[Study on andrographolide solid dispersion vectored by hydroxyapatite].

OBJECTIVE: To prepare andrographolide solid dispersion, with hydroxyapatite as vector, in order to increase drug dissolution. METHOD: Andrographolide and hydroxyapatite were dispersed in 95% ethanol. The solvent evaporation method was adopted to prepare andrographolide solid dispersion, in order to study its dissolution behavior, stability and physical characteristics. RESULT: The solid dispersion prepared with andrographolide and hydroxyapatite with the proportion of 1:8 existed in the vector in an amorphous form, according to differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction. The in vitro dissolution of andrographolide solid dispersions was up to 93% at 45 min. After the accelerated stability test for three months, the drug dissolution and content in andrographolide solid dispersion showed no significant change. CONCLUSION: The prepared solid dispersions with hydroxyapatite as the vector can effectively improve the stability and dissolution of water-insoluble drug andrographolide.

[Study on solidifying volatile oil of cinnamon with colloidal silicon dioxide SYLOID244FP].

OBJECTIVE: To evaluate the properties of solidifying volatile oil of cinnamon with colloidal silicon dioxide SYLOID244FP. METHOD: Volatile oil of cinnamon was solidified by SYLOID244FP. The amount of SYLOID244FP was optimized with the cinnamaldehyde yield as criteria. Curing powder was characterized by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC). The effects of SYLOID244FP on dissolution in vitro and thermal stability of cinnamaldehyde were studied. RESULT: The optimum solidification ratio of SYLOID244FP to volatile oil of cinnamon was 1: 1. Dissolution rate of cinnamaldehyde increasesd and its thermal stability improved after volatile oil of cinnamon was solidified. CONCLUSION: Solidifying herbal volatile oil with SYLOID244FP deserves studying further.

[Essence of material base in geoherbs: specificality of constituent structure].

Geoherbs, playing an indispensable role in the protection and the treatment of disease, has been demonstrated to be the treasure in Chinese medicine clinical. Geoherbs possessed the best quality and curative effect due to their distinctive inside chemical ingredients/components. In recent years, a lot of achievements were obtained in geoherbs research on chemistry; however, there was also much confusion in existence. More and more studies revealed that the better curative effect on geoherbs was attributed to its architectural feature with steady and well-organized in unique ingredients/components constituent, but not for the characteristic single chemical ingredient. The "constituent structure theory" suggested that the material base of geoherbs consist of different components of which compatibility proportion relationship was optimal. In addition, the single active ingredients had their unique three-dimensional structure. This paper explained the peculiarity of geoherbs material base based on constituent structure theory from there layers and multi-dimensional structure to geoherbs material base research in a new way.

[Multi-dimensional structure quality control over Salvia miltiorrhiza injection based on component structure theory].

As the preparation process from Salvia miltiorrhiz herbs to S. miltiorrhiz injection involves complicated technology and has relatively more factors impacting quality safety, the overall quality control is required for its effectiveness and safety. On the basis of the component structure theory, and according to the material basis of S. miltiorrhiz injection, we discussed the multi-dimensional structure and process dynamic quality control technology system of the preparation, in order to achieve the quality control over the material basis with safety and effectiveness of S. miltiorrhiz injection, and provide new ideas and methods for production quality standardization of S. miltiorrhis injection.

[Study on Xinyueshu spray drying assisted with copovidone and its effect on powder property].

To study the application characteristics of copovidone (PVP-S630) in Xinyueshu extracts during the spray drying process, and its effect on such pharmaceutical properties as micromeritics and drug release behavior. PVP-S630 was added into Xinyueshu extracts to study on the spray drying, the effect of different dosages of PVP-S630 against the wall sticking effect of the spray drying, as well as the power property of Xinyueshu spray drying power and the dissolution in vitro behavior of the effective component of hyperoside. The results showed that PVP-S630 revealed a significant anti-wall sticking effect, with no notable change in the grain size of the spray drying power, increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior of hyperoside. It was worth further studying the application of PVP-S630 in spray drying power of traditional Chinese medicine.

The in vitro protective effects of curcumin and demethoxycurcumin in Curcuma longa extract on advanced glycation end products-induced mesangial cell apoptosis and oxidative stress.

