Mohd Azharuddin

Colon targeted drug delivery system is capable of protecting the drug in route to the colon i.e. drug gets released and absorbed once it reaches the colon. A multiparticulate system combining pH sensitive property and biodegradability has been investigated to prepare and evaluate Eudragit S-100 coated Sodium alginate microspheres for colon targeting of Tramadol Hydrochloride. Uncoated Tramadol Hydrochloride microspheres were prepared by ionotropic gelation technique using different ratios of Tramadol Hydrochloride and Sodium alginate. Coated Tramadol Hydrochloride microspheres were prepared by coacervation phase separation technique using different ratios of uncoated Tramadol Hydrochloride and Eudragit S-100/ Eudragit L-100. Uncoated and coated Tramadol Hydrochloride microspheres were evaluated for percentage yield, particle size, surface morphology, flow properties, drug content and entrapment efficiency and were found to be within the acceptable range. The uncoated microspheres sustained the release upto 8 hrs whereas coated microspheres sustained the release upto 12 hrs in a pH progression medium mimicking the condition of GIT. The drug release from MC4 formulation coated with Eudragit S-100 (1:4) showed desired rate as there was no drug release observed upto 4-5 hrs, while in colonic fluid controlled drug release was observed releasing about 69.66 % after 12 hrs. The release kinetics followed Peppas showing Super Case II transport. Stability studies suggested formulations were stable. It is concluded from the present investigation that Eudragit S-100 coated Sodium alginate microspheres are promising controlled release carriers for colon targeted delivery of Tramadol Hydrochloride.

Helminthes are the most common infections in man, affecting a large proportion of the world’s population. Study includes alcoholic extracts of Anacardium occidentale, Mangifera indica and combination of Anacardium occidentale and Mangifera indica leaves extracts (1:1) were evaluated for their anthelmintic activity using Pheretima posthuma model. Three concentrations (10, 20 and 50 mg/ml) of each extracts were used for this study which involved the determination of time of paralysis and time of death of the worms. Extracts obtained from both leaves not only paralyzed but also killed the earthworms. Among the two drug extracts, Mangifera indica showed maximum vermifuge and vermicidal activity at the concentration of 50 mg/ml. Combination of alcoholic extracts of Anacardium occidentale and Mangifera indica also showed a significant anthelmintic activity. Observations were comparable with the standard drug at concentration of 20 mg/ml. On the basis of the observations, it was concluded that both Anacardium occidentale and Mangifera indica leaves extracts have a potential anthelmintic property.

Granisetron hydrochloride is a novel serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. It is well absorbed from the gastrointestinal tract, but its oral bioavailability is low (60%) due to extensive first-pass metabolism which makes it an ideal candidate for rapid release drug delivery system. Hence, an attempt was made to prepare and evaluate fast dissolving oral films containing Granisetron hydrochloride as a model drug by solvent casting method using natural and synthetic polymers. Various formulations were developed with varying concentration of polymers like, CMC, HPMC and Pullulan. Citric acid was used as a disintegrating agent and Propylene glycol as a plasticizer. The prepared oral films were evaluated for their physicochemical and mechanical parameters such as Physical appearance, surface texture, Weight uniformity, surface pH, ,thickness uniformity, percentage moisture absorption, loss on drying, disintegration time, drug content uniformity, folding endurance, tensile strength, percentage elongation, in-vitro drug release, and stability studies. In-vitro release rate of Granisetron hydrochloride was studied in phosphate buffer pH 6.8. F7, F10 showed maximum release rate about 93.95% and 95.29% in 180 seconds respectively, whereas F3 showed 60.98%. The mechanism of drug release of fast dissolving oral film was found to be to be non-fickian diffusion following first order kinetics. The selected fast dissolving oral films were found to be superior to marketed conventional tablet. Short term stability studies of selected films indicated that there is no significant change with respect to physical appearance, disintegration time, drug content and in-vitro drug release.

Olmesartan medoxomil is an angiotensin II antagonist used as an antihypertensive drug which has poor oral bioavailability. Hence, an attempt was made to prepare and evaluate mucoadhesive buccal films containing Olmesartan medoxomil as model drug. Various mucoadhesive buccal films were prepared by employing HPMC alone, and in combination with Eudragit RL100, Carbapol 934, Ethyl cellulose were prepared by solvent casting method using ethanol , water and acetone as solvents, tween 80 as solubilising agent and glycerine as plasticizer. The prepared mucoadhesive buccal films were evaluated for their physic-chemical parameters such as thickness uniformity, weight uniformity, folding endurance, drug content , surface pH, swelling index, bioadhesion, percentage moisture loss and uptake, vapor transmission rate. The formulations exhibited good results. In – vitro drug release studies were conducted for OLM loaded films in phosphate buffer (pH 6.8) solution. The drug release was in the range of 67 to 90 % in 6hrs.. Stability studies were carried out with selected formulation. In- vivo release was evaluated in rabbits by patch test and it showed good correlation with the in-vitro release data. Drug release was found to be diffusion following zero order as per kinetic studies.

  Aceclofenac is a non-steroidal anti-inflammatory, analgesic and antipyretic drug used in the treatment of rheumatic arthritis, post-traumatic pain, masculo-skeletal and joint disorder. Problem with this drug is poor solubility in water hence poor bioavailability after oral administration. The objective of the research work was to develop and evaluate mouth dissolving tablets of Aceclofenac by using sublimation technique. The sublimation technique is used to increase the porosity of the tablets in which camphor was used as subliming agents which in turn forms the porous structure on the surface of tablets after sublimation. Aspartame was used as sweetening agent. The formulated tablets were evaluated for different parameters like weight variation, hardness, friability, drug content, disintegration time, wetting time, water absorption ratio, and In-vitro dissolution studies. Based on the results, formulation F-3 & F-6 containing Crosprovidon and Kyron T-314 10% concentration as superdisintegrants showed the least wetting time of about 17 & 13 sec, disintegration time of 25 & 18 sec and drug release of about 89.13 & 99.14% within 180 sec respectively and was found to be promising and selected as the optimized formulations. From the results, it was concluded that mouth dissolving tablets with improved Aceclofenac dissolution could be prepared by sublimation of tablets containing suitable subliming agent. Key words: Aceclofenac, mouth dissolving tablets, in-vitro, sublimation technique.