2.Research advance on pediatric antipyretic.
Chinese Journal of Contemporary Pediatrics 2008;10(6):759-761
5.Preparation of salvianolic acid B, tanshinone Ⅱ_A, and glycyrrhetinic acid lipid emulsion and its protective effect against acute liver injury induced by acetaminophen.
Xiu-Rong ZHANG ; Tao LIN ; Xiu-Li WANG ; Xiao-Jie WANG ; Heng GU
China Journal of Chinese Materia Medica 2022;47(17):4634-4642
Salvianolic acid B(Sal B), tanshinone Ⅱ_A(TSN Ⅱ_A), and glycyrrhetinic acid(GA) lipid emulsion(GTS-LE) was prepared by the high-speed dispersion method combined with ultrasonic emulsification.The preparation process of the emulsion was optimized by single-factor method and D-optimal method with appearance, centrifugal stability, and particle size of the emulsion as evalua-tion indexes, followed by verification.In vitro release of Sal B, TSN Ⅱ_A, and GA in GTS-LE was performed by reverse dialysis.In vivo pharmacokinetic evaluation was carried out in mice.The acute liver injury model was induced by acetaminophen.The effect of oral GTS-LE on the acute liver injury was investigated by serum liver function indexes and pathological changes in liver tissues of mice.The results showed that under the optimal preparation process, the average particle size of GTS-LE was(145.4±9.25) nm and the Zeta potential was(-33.6±1.45) mV.The drug-loading efficiencies of Sal B, TSN Ⅱ_A, and GA in GTS-LE were above 95%, and the drug release in vitro conformed to the Higuchi equation.The pharmacokinetic results showed that the C_(max) of Sal B, TSN Ⅱ_A, and GA in GTS-LE was 3.128, 2.7, and 2.85 times that of the GTS-S group, and AUC_(0-t) of Sal B, TSN Ⅱ_A, and GA in GTS-LE was 3.09, 2.23, and 1.9 times that of the GTS-S group.After intragastric administration of GTS-LE, the activities of alanine aminotransferase and aspartate aminotransferase were significantly inhibited, the content of malondialdehyde was reduced, and the structure of hepatocytes recovered to normal.In conclusion, GTS-LE can delay the release of Sal B and promote the release of TSN Ⅱ_A and GA.The encapsulation of three drug components in the emulsion can improve the oral bioavailability to varying degrees and can effectively prevent the acute liver injury caused by acetaminophen.
Abietanes/therapeutic use*
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Acetaminophen/therapeutic use*
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Alanine Transaminase/metabolism*
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Animals
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Antipyretics/therapeutic use*
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Aspartate Aminotransferases/metabolism*
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Benzofurans/therapeutic use*
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Chemical and Drug Induced Liver Injury/prevention & control*
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Depsides/therapeutic use*
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Emulsions
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Glycyrrhetinic Acid/therapeutic use*
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Liver/drug effects*
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Malondialdehyde
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Mice
6.A randomized, double blind, and controlled clinical trial of the non-addictive propacetamol in postoperative analgesia.
En-ling MA ; Xiu-rong WANG ; Zhu-ming JIANG ; Yu CUI ; Rong WANG ; Jia LIU
Acta Academiae Medicinae Sinicae 2003;25(3):329-332
OBJECTIVETo compare the postoperative analgesic efficacy and safety of the non-addictive propacetamol hydrochloride (Pro-Bufferin) injection and dolantin in a prospective, randomized, double blind and controlled clinical trial.
