BACKGROUND AND OBJECTIVES: Pain is one of the most troublesome discomfort accompanying tonsillectomy. Pharyngeal muscle spasm is one of the causes of post-tonsillectomy pain. We investigated the effect of an oral central muscle relaxant agent (chlorophenesin carbamate: CPC) on post-tonsillectomy pain. MATERIALS AND METHOD: Thirty adult patients undergoing tonsillectomy were included in this study. Basic pain control per oral administration consisted of 3.0 g/day (t.i.d.) salicylsalicylic acid and intramuscular injection of 5 mg diclofenac sodium (DCF) on demand. The patient population was divided into CPC group (n=15) and control group (n=15) randomly. CPC Group (n=15) received additional oral ingestion of 375 mg (t.i.d.) CPC for 7 days after operation. Pain assesment was peformed using visual analogue scale (VAS) at rest and while swallowing at the first (POD1) and seventh (POD7) day of the operation. Pain relief score (PRS) is the difference between VAS at POD1 and POD7. The number of injection of DCF was compared also. RESULTS: VAS of CPC group and the control at POD1 were 1.9+/-1.7/4.8+/-2.3 (rest/swallowing) and 2.8+/-1.6/5.2+/-1.9, respectively. VAS of CPC group and the control at POD7 were 1.5+/-1.8/3.4+/-1.9 and 1.8+/-1.3/3.5+/-1.5, respectively. The VAS scores of the two groups at POD1 and POD7 are not significantly different. The PRS of CPC group and the control group were 1.7+/-0.7/1.4+/-1.4 (rest/swallowing) and 1.0+/-1.0/1.6+/-1.2 (rest/swallowing), respectively. No significant difference in PRS was observed between the two study groups. The number of injection of DCF between the two groups is not significantly different. CONCLUSION: No significant benefit is found for the use of oral muscle relaxant agent after tonsillectomy.
Administration, Oral ; Adult ; Deglutition ; Diclofenac ; Eating ; Equidae ; Humans ; Injections, Intramuscular ; Pharyngeal Muscles ; Spasm ; Tonsillectomy

Two different salts of diclofenac, diclofenac sodium and diclofenac potassium, in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study. Biochemical and physiological parameters were also measured in both normal and dehydrated states. Diclofenac levels in plasma were determined using a validated reversed phase HPLC method. Primary kinetic parameters i.e. AUC(0-infinity), Cmax, Tmax and other disposition kinetics were obtained with non-compartmental procedure. Biochemical parameters i.e. packed cell volume, plasma glucose and total lipid concentration in dehydrated rabbits increased significantly. Plasma concentration of diclofenac sodium and diclofenac potassium decreased significantly in water deprived rabbits. In comparison, diclofenac potassium in normal and dehydrated state of the same group of rabbits showed a significantly increased plasma concentration when compared with diclofenac sodium.
Administration, Oral ; Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; blood ; pharmacokinetics ; Area Under Curve ; Biological Availability ; Dehydration ; metabolism ; Diclofenac ; administration & dosage ; analogs & derivatives ; blood ; pharmacokinetics ; Rabbits ; Tablets

PURPOSE: To report a case of anterior chamber irrigation with distilled water during cataract operation. METHODS: During the cataract operation of 56 year-old male patient, corneal edema and anterior chamber hazziness were noted after anterior chamber irrigation with distilled water for a minute. Distilled water was replaced rapidly balanced salt solution (BSS) as irrigation solution and operation was completed. At postoperative one day, corneal edema and anterior chamber exudative membrane were formed. After topical 5% NaCl, 1% prednisolone treatment, corneal edema and exudative membrane disappeared at postoperative sixth week. BCVA was 0.6. At postoperative ninth week, the patient complained of decreased visual acuity. On fundus exmination and flourescein angiography, cystoid macular edema (CME) was detected. RESULTS: After prednisolone oral administration and diclofenac eyedrop instillation, CME improved. At postoperative 24th month, BCVA was 0.8 and CME disappeared. CONCLUSIONS: From our experience of a case of anterior chamber irrigation with distilled water during cataract operation, if balanced salt solution replaces hypotonic solution rapidly as irrigation solution, corneal and other complications are managed properly, long term visual acuity appears good.
Administration, Oral ; Angiography ; Anterior Chamber* ; Cataract* ; Corneal Edema ; Diclofenac ; Humans ; Macular Edema ; Male ; Membranes ; Middle Aged ; Prednisolone ; Visual Acuity ; Water*

