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@#Nanocrystals are nanoscale (1-1000 nm) dispersion systems in which small numbers of surfactants or polymers are used as stabilizers to disperse insoluble drug particles in water or oil. Nanocrystals enjoy not only high drug content, but also a simple and mature preparation process. At present, 24 nanocrystals products that have been marketed mainly focus on enhancing the solubility and bioavailability of poorly soluble drugs. And recent years have witnessed an increasing number of research reports on target drug delivery of nanocrystals through particle size control and surface modification. This paper mainly introduces three targeting strategies for prolonging the in vivo circulation time of nanocrystals, increasing the affinity for tumor cells and achieving the response to internal and external stimuli, and discusses the current challenges in the application of nanocrystal technology to targeted anti-tumor drugs.
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OBJECTIVE： To establish the method for simultaneous determination of four known related substances （olmesartan，olmesartan ester dimer ，olmesartan ester alkene ，benzothiadiazine impurity ，called impurity A ，B，C，D for short ）in Olmesartan medoxomil hydrochlorothiazide tablets. METHODS ：HPLC-principal component self-control with correction factor were adopted. The determination was performed on YMC-Triart C 8 column with mobile phase A consisted of acetonitrile- 0.015 mol/L potassium dihydrogen phosphate solution （pH adjusted to 2.8 with phosphoric acid ）（70 ∶ 30，V/V），mobile phase B consisted of acetonitrile-0.015 mol/L potassium dihydrogen phosphate solution （pH adjusted to 2.8 with phosphoric acid ）（15 ∶ 85，V/V）at the flow rate of 0.8 mL/min（gradient elution ）. The detection wavelength was set at 265 nm，and column temperature was 25 ℃. The temperature of injector was 4 ℃；the injection volume was 10 μL. RESULTS：The correction factors of impurity A ，B，C，D were 1.42，1.17，0.89，0.92，respectively. The linear range of olmesartan medoxomil ，hydrochlorothiazide and impurity A ，B，C，D were 0.252 7-7.580 0，1.152 1-4.562 9，0.244 0-18.299 0，0.244 7-3.670 8，0.265 2-3.978 3 and 0.149 9-4.497 3 μg/mL（r≥ 0.999 7），respectively. The limits of detection were 0.084 2，0.050 7，0.081 3，0.081 6，0.088 4，0.050 0 μg/mL，respectively. The quantitative limits were 0.252 7，0.152 1，0.244 0，0.244 7，0.265 2 and 0.149 9 μg/mL，respectively. The results of intermediate precision ，stability（24 h）and repeatability tests all met the relevant requirements. The average recovery rates were 104.00％-108.04％，102.00％-104.94％，100.99％-106.89％，92.00％-95.18％，102.00％-105.06％，103.90％-107.00％（n＝3）， respectively. The contents of impurity A ，B and D in 3 batches of Olmesartan medoxomil hydrochlorothiazide tablets were 0.90％ -1.00％ ，0-0.11％ ，0.16％ -0.24％ ，respectively. The impurity C and other impurities were not detected. There is no significant difference between the results measured by the established method and by the external standard method. CONCLUSIONS：The method has been proved to be highly sensitive and reproducible. It can be used to simultaneously determine four known substances in Olmesartan medoxomil hydrochlorothiazide tablets.
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@#Carbon nanomaterials are one of the hotspots in the research of drug delivery systems for cancer. Compared with the traditional drug delivery systems for cancer treatment, carbon nanomaterials can be used as drug carriers after modification based on their advantages of large specific surface area and unique optical properties. They have the characteristics of high drug loading, good biocompatibility, tumor targeting and lasting action time, indicating great potential and development space. In this paper, the properties and functions of quantum dots, carbon nanotubes, graphene oxide and mesoporous carbon nanospheres are introduced in the order of dimensional quantum properties. The current research focus and existing problems of carbon nanomaterials are discussed in order to provide a reference for the safe and effective application of carbon nanomaterials in tumor therapy.
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Objective To establish a determination method for leuprolide acetate microspheres. Methods HPLC was performed on Inertsil ODS-SP (150×4.6 mm×5μm) with mobile phase consist of 0.1 mol/L of Ammonium Dihydrogen Phosphate(adjust its pH to 7.00±0.05 with Ammonium Hydroxide) and Acetonitrile in ratio of 3:1(V/V),and the flow rate was 1.0 mL/min.The wavelength was 220 nm and column temperature was 30℃. The injection volume was 20 μL. Results The linear range of leuprolide acetate was 20.0-160.0μg/mL (r=0.9999) with an average recovery of 99.80%,RSD=0.63%(n=9). Conclusion The method of HPLC was accurate,reliable and specific, which could be used to determinate the assay of leuprolide acetate microspheres and for quality control of microspheres.
