Enhanced hypotensive effect of nimodipine solid dispersions produced by supercritical CO2 drying

被引：19

作者：

Riekes, Manoela Klueppel ^{[1
]}

Caon, Thiago ^{[1
]}

da Silva, Jose, Jr. ^{[2
]}

Sordi, Regina ^{[3
]}

Kuminek, Gislaine ^{[1
]}

Bernardi, Larissa Sakis ^{[4
]}

Rambo, Carlos Renato ^{[2
]}

Maduro de Campos, Carlos Eduardo ^{[5
]}

Fernandes, Daniel ^{[6
]}

Stulzer, Hellen Karine ^{[1
]}

机构：

[1] Univ Fed Santa Catarina, Programa Posgrad Farm, BR-88040970 Florianopolis, SC, Brazil

[2] Univ Fed Santa Catarina, Programa Posgrad Engn Elet, BR-88040970 Florianopolis, SC, Brazil

[3] Univ Fed Santa Catarina, Programa Posgrad Farmacol, BR-88040970 Florianopolis, SC, Brazil

[4] Univ Estadual Centro Oeste, Dept Ciencias Farmaceut, BR-85040080 Guarapuava, Brazil

[5] Univ Fed Santa Catarina, Programa Posgrad Fis, BR-88040970 Florianopolis, SC, Brazil

[6] Univ Estadual Ponta Grossa, Programa Posgrad Ciencias Farmaceut, BR-84030900 Ponta Grossa, Brazil

来源：

POWDER TECHNOLOGY | 2015年 / 278卷

关键词：

Nimodipine; PVP K-30; Solid dispersions; Supercritical fluid technology; WATER-SOLUBLE DRUGS; ORAL BIOAVAILABILITY; PHYSICOCHEMICAL CHARACTERIZATION; DISSOLUTION RATE; SOLVENT EVAPORATION; FLUID TECHNOLOGIES; PARTICLE DESIGN; PHYSICAL STATE; ANTISOLVENT; TABLETS;

D O I：

10.1016/j.powtec.2015.03.029

中图分类号：

TQ [化学工业];

学科分类号：

0817 ;

摘要：

Solid dispersions of nimodipine and PVP K-30 were prepared by supercritical fluid technology at three drug:carrier ratios (1:9, 2:8,3:7, w/w). The samples were characterized by X-ray powder diffraction, infrared spectroscopy and scanning electron microscopy, and evaluated by means of their solubility, dissolution rate and hypotensive effect. The solid dispersion with the highest amount of PVP K-30 (SD 1:9) presented an amorphous state, a porous surface and hydrogen bonds between nimodipine and the carrier. On the other hand, the other solid dispersions were semicrystalline. All formulations enhanced the solubility and dissolution rate of nimodipine and the best results were found for SD 1:9. This formulation promoted an increase of more than 1300% in the solubility of nimodipine, besides releasing 100% of the drug within 5 min. When submitted to in vivo studies SD 1:9 decreased significantly the mean arterial pressure and also reduced its phenylephrine-induced increase. (C) 2015 Elsevier B.V. All rights reserved.

引用

页码：204 / 210

页数：7

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