中空坐剤の病院薬局製剤への応用 ＩＩ． 塩酸モルヒネ坐剤

Abstract

The evaluation of morphine hydrochloride (MOR) hollow type suppository was carried out by a comparison between rectal and intravenous administrations of MOR in rabbits.The hollow type suppository containing three doses of MOR (1mg/kg, 3mg/kg, 10mg/kg) was used for the rectal administration, and the aqueous solution of MOR (20mg/ml) was used for the intravenous administration (3mg/kg).The serum concentration of MOR was measured with gas chromatography-mass spectrometer by selected ion monitoring method.The absorption constant of MOR from suppository had dose-dependent characteristics, although the peak serum concentrations (1mg/kg;38.8ng/ml, 3mg/kg;61.9ng/ml, 10mg/kg;137.1ng/ml) were reached within 0.4 hours, respectively The area under the curve of serum concentration (AUC) after rectal administration were compaired with the AUC after intravenous administration.The bioavailability (AUCrectl/AUCiv×Doseiv/Doserectal×100) were 90%(1mg/kg), 62%(3mg/kg) and 53%(10mg/kg), respectively.These data suggested that the absorption of MOR had dose-dependency. We used hollow type supporitory of MOR for the pain control of patients with cancer for 6 years.It was required to administer every 4-6 hours for pain control.Thus, it was concluded that MOR hollow type suppository could be useful for the pain control of patients with cancer, especially for the patients who were not able to ingest the oral preparations and the patients who need individual dosage adjustment.