METHODSAfter the pain intensity was assessed when the patients were undergone thoracic and abdominal selective surgery became fully conscious, 40 consecutive patients with moderate to severe postoperative pain (equivalent to Pain Grade I and II of American Anesthesia Association classification) were randomized into the study against the control groups. The two groups were similar for age, sex, height/weight, disease categories, operation categories, anesthesia methods and duration, vital signs, hepatorenal function, and blood cell count (P = 0.06-0.93). In the study group, 2 g propacetamol in 100 ml normal saline (NS) intravenously with 1.0 ml NS intramuscularly as the placebo control to dolantin were administered. In the control group, 1.6 g mannitose in 100 ml NS intravenously as the placebo control to propacetamol with 50 mg dolantin (1.0 ml) intramuscularly as the positive control to propacetamol were administered. The intensity change of postoperative pain was then evaluated 10 times with visual analog scale and verbal describing scale during 6 h from the beginning of propacetamol infusion. Vital signs and adverse reactions were also documented. After all data were put into the computer, the blinding codes were decoded and the statistic analysis was then made.
RESULTSThere was no significant difference (P = 0.93) about the area under the curve of "Pain Relieve Score vs. Time". The "starting to effect" time (15-30 min), analgesic duration (6 h) and the percentage of excellent or good analgesic effect (90%) in the two groups were the same. Adverse reactions didn't reached the statistic different level (P = 0.35).
CONCLUSIONSPropacetamol HCL injection 2 g intravenously could be an alternative to dolantin 50 mg intramuscularly for moderate to severe postoperative pain with its advantage of being non-addictive.
Acetaminophen ; analogs & derivatives ; therapeutic use ; Adult ; Aged ; Analgesics ; therapeutic use ; Double-Blind Method ; Female ; Humans ; Male ; Meperidine ; therapeutic use ; Middle Aged ; Pain, Postoperative ; drug therapy
8.Comparison of preemptive analgesia efficacy between etoricoxib and rofecoxib in ambulatory gynecological surgery.
Wei LIU ; C C LOO ; H M TAN ; Tie-Hu YE ; Hong-Zhi REN
Acta Academiae Medicinae Sinicae 2004;26(6):666-670
OBJECTIVETo compare the preemptive analgesia efficacy between two cycloxygenase-2 inhibitors, rofecoxib and etoricoxib in the ambulatory uterine evacuation patients.
METHODSIn this randomized, double-blinded, placebo-controlled trial 60 patients were randomly divided into three groups and received a single dose of placebo, rofecoxib 50 mg, or etoricoxib 120 mg, respectively, before operation. Patient's visual analogue score (VAS) was rated postoperatively at 15 min, 30 min, 60 min, time-to-discharge, 6 h and 24 h. Fentanyl (in post-anesthesia care unit) and paracetamol (at home) were supplementary analgesics and the dosage was also recorded. Patient's satisfaction score was rated at 24 h postoperatively.
RESULTSEtoricoxib 120 mg and rofecoxib 50 mg were significantly superior to placebo at 6 h postoperatively (P < 0.05) while there was no significant differences of VAS at other time points. The amounts of Fentanyl used in post-anesthesia care unit were similar in three groups, but paracetamol taken at home was much less in rofecoxib group and etoricoxib group than in placebo group (P < 0.01). Compared to rofecoxib, etoricoxib provided better pain relief after discharge (P < 0.05). The overall pain management satisfaction score was significantly higher in etoricoxib group (96 +/- 7) than in other groups (P < 0.01).
CONCLUSIONPreemptive rofecoxib 50 mg and etoricoxib 120 mg may significantly decrease VAS at 6 h postoperatively, and reduce the usage of analgesics in ambulatory uterine evacuation patients. Etoricoxib 120 mg offeres better pain relief at home compared with rofecoxib 50 mg.
Abortion, Induced ; adverse effects ; Acetaminophen ; therapeutic use ; Adolescent ; Adult ; Ambulatory Surgical Procedures ; Analgesics, Non-Narcotic ; therapeutic use ; Analgesics, Opioid ; therapeutic use ; Cyclooxygenase Inhibitors ; therapeutic use ; Double-Blind Method ; Female ; Fentanyl ; therapeutic use ; Humans ; Lactones ; therapeutic use ; Pain Measurement ; Pain, Postoperative ; prevention & control ; Preoperative Care ; Pyridines ; therapeutic use ; Sulfones ; therapeutic use
9.Comparison of Parecoxib and Proparacetamol in Endoscopic Nasal Surgery Patients.
