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@#In order to guarantee the quality of traditional Chinese medicines (TCMs), the crystallization transformation of complex extracts of TCMs and the influence of solid form on their physicochemical properties were studied.The extract of total flavonoids from Pueraria lobata was taken as a model.Crystallization transformation happened when lofting under different conditions, and the intrinsic dissolution tests were carried out.It was found that humidity was the key factor to induce crystallization of total flavonoids from Pueraria lobata.The greater the wettability was, the more the crystallization was.The dissolution rate of total flavonoids from Pueraria lobata with the most crystallization amount significantly decreased by 96.51% compared to the sample without crystallization.After further simulating the preparation process of total flavonoids from Pueraria lobata, it was found that the wet granulation process with introduced water would also lead to crystallization and reduced dissolution rate.As for all crystallization samples, there was an inversely proportional relationship between the dissolution rates and the amount of crystallization.The risk of crystallization existed both in the storage and preparation process of TCM extracts.Crystallization would significantly affect the dissolution rate, and thus the quality of TCM products.In this study, the crystallization transformation of amorphous complex TCM extracts was discovered, and the effect of the crystallization transformation on its dissolution behavior was systematically studied, which provides a new research idea for assuring the quality of TCM products and promoting the improvement of TCM preparation level.
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@#In recent years, bio-metal organic frameworks (Bio-MOFs) synthesized with biocompatible ligands have been widely investigated as a potential drug delivery carrier due to their large specific surface area and porosity, rich host-guest intermolecular interactions, and good biocompatibility.In this review, we summarized the design methods of Bio-MOFs including structural and toxic factors, as well as a variety of drug loading methods including click chemistry, with particular focus on recent research advances in Bio-MOFs for pulmonary drug delivery systems, improving pharmaceutical properties of drugs, sustained and controlled drug release, stimulation response and targeted drug delivery systems.Finally, we summarized the bottlenecks that constrain the development of Bio-MOFs in clinical studies of actual pharmaceutical formulations and their future directions for approved formulations, aiming to provide some theoretical reference for promoting the application of Bio-MOFs in drug delivery systems.
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@#Topical preparations for skin, including the commonly used dosage forms of ointments, creams, gels, patches and plasters, are convenient and can avoid the first-pass effect of drugs.Rheological study, which describes the flow characteristics and mechanical properties of products relevant to their Critical Quality Attributes, has become the main focus for topical preparations.Liquid and solid behaviors of products are usually investigated via steady rheology as well as dynamic rheology.This article reviews the research on topical preparations for skin and the data analysis models based on two rheological methods, aiming to provide some references for the rheological evaluation of topical preparations.
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@#Lenvatinib mesylate (LF), a multi-target tyrosinase inhibitor mainly used in the treatment of a variety of cancers, has low oral bioavailability mainly due to its gelation during the dissolution process. In the current study, in order to enhance dissolution and eliminate gelation of LF, a supramolecular coamorphous system of LF-baicalein (BAI) (molar ratio, 1∶1) was prepared by rotary evaporation and characterized by PLM, PXRD, DSC and FTIR. Results indicated the formation of coamorphous system with a single Tg of 118 °C. Different from original LF crystal, no gelation phenomenon was observed during the dissolution of coamorphous LF-BAI. In addition, the dissolution rate of LF was increased by 2.2-fold after coamorphization. Meanwhile, the dissolution rate of the co-former BAI was also enhanced by more than 25.4-fold. Stability test showed that the prepared coamorphous system had a good physical stability for at least 90 days under 25 °C/ 60%RH and 40 °C /75%RH conditions.
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@#Baicalein(BE), a natural flavonoid mainly extracted from Radix Scutellaria, has comprehensive pharmacological actions such as anti-inflammation, anti-virus and anti-cancer activities. It belongs to BCS class II compound with relatively low oral bioavailability. The current study aims to improve its aqueous solubility and dissolution and hence to enhance its oral absorption by cocrystallization technique. Slurry crystallization method was employed to prepare baicalein cocrystal with co-former caffeine(CA), followed by physicochemical characterizations with DSC, XRPD and FTIR. Compared to BE and physical mixture of BE and CA, BE-CA cocrystal had a significantly higher dissolution of BE. In addition, in comparison to BE, this cocrystal achieved reduced time to peak(tmax)as well as significantly higher peak plasma concentrations(cmax)and area under the curve(AUCs)for both BE and its active metabolite baicalin(BI)in rats, suggesting enhanced the oral bioavailability of BE.
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@#Lyotropic liquid crystal system is formed by the amphiphilic molecules dissolving in polar solvents with a special geometric structure. Lamellar, cubic and hexagonal mesophases are some of the most common lyotropic liquid crystal systems. Recently, they have attracted much research attention because of their distinctive structures and physico-chemical properties(like strong bioadhesion, high permeability, low liquidity, and slow released drug), and have been widely used as carriers for drug delivery systems, especially in transdermal and mucosal fields. According to the research about lyotropic liquid crystal and nasal route of administration in our group, and the related references in recent years, we investigate the technical strategies about the using of lyotropic liquid crystal in transdermal and mucosal drug delivery system. Among them, we specially put the emphasis on the application prospects of lyotropic liquid crystal in the nasal mucosal administration, and then provide a theoretical basis and future research directions in the development of lyotropic liquid crystal in transdermal and mucosal administration fields.
