基于板蓝根中（R,S）-告伊春含量研究板蓝根加工方法

目的 研究不同干燥方法及软化切制方法对板蓝根中（R,S）-告伊春含量的影响,从而建立提升黑龙江产板蓝根质量的加工方法。方法 采用高效液相色谱法对板蓝根中（R,S）-告伊春含量进行测定,比较晒干与烘干板蓝根药材的（R,S）-告伊春含量差异,比较不同投料形式板蓝根颗粒和饮片中（R,S）-告伊春含量差异。结果 60 ℃烘干后的板蓝根药材中（R,S）-告伊春含量高于晒干的板蓝根药材,且能明显缩短板蓝根药材的产地干燥时间;经软化切制的板蓝根饮片中（R,S）-告伊春含量明显高于板蓝根粗颗粒。结论 在板蓝根产地加工过程中,可用烘干法代替晒干法;以板蓝根药材作为中成药投料,建议采用软化切制后的板蓝根饮片。     

Elucidation of Solution State Complexation in Wet-Granulated Oven-Dried Ibuprofen and β-Cyclodextrin: FT-IR and 1H-NMR Studies

The effect of oven-dried wet granulation on the complexation of β-cyclodextrin with ibuprofen (IBU) in solution was investigated using Fourier transform infrared spectroscopy (FT-IR), proton nuclear magnetic resonance (¹H NMR), and molecular modeling. Granulation was carried out using 5 mL of three different granulating solvents; water, ethanol (95% v/v), and isopropanol and the granules were oven-dried at 60°C for 2 h. The granules were compared to oven-dried physical mixture and conventionally prepared complex. Phase solubility study was performed to investigate the stability of the granulation-formed complexes in solution. FT-IR was used to examine the complexation in the granules while ¹H NMR, and molecular modeling studies were carried out to determine the mechanism of complexation in the water-prepared granules. The solubility studies suggested a 1:1 complex between IBU and βCD. It also showed that the stability of the complex in solution was in the following order with respect to the granulating solvents: ethanol > water > isopropanol. The FT-IR study revealed a shift in the carboxylic acid stretching band and decrease in the intensities of the C-H bending bands of the isopropyl group and the out-of-plane aromatic ring, of IBU, in granules compared to the oven-dried physical mixture. This indicated that granules might have some extent of solid state complexation that could further enhance dissolution and the IBU–βCD solution state complexation. ¹H NMR showed that water prepared oven-dried granules had a different ¹H NMR spectrum compared to similarly made oven-dried physical mixture, indicative of complexation in the former. The ¹H NMR and the molecular modeling studies together revealed that solution state complexation from the granules occurred by inclusion of the isopropyl group together with part of the aromatic ring of IBU into the βCD cavity probably through its wider side. These results indicate that granulation process induced faster complexation in solution which enhances the solubility and the dissolution rate of poorly soluble drugs. The extent of complexation in the granules was dependent on the type of solvent used.     

Incidence of drying on microstructure and drug release profiles from tablets of MCC–lactose–Carbopol and MCC–dicalcium phosphate–Carbopol pellets

The influence of intragranular excipients (lactose or dicalcium phosphate) and the drying procedure and conditions (oven-drying and freeze-drying after freezing at -30 or -196 degrees C) on the properties of tablets of MCC-Carbopol pellets was evaluated. The drying procedure caused remarkable differences in pellet size and porosity (freeze-dried pellets were 3-fold more porous than those oven dried). Theophylline release from pellets was completed in less than 30 min and followed first-order kinetics, with a rate closely related to the intragranular porosity. The total porosity of the tablets (5-10%) was conditioned by the compression force (10-20 N), the drying procedure applied to the pellets and the coexcipient nature. Their intergranular porosity ranged inversely to the initial porosity of pellets due to the greater deformability of the most porous ones. A wide range of theophylline release rates were achieved depending on the drying procedure; tablets prepared from freeze-dried pellets sustained the release for 3h. Most profiles showed a bimodal kinetics with an initial zero-order release (while the tablets did not completely disintegrate) that changed, after a certain time, to a first-order kinetics. The intergranular porosity determined drug release rate up to disintegration. Then, the release kinetics became first-order and the rate constant, which was conditioned by the intragranular porosity, showed a complex dependence on the drying procedure, the compression force, and the nature of coexcipient. In sum, the modulation of drug release profiles from tablets of MCC-Carbopol pellets through an adequate control of the effects of the coexcipient nature, the drying procedure of pellets, and the compression force on the inter- and intragranular porosity opens interesting possibilities to control the release of hydrosoluble drugs.