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Background: The World Health Organization (WHO) has released fresh information showing that the number of caesarean sections performed worldwide has increased and now accounts for more than one in five (21%) deliveries. 89.8% of women experienced significant post-operative discomfort following a caesarean section and 84.2% reported to have moderate to severe pain. This study aimed to compare diclofenac, paracetamol infusion, and a combination of both in patients of post-caesarean for pain management.Methods: The study was a cross-sectional study carried out in the department of obstetrics and gynaecology at a tertiary care hospital in a rural area of Panipat, Haryana. A total number of 102 women who underwent caesarean section were taken for the study. They were divided into 3 groups each having 34 women. The first group was given diclofenac, the second was given paracetamol infusion and the third was given a combination of both for pain management.Results: In our study we have done visual analog score (VAS) scoring at 0, 1, 6, 12, 18 and 24 hours and we found that the mean VAS score in group 3 was highest when compared to other two groups. We also found that on comparing data of VAS score between the three groups the p value came out to significant that is p?0.001.Conclusions: We found that combination therapy had good results in comparison to individual therapy and had fewer side effects.
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Films were prepared (viz. CDF1, CDF2, CDF3, CDF4, CDF5) using five parts of 10% w/w of mucilage of gum of Cordia dichotoma with different proportions of plasticizers methyl paraben and glycerine. The films were casted on mercury plate. Films prepared with different proportion of gum and 0.2 % w/v methyl paraben, 2.5% w/v of glycerine showed satisfactory drying after 24 h. They were evaluated for qualitative phytochemical analysis followed by mechanical properties like water uptake, tensile strength, folding endurance, and water vapor transmission rate and stability studies also done for plane film. Further, the gum was evaluated for release parameter with model drug diclofenac sodium (0.5% w/w) with same composition of methyl paraben and glycerine. The study found that the CDF3 film shows the best result among other batches of C. dichotoma.
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Introducción: El uso de fármacos con potencial cardiotóxico para tratar enfermedades no cardiovasculares coexistentes resulta un agravante evitable. Objetivo: Evaluar la prescripción de 5 fármacos cardiotóxicos en pacientes con enfermedades cardiovasculares. Métodos: Se realizó un estudio descriptivo transversal (enmarcado en los estudios de utilización de medicamentos) de marzo a diciembre de 2020 en el Policlínico Santa Cruz (Artemisa, Cuba), en una población de 234 sujetos con enfermedades cardiovasculares que habían sido tratados con domperidona, azitromicina, ciprofloxacina, ibuprofeno y diclofenaco. Las variables estudiadas fueron: sexo, edad, consumo de fármacos cardiotóxicos, motivo de indicación, enfermedades cardiovasculares, forma farmacéutica, dosis diaria, intervalo de las dosis y duración del tratamiento. Se realizó un análisis estadístico descriptivo. Resultados: Los fármacos más prescritos fueron la azitromicina (n= 63), el ibuprofeno (n= 59) y la ciprofloxacina (n= 57). Sus principales motivos de indicación fueron, respectivamente, la neumonía adquirida en la comunidad (38,1 por ciento), las infecciones de piel y tejidos blandos (28,8 por ciento), y las infecciones del tracto urinario (43,8 por ciento). La principal enfermedad cardiovascular fue la hipertensión arterial. Para los 5 fármacos seleccionados se reportó su esquema terapéutico (forma farmacéutica, dosis diaria, intervalo de dosis y duración del tratamiento). Conclusiones: Aunque en todos los casos el motivo de indicación es el adecuado, los fármacos pueden sustituirse por otros de menor riesgo cardiovascular. En su mayoría, los esquemas terapéuticos son correctos, salvo en los casos de la domperidona (duración prolongada) y el diclofenaco (altas dosis)(AU)
