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The solid-solid transition of phenylbutazone polymorphs by heating was investigated by differential scanning calorimetry (DSC) and X-ray diffractometry, and also the difference in dissolution rate due to the polymorphism was confirmed. There were observed three polymorphs of phenylbutazone. Form I melted at 103°, Form II twice at 93° and at 103°, and Form III at 93°. Furthermore, the mutual transition phenomenon by heating among these three polymorphs was observed by DSC. Analyzing the dissolution curves of Forms I and II obtained by the stationary disk method and poltting the saturated concentration of the respective forms, the transition temperature estimated was 98° and the heat of transition 210 cal/mole. Form III was transformed to Form II through compression above a certain compressional pressure and to the intermediate form of Form II and Form III (designated here as "pseudo-Form III") under the compressional pressure 1 ton/cm2. Therefore, the intrinsic dissolution rate of Form III was not obtained. However, the dissolution rate of "pseudo-Form III" was faster than any of Form I and II. Accordingly, it was suggested that if the transition of Form III could be suppressed, more soluble preparations of phenylbutazone would be available.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 24 (6), 1169-1172, 1976
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204164230016
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- NII論文ID
- 110003635114
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DyaE28XkvVeitLc%3D
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- ISSN
- 13475223
- 00092363
- http://id.crossref.org/issn/00092363
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- PubMed
- 1021282
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可