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Anti-diarrheal effects of wood creosote pill preparation compounded with four crude drugs on castor oil-induced diarrhea in rats and the role of crude drugs in the expression of the efficacy

By Baba Tatsuya, Nishino Takao and Tani Tadato


Wood creosote pill preparation, in which 4 crude drug powders, Gambir, Phellodendri Cortex, Glycyrrhizae Radix, and Citri Unshiu Pericarpium are compounded, has been used for diarrhea. In the present study, the significance of the compounding of these crude drug powders was examined in castor oil-induced diarrhea model in rats. Oral administration of small wood creosote pill (P4Rx5) exerted anti-diarrheal action for up to 3 hours and intestinal peristaltic motility-suppressive action, which was assessed by charcoal meal test. These suppressive actions were not noted in the groups of the rats receiving wood creosote alone at a dose level (11mg/kg) that is contained in P4Rx5. From these findings, it was revealed that crude drugs compounded were responsible for the anti-diarrheal and intestinal peristaltic motility-suppressive actions of P4Rx5. Pharmacological actions were examined for variant pills (without one of the crude drug powders), revealing that Citri Unshiu Pericarpium was responsible for retention of the anti-diarrheal effects and the suppression of castor oilinduced intestinal peristaltic motility by P4Rx5. Furthermore, it was found that the compounded crude drug powders increased the AUC of guaiacol (a major anti-diarrheal component of wood creosote), being involved in the intestinal peristaltic motility-suppressive action of P4Rx5. The results obtained in the present study may provide evidence supporting the usefulness of the compounding of the crude drugs in traditional wood creosote pills such as "Seiro-gan", and give a rationale for development of new preparations compounding wood creosote with crude drug powders. 4種類の生薬末(阿仙薬, 黄柏, 甘草, 陳皮)を配合したwood creosote丸剤は下痢の治療薬として古くから用いられている。この報告ではこれら生薬末の配合意義をcastor oil処理したラットを用いて検討した。ラットに経口投与できる大きさに調製したwood creosote丸剤(P4Rx5)は投与3時間後まで有意な止瀉作用を示し腸蠕動運動も抑制した。この止瀉作用と腸蠕動運動抑制作用は, P4Rx5と同量のwood creosote (11mg/kg)を単独で投与した群では認められなかった。これらのことからP4Rx5に配合されている4生薬末がこれらの抑制作用に関与していることが明らかになった。次にP4Rx5から1生薬末を抜いた丸剤で同様の検討を行った結果, 陳皮末(CUP2)が元のP4Rx5の止瀉作用の持続性を高め, さらに腸蠕動運動の抑制に寄与していることが明らかになった。さらに配合された生薬末はguaiacol (wood creosoteの主要な止瀉成分)のAUCを増加させ, P4Rx5の腸蠕動運動の抑制作用に寄与していることが明らかになった。今回の結果は4種類の生薬末を配合したwood creosote丸剤(伝統薬: 正露丸)における配合生薬の意味を解析し有用性を支持する証拠となる。このような評価方法はwood creosote丸製剤の配合生薬を改変する指標となる

Topics: Wood creosote, guaiacol, castor oil-induced diarrhea, intestinal peristaltic motility, Citrus unshiu
Publisher: 和漢医薬学会
Year: 2005
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