Evaluation of gastric tolerability, antinociceptive and antiinflammatory activity of combination NSAIDs in rats

Kalra, Bhupinder Singh; Shalini, .; Chaturvedi, Shashi; Tayal, Vandana; Gupta, Usha

doi:10.4103/0970-9290.59439

Cited by 13 publications

(12 citation statements)

References 14 publications

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“…Rats were anesthetized with urethane (0.5 ml 25% w/v ip), and 100 μl of 1% w/v carrageenan physiological solution was injected subcutaneously into the left hind paw. An hour later, a defined weight of the tested tablet containing NIM dose (9 mg/100 g) [Bianchi et al., ; Kalra et al., ], similar dose of unmodified NIM powder, and complexed NIM were separately dispersed in 5 ml distilled water and immediately given to the rat by gavage. The paw volume was measured after 0.5, 1, 2, 3, 4, and 5 h using a plethysmometer.…”

Section: Methodsmentioning

confidence: 99%

Nimesulide/Methyl β‐Cyclodextrin Inclusion Complexes: Physicochemical Characterization, Solubility, Dissolution, and Biological Studies

Auda

2013

Drug Development Research

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Nimesulide (NIM) is an insoluble nonsteroidal anti-inflammatory drug (NSAID). Complexation of drug with methyl β-cyclodextrin was evaluated to improve solubility and dissolution rate of NIM. Complexation was achieved via a coevaporation technique to obtain different drug to polymer molar ratios (1:1, 1:2, and 1:3). The physicochemical characterization of the systems using powder X-ray diffraction and infrared spectroscopy was carried out to understand the influence of this technological process on the physical status of single components and complex systems and to detect possible interactions between drug and carrier. Moreover, quantitative solubility and in vitro dissolution studies of NIM alone and NIM inclusion complexes were studied in the dissolution media of phosphate buffer pH 5.5 and 7.4. The analysis provided existence of a molecular interaction between drug and carrier together in the complex state. The study showed that the inclusion systems enhanced of drug solubility, dissolution rate, and anti-inflammatory activity.

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Section: Methodsmentioning

confidence: 99%

Nimesulide/Methyl β‐Cyclodextrin Inclusion Complexes: Physicochemical Characterization, Solubility, Dissolution, and Biological Studies

Auda

2013

Drug Development Research

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“…A large percentage of such duodenal and peptic ulcers are caused by helicobacter pylori induced gastroduodenitis, while only 20% are caused by nonsteroidal antiphlogistics [4,5] In this case, helicobacter pylori colonisation of the mucosa was not responsible for the development of an ulcer. Usually, the gastric bleeding due to ulcers is caused by erosion of the submucosal venous or arterial vessels.…”

Section: Discussionmentioning

confidence: 99%

Severe gastric variceal haemorrhage due to splenic artery thrombosis and consecutive arterial bypass

et al. 2011

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BackgroundUpper gastrointestinal haemorrhage is mainly caused by ulcers. Gastric varicosis due to portal hypertension can also be held responsible for upper gastrointestinal bleeding. Portal hypertension causes the development of a collateral circulation from the portal to the caval venous system resulting in development of oesophageal and gastric fundus varices. Those may also be held responsible for upper gastrointestinal haemorrhage.Case presentationIn this study, we describe the case of a 69-year-old male with recurrent severe upper gastrointestinal bleeding caused by arterial submucosal collaterals due to idiopathic splenic artery thrombosis. The diagnosis was secured using endoscopic duplex ultrasound and angiography. The patient was successfully treated with a laparoscopic splenectomy and complete dissection of the short gastric arteries, resulting in the collapse of the submucosal arteries in the gastric wall. Follow-up gastroscopy was performed on the 12th postoperative week and showed no signs of bleeding and a significant reduction in the arterial blood flow within the gastric wall. Subsequent follow-up after 6 months also showed no further gastrointestinal bleeding as well as subjective good quality of life for the patient.ConclusionSubmucosal arterial collaterals must be excluded by endosonography via endoscopy in case of recurrent upper gastrointestinal bleeding. Laparoscopic splenectomy provides adequate treatment in preventing any recurrent bleeding, if gastric arterial collaterals are caused by splenic artery thrombosis.

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“…The appropriate body weight adjusted doses of test drugs as extrapolated from doses used in similar studies conducted previously to be 13.5 mg/200 g rat and 1.45 mg/20 g mouse for paracetamol, and 1.8 mg/200 g rat and 0.26 mg/20 g mouse for nimesulide were used. [78]…”

Section: Methodsmentioning

confidence: 99%

Comparison of analgesic effects of nimesulide, paracetamol, and their combination in animal models

2010

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Objectives:To compare the analgesic activity of nimesulide and paracetamol alone and their combination in animal models for the degree of analgesia and the time course of action.Materials and Methods:Analgesia was studied in albino rats using formalin test and in albino mice using writhing test and the radiant heat method. For each test, four groups of six animals each were orally fed with a single dose of nimesulide, paracetamol, and combination of nimesulide + paracetamol and gum acacia as control, respectively.Results:In all the three test models, all three drug treatments showed significant analgesia (P < 0.001) as compared to control, but there was no significant difference in the analgesia produced by either drugs alone or in combination. The radiant heat method demonstrated a quicker onset and longer duration of action with nimesulide, whereas writhing test showed a quicker onset of action with paracetamol. In formalin test, greater degree of analgesia was seen with individual drugs than that of the combination, though this difference was not statistically significant.Conclusions:Nimesulide and paracetamol combination offers no advantage over nimesulide alone or paracetamol alone, either in terms of degree of analgesia or onset of action. Therefore, our study supports the reports claiming irrationality of the fixed dose combination of nimesulide and paracetamol.

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Evaluation of gastric tolerability, antinociceptive and antiinflammatory activity of combination NSAIDs in rats

Cited by 13 publications

References 14 publications

Nimesulide/Methyl β‐Cyclodextrin Inclusion Complexes: Physicochemical Characterization, Solubility, Dissolution, and Biological Studies

Nimesulide/Methyl β‐Cyclodextrin Inclusion Complexes: Physicochemical Characterization, Solubility, Dissolution, and Biological Studies

Severe gastric variceal haemorrhage due to splenic artery thrombosis and consecutive arterial bypass

Comparison of analgesic effects of nimesulide, paracetamol, and their combination in animal models

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