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Design And Qbd Based Development Of Orodispersible Tablet Comprising Co-crystallized Anti-migraine Drug
Project Description :

Design and qbd based development of orodispersible tablet comprising co-crystallized anti-migraine drug background & rationale: migraine is a common headache disorder characterized by recurrent attacks of moderate or severe intensity. migraine headache is prevailing, disabling and essentially treatable, but still under-estimated and under-treated. early diagnosis and treatment of migraine improves the quality of life of patient. more than 60% of synthesized drugs and 40% of drugs in development are poorly soluble and exhibits bioavailability issues. over the last decade, there has been a growing interest in pharmaceutical cocrystal design, which appears to be a promising strategy for improving the bioavailability of drugs with low aqueous solubility. cocrystallisation of drugs with coformers is a promising method for modifying the solid state properties of the drugs, such as solubility and dissolution. rapid onset and improved bioavailability are desirable and hence, there is a strong scientific and clinical need to prepare novel cocrystals possessing modified solubility and dissolution rate which is further formulated as oro-dispersible tablets to improve the treatment of acute migraine attacks and prevention of migraine. methods: drug selection was justified based on the data obtained through in silico screening using swissadme, admet and molinspiration. cocrystals of the selected drug were prepared by solvent evaporation method. the solubility and melting point of the crystalline phase was determined. the potential cocrystals was characterized by ir, dsc and xrpd. other pharmaceutical properties like solubility and dissolution rate were also evaluated. orodispersible tablets of the prepared cocrystals were formulated, optimized using qbd approach and evaluated. results and discussion: the cocrystals that were prepared revealed the variation in melting point and solubility. the analysis of ir indicated the shifting of characteristic bands of pure drug. the changes in 2θ values in xrpd was observed. dsc spectra of cocrystals indicated altered endotherms corresponding to the melting point. the proposed technique was found to enhance the drug solubility by 7 folds. the cocrystals exhibited faster dissolution rate about 54% increase as compared to pure drug and 20% increase as compared to marketed formulation as shown in figure 1. the use of box-behnken response surface methodology with three factors and two levels helped to found the relationship between factors and responses. seventeen formulations offered by the box–behnken design through design expert software (version 11) were prepared. all the formulations were characterized for parameters such as, hardness, thickness, weight variation, friability, dissolution and disintegration time. the final formula was prepared based on predicted and observed values. the prepared batch was compared with dissolution rate of pure drug and marketed formulation as shown in figure 2. the orodispersible tablets of cocrystals were successfully prepared by direct compression method using superdisintegrant with improved disintegration time and dissolution rate. benefits to society/ cost benefits analysis : 1. as the solubility of drug was reported in methanol (solvent) but we have synthesized the cocrystals using ethanol as a solvent which is considered as a green solvent that is solvents with low toxic potential and less environmental hazardous as compared to methanol. 2. the proposed technique was found to enhance the 7 folds solubility. through this experimental evaluation the solubility, dissolution rate and bioavailability also increases which will lead to increase in the therapeutic efficacy and ultimately reduce the cost of the therapy as compared to conventional dosage form. conclusions: the model drug cocrystal with modified properties was prepared with a suitable coformer and formulated as orodispersible tablets having faster disintegration and greater dissolution rate. thus, it can be concluded that the optimized formulation with desirable parameters can be obtained by box–behnken design with the response and variable relation. references: 1. elder d, et al., use of pharmaceutical salts and cocrystals to address the issue of poor solubility. international journal of pharmaceutics, 2013. 453(1): p. 88-100. 2. panzade p, et al., pharmaceutical cocrystals of piroxicam: design, formulation and evaluation. advanced pharmaceutical bulletin, 2017. 7(3): p. 399-408.

 
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Project Details :
  • Date : Jul 30,2022
  • Innovator : Kunika Champanerkar
  • Guide Name : Dr. Norma Rebello
  • University : University of Mumbai
  • Submission Year : 2022
  • Category : Pharmacy
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