To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross-over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained released suppository (tested formulation, T) and progesterone suppository (reference formulation, R) was administered; a multiple dose of 2.75 mg/kg was given up to seven times with an interval of 8 h. Concentrations in serum were determined by a competitive enzyme immunoassay. The main parameters of T were: for single and multiple doses, Cmax was 48.8 +/- 11.8 ng/mL and 43.5 +/- 9.4 ng/mL, Tmax was 0.5 +/- 0.3 h and 0.4 +/- 0.3 h, AUC(0-24 h) was 362.4 +/- 143 ng x h x mL(-1) and 310.6 +/- 70.3 ng x h x mL(-1), respectively. The relative bioavailability of T to R were (104.2 +/- 13.4)% and (111.4 +/- 19.1)%, respectively. Statistical analysis showed that the two formulations were bioequivalent and T had sustained released feature.
Administration, Rectal ; Biological Availability ; Cross-Over Studies ; Progesterone/administration & dosage ; Progesterone/*pharmacokinetics ; Random Allocation ; Suppositories

Several models of experimental ulcerative colitis have been reported previously. However, none of these models showed the optimum characteristics. Although dextran sulfate sodium-induced colitis results in inflammation resembling ulcerative colitis, an obvious obstacle is that dextran sulfate sodium is very expensive. The aim of this study was to develop an inexpensive model of colitis in rats. Sprague-Dawley rats were treated with 2% dextran sulfate sodium in drinking water for 3 d followed by an intracolonic administration of 30% ethanol. The administration of 2% dextran sulfate sodium followed by 30% ethanol induced significant weight loss, diarrhea and hematochezia in rats. Severe ulceration and inflammation of the distal part of rat colon were developed rapidly. Histological examination showed increased infiltration of polymorphonuclear leukocytes, lymphocytes and existence of cryptic abscesses and dysplasia. The model induced by dextran sulfate sodium at lower concentration followed by 30% ethanol is characterized by a clinical course, localization of the lesions and histopathological features similar to human ulcerative colitis and fulfills the criteria set out at the beginning of this study.
Acute Disease ; Administration, Rectal ; Animals ; Colitis, Ulcerative ; chemically induced ; pathology ; Dextran Sulfate ; administration & dosage ; Disease Models, Animal ; Drug Administration Schedule ; Ethanol ; administration & dosage ; Female ; Rats

OBJECTIVETo study the therapeutic effect and feasibility of rectoclysis with Tuihuang decoction (RTD) in treating hyperbilirubinemia of newborns.

METHODSOne hundred and seventy-five newborns with hyperbilirubinemia were randomly divided into the treated group and the control group. They were treated with western medicine plus double faced blue treatment while the treated group were given RTD additionally. Blood bilirubin was detected by micro-bilirubin detector daily during the treatment course. The time of jaundice regression, the speed of blood bilirubin reducing, liver function, and condition of rebounding were observed.

RESULTSThe 7-day curative rate of jaundice in the treated group was superior to that in the control group, showing significant difference (P < 0.05). The average speed of blood bilirubin reducing daily in the treated group was quicker than that in the control group (P < 0.01). The improvement of liver function, such as AST, ALT and gamma-GT in the treated group was superior to that in the control group (P < 0.01). Rebound rate of blood bilirubin in the control group was significantly higher than that in the treated group (P < 0.05).

CONCLUSIONRTD is an ideal therapy for treatment of hyperbilirubinemia of newborn, it shows obvious clinical efficacy and can effectively prevent the rebound of blood bilirubin.

Administration, Rectal ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Humans ; Hyperbilirubinemia ; drug therapy ; Infant, Newborn ; Jaundice, Neonatal ; drug therapy ; Male ; Phytotherapy

Administration, Rectal ; Adolescent ; Adult ; Drugs, Chinese Herbal ; administration & dosage ; Endometriosis ; drug therapy ; Female ; Humans ; Middle Aged ; Phytotherapy

