• Archives of Pharmacal Research
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• v.28 no.4
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• pp.502-508
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• 2005

Titrated extract of Centella asiatica (TECA) contains three principal ingredients, asiaticoside (AS), asiatic acid (AA), and madecassic acid (MA). These components are known to be clinically effective on systemic scleroderma, abnormal scar formation, and keloids. However, one problem associated with administration of TECA is its low solubility in aqueous as well as oil medium. In this study, various nonionic surfactants and bile salts as anionic surfactant were tested and screened for solubilizing TECA with a view to developing topical hydrogel type of ointment which is stable physicochemically, and has better pharmacological effects. When TECA was incorporated into various nonionic surfactant systems, labrasol had the most potent capacity for solubilizing TECA. In cases of bile salt systems, Na-deoxycholate (Na-DOC) had foremost solubilizing capacity, even more than labrasol. In differential scanning calorimetric study, the peaks of AA, MA, AS and Na-DOC disappeared at the coprecipitate of $1\%$ TECA and $1\%$ Na-DOC, suggesting the optimum condition of Na-DOC for solubilizing TECA. When the physicochemical stability of hydrogel containing this mixture was assessed, it was stable at room temperature for at least one month. Pharmacologically it significantly decreased the size of wound area at the $9^{th}$ day when applied to the wound area of rat dorsal skin. Taken together, solubility of TECA was dramatically improved by using non ionic and anionic surfactant systems, and Na-DOC was found to be the most effective solubilizer of TECA in formulating a TECA-containing hydrogel typed ointment. Moreover this gel was considered to be applicable to clinical use for wound healing effect.

• Archives of Pharmacal Research
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• v.24 no.3
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• pp.219-223
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• 2001

Nasal absorption of procyclidine, a synthetic anticholinergic compound, was investigated in Wistar rats and Beagle dogs. The dosing solution was prepared by dissolving$^{14}C$-procyclidme in 50% ethanolic saline. The dosing solution was administered intravenously and intranasally to rats at a dose of 0.6 mg/kg (i.e., $60{\mu}$l/kg in the form of a 1% w/v solution), and intravenously, orally and intranasally to doss at a dose of 0.3 mg/kg(i.e., $6{mu}$l/kg in the form of a 5% w/v solution). Blood samples were taken from an artery of the animals through the catheter for periods of 1200 (for rats) and 1440 min (for dogs), and the radioactivity in the samples was determined by liquid scintillation counting. The nasal bioavailability of Procyclidine in rats and dogs, based on the radioactivity was calculated to be 81.1 and 98.6% respectively. In both rats and dogs, the plasma profiles of procyclidine following nasal administration were very close to those following intravenous administration, leading to nearly superimposable profiles between the two protocols. In dogs, nasal administration resulted in significantly higher plasma concentrations during the first 30 min period compared to oral administration, suggesting the superiority of the nasal route over the oral route in terms of a prompt expression of the pharmacological effect of the drug. The results obtained in this study indicate that procyclidine is rapidly and nearly completely absorbed via the nasal route. In conclusion, nasal administration represents a viable alternative to intravenous administration in the case of procyclidine.

• Archives of Pharmacal Research
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• v.29 no.4
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• pp.323-327
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• 2006

The objective of this study was to examine the pharmacokinetics of organic cations in intrahepatic cholestatic rats. A pretreatment with $17{\alpha}$-ethynylestradiol was used to induce intrahepatic cholestasis, and tributylmethylammonium (TBuMA) was used as a representative model organic cation. When $[^3H]$TBuMA was intravenously administered, the AUC value for TBuMA was significantly increased by $79\%$ in cholestasis, and its total systemic clearance was consequently decreased by $46\%$. In addition, the in vivo hepatic uptake clearance of TBuMA from the plasma to the liver was decreased by $50\%$ in cholestasis. The concentration of bile salts in plasma was increased by 2.1 fold in cholestatic rats. Since TBuMA forms ion-pair complexes with anionic components such as bile salts, the decreased hepatic uptake of TBuMA in cholestasis may be due to a change in endogenous components, e.g., bile salts in the plasma. In isolated normal hepatocytes, the uptake clearance for TBuMA in the presence of cholestatic plasma was decreased by $20\%$ compared with normal plasma. Therefore, we conclude that the inhibition of the hepatic uptake process by the cholestasis may be in part due to the increased formation of ion-pair complexes of TBuMA with bile salts in the plasma.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.978-983
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• 2002

