ABSTRACT
Buccal tablets
Diclofenac sodium
Drug release
Mucoadhesion
Mucoadhesive tablets
Release kinetics
ABSTRACT
Abstract Excessive intake of non-steroidal anti-inflammatory drugs such as, diclofenac sodium (DS) may lead to toxicity in the rats. In this work, we aimed to examine the protective impact of lentil extract (LE) and folic acid (FA) on the hematological markers, the kidney tissue oxidative stress and the renal function against diclofenac sodium (DS) in male albino rats. The rats (120-150 g) were divided into four equal groups randomly, the first group kept as the untreated control. The second group was administrated with DS (11.6 mg/kg b.wt. orally once/day). The third group was received DS+FA (11.6 mg/kg b.wt.+76.9 microgram/kg b.wt.) orally once/day. The fourth group was treated with DS+LE (11.6 mg/kg b.wt.+500 mg/kg b.wt.) orally once/day. After four weeks, the results revealed that DS produced a significant decrease in the values of red blood cells (RBCs), hemoglobin concentration (Hb), hematocrit (HCT) and white blood cells (WBCs). On the other hand, there was a significant increase in the platelets count. Also, DS induced a renal deterioration; this was evidenced by the significant increase in the serum levels of urea, creatinine, uric acid, Na, Ca, Mg as well as the nitric oxide (NO) level in the kidney tissue. Also, there were a significant reduction in the serum levels of potassium (K) and reduced glutathione (GSH) in the kidney homogenates. Moreover, the findings in the rats treated by DS+LE or DS+FA showed a potential protection on the hematological markers, oxidative stress in the kidney tissue and the renal function disturbed by DS. LE and FA could play a potent role for the prevention the adverse hematological, the kidney tissue oxidative stress and the renal dysfunction caused by DS via their anti-oxidative and bioactive phytochemicals.
Resumo A ingestão excessiva de anti-inflamatórios não esteroidais, como o diclofenaco de sódio (DS), pode causar toxicidade em ratos. Neste trabalho, objetivamos examinar o impacto protetor do extrato de lentilha (LE) e ácido fólico (AF) em marcadores hematológicos, no estresse oxidativo do tecido renal e na função renal contra o diclofenaco de sódio (DS) em ratos albinos machos. Os ratos (120-150 g) foram divididos em quatro grupos iguais aleatoriamente, sendo o primeiro grupo mantido como controle não tratado. O segundo grupo foi administrado com DS (11,6 mg / kg de peso corporal por via oral uma vez / dia). O terceiro grupo recebeu DS + FA (76,9 mg / kg de peso corporal por via oral uma vez / dia). O quarto grupo foi tratado com DS + LE (500 mg / kg de peso corporal por via oral uma vez / dia). Após quatro semanas, os resultados revelaram que o DS produziu uma diminuição significativa nos valores de glóbulos vermelhos (RBCs), concentração de hemoglobina (Hb), hematócrito (HCT) e glóbulos brancos (WBCs). Por outro lado, houve um aumento significativo na contagem de plaquetas. Além disso, o DS induziu uma deterioração renal; isso foi evidenciado pelo aumento significativo dos níveis séricos de ureia, creatinina, ácido úrico, Na, Ca, Mg e também do nível de óxido nítrico no tecido renal. Além disso, houve uma redução significativa nos níveis séricos de potássio (K) e glutationa reduzida (GSH) nos homogenatos renais. Além disso, os achados nos ratos tratados com DS + LE ou DS + FA mostraram uma proteção potencial sobre os marcadores hematológicos, estresse oxidativo no tecido renal e função renal perturbada pelo DS. LE e AF podem desempenhar um papel potente na prevenção do estresse hematológico adverso, do estresse oxidativo do tecido renal e da disfunção renal causada pelo DS por meio de seus fitoquímicos antioxidantes e bioativos.
Subject(s)
Animals , Rats , Diclofenac/toxicity , Lens Plant , Plant Extracts/pharmacology , Oxidative Stress , Folic Acid , AntioxidantsABSTRACT
Objective:To evaluate the analgesic effect and adverse reactions of butorphanol after stopping patient controlled intravenous analgesia (PCIA) pump in cesarean section.Methods:One hundred and twenty patients with cesarean section in Tongji Hospital Affiliated to Tongji Medical College, Huazhong University of Science and Technology from March 20, 2021 to December 8, 2021 were divided into three groups as follows: butorphanol group, diclofenac sodium suppository group and control group and there were 40 patients in each group. The vital signs, analgesic effect and adverse reactions among the three groups were compared. Meantime, the bladder and gastrointestinal function recovery and neonatal jaundice in three groups were also compared.Results:The visual analogue score (VAS) in butorphanol group was significantly lower than that of control group at 3 and 4 h after stopping PCIA pump: (2.16 ± 0.09) scores vs. (2.72 ± 0.25) scores, (2.21 ± 0.10) scores vs. (2.72 ± 0.21) scores, P< 0.05, but there was no significant difference in VAS at 6 and 12 h after stopping PCIA pump. VAS in diclofenac sodium suppository group was significantly lower than that of control group at 3 h after stopping PCIA pump: (2.06 ± 0.10) scores vs. (2.16 ± 0.09) scores, P<0.05, but there was no significant difference in VAS at 4, 6 and 12 h ( P>0.05). The 3 h VAS of butorphanol group was lower than that of diclofenac sodium suppository group, but the difference was not statistically significant ( P>0.05). The VAS of butorphanol group was lower than that of diclofenac sodium suppository group at 4 h after operation: (2.21 ± 0.10) scores vs. (2.56 ± 0.12) scores, and the difference was statistically significant ( P<0.05). The first time of getting out of bed and urination time in butorphanol group were later than diclofenac sodium suppository group and control group: (28.32 ± 1.36) h vs. (25.94 ± 0.92) h and (24.50 ± 0.64) h, (29.05 ± 1.67) h vs. (26.76 ± 1.05) h and (25.06 ± 0.65) h, and the difference was statistically significant ( P<0.05). While the anal exhaust time in diclofenac sodium suppository group was delayed, but the difference was not statistically significant ( P>0.05). Conclusions:The analgesic effect of butorphanol is better than diclofenac sodium suppository after stopping PCIA pump in cesarean section, but nursing care should be strengthened to urge patients to take early activities to reduce the occurrence of urinary retention.