Introduction: The use of drugs with cardiotoxic potential to treat coexisting noncardiovascular diseases results in avoidable aggravation. Objective: To assess the prescription of 5 cardiotoxic drugs in patients with cardiovascular disease. Methods: A cross-sectional descriptive study (framed in the studies of drug utilization) was carried out from March to December 2020 in the Policlínico Santa Cruz (Artemisa, Cuba), in a population of 234 subjects with cardiovascular diseases who had been treated with domperidone, azithromycin, ciprofloxacin, ibuprofen and diclofenac. The variables studied were: sex, age, consumption of cardiotoxic drugs, reason for indication, cardiovascular disease, pharmaceutical form, daily dose, dose interval, and duration of treatment. Descriptive statistical analysis was performed. Results: The most prescribed drugs were azithromycin (n= 63), ibuprofen (n= 59) and ciprofloxacin (n= 57). Their main reasons for indication were, respectively, community-acquired pneumonia (38.1 percent), skin and soft tissue infections (28.8 percent), and urinary tract infections (43.8 percent). The main cardiovascular disease was arterial hypertension. For the 5 selected drugs, their therapeutic scheme (pharmaceutical form, daily dose, dose interval and duration of treatment) was reported. Conclusions: Although in all cases the reason for indication was adequate, the drugs can be substituted by others of lower cardiovascular risk. For the most part, the therapeutic regimens are correct, except in the cases of domperidone (prolonged duration) and diclofenac (high doses)(AU)
Sujet(s)
Humains , Ordonnances médicamenteuses , Maladies cardiovasculaires/traitement médicamenteux , Cardiotoxines/toxicité , Pharmacovigilance , Ciprofloxacine/usage thérapeutique , Diclofenac/usage thérapeutique , Ibuprofène/usage thérapeutique , Épidémiologie Descriptive , Études transversales , Azithromycine/usage thérapeutique , Dompéridone/usage thérapeutiqueRÉSUMÉ
Objective: A natural gum from Vateria indica was investigated as a novel matrix-forming material for sustained drug delivery using diclofenac potassium as a model drug.Methods: In the current investigation, we formulated a matrix tablet using chloroform soluble gum portion of Vateria indica modified gum (VIMG) as a natural matrix-forming agent. It was used with a drug-polymer ratio ranging from 1:0.5 to 1:4.5. The pre-compression study of the powder blends was done by calculating bulk density, tapped density, angle of repose, and carr’s index, compressibility, and hausner’s ratio. The tablets were prepared by direct compression method and prepared tablets were evaluated and were found according to the official guidelines by pharmacopeia. The in vitro drug release was carried out using USP paddle type II apparatus and the release was found to be sustained.Results: The formulation VIMG-5 containing drug: polymer ratio 1:2.5 showed the 96.26%±1.73 drug release in 12 h. The results showed that chloroform soluble fraction of Vateria indica can be used as a drug release modifier to delay the rate of drug release, which depended on the amount of gum composition, as the concentration of gum was increased, there was sustained the drug release with promising accelerated stability.Conclusion: The evaluation studies on sustained release matrix tablets using Vateria indica chloroform soluble portion of gum as natural material demonstrate the multivariate applications such as matrix forming, binder, and release retardant of the gum in tablet formulation.
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Diclofenac medication has been extensively used for anti-inflammatory, anti-pyretic, and analgesic actions. Its abiding usage and overdose have induced toxicity and harmful effects on the liver, kidney, and gastrointestinal tract. The research aims to scrutinize the protective effect of Madhuca longifolia seed oil against diclofenac-induced toxicity in female Wistar albino rats. A period of 10 days of study was aimed at 7 groups; Group 1 was assigned as normal control. Group 2 has been administered diclofenac (50 mg/kg b.w. /day, i.p.) only on the last two days of each study period. Group 3 and Group 4 have been pre-treated with 1 mL, and 2 mL of Madhuca longifolia seed oil, respectively, and diclofenac was induced as per Group 2. Group 5 was treated with the standard drug silymarin and diclofenac. Group 6 and Group 7 were given 1 mL and 2 mL of Madhuca longifolia seed oil alone. After the study period, parameters like liver enzyme markers, renal enzyme markers, and antioxidants were measured, and tissue samples were analyzed for histopathological changes. The results proved that pre-treatment of 1 mL of Madhuca longifolia seed oil has efficacy against diclofenac-induced toxicity.
