A. R. Shabaraya

Gastroretentive systems have the unique quality to remain in the gastric region for several hours. Due to this they prolong the gastric residence time of the drug significantly. Floating microspheres possess the advantage of better flowing properties attributed to the use of low density polymers. Clarithromycin is a broad-spectrum antibiotic and extensively absorbed orally. It is used in the eradication of H. Pylori infection combined with an acid suppressing agent. Clarithromycin floating microspheres were prepared using polymer Ethyl Cellulose in different concentrations by solvent evaporation method. The FTIR studies showed no interaction between drug and polymers. The floating microspheres were evaluated for angle of repose, percentage yield, particle size, SEM, buoyancy percentage, drug content, percentage drug entrapment, in-vitro dissolution studies, kinetics of drug release and stability studies. Formulation F3 was found to be the best formulation showing the highest degree of sustained release that is 73.86% at the end of 12 hours. Formulations were seen to follow zero order release profile and Korsemeyer-Peppas model was the best fitting model. Marginal changes were observed in the drug content, buoyancy time and In-vitro dissolution studies which are insignificant. Storage conditions were carried out at 40±20C/75±5%RH for 6 months.

Sublingual administration of the drug is known as placement of the drug under the tongue and drug reaches directly in to the blood stream. The concept of formulating sublingual tablets of Prochlorperazine maleate offers suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic. Bitter taste of Prochlorperazine maleate was masked by inclusion complex with β-cyclodextrin and then sublingual tablets were prepared using various natural superdisintegrants such as hibiscus-rosa and fenugreek and synthetic superdisintegrants like Indion 414 and kyron T-314 in different concentrations by direct compression method. Prepared tablets were subjected to different evaluation parameters such as hardness, thickness, friability, weight variation, drug content uniformity, in-vitro disintegration time, water absorption ratio, wetting time, in vitro dissolution studies and stability studies are carried out by using best formulation. Overall, formulation F3 (10 mg of Indion 414) and F9 (10 mg of Hibiscus-rosa) based on disintegration time, wetting time and drug release were found to be an excellent formulations. Hence It was found that there was no significant difference between F3 and F9, which shows that natural superdisintegrants (10 mg of Hibiscus rosa) is as good as synthetic superdisintegrants (10 mg of Indion 414). Hence it proves that synthetic disintegrant can be replaced by natural disintegrants due to easy availability and compatibility.

Periodontitis is an inflammatory response to the overgrowth of anaerobic pathogenic organisms such as spirochetes and bactericides in the sub gingival plaque. If it is unchecked, results in the destruction of the bone and soft tissues supporting to the tooth, which leads to tooth loss. For treatment of these diseases we are preparing local drug delivery system of Levofloxacin dental strips. This helps to get local as well as sustained action against organism. Here we are used HPMC and ethyl cellulose as rate controlling polymer and dibutyl phthalate as plasticizers. Which shows tensile strength varies from 1.55-1.87 kg/cm2,the thickness varies from 0.33±0.002mm to 0.38±0.008mm. The weight variation and drug content was found to be uniform in all the formulation and folding endurance was found to be more than 200 in all the strips. In vitro dissolution was carried out by using static dissolution method and in vitro anti- bacterial activity was carried out by E.coli and S.aureus the zone of inhibition was calculated. The stability study was carried out under accelerated condition to found out the stability of all the formulation.

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.

Dental implant is a pharmaceutical device in the form of strip with very small loading and size of 0.25 sq cm. For site-specific one-time continuous delivery of Gatifloxacin an antimicrobial compound with excellent activity against anaerobic micro-organism in the treatment of periodontal disease was prepared by solvent casting technique using ethyl cellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose K4M and Eudragit RL-100 with dibutylphthalate as plasticizer. The physicochemical parameters like thickness, weight variation, content uniformity and release characteristics were evaluated The drug release was initially high on day one to achieve immediate therapeutic level of drug in pocket, followed by marked fall in release by day two, and progressive moderate release profile to maintain therapeutic level following anomalous transport mechanism. Formulation F6 released 97.34% of drug at the end of 144 h and was considered as best formulation. In vitro antibacterial activity was carried out on Streptococcus mutans .