• Journal of Pharmaceutical Investigation
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• v.39 no.5
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• pp.381-386
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• 2009

We previously showed that the water extracts of rice wine-baked Scutellaria baicalensis Georgi (RWBS) ameliorated colonic inflammation more than crude Scutellaria baicalensis (CS) after oral administration. The aim of this study is to compare the effect of rectal and oral administration of RWBS in the experimental colitis. Experimental colitis was induced in mice by daily treatment with 5% dextran sulfate sodium (DSS) in the drinking water for 7 days. Water was used as vehicle of oral administration, while Carbopol/PEG mucoadhesive gel was used as vehicle of rectal administration. RWBS and RWBS gel (RWBSG) were administered once per day for 7 days. RWBS and RWBSG significantly attenuated the disease activity index (DAI) calculated as the sum of scores of body weight loss, stool consistency and rectal bleeding. Furthermore, RWBS and RWBSG reduced the mucosal myeloperoxidase activity and COX-2 (cyclooxygenase-2) expression in colon tissue. Anti-inflammatory effect of CS on colonic inflammation was increased by baking with rice wine in both oral and rectal administration. Moreover, anti-inflammatory effects of oral administration on colonic inflammation was greater than those of rectal administration. Further study would be required for the development of intra-rectal formulation.

• Journal of Pharmaceutical Investigation
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• v.16 no.4
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• pp.148-151
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• 1986

This paper was designed to investigate the influence of different suppository bases on both the rectal absorption and dissolution rate of lithium carbonate, and to compare bioavailability from rectal administration with that from oral administration. The dissolution rates were in such order as PEG 4000, surfactant A (Witepsol 15+sodium lauryl sulfate), surfactant B (Witepsol 15+cholic acid), Witepsol 15 and cacao butter. Among various suppository bases, the blood level of lithium carbonate after rectal administration was increased in the following order: surfactant A>surfactant B>PEG 4000>Witepsol 15>cacao butter. When it comes to compare oral with rectal administration in AUC values, surfactants and PEG 4000 showed similar blood levels to oral administration, but lipophilic bases such as Witepsol 15 and cacao butter showed far lower blood level than oral administration. Peak time in oral administration was 2 hrs, but those in rectal administration using various suppository bases were $6{\sim}8$ hrs.

• Journal of Pharmaceutical Investigation
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• v.24 no.3
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• pp.115-129
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• 1994

In the present study, quantitative and qualitative histology was used to assess the effects of ibuprofen suppositories with various treatments on the rectal mucosa of rats. Two suppositories were prepared with Witepsol W35 and compared with two commercial ibuprofen suppositories Reference I (Showa Pharm.ind., Tokyo, Japan), Reference II (P.Pharm., Seoul, Korea). Single and multiple dose(dosing interval 4 hr, n=4) studies were conducted. All suppositories significantly increased epithelial cell loss, but the extent of rectal irritation was variable. These studies showed that the incorporation of ibuprofen into the suppository bases increases the morphological change in rectal tissue both for the single and multiple administrations of suppositories, but which was significantly recovered within 24 hr although the interanimal variability in scores was very substantial. Multiple administration of ibuprofen suppositories caused significant damage to rectal mucosa, but it must be considered that these were under the severe condition, that is, interval of administration (4 hr) was three times shorter than normal interval of administration and dose was fifteen times larger than usual human dose. Aluminum oxide $(Al_2O_3)$, a dispersing agent, slightly increased the irritation of rectal mucosa in rats at 5 hr and 24 hr after multiple administration, but it was possible to ignore the difference of irritation in the data at 5hr and 24hr after single administration. Finally, it was concluded that Witepsol W35 and ibuprofen had a slight rectal mucosa-irritating effect on the usual human dose, and ibuprofen suppositories prepared with Witepsol W35 or Witepsol W35, $Al_2O_3$ showed almost similar extent of rectal irritation with commercial ibuprofen products.

