• Journal of Pharmaceutical Investigation
• /
• v.10 no.3
• /
• pp.27-32
• /
• 1980

This paper was to investigate the biovailability of antipyrine, ampicillin and protein binding in pathological rats and rabbits pretreated with typhoid vaccine. The results are as follows: The absorption of antipyrine and ampicillin respectively were reduced in rats pretreated with typhoid vaccine as compared with those of normal rats. Especially absorption of ampicillin was more decreased than those of antipyrine. The blood level of antipyrine in severe state was decreased but in mild state. Blood level of ampicillin was decreased in mild state as well as in severe state. Relative bioavailability of antipyrine and ampicillin were mostly decreased in rabbits pretreated with typhoid vaccine except that of antipyrine in mild state. Renal clearance of antipyrine was not affected, but that of ampicillin was apt to increase. Protein binding of antipyrine and ampicillin were decreased by high concentration of typhoid vaccine.

• Journal of Pharmaceutical Investigation
• /
• v.12 no.1
• /
• pp.23-30
• /
• 1982

The effect of various surfactants on the absorption of antipyrine was studied using goldfish and rat. The results are as follows. The threshold concentration of antipyrine was reduced by various surfactants. Overturn time and death time of goldfish, in solution containing different concentration of antipyrine was reduced by the presence of various surfactants. Plots of reciprocal death time versus antipyrine concentration were linear with a positive concentration intercept such as minimum effective concentration. The absorption of antipyrine from rat small intestine was increased by administration with surfactants. As results, is believed to be one of rendering the goldfish membrane or rat small intestine more permeable to antipyrine.

• Archives of Pharmacal Research
• /
• v.14 no.3
• /
• pp.195-198
• /
• 1991

As potential antibacterial agents, several antipyrine derivatives were synthesized from 4-formylantipyrine and antibacterial activities of the synthesized compounds were also examined.

• Journal of Pharmaceutical Investigation
• /
• v.25 no.3
• /
• pp.193-204
• /
• 1995

In order to examine the effect of extrahepatic cholestasis induced by common bile duct ligation on the hepatic function, the pharmacokinetics of antipyrine and d-propranolol were investigated in rats. In addition, in an attempt to observe the degree of direct hepatic injury, light and electron microscopic observations and conventional pathologic test using serum were performed. Five days after common bile duct ligation, antipyrine(15 mg/kg) and d-propranolol(3 mg/kg) were intravenously administrated to the rats, respectively. The total clearances of antipyrine and d-propranolol were significantly(p<0.05) decreased. Because hepatic clearance of antipyrine poorly extracted by the liver and that of d-propranolol highly extracted by the liver are respectively dependent on the hepatic intrinsic clearance and the hepatic blood flow, it may be concluded that extrahepatic cholestasis following five days after common bile duct ligation decreased the hepatic intrinsic clearance and the hepatic blood flow. SGPT, SGOT, cholesterol, bilirubin(total bilirubin, direct bilirubin) and alkaline phosphatase were significantly increased(p<0.05). The proliferation of bile ducts was prominent, and degeneration and necrosis of hepatocytes were observed by light microscope. Also, ultrastructurally, bile canaliculi were containing the amorphous materials and losing microvilli, and SER and RER in hepatocytes were dilated and vacuolated.

• Toxicological Research
• /
• v.12 no.2
• /
• pp.265-270
• /
• 1996

Effects of a single administration of dichloromethane (DCM) on the hepatic drug metabollzing activity were determined using adult female rats. Rats were treated with DCM (3 mmol/kg, ip) and the disappearance of antipyrine (100 mg/kg, iv) or ethanol (2 g/kg, ip) from blood was measured. The blood concentration and half-life of antipyrine was not influenced by DCM administration. And DCM did not alter the blood concentration of ethanol measured for 240 min after the treatment. The effect of DCM treatment on in vitro cytochrome P-450-dependent enzyme activities was examined as well. No significant difference in either aniline hydroxylase or aminopyrine N-demethylase was observed in hepatic microsomal fractiorts of rats treated with DCM 24 hr prior to sacrifice. The present study indicates that acutely given DCM does not alter the metabolism of xenobiotics in vivo. The failure of DCM to alter the in vitro hepatic microsomal drug metabolizing activity was also noted.

• Archives of Pharmacal Research
• /
• v.15 no.1
• /
• pp.1-4
• /
• 1992

4-Acetylantipyrine 1 underwent condensation with 4-formyl-antipyrine 2 to give 3. Condensation of either 3 with 1 or 1 with 2 in a molar ratio of (2 :1) afforded 4. Cyclization of 4 in the presence of PPA and ammonium acetate or 4-aminoantipyrine in the presence of glacial acetic acid gave 5-6 respectively. Claisen condensation of 1 with ethyl acetate and diethyl oxalate afforded compounds 8-10. The reaction of 1 and 2 with indole in ethanol/conc. hyddrochloric acid was also investigated.

