2 0 0 0 OA 医薬品開発における物性評価の重要性
- 著者
- 芦澤 一英
- 出版者
- 公益社団法人 日本薬理学会
- 雑誌
- 日本薬理学雑誌 (ISSN:00155691)
- 巻号頁・発行日
- vol.127, no.3, pp.213-216, 2006 (Released:2006-05-01)
- 参考文献数
- 12
- 被引用文献数
- 5 7
近年,製薬企業は効率的な新薬開発実施のために製品開発のスピード化が強く要請されている.一方,開発候補化合物の約4割が生物薬剤学的性質に基づく理由で開発段階においてドロップアウトし,開発コストを押し上げ創薬難度を高める原因になっている.そのため,創薬のスピードアップには,探索段階における莫大な数の試験サンプルの合成や評価を実施する際に,経口吸収性に関わる溶解度や脂溶性などの物性評価も,同時に短時間で実施することが重要である.また,開発候補化合物は,最終的な原薬と製剤の品質保持を考慮し,原薬開発基本形である塩形および結晶形を選定する必要がある.新しい化合物を医薬品として世に送り出すためには,開発の早い段階であらゆる化合物特性をよく調べておくことが重要であり,本稿は「創薬段階における物性評価の重要性」についてまとめた.
1 0 0 0 OA 研究人生を振り返って思うこと
- 著者
- 芦澤 一英
- 出版者
- 公益社団法人 日本薬学会
- 雑誌
- MEDCHEM NEWS (ISSN:24328618)
- 巻号頁・発行日
- vol.18, no.4, pp.20-23, 2008-11-01 (Released:2020-12-22)
- 参考文献数
- 3
1 0 0 0 OA 新規抗生物質E1040の固体安定性と製剤化研究について
- 著者
- 芦澤 一英 内川 清彦 服部 禎一 石橋 泰雄 三宅 康夫 里 忠
- 出版者
- 公益社団法人 日本薬学会
- 雑誌
- YAKUGAKU ZASSHI (ISSN:00316903)
- 巻号頁・発行日
- vol.110, no.3, pp.191-201, 1990-03-25 (Released:2008-05-30)
- 参考文献数
- 45
- 被引用文献数
- 1 2
In designing the dosage form, one major factor controling their physicochemical properties is solid forms of the drug powder. The method for improving the physicochemical stability of unstable β-lactam antibiotics is very important. E1040 is a novel parenteral 3-betaine type cephalosporin which has a broad antibacterial spectrum and potent activities against Citrobacter, freundii, Enterobacter cloacase, and glucose-nonfermentative bacteria, including P. aeruginosa. The present study was intended to provide the solid-state chemical stability of perenteral steril dry dosage form of E1040. The chemical stability differences among the various solid forms, dry amorphous, additive freeze dried amorphous solid and crystalline powder, were evaluated as a function of temperature by thermo stress tests. Freeze dried anhydrous amorphous form was the first steril dry dosage form investigated during the preformulation study. However, this compound is chemically unstable, in the titer of them, reduction are observed in the freeze dried amorphous solid. In order to select the most suitable solid form of E1040, two methods were used. One was crystalline solid and the other was NaCl additive freezedried formulation. Through our experiments, the solid-state chemical stabilization can be achieved by these two methods (effect of crystal structure and effect of NaCl additive).
1 0 0 0 OA 医薬品の多形現象と晶析の科学(結晶多形シンポジウムI)
- 著者
- 芦澤 一英
- 出版者
- 日本結晶成長学会
- 雑誌
- 日本結晶成長学会誌 (ISSN:03856275)
- 巻号頁・発行日
- vol.30, no.3, pp.21-22, 2003-07-05 (Released:2017-05-31)
- 参考文献数
- 2
In the pharmaceutical drug development, the following are carried out : Polymorphic search and physical properties evaluation for choosing the polymorphism it chooses optimum crystal form of the drug substance. In next stage, the research of the scale-up for manufacturing process and formulation of the drug substance is carried out. In this paper, the case of the research on polymorphism and evaluation in pharmaceutical drug development is introduced.
1 0 0 0 OA X線回折と光音響赤外スペクトル測定法によるE1040結晶の結晶化度の評価について
- 著者
- 芦澤 一英 内川 清彦 服部 禎一 石橋 泰雄 三宅 康夫 里 忠
- 出版者
- 公益社団法人 日本薬学会
- 雑誌
- YAKUGAKU ZASSHI (ISSN:00316903)
- 巻号頁・発行日
- vol.110, no.3, pp.202-209, 1990-03-25 (Released:2008-05-30)
- 参考文献数
- 34
An X-ray diffraction methods and Fourier transform infrared analysis with photoacoustic detector (FTIR-PAS) for estimation of the degree of crystallinity of crystalline E1040 formulation was established. The X-ray procedure to determine the crystallinity of E1040 was based upon the measurement of the total scattering and the scattering from the crystalline region of the drug. The FTIR-PAS procedures are based upon the measurement of the peak height ratio at 1628 cm-1 and measurement of the spectral region between 2400 and 3700 cm-1 by the Partial least squares (PLS) techniques. The data of the degree of crystallinity from the X-ray diffraction methods are consistent with the data from FTIR-PAS methods. The increase of the degree of crystallinity of the drug formulation decreased the decomposition rate of E1040. As a result, it had become apparent that two analytical procedures were actually valid. This assured optimizing process conditions which affect the improvement of crystallinity.