To evaluate the efficacy and safety of compound Decumbent Corydalis Rhizome (DCR) in treating patients with knee osteoarthritis (OA). Totally 79 patients with knee osteoarthritis were selected from out-patient and inpatient departments of West China Hospital and randomly divided into the test group and the control group. The test group (n = 41) was given Compound DCR with the dosage of 1.8 g · d(-1), while the control group (n = 38) was administered with diclofenac sodium with the dosage of 75 mg · d(-1). After 12 weeks of treatment, the total efficacy rates based on patients/physicians evaluation for experimental and control groups were 68.29%, 63.41% and 71.05%, 63.16%, respectively, without significant difference between the two groups. Both of the two groups showed significant improvements in the main efficacy indexes (pain on walking 20 m) and minor indexes (tenderness on palpation, Western Ontario and McMaster Universities OA index (WOMAC) and Short-Form Health Survey (SF-36 ), but without significant difference in efficacy between them. The incidence of related adverse events was 24.39% in the test group and 47.37% in the control group, respectively, with significant differences between the two groups (P < 0.05). In the controlled study, compound DCR is as efficient as diclofenac sodium but more tolerable, with a good clinical application prospect.
Adult ; Aged ; Corydalis ; chemistry ; Diclofenac ; administration & dosage ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Humans ; Male ; Middle Aged ; Osteoarthritis, Knee ; drug therapy ; Rhizome ; chemistry ; Treatment Outcome

OBJECTIVESynthetical evaluation of promoting effect of some kinds of transdermal enhancers was carried through.

METHODDiclofenac sodium was used as model, and azone and l-menthol and synthetic borneol and olieic acid and essential oil from Cnidium monnieri were used as transdermal enhancers. Transdermal absorption experimentation of diclofenac sodium on the device of penetrating skins in vitro was done. Cumulation of permeation amount and penetrating rates and steady fluxes and lag times were observed, and grey relational cluster method was used to evaluate the promoting effect of some kinds of transdermal enhancers.

RESULTAs for promoting effect on diclofenac sodium, azone and l-menthol were the best, and synthetic borneol and olieic acid ranked behind.

CONCLUSIONGrey relational cluster method can evaluate promoting effect objectively and fairly.

Administration, Cutaneous ; Animals ; Azepines ; pharmacology ; Bornanes ; pharmacology ; Cluster Analysis ; Cnidium ; chemistry ; Diclofenac ; administration & dosage ; pharmacokinetics ; Male ; Menthol ; pharmacology ; Oils, Volatile ; isolation & purification ; pharmacology ; Rabbits ; Skin Absorption ; drug effects

Acanthamoeba Keratitis ; diagnosis ; drug therapy ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; Atropine ; administration & dosage ; Cornea ; pathology ; Diagnosis, Differential ; Diclofenac ; administration & dosage ; Drug Administration Schedule ; Drug Therapy, Combination ; Follow-Up Studies ; Humans ; Mydriatics ; administration & dosage ; Ophthalmic Solutions ; Retrospective Studies

Hydroxyethyl chitin (HECH) is a water soluble chitin derivative made by etherification of chitin, ethylene chlorohydrin was used as etherification reagent in this reaction. A novel interpenetrating polymer network (IPN) composed of HECH/PAA was prepared. The IR spectra confirmed that HECH/PAA was formed through chemical bond interaction. The sensitivity of this hydrogel to temperature and pH was studied. The swelling ratio of this hydrogel in artificial intestinal juice is much greater than that in artificial gastric juice. The IPN hydrogel exhibited a typical pH-sensitivity, and its degree of swelling ratio increased with the increase of temperature. The sustained-release drug system of Dichlofenac potassium was prepared by using HECH/PAA as the drug carrier. The release experiment showed a perfect release behavior in artificial intestinal juice. This IPN is expected to be used as a good drug delivery system of enteric medicine.
Acrylates ; administration & dosage ; chemistry ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; Chitin ; administration & dosage ; analogs & derivatives ; chemistry ; Delayed-Action Preparations ; Diclofenac ; administration & dosage ; Drug Carriers ; chemical synthesis ; Drug Delivery Systems ; Hydrogel, Polyethylene Glycol Dimethacrylate ; administration & dosage ; chemistry ; Hydrogen-Ion Concentration

BACKGROUND: NSAIDs and methotrexate induce gut damage and bacterial translocation (BT). However, there is no study examining the combined effects of methotrexate and NSAID on gut damage and BT. We examined the combined effects of methotrexate and NSAID-induced enteropathy and bacterial translocation in an experimental animal model. METHODS: Rats received either no drug, NSAID alone (diclofenac 80 mg/kg and 120 mg/kg per os), methorexate alone (20 mg/kg per os) or NSAID with methotrexate. Gut barrier dysfunction, the degree of intestinal adhesion, stool pellet number, bacterial number of total aerobes and Gram negatives in the distal ileal and cecal contents and the number of Gram negatives in the mesenteric lymph nodes, liver, spleen, kidney and heart were measured. RESULTS: Administration of diclofenac or methotrexate alone caused an increase in gut barrier dysfunction and intestinal adhesion and a decrease in stool pellet number. Administration of diclonfenac alone induced enteric bacterial overgrowth and increased BT to the mesenteric lymph nodes, liver, spleen, kidney and heart. Administration of methotrexate alone induced enteric bacterial undergrowth and BT to the mesenteric lymph nodes, liver, spleen but not to the kidney and heart. The supplements with methotrexate increased the NSAID-induced gut barrier dysfunction and intestinal adhesion, and decreased the stool pellet number. However, the reduced NSAID-induced enteric Gram negative bacterial overgrowth (with a dose of diclofenac of 80 mg/kg) and BT to the liver, spleen, kidney and heart. COCNLUSION: Methotrexate increases NSAID-induced intestinal damage, but reduces NSAID-induced BT to the liver, spleen, kidney and heart in experimental animals.
Administration, Oral* ; Animals ; Anti-Inflammatory Agents ; Anti-Inflammatory Agents, Non-Steroidal ; Bacterial Translocation* ; Diclofenac* ; Heart ; Kidney ; Liver ; Lymph Nodes ; Methotrexate* ; Models, Animal* ; Rats* ; Spleen