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Objective To prepare vardenafil hydrochloride orally disintegrating tablets and evaluate their quality. Methods The tablets were prepared by direct power compression method, using crosslinking povidone ( PVPP ) as disintegrants. The preparation method was optimized by response surface test using amount of PVPP, menthol and taste-masking agents as factors with disintegrating time and distance of bitterness as index. The results of taste of orally disintegrating tablets were determined by electronic tongue, comparing to the results of taste tests. At the same time, the properties of the tablets were evaluated using appearance, content uniformity, disintegrating time, et al. as index. Results The optimal formula was as follows:PVPP 13. 26%, menthol 0. 43%, taste-masking agent SGxj 1. 26%. The results on evaluation of electronic tongue were consistent with the results of taste tests. The quality of the prepared tablets was in line with standard. The disintegrating time was (22. 34 ± 0. 34 ) s. Conclusion The preparation technology of orally disintegrating tablets is simple, and controllable in quality.
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OBJECTIVE:To investigate the influential factors for the stability of gardenia yellow solution. METHODS:Using pigment loss rate as index,the stability of gardenia yellow solution was investigated within 12 h under different light(strong light, natural light,dark place),temperature(4,25,60,80 ℃),pH(3.0,5.0,7.0,9.0,11.0),oxidant concentration(hydrogen per-oxide solution,0,0.1%,0.2%,0.3%) conditions. The effects of 3 natural antioxidants as tea polyphenol,rosmarinic acid and grape seed extract on the stability of gardenia yellow solution were investigated within 12 h under different light(strong light,natu-ral light,dark place) and temperature (25,60,80 ℃) conditions;the effects of different concentrations of tea polyphenol (0, 0.05%,0.1%,0.2%)on the stability of gardenia yellow solution were also investigated within 12 h. RESULTS:The pigment loss rates were 20%,10% and 10% within 12 h under 3 light conditions;5%,5%,30% and 60% under 4 temperature conditions;12%,6%,6%,6% and 16% under 5 pH conditions;4%,12%,15% and 18% under 4 oxidant concentrations. After adding 3 antioxidants,pigment loss rate decreased by 10% under different light and temperature conditions except for 80 ℃,and the de-crease of tea polyphenol was most significant;among 4 concentrations of tea polyphenol,pigment loss rate was the lowest in 0.1%group. CONCLUSIONS:Gardenia yellow solution can't keep stable under strong light and high temperature;3 antioxidants can im-prove the stability of gardenia yellow solution,especially 0.1%tea polyphenol.
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With the popularity of the concept of being ?natural?and ?vegetarian?;plant soft capsules have gained widespread attention in pharmaceutical markets of many countries.Looking for new materials of plant soft capsules and developing the new technologies have become a inevitable requirement due to the traditional gelatin soft capsules could not meet the increasing daily life demand of people.The review illustrates the characteristics of the commonly used plantsoft capsule materials such as modified starch;gelatin or synthetic polymers;as well as the application of advanced technology concerning capsule shell and core material;providing a reference for the development and application of new plant soft capsules.The promising expectation of plant soft capsules are also illustrated.
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Objective To optimize the HP-?-cyclodextrin(HP-?-CD)inclusion process condition for volatile oils from Anti-virus Oral Solution. Methods The process conditions were screened by determining the inclusion rate of volatile oils and the yield of inclusion compound,and by comparing the inclusion effect of supersonic method,saturated water solution method and grinding method.The optimum condition was investigated by the orthogonal test. The inclusion compound was identified by TLC,differential scanning calorimetry(DSC) and ultraviolet spectrophotometry (UV). Results The optimum preparation conditions for inclusion were established as follows: the proportion of volatile oils and HP-?-cyclodextrin was 1 ∶12,the inclusion temperature was at 45 ℃and the inclusion time was 3 hours .The inclusion rate of volatile oils was 66.71 %,and the yield of inclusion compound was 90.07 %. Conclusion The complex prepared under the optimized condition is stable and has a highest inclusion rate.
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Objective To determine the content of astragaloside Ⅳin Qi Zao Granules.Methods Equipped with the evaporative light scattering detector (ELSD), a RP-HPLC method was established. The chromatographic column was C18 and the column temperature was at 30 ℃.The drift tube temperature was at 40 ℃and the evaporative gas was nitrogen with pressure of 3.5 bar.The mobile phase was acetonitrile-water(30∶70) and the flow rate was 1mL/min. Results This method showed a good linear relationship in the range of 2.51～50.2 ?g astragaloside Ⅳ. The average recovery was 98.13 %with RSD being 1.28 %. Conclusion The method is sensitive and accurate and can be used for the quality control of Qi Zao Granules.