Objective: The objective of the present work was the preparation and evaluation of mouth dissolving tablets (MDTs) of meloxicam using natural superdisintegrants. Methods: Meloxicam is BCS Class II (low soluble, and high permeable) drug increasing the dissolution properties of the poorly water-soluble drug meloxicam using a solid dispersion method (solvent evaporation method). Solvent evaporation method using drug and carrier as polyethylene glycol (PEG)-6000 and PEG-15,000 the ratio of 1:1, 1:2 (drug:carrier), and acetone as solvent. In house prepared banana powder were used as natural superdisintegrant. Manufacturing of MDT was done by the direct compression method. In this MDTs, various excipients were used such as mannitol used as the diluent, sodium saccharin used as a sweetening agent, Avicel pH-102 used as a binding agent, and talc and sodium lauryl sulfate (SLS) used as lubricant and glidant. The best formula of the tablet was selected according to the disintegration time (DT) and friability tests. Results: The results have shown that an increase in the meloxicam solubility was obtained using solid dispersion with the solvent evaporation method using PEG-15000 as a carrier in the ratio of 1:2 (drug:carrier). Taste masking was also done by a solid dispersion method. Tablet prepared with in house prepared banana powder gave less DT (70 s) as compared to tablet prepared with branded banana powder (80 s), but formulation F5 failed in friability testing. Improved strength of tablet obtained using SLS (<1%) also showed an increase in the dissolution performance of the tablet in formulation F6. This F6 formulation having 10% natural super disintegrating agent (in house prepared banana powder) has shown 99% cumulative drug release within 18 min. It also passed the friability test. Conclusion: Accordingly, the solubility of meloxicam was successfully enhanced through solid dispersion with carrier PEG-15,000 and formulated as a MDT to improve its oral absorption. PEG has also been used as a taste masking agent in these formulations. It was concluded that in house banana powder had excellent DT as compared to branded banana powder. Banana powder is “economical” and “easily available” than other commonly used synthetic superdisintegrants. The process of banana powder preparation is eco friendly. The meloxicam MDT formulated with natural superdisintegrant in house prepared banana powder found to pass all pharmacopeial tests.
Objective: The objective of this study was to assess the development of ethosomal drug delivery system for site-specific topical delivery of rizatriptan benzoate (RBZ) for sustained action.Methods: In the present study ethosomes were prepared using the cold method. The formulation was optimized using 33 full factorial designs. The lipid concentration (X1), ethanol concentration (X2) and stirring speed (X3) were selected as independent factors and the vesicle size (Y1) and % entrapment efficiency (Y2) were selected as dependent variables.Results: The equation of multiple regression revealed that there was no significant interaction among factors. The lipid concentration had a positive effect on vesicle size while ethanol concentration and stirring speed had a negative effect. For entrapment efficiency, all factors showed a positive effect while lipid concentrative found to be the main influencing factor. The formulation F4E459 (4% SPC, 45% v/v ethanol 900 RPM), which was characterized by optimum vesicle size (5.5 µm) and high entrapment efficiency (93.32%), was considered to be an optimal formulation. The scanning electron microscopy (SEM) results showed that RBZ ethosome have a smooth surface. The polydispersity index (PI) and zeta potential of the optimized formulation were found to be 0.493±0.021and–21.3 mV respectively. In vitro permeation through rat abdominal skin from the ethosomal gel followed Higuchi diffusion model over a period of 8 h.Conclusion: The results obtained in this research work clearly indicated a promising potential of ethosomal carrier system of RBZ for migraine treatment with a topical approach for sustained action.
Objective: To develop and evaluate the mucoadhesive microsphere using combinations of natural polymers chitosan and xanthan gum for sustained release. Methods: In the present work mucoadhesive microspheres were prepared by using natural polymers like chitosan and xanthan gum by using the emulsion chemical cross-linking method. Chemical cross-linking was done by using glutaraldehyde. The 22 factorial design was employed to show the effect of cross-linking agent and processing factor-like stirring and speed. Prepared microspheres were evaluated for their particle size, surface morphology, drug entrapment efficiency, in vitro drug release, swelling index, and mucoadhesive strength. Results: The size of microspheres of factorial batches were in the range of 26-46 µm. The swelling index was showed in the range of 1.51-1.66 percentage. The equation of multiple regression revealed that there was significant interaction among factors. The glutaraldehyde concentration had a positive effect on % entrapment efficiency, % cumulative drug release and % mucoadhesion. Stirring speed showed a negative impact on % entrapment efficiency, % cumulative drug release and % mucoadhesion. The interactive effect of glutaraldehyde concentration and the stirring speed was found to be positive for % entrapment efficiency and % cumulative drug release. In vitro drug release study of optimized formulation F2 show 96 % of drug release with 6 h indicating sustained release behavior with diffusion mechanism. The SEM image of the optimized batch was spherical with a porous surface. Conclusion: The results obtained in this research work indicated that a promising potential of chitosan and xanthan gum combination for the preparation of the mucoadhesive microsphere of Racecadotril.
Dicyclomine hydrochloride have major problem to its bitter taste. Due to its bitter taste pediatric and geriatric patients have less acceptability. The objective of present work was preparation and evaluation of chewable tablets of Dicyclomine hydrochloride by using Ion exchange resin for taste masking. Taste masking of Dicyclomine HCl was done by using weak cation exchange resin such as Tulsion 335 and Kyron T 159. When comparing drug loading capacity it noticed that Tulsion 335 showed high drug loading as compared to Kyron T 159 at 1: 5 drug –resin ratio. Maximum drug bounding was observed with 90 min swelling time and 90 min stirring time. Manufacturing of chewable tablet was done by direct compression method. In this formulation various excipients were used such as crospovidone as disintegrant, mannitol as a diluent, Sucralose as sweetener The powder blend and tablet formulation was evaluated for precompression and post compression study respectively. The results have shown maximum drug loading was obtained using Tulsion 335 as ion exchange resin in the ratio of 1:5 (drug: resign). Taste masking was evaluated with invitro threshold value.
The objectives of present investigation is to improve the solubility and rate of dissolution of poorly aqueous soluble drug lansoprazole by preparing solid dispersion with amphiphilic carrier Soluplus in 1:2 concentration by using solvent evaporation method, solvent melting method and microwave oven method and selecting the best solid dispersion. The drug and excipient compatibility study of selected solid dispersion was performed by FTIR and DSC. These study showed no interaction in drug and carrier. The sublingual tablet represents an innovative drug delivery system, sublingual tablet of lansoprazole was formulated by incorporating selected solid dispersion with combination of novel superdisintegrants and taste maskers like Indion-414 and Kyron T-314 by using direct compression method. The sublingual tablet showed the rapid disintegration within average 32 seconds. All the evaluations were performed and complies with the pharmacopoeial standards. The drug and excipient compatibility study of lansoprazole sublingual tablet was also performed by FTIR and DSC. These study showed no interaction in drug and excipients. The formulation F9 (12 % superdisintegrants) showed 98.42% of cumulative drug release within 8 min with zero order release pattern. These novel formulation lansoprazole sublingual tablet showed quick on set of action and may be found to be beneficial, convenient for pediatrics, geriatrics, and psychiatric patients and patients with swallowing difficulties and in situations where water is not available.
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