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Diclofenac medication has been extensively used for anti-inflammatory, anti-pyretic, and analgesic actions. Its abiding usage and overdose have induced toxicity and harmful effects on the liver, kidney, and gastrointestinal tract. The research aims to scrutinize the protective effect of Madhuca longifolia seed oil against diclofenac-induced toxicity in female Wistar albino rats. A period of 10 days of study was aimed at 7 groups; Group 1 was assigned as normal control. Group 2 has been administered diclofenac (50 mg/kg b.w. /day, i.p.) only on the last two days of each study period. Group 3 and Group 4 have been pre-treated with 1 mL, and 2 mL of Madhuca longifolia seed oil, respectively, and diclofenac was induced as per Group 2. Group 5 was treated with the standard drug silymarin and diclofenac. Group 6 and Group 7 were given 1 mL and 2 mL of Madhuca longifolia seed oil alone. After the study period, parameters like liver enzyme markers, renal enzyme markers, and antioxidants were measured, and tissue samples were analyzed for histopathological changes. The results proved that pre-treatment of 1 mL of Madhuca longifolia seed oil has efficacy against diclofenac-induced toxicity.
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Background: Osteoarthritis (OA) is a significant contributor to chronic pain, mainly affecting lower extremity joints like the knee and hip, and causing considerable impairment in elderly individuals. OA treatment focuses on easing discomfort and enhancing mobility. Despite their adverse unfavorable effects, non-steroidal anti-inflammatory medications (NSAIDs) are frequently used for symptom alleviation. However, there is still a need for secure and efficient alternative therapies that could provide OA patients with both symptomatic relief and disease-modifying benefits. Despite the indisputable fact that the disease has a substantial socioeconomic impact on patients, there is not much research available to reflect on the medicine prescription pattern in OA. Aim and Objectives: The objectives of this study were to assess the prescription pattern and their rationality in patients with OA in a tertiary care hospital. Materials and Methods: A cross-sectional, prospective, and observational study conducted in the orthopedics department for all newly diagnosed and old treated patients with OA. Around 350 patients were taken into the study and their prescriptions were scrutinized. Descriptive statistics were used to analyze the data and present it as percentages. Results: Over 61.7% of females were affected compared to 38.3% of males with OA. The knee joint (76.2%) followed by the hip joint (13.7%) were the most common joints involved. Aceclofenac and diclofenac were the most common NSAIDs used in the patients, whereas piroxicam was the least prescribed drug. Gastroprotective agents, calcium supplements, and SYSDOA were the commonest adjuvants used in the treatment of OA patients. Conclusions: Even though NSAIDs are favored, SYSDOA and non-pharmacological treatments such as lifestyle changes, and frequent mild exercise have changed the treatment plan for OA
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Background: Inflammation is described as a localized physical condition whereat part of the body becomes swollen, reddened, hot, and consistently painful, largely as a response to injury or infection. Aim and Objectives: The current study is designed to study the Abutilon indicum for its anti-inflammatory activity in albino rats-induced paw edema by carrageenan. Materials and Methods: Randomly 30 albino rats from both sexes were taken and divided into five groups, six in each. Normal saline 25 mL/kg (control), diclofenac 9 mg/kg (standard), and three different doses of plant extract (EEAI) such as 250, 500, and 1000 mg/kg (3 test groups) were given in respective groups, after 1-h injection of 0.1 mL of 0.2% carrageenan solution into the sub plantar region of the right hind paw. At 0 h, after 1, 2, and 3 h, paw edema volume was measured by mercury displacement method using plethysmograph. The percentage of edema inhibition was measured in all five groups. Results: The percentage of edema inhibition for EEAI 500 mg/kg was 6.20%, 17.8%, and 26.72% after 1st, 2nd and 3rd h respectively and for EEAI 1000 mg/kg was 8.26%, 20.7%, 31.61% after 1st, 2nd, and 3rd h, respectively. Significant edema inhibition was observed after 2nd and 3rd h of drug administration (P < 0.05) in both groups treated with EEAI 500 and 1000 mg/kg. Conclusion: Ethanolic extract of A. indicum had shown dose dependent anti-inflammatory activity.
