| Arthritis is a relatively common occurrence in human joints and surrounding tissue inflammatory diseases. The number of patients with arthritis have more than100million and the number is increasing. In severe cases of arthritis cause joint deformity, causing dysfunction, severe cases may lead to disability, the quality of life of patients pose a serious hazard. Diclofenac is a common treatment for arthritis potent non-steroidal anti-inflammatory drugs, aspirin and anti-inflammatory effect is stronger than pain. In addition to the treatment of acute and chronic arthritis, osteoarthritis and other inflammatory, can also be used to relieve a variety of pain after surgery and trauma, has also been antipyretic effect, a wider range of applications. Rapid and complete oral absorption of diclofenac sodium, no accumulation of long-term use, but its short half-life of about2h, and significant gastrointestinal reactions, severe cases can cause gastric perforation. To reduce the frequency of administration, reducing the occurrence of adverse reactions, improve patient compliance, subject to SURELEASE(?) as the capsule material, prepared by spray drying of diclofenac sodium sustained release microspheres, followed by powder prepared by direct compression tablets of diclofenac sodium delayed-release tablets prepared product quality control and compliance.First, in vitro analysis of diclofenac sodium studies, the establishment of a method for the determination of diclofenac sodium content and in vitro release of UV spectrophotometry. Accessories for determination without interference, diclofenac sodium concentration in the range of8～32μg/ml good linear relationship, linear regression equation:A=0.0245C+0.0121, r=0.9992. Examines the average recoveries and intra-day precision, are satisfactory method is simple and specific. Establish a method for evaluating in vitro release profile similar factor method. Were established for the determination of diclofenac sodium release and sustained-release tablets release microspheres of approach.Secondly, diclofenac sodium delayed-release microspheres were screened and technology research prescription. Spray drying process conditions were single factor, determines the optimal spray drying process:inlet temperature160℃, the pump speed is280ml/h, into the wind speed4.3m/s, through needle frequency of middle, nozzle diameter0.5mm. Of the capsule material were investigated to determine the choice of SURELEASE(?) as capsule material, and then examines the amount of capsule material, after considering the choice of3percent concentration capsule material spray drying. After the confrontation sticky agents and plasticizers inspected to determine talc as an anti-stick agent, polyethylene glycol as a plasticizer. On the basis of single factor experiment, select capsule material ratio, the amount of anti-stick agents, plasticizers amount as factors orthogonal design experiments to investigate the composite index to determine the optimal prescription. The quality of diclofenac sodium sustained release microsphere prepared to inspect microspheres morphology, particle size distribution, drug loading, encapsulation efficiency and release are in line with requirements.Finally, diclofenac sodium delayed-release tablets were prescribed screening and preparation. The topic chosen easy-powder prepared by direct compression method were sustained-release tablets, for tableting pressure were investigated to determine the selection control tablet hardness at5～7kg of pressure. Single factor determines the materials, orthogonal experiment investigated the impact of drug dissolution of materials, integrated score results were analyzed to determine the amount of materials, and ultimately determine the optimal prescription tablets prepared. The quality of the preparation of diclofenac sodium delayed-release tablets were investigated, the result is:Appearance good; tablet weight differences compliance; content little deviation, RSD values were less than2; measured release of three batches of sustained-release tablets were prepared by The results show a stable release, good reproducibility. Release mechanism for sustained-release tablets conducted a preliminary study, the drug release for drug diffusion and dissolution coexist. The stability of diclofenac sodium delayed-release tablets were studied, which at high temperatures, high humidity and light, appearance, content and release were not changed significantly. Accelerated testing study no significant change indicators, diclofenac sodium sustained release tablets prepared can be stable over a longer period. |
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