Small intestinal transit (SIT) has often been regarded as an index of pathophysiological state of postoperative ileus (PI) in rats. The reliability of SIT as an index of PI was examined in the present study. PI was induced via abdominal surgery (i.e., laparotomy with evisceration and manipulation) in rats. For one group of PI-induced rats, SIT of a charcoal test meal was measured. When necessary, the physical state (i.e., severity and site of distension) of the gastrointestinal (GI) tract in each rat was visually examined. For another group of PI-induced rats, abdominal X-ray radiographs were obtained after introducing the barium sulfate suspension. The abdomen was then opened and the physical state of the GI tract was visually examined. The SIT was decreased in most of the PI-induced rats, and the GI distension was observed, with substantial intersubject variations, in all of the PI-induced rats. However, no linear relationship was evident between the SIT and the severity of GI distension (e.g., at 20 h after PI induction). Instead, the severity and site of GI distension could be monitored by the X-ray radiology. Therefore, the use of SIT as an index of PI should be substantially limited.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.9
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• pp.4335-4339
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• 2012

Background: Whether sirolimus is useful in the prevention of non-melanoma skin cancer (NMSC) remains unclear and we therefore performed this meta-analysis of randomized controlled trials to test the hypothesis that Sirolimus-based immunosuppression is associated with a decrease in NMSC. Methods: The main outcomes were NMSC, squamous-cell carcinoma and basal-cell carcinoma. The pooled risk ratio (RR) with its 95% confidence interval (95%CI) were used to assess the effects. Results: 5 randomized trials involving a total of 1499 patients receiving kidney transplantation were included. Patients undergoing Sirolimus-based immunosuppression had much lower risk of NMSC (RR = 0.49, 95%CI 0.32-0.76, P = 0.001). Subgroup analyses by tumor type showed that Sirolimus-based immunosuppression significantly decreased risk of both squamous-cell carcinoma (RR = 0.58, 95%CI 0.43-0.78, P < 0.001) and basal-cell carcinoma (RR = 0.56, 95%CI 0.37-0.85, P = 0.006). The quality of evidence was high for NMSC, and moderate for squamous-cell carcinoma and basal-cell carcinoma. No evidence of publication bias was observed. Conclusion: High quality evidence suggests that Sirolimus-based immunosuppression decreases risk of non-melanoma skin cancer, and Sirolimus has an antitumoral effect among kidney-transplant recipients.

• CELLMED
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• v.1 no.1
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• pp.2.1-2.16
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• 2011

Diverse medicinal uses of different types of products obtainable from Brassica juncea have been known for centuries. Most such traditionally known uses of the plant have been centered on its seeds and oils obtainable from them. During more recent decades diverse bio-active molecules and their therapeutically interesting pharmacological properties of its green edible leaves have also been described, and they are now often considered to be effective substitutes for other so called "healthy" Brassica vegetables. However, little concentrated effort has yet been made to obtain a pharmacologically better defined phytopharmaceutical from this easily cultivable plant of commercial interest in many underdeveloped and developing countries. The main aim of this overview is to point out some possibilities for designing and developing such products from the plant for combating the rapidly spreading obesity epidemic in the developed countries and some other countries. Efforts to achieve such goals could as well be an economically more feasible, and culturally more acceptable, starting point for better understanding the potential health benefits of other vegetarian foods.

