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      Characterization of nifedipine solid dispersions

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      International Journal of Pharmaceutics
      Elsevier BV

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          Abstract

          The sublingual administration of nifedipine (NIF) is currently used in clinical practice. The sublingual administration of NIF solid dispersions (SD), by using a suitable dispenser, appears an interesting approach in the treatment of moderate and severe hypertensive emergencies. With this aim nine SD made of NIF and a low viscosity hydroxypropylmethylcellulose (HPMC) in different ratio were prepared by means of spray-drying technique and their structure was studied. Moreover, the drug dissolution properties from SD were verified. The characteristic peaks of crystalline NIF were not detectable by using the X-ray analysis when the NIF/HPMC ratios were lower than 50/50 w/w. In thermograms obtained from SD, the NIF melting endothermic peak disappeared when NIF/HPMC ratios were lower than 30/70 w/w; the experimental Tg values of SD were lower than the Tg values predicted by Gordon Taylor equation suggesting some type of non-ideality of mixing. In the SD FTIR spectra the NH stretching vibrations and the C=O stretch in esteric groups of NIF shift to free NH and C=O regions indicating the rupture of intermolecular hydrogen bond in the crystalline structure of NIF. The prepared SD improved the NIF dissolution rate in comparison with that of commercial NIF or NIF/HPMC physical mixtures. Moreover, the concentration of NIF in the dissolution medium increased decreasing the NIF content.

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          Influence of water-soluble polymers on the dissolution of nifedipine solid dispersions with combined carriers.

          The objective of this investigation was to clarify the influence of water-soluble polymers on the dissolution behavior of nifedipine from solid dispersions with combined carriers. All the solid dispersions of nifedipine were prepared by the fusion method using nicotinamide and 4 different water-soluble polymers, hydroxypropylmethyl-cellulose (HPMC), polyvinylpyrrolidone (PVP), partially hydrolyzed polyvinyl alcohol (PVA) and pullulan. HPMC, PVP or PVA dissolved in the fused liquid of nicotinamide and operated efficiently on the amorphous formation of nifedipine in solid dispersions. In dissolution studies, the drug concentration for these dispersions increased to more than twice intrinsic drug solubility. The rank order of the drug concentration was HPMC > PVP > PVA. However, since pullulan did not dissolve in the fused nicotinamide, nifedipine was present as a crystalline state in the solid dispersion; the supersaturation behavior of the drug was scarcely observed. The compatibility, namely, the solubility and miscibility, between nicotinamide or nifedipine and the polymers, was determined by differential scanning calorimetry using the mixtures treated with fusing and subsequent rapid cooling. Both HPMC and PVP exhibited high compatibility not only with nicotinamide but also with nifedipine. The crystallization behavior of nifedipine from a supersaturated solution containing nicotinamide or the polymers was studied. The inhibitory effect of HPMC or PVP for drug crystallization was evident, which would be related not to the solubilizing effect but to the adhesive force of the polymer for the drug. Therefore, it was understood that the use of a polymer with high compatibility and adhesion with nifedipine provides a high supersaturation level of the drug in dissolution. Further, the solubility parameter was found to be useful for selecting a suitable polymer as a component of combined carriers.
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            Crystal structures of calcium channel antagonists: 2,6-dimethyl-3,5-dicarbomethoxy-4-[2-nitro-, 3-cyano-, 4-(dimethylamino)-, and 2,3,4,5,6-pentafluorophenyl]-1,4-dihydropyridine

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              Comparative study of buccoadhesive formulations and sublingual capsules of nifedipine.

              The pharmacodynamics of nifedipine administered via the oral mucosa was investigated in hypertensive patients. The effect of two buccoadhesive formulations, tablets and films, was compared with the commercially available sublingual capsule in a complete cross-over study in six patients. All three formulations elicited onset of action 10 min after administration. The sublingual capsule and the buccoadhesive film revealed peak response at 30 min. The buccoadhesive tablet, however, exhibited a delayed peak response at 45 min. Analysis of variance indicated that, although time-dependent differences in the formulations were suggested, there was no significant difference in the overall effect produced by the three formulations. The results of the study suggest that the buccoadhesive formulations of nifedipine were comparable in performance with the sublingual capsule.
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                Author and article information

                Journal
                International Journal of Pharmaceutics
                International Journal of Pharmaceutics
                Elsevier BV
                03785173
                August 2002
                August 2002
                : 242
                : 1-2
                : 313-317
                Article
                10.1016/S0378-5173(02)00173-4
                12176270
                3e936624-fada-4125-9535-9b3e52370100
                © 2002

                https://www.elsevier.com/tdm/userlicense/1.0/

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