Irinotecan suppository was prepared using the moulding method with a homogeneous blend. A sensitive and specific fluorescence method was developed and validated for the determination of irinotecan in plasma using HPLC. The pharmacokinetics of intravenous administered and rectal administered in rabbits was investigated. Following a single intravenous dose of irinotecan (50 mg/kg), the plasma irinotecan concentration demonstrated a bi-exponential decay, with a rapid decline over 15 min. C(max), t(1/2), AUC(0-30h) and AUC(0-infinity) were 16.1 +/- 2.7 g/ml, 7.6 +/- 1.2 h, 71.3 +/- 8.8 microg.h/ml and 82.3 +/- 9.5 microg.h/ml, respectively. Following rectal administration of 100 mg/kg irinotecan, the plasma irinotecan concentration reached a peak of 5.3 +/- 2.5 microg/ml at 4 h. The AUC(0-30h) and AUC(0-infinity) were 32.2 +/- 6.2 microg.h/ml and 41.6 +/- 7.2 microg.h/ml, respectively. It representing ~50.6% of the absolute bioavailability.
Administration, Rectal* ; Biological Availability ; Chromatography, High Pressure Liquid ; Fluorescence ; Pharmacokinetics ; Plasma ; Rabbits

Irinotecan suppository was prepared using the moulding method with a homogeneous blend. A sensitive and specific fluorescence method was developed and validated for the determination of irinotecan in plasma using HPLC. The pharmacokinetics of intravenous administered and rectal administered in rabbits was investigated. Following a single intravenous dose of irinotecan (50 mg/kg), the plasma irinotecan concentration demonstrated a bi-exponential decay, with a rapid decline over 15 min. C(max), t(1/2), AUC(0-30h) and AUC(0-infinity) were 16.1 +/- 2.7 g/ml, 7.6 +/- 1.2 h, 71.3 +/- 8.8 microg.h/ml and 82.3 +/- 9.5 microg.h/ml, respectively. Following rectal administration of 100 mg/kg irinotecan, the plasma irinotecan concentration reached a peak of 5.3 +/- 2.5 microg/ml at 4 h. The AUC(0-30h) and AUC(0-infinity) were 32.2 +/- 6.2 microg.h/ml and 41.6 +/- 7.2 microg.h/ml, respectively. It representing ~50.6% of the absolute bioavailability.
Administration, Rectal* ; Biological Availability ; Chromatography, High Pressure Liquid ; Fluorescence ; Pharmacokinetics ; Plasma ; Rabbits

PURPOSE: During transrectal ultrasound guided prostate biopsy, 65% to 90% of patients reportedly have discomfort. We compared the anesthetic effects of a periprostatic injection of lidocaine under ultrasound guidance with the effects of a rectal instillation of lidocaine gel before the transrectal ultrasound guided prostate biopsy. MATERIALS AND METHODS: A prospective randomized double-blind study was performed in 72 patients requiring a systematic biopsy of the prostate. Patients were randomized into two groups according to the method of anesthetic delivery that was used. Group 1 consisted of 37 patients who intrarectally received 10 ml of 2% lidocaine gel 10 minutes before biopsy, and 5 ml of normal saline was injected into the periprostatic nerve plexus just before biopsy under ultrasound guidance using an 18 gauge 16 cm needle on each side. Group 2 consisted of 35 patients who received 10 ml of sterile gel without lidocaine and a 5 ml 1% lidocaine injection using the same method as group 1. The pain score was assessed using a visual analogue scale immediately after biopsy. RESULTS: There was a statistical difference in the mean pain score between the two groups (5.1+/-1.7 in group 1 versus 3.3+/-1.5 in group 2) (p<0.001), but The complication rates were not significantly different. CONCLUSIONS: We believe that performing the transrectal ultrasound guided prostatic nerve blockade before biopsy significantly diminishes the discomfort associated with the procedure, which, in turn, improves patient tolerance more so than rectal instillation of lidocaine gel. In addition, this procedure is a safe, simple, and rapid technique that should be considered in all patients undergoing transrectal ultrasound guided prostate biopsy.
Administration, Rectal* ; Anesthetics ; Biopsy* ; Double-Blind Method ; Humans ; Lidocaine* ; Needles ; Nerve Block ; Prospective Studies ; Prostate* ; Ultrasonography*