• Advances in Traditional Medicine
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• v.7 no.2
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• pp.121-127
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• 2007

Curcumin, a dietary pigment responsible for the yellow color of curry, has been used for the treatment of inflammatory diseases and exhibits a variety of pharmacological effects such as anti- inflammatory, anti-tumor, anti-oxidant, and anti-viral activity. In order to examine the potency of the curcumin in inflammation we used carrageenan induced rat hind paw odema model. As curcumin is practically water insoluble, it is hypothesized that pharmacological activity of curcumin could be improved by enhancing its water solubility. Water soluble complexes of curcumin with cyclodextrins were prepared and screened for greater solubility. Pure curcumin 100 mg/kg body weight along with curcumin complexes equivalent to 100 mg/kg body weight of pure curcumin were tested for the anti-inflammatory activity in Wister rats male rats using carrageenan induced hind paw edema model and compared with that of the reference compound diclofenac sodium at a dose level of 10 mg/kg body weight. Results were statistically analyzed using ANOVA. All the treatment groups showed statistically significant anti-inflammatory activity compared with that of vehicle control and positive control.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2003.11a
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• pp.109-109
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• 2003

Taurine is present in a variety of tissue and exhibits many important physiological functions in many tissues. Although it is known that many tissues mediate taurine transport, its functions of taurine transport in bone have not been identified yet. In the present study, we investigated the expression of taurine transporter (TauT) and taurine uptake using mouse stromal ST2 cells and osteoblast-like MC3T3-El cells, which is bone related cells. Detection of TauT mRNA expression in these cells were performed by reverse transcription polymerase chain reaction (RT-PCR). The activity of TauT was assessed by measuring the uptake of ［$^3$H］taurine in the presence or absence of inhibitors. TauT mRNA was detected in these cells. ［$^3$H］Taurine uptake was dependent upon the presence of extracellular sodium, chloride and calcium ions, and inhibited by cold-taurine and ${\beta}$-alanine. These results suggest that taurine has biological functions in bone and some effect on the bone cells.

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.392-399
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• 2002

The effects of vehicles and penetration enhancers on the in vitro permeation of melatonin through dorsal hairless mouse skin were investigated. Propylene glycol laurate (PGL), isopropyl myristate (IPM), propylene glycol monolaurate (PGML) and propylene glycol monocaprylate (PGMC) showed high permeation fluxes and PGL, PGML and PGMC decreased lag time significantly. In both of the binary co-solvents of diethylene glycol monoethyl ether (DGME)-PGL and DGME-IPM, the highest fluxes were achieved at 20% of DGME, which were $10.5{\pm}1.5$ and $9.1{\pm}2.4{\;}{\mu\textrm{g}}/cm^2/h$, respectively. Among fatty acids used as a permeation enhancer, capric acid and oleic acid in DGME-PGL (80:20 v/v) showed relatively high enhancing effects. Capric acid also shortened the lag time of melatonin from $2.4{\pm}0.7{\;}to{\;}1.3{\pm}0.2{\;}h$. Oleic acid, however, failed to shorten the lag time. Therefore, for effective solution formulations in terms of permeation flux and lag time, capric acid-containing DGME-PGL (80 : 20 v/v) could be used to enhance the skin permeation of melatonin.

• Korean Journal of Pharmacognosy
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• v.24 no.1
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• pp.38-46
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• 1993

Two kinds of gangliosides contained in deer horns were determined by integrating the peaks of TLC densitometry. Japanese deer horn originated from China showed the highest gangliosides among tested samples and the upper parts in deer horns showed higher gangliosides than the lower parts. In the case of graded samples, the best grade A showed the highest content and the worst grade E did the lowest content. Sixteen kinds of free amino acids were analyzed by auto amino acid analyzer. The lower region the deer horn was, the more the total content of free amino acids was and several kinds of amino acids were contained quite regularly.