• Journal of Pharmaceutical Investigation
• /
• v.37 no.3
• /
• pp.131-135
• /
• 2007

A previous report recently demonstrated that ultrasound-induced hyperthermia (USHT:0.4 watts (W)/$cm^2$ at $41^{\circ}C$) could increase cellular uptake of P-glycoprotein (P-gp) substrates in P-gp expressing cancer cell lines. Since P-gp plays a major role in limiting drug permeability in the multi-drug resistant (MDR) cells, studies were conducted to elucidate the mechanism of USHT on cellular accumulation of P-gp and non-P-gp substrate in MDR cells. To accomplish this aim, we studied the effects of USHT on the accumulation of P-gp substrate, R123 and non-P-gp substrate, antipyrine in MDR cells. We demonstrated that USHT increased permeability of hydrophobic molecules (R123 and $[^{14}C]$-antipyrine). The enhanced permeability is reversible and size-dependent as USHT produces a much larger effect on cellular accumulation of $[^{14}C]$-antipyrine (MW 188) than that of R123 (MW 380.8). These results suggest that USHT could affect MDR cells more sensitive than BBMECs. Also, the present results point to the potential use of USHT to increase cellular uptake of P-gp recognized substrates, mainly anti-cancer agents into cancer cells.

• The Korean Journal of Physiology
• /
• v.1 no.2
• /
• pp.157-168
• /
• 1967

The entry of antipyrine and urea from the peritoneal cavity of rabbit into organ tissue and blood plasma was studied. Two hundred mg of antipyrine plus 300 mg of urea in 10 ml Ringer's solution was injected into the peritoneal cavity of anesthetized rabbit. The injection was made from above of a rabbit kept tying right side down and it enabled part of the abdominal organs (liver, intestine, kidney) was immersed in the injected solution and kept high concentration gradient throughout the experimental period. The remaining part of the organs was revered only by a thin film of the test solution. Subsequently, in this part of the organs the concentration gradient of the diffusible substances during entry was presumed to decrease as time elapsed. Four pieces of the liver tissue were taken namely, the right superficial, right deep, left superficial and left deep portions. Two were taken from the small intestine, one from the portion which was immersed in. the fluid and the other from that above the fluid mass. Both kidneys were separately analyzed. As a remote organ the gastrocnemius muscle was taken from the right leg of the animal. The intervals which were the time periods elapsed after injections were 5,7,10,15 or 30 minutes. At each point 5 animals were sacrificed and the concentrations of the test substances in the tissue water were measured. The results obtained were as follows. 1. In the liver the right portion which was immersed in the fluid showed higher concentration if the test substances than the left portion and the superficial region exceeded the deep region. The concentrations diminished as the time elapsed after infusion, particulary in the case of antipyrine, suggesting circulatory removal of the substances. In urea such decreasing tendency of the concentration was not obvious, and suggested slower removal rate of it as compared with that of antipyrine. 2. In the small intestine there was no regional difference in the concentration of the test substances. Because of the intestinal motility different portions of the intestine were seemed to have bathed in the fluid of the same concentration. In general the concentrations in the intestinal wall exceeded those of the liver, suggesting a slower removal rate than in the latter. 3. In the kidney the accumulation of the endogenous urea was predominant, and the accumulating mechanism in the renal tissue went on during the period of the experiment. Therefore it revealed increasing tendencies as the time elapsed. The penetration of the test substances in this organ from the peritoneal cavity seemed to be slower than in other abdominal organs, namely liver or small intestine. Part of the test substances in the kidney were obviously brought by the blood stream. 4. Rapid exponential decay of the concentration of antipyrine and of the osmolality of the peritoneal fluid was attributed to the extensive removal through the whole dimension of the peritoneal surface, and the remote organ such as the gastrocnemius muscle attained a fairly close value to that of the abdominal organs in less than 30 minutes. The factors which related to the absorption rate were discussed. They were the concentration gradient, permeability and the regional perfusion rate.

• The Journal of the Korean dental association
• /
• v.15 no.9
• /
• pp.717-718
• /
• 1977

• Asian-Australasian Journal of Animal Sciences
• /
• v.6 no.4
• /
• pp.577-580
• /
• 1993

Six lactating crossbred cows and six Murrah buffaloes, maintained under similar conditions of feeding and management were studied for body composition by the antipyrine dilution technique. Measurements were made at the start of the experiment when the animals had completed about 50 days in lactation and thereafter at monthly intervals up to 90 days of the experimental period. The percent body water estimates in both species at different time intervals did not change significantly. Percent body fat and protein content also remained unchanged. The correlation coefficient between body composition parameters and various hormones (growth hormone, insulin, $T_3$ and $T_4$) were generally low and non-significant. It was concluded that body composition studies using body water are not sufficiently sensitive to predict changes in body composition of lactating cows and buffaloes and/or the changes in body composition during lactation are not very drastic.