Solid dispersions (SD) as a preparation of intermediates have played an important role in improving the dissolution of insoluble drugs and its bioavailability.SD technique is one of the most promising techniques to improve the dissolution and solubility of insoluble drugs,and the development of SD technique will promote the gradual perfection in preparative field.This review focuses on the carrier materials of SD,various new preparation techniques and their comparisons,application of solid dispersion formulations,and stability problems of SD.The factors influencing the stability of SD are described,and the effective measures to prevent the aging of SD are put forward.Finally,the review puts forward the practical suggestions of the solid dispersion technique.

Objective To analyze the clinical and genetic characteristics of 10 Chinese patients with 17? hydroxylase/17,20 lyase deficiency (17OHD). Methods Clinical features and laboratory data were collected from 7 kindreds with 17OHD. PCR products and subclone sequencing were performed to screen the mutation of CYP17A1 gene. Results All patients had typical clinical presentation of sexual infantilism, hypertension and hypokalemia. The laboratory examinations indicated decreased plasma cortisol, 17-hydroxy progesterone, estradiol and testosterone, and elevated blood adrenocorticotrophic hormone(ACTH), follcie-stimulating hormone(FSH) and luteinizing hormone(LH). CT scan showed bilateral adrenal hyperplasia. 5 CYP17A1 mutations were identified, 4 of which are novel types D487_F489del, the most frequent mutation, was identified in 4 families and 45% alleles. Conclusion Our study indicates that 17OHD should be considered in the diagnosis of patients with sexual infantilism. D487_F489del is the most frequent mutation in Chinese 17OHD patients.

OBJECTIVETo characterize genotypic resistance within HBV RT region in chronic hepatitis B (CHB) patients with nucleos(t)ide analogue (NA) treatment.

METHODSSerum samples of 229 CHB patients with NA treatment were obtained. Full-length HBV RT sequences were amplified, sequenced and analyzed, on the following NA resistant (NAr) mutations belonging to different NAr pathways.

RESULTSAmong 229 HBV isolates, 14.41% (33/229) and 85.59% (196/229) were genotype B and C, respectively; and the patients with HBV genotype C may be more susceptible to develope resistant mutations than patients with HBV genotype B(chi2 = 2.95, P < 0.05). NAr mutations were detected in 63 CHB patients. Mutations were not found at rtI169, rtT184, rtA194 or rtS202. RtM204 mutations were detected at the highest frequency among 63 mutants (40/63, 63.49%) and found to display 11 combination mutation patterns, in which rtM204I were associated with rtL80I/V and rtL180M, and rtM204V were associated with rtL1l80M, respectively. Conclusions There are complicated mutation patterns in the HBV RT region for chronic hepatitis B (CHB) patients with nucleos(t)ide analogue (NA) treatment. RtM204V/I mutation was the highest.

Adolescent ; Adult ; Aged ; Antiviral Agents ; therapeutic use ; Female ; Hepatitis B virus ; drug effects ; enzymology ; genetics ; Hepatitis B, Chronic ; drug therapy ; virology ; Humans ; Male ; Middle Aged ; Mutation ; drug effects ; Nucleosides ; therapeutic use ; Nucleotides ; therapeutic use ; RNA-Directed DNA Polymerase ; genetics ; metabolism ; Viral Proteins ; genetics ; metabolism ; Young Adult

OBJECTIVETo assess the effect of intra-abdominal hypertension (IAH) on hemodynamics of severe acute pancreatitis (SAP) in porcine model.

METHODSFollowing baseline registrations, SAP was induced in 12 animals. The N(2) pneumoperitoneum was used to increase the intra-abdominal pressure to 30 mmHg (1 mmHg = 0.133 kPa) in 6 of 12 SAP animals thereafter and keep constant during the experiment. The investigation period was 12 h. Heart rate, cardiac output (CO), central venous pressure (CVP), mean arterial pressure and pulmonary arterial wedge pressure (PAWP) were continuously measured with the aid of balloon tipped flow-directed catheter and electrocardiography monitor. Oxygen partial pressure of artery (PaO(2)), carbon dioxide partial pressure of artery (PaCO(2)), ScvO(2), base excess (BE), and blood lactic acid (LAC) were measured by acid-base analysis.

