The effect of mechanical grinding on the formation and crystallinity changes of the inclusion complex of acetaminophen and?-cyclodextrin

Lin, Shan‐Yang; Lee, Chun-Sen

doi:10.1007/bf01080458

Cited by 15 publications

(4 citation statements)

References 19 publications

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“…The average R f values for both the RBG reference and inclusion complexes in ethanol were the same (0.49), which could be due to the inclusion complex having dissolved in ethanol [ 43 , 44 ]. On the other hand, no spot was noted in ethyl acetate because RBG was encapsulated into the cavity for both CDs and no decomposed compound occurred in ethyl acetate [ 45 ]. Combined with the above FTIR, PXRD, DSC, SEM, and TLC results, all these results confirmed that RBG formed inclusion complexes with β-CD and HP-β-CD, and no complex was formed by their physical mixture.…”

Section: Resultsmentioning

confidence: 99%

Enhancement of Dissolving Capacity and Reducing Gastric Mucosa Irritation by Complex Formation of Resibufogenin with β-Cyclodextrin or 2-Hydroxypropyl-β-cyclodextrin

et al. 2022

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Resibufogenin (RBG) is a natural medicinal ingredient with promising cardiac protection and antitumor activity. However, poor solubility and severe gastric mucosa irritation restrict its application in the pharmaceutical field. In this study, the inclusion complex of RBG with β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) was prepared using the co-evaporation method, and the molar ratio of RBG to CD was determined to be approximately 1:2 by continuous variation plot for both CDs. The formation of inclusion complexes between RBG and each CD (RBG/β-CD and RBG/HP-β-CD) was evaluated by phase solubility study, Fourier transform infrared spectroscopy, and thin-layer chromatography. Powder X-ray diffraction and differential scanning calorimetry confirmed drug amorphization and encapsulation in the molecular cage for both CDs. Moreover, the inclusion complexes’ morphologies were observed using scanning electron microscopy. The dissolution rate of the inclusion complexes was markedly improved compared to that of RBG, and the complexes retained their antitumor activity, as shown in the in vitro cytotoxicity assay on a human lung adenocarcinoma cancer (A549) cell line. Moreover, less gastric mucosal irritation was observed for the inclusion complex. Thus, the inclusion complex should be considered a promising strategy for the delivery of poorly water-soluble anticancer agents, such as RBG.

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Section: Resultsmentioning

confidence: 99%

Enhancement of Dissolving Capacity and Reducing Gastric Mucosa Irritation by Complex Formation of Resibufogenin with β-Cyclodextrin or 2-Hydroxypropyl-β-cyclodextrin

et al. 2022

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“…This endothermic peak might be related to polymorphism or a molecular interaction. In this study, grinding and heating processes were used to examine the unknown peak at 145 ~ because both are supposed to be able to improve the inclusion complex formation between acetaminophem and fl-eyclodextrin [20][21]. Figure 4 shows the effect of grinding on the DSC curves of CPZ and the CPZ-magnesium stearate mixture.…”

Section: Resultsmentioning

confidence: 99%

Compatibility problems of chlorpromazine HCl-stearate lubricants examined by differential scanning calorimetry

Lin¹,

Kao²

1990

Journal of Thermal Analysis

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Differential scanning calorimetry (DSC) was used to investigate the interactions between chlorpromazine HC1 (CPZ) and stearate lubricants. The phase diagram was constructed for each CPZ-stearate system. An unknown endothermic peak at 145~ was found for the CPZstearate lubricants; this was affected by the grinding and heating processes. This unknown endothermic peak proved to relate to a polymorphism transition but was not an incompatibility problem. Three polymorphisms of CPZ were also determined by DSC analysis and IR spectrophotometry.It is well known that drug-excipient interactions can exert significant influences on the physico-chemical properties, manufacture and bioavailability of a solid dosage form [1][2][3]. Drug-excipient compatibility testing is a practically reliable preformulation tool to select appropriate excipients for each dosage form design. Thermal methods such as differential thermal analysis (DTA) or differential scanning calorimetry (DSC) are welldeveloped techniques for the detection of incompatibility in drug-excipient mixture [4][5][6]. Since the thermal analysis used is relatively fast, easily interpreted, accurately predictive, and requires only a few test samples, it has been suggested in many studies for the routine screening of potential drugexcipient interactions in preformulation stability testing [7][8][9][10].

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“…The peculiar thermal behavior of PA-betaCD kneaded mixtures (exo-endo sequence) has been observed also in other drug-cyclodextrin systems [6]. Amorphization actually represents a rather common result of cogrinding or freeze-drying drug-cyclodcxtfins mixtures and it must be considered when flat thermal profiles and X-ray diffraction patterns on powder are invoked as evidences of inclusion [7].…”

Section: Discussionmentioning

confidence: 96%

Solid-state microcalorimetry on drug-cyclodextrin binary systems

Giordano

Bruni

Bettinetti

1992

Journal of Thermal Analysis

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Differential scanning calorimetry DSC has been applied to the analysis of drugcyclodextrin binary systems in order to gain experimental evidence of the interaction and determine the stoichiometry of the inclusion compound. Two model systems, paracetamolbetacyclodextrin and vinburnineg-ammacyclodextrin were tested through the comparison of thermal behaviors of interacted and non-interacted mixtures containing excess drug. DSC allowed a confirmation of both interaction and stoichiometry of the inclusion compounds.

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The effect of mechanical grinding on the formation and crystallinity changes of the inclusion complex of acetaminophen and?-cyclodextrin

Cited by 15 publications

References 19 publications

Enhancement of Dissolving Capacity and Reducing Gastric Mucosa Irritation by Complex Formation of Resibufogenin with β-Cyclodextrin or 2-Hydroxypropyl-β-cyclodextrin

Enhancement of Dissolving Capacity and Reducing Gastric Mucosa Irritation by Complex Formation of Resibufogenin with β-Cyclodextrin or 2-Hydroxypropyl-β-cyclodextrin

Compatibility problems of chlorpromazine HCl-stearate lubricants examined by differential scanning calorimetry

Solid-state microcalorimetry on drug-cyclodextrin binary systems

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