Application of Polyglycolized Glycerides in Protection of Amorphous Form of Etoricoxib during Compression
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概要
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Polymorphic transition and stability problems during amorphous drug formulation are the major limiting factors in pharmaceutical technology. The purpose of the study was to evaluate the ability of polyglycolized glycerides (Gelucire) in protection of amorphous form of drug during compression and shelf life with lower proportion. Amorphous etoricoxib (AET) was prepared by spray drying technique. Tablets of AET and melt granules of AET (MG-AET) with Gelucire 50/13 were prepared. Tablets parameters like hardness, disintegration and content uniformity were evaluated. Tablets were evaluated immediately after compression and on storage for 3 months at ambient conditions to determine degree of transformation using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and dissolution profiles. Spray drying yielded the amorphous etoricoxib. Content uniformity in the tablet was in between 95 to 105%. Other parameters like disintegration and hardness were well within the limits. The results showed significant difference in the degree of crystallinity between AET tablet and MG-AET tablet. MG-AET tablet showed absence of crystallinity after 3 months storage. The reason could be formation of hydrogen bonding between the Gelucire and AET. Also Gelucire can be tableted very easily under low pressure and showed elastic recovery. Gelucire yielded a soft embedding during tableting, which prevented the polymorphic transformation. Polyglycolized glycerides (Gelucire 50/13) are able to protect amorphous etoricoxib during compression. As excipient required is low, it became possible to prepare tablet formulation as compared to other excipient like polyvinylpyrrolidon (PVP).
- 2007-10-01
著者
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Mahadik Kakasaheb
Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy
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TAKADA Kanji
Department of Pharmacokinetics, Kyoto Pharmaceutical University
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Paradkar Anant
Department Of Pharmaceutics Bharati Vidyapeeth University Poona College Of Pharmacy
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Shimpi Shamkant
Department Of Pharmaceutics Bharati Vidyapeeth University Poona College Of Pharmacy
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Takada Kanji
Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories
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Mahadik Kakasaheb
Department Of Pharmaceutics Bharati Vidyapeeth University Poona College Of Pharmacy
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