Preparation of Bupleurum Nasal Spray and Evaluation on Its Safety and Efficacy
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- Xie Yueling
- Department of Pharmaceutics, School of Pharmacy, Fudan University
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- Lu Wei
- Department of Pharmaceutics, School of Pharmacy, Fudan University
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- Cao Shilei
- Department of Pharmaceutics, School of Pharmacy, Fudan University
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- Jiang Xinguo
- Department of Pharmaceutics, School of Pharmacy, Fudan University
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- Yin Ming
- Department of Pharmacology, School of Pharmacy, Shanghai Jiaotong University
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- Tang Wenlu
- Department of Pharmacology, School of Pharmacy, Shanghai Jiaotong University
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抄録
Radix Bupleuri is widely used in traditional medicine for the treatment of fever, pain, and inflammation associated with influenza or the common cold. The essential oil extracted from the herb is generally claimed to play the major role in the efficacious treatment of fever. The purpose of the present study was to formulate an intranasal delivery system for the essential oil in an aqueous solution used in the form of nasal spray. From 450 g Radix Bupleuri was extracted the essential oil in the amount of about 0.2 ml, which was slightly water-soluble and viscous with low-fluidity. In order to dissolve the essential oil evenly in the aqueous solution, tween-80 (TW-80, used in 10% (w/v) solution), propylene glycol (PG) and diethylene glycol monoethyl ether (TC) were selected as the favorable solubilizing agents, whose amount was respectively determined by L16(45) orthogonal design. An aqueous solution with clarity and no ciliotoxicity was prepared when TW-80 8% (v/v), PG 14.4% (v/v) and TC 14.4% (v/v) were added. Employed to evaluate the acute toxicity, the rats grew well and were kept active and healthy within 14 d after an intranasal administration of this preparation at the dose of oil from 10 g Bupleuri/kg (50-fold higher than the clinical dose), indicating that there would be no serious toxicity at the normal dose. Intranasal administration of this preparation to 2 kg rabbits with fever induced by subcutaneous injection of turpentine decreased body temperature markedly (0.5, 0.8 and 1.0 °C respectively at the dose of oil from 1, 2 and 4 g Bupleuri/body). In addition, the administration significantly reduced fever in 200 g rats induced by intramuscular injection of colicine suspension (0.6 °C at the dose of oil from 0.8 g Bupleuri/body). The results suggest that the formulation of nasal spray for the essential oil from Radix Bupleuri can be potentially effective in the treatment of fever.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 54 (1), 48-53, 2006
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
- 1390282679145162880
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- NII論文ID
- 110004820322
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 7756610
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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
- NDL
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- 使用不可