Preparation and Characterization of Polylactic Acid Microspheres Containing Water-Soluble Anesthetics with Small Molecular Weight
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概要
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Polylactic acid (PLA) microspheres containing water-soluble anesthetics (phenobarbital sodium, pentobarbital sodium, procaine hydrochloride, lidocaine hydrochloride, or dibucaine hydrochloride) with low molecular weight were prepared using a water-in-oil-in-water (w/o/w) emulsion solvent evaporation method, and the optimization of preparative conditions was performed. In the microencapsulation of sodium salt anesthetics (phenobarbital sodium, pentobarbital sodium) into PLA matrix, the addition of NaCl (10% (w/v)) into the external aqueous phase and the choice of comparatively high concentration of PLA (16% (w/v)) in CH_2Cl_2 significantly improved drug loading efficiency compared to the case when no additives were added to the external aqueous phase, or low PLA concentration (4% (w/v)) in CH_2Cl_2 was employed in the manufacturing process. The loading efficiency of hydrochloride salt anesthetics (procaine hydrochloride, lidocaine hydrochloride, or dibucaine hydrochloride) in PLA microspheres, in constract, was dramatically improved using the alkalic buffer solution as the external aqueous phase. The mean volume diameter was obtained in the region of 20-30 μm and normal distribution for prepared microspheres in all cases. PLA microspheres containing 10% (theoretical) of various anesthetics exhibited so-called burst releases, but, some portion of the loaded anesthetics still remained in the microspheres at 7 d.
- 公益社団法人日本薬学会の論文
- 1997-03-15
著者
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Nakajima Yukiko
Department Of Pharmacy The University Of Tokyo Hospital Faculty Of Medicine The University Of Tokyo
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MATSUYAMA KENJI
Faculty of Pharmaceutical Sciences, Kyushu University
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Matsuyama Kenji
Faculty Of Pharmaceutical Sciences Kyushu University
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Matsuyama Kenji
School Of Pharmaceutical Sciences Mukogawa Women's University
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Matsuyama Kenji
Department Of Clinical Pharmacy Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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NAGAREYA Noriko
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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Nishikata Mayumi
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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UCHIDA Takahiro
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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Nakai Aki
School Of Pharmaceutical Sciences Mukogawa Women's University
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Nishikata M
School Of Pharmaceutical Sciences Mukogawa Women's University
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Uchida Takahiro
Faculty Of Pharmaceutical Sciences Kyushu University
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Nakada Y
Nippon Organon K. K. Osaka Jpn
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Konishi Yuriko
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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Yoshida K
Unit Of Chemistry Faculty Of Engineering And High Technology Research Center Kansai University
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YOSHIDA Kazushi
Teikoku Zouki Pharmaceutics
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NAKADA Yoichi
Toray Industries Inc.,
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NAKAI Aki
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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Nagareya N
Mukogawa Women's Univ. Nishinomiya City Jpn
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Nagareya Noriko
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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