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Asian Journal of Pharmaceutical Sciences 2018年第2期13卷 113-119页

作者： Takashi Osamura Yoshiko Takeuchi Risako Onodera Masahiro Kitamura Yoshiteru Takahashi Kohei Tahara Hirofumi Takeuchi Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University Pharmaceutical Technology Department Sawai Pharmaceutical Co.Ltd

We previously determined "tableting properties" by using a multi-functional single-punch tablet press(GTP-1). We plotted "Compactability" on the x-axis against "Manufacturability"on the y-axis to allow visual evaluation of "tableting properties". Here, we examined whether this evaluation method can be used in the formulation design of tablets prepared by wet granulation. We used the GTP-1 to measure "tableting properties" with different amounts of binder, disintegrant, and lubricant, and compared the results with those of tableting on a commercial rotary tableting machine. tableting failures(capping and binding in particular) occurred when samples that had been evaluated as having poor "Compactability" or"Manufacturability" on the GTP-1 were compressed on the rotary tableting machine. Thus,our evaluation method predicted tableting failure at the commercial scale. The method will prove useful for scaling up production.

关键词： tableting formulation design wet granulation capping binding single-punch tablet press

Prediction of effects of punch shapes on tableting failure by using a multi-functional single-punch tablet press

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Asian Journal of Pharmaceutical Sciences 2017年第5期12卷 412-417页

作者： Takashi Osamura Yoshiko Takeuchi Risako Onodera Masahiro Kitamura Yoshiteru Takahashi Kohei Tahara Hirofumi Takeuchi Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University1-25-4Daigaku-NishiGifu501-1196Japan Pharmaceutical Technology Department Sawai Pharmaceutical Co.Ltd12-34HiroshibachoSuita-ShiOsaka564-0052Japan

We previously determined 'tableting properties' by using a multi-functional single-punch tablet press(GTP-1). We proposed plotting 'Compactability' on the x-axis against'Manufacturability' on the y-axis to allow visual evaluation of 'tableting properties'. Various types of tableting failure occur in commercial drug production and are influenced by the amount of lubricant used and the shape of the punch. We used the GTP-1 to measure'tableting properties' with different amounts of lubricant and compared the results with those of tableting on a commercial rotary tableting machine. Tablets compressed with a small amount of lubricant showed bad 'Manufacturability', leading to sticking of powder on punches.We also tested various punch shapes. The GTP-1 correctly predicted the actual tableting results for all punch shapes. With punches that were more likely to cause tableting failure, our system predicted the effects of lubricant quantity in the tablet formulation and the occurrence of sticking in the rotary tableting machine.

关键词： tableting Formulation design Lubricant Punch shape Single-punch tablet press Losartan potassium

Improved tabledng behavior of paracetamol in the presence of polyvinylpyrrolidone additive: Effect of mixing conditions

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Particuology 2019年第2期17卷 9-18页

作者： Ayuk Agbor Rose Waseem Kaialy School of Pharmacy Faculty of Science and Engineering University of Wolverhampton Wolverhampton WV1 1LY UK

Monoclinic paracetamol (PA) is notorious as a poorly compactible model drug. Polyvinylpyrrolidone (PVP) is a polymer that can act as an effective binder to improve the mechanical properties of PA. It is surprising however that the role of mixing conditions on the physicochemical and mechanical properties of PA-PVP mixtures has not been reported previously. The results of this work showed that PA-PVP mixtures containing 5%(w/w) PVP prepared using high energy mixing conditions had considerably smaller particle size distributions and higher cohesivities than mixtures prepared using low energy mixing conditions. Solid-state analysis did not detect any change in the monoclinic crystalline form of PA after mixing with PVP. The following rank order of tabletability for PA-PVP mixtures was obtained according to the mixing condition: low shear-medium sheartableting.

关键词： Direct compression Interactive mixtures Hydrogen bonding Mechanical properties Physicochemical properties tableting

Assessment and prediction of tablet properties using transmission and backscattering Raman spectroscopy and transmission NIR spectroscopy

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Asian Journal of Pharmaceutical Sciences 2016年第4期11卷 547-558页

作者： Elisabeth Peeters Ana Filipa Tavares da Silva Maunu Toiviainen Jeroen Van Renterghem Jurgen Vercruysse Mikko Juuti Joao Almeida Lopes Thomas De Beer Chris Vervaet Jean-Paul Remon Laboratory of Pharmaceutical Technology Ghent UniversityOttergemsesteenweg 4609000GhentBelgium Laboratory of Pharmaceutical Process Analytical Technology Ghent UniversityOttergemsesteenweg 4609000GhentBelgium REQUIMTE Department of Chemical SciencesUniversity of PortoRua de Jorge Viterbo Ferreira2284050-313PortoPortugal VTT Technical Research Centre of Finland Optical Measurement TechnologiesKaitoväylä190570 OuluFinland

This study investigated whether Raman and Near Infrared(NIR) spectroscopy could predict tablet properties. Granules were produced on a continuous line by varying granulation parameters. tableting process parameters were adjusted to obtain uniform tablet weight and thickness. Spectra were collected offline and tablet properties determined with traditional analyzing methods. Partial Least Squares(PLS) regression was used to correlate spectral information to tablet properties, but predictive models couldn’t be established. Principal component analysis(PCA) was effectively used to distinguish theophylline concentrations and hydration levels and multiple linear regression(MLR) analysis allowed insight on how granulation parameters affect granule and tablet properties.

关键词： Continuous production PAT Granulation tableting NIR Raman

A study on the plasticization of sustained release coatings for their ability to withstand the damaging effects of compaction on coated pellets

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 209-210页

作者： Chan Pui Sheon Sivaram Nallamolu Paul Wan Sia Heng Department of Pharmaceutical Technology International Medical University57000 Malaysia Department of Pharmacy National University of Singapore117543 Singapore

Pharmaceutical solid dosage forms are commonly coated to modify the release of drugs. Due to the disadvantages of coated single-unit dosage forms, such as occurrences of dose dumping and local irritation, coated multi-particulates are preferred.Coated multi-particulates can eventually be filled into capsules or compressed into tablets.

关键词： MUPS tableting Plasticizer(TEC) Pellets