Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 3

NSAIDs Related Abstracts

3 Development of an Erodable Matrix Drug Delivery Platform for Controled Delivery of Non Steroidal Anti Inflamatory Drugs Using Melt Granulation Process

Authors: M. Sudhakar, Vinay U. Rao, A. Hilsana

Abstract:

Even though a number of non-steroidal anti-inflammatory drugs (NSAIDS) are available with different chemistries, they share a common solubility characteristic that is they are relatively more soluble in alkaline environment and practically insoluble in acidic environment. This work deals with developing a wax matrix drug delivery platform for controlled delivery of three model NSAIDS, Diclofenac sodium (DNa), Mefenamic acid (MA) and Naproxen (NPX) using the melt granulation technique. The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35% in 1 hour and not less than 80% Q in 24 hours. Full factorial design of experiments was followed for optimization of the formulation.

Keywords: NSAIDs, controlled delivery, target product profile, melt granulation

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2 (Anti)Depressant Effects of Non-Steroidal Antiinflammatory Drugs in Mice

Authors: Horia Păunescu

Abstract:

Purpose: The study aimed to assess the depressant or antidepressant effects of several Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) in mice: the selective cyclooxygenase-2 (COX-2) inhibitor meloxicam, and the non-selective COX-1 and COX-2 inhibitors lornoxicam, sodium metamizole, and ketorolac. The current literature data regarding such effects of these agents are scarce. Materials and methods: The study was carried out on NMRI mice weighing 20-35 g, kept in a standard laboratory environment. The study was approved by the Ethics Committee of the University of Medicine and Pharmacy „Carol Davila”, Bucharest. The study agents were injected intraperitoneally, 10 mL/kg body weight (bw) 1 hour before the assessment of the locomotor activity by cage testing (n=10 mice/ group) and 2 hours before the forced swimming tests (n=15). The study agents were dissolved in normal saline (meloxicam, sodium metamizole), ethanol 11.8% v/v in normal saline (ketorolac), or water (lornoxicam), respectively. Negative and positive control agents were also given (amitryptilline in the forced swimming test). The cage floor used in the locomotor activity assessment was divided into 20 equal 10 cm squares. The forced swimming test involved partial immersion of the mice in cylinders (15/9cm height/diameter) filled with water (10 cm depth at 28C), where they were left for 6 minutes. The cage endpoint used in the locomotor activity assessment was the number of treaded squares. Four endpoints were used in the forced swimming test (immobility latency for the entire 6 minutes, and immobility, swimming, and climbing scores for the final 4 minutes of the swimming session), recorded by an observer that was "blinded" to the experimental design. The statistical analysis used the Levene test for variance homogeneity, ANOVA and post-hoc analysis as appropriate, Tukey or Tamhane tests.Results: No statistically significant increase or decrease in the number of treaded squares was seen in the locomotor activity assessment of any mice group. In the forced swimming test, amitryptilline showed an antidepressant effect in each experiment, at the 10 mg/kg bw dosage. Sodium metamizole was depressant at 100 mg/kg bw (increased the immobility score, p=0.049, Tamhane test), but not in lower dosages as well (25 and 50 mg/kg bw). Ketorolac showed an antidepressant effect at the intermediate dosage of 5 mg/kg bw, but not so in the dosages of 2.5 and 10 mg/kg bw, respectively (increased the swimming score, p=0.012, Tamhane test). Meloxicam and lornoxicam did not alter the forced swimming endpoints at any dosage level. Discussion: 1) Certain NSAIDs caused changes in the forced swimming patterns without interfering with locomotion. 2) Sodium metamizole showed a depressant effect, whereas ketorolac proved antidepressant. Conclusion: NSAID-induced mood changes are not class effects of these agents and apparently are independent of the type of inhibited cyclooxygenase (COX-1 or COX-2). Disclosure: This paper was co-financed from the European Social Fund, through the Sectorial Operational Programme Human Resources Development 2007-2013, project number POSDRU /159 /1.5 /S /138907 "Excellence in scientific interdisciplinary research, doctoral and postdoctoral, in the economic, social and medical fields -EXCELIS", coordinator The Bucharest University of Economic Studies.

Keywords: Antidepressant, NSAIDs, depressant, forced swim

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1 The Addition of Opioids to Bupivacaine in Bilateral Infraorbital Nerve Block for Postoperative Pain Relief in Paediatric Patients for Cleft Lip Repair-Comparative Effects of Pethidine and Fentanyl: A Prospective Randomized Double Blind Study

Authors: Mrudula Kudtarkar, Rajesh Mane

Abstract:

Introduction: Cleft lip repair is one of the common surgeries performed in India and the usual method used for post-operative analgesia is perioperative opioids and NSAIDs. There has been an increase in use of regional techniques and Opioids are the common adjuvants but their efficacy and safety have not been studied extensively in children. Aim: A prospective, randomized, double-blind study was done to compare the efficacy, duration and safety of intraoral infraorbital nerve block on post-operative pain relief using bupivacaine alone or in combination with fentanyl or pethidine in paediatric cleft lip repair. Methodology: 45 children between the age group 5 – 60 months undergoing cleft lip surgery randomly allocated into 3 groups of 15 each received bilateral intraoral infraorbital nerve block with 0.75ml of solution. Group B received 0.25% bupivacaine; group P received 0.25% bupivacaine with 0.25mg/kg pethidine, group F received 0.25% bupivacaine with 0.25microgm/kg fentanyl. Sedation after recovery, post-operative pain intensity and duration of post-operative analgesia were assessed using Modified Hannallah Pain Score. Results: The mean duration of analgesia was 17.8 hrs in Group B, 23.53 hrs in Group F and 35.13 hrs in Group P. There was statistically significant difference between the means of the three groups- ANOVA (p < 0.05). Conclusion: Thus we conclude that addition of fentanyl or pethidine to bupivacaine for Bilateral Intraoral Infraorbital Nerve Block prolong the duration of analgesia with no complications and can be used safely in paediatric patients.

Keywords: NSAIDs, cleft lip, infraorbital block, Opiods

Procedia PDF Downloads 113