ABSTRACT
Excessive intake of non-steroidal anti-inflammatory drugs such as, diclofenac sodium (DS) may lead to toxicity in the rats. In this work, we aimed to examine the protective impact of lentil extract (LE) and folic acid (FA) on the hematological markers, the kidney tissue oxidative stress and the renal function against diclofenac sodium (DS) in male albino rats. The rats (120-150 g) were divided into four equal groups randomly, the first group kept as the untreated control. The second group was administrated with DS (11.6 mg/kg b.wt. orally once/day). The third group was received DS+FA (11.6 mg/kg b.wt.+76.9 microgram/kg b.wt.) orally once/day. The fourth group was treated with DS+LE (11.6 mg/kg b.wt.+500 mg/kg b.wt.) orally once/day. After four weeks, the results revealed that DS produced a significant decrease in the values of red blood cells (RBCs), hemoglobin concentration (Hb), hematocrit (HCT) and white blood cells (WBCs). On the other hand, there was a significant increase in the platelets count. Also, DS induced a renal deterioration; this was evidenced by the significant increase in the serum levels of urea, creatinine, uric acid, Na, Ca, Mg as well as the nitric oxide (NO) level in the kidney tissue. Also, there were a significant reduction in the serum levels of potassium (K) and reduced glutathione (GSH) in the kidney homogenates. Moreover, the findings in the rats treated by DS+LE or DS+FA showed a potential protection on the hematological markers, oxidative stress in the kidney tissue and the renal function disturbed by DS. LE and FA could play a potent role for the prevention the adverse hematological, the kidney tissue oxidative stress and the renal dysfunction caused by DS via their anti-oxidative and bioactive phytochemicals.
A ingestão excessiva de anti-inflamatórios não esteroidais, como o diclofenaco de sódio (DS), pode causar toxicidade em ratos. Neste trabalho, objetivamos examinar o impacto protetor do extrato de lentilha (LE) e ácido fólico (AF) em marcadores hematológicos, no estresse oxidativo do tecido renal e na função renal contra o diclofenaco de sódio (DS) em ratos albinos machos. Os ratos (120-150 g) foram divididos em quatro grupos iguais aleatoriamente, sendo o primeiro grupo mantido como controle não tratado. O segundo grupo foi administrado com DS (11,6 mg / kg de peso corporal por via oral uma vez / dia). O terceiro grupo recebeu DS + FA (76,9 mg / kg de peso corporal por via oral uma vez / dia). O quarto grupo foi tratado com DS + LE (500 mg / kg de peso corporal por via oral uma vez / dia). Após quatro semanas, os resultados revelaram que o DS produziu uma diminuição significativa nos valores de glóbulos vermelhos (RBCs), concentração de hemoglobina (Hb), hematócrito (HCT) e glóbulos brancos (WBCs). Por outro lado, houve um aumento significativo na contagem de plaquetas. Além disso, o DS induziu uma deterioração renal; isso foi evidenciado pelo aumento significativo dos níveis séricos de ureia, creatinina, ácido úrico, Na, Ca, Mg e também do nível de óxido nítrico no tecido renal. Além disso, houve uma redução significativa nos níveis séricos de potássio (K) e glutationa reduzida (GSH) nos homogenatos renais. Além disso, os achados nos ratos tratados com DS + LE ou DS + FA mostraram uma proteção potencial sobre os marcadores hematológicos, estresse oxidativo no tecido renal e função renal perturbada pelo DS. LE e AF podem desempenhar um papel potente na prevenção do estresse hematológico adverso, do estresse oxidativo do tecido renal e da disfunção renal causada pelo DS por meio de seus fitoquímicos antioxidantes e bioativos.