Yigal LEYKIN ; Andrea CASATI ; Alessandro RAPOTEC ; Massimiliano DALSASSO ; Luigi BARZAN ; Guido FANELLI ; Tommaso PELLIS
Yonsei Medical Journal 2008;49(3):383-388
PURPOSE: The aim of the study was to compare the efficacy of parecoxib for postoperative analgesia after endoscopic turbinate and sinus surgery with the prodrug of acetaminophen, proparacetamol. MATERIALS AND METHODS: Fifty American Society of Anesthesiology (ASA) physical status I-II patients, receiving functional endoscopic sinus surgery (FESS) and endoscopic turbinectomy, were investigated in a prospective, randomized, double-blind manner. After local infiltration with 1% mepivacaine, patients were randomly allocated to receive intravenous (IV) administration of either 40mg of parecoxib (n=25) or 2g of proparacetamol (n=25) 15 min before discontinuation of total IV anaesthesia with propofol and remifentanil. A blinded observer recorded the incidence and severity of pain at admission to the post anaesthesia care unit (PACU) at 10, 20, and 30 min after PACU admission, and every 1 h thereafter for the first 6 postoperative h. RESULTS: The area under the curve of VAS (AUC(VAS)) calculated during the study period was 669 (28-1901) cm·min in the proparacetamol group and 635 (26-1413) cm·min in the parecoxib group (p=0.34). Rescue morphine analgesia was required by 14 patients (56%) in the proparacetamol group and 12 patients (48%) in the parecoxib (p> or=0.05), while mean morphine consumption was 5-3.5mg and 5-2.0mg in the proparacetamol groups and parecoxib, respectively (p> or=0.05). No differences in the incidence of side effects were recorded between the 2 groups. Patient satisfaction was similarly high in both groups, and all patients were uneventfully discharged 24h after surgery. CONCLUSION: In patients undergoing endoscopic nasal surgery, prior infiltration with local anaesthetics, parecoxib administered before discontinuing general anaesthetic, is not superior to proparacetamol in treating early postoperative pain.
Acetaminophen/administration & dosage/analogs & derivatives/*therapeutic use
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Adult
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Analgesics, Non-Narcotic/administration & dosage/therapeutic use
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Cyclooxygenase Inhibitors/administration & dosage/therapeutic use
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Double-Blind Method
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Endoscopy/methods
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Female
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Humans
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Infusions, Intravenous
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Injections, Intravenous
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Isoxazoles/administration & dosage/*therapeutic use
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Male
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Middle Aged
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Nasal Polyps/surgery
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Pain, Postoperative/*drug therapy
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Prodrugs/administration & dosage/*therapeutic use
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Prospective Studies
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Sinusitis/surgery
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Treatment Outcome
10.Regular paracetamol in severe dengue: a lethal combination?
Chin Seng GAN ; Sze Yee CHONG ; Lucy Chai See LUM ; Way Seah LEE
Singapore medical journal 2013;54(2):e35-7
An eight-month-old female infant with severe dengue disease, who was repeatedly given therapeutic paracetamol for severe dengue, developed fulminant liver failure with encephalopathy, gastrointestinal haemorrhage and severe coagulopathy. She responded to supportive measures and N-acetylcysteine infusion. This case highlights the potential danger of administering repeated therapeutic doses of paracetamol in childhood severe dengue disease with hepatitis.
Acetaminophen
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adverse effects
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therapeutic use
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Antipyretics
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adverse effects
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therapeutic use
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Blood Coagulation
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Female
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Hepatic Encephalopathy
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drug therapy
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Humans
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Infant
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Liver Failure, Acute
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chemically induced
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Severe Dengue
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drug therapy
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Treatment Outcome