The release behavior of single pellet was investigated by LC/MS/MS method with tamsulosin hydrochloride (TSH) as the model drug of the research and then the pellets were divided into four groups according to the drug loading. Comparison of dissolution profiles of each group and capsule were performed using f1 and f2 factor methods to study the difference and similarity. The release profiles of single pellet, each group and capsule were analyzed using principle component analysis (PCA). The particle system was built through Matlab to get the target release profile. The result of this research demonstrated the release behavior of single pellet correlated well with the drug loading. While the dissolution profile of capsule as a reference, the similarity factor of dissolution profiles of the lower drug loading groups were 62.2, 67.1, 53.9, respectively and, 43.3 for highest drug loading group. The particle systems with different pellet distribution and same release profiles were built through release behavior of single pellet. It is of significance to investigate the release behavior of single pellets for studying the release regularity of multiple-unit drug delivery system.

Objective To explore the efficacy and safety of modified transobturator tape (TOT) for female stress urinary incontinence (SUI).Methods From June 2015 to June 2017,a total of 87 SUI patients,including 35 patients underwent standard TOT operation (standard TOT group) and 52 patients underwent modified TOT operation (modified TOT group),were retrospectively reviewed.There was no statistical difference of age [(59.7 ± 10.3) yea~ vs.(56.3 ± 9.1) years],BMI [(24.I ± 9.7) kg/m2 vs.(24.6 ± 9.3) kg/m2],diabetes history [31.4％ (11/35) vs.26.9％ (14/52)],mixed urinary incontinence [45.7％ (16/35) vs.48.1％ (25/52)] and the daily amount of urine pad [(4.3 ±2.7) vs.(3.9 ± 2.1)] between the two groups (P ＞ 0.05).The operative time,intraoperative complications,and postoperative complications were collecteded in two groups.Patients were followed up at 3 months,6 months,and 1 year after surgery.Results There was no significant difference in operation time [(21.1 ± 4.3) min vs.(20.5 ± 5.7) min],intraoperative hemorrhage [(18.3 ± 9.1) ml vs.(25.7 ± 8.3) ml] and postoperative incidence of urinary retention [2.9％ (1/35) vs.3.8％ (2/52)] between the two groups (P ＞ 0.05).The incidence of postoperative leg pain was significantly lower in modified TOT group than in TOT group[1.9％ (1/52) vs.20.0％ (7/35),P ＜ 0.05].There was no significant difference in subjective cure rate and objective cure rate between the two groups at 3 months,6 months and 1 year after surgery (P ＞ 0.05).Conclusions Compared with the standard TOT,the modified TOT of modified puncture port has a similar cure rate and efficiency.However,the use of modified TOT can significantly reduce the incidence of postoperative short-term leg pain,but the long-term efficacy still needs to be further followed-up.

Cyclodextrin metal-organic framework (CD-MOF) as a highly porous supramolecular carrier could be one of the solutions to the insolubility of isosteviol (STV). The solubility of STV was lower than 20.00 ng/mL at pH 1.0 and pH 4.5, whilst its solubility increased to 20,074.30 ng/mL at pH 6.8 and 129.58 ng/mL in water with a significant pH-dependence. The

Tremendous efforts have been devoted to the enhancement of drug solubility using nanotechnologies, but few of them are capable to produce drug particles with sizes less than a few nanometers. This challenge has been addressed here by using biocompatible versatile -cyclodextrin (-CD) metal-organic framework (CD-MOF) large molecular cages in which azilsartan (AZL) was successfully confined producing clusters in the nanometer range. This strategy allowed to improve the bioavailability of AZL in Sprague-Dawley rats by 9.7-fold after loading into CD-MOF. The apparent solubility of AZL/CD-MOF was enhanced by 340-fold when compared to the pure drug. Based on molecular modeling, a dual molecular mechanism of nanoclusterization and complexation of AZL inside the CD-MOF cages was proposed, which was confirmed by small angle X-ray scattering (SAXS) and synchrotron radiation-Fourier transform infrared spectroscopy (SR-FTIR) techniques. In a typical cage-like unit of CD-MOF, three molecules of AZL were included by the -CD pairs, whilst other three AZL molecules formed a nanocluster inside the 1.7 nm sized cavity surrounded by six -CDs. This research demonstrates a dual molecular mechanism of complexation and nanoclusterization in CD-MOF leading to significant improvement in the bioavailability of insoluble drugs.