TECHNOLOGICAL STUDY OF PREPARING DICLOFENAC GEL / Монголын эм зүй, эм судлал

ABSTRACT

Introduction: It is required to develop drug formulations and increase local preparations substituting the import preparations. The utilization of a new drug formulation of diclofenac gel is an example of a medicine which is encouraged to be prepared locally. Diclofenac gel is a cyclooxygenase inhibitor, which is a non-steroidal anti-inflammatory drug (NSAID) taken to reduce inflammation and as an analgesic reducing pain in certain conditions. It is important to develop technology and standard for diclofenac gel type of medicine in Mongolia.In 2010, domestic manufacturers produced about 30- 40 percentage of demand in Mongolia. However, there are many manufacturers that produce the same type of medicines. This shows that there is a need for local manufacturers to meet local demand. It is an indication of urgency in bringing in new technologies, new drug formulations, activating drug research and scientific work in domestic drug industry.Based on research, in 2011, non-steroidal anti- inflammatory drugs were the most sold drugs, which had a market share of 29.2%. Also in 2010, non- steroidal anti-inflammatory drugs of gel formulation had a market share of 130 million Tugriks.In 2011, there were nine different manufacturers of diclofenac gel have been registered to Mongolian Medicine Registrar/LICEMED/. They are:-Clafen 1%-20.0 produced in Antibiotice Ltd, Romania-Feloran 1%-60.0 produced in Bаlkanpharma Troyan AD, Poland-Almiral1%-10.0/25.0 produced in Medochemie Ltd, Cyprian-Olfen 1%-20.0 produced in Mepha Ltd, Switerland-Voltaren 1%-20.0/50.0 produced in Novartis pharma,Switzerland-Dicloran Plus 1%-30.0 produced in Unique pharmaceutical laboratories, India-DiclofenacAcri 1%-30.0 produced in Acrihin Ltd, Russia-Diclovit 1%-20.0 produced in Nijpharm, Russia-Diclomol 1%-20.0 produced in Win Medicare Ltd, India.These gels are packaged between 20-60 grams and the are price ranges from 2,700-12,000 Tugriks.In the world, nowadays diclofenac gel is most commonly produced.Diclofenac gel is colorless, and it penetrates the affected area quickly and effectively. The gel has an advantage of delivering full drug concentration to the affected area quickly, while it is convenient and pleasant to use.Purpose of study: The purpose of study’s to develop a Diclofenac gel technology for the first time in Mongolia. In order to reach my purpose, which owe as follows:• To determine convenient ingredients and gel baseof gel formulations• To develop a layout explaining gel manufacturingtechnology• To formulate raw ingredients based on the developed of the gel• To develop an evaluation and quality control systemfor producing gelMaterials and methods: Research work was done at the Monos School of Pharmacy and Drug Research Institute.Triethanolamin and Glycerin from Tsetsuuh LLC, Diclofenac sodium, hydroxypropylmethylcellulose, and menthol from Monos Pharm LLC, Carbomer 940, Ultrez-21 and Propylenglycol from Monos Cosmetic LLC were used for this research.To determine the drug ingredient: To determine gel formulations, primary and secondary ingredients were chosen carefully to maintain chemical compatibility and stability.Developed gel formulation was checked forquality control, which includes drug content, pH,appearance/Homogeneity/, and viscosity by Russian Pharmacopoeia XI and Mongolian Primary Pharmacopoeia. Permeability studies and skin irritation test was performed by USP.Result: First, carbopol concentrations of 0.5%, 1.0%, 1.5% and 1.2%, Ultrez-21 concentrations of 0.5%,0.8%, and 1%, and hydroxypropylmethylcelluloseconcentrations of 3%, 4%, 5% were prepared as gel formulations.Of those, carbopol concentrations of 1.2% and 1.5%, and Ultrez-21 concentrations of 0.8% and 1.0% were relatively better compared to other concentrations in terms of meeting drug content, appearance, pH level, and viscosity requirements. 0.2 gram of Menthol was added to provide comfort and pleasant odor when gel is applied as well as providing release of diclofenac sodiumFinal products were compared to similar diclofenac gels in the market in terms of pH level, drug content, skin irritation, and release of active substance. Of those final products, Ultrez-21 concentration of 1% resulted to be the most similar to the diflofenac gels in the market that satisfy the qualities mentioned above.Conclusion:1. The Ultrez-21 1% is determined to be the best gelling agent and 0.2 gram of Menthol is determined to be the best amount for increasing drug permeability.2. Developed technological procedure for preparingdiclofenac gel.3. To determine criteria for quality control, gel drug content, appearance, pH and viscosity were shown to be the most convenient measures.