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Objective: Chlorpheneramine maleate is a first-generation antihistamine drug used in the treatment of allergic conditions like rhinitis, urticaria, and cough cold, etc. In present work, the challenge has been made to develop an orally disintegrating tablet of chlorpheneramine maleate with an increase in bioavailability and patient compliance. Methods: The sublimation technique was used to prepare orally disintegrating tablets. Porous tablet prepared after sublimation of camphor at 60 °C in a hot air oven for 60 min. In the research work, 32full factorial design used to find out the effect of two variables like the amount of Crospovidone and Croscarmellose sodium. Results: All prepared formulations were analyzed for various parameters. DSC of pure drug and optimized formulation A (9) showed purity of sample and compatibility of all ingredients with each other. In FTIR study of pure drug and optimized formulation A (9) no major shifts were seen. An optimized formulation (A9) was found to have good hardness (3.2 kg/cm2), friability (<1%), disintegration time (26 s), % drug release (99.77 %) within 6 min. Conclusion: The result obtained showed that orally disintegrating tablet of chlorpheneramine maleate enhances dissolution rate, improves bioavailability which will improve patient compliance.
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Objective: The main aim of the present research work was to formulate fast dissolving tablets of famotidine by direct compression method and to evaluate the effect of synthetic super disintegrating agent on drug release pattern. Methods: The fast dissolving tablets were prepared by using crospovidone, croscarmellose sodium, sodium starch glycolate as superdisintegrants (2, 4 and 6 %w/w), mannitol 20 % and microcrystalline cellulose (44, 46 and 48 % w/w) as a directly compressible vehicle. All the prepared tablets were evaluated for hardness, friability, drug content uniformity, weight variation, disintegrating time, wetting time and in vitro drug release studies. Results: All the prepared fast dissolving tablets formulations were within the Pharmacopoeial standards limits. Based on in vitro drug release studies (>90 % within 30 min), the optimised formulations were optimised tested for the short term stability (at 40 ˚C/75% RH for 3 mo) and drug excipient interaction (fourier transform infrared spectroscopy). Conclusion: Hence, formulation prepared with 6 % w/w of crosspovidine and 44 % w/w of microcrystalline cellulose as emerged as the overall best formulation (>90 % within 30 min) compared to marketed product (>70 % within 30 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro drug release (p<0.05).
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@#The surface solid dispersion of honokiol was prepared by melting method with croscarmellose sodium as carrier to improve the dissolution rate of honokiol, taking the advantage of its low melting point. The dissolution rate and stability test of surface solid dispersion of honokiol were carried out. Its physical properties were then investigated by DSC, PXRD and SEM analysis. The results indicated that the dissolution rate of honokiol from sodium solid dispersion was more than 90% at 15 min while its mean dissolution time was significantly decreased. Honokiol was distributed on the surface of croscarmellose sodium in the form of microcrystal; moreover, its dissolution behavior didn′t change significantly after six months of stability tests. Therefore, surface solid dispersion of honokionl could be prepared by simple process. The formed solid dispersion achieved high drug loading and fast in vitro dissolution rate, which could provide a novel idea for developing solid preparations of honokiol.
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In this study, solid dispersion system of magnolol in croscarmellose sodium was prepared by using the solvent evaporation method, in order to increase the drug dissolution. And its dissolution behavior, stability and physical characteristics were studied. The solid dispersion was prepared with magnolol and croscarmellose sodium, with the proportion of 1∶5, the in vitro dissolution of magnolol solid dispersion was up to 80.66% at 120 min, which was 6.9 times of magnolol. The results of DSC (differential scanning calorimetry), IR (infra-red) spectrum and SEM (scanning electron microscopy) showed that magnolol existed in solid dispersion in an amorphous form. After an accelerated stability test for six months, the drug dissolution and content in magnolol solid dispersion showed no significant change. So the solid dispersion prepared with croscarmellose sodium as the carrier can remarkably improve the stability and dissolution of magnolol.