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Buccal tablets
Diclofenac sodium
Drug release
Mucoadhesion
Mucoadhesive tablets
Release kinetics
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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.
Sujet(s)
Humains , Diclofenac , Électroacupuncture , Goutte articulaire/traitement médicamenteux , Préparations à action retardée , Thérapie par acupuncture , ArthralgieRÉSUMÉ
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.
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Objective:To explore the effect of diclofenac sodium suppository combined with tramadol sustained-release tablets on postoperative pain relief and recovery in patients with mixed hemorrhoids.Methods:Sixty patients with mixed hemorrhoids who underwent external dissection and internal ligation at the Shenzhen Traditional Chinese Medicine Proctology Hospital from September to October 2023 were selected and randomly divided into A group and AS group using a random number table method, with 30 patients in each group. The group A patients received oral tramadol sustained-release tablets 4 hours after surgery, while the group AS received diclofenac sodium suppositories for anal canal therapy in addition to the group A. Two groups were compared for postoperative pain [Visual Analog Scale (VAS)] and patient comfort [Numerical Rating Scale (NRS)], cumulative tramadol consumption, supplementary rescue pethidine needs, and adverse reactions at 4, 8, 24, and 48 hours.Resultsl:The VAS of the AS group were lower than those of the A group at 4, 8, 24, and 48 hours after surgery. The NRS scores of the group A patients at 4, 8, and 24 hours were significantly better than those of the group AS. The cumulative consumption of tramadol in the AS group at 4, 8, 24, and 48 hours after surgery was significantly lower than that in the A group; The demand rate for postoperative rescue of pethidine in the group A was significantly higher than that in the group AS. The incidence of nausea in the group A was significantly higher than that in the group AS.Conclusions:The combination of postoperative diclofenac sodium suppositories and oral tramadol sustained-release tablets for mixed hemorrhoid surgery has a significant improvement effect on pain. It can reduce the dosage of tramadol, reduce the need for rescue and supplementary analgesia, and have fewer adverse reactions.
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Abstract Diclofenac sodium (DF) is a non-steroidal anti-inflammatory drug (NSAID) that possesses antipyretic, analgesic, antinociceptive and anti-inflammatory activities. Like other NSAIDs, DF is known to be associated with renal, cardiovascular, and gastrointestinal complications. The present study was carried out to evaluate the adverse effects of DF in vivo in wistar albino rats and to assess if oral administration of the organic osmolyte betaine mitigates the adverse effect of DF. Eighteen male Wistar rats were divided into three groups, one group of animals was fed orally with 20 mg/kg of DF once/day, and the other group received a combination of 20 mg/kg of DF and 30 mg/kg of betaine, once/day. Apart from the hematological and biochemical parameters, histopathological changes in the liver, lungs, brain, heart and kidney were also investigated. Histopathological alterations that were found in the liver, kidney, and lungs of DF-treated animals were found to be minimal or absent in DF + betaine-treated animals, as compared to untreated control. The results showed that betaine mitigates the adverse effects associated with DF treatment.
Sujet(s)
Animaux , Mâle , Rats , Bétaïne/agonistes , Diclofenac/effets indésirables , Préparations pharmaceutiques/administration et posologieRÉSUMÉ
Abstract Hedera nepalensis (H. nepalensis) , belonging to the family Araliaceae, is a medicinal plant traditionally used to treat stomach problems. The current study investigated the gastroprotective potential and the mechanism of action of H. nepalensis in diclofenac-and ethanol-induced ulcer models. Anti-oxidant and lipid peroxidation inhibitory prospects of H. nepalensis were checked out by free radical scavenging assay and UV spectrophotometer respectively. Effect of H. nepalensis on the pH, gastric total acidity of gastric juice and protective effects of H. nepalensis against ulcer models have been examined. Histopathological studies have been carried out. The aqueous methanol extract of H. nepalensis (100 µg/mL) showed anti-oxidant (83.55%) and lipid peroxidation inhibitory (70.88%) potential at 1000 µg/mL; the extract had no buffer potential. The extract (400 mg/kg) significantly (81.12% and 63.46%) showed gastroprotective effect in diclofenac and ethanol-induced rat ulcer models respectively. Histopathological studies confirmed the biochemical findings. FTIR analysis showed the presence of carboxylic acid, alkanes, conjugated alkanes, aldehydes and alkyl-aryl ethers. Gallic acid, M-coumaric acid and quercetin were found by HPLC analysis. H. nepalensis exhibited significant protection against diclofenac and ethanol induced gastric damage by anti-oxidant and lipid peroxidation suppression effects suggesting potential broad utility in treatment of diseases characterized with gastric damage.