Subject(s)
Male , Animals , Rats , Diclofenac/toxicity , Oxidative Stress , Lens Plant , Kidney/drug effects , Hematologic Tests , Folic Acid/pharmacologyABSTRACT
Abstract Excessive intake of non-steroidal anti-inflammatory drugs such as, diclofenac sodium (DS) may lead to toxicity in the rats. In this work, we aimed to examine the protective impact of lentil extract (LE) and folic acid (FA) on the hematological markers, the kidney tissue oxidative stress and the renal function against diclofenac sodium (DS) in male albino rats. The rats (120-150 g) were divided into four equal groups randomly, the first group kept as the untreated control. The second group was administrated with DS (11.6 mg/kg b.wt. orally once/day). The third group was received DS+FA (11.6 mg/kg b.wt.+76.9 microgram/kg b.wt.) orally once/day. The fourth group was treated with DS+LE (11.6 mg/kg b.wt.+500 mg/kg b.wt.) orally once/day. After four weeks, the results revealed that DS produced a significant decrease in the values of red blood cells (RBCs), hemoglobin concentration (Hb), hematocrit (HCT) and white blood cells (WBCs). On the other hand, there was a significant increase in the platelets count. Also, DS induced a renal deterioration; this was evidenced by the significant increase in the serum levels of urea, creatinine, uric acid, Na, Ca, Mg as well as the nitric oxide (NO) level in the kidney tissue. Also, there were a significant reduction in the serum levels of potassium (K) and reduced glutathione (GSH) in the kidney homogenates. Moreover, the findings in the rats treated by DS+LE or DS+FA showed a potential protection on the hematological markers, oxidative stress in the kidney tissue and the renal function disturbed by DS. LE and FA could play a potent role for the prevention the adverse hematological, the kidney tissue oxidative stress and the renal dysfunction caused by DS via their anti-oxidative and bioactive phytochemicals.
Resumo A ingestão excessiva de anti-inflamatórios não esteroidais, como o diclofenaco de sódio (DS), pode causar toxicidade em ratos. Neste trabalho, objetivamos examinar o impacto protetor do extrato de lentilha (LE) e ácido fólico (AF) em marcadores hematológicos, no estresse oxidativo do tecido renal e na função renal contra o diclofenaco de sódio (DS) em ratos albinos machos. Os ratos (120-150 g) foram divididos em quatro grupos iguais aleatoriamente, sendo o primeiro grupo mantido como controle não tratado. O segundo grupo foi administrado com DS (11,6 mg / kg de peso corporal por via oral uma vez / dia). O terceiro grupo recebeu DS + FA (76,9 mg / kg de peso corporal por via oral uma vez / dia). O quarto grupo foi tratado com DS + LE (500 mg / kg de peso corporal por via oral uma vez / dia). Após quatro semanas, os resultados revelaram que o DS produziu uma diminuição significativa nos valores de glóbulos vermelhos (RBCs), concentração de hemoglobina (Hb), hematócrito (HCT) e glóbulos brancos (WBCs). Por outro lado, houve um aumento significativo na contagem de plaquetas. Além disso, o DS induziu uma deterioração renal; isso foi evidenciado pelo aumento significativo dos níveis séricos de ureia, creatinina, ácido úrico, Na, Ca, Mg e também do nível de óxido nítrico no tecido renal. Além disso, houve uma redução significativa nos níveis séricos de potássio (K) e glutationa reduzida (GSH) nos homogenatos renais. Além disso, os achados nos ratos tratados com DS + LE ou DS + FA mostraram uma proteção potencial sobre os marcadores hematológicos, estresse oxidativo no tecido renal e função renal perturbada pelo DS. LE e AF podem desempenhar um papel potente na prevenção do estresse hematológico adverso, do estresse oxidativo do tecido renal e da disfunção renal causada pelo DS por meio de seus fitoquímicos antioxidantes e bioativos.
ABSTRACT
OBJECTIVE@#To observe the immediate analgesic effect of electroacupuncture (EA) combined with diclofenac sodium on acute gouty arthritis (AGA).@*METHODS@#A total of 90 patients with AGA were randomly divided into a low-dose medication (LM) group (30 cases, 1 case was eliminated, 1 case dropped off), a conventional medication (CM) group (30 cases, 1 case dropped off) and a combination of acupuncture and medication (AM) group (30 cases ). The LM group was given oral administration of 50 mg diclofenac sodium sustained-release capsule; the CM group was given oral administration of 100 mg diclofenac sodium sustained-release capsule; on the basis of the treatment of LM group, the AM group was treated with electroacupuncture at ashi points, Dadu (SP 2), Taichong (LR 3), Taibai (SP 3), Neiting (ST 44), Sanyinjiao (SP 6), Zusanli (ST 36) and Yinlingquan (SP 9) on the affected side, and Taichong (LR 3) and Zusanli (ST 36), Sanyinjiao (SP 6) and Yinlingquan (SP 9) were connected to electroacupuncture respectively, continuous wave, 2 Hz in frequency. The visual analogue scale (VAS) scores of pain before treatment and after 10 min, 2 h, 4 h and 6 h of treatment completion, joint tenderness and swelling scores before treatment and after 10 min and 6 h of treatment completion were compared, and the rate of diclofenac sodium addition within 24 h after treatment completion was recorded among the three groups.@*RESULTS@#After 10 min of treatment completion, the scores of VAS, joint tenderness and joint swelling in the AM group were lower than those before treatment (P<0.05), and the VAS score in the AM group was lower than that in the other two groups (P<0.05). After 2, 4 and 6 h of treatment completion, the VAS scores of the three groups were lower than those before treatment (P<0.05), and the scores in the AM group were lower than those in the LM group (P<0.05). After 6 h of treatment completion, the joint tenderness scores of the three groups and the joint swelling scores of the AM group and the CM group were lower than those before treatment (P<0.05), and the joint tenderness and swelling scores of the AM group were lower than those of the LM group (P<0.05). The rate of diclofenac sodium addition was 3.3 % (1/30) and 3.4 % (1/29) in the AM group and the CM group, respectively, which were lower than 17.9% (5/28) in the LM group (P<0.05).@*CONCLUSION@#Electroacupuncture combined with diclofenac sodium have a good immediate analgesic effect in the treatment of AGA, and have the advantages of small dosage of analgesic drugs and less adverse reactions.