This study investigated the toxicity of commercial non-steroid anti-inflammatory drug (NSAID) eye solutions against corneal epithelial cells in vitro. The biologic effects of 1/100-, 1/50-, and 1/10-diluted bromfenac sodium, pranoprofen, diclofenac sodium, and the fluorometholone on corneal epithelial cells were evaluated after 1-, 4-, 12-, and 24-hr of exposure compared to corneal epithelial cell treated with balanced salt solution as control. Cellular metabolic activity, cellular damage, and morphology were assessed. Corneal epithelial cell migration was quantified by the scratch-wound assay. Compared to bromfenac and pranoprofen, the cellular metabolic activity of diclofenac and fluorometholone significantly decreased after 12-hr exposure, which was maintained for 24-hr compared to control. Especially, at 1/10-diluted eye solution for 24-hr exposure, the LDH titers of fluorometholone and diclofenac sodium markedly increased more than those of bromfenac and pranoprofen. In diclofenac sodium, the Na+ concentration was lower and amount of preservatives was higher than other NSAIDs eye solutions tested. However, the K+ and Cl- concentration, pH, and osmolarity were similar for all NSAIDs eye solutions. Bromfenac and pranoprofen significantly promoted cell migration, and restored wound gap after 48-hr exposure, compared with that of diclofenac or fluorometholone. At 1/50-diluted eye solution for 48-hr exposure, the corneal epithelial cellular morphology of diclofenac and fluorometholone induced more damage than that of bromfenac or pranoprofen. Overall, the corneal epithelial cells in bromfenac and pranoprofen NSAID eye solutions are less damaged compared to those in diclofenac, included fluorometholone as steroid eye solution.
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage/*toxicity ; Benzophenones/administration & dosage/toxicity ; Benzopyrans/administration & dosage/toxicity ; Bromobenzenes/administration & dosage/toxicity ; Cell Movement/drug effects ; Cells, Cultured ; Diclofenac/administration & dosage/toxicity ; Epithelial Cells/drug effects/metabolism/ultrastructure ; Epithelium, Corneal/cytology/*drug effects/metabolism ; Fluorometholone/administration & dosage/toxicity ; Humans ; L-Lactate Dehydrogenase/metabolism ; Microscopy, Electron, Transmission ; Ophthalmic Solutions ; Propionates/administration & dosage/toxicity

AIMTo prepare diclofenac sodium liposomes and observe its ocular pharmacokinetics in rabbits.

METHODSThe diclofenac sodium cationic liposomes were prepared by reverse-phase evaporation methods and the formula of liposome was optimized with uniform design. HPLC method was established and validated for the determination of diclofenac sodium in precornea, cornea and aqueous humor of rabbit eye. Liposome and eyedrop solution 50 microL with total 50 microg diclofenac sodium were instilled to eyes of rabbits, separately. Samples of tear, cornea and aqueous humor were collected at different time intervals after rabbits were sacrificed. The ocular pharmacokinetics was investigated by the concentration-time data of tear, cornea and aqueous humor.

RESULTSThe mean particle size of the diclofenac sodium liposomes was 226.5 nm with zeta potential of + 18. 1 mV. The entrapment efficiency reached 63%. Compared with solution, liposome was characterized by slower clearance in precornea. The concentration of diclotenac in cornea and aqueous humor instilled with liposome were higher than that with eye-drop solution. Cmax of diclofenac sodium in aqueous humor instilled with liposome and eye-drop solution were (0.69 +/- 0.25) and (0.48 +/- 0.19) microg x mL(-1) and (36.68 +/- 11.7) and (21.82 +/- 8.6) microg x g(-1) in cornea, respectively. But no significant difference were found to Tmax in aqueous humor and cornea between liposome and eyedrop, T(1/2) of diclofenac in aqueous humor and cornea with liposoine were longer than that with eye-drop solution. The ocular bioavailability of liposome in aqueous humor was 211% compared with that of eyedrop.

CONCLUSIONDiclofenac sodium cationic liposomes can increase the corneal contact time, enhance the corneal permeability of diclofenac sodium and improve its ocular bioavailability.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; chemistry ; pharmacokinetics ; Aqueous Humor ; metabolism ; Area Under Curve ; Biological Availability ; Chromatography, High Pressure Liquid ; Cornea ; metabolism ; Diclofenac ; administration & dosage ; chemistry ; pharmacokinetics ; Drug Compounding ; Liposomes ; Microscopy, Electron, Transmission ; Particle Size ; Rabbits ; Random Allocation