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<p><b>OBJECTIVE</b>To formulate diclofenac sodium as fast dissolving tablets (FDTs) using fenugreek gum as a natural superdisintegrant which also possess anti-inflammatory activity.</p><p><b>METHODS</b>An attempt was made to extract the fenugreek gum and evaluated it for various physicochemical characterizations. The swelling index and viscosity of fenugreek gum was 221% and 293.4 mpa.s respectively. FDTs of diclofenac sodium was formulated by direct compression technique using different concentrations (1%-6%, w/w) of fenugreek gum as a natural superdisintegrant and compared with renowned synthetic superdisintegrants like sodium starch glycolate and croscarmellose sodium. The anti-inflammatory activity of a formulation was evaluated with carrageenan induced experimental rats.</p><p><b>RESULTS</b>The formulated tablets were evaluated for various physical tests like weight variation, friability, hardness and results complied with the limits. The drug release from all the formulations ascertained first order kinetics. Among all the formulations F3 containing fenugreek gum with the concentration of 6% produced least disintegrating time 21 seconds resulting in higher drug release rate 93.74% at the end of 25 min. Hence, it was considered as optimized formulation. The present study revealed that the fenugreek gum as a natural superdisintegrant showed better disintegrating property than the most widely used synthetic superdisintegrants like sodium starch glycolate and croscarmellose sodium in the formulations of FDTs.</p><p><b>CONCLUSIONS</b>The results suggested that the fenugreek gum act as a good super disintegrating agent and it showed promising additive anti-inflammatory activity with diclofenac sodium.</p>
ABSTRACT
Objective: To formulate diclofenac sodium as fast dissolving tablets (FDTs) using fenugreek gum as a natural superdisintegrant which also possess anti-inflammatory activity.Methods:physicochemical characterizations. The swelling index and viscosity of fenugreek gum was 221% and 293.4 mpa.s respectively. FDTs of diclofenac sodium was formulated by direct compression technique using different concentrations (1%-6%, w/w) of fenugreek gum as a natural superdisintegrant and compared with renowned synthetic superdisintegrants like sodium starch glycolate and croscarmellose sodium. The anti-inflammatory activity of a formulation was evaluated with carrageenan induced experimental rats.Results:An attempt was made to extract the fenugreek gum and evaluated it for various friability, hardness and results complied with the limits. The drug release from all the formulations ascertained first order kinetics. Among all the formulations F3 containing fenugreek gum with the concentration of 6% produced least disintegrating time 21 seconds resulting in higher drug release rate 93.74% at the end of 25 min. Hence, it was considered as optimized formulation. The present study revealed that the fenugreek gum as a natural superdisintegrant showed better disintegrating property than the most widely used synthetic superdisintegrants like sodium starch glycolate and croscarmellose sodium in the formulations of FDTs. The formulated tablets were evaluated for various physical tests like weight variation, Conclusions: The results suggested that the fenugreek gum act as a good super disintegrating agent and it showed promising additive anti-inflammatory activity with diclofenac sodium.
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In the present work, orodispersible tablets of Alfuzosin Hcl were prepared by direct compression and sublimation methods with a view to enhance patient compliance. In these methods, varying concentrations of crospovidone, sodium starch glycolate and croscarmellose sodium of 3.3, 6.6 and 10% w/w were used, along with camphor used as subliming agent in sublimation method. The prepared batches of tablets were evaluated for hardness, friability, drug content, wetting time, dispersion time, disintegration time and dissolution studies. Based on disintegration time (approximately 13-18 seconds) all the promising formulations (from each method) were tested for in-vitro drug release pattern (in pH 6.8 phosphate buffer), drug-excipient interaction (FTIR spectroscopy) and short term stability studies. Among the promising formulations, the formulation F4 and F14 containing 10% w/w Crospovidone emerged as the overall best formulation (t50%1.79 and 1.21 minutes) based on drug release characteristic (in pH 6.8 phosphate buffer) compared to controlled formulation F1 (t50% >10 minutes).
ABSTRACT
The selection of a suitable superdisintegrant for a rapidly disintegrating dosage form is of the utmost importance, since disintegration time (DT) is a critical parameter. An experimental design was implemented, to find out the effects of superdisintegrants (sodium starch glycolate, crospovidone, croscarmellose sodium and methacrylic copolymer with divinyl benzene), at 2, 4, 6% w/w, on tablet hardness, with respect to DT. Methacrylic copolymer with divinyl benzene (at 4 wt%) was selected as the best superdisintegrant, adequate for the formulation of dispersible Tramadol tablets. With increasing hardness, there was a considerable increase in DT at all concentrations of superdisintegrants. A combination of crospovidone and methacrylic copolymer with divinyl benzene showed a remarkable drop in DT to 0.33 min. The stability of the batch with lowest DT was also tested under various conditions and the results suggested that there was no degradation over the test period.