Subject(s)
Humans , Diclofenac , Electroacupuncture , Arthritis, Gouty/drug therapy , Delayed-Action Preparations , Acupuncture Therapy , ArthralgiaABSTRACT
Abstract The aim of this study was to investigate the physicochemical and biological properties of an experimental tricalcium silicate-based repair cement containing diclofenac sodium (CERD). For the physicochemical test, MTA, Biodentine and CERD were mixed and cement disc were prepared to evaluate the setting time and radiopacity. Root-end cavity were performed in acrylic teeth and filled with cements to analyze the solubility up to 7 days. Polyethylene tubes containing cements were prepared and calcium ions and pH were measured at 3h, 24h, 72h and 15 days. For the biological test, SAOS-2 were cultivated, exposed to cements extracts and cell proliferation were investigated by MTT assay at 6h, 24h and 48h. Polyethylene tubes containing cements were implanted into Wistar rats. After 7 and 30 days, the tubes were removed and processed for histological analyses. Parametric and nonparametric data were performed. No difference was identified in relation to setting time, radiopacity and solubility. Biodentine released more calcium ion than MTA and CERD; however, no difference between MTA and CERD were detected. Alkaline pH was observed for all cements and Biodentine exhibited highest pH. All cements promoted a raise on cell proliferation at 24h and 48h, except CERD at 48h. Biodentine stimulated cell metabolism in relation to MTA and CERD while CERD was more cytotoxic than MTA at 48h. Besides, no difference on both inflammatory response and mineralization ability for all cement were found. CERD demonstrated similar proprieties to others endodontic cements available.
Resumo O objetivo deste estudo foi investigar as propriedades físico-químicas e biológicas de um cimento reparador experimental à base de silicato de tricálcio contendo diclofenaco de sódio (CERD). Para o teste físico-químico, MTA, Biodentine e CERD foram manipulados e discos de cimentos foram preparados para avaliar o tempo de presa e a radiopacidade. Retrocavidades foram feitas em dentes de acrílico e preenchidas com cimentos para análise de solubilidade por 7 dias. Tubos de polietileno contendo cimentos foram preparados e os íons cálcio e o pH foram mensurados às 3h, 24h, 72h e 15 dias. Para o teste biológico, SAOS-2 foram cultivadas, expostas aos extratos de cimentos e a proliferação celular foi investigada pelo ensaio de MTT às 6h, 24h e 48h. Tubos de polietileno contendo cimentos foram implantados em ratos Wistar. Após 7 e 30 dias, os tubos foram removidos e processados para análises histológicas. Dados paramétricos e não paramétricos foram realizados. Nenhuma diferença foi identificada em relação ao tempo de presa, radiopacidade e solubilidade. Biodentine liberou mais íons de cálcio do que MTA e CERD; no entanto, nenhuma diferença entre MTA e CERD foi detectada. O pH alcalino foi observado para todos os cimentos e o Biodentine exibiu o pH mais alto. Todos os cimentos promoveram aumento na proliferação celular às 24h e 48h, exceto o CERD às 48h. Biodentine estimulou o metabolismo celular em relação ao MTA e CERD, enquanto CERD foi mais citotóxico do que MTA em 48h. Além disso, nenhuma diferença foi encontrada na resposta inflamatória e na capacidade de mineralização para todos os cimentos. CERD demonstrou propriedades semelhantes a outros cimentos endodônticos disponíveis.
ABSTRACT
Objective:To investigate the application of cromolyn sodium combined with diclofenac sodium eye drops in allergic conjunctivitis (AC) and its effect on tear film function, interleukin-10 (IL-10), interleukin-17 (IL-17) and immunoglobulin E(IgE).Methods:From April 2018 to May 2020, 78 patients with AC collected in Liaoning Armed Police Crops Hospital were divided into control group and observation group according to the random number table method (39 cases in each group). The control group was given cromolyn sodium eye drops, and the observation group was given cromolyn sodium combined with diclofenac sodium eye drops. The efficacy, clinical symptoms, changes of signs, tear film function [tear film rupture time (BUT), Schirmer I test (SIt)], tear inflammation indicators [interleukin-4 (IL-4), tumor necrosis factor-α (TNF-α), IL-10, IL-17], tear allergy mediators [eosinophil cationic protein (ECP), hyaluronic acid (HA), IgE] and safety.Results:The total effective rate of observation group was 100.00%, which was higher than that of control group (84.62%), with statistically significant difference ( P<0.05). After treatment, the scores of eye itching, tearing, photophobia, eye secretion, conjunctival hyperemia, conjunctival edema and blepharoconjunctival papillary follicular hyperplasia in the two groups were significantly lower than those before treatment, and the observation group was lower than the control group, with statistically significant difference (all P<0.05). The BUT in the observation group was higher than that in the control group after treatment, with statistically significant difference ( P<0.05). After treatment, the tear levels of IL-4, TNF-α, IL-10 and IL-17 in the observation group were lower than those in the control group, with statistically significant difference (all P<0.05). After treatment, the tear ECP, HA and IgE level in the observation group were lower than those in the control group, with statistically significant difference (all P<0.05). There was no significant difference in the incidence of adverse reactions between the two groups ( P>0.05). Conclusions:Cromolyn sodium combined with diclofenac sodium eye drops is effective in the treatment of AC, which can effectively improve the clinical symptoms and signs, promote stable tear film function, alleviate local metamorphosis and inflammation, and has good safety.