Sujet(s)
Plantes médicinales , Estomac/malformations , Ulcère gastrique/anatomopathologie , Araliaceae/classification , Hedera/classification , Ulcère/induit chimiquement , Diclofenac/agonistes , Chromatographie en phase liquide à haute performance/méthodes , Spectroscopie infrarouge à transformée de Fourier/méthodes , AntioxydantsRÉSUMÉ
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.
Sujet(s)
Animaux , Rats , Diclofenac/toxicité , Lens , Extraits de plantes/pharmacologie , Stress oxydatif , Acide folique , AntioxydantsRÉSUMÉ
Abstract The form of drug administration affects the success of treatment, since it can influence adherence of the patient to the therapy. The use of orodispersible films has emerged as a way to overcome some drawbacks of conventional methods of drug delivery, especially for patients experiencing difficulty in swallowing. These films are prepared using a matrix that incorporates the drug and contains other substances that confer the properties of the system. The present work describes the use of thermoplastic starch as a carrier for the model drug diclofenac, including film preparation and testing of its orodispersible potential. Preparation of the film employed a microwave oven to gelatinize and plasticize corn starch, with incorporation of the model drug, followed by solvent-casting. The samples were characterized using mechanical tests, analyses of water uptake and water content, and Fourier transform infrared spectroscopy. The results indicated that the film presented promising properties as an alternative system for oral drug administration, with good incorporation and distribution of the drug in the matrix. The material displayed satisfactory mechanical properties, which are crucial for this type of material, due to the need for oral administration and handling before use.
Sujet(s)
Amidon/agonistes , Diclofenac/analyse , Préparations pharmaceutiques/administration et posologie , Spectroscopie infrarouge à transformée de Fourier/méthodesRÉSUMÉ
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.
Sujet(s)
Mâle , Animaux , Rats , Diclofenac/toxicité , Stress oxydatif , Lens , Rein/effets des médicaments et des substances chimiques , Tests hématologiques , Acide folique/pharmacologieRÉSUMÉ
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.
RÉSUMÉ
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.
RÉSUMÉ
Background: Pain is the most common symptom in various pathological conditions requiring appropriate treatment with analgesics. Use of analgesics is limited by various adverse drug effects. The present study was aimed to evaluate the analgesic activity of hydroalcoholic extract of Costus pictus leaves in Wistar albino rats. Aim and Objective: The objective of this study is to evaluate the analgesic activity of hydroalcoholic extract of C. pictus leaves in Wistar albino rats. Materials and Methods: The study was conducted on 30 Wistar albino rats and was divided into five groups each of six rats. Group-I (Sterile water-equivalent volume/po), Group-II Morphine (5 mg/kg/ip), Group-III CPHAE (200 mg/kg/po), Group-IV CPHAE (400 mg/kg/po), and Group-V Diclofenac (12.5 mg/kg/po). All the rats were administered respective drugs before starting of 30 min of experiment. Central analgesic (Tail clip and hot plate) and peripheral analgesic (Writhing test) methods were used to evaluate the analgesic activity. The data were recorded and analyzed with SPSS software. Results: Group-II, III, IV and V showed significant analgesic activity compared to Group-I in both central and peripheral animal models. Group-II showed significant effect compared to Group-III and IV in the central analgesic activity. Group-V showed significant effect compared to Group-III and IV in peripheral analgesic activity. Group-IV showed significant effect compared to Group-III. Conclusion: High dose of (400 mg/kg) C. pictus plant extract showed significant analgesic activity in the central and peripheral animal models compared to low dose.