• YAKHAK HOEJI
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• v.31 no.5
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• pp.286-295
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• 1987

The relationship between in vitro release and in vivo bioavailability of acetaminophen from suppositories was investigated. Effect of glycyrrhizin on the drug release and rectal absorption in rats was also examined. Suppositories containing 25mg of acetaminophen were prepared with Wecobee FS (fatty base) or PEG (water-soluble base) bases. The release from the suppositories were determined with USP rotating basket dissolution apparatus and with the suppository release tester. The temperature of the dissolution medium was very critical for the dissolution of acetaminophen from Wecobee FS suppositories. The bioavailability of acetaminophen was calculated from the plasma concentration-time curve after rectal administration of the suppositories to the rats. There were no significant differences in AUC following rectal administration of Wecobee FS and PEG suppositories, but the release and absorption from the Wecobee FS suppositories were faster than those from PEG suppositories. The dissolution rate obtained by the suppository release tester was better correlated with in vivo absorption rate constant than that by the USP dissolution apparatus. It suggests that the partitioning between rectal fluid and suppository base is the rate-limiting step in the rectal absorption of acetaminophen from suppositories. Glycyrrhizin was found not to affect in vitro dissolution and rectal absorption of acetaminophen.

• Journal of Pharmaceutical Investigation
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• v.27 no.3
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• pp.189-198
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• 1997

The purpose of the present study was to investigate the effect of medium chain fatty acid salts, reported as enhancers in insulin nasal absorption, on the rectal absorption of insulin in rats. The serum glucose and remained insulin level in perfusate were measured after rectal recirculation of insulin with or without sod. laurate, sod. caprate and sod. caprylate in situ. The addition of sod. laurate or sod. caprate reduced serum glucose concentration considerably. Sod. caprate (1.0%) showed the greatest promoting effect on the decrement of serum glucose. Eudispert hv hydrogels containing insulin with medium chain fatty acid salts were, thereby, prepared and evaluated. The release rate of insulin from Eudispert hv hydrogels was reduced with an increase in the content of Eudispert hv, and was raised with increasing NaOH concentration. Ten percent Eudispert hv hydrogels were offered for the rectal administration of insulin. The addition of 1.0% sod. caprate reduced serum glucose concentration remarkably after rectal administration of 10% Eudispert hv hydrogels containing insulin. The level of glucose decrement was greater by 30% compared to subcutaneous administration of insulin solution. From the above findings, Eudispert hv hydrogels would be used as useful rectal delivery systems of insulin.

• Journal of Pharmaceutical Investigation
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• v.12 no.3
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• pp.88-92
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• 1982

Insulin administration rectally with the liposome has the hypoglycemic effect in the rabbits. The reducton in blood sugar was maximum at about 60 minutes after administration and continued for 4 hrs. at low level in these experiments. No hypoglycemic effect was observed in control administrated rectally without liposome. Rectal absorption of insulin has been effected by addition of the bile salt, as the protective agent which prevented denaturation and the phastransition of insulin in liposome-encapsulation. As a matter of the fact, a significant hypoglycemic action was obtained when the insulin-liposome was given by rectal administration. The use of this agent to enhance insulin absorption offers the possibility of a new approach to rectal insulin therapy.

• The Journal of Korean Obstetrics and Gynecology
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• v.21 no.3
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• pp.1-17
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• 2008

Purpose: Scutellaria baicalensis is a herb which has effect of eliminating heat, drying dampness, purging away fire, detoxicating. Clinically, has been used to remove fever and control of inflammation. We have studied in series to investigate the effective traditional oriental medicines of treatment for endometriosis. In this study, the effects of Scutellaria baicalensis administrated orally or rectally on surgically induced endometriosis in rat were investigated. Methods: The endometrial tissues of rats were autografted to their small intestine. Rats with surgically induced endometriosis were administered with Scutellaria baicalensis extracts for 40 days orally or rectally. We observed the tissue size of ectopic uterine implants at the mesenteric with the naked eye and examined the concentration of estradiol, progesterone, $TNF-{\alpha}$ and IL-2, IL-4, IL-6 and IL-10 in serum. Also, we inquired which was more effective between oral administration groups and rectal administration groups. Results: The size of ectopic uterine implants of orally or rectally treated groups was much smaller than those of control groups. The concentrations of estradiol, progesterone, $TNF-{\alpha}$, IL-2 and IL-6 were significantly decreased in oral administration experimental group compared with the control group. The concentrations of progesteron, $TNF-{\alpha}$, IL-2 and IL-6 were significantly decreased in rectal administration experimental group compared with the control group. The efficiency of oral administration group was better than that of rectal administration group at the serum concentration of estradiol and IL-4. Conclusion: Our data suggest that Scutellaria baicalensis inhibit the inflammation induced from ectopic uterine implants at the mesenteric wall and inhibit the growth of ectopic uterine implants. Judging from the above results, it can be suggested that Scutellaria. baicalensis should be a useful agent for inhibiting the inflammation induced from ectopic uterine implants and the proliferation of endometriosis. Maybe, oral administration of Scutellaria baicalensis is more effective than rectal administration.

