A study to compare ibuprofen effervescent granules with ibuprofen tablets in the treatment of acute dental pain.

Sharma NK, Kindelan JD, Hutchinson D, Lancaster L.

Source
Pinderfields General Hospital, Wakefield.

Abstract
PURPOSE OF STUDY: To compare both the speed of onset and efficacy of the analgesia produced by the effervescent granule formulation with that produced by the conventional-release tablet formulation of ibuprofen in patients suffering acute dental pain and to record the incidence and severity of any adverse events. POPULATION STUDIED: Dental out-patients of either sex and over 16 years of age requiring surgical removal of unilateral or bilateral lower third molar teeth under general anaesthesia as day cases. METHODS: A total of 50 patients received the effervescent granules formulation of ibuprofen 600 mg (Brufen Granules) as study treatment and 50 received the 600 mg tablet formulation in this investigator-blind, parallel-group multiple-dose study. Surgery was performed under general anaesthesia by one or two dental surgeons. Patients received either one sachet of ibuprofen granules or one tablet of ibuprofen at six-hourly intervals for up to 24 hours once postoperative pain became moderate to severe. FINDINGS: Both treatments were shown to be efficacious in treating post-operative dental pain. The granules were found to give significantly better pain relief in the first 30 minutes following the first dose. This may be owing to a more rapid absorption from the granules formulation in these patients and/or a local action of ibuprofen in solution in the mouth. CONCLUSION: The effervescent soluble form of ibuprofen (Brufen Granules) is preferable to the conventional tablet form in managing the immediate dental pain experienced post-operatively by most patients because of its faster onset of action.

[Evaluation of the antipyretic safety and accuracy of two pediatric ibuprofen formulations].
[Article in Spanish] Dez Domingo J, Planelles Cantarino MV, Moreno Madrid F, Uberos Fernndez J, Moreno Martn J, Molina Carballo A, Antelo Cortizas J, Armenteros Gonzlez S, Domnguez Granados R, Moreno Carretero E.

Source
Centro de Salud de Nazaret. Valencia. diez_jav@gva.es

Abstract
AIM: To compare the efficacy and to evaluate the clinical bioequivalence of two different formulations of ibuprofen (suspension and effervescent granules) in febrile children. METHODS: An open, randomized, multicenter study. Febrile children (axillary temperature 38 degrees C) weighing more than 25 kg, admitted into the emergency departments of the participating hospitals were randomly assigned to either of the two treatment groups: ibuprofen suspension (7 mg/kg) or effervescent granules at the following dosages: 200 mg in children weighing 2540 kg or 400mg in children weighing 3540 kg and with an axillary temperature above 39 degrees C. This latter dose of 400 mg was also given to children weighing more than 40 kg.The investigators took axillary temperature before treatment and 30, 60, 90, 120, 180 and 240 min after administration of the corresponding dose. Possible adverse events were noted. RESULTS: A total of 103 patients were included in the study; 51 received the effervescent granules and 52 received the suspension formulation. The mean temperature was reduced in both groups during the study (p < 0.005). No differences were found between the formulations. The mean differences of temperatures at each point of the study were within the clinical bioequivalence interval (+/-0.5 degrees C). Only one patient had an axillary temperature of 35.9 degrees C. This was the only adverse event recorded in the study. CONCLUSIONS: Both ibuprofen formulations were effective in reducing fever and may be considered clinically bioequivalent.

Dissolution and pharmacokinetics of a novel micronized aspirin formulation.

Voelker M, Hammer M. Source Bayer Consumer Care, Morristown, NJ, USA, michael.voelker@bayer.com. Abstract Aspirin (acetylsalicylic acid, ASA) has been used as an analgesic, antipyretic and antiinflammatory drug for many years. A new 500 mg aspirin tablet formulation containing micronized active ingredient and an effervescent component has been developed for potential improvement in the onset of action for acute pain treatment. This paper describes the dissolution and the pharmacokinetics of the new formulation in comparison with regular aspirin tablets, aspirin granules and aspirin effervescent tablets. Micronized aspirin tablets dissolve significantly faster over a pH range from 1.2 to 6.8 compared to regular 500 mg aspirin tablets. Plasma concentration time curve comparison to regular 500 mg aspirin tablets showed a substantial improvement in the time to maximum plasma concentrations (T (max)) (ASA 17.5 min vs. 45 min) and an increase in maximum plasma concentration (C (max)) (ASA 13.8 g/ml vs. 4.4 g/ml) while the overall extent of exposure (AUC) remains almost unchanged. The data suggest a potential improvement for onset of action in treating acute pain with the new micronized aspirin formulation.

