STUDIES ON SUSTAINED-RELEASE SUPPOSITORIES .3. RECTAL ABSORPTION OF MORPHINE IN RABBITS AND PROLONGATION OF ITS ABSORPTION BY ALGINIC ACID ADDITION

被引:13
作者
KAWASHIMA, S
INOUE, Y
SHIMENO, T
FUJIWARA, H
机构
[1] GREEN PHARM, NONOICHI 921, JAPAN
[2] PUBL ISHIKAWA CHUO HOSP, MATTOH 924, JAPAN
关键词
alginic acid; bioavailability; high performance liquid chromatography; macrogol; morphine; prolonged absorption; rectal administration; suppository; sustained release; Witepsol;
D O I
10.1248/cpb.38.498
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Rectal absorption of morphine from various kinds of suppository bases was investigated. The extent of bioavailability of morphine by rectal administration varied with the bases used (30.5—97.5%), but every value was higher than that in the case of oral administration (13.5%). Witepsol bases were preferable to macrogol base for the rectal absorption of morphine. In particular, Witepsol S-55 or W-35 gave a higher plasma peak level than H-15 or E-75, whereas the difference in the mean residence times obtained from these bases could not be regarded as significant. Sustained-release suppositories of morphine could be prepared simply by mixing alginic acid (Alg) with morphine in a suppository base. Further, prolonged rectal absorption could be obtained by using these sustained-release suppositories, and the absorption rate was controlled by the amount of Alg added. It seems likely that the sustained release was due to the binding of morphine to Alg from the results of partition coefficient and binding ratio measurements in aqueous solution. The rapid initial absorption and the subsequent prolonged absorption of morphine simultaneously obtained from the morphine–Alg suppository may be useful in the clinical context. © 1990, The Pharmaceutical Society of Japan. All rights reserved.
引用
收藏
页码:498 / 505
页数:8
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[1]   INFLUENCE OF PH ON THE BUCCAL ABSORPTION OF MORPHINE-SULFATE AND ITS MAJOR METABOLITE, MORPHINE-3-GLUCURONIDE [J].
ALSAYEDOMAR, O ;
JOHNSTON, A ;
TURNER, P .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1987, 39 (11) :934-935
[2]  
BEHAR M, 1979, LANCET, V1, P527
[3]  
CHRUBASK J, 1985, ANESTHESIOLOGY, V62, P363
[4]  
ELLIOTT HW, 1954, P SOC EXP BIOL MED, V85, P77
[5]  
ELLISON NM, 1984, CLIN PHARMACY, V3, P614
[6]   A MATHEMATICAL-MODEL FOR DRUG RELEASE FROM O/W EMULSIONS - APPLICATION TO CONTROLLED RELEASE MORPHINE EMULSIONS [J].
FRIEDMAN, D ;
BENITA, S .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1987, 13 (9-11) :2067-2085
[7]  
FUJIMOTO JM, 1957, J PHARMACOL EXP THER, V121, P340
[8]  
GOODMAN LS, 1965, PHARMACOL BASIS, P258
[9]   STABILITY OF MORPHINE SOLUTIONS IN PLASTIC SYRINGES DETERMINED BY REVERSED-PHASE ION-PAIR LIQUID-CHROMATOGRAPHY [J].
HUNG, CT ;
YOUNG, M ;
GUPTA, PK .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1988, 77 (08) :719-723
[10]   INTERSPECIES DIFFERENCE IN DRUG PROTEIN BINDING-TEMPERATURE AND PROTEIN-CONCENTRATION DEPENDENCY - EFFECT ON CALCULATION OF EFFECTIVE PROTEIN-FRACTION [J].
IGARI, Y ;
SUGIYAMA, Y ;
AWAZU, S ;
HANANO, M .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1981, 70 (09) :1049-1053