• Journal of Pharmaceutical Investigation
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• 제23권3호
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• pp.127-132
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• 1993

The effect of omeprazole (OPZ) suppository on rat rectal mucosa was investigated microscopically. The suppository was prepared with Witepsol H15 base by molding method. Rectal irritation was evaluated according to defined pathological features. The suppository produced a slight damage to the rectal mucosa at 1 hr after the interectal administration, which was almost completely recovered within 24 hr. The damage was not due to OPZ but due to suppository base, Witepsol H15, itself, since Witepsol H15 suppository without OPZ produced the same damage. Therefore, it was concluded that OPZ itself has no rectal mucosa-irritating effect and thus can be developed as a suppository dosage form without any further toxicity problems.

• Journal of Pharmaceutical Investigation
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• 제24권3호
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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.

• 약학회지
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• 제43권2호
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• pp.150-159
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• 1999

Hollow type suppositories inserted polyvinyl alcohol (PVA) hydrogel capsule containing propranolol·HCI (PPH) were prepared using different bases, polyethylene glycol (PEG), Witepsol H-15 (WH-15) and Witepsol W-35 (WW-35) to improve the controlled release of PPH. The release of PPH from the hollow type suppository inserted PVA hydrogel capsule was retarded than that from PEG, WH-15, or WW-35 hollow type suppositories in rat rectal cavity. When the suppositories were administered to rats, the controlled release of PPH was proved by the plasma concentration-time-profiles of PPH. No significant difference (p〈0.05) among the three different hollow type suppositories was observed in terms of AUC and MRT of PPH. WH-15 hollow type suppository inserted 12% of PVA hydrogel capsule caused irritation to rat rectal mucosa. However, the WH-15 hollow type suppository inserted PVA hydrogel capsule caused no severe irritation on rectal mucosa. The application of the hollow type suppositories using PVA in sustained rectal delivery of drugs might be feasible.

• 한국동물위생학회지
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• 제24권4호
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• pp.375-377
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• 2001

Rectal stricture occurred in 2 finishing pigs submitted for necropsy from Moguchon, the meat processing plant, chonbuk. Grossly, the wall of the rectum was harden and thickened by fibrous tissue. Anteriro to the stricture, the descending colon was dilated up to 30cm in diameter, filled with gas and pasty green fluidal feces. Histologically, the epithelia of rectal mucosa were necrotized. The mucosa and submucosa of rectum were infiltrated by macrophages, eosinophils and lymphocytes. This infiltration was the most extensive in the deeper layer of submucosa and intensive fibrosis was observed in deeper submucosa layer. This case is report for rectal stricture of finishing pig.

• Journal of Yeungnam Medical Science
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• 제27권2호
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• pp.150-154
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• 2010

The gastrointestinal tract(GI) is the most frequently involved site of mucosa associated lymphoid tissue(MALT) lymphoma. Stomach is the most common site of involvement among the GI tract. In some case of MALT lymphoma, it is detected in colon. Almost all diagnosis is established by pathological examination of the surgical or endoscopic specimens. We reported a case of rectal MALT lymphoma by colonoscopic polypectomy.

• Radiation Oncology Journal
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• 제31권2호
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• pp.81-87
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• 2013

Purpose: To describe chronic rectal mucosal damage after pelvic radiotherapy (RT) for cervical cancer and correlate these findings with clinical symptoms and radiation dose. Materials and Methods: Thirty-two patients who underwent pelvic RT were diagnosed with radiation-induced proctitis based on endoscopy findings. The median follow-up period was 35 months after external beam radiotherapy (EBRT) and intracavitary radiotherapy (ICR). The Vienna Rectoscopy Score (VRS) was used to describe the endoscopic findings and compared to the European Organization for Research and Treatment of Cancer (EORTC)/Radiation Therapy Oncology Group (RTOG) morbidity score and the dosimetric parameters of RT (the ratio of rectal dose calculated at the rectal point [RP] to the prescribed dose, biologically effective dose [BED] at the RP in the ICR and EBRT plans, ${\alpha}/{\beta}$ = 3). Results: Rectal symptoms were noted in 28 patients (rectal bleeding in 21 patients, bowel habit changes in 6, mucosal stools in 1), and 4 patients had no symptoms. Endoscopic findings included telangiectasia in 18 patients, congested mucosa in 20, ulceration in 5, and stricture in 1. The RP ratio, $BED_{ICR}$, $BED_{ICR+EBRT}$ was significantly associated with the VRS (RP ratio, median 76.5%; $BED_{ICR}$, median 37.1 $Gy_3$; $BED_{ICR+EBRT}$, median 102.5 $Gy_3$; p < 0.001). The VRS was significantly associated with the EORTC/RTOG score (p = 0.038). Conclusion: The most prevalent endoscopic findings of RT-induced proctitis were telangiectasia and congested mucosa. The VRS was significantly associated with the EORTC/RTOG score and RP radiation dose.