ABSTRACT
Abstract Design of experiment (DoE) is a useful time and cost-effective tool for analyzing the effect of independent variables on the formulation characteristics. The aim of this study is to evaluate the effect of the process variables on the characteristics involved in the preparation of Diclofenac Sodium (DC) loaded ethylcellulose (EC) nanoparticles (NP) using Central Composite Design (CCD). NP were prepared by W/O/W emulsion solvent evaporation method. Three factors were investigated (DC/EC mass ratio, PVA concentration, homogenization speed) in order to optimize the entrapment efficiency (EE) and the particle size of NP. The optimal formulation was characterized by Fourier Transform Infrared (FTIR), Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and in vitro release. Optimized formulation showed an EE of 49.09 % and an average particle size of 226.83 nm with a polydispersity index of 0.271. No drug-polymer interaction was observed in FTIR and DSC analysis. SEM images showed that the particles are spherical and uniform. The in vitro release study showed a sustained release nature, 53.98 % of the encapsulated drug has been released over 24hours period. This study demonstrated that statistical experimental design methodology can optimize the formulation and the process variables to achieve favorable responses.
Subject(s)
Pharmaceutical Preparations , Diclofenac/analysis , Process Optimization , Nanoparticles/analysis , In Vitro Techniques/instrumentation , Calorimetry, Differential Scanning/instrumentation , Microscopy, Electron, Scanning/methods , Spectroscopy, Fourier Transform Infrared , Costs and Cost Analysis/methods , Methodology as a Subject , Fourier AnalysisABSTRACT
@#AIM: To evaluate the clinical effects and safety of Loratadine combined with Diclofenac sodium eye drops in the treatment of allergic conjunctivitis by system review.METHODS:Using “Loratadine” “Diclofenac sodium” and “allergic conjunctivitis” as keywords, a randomized controlled trial of Loratadine combined with diclofenac sodium in the treatment of allergic conjunctivitis was searched in Embase, Cochrane library, Pubmed, CNKI, Wanfang database, VIP and SionMed. The retrieval time is from the establishment of the database to July 2021. The risk bias tool provided by the Cochrane cooperation scale was used to assess the risk bias of included studies of RCTs. The publication bias of the included studies was assessed by the Egger's test. Meta-analysis of clinical efficiency, incidence of adverse effects, ocular itch score, and discharge score were using RevMan 5.3. Descriptive analysis were performed on the results with high heterogeneity.RESULTS:A total of 19 articles were included, all of which were Chinese literatures, including 1 931 patients(2 044 eyes). The control group was treated with Loratadine, and the experimental group was treated with Loratadine combined with Diclofenac sodium eye drops. The Meta-analysis showed that the clinical effect of experimental group was better than control group(<i>OR</i>=4.43, 95%<i>CI</i>:3.26-6.03,<i>P</i><0.00001).The incidence of adverse reaction was lower than control group(<i>OR</i>=0.32, 95%<i>CI</i>:0.2-0.52,<i>P</i><0.00001). The Score of ocular itching(<i>MD</i>=-0.36, 95%<i>CI</i>:-0.39 to -0.33,<i>P</i><0.00001)and discharge(<i>MD</i>=-0.24,95%<i>CI</i>: -0.31 to -0.18,<i>P</i><0.00001)in experimental group was lower than control group. All the studies on hyperemia and edema of conjunctiva, conjunctival papilla or follicle proliferation and foreign body sensation in patients with allergic conjunctivitis showed that the experimental group could significantly reduce the above symptoms(all <i>P</i><0.05). Egger's test was performed on the total effective rate, the incidence of adverse reaction. The results showed that there was publication bias in the total effective. Trim and fill method showed that the publication bias did not affect the results.CONCLUSION: On the basis of the oral Loratadine, combined with Diclofenac sodium eye drops has a certain clinical efficacy in the treatment of allergic conjunctivitis, which can improve the clinical symptoms such as ocular itching, foreign body sensation, hyperemia and edema of conjunctiva, and the incidence of adverse reactions is low, which can provide evidence-based basis for the drug treatment of allergic conjunctivitis in the future. However, due to the low intensity of the included research evidence, more multicenter, randomized double-blind clinical trials are needed in the future, so that to improve the evidence intensity.