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@#The purpose of this study was to investigate the formation thermodynamics of baicalein(BE)-nicotinamide(NCT)cocrystals in three solvents including ethyl acetate, acetone and trichloromethane. The solubilities of BE, NCT and BE-NCT in the above solvents at 25 °C were measured. Ternary phase diagrams(TPDs)of the BE-NCT-solvent systems were established. The non-linear fitting equation according to 1 ∶1 complexation mechanism of BE-NCT cocrystals demonstrated a good correlation between calculated and experiment data. ΔG0< 0 suggested that BE-NCT cocrystal formation was a spontaneous process. Among the organic solvents studied, the absolute value of ΔG0 in trichloromethane was significantly lower than that in the other two solvents. In addition, the cocrystallization zone in trichloromethane was far away from stoichiometric line. This study provides a theoretical foundation for solvent selection and preparation-condition optimization of BE-NCT cocrystals.
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@#Myricetin(MYR)was cocrystallized with caffeine(CAF)by suspension and the single crystal of MYR-CAF cocrystal was cultured by slow solvent evaporation. Cocrystals obtained by two different methods were the same in crystal form after characterization with X-ray diffraction. Structural analysis of single crystal of MYR-CAF showed that its crystal system and the space group were monoclinic and P21/n, respectively. In MYR-CAF cocrystal, 4′-OH in ring B and 7-OH in ring A of MYR interacted with CAF at(8)C=N and(2)C=O through hydrogen bonds. In comparison to the original MYR crystal, the intrinsic dissolution rate of MYR was significantly enhanced for about 17-fold after cocrystallization with CAF.
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The drug release characteristics ofDa Chuanxiong Fang multiunit drug delivery system (DCXFMDDS) in vivo and in vitro were evaluated. Ferulic acid (FA) and senkyunolide I (SI) were used as marker components, which were two of the effective components of Da Chuanxiong Fang. And their contents were determined by HPLC. Drug release characteristics in vitro of DCXFMDDS and Da Chuanxiong pills and pharmacokinetics characteristics of DCXFMDDS and Da Chuanxiong Fang active fraction (DCXFAF) in rats were compared. It was obvious that FA released from the DCXFMDDS in a sustained fashion but SI in a fast fashion both in vitro and in vivo. The releasing process and the releasing mechanism of FA and SI from DCXFMDDS were different, but the AUC value indicated that compared with DCXFAF the extent of absorption of FA and SI from DCXFMDDS was increased. Though from the same multiunit drug delivery system, FA an SI had different drug release characteristics both in vitro and in vivo, and that may be one of the reason why DCXFMDDS has the good properties such as rapid and long-lasting effect and high efficiency.
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<p><b>OBJECTIVE</b>To study the constituents absorbed into blood following the intragstric administration of Dachuanxiong Fang active parts(DCXF) to the experimental migrainous model rats induced by nitroglycerin.</p><p><b>METHOD</b>The UPLC-MS was used as the analytic method. The DCXF, Chuanxiong active parts, Tianma active parts, gastrodin, ferulic acid and senkyunolide I were used as the control samples. The information on the total ion chromatogram, mass chromatogram and the mass spectrogram were synthetically analyzed to confirm the constituents absorbed into blood.</p><p><b>RESULT</b>Ten of the DCXF constituents were detected in the rats plasma post the intragastric administration of DCXF, in whitch four including gastrodin came from Tianma active parts and six including ferulic acid and senkyunolide I from Chuanxiong active parts.</p><p><b>CONCLUSION</b>The findings abtained from the study can provide the useful information for the determination of bioactive substances of the DCXF.</p>
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Animais , Masculino , Ratos , Benzofuranos , Sangue , Álcoois Benzílicos , Sangue , Cromatografia Líquida de Alta Pressão , Métodos , Ácidos Cumáricos , Sangue , Medicamentos de Ervas Chinesas , Farmacocinética , Glucosídeos , Sangue , Espectrometria de Massas , Métodos , Ratos Sprague-DawleyRESUMO
Oral sustained- and controlled-release drug delivery systems of traditional Chinese medicine (TCM) are a research hotspot in the development of drug-delivery systems for TCM. The quality evaluation system is an important guarantee for the safety and efficiency of these drug-delivery systems. In this paper the methods to construct such quality evaluation system were discussed.
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Objective To set up a RP-HPLC method for determining gastrodin and ferulic acid in drug delivery system of Dachuanxiong simultaneously. Methods ODS-2 Hypersil column was used with methanol-1% glacial acetic acid as solution gradient elution. The flow rate was 1 mL/min and column temperature was 25 ℃. The wavelength of detector of gastrodin was 270 nm, and ferulic acid was 322 nm. Results Gastrodin and ferulic acid can be separated well with other components within 40 minutes. The linear range of gastrodin was 0.092～1.840 ?g (r =1.000 0), and ferulic acid was 0.122～2.440 ?g (r =1.000 0). The average recovery rate of gastrodin was 99.50% with RSD=1.23% (n =5), and ferulic acid was 101.5% with RSD=1.52% (n=5). Conclusion The method is simple, rapid, accurate and reliable, and can be used for determining gastrodin and ferulic acid in drug delivery system of Dachuanxiong simultaneously.