• The Korean Journal of Pharmacology
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• v.10 no.1 s.15
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• pp.61-65
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• 1974

Berberis koreana Palibin belonging to Berberidaceae family, a common herb in Korea, has been contained some quantity of Berberine analogue and other ingredients. Authors therefore paid attention to its pharmacological actions and examined the effects on sleep duration and rectal temperature in mouse with crystal (A) from Berberis koreana Palibin in Korean native plans. The experiment searching for the effect on sleep duration was performed with pretreatment of Berberis Koreana Palibin crystal (A) 30 min before the administration of 25 % ethanol, and its crystal were also administered intraperitoneally with the intention to examine the effect on rectal temperature in mouse. The results of the experiment were as follows; 1. Crystal (A) from Berberis koreana Palibin was made by extraction with ethanol and HCI. 2. Crystal (A) enhanced the hypnotic activity of alcohol in concentratins of 0.1 mg/10g or 0.15 mg/10g. 3. Rectal temperatures in mice were significantly reduced with administration of crystal (A) in concentrations of 0.1 mg/10g or 0.15 mg/10g. 4. The maximal reduction of rectal temperature and potentiation of the hypnotic activity were observed at 30 min after its administration. From the above results, it is clear that crystal (A) from Berberis koreana Palibin exerts the potentiation of hypnotic action of alcohol and reduction of rectal temperature in normal mouse. Its pharmacological effects are probably derived from the action upon the central nervous system.

• The Journal of Korean Obstetrics and Gynecology
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• v.20 no.2
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• pp.43-59
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• 2007

Purpose : Astragalus membranaceus is a herb which has effectiveness of energy increase, protection against pathogenic and organ immune response control. Endometriosis has been thought to be related with immune response in uterus. Therefore in this study, the effects of Astragalus membranaceus on endometriosis were investigated. Methods : The endometrial tissue was autografted to rat's small intestine. Rats with surgically induced endometriosis was administerd with Astragalus membranaceus extracts for 40 days orally or rectally. We observed the size of ectopic uterine implants at the mesenteric with the naked eye and examined the concentrations of estradiol, progesterone, $TNF-{\alpha}$ and IL-2, IL-4, IL-6 and IL-10 in serum. Also, we inquired out the efficiency between oral and rectal administration groups. Results : The size of ectopic uterine implants of oral and rectal treated groups were much smaller than those of control groups. The concentration of estradiol, progesterone. $TNF-{\alpha}$ and IL-2 were significantly decreased in oral administration experimental group compared with the control group. The concentration of progesterone were significantly decreased in rectal administration experimental group compared with the control group. The efficiency of oral administration group was better than that of rectal administration group in the serum concentration of estradiol, $TNF-{\alpha}$ and IL-2. Conclusion : Our data suggest that Astragalus membranaceus reduce the size of ectopic uterine implants at the mesenteric wall and inhibit the growth of ectopic uterine implants. Judging from the above results, it can be suggested that Astragalus membranaceus should be a useful agent for inhibiting the proliferation of uterine endometrial tissue. May be, oral administration of Astragalus membranaceus is more effective than rectal administration for inhibiting the proliferation of endometriosis.

• YAKHAK HOEJI
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• v.37 no.5
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• pp.427-436
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• 1993

The pharmacokinetics and relationship between in vitro dissolution and in vivo fraction absorbed were investigated after intravenous(iv) injection of omeprazole(OMZ), oral administration of OMZ capsules and rectal administration of 8 types of suppositories. The plasma concentration of OMZ (C$_{p}$)-time (t) curve after iv. administration fitted a two-compartment open model and the equation which best fitted the pharmacokinetics of OMZ was $C_{p}$ = 13.936 $e^{-8.78t}$+2.973 $e^{-0.716t}$. The bioavailabilities of OMZ in Witepsol H15 base (Supp-2) and PEG 4000 base (Supp-6) suppositories were 40.7% and 33.4%, respectively, which are higher(p<0.001) than 13% of oral administration of capsule. The avoidance fractions of the first-pass metabolism for Supp-2 and Supp-6 suppositiories were 31.8% and 23.4%, respectively, suggesting that the rectal application of OMZ may be a more adequate route of administration than oral one.