Preparation and evaluation of fastdisintegrating effervescent tablets of glibenclamide.

Jacob S, Shirwaikar A, Nair A. Source Department of Pharmaceutics, Manipal Academy of Higher Education, Manipal, Karnataka, India. sherinjacob6001@yahoo.co.in Abstract Fast-dissolving effervescent tablets (FETs) were prepared by the modification of nonreactive liquid-based wet granulation technique. Effervescent systems are not stable in the presence of trace amount of moisture, and elimination or inactivation of free water is the key to stability apart from manufacturing in controlled humidity environment. Our main objective of the project was to develop FETs of glibenclamide based on highly plastic granules that can be compressed at low pressure to form fast-melting pharmaceutical tablets. In this study, we have screened various acid and carbonate sources for the effervescent system. Citric acid was coated with plastic materials such as polyethylene glycol (PEG), which provide a physical barrier to the reaction. The inherent hygroscopic nature of PEG could decrease the affinity for moisture of effervescent mixtures and can provide a stabilizing effect. Sodium bicarbonate was blended with sugar alcohol like mannitol, which would give a protective coating. PEG 1000 melts at body temperature (approximately 37 degrees C) and thereby does not delay the reaction between the acid source and base. The present formulation using citric acid-sodium bicarbonate and citric acid-sodium glycine carbonate tablet with PEG and mannitol was found to have better reaction properties and reaction stability than does the standard citric acidsodium bicarbonate tablet. FETs of glibenclamide might aid in dissolution due to increase in microenvironmental pH around the granules and saliva. Sensory study on disintegration time and mouth feel attributes ranked the present formulation based on grittiness, chalkiness, and overall preference as best.

Effervescent granule based proliposomes of ibuprofen.

Katare OP, Vyas SP, Dixit VK.

Source Department of Pharmaceutical Sciences, Dr. H. S. Gour Vishwavidyalaya Sagar, India. Abstract Proliposomes of ibuprofen were successfully prepared using effervescent granules as solid carriers of dried phospholipids along with other lipids (soyabean lecithin, stearylamine and cholesterol). Liposomes of regular size with uniform size distribution resulted when proliposomal formulations were hydrated under the effervescence produced by the production of carbon dioxide gas. The inert atmosphere of carbon dioxide gas prevents the chance of oxidative degradation of phospholipids. The size distribution of liposomes was noted to be related to the degree of agitation provided by effervescence. Encapsulation efficiency of liposomes derived from proliposomes was shown to be nearly 100 per cent. Preparations were shown to be quite stable at 20 degrees C when stored under an umbrella of nitrogen. The enhanced anti-inflammatory activity of ibuprofen entrapped in liposomes was exhibited when compared with plain ibuprofen following intravenous administration using the carrageenan induced paw oedema test

Preparation and performance evaluation of plain proliposomal systems for cytoprotection.

Katare OP, Vyas SP, Dixit VK.

Source
Department of Pharmaceutical Sciences, Dr H.S. Gour Vishwavidyalaya, Sagar, India.

Abstract

Plain liposomal systems composed of soyabean lecithin, cholesterol and stearylamine were formulated using various approaches. The prepared products were characterized and evaluated for their cytoprotective performance against the necrotizing NSAID's (i.e. aspirin and phenylbutazone). Liposomes derived from proliposomes (effervescent granules based) demonstrated the best cytoprotective activity and physical and stability characteristics. This system was shown to be superior. An increased availability of regular and small sized liposome born phospholipids to the damaged mucosal systems accounted for its better and enhanced performance.