Chlorhexidine is widely used as an antiseptic and disinfectant in medical and nonmedical environments. Although the sensitization rate seems to be low, its ubiquitous use raises the possibility of sensitization in many patients and medical care workers. We describe a patient with anaphylaxis during digital rectal examination with chlorhexidine jelly. Urticaria, angioedema, dyspnea, and hypotension developed within a few minutes of the rectal examination. The patient fully recovered after treatment with epinephrine and corticosteroids. Skin tests for chlorhexidine were undertaken 5 weeks later, showing positive prick and intradermal skin tests. Within 30 min of the skin test, the patient complained of febrile sensation, chest tightness, angioedema, and urticaria on the face and trunk. An enzyme allergosorbent test for latex was negative. We present this case to alert clinicians about hypersensitivity to chlorhexidine that could potentially be life-threatening. We suggest that chlorhexidine should be recognized as a causative agent of anaphylaxis during procedural interventions.
Administration, Topical ; Adrenal Cortex Hormones/administration & dosage ; Anaphylaxis/*chemically induced/drug therapy ; Anti-Infective Agents, Local/administration & dosage/*adverse effects ; Chlorhexidine/administration & dosage/*adverse effects ; *Digital Rectal Examination ; Epinephrine/administration & dosage ; Humans ; Male ; Middle Aged ; Sympathomimetics/administration & dosage

Telomerase, an enzyme associated with cellular immortality, is expressed by most malignant cells and is inactive in most normal somatic cells, with the exception of proliferative stem cells, germ cells and activated lymphocytes. Measuring telomerase activity clinically may provide useful diagnostic and prognostic information of cancer. The purpose of this study was to investigate the change in telomerase activity following chemoradiation in rectal cancer, which almost always produces positive enzymatic activity. A total of 24 tumor tissue samples were used in this study, consisting of 12 paired specimens before and 4 week after chemoradiation. Telomerase activity was determined by PCR-based telomeric repeat amplification protocol (TRAP) assay. The telomerase activity was positive in 10 out of 12 patients (83%) in pre-irradiated and post-irradiated states. The levels of telomerase activity was decreased in 8 out of 10 patients after chemoradiation (80%) and two cases showed no change in enzymatic activity. One case showed no activity in either sample. The other case showed no enzymatic activity in the pre-irradiated sample, but showed weak activity in the post-irradiated sample. These data indicate that telomerase activity in rectal cancer is reduced after neoadjuvant chemoradiation therapy, possibly suggesting a mechanism of downstaging following chemoradiation therapy in cancer.
Adult ; Aged ; Antimetabolites, Antineoplastic/administration & dosage ; Antineoplastic Agents/administration & dosage ; Cisplatin/administration & dosage ; Combined Modality Therapy ; Enzyme Activation/radiation effects ; Enzyme Activation/drug effects ; Female ; Fluorouracil/administration & dosage ; Gene Amplification ; Human ; Male ; Middle Age ; Rectal Neoplasms/radiotherapy* ; Rectal Neoplasms/enzymology* ; Rectal Neoplasms/drug therapy ; Telomerase/metabolism*

PURPOSE: Capecitabine is an oral fluoropyrimidine carbamate and it is known as an effective radiosensitizer. Capecitabine and its metabolite reach their peak concentration in the plasma at 1~2 hours after a single oral administration of capecitabine and the levels fall rapidly thereafter. To verify the radiosensitizing effect of capecitabine that is based on such pharmacokinetic characteristics, we performed a retrospective analysis on the optimal timing of capecitabine administration with performing preoperative chemoradiation for locally advanced rectal cancer. MATERIALS AND METHODS: Among 171 patients who were treated with preoperative radiotherapy and concurrent capecitabine administration for rectal cancer, 56 patients were administered capecitabine at 1~2 hours before radiotherapy (group A), and at other time in the other 115 patients (group B). Total mesorectal excision was done at 4 to 6 weeks after the completion of chemoradiation. The radiosensitizing effect of capecitabine was evaluated on the basis of the pathological response. RESULTS: Complete pathological regression of the primary tumor was observed in 12 patients (21.4%) for group A and in 11 patients (9.6%) for group B (p=0.031). Residual disease less than 0.5 cm (a good response) was observed in 19 patients (33.9%) for group A and in 23 patients (20.0%) for group B (p=0.038). On multivariate analysis, the capecitabine ingestion time showed marginal significance. CONCLUSION: When performing preoperative chemoradiation for locally advanced rectal cancer, the radiosensitizing effect of capecitabine was enhanced when it was administered 1 hour before radiotherapy.
Administration, Oral ; Combined Modality Therapy ; Eating ; Humans ; Multivariate Analysis ; Plasma ; Radiation-Sensitizing Agents ; Radiotherapy ; Rectal Neoplasms* ; Retrospective Studies ; Capecitabine