Curcuma longa L. (CLL), a traditional herbal medicine, has been widely used for the prevention of diabetic vascular complications in recent years. However, the protective effects of curcuminoids in CLL on the AGEs-induced damage to mesangial cell are not fully understood. In this present study, dihydroethidium, superoxide dismutase kit, malondialdehyde kit, and acridine orange/ethidium bromide staining methods were used to evaluate the activities of curcumin and demethoxycurcumin (10(-11)-10(-9) M) on AGEs-induced oxidative stress and apoptosis, which were associated with the damage to mesangial cell. The results showed that these two compounds could significantly restore advanced glycation end products (AGEs)-induced apoptosis to normal levels (IC50 = 3.874 × 10(-11) M for curcumin and IC50 = 6.085 × 10(-11) M for demethoxycurcumin) and reduce remarkably reactive oxygen species generation in mesangial cell. Furthermore, curcumin and demethoxycurcumin dramatically elevated AGEs-decreased superoxide dismutase activity while significantly reducing AGEs-increased malondialdehyde content in cell culture supernatant. Our results suggest that both curcumin and demethoxycurcumin have a significant protective potential to the prevention of diabetic nephropathy.

[Study on nano-CaCO3 applicated in Xin Yue Shu Capsules preliminarily].

OBJECTIVE: To investigate the characteristics of nano-CaCO3 applicated in Xin Yue Shu Capsules. METHODS: Studied the effect of different dosages of aerosil or nano-CaCO3 on fluidity, bulk density, moisture absorption of Xin Yue Shu capsules spray drying powder. In vitro dissolution and ferulic acid stability of Xin Yue Shu capsules was observed. RESULTS: It significantly improved powder fluidity and bulk density of Xin Yue Shu spray drying powder when aerosil or nano-CaCO3 was added. But there was no significant effect on powder moisture absorption, ferulic acid in vitro dissolution and ferulic acid stability. CONCLUSION: The effect of Nano-CaCO3 on improving powder fluidity and bulk density applicated in the spray drying powder of traditional Chinese medicine deserves studying further.

[Studies on sustained release solid dispersion of tripterine carried by HPMC-stearic acid].

OBJECTIVE: To prepare the sustained release solid dispersion of tripterine, using HPMC-stearic acid with the intention of improving drug dissolution and controlling drug releases moderate, so that the drug performances lower toxicity. METHOD: Tripterine sustained release solid dispersions was prepared by the solvent method with different weight ratios of HPMC-stearic acid and tripterine, which were dissolved in 95% ethanol. And in vitro dissolution experiment was conducted. Differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction can prove the formation of solid dispersions. RESULT: The ideal tripterine sustained release solid dispersions were prepared under the condition as follows, the weight ratio of tripterine and HPMC-stearic acid was 1: 10, and the release rate of drug can keep moderate and controllable. In vitro cumulative release of tripterine sustained release solid dispersion is up to more than 90% after 8 h, and the tripterine exist as amorphous in the solid dispersion. CONCLUSION: The sustained release solid dispersion of tripterine, carried by HPMC-stearic acid, can improve the release of tripterine effectively and controls the release rate keep moderate and controllable, and the preparation process is simple, which has potential applications.

Eco-Friendly and Biodegradable Biopolymer Chitosan/Y2O3 Composite Materials in Flexible Organic Thin-Film Transistors.

The waste from semiconductor manufacturing processes causes serious pollution to the environment. In this work, a non-toxic material was developed under room temperature conditions for the fabrication of green electronics. Flexible organic thin-film transistors (OTFTs) on plastic substrates are increasingly in demand due to their high visible transmission and small size for use as displays and wearable devices. This work investigates and analyzes the structured formation of aqueous solutions of the non-toxic and biodegradable biopolymer, chitosan, blended with high-k-value, non-toxic, and biocompatible Y2O3 nanoparticles. Chitosan thin films blended with Y2O3 nanoparticles were adopted as the gate dielectric thin film in OTFTs, and an improvement in the dielectric properties and pinholes was observed. Meanwhile, the on/off current ratio was increased by 100 times, and a low leakage current was observed. In general, the blended chitosan/Y2O3 thin films used as the gate dielectric of OTFTs are non-toxic, environmentally friendly, and operate at low voltages. These OTFTs can be used on surfaces with different curvature radii because of their flexibility.

