Formulation and Evaluation of Mouth Dissolving Film of Prochlorperazine Maleate

This research work was aimed to enhance the oral bioavailability and provide faster onset of action of Prochlorperazine maleate (used for the treatment nausea and vomiting) by formulating its mouth dissolving film (MDF). Prochlorperazine belongs to BCS II and oral bioavailability of it’s about 11-15%. The MDF of Prochlorperazine  maleate was prepared by solvent casting  method using HPMC (film forming agent),Glycerol (plasticizer), Betacyclodextrin (solubilizing agent), Citric acid (saliva stimulating agent), Mannitol (sweetening agent). The formulation was optimized by two factors, three levels (32) was used for the formulation optimization of fast dissolving film of Prochlorperazine maleate and experimental trials are performed on all 9 formulation. In which the amount of HPMC, Glycerol were selected as independent variables (factor) varied at three different level: low (-1), medium (0), and high (+1) levels. The drug release and disintegration time used as dependent variables (response). and formulation was evaluated for weight variation, thickness, folding endurance, drug content, in- vitro disintegration, in vitro dissolution study and stability study. Based on results it was concluded that MDF (F3) showed enhanced bioavailability and faster onset of action. Keywords: Prochlorperazine maleate, Mouth dissolving film, bioavailabilit

FORMULATION AND OPTIMIZATION OF FAST DISSOLVING TABLETS OF PROMETHAZINE THEOCLATE USING 32 FACTORIAL DESIGN

The fast dissolving tablets of Promethazine Theoclate were prepared by sublimation technique, using 32 full factorial design. This research work aimed to study and to develop a unique drug delivery system for immediate release of drugs which can dissolve readily when placed in the oral cavity. The different subliming agents (Camphor, Urea and Menthol) in varying concentration (5-15% w/w) were used to develop the tablets. Total 12 formulations were prepared and evaluated for pre-compression and post compression characteristics. The optimization of the batches was carried out using 32 full factorial design and results of polynomial equation were analyzed using ANOVA and regression analysis. By the use of desirability approach final optimized formulation was prepared

FORMULATION AND EVALUATION OF BILAYER TABLET OF METRONIDAZOLE AND DICYCLOMINE HYDROCHLORIDE FOR TREATMENT OF IRRITABLE BOWEL DISEASE

The aim of the present study was to prepare bi-layer tablet of Metronidazole and Dicyclomine Hydrochloride for the effective treatment of Irritable Bowel Disease. Metronidazole and Dicyclomine Hydrochloride were formulated as immediate and sustained release layer respectively. The rational for formulation of bi-layer tablet of these two combinations was Metronidazole (immediate release) is strong antibiotic usually applied for antidiarrheal to treat inflammation of the large intestine and Dicyclomine Hydrochloride (Sustained release) is anticholinergic drug primarily used for irritable bowel disease. Bilayer tablet was suitable for maximizing the efficacy of drugs in irritable bowel disease

FORMULATION AND EVALUATION OF MOUTH DISSOLVING FILM OF TADALAFIL

This research work was aimed to enhance the oral bioavailability and provide faster onset of action of Tadalafil (used for the treatment of the erectile dysfunction (ED) and pulmonary arterial hypertension) by formulating its mouth dissolving film (MDF). Tadalafil belongs to BCS class II and the oral bioavailability of it’s about 28%. The MDF of Tadalafil was prepared by solvent casting method using HPMC-E5 (film forming agent), Methyl cellulose (thickening agent), Propylene glycol (plasticizer), Tween-80 (solubilizing agent), Microcrystalline cellulose (disintegrating agent), Citric acid (saliva stimulating agent), Sucrose (sweetening agent), Vanillin (flavoring agent), EDTA disodium (preservative). The formulation was optimized by two factors, three level (23) full factorial design using concentration of Plasticizer (X1) and concentration of film forming agent (X2) as independent variables and formulation was evaluated for uniformity of mass, thickness, folding endurance, drug content uniformity, in-vitro disintegration, in-vitro drug dissolution study and stability study. Based on results it was concluded that MDF (F5) showed enhanced bioavailability and faster onset of action as compared to available tablet dosage form

Repurposing Thioridazine (TDZ) as an anti-inflammatory agent

Nuclear factor-kB (NF-kB) is a crucial transcription factor in the signal transduction cascade of the inflammatory signaling. Activation of NF-κB depends on the phosphorylation of IκBα by IκB kinase (IKKβ) followed by subsequent ubiquitination and degradation. This leads to the nuclear translocation of the p50- p65 subunits of NF-κB, and further triggers pro-inflammatory cytokine gene expression. Thus, in the need of a more effective therapy for the treatment of inflammatory diseases, specific inhibition of IKKβ represents a rational alternative strategy to the current therapies. A computer-aided drug identification protocol was followed to identify novel IKKβ inhibitors from a database of over 1500 Food and Drug Administration (FDA) drugs. The best scoring compounds were compared with the already known high-potency IKKβ inhibitors for their ability to bind and inhibit IKKβ by evaluating their docking energy. Finally, Thioridazinehydrochloride (TDZ), a potent antipsychotic drug against Schizophrenia was selected and its efficiency in inhibiting IκBα protein degradation and NF-κB activation was experimentally validated. Our study has demonstrated that TDZ blocks IκBα protein degradation and subsequent NF-κB activation to inhibit inflammation. Thus, it is a potential repurposed drug against inflammation