ABSTRACT
Objective:To explore the therapeutic role of morin against L-arginine-induced acute pancreatitis in rats. Methods:The group 1 received two intraperitoneal injections of normal saline, and groups 2-4 were given two intraperitoneal injections of L-arginine (250 mg/100 g body weight) at 1 h interval to induce acute pancreatitis. Subsequently, group 2 received no further treatment while groups 3 and 4 were treated with morin (30 mg/kg) and diclofenac sodium (30 mg/kg), respectively. Blood glucose and serum levels of insulin, α-amylase, malondialdehyde, myeloperoxidase, alanine aminotransferase, aspartate aminotransferase and cholesterol were measured. Moreover, histopathological study was carried out to investigate the effect of morin treatment on physiology of the pancreas. Results:L-arginine significantly altered the level of blood glucose and serum levels of insulin, α-amylase, malondialdehyde, myeloperoxidase, alanine aminotransferase, aspartate aminotransferase and cholesterol. Treatment with morin or diclofenac sodium significantly improved the levels of these biomarkers. Furthermore, morin showed more significant effect than diclofenac sodium. Histopathological analysis verified that morin protected the pancreas from deleterious effects of L-arginine. Conclusions:Morin plays a protective role against L-arginine-induced acute pancreatitis via reducing lipid peroxidation and tissue inflammation, and attenuating acute pancreatitis-associated alteration in insulin secretion and glucose metabolism.
ABSTRACT
@#AIM: To analyze the therapeutic effect of loratadine combined with diclofenac sodium eye drops in the treatment of allergic conjunctivitis, and the influence on tear film stability and tear-related indexes.<p>METHODS: A prospective study was conducted among 93 patients(186 eyes)with allergic conjunctivitis admitted to the hospital between January 2019 and January 2020. They were randomly divided into observation group(<i>n</i>=47, 94 eyes, treated with loratadine and diclofenac sodium eye drops)and control group(<i>n</i>=46, 48 eyes, treated with loratadine). All patients received 2wk of treatment. The improvement of ocular symptoms and signs after treatment was evaluated. Schirmer I test(SⅠt)and break up time(BUT)were used to evaluate the tear film stability. The height, depth and cross-sectional area of lacrimal rivus were measured by anterior segment related optical coherence tomography. Tear specimens were collected to detect changes in tear hyaluronic acid(HA), group ⅡA secretory phospholipase A2(sPLA2-Ⅱa and eosinophil cationic protein(ECP). The occurrence of adverse reactions was counted.<p>RESULTS: After 2wk of treatment, the scores of main symptoms and signs were reduced in the two groups(<i>P</i><0.05), and the observation group had lower scores than the control group(<i>P</i><0.05). SⅠt and BUT were increased in the two groups(<i>P</i><0.05), which were longer in the observation group than in the control group(<i>P</i><0.05). The height of lacrimal rivus increased, depth increased, and cross-sectional area were increased in the two groups(<i>P</i><0.05). Besides, the above indexes in observation group were higher than those in the control group(<i>P</i><0.05). Meanwhile, HA, ECP and sPLA2-Ⅱa were decreased in the two groups(<i>P</i><0.05), which were lower in the observation group than in the control group(<i>P</i><0.05). No significant differences were found between the 2 groups in the incidence of adverse reactions(12.8% <i>vs</i> 10.9%, <i>P</i>>0.05).<p>CONCLUSION: The overall effect of loratadine combined with diclofenac sodium eye drops is better than that of loratadine alone in the treatment of allergic conjunctivitis. The combined treatment can improve symptoms, signs and tear film stability, reduce inflammatory mediators in tears, and promote recovery of tear film function. Besides, it is safe and feasible.
ABSTRACT
Psoriatic arthritis (PsA) is a complicated psoriasis comorbidity with manifestations of psoriatic skin and arthritic joints, and tailoring specific treatment strategies for simultaneously delivering different drugs to different action sites in PsA remains challenging. We developed a need-based layered dissolving microneedle (MN) system loading immunosuppressant tacrolimus (TAC) and anti-inflammatory diclofenac (DIC) in different layers of MNs,
ABSTRACT
Objective: To investigate the analgesic activity of methanolic extract of Entada phaseoloides (MEEP) along with its molecular mechanistic pathway. Methods: Swiss albino female mice and Wistar rats of either sex were administered orally with MEEP extracts (100, 200 and 400 mg/kg) and pentazocine, tramadol and diclofenac sodium, as standard drugs. Following administration, anti-nociceptive activity was evaluated using an acetic acid-induced writhing test, Eddy’s hot plate, and hot water immersion test. Serum was collected for molecular expression of various proteins and genes using Reverse Transcriptase PCR and Western Blotting. Results: Acetic acid writhing test, a frequently used method to assess peripheral analgesic activity, revealed that MEEP reduced peripherally induced pain in a dose-dependent manner. Likewise, Eddy’s hot plate and hot water immersion methods, often implicated for testing central analgesic activities, showed that MEEP is bestowed with the capability to counteract analgesia in a dose and time-dependent manner. Pro-inflammatory cytokines and factors like COX-2, IL-6, TNF-α, and NF-κB that cause inflammatory responses and pain were significantly reduced, suggesting its analgesic and anti-inflammatory potential. This analgesic and the anti-inflammatory role played by MEEP is also supported by the up-regulation of anti-inflammatory cytokine IL-10 and COMT and COX-1 enzyme demonstrated no significant difference between the groups. Conclusion: The study revealed the weak peripheral and potent central analgesic property MEEP by modulating pro-inflammatory and anti-inflammatory pathways.