• Journal of Pharmaceutical Investigation
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• 제27권2호
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• pp.99-108
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• 1997

To evaluate the feasibility of mucosal delivery of thyrotropin releasing hormone (TRH) through various mucosae, enzymatic degradation and stabilization of TRH in the nasal, rectal and duodenal extracts of rabbits were studied. TRH in the extracts was assayed by HPLC and its degradation was found to follow apparent first-order kinetics. The residual concentrations of TRH in the mucosal extracts of nasal, rectal and duodenal segments after 24 hr of incubation were found to be $65.1({\pm}1.1),\;19.7({\pm}2.7)$ and 0%, and in the serosal extracts, $65.6({\pm}5.5),\;75.2({\pm}1.1)$ and $68.7({\pm}1.4)%$, respectively. This result suggests that there is a significant difference in the activity of TRH-degrading enzymes among the sites of administration. The inhibition of TRH degradation in the mucosa extracts was kinetically investigated using various additives such as thimerosal, benzalkonium chloride, disodium edetate, ${\sigma}-phenanthroline$, dithiothreitol and dithioerythritol, and $IC_{50}$ values of inhibitors were calculated. The results obtained showed that thimerosal (0.5 mM) and benzalkonium chloride (0.141 mM) protected TRH from the enzymatic degradation in all the mucosa extracts more than 95% after 24 hr of incubation.

• Parasites, Hosts and Diseases
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• 제30권1호
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• pp.59-62
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• 1992

동남아시아를 여행하고 귀국한 후부터 시작된 약 1개월 동안의 복통, 설사 및 체중 감소를 주소로 내원한 서울이 거주지인 32세의 남자 환자가 구충증으로 진단되었다. 혈액 검사상 백혈구 수(16,750개111) 및 호산구의 백분율(33.7%)이 모두 상승되어 있었으나 빈혈 소견은 없었다. 대변 검사상 전형적인 구충의 충란이 대량 발견되었으며, S상결장경검사시 직장에서 적출된 충체 3마리를 관찰한 결과, 기생 부위가 전형적이지는 않았으나, 구강 및 생식기 등의 형태학적인 특징을 고려하여 듀비니구충(Ancylestoma duodenale)의 성충(♂: 1, ♀: 2마리)으로 동정 할 수 있었다. 구충제 (aetendazole)를 투여한 후 상기한 모든 증상이 급속히 호전되었다. 해외 여행시 감염되어 국내에 수입된 기생충 감염의 한 중례로 생각되며, 인체의 대장에 이소기생 (이소기생)한 구충 감염을 직접 확인한 드문 경우로 생각된다.

• 약학회지
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• 제38권5호
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• pp.530-543
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• 1994

To study the feasibility of transmucosal delivery of leucine enkephalin (Leu-Enk) and $[D-ala^2]$-leucine enkephalinamide (YAGFL), their degradation extents and pathways in various rabbit mucosa extracts were investigated by high performance liquid chromatography. The degradation of Leu-Enk and YAGFL was observed to follow the first-order kinetics. The degradation half-lives of Leu-Enk in the nasal, rectal and vaginal mucosal extracts were 1.62, 0.37 and 1.12 hrs and those of YAGFL were 30.55, 9.70 and 6.82 hrs, respectively, indicating Leu-Enk was degraded in a more extensive and rapid manner than YAGFL. But the mucosal and serosal extracts of the same mucosa showed the similar degradation rates for both pentapeptides. The degradation was most rapid in the neutral pH and increasing concentrations of substrates retarded the degradation rates. The maior hydrolytic fragments of Leu-Enk were Des-Tyr-Leu-Enk and tyrosine, indicating the enzymatic hydrolysis by aminopeptidases. However, the data also suggested endopeptidases such as dipeptidyl carboxypeptidase and dipeptidyl aminopeptidase could play some role in the degradation of Leu-Enk. On the other hand, the hydrolytic fragments of YAGFL in all the mucosa extracts were mainly Tyr-D-Ala-Gly and Phe-Leu-Amide, demonstrating the hydrolytic breakdown by endopeptidases. The degradation pathways were further explored by concomitantly determining the formation of smaller metabolites of primary hydrolytic fragments of Leu-Enk and YAGFL in the mucosa extracts.

• Biomolecules & Therapeutics
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• 제7권3호
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• pp.263-270
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• 1999

The in vitro permeation of thyrotropin-releasing hormone (TRH) through rabbit nasal, rectal and duodenal mucosae was studied in the absence and presence of an enzyme inhibitor and permeation enhancer. TRH in the donor and receptor solutions was assayed by HPLC. When thimerosal (TM, 0.5 mM) was added to the donor cell as an inhibitor, the permeation rate of TRH (200 $\mu\textrm{g}$/ml) increased linearly as a function of time. Fluxes of TRH through the nasal, rectal and duodenal mucosae were found to be 33.3$\pm$5.9, 11.8$\pm$1.9 and 9.6$\pm$0.7 $\mu\textrm{g}$/$\textrm{Cm}^2$/hr, respectively. The addition of sodium glycocholate, glycyrrhizic acid ammonium salt, sodium taurodihydrofusidate or L-$\alpha$-lysophosphatidylcholine to the donor solution containing TM did not result in the significant increase of permeation flux except for the duodenal mucosa, comparing with that in the presence of TM alone. Consequently, it was suggested that the nasal route was advantageous for systemic delivery of TRH, and the addition of TM and/or an enhancer was necessary to maximize the transmucosal permeation of TRH.