior of Aspirin-Tableted Microcapsules

Abstract

Aspirin ethylcellulose microcapsules were tableted by compression with or without excipients (lactose or polyvinylpyrrolidone [PVP]). The effects of the amount of the excipients and microcapsule size on the crushing strength and release rate of aspirin from tableted microcapsules were investigated. Tablets without excipients had a crushing strength that was independent of the applied pressure and microcapsule size. An increase in compression pressure from 15 to 60 MPa resulted in an increase in the crushing strength of tablets containing 20% or 40% w/w lactose, but the reverse results were obtained for the tableted microcapsules containing 20% or 40% w/w PVP. Results showed that the release rate of aspirin from microcapsules containing lactose or PVP was independent of the compression pressure with the exception of tablets containing 40% w/w lactose. In vitro release profiles of aspirin from tableted microcapsules containing lactose or PVP showed that increasing the concentration of the excipients resulted in an increase in the release rate of aspirin. Values of n were changed by the compression pressure and the added excipients.

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“…Tablet hardness and disintegration time increase with an increase in compression force ( Table 7 and Table 8). It is in consistent with the findings of the affect of compression forces on Aspirin tablets 21 and Cefuroxime Axetil 22 .…”

Impact of Crystal Habit on Solubility of Ticagrelor

“…The growth rate of the crystal surface will be controlled by a combination of structure-related factors, such as dislocations and intermolecular bonds, and by exterior factors such as solvents, rate of agitation, additives, temperature, etc. [28][29][30][31][32][33][34][35].This study aims to systematically investigate how crystal behavior affects the ticagrelor's solubility. TICA form II (TICA-II) with different crystal habits were prepared by controlling the crystallization process.…”

Analysis of Counterfeit Pharmaceutical Tablet Cores Utilizing Macroscopic Infrared Spectroscopy and Infrared Spectroscopic Imaging

“…10À14 As a consequence, having the proper crystalline form of the API can be just as important as having the correct API. 15 Since excipients also directly affect drug release efficacy, API stability, 16À19 and tablet pH, 20 similar health hazards can be associated with having an improper excipient profile. The presence of the incorrect excipients and/or absence of correct excipients can create API ABSTRACT: Advantages and limitations of analyzing authentic and counterfeit pharmaceutical tablets with both macro (nonimaging) attenuated total internal reflection Fourier transform infrared (ATR-FT-IR) spectroscopy and micro ATR-FT-IR spectroscopic imaging have been evaluated.…”

“…with limited sample preparation. − Further, these techniques can often differentiate API polymorphs (different API crystalline forms). , This capability is important since the crystalline form of an API can affect its efficacy, stability, and solubility, which can have a significant impact on the toxicity of the drug and/or the bioavailability of the drug in the body. − As a consequence, having the proper crystalline form of the API can be just as important as having the correct API . Since excipients also directly affect drug release efficacy, API stability, − and tablet pH, similar health hazards can be associated with having an improper excipient profile. The presence of the incorrect excipients and/or absence of correct excipients can create API stability issues, which can lead to faster API degradation, higher impurity levels, and ultimately a greater potential for adverse patient reactions. − Because vibrational spectroscopic techniques are selective and sensitive to most APIs, excipients, and subtle API crystallinity differences, the role of these techniques is continuing to expand for the analysis of counterfeit pharmaceutical products. ,− …”