• Journal of Pharmaceutical Investigation
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• 제41권2호
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• pp.83-90
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• 2011

Main objectives of this study were to investigate the effects of a lubricant, magnesium stearate, as blended in a hydrophilic matrix tablet and to identify significant factors using a tablet ejection force and a swelling property. The characteristics of tablet ejection were evaluated with three different compression forces (30, 40, and 60 MPa) and two controlled factors, amount of magnesium stearate and its mixing time. A hydrophilic model drug (terazosin HCl dihydrate) was regarded as a default factor. Tablet swelling was also evaluated. The optimal amount of PEG compared to PEO was set to be 88.50% w/w. As the amount of magnesium stearate was varied from 0.79% to 2.20% w/w, the amount of PEO and PEG was adjusted to meet the tablet's total weight while maintaining the ratio between the two excipients constant. As the mixing time of magnesium stearate was increased, the tablet ejection force and the swelling property were decreased. As the amount of magnesium stearate was increased, the tablet ejection force and the swelling property were decreased since the increased mixing time and the amount of magnesium stearate induced hydrophobic properties of the matrix tablet more effectively. The ejection force of the tablet increased as a result of increase in the compression force, which means that the breaking of tablet/die-wall adhesion energy was also increased when the compression energy was increased. The results gavea valuable guide how to choose suitable amount of the lubricant with processing conditions for the development of hydrophilic matrix formulations.

• 한국임상약학회지
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• 제33권2호
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• pp.86-96
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• 2023

Background: Using KIDS-KAERS database (KIDS-KD) from 2016 to 2020, the aim is to investigate signals of adverse events of alpha-adrenoceptor antagonists and to present adverse events that are not included in the precautions for use when marketing approval. Methods: This study was conducted by disproportionality analysis. Data mining analysis was performed to detect signals of alpha-adrenoceptor antagonists, such as terazosin, doxazosin, alfuzosin, silodosin, and tamsulosin. The signal was defined by three criteria as proportional reporting ratio (PRR), reporting odds ratio (ROR), and information component (IC). Detected signals were compared with product labeling and the European Medicines Agency-Important Medical Events list. Results: Out of the total number of 408,077 reports for adverse events, 6,750 cases were reported as adverse events of alpha-adrenoceptor antagonists. Dizziness, mouth dryness, hypotension postural, and oedema peripheral are identified as common adverse events of five alpha-adrenoceptor antagonists and are typically listed on drug labels. However, new signals were detected for pneumonia, chronic obstructive airway disease, eye diseases such as glaucoma and cataracts, fracture, and ileus of tamsulosin that were not previously listed on the drug labels in Korea. Conclusions: This study identified signals related to adverse drug reactions of alpha-adrenoceptor antagonists and presented serious adverse events, suggesting new adverse reactions to be aware of when using alpha-adrenoceptor antagonists.