تصييغ الابيوبروفين 600ملغم باودر فوار كجرعة دوائية فموية

Abstract

Abstract Ibuprofen is one of the most widely used drug to relieve mild to moderate pain such as dental discomfort ,post-operative pain ,headaches, menstruation pain as well as treatment for fever rheumatoid arthritis , osteoarthritis and to treat soft tissue injuries such as sprains , tendonitis among other condition. It belong to the group of drug called non-steroidal anti inflammatory drug (NSAID). The aim of this research is to formulate of Ibuprofen(600mg) effervescent powder (sachet) which is abig wide spread uses in Iraqi drug Two formula were prepared using different additives , after has been checked and ensure getting the required physical and chemical specification including the assay of the active ingredient exposed the selected batches to different temperatures by monitoring and assessing the change taken place , The selected formula was introduced in to exaggerated different temperatures ,the shelf-life was calculated.

Key words: Ibuprofen, sachet, inflammatory, analgesic.

Introduction Ibuprofen was the first member of propionic acid derivatives to be introduced in (1969) as a better alternative to Aspirin. Gastric discomfort, nausea anvomiting, though less than aspirin or indomethacin, are still the most common side effects. .[1] A low dose ibuprofen is as effective as aspirin and paracetamol for the indications normally treated with over the counter medications. It is widely used as an analgesic, an anti inflammatory and an antipyretic agent. Recemic ibuprofen and S(+) enantiomer are mainly used in the treatment of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, management of spondylitis, osteoarthritis, rheumatoid arthritis and soft tissue disorder.[2] Ibuprofen a propionic acid derivative (NSAID) used management of mild to moderate pain and inflammation in condition such as dysmenorrheal, headache including migraine, postoperative pain , dental pain , musculoskelal and joint disorder such as ankylosing spondylitis , osteoarthritis.[3]

Ibuprofen is a benzen acetic acid .α-methyl-4-(2-methyl propyl ) (+)_ p + sobutyl hydrotropic acid. Ibuprofen is a white to off-white crystalline powder having slightly characteristic odour, practically insoluble in water, very soluble in alcohol, in acetone , in chloroform and in methyl alcohol slightly soluble in ethyl acetate.Ibuprofen sacchet contain not less than 90% and not more than 110% of the labeled amount of C13H18O2 molecular weight 206.28.[4]

Experimental work Materials: All the used materials in this study are complied with BP 2010,USP 35 NF 30 compendia specifications. These include: Ibuprofen (very fine powder) ,A vicel pH101, cros caramellose sodium, manitol, sodium bicarbonate ,sodium lauryl sulfate ,tartaric acid ,citric acid , sodium saccharin, all the materials and quantities showed in table no. (1) . Equipments: Different balances, sieve with aperture (250 µ, 2000 µ and 1400 µ), Kenwood mixer and kneader, oven with st. st. trays or fluid bed dryer, rotar granulator with sieve mesh (12), cubic mixer and Filling & packaging machine. Physical tests- The following tests were performed for sachet for the prepared formula that is weight variation taste. Chemical tests involve Assay and content uniformity: Assay limit; should be within (90-110 %) .detection of the drug involves HPLC system which is composed of the following parts: column: C18, (25 cm) length. Flow rate is (1 ml / min). The mobile phase composed of: glacial acetic acid (10 ml)/ methanol (800 ml) distilled water to(1000 ml), and detector wave length (276nm). Dissolution test for the prepared formula was performed in (900 ml) of PH: (7.5) (0.2M) phosphate buffer, apparatus (2) RPM: (50) for (30 min)at (276 nm) according to pharmacopoeia not less than (80%) of the labeled amount of the drug is dissolved in (30 minutes).

Active ingredient and additives Table no.1: Reference specifications of the materials used in the formulation. Formula for (100) sachet Weight mg. Per one sacchet Weight gm.Per 100 sacchet Specifications reference Name of the material Item 600 60 gm BP 2010,USP 35 NF 30 Ibuprofen(very fine powder) 1 220 22 gm BP 2010,USP 35 NF 30 Avicel PH 101 2 8 0.8 gm BP 2010,USP 35 NF 30 Sodium lauryl sulfate 3 100 10 gm BP 2010,USP 35 NF 30 Croscarmellose sodium 4 320 32 gm BP 2010,USP 35 NF 30 Tartaric acid 5 800 80 gm BP 2010,USP 35 NF 30 Citric acid 6 12 1.2 gm BP 2010,USP 35 NF 30 Sodium saccharin 7 400 40 gm BP 2010,USP 35 NF 30 Sodium bicarbonate 8 1200 120 gm BP 2010,USP 35 NF 30 Mannitol 9

Procedures 1- The following materials were sieved at( 250m): Ibuprofen Avicel PH 101 Croscarmellose sodium Mannitol Sodium bicarbonate Sodium lauryl sulfate 2-The sieved powders in No.1 were charged into the kneader and mixed for (8 minutes) at low speed. Prepared the granulating solution as the following; 3-Dissolve(3.27gm) PVP in(31.2 ml) ethanol (96%)with continuous stirring until a clear solution was formed obove powder. 4¬-The following materials were sieved at (250m): Tartaric acid , citric acid and sodium saccharin 5-Dissolve (1.1gm) pvp in (11.15) ethanol (96%) then mixing with powder in No. 4 at low speed for (12 min) until good granulation was formed . 6¬-Mixing all obove in knewood mixture then drying the granulation in oven with st st trays leave it until complet drying 7-Sieving dry granulation with aperture sieve (1.40mm)mesh(No.14) 8-Collecting the granules in poly ethylene sacs filling and packaging in sachet closing very well them keeping away from moisture and light

Specifications Table no.2: Specification of ibuprofen 600 mg sachet 3 gm Weight of sachet Each sachet content 600 mg ibuprofen Content Sweet acid after dissolving in water Taste 3.5 – 4.5 pH 95 – 105 % Assay limit

Discussion The required information to create a suitable formula for Ibuprofen 600 mg sachets were collected from the available references, and three formule by using different additives with different ratios were done, then after the required primary physical specifications and the assay of the active ingredient were estimated and certified the stability study to the primary batches has been started (expose the blistered tablets to the following) : 1-Accelerated stability study(40 º C ± 2 º C and 75% ± 5% RH for 6 months). 2-Long term stability study(30 º C ± 2 º C and 65% ± 5% RH for 12 months) 3-Real time stability study(25 º C ± 2 º C and 60% ± 5% RH for 36 months) Then by monitoring and assessing the changes that will take place, the formula which will show good stability under all temperatures will be selected and the tentative expiry date could be calculated.

References 1- Tripathi KD. Non steroidal anti inflammatory drugs and anti pyretic analgesics. In: Essentials of medical pharmacology. 5th edn., Jaypee Brothers, New Delhi, 2003. p. 176. 2- Rabia bushra and nousheen aslam , An Overview of Clinical Pharmacology of Ibuprofen, oman med. J.2010Jul:25(3):155-1661. 3- Pharmaceutical press, Martindale (extra pharmacopoeia) 37. P. 66, 2011 . 4- British Pharmacopoeia commission, British Pharmacopoeia 2013. 5- United State Pharmacopeia convention , U.S.P.35 National formulary 30,