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles.

We prepared solid dispersions (SDs) of tanshinone IIA (TSIIA) with silica nanoparticles, which function as dispersing carriers, using a spray-drying method and evaluated their in vitro dissolution and in vivo performance. The extent of TSIIA dissolution in the silica nanoparticles/TSIIA system (weight ratio, 5:1) was approximately 92% higher than that of the pure drug after 60 minutes. However, increasing the content of silica nanoparticles from 5:1 to 7:1 in this system did not significantly increase the rate or extent of TSIIA dissolution. The physicochemical properties of SDs were investigated using scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and Fourier transforms infrared spectroscopy. Studying the stability of the SDs of TSIIA revealed that the drug content of the formulation and dissolution behavior was unchanged under the applied storage conditions. In vivo tests showed that SDs of the silica nanoparticles/TSIIA had a significantly larger area under the concentration-time curve, which was 1.27 times more than that of TSIIA (P < 0.01). Additionally, the values of maximum plasma concentration and the time to reach maximum plasma concentration of the SDs were higher than those of TSIIA and the physical mixing system. Based on these results, we conclude that the silica nanoparticle based SDs achieved complete dissolution, increased absorption rate, maintained drug stability, and showed improved oral bioavailability compared to TSIIA alone.

Protection of glycyrrhizic acid against AGEs-induced endothelial dysfunction through inhibiting RAGE/NF-κB pathway activation in human umbilical vein endothelial cells.

ETHNOPHARMACOLOGICAL RELEVANCE: Licorice (Glycyrrhiza uralensis roots) is used as a traditional medicine for the treatment of diabetes mellitus and its vascular complications. Glycyrrhizic acid (GA, also known as Glycyrrhizin), a triterpenoid saponin glycoside, is considered to be a bioactive component in Licorice and is beneficial to diabetic vascular complications. AIM OF STUDY: The present study was conducted to evaluate the potential protective activities on AGEs-induced endothelial dysfunction, including anti-apoptosis, antioxidant stress and anti-proinflammatory responses, and explore the underlying mechanism. MATERIALS AND METHODS: Human umbilical vein endothelial cells (HUVECs) were incubated and pre-treated with GA (10(-9)-10(-6)M) or RAGE-Ab (5µg/ml) in the presence or absence of 200µg/ml AGEs. AO/EB fluorescence staining assay was performed to evaluate anti-apoptosis activity. The superoxide dismutase (SOD) activity and malondialdehyde (MDA) level in cell supernatant were detected by kits while the intracellular reactive oxygen species (ROS) generation was determined by 2,7-dichlorodihydrofluorescin diacetate (DCFH-DA) kit. Immunocytochemistry analysis was designed to determine transforming growth factor beta1(TGF-ß1) protein expression while immunofluorescence analysis for RAGE and NF-kB. The protein expressions of TGF-ß1, RAGE and NF-kB were analyzed by Western blot analysis. RESULTS: Pretreatment with GA at a concentration of 10(-8)-10(-6)M significantly reduced the AGEs-induced apoptosis in HUVECs. GA significantly increased antioxidant enzyme SOD activity and decreased peroxide degradation product MDA level in a dose-dependent manner. Furthermore, GA also remarkably inhibited the overgeneration of AGEs-induced ROS. Both immunocytochemistry analysis and western blot analysis showed that GA significantly decreased the protein expression of poinflammatory cytokine TGF-ß1 in a similar manner which RAGE-Ab did. Additionally, AGEs-induced RAGE and NF-kB protein expressions were down-regulated significantly by the pretreatment with GA or RAGE-Ab. CONCLUSION: These findings provide evidences that GA possesses protective activity on AGEs-induced endothelial dysfunction, including anti-apoptosis, anti-inflammation and antioxidant stress, via inhibiting RAGE/NF-kB pathway. GA might be an alternative for the prevention and treatment of diabetic vascular complications in an appropriate dosage.