Design and development of buccal mucoadhesive drug deliverysystem for perindopril

The main objective of present study was to develop a buccal mucoadhesive drug delivery system for perindopril.Perindopril buccal mucoadhesive patches were developed by solvent casting technique using hydroxy propylmethylcellulose [HPMC], polycarbophil, sodium carboxymethylcellulose [SCMC] and sodium alginate as polymersfor extended release of perindopril. Glycerine and DMSO were used as plasticizer and penetration enhancerrespectively. Ethanol, methanol and dichloromethane were used as solvents. FTIR and DSC studies revealed nointeraction between drug and polymers. The drug content in the perindopril patches was found to be uniform. The filmsexhibited good physical and mechanical properties. The surface pH of all the patches was within salivary pH range.Residual solvent content in patches are below the tolerated limits. The patches were found to have an extended releaseof the drug upto a period of 12 hours during ex vivo permeation studies with non-Fickian diffusion mechanism. Thepresent study demonstrated the possibility of designing a buccal drug delivery system for perindopril

Improved dissolution and micromeritic properties of naproxen from spherical agglomerates: preparation, in vitro and in vivo characterization

Naproxen, an anti-inflammatory drug, exhibits poor aqueous solubility, which limits the pharmacological effects. The present work was carried out to study the effect of agglomeration on micromeritic properties and dissolution. Naproxen agglomerates were prepared by using a three solvents system composed of acetone (good solvent), water (non-solvent) and dichloromethane (bridging liquid). Differential Scanning Calorimetry (DSC) results showed no change in the drug after crystallization process. X-Ray Powder Diffraction (XRPD) studies showed the sharp peaks are present in the diffractograms of spherical agglomerates with minor reduction in height of the peaks. The residual solvents are largely below the tolerated limits in the agglomerates. Scanning Electronic Microscopy (SEM) studies showed that agglomerates were spherical in structure and formed by cluster of small crystals. The agglomerates exhibited improved solubility, dissolution rate and micromeritic properties compared to pure drug. Anti-inflammatory studies were conducted in Wistar strain male albino rats and naproxen agglomerates showed more significant activity than the pure drug.

Naproxeno, fármaco anti-inflamatório, apresenta baixa solubilidade em água, o que limita os efeitos farmacológicos. O presente trabalho foi realizado para estudar o efeito da aglomeração nas propriedades micromeríticas e na dissolução. Aglomerados de naproxeno foram preparados por meio da utilização de sistema de três solventes composto de acetona (bom solvente), água (não-solvente) e diclorometano (líquido de ligação). A DSC não resulta mostrou nenhuma mudança na droga depois de processo de cristalização. Estudos de difração de Raios X do Pó (XRPD) mostraram picos agudos nos difratogramas de aglomerados esféricos, com redução mínima dea altura dos picos. Os solventes residuais estão amplamente abaixo dos limites tolerados nos aglomerados. Os estudos de Microscopia Eletrônica de Varredura (SEM) mostraram que esses aglomerados eram de estrutura esférica e formados por grupos de pequenos cristais. Os aglomerados apresentaram solubilidade, taxa de dissolução e propriedades micromeríticas aprimoradas em comparação com o fármaco puro. Estudos anti-inflamatórios foram conduzidos em ratos Wistar albinos masculinos e os aglomerados de naproxeno mostraram atividade mais significativa do que o fármaco puro.