ABSTRACT
OBJECTIVE To establish the ultra-high performance liquid chromatography-mass spectrometry/mass spectrometry method for simultaneous determination of liquiritin ， naringin， hesperidin， neohesperidin， nobiletin， atractylenolide Ⅲ ， imperatorin，honokiol，isoimperatorin and magnolol in Huoxiang zhengqi soft capsules. METHODS Twelve batches of Huoxiang zhengqi soft capsules were extracted by ultrasonic extraction with ethanol. The determination was performed on Ultimate XB-C 18 column with mobile phase consisted of acetonitrile - 0.1％ formic acid solution for gradient elution at the flow rate of 0.4 mL/min. The column temperature was 30 ℃. The electrospray ionization source was applied to carry out the positive and negative ion scanning with multiple react ion monitoring mode. RESULTS The linear range of liquiritin ，naringin，hesperidin，neohesperidin， nobiletin，atractylenolide Ⅲ ，imperatorin，honokiol，isoimperatorin and magnolol were 1.64-52.40，1.73-55.20，1.54-49.20， 1.71-54.80，1.74-55.60，4.19-134.00，1.51-48.40，1.61-51.60，1.80-57.60，1.74-55.60 ng/mL（r≥0.999 5），respectively. The limits of quantitation were 0.41，0.43，0.19，0.43，0.11，1.05，0.19，0.40，0.45，0.11 ng/mL，respectively. RSDs of precision ，stability （24 h）and repeatability tests were all lower than 6％. Average recoveries were 102.42％，98.65％，98.34％，101.48％，96.74％， 100.40％，104.92％，98.53％，99.50％，105.40％（RSD＝1.34％-5.44％，n＝9）. The contents of the above 10 constituents in 12 batches of Huoxiang zhengqi soft capsules were 201.21-287.89，5.03-20.37，1 465.56-1 988.35，5.35-9.01，217.09-306.44，1.91- 16.17，1 081.59-1 377.12，2 388.34-2 915.13，341.26-397.45 and 7 633.47-8 976.99 μg/g，respectively. CONCLUSIONS The established method for content determination is convenient ，sensitive and accurate ，which can be used for the quality control and evaluation of Huoxiang zhengqi related preparations.
ABSTRACT
Enteric-soluble soft capsule is a kind of new preparation that does not disintegrate in the stomach ，but releases rapidly in the intestinal tract to play a pharmacodynamic role. It has the unique advantages of improving drug stability ，reducing drug irritation ，delivering drugs directionally to the intestinal tract ，and prolonging drug action time. In this paper ，the decomposition and release mechanism ，application advantages ，classification of enteric-soluble coating materials and preparation methods of enteric-soluble soft capsule are sorted and summarized ，in order to provide reference for further development of this type of preparation.
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Objective:To investigate the finite element analysis and early-stage clinical effects of double bundle anterior cruciate ligament (ACL) reconstruction with femoral direct fiber insertion.Methods:From June 2016 to June 2017, a total of 26 cases of ACL reconstruction were analyzed retrospectively, including 15 males and 11 females, mean age 30.5±4.6 years. All the patients underwent ACL reconstruction by the same operator. The early-stage clinical effects were evaluated by the finite element analysis, pivot shift test, Lachman test, preoperative and postoperative IKDC score, Lyshlom score, KT-2000, 3D-CT and MRI.Results:The finite element analysis confirmed theoretically that the double bundle ACL reconstruction with femoral direct fiber insertion could restore the stability and biomechanics of knee effectively. The results of pivot shift test were negative, and the Lachman test were negative except one first-stage positive after operation. 3D-CT showed that the bone tunnel was located in the direct fiber area. MRI showed clearly the ACL of double bundle after operation. Lysholm score increased from 56.5±3.6 pre-operation to 61.9±3.2 at three months after operation, and up to 88.5±2.0 two years after operation with statistically significant difference ( F=824.72, P<0.001). IKDC score increased from 48.3±2.8 before operation to 58.0±2.0 at three months after operation, and to 92.5±2.6 at two years after operation with statistically significant difference ( F=2 256.66, P<0.001). KT-2000 side-side difference decreased from 5.6±0.7 mm to 1.6±0.5 mm at three months after operation, and to 1.5±0.6 mm at two years after operation with statistically significant difference ( F=389.14, P<0.001). Conclusion:The double bundle ACL reconstruction with femoral direct fiber insertion can effectively restore the stability and the biomechanical environment of knee joint with satisfied early-stage clinical effects.
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OBJECTIVE： To investigate in vitro release rate and in vivo pharmacokinetics of Resveratrol/hydroxypropyl-β- cyclodextrin/chitosan sustained-release pellets （RES/HP-β-CD/Chitosan） in rats. METHODS： In vitro release rate of RES raw materials， RES-HP-β-CD complexes （RES/HP-β-CD） and RES/HP-β-CD/Chitosan in water within 12 h were investigated by paddle method. The pharmacokinetic characteristics of RES raw materials， RES/HP-β-CD and RES/HP-β-CD/Chitosan were compared within 720 min after intragastric administration. RESULTS： Compared with RES raw materials， in vitro release rate of RES/HP-β-CD was increased significantly， and 120 min accumulative release rate reached 87％. Compared with RES/HP-β-CD， in vitro release rate of RES/HP-β-CD/Chitosan were relieved significantly； release time prolonged significantly； 12 h accumulative release rate was 72％. The pharmacokinetic parameters of RES raw materials， RES/HP-β-CD and RES/HP-β-CD/Chitosan included that cmax were 473.3， 2 492.2， 590.5 ng/mL； t1/2 were 2.6， 0.5， 4.6 h； AUC0-12 h were 514.7， 824.6， 2 778.5 ng·h/mL. Compared with RES raw materials， relative bioavailability of RES/HP-β-CD and RES/HP-β-CD/Chitosan were 172.5％ and 540.0％. CONCLUSIONS： RES/HP-β-CD/Chitosan shows good sustained-release effect， and its bioavailability is significantly higher than that of RES raw materials， RES/HP-β-CD.
ABSTRACT
OBJECTIVE： To prepare Resveratrol-hydroxypropyl-β-cyclodextrin-chitosan sustained-release pellets （RES-HP-β- CD-Chitosan）， and to characterize it. METHODS： Resveratrol raw material， HP-β-cyclodextrin and chitosan were collected with ratio of 1 ∶ 7 ∶ 0.25. Resveratrol-HP-β-cyclodextrin inclusion compound were prepared by solvent method， and then added into chitosan， RES-HP-β-CD-Chitosan were prepared by spray drying method. Particle size of prepared sustained-released pellets were observed by optical microscope. X-ray， DSC， IR and SEM were used to characterize RES-HP-β-CD-Chitosan. The contents of resveratrol in prepared sustained-released pellets were determined by UV spectrum， and drug-loading amount and encapsulation efficiency were calculated. RESULTS： Particle size of prepared RES-HP-β-CD-Chitosan was （2.23±0.35） μm （n＝300）. Characterization results show that RES-HP-β-CD-Chitosan was spherical in shape； shrinkage was found on the surface of microspheres， and resveratrol was included in HP-β-cyclodextrin in molecule or amorphous state. Drug-loading amount of prepared RES-HP-β-CD-Chitosan was 11.67％ （n＝3）， encapsulation efficiency was 96.27％ （n＝3）. CONCLUSIONS： RES-HP-β-CD- Chitosan is prepared successfully.