ABSTRACT
OBJECTIVE: To evaluate the bacteriostatic efficacy of diclofenac sodium eye drops and to explore the reasonable dose of benzalkonium chloride, ethylparaben and thimerosal in diclofenac sodium eye drops. METHODS: According to the method of bacteriostatis effect test in 2015 edition of Chinese Pharmacopoeia (Ch.P),and Escherichia coli, Staphylococcus aureus, Pesudomonas aeruginosa, Candida albicans and Aspergillus niger as test strains,the bacteriostatis effect of diclofenac sodium eye drops from 10 batches of the samples was determined. Also, the concentration gradient of benzalkonium chloride, ethylparaben and thimerosal in diclofenac sodium eye drops was designed to investigate the optimum bacteriostatic concentration. RESULTS: The samples from 3 manufacturers could reach level B, no sample could reach level A,and those from 7 manufacturers did not comply with the specification. When the concentration of thimerosal was 0.01 mg•mL-1 and the concentration of ethylparaben was 0.3 mg•mL-1 in diclofenac sodium eye drops, the bacteriostatic efficacy could reach level B. When the concentration of benzalkonium chloride was 0.01 mg•mL-1, the bacteriostatic efficacy could reach level A. CONCLUSION: The bacteriostatis effect of diclofenac sodium eye drops from 10 batches of the samples is not good, It is recommended that these manufacturers should optimize the type and concentration of antimicrobial agents and optimize their formulation based on both biological tests and physical-chemical tests to ensure drug safety.
ABSTRACT
Objective • To investigate the safety and efficacy of focused low-intensity pulsed ultrasound (FLIPUS) therapy on the patients with knee osteoarthritis (KOA). Methods • A total of 100 subjects with KOA from August 2018 to August 2019 in the Department of Rehabilitation Medicine at the Second Affiliated Hospital of Chongqing Medical University were sequentially randomized into group A and group B. Among them, FLIPUS was adopted to treat the 50 patients in group A, and the diclofenac sodium was adopted to treat the other 50 patients in group B. Visual analogue scale (VAS), Western Ontario McMaster Universities Osteoarthritis Index (WOMAC) and Lequesne index (LI) were used to evaluate knee joint pain, the structure and function of the affected knee joint, and the severity of the affected knee joint at baseline, on day 3, day 6 and day 10 after treatment respectively. The knee range of motion (KROM) and maximum walking speed (MWS) were used to evaluate the knee joint movement and walking function at baseline and on day 10 after treatment respectively. Results • There were on significant differences between two groups with respect to KOA evaluation indexes (P>0.05). Compared with those in group B, patients in group A showed significant improvements in VAS and WOMAC scores on day 6 and day 10 after treatment (P=0.021, P=0.000; P=0.005, P=0.001). Meanwhile, patients in group A had higher LI scores than those in group B on day 10 after treatment (P=0.000). In addition, patients in group A showed significant improvements in MWS (P=0.006) and non-significant improvements in KROM (P=0.064) on day 10 after treatment. Conclusion • FLIPUS is a safe and effective treatment modality for relieving pain and improving the functions of patients with KOA.
ABSTRACT
Diclofenac sodium is a nonsteroidal anti-inflammatory drug often obtainable as a prescription drug or over the counter. It is very effective in the control of inflammation and pain due to arthritis or pains arising following many disease conditions becauseof its antipyretic, anti inflammatory and analgesic potentials. Despite the beneficial effects of diclofenac sodium, it has been implicated in some adverse effects. In this study, we examined the effect of acute and chronic administration of diclofenac sodium on some hematological (PCV, WBC differentials) and coagulation (prothrombin time, activated partial prothrombin time and platelets count) parameters of albino Wister rats using the standard methods. Twenty four Albino Wister rats were divided intothree groups of 8 rats and grouped as control, acute study and chronic study. The rats were administered 0.2 mg of diclofenac sodium for 24 hours for acute and 3 weeks for chronic studies respectively. The rats were sacrificed and blood collected for analysis of PCV, WBC differentials, prothrombin time, activated partial prothrombin time and platelets count using the standard methods. Results show that acute administration of diclofenac sodium at 0.2 mg has no effect on hematological and coagulation parameters, but chronic administration could instigate significant reduction in PCV, platelets count, neutrophils and monocytes (p<0.001), whilethere is a significant increase in PT, INR, lymphocytes (p<0.001). Considering these alterations, it is advisable that this drug should be made a strictly prescription drug in order to prevent indiscriminate use of this medication and to prevent attendant anemia and coagulopathy that may follow chronic use.
ABSTRACT
The toxic effects of different doses of diclofenac sodium (DS) on the kidney on the postnatal period (0-7 days) by morphometrical and immunohistochemical methods were investigated. For this purpose, 15 female adult wistar albino rats were used and divided into 5 main groups. Group Ia served as normal control, physiologic group Ib received normal saline, group II received low dose (3.9 mg/kg), group III received medium dose (9 mg/kg) and group IV received high dose (18 mg/kg). Male offspring's from 0-7 days after birth were used in this study. On the 8th day of postnatal life, all animals were anesthetized. Then, the kidney samples were analyzed. Haematoxylin and eosin staining showed degeneration and necrosis, apparent atrophy of the glomeruli, mononuclear cell infiltration, congested vessels, increased fibrous tissue and distortion of the proximal convoluted tubules with interruption of the brush margin of the DS treated group. Increased level of Caspase-3 and upregulation of TNF-α with different doses of DS. In light of our findings, DS may lead to adverse effects that are dose-dependent in the prenatal subjected kidney to this drug.
Se investigaron los efectos tóxicos de diferentes dosis de diclofenaco sódico (DS) en el riñón de ratas, durante su período postnatal (0-7 días), por métodos morfométricos e inmunohistoquímicos. Para este propósito, se utilizaron 20 crías macho, de ratas Wistar albinas, y se dividieron en 5 grupos principales. El grupo Ia sirvió como control normal, el grupo fisiológico Ib recibió solución salina normal, el grupo II recibió una dosis baja de DS (3,9 mg/kg), el grupo III recibió una dosis media de DS (9 mg/kg) y el grupo IV recibió una dosis alta de DS (18 mg/kg). Se administraron los medicamentos de 0 a 7 días después del nacimiento de las ratas. En el octavo día de vida postnatal, todos los animales fueron sacrificados. Luego, se analizaron las muestras de riñón. Mediante hematoxilina-eosina se evidenció degeneración y necrosis, aparente atrofia de los glomérulos, infiltración de células mononucleares, vasos congestionados, aumento del tejido fibroso y distorsión de los túbulos contorneados proximales, con interrupción del margen en cepillo del grupo tratado con DS. Se detectó un aumento del nivel de caspasa-3 y regulación al alza de TNF-α con diferentes dosis de DS. A la luz de nuestros hallazgos, la DS puede provocar efectos adversos en el riñón, que dependen de la dosis de este medicamento administrada en el período posnatal.
Subject(s)
Animals , Female , Rats , Diclofenac/toxicity , Kidney/drug effects , Staining and Labeling , Immunohistochemistry , Diclofenac/administration & dosage , Rats, Wistar , Apoptosis/drug effects , Kidney/growth & development , Kidney Tubules, Proximal/drug effects , Animals, NewbornABSTRACT
Background: Levocetirizine, the R-enantiomer of Cetirizine has pharmacokinetically and pharmacodynamically favourable characteristics, with rapid onset of action, high bioavailability, high affinity for and occupancy of the H1-receptor, limited distribution, minimal hepatic metabolism together with minimal side effects. Non-steroidal anti-inflammatory drugs (NSAIDs) have been used for many years for analgesic, anti-inflammatory, and more recently in the case of aspirin, antithrombotic purposes. Because of the significant side effect profiles of steroidal and NSAID medications, there is a greater interest in newer compounds such as antihistaminic drugs. This article will consider the potential or otherwise of the reported analgesic and anti-inflammatory effects of levocetirizine to enhance its effectiveness in the treatment of allergic disease with pain.Methods: Albino Wistar rats of either sex weighing 150-250 grams were used. For both Analgesic activity and Anti-inflammatory activity, 4 groups consisting of 6 animals per group were used. Group I: Control: 1% Gum acacia. 2ml/kg, Group II: Standard drug: Diclofenac sodium 4.5mg/kg; Group III: Test Drug 1: Levocetirizine 1mg/kg; Group IV: Test Drugs 2: Levocetirizine 1mg/kg+Diclofenac sodium 4.5mg/kg. Drugs were administered orally. For analgesic activity, Tail clip method and Hot plate method was used. For acute anti-inflammatory activity Carrageenan induced rat paw oedema method was used.Results: Levocetirizine, is found to have significant analgesic activity in rats (1 mg/kg dose) alone and in combination with Diclofenac Sodium in Haffner’s Tail Clip method and Eddy’s Hot Plate Method. Levocetirizine also has got prominent anti-inflammatory activity in acute models evidenced by percentage inhibition of acute rat paw oedema.Conclusions: Levocetirizine possess analgesic and acute anti-inflammatory activity alone and in combination with Diclofenac sodium.
ABSTRACT
Abstract: The study describes method development and subsequent validation of HPTLCmethod for simultaneous estimation of paracetamol (PCM), diclofenac sodium (DCL) anddicyclomine hydrochloride (DICY) in marketed combined tablet dosage form. The drugs wereextracted from marketed tablet dosage form: Spasmodart. The separation was carried out onaluminium sheet precoated with silica gel 60 F254 using toluene: ethylacetate: methanol: formicacid (5.5:3.5:2:0.02, v/v/v/v) as a mobile phase. The spots were scanned densitometrically at266 nm wavelength for paracetamol and diclofenac sodium. The plate was then dipped in panisaldehyde reagent and spots of dicyclomine hydrochloride were scanned at 638 nmwavelength. The Rf values of paracetamol, diclofenac sodium and dicyclomine hydrochloridewere found to be 0.41, 0.71and 0.24 respectively. Calibration curves were linear in range of3250-9750ng/spot, 500-1500ng/spot and 200-600ng/spot for PCM, DCL and DICY respectively.The limit of detection (LOD) for paracetamol, diclofenac sodium and dicyclomine hydrochloridewere found to be 812.5, 125 and 50ng/spot respectively. The suitability of this method forquantitative determination of compounds was proved by validation in accordance with ICHGuidelines. Therefore this method can be applied for routine analysis of these drugs in tabletformulation.