RESULTSIn the IAH group, CO decreased significantly at 12 h, CVP and PAWP increased significantly at 3 h, 6 h and 12 h compared with SAP group (all P < 0.05). Peak inspiration pressure increased immediately after pneumoperitoneum in the IAH group, to (50.2 ± 3.1) cmH(2)O (1 cmH(2)O = 0.098 kPa) and (49.8 ± 0.9) cmH(2)O at 6 h and 12 h respectively. The pH, PaO(2), ScvO(2) and BE showed a tendency to fall in the IAH group. PaCO(2) and LAC were increased significantly in the IAH group (all P < 0.05).

CONCLUSIONSThere were remarkable and relatively irreversible effects on global hemodynamics in response to sustained IAH of 12 h with the underlying condition of SAP. Abdominal decompression is beneficial for patients of SAP with IAH.

Animals ; Disease Models, Animal ; Female ; Hemodynamics ; physiology ; Intra-Abdominal Hypertension ; Male ; Pancreatitis, Acute Necrotizing ; physiopathology ; Swine

OBJECTIVETo observe the effects of Yixin Kangtai Capsule (YKC) on sperm concentration and motility, superoxide dismutase (SOD) and malondialdehyde (MDA) in aged SD rats, and to explore its possible mechanisms of action.

METHODSWe randomly assigned fifty 24-month-old male SD rats to five groups of equal number: blank control, testosterone undecanoate, high-dose YKC, medium-dose YKC and low-dose YKC, and treated them intragastrically with physiological saline at 10 ml/kg, testosterone un-decanoate suspension at 4 mg/kg, and YKC at 0.6 g/kg, 0.3 g/kg and 0.15 g/kg, respectively, once a day for 30 days. Then we harvested the epididymides, which were stripped of fat and envelope, cut into pieces and placed in the saline at 37 degrees C for 10 to 15 minutes. Then we detected the sperm parameters with the Weili CASA sperm analysis system, measured the levels of serum SOD and MDA, and, following HE staining, observed the histomorphological changes of the testicular tissue under the light microscope.

RESULTSCompared with the controls, the rats treated with high-, medium- and low-dose YKC exhibited significantly increased sperm concentration ([152.3 +/- 24.0] x 10(6)/ml vs [334.5 +/- 97.7], [302.7 +/- 158.9] and [221.4 +/- 75.6] x 10(6)/ml, P < 0.05) and markedly improved sperm motility ([26.5 +/- 2.0]% vs [35.5 +/- 5.9], [33.1 +/- 5.4] and [28.4 +/- 2.1]%, P < 0.01). High-dose YKC significantly increased the level of serum SOD ([22.0 +/- 5.3] U/ml, P < 0.01) and reduced the content of MDA ([13.6 +/- 4.6] nmol/ ml, P < 0.01). Testicular histology showed that YKC induced more active proliferation of cells, and increased the number of dividing cells and that of mature sperm in the lumen, with little interstitium, abundant blood vessels, and well-developed stromal cells.

CONCLUSIONYixin Kangtai Capsule can improve spermatogenesis in aged SD rats by regulating the levels of SOD and MDA.

Aging ; Animals ; Drugs, Chinese Herbal ; pharmacology ; Male ; Malondialdehyde ; blood ; Rats ; Rats, Sprague-Dawley ; Sperm Motility ; drug effects ; Spermatogenesis ; drug effects ; Superoxide Dismutase ; blood

Objective To master the prevalence status of schistosomiasis in Yunnan Province in 2016,so as to provide the evidence for formulating the control strategy and intervention measures. Methods The schistosomiasis heavy-endemic villages were selected from each of 18 endemic counties as the survey sites. Then,the serological and etiological tests were carried out in the local residents and floating population,and the infection status of the livestock,field feces and Oncomelania hupensis snails were surveyed. Results The serum positive rate of schistosomiasis of local residents was 8.78％and the serum positive rate was 2.26％of floating population. No schistosome eggs were found in the stool examinations in the population. The area with snails was 80.0546 hm2 in 2016 with an increasing rate of 45.47％compared to that in 2015. The average density of living snails was 0.0317/0.1 m2. No schistosome-infected snails were found for the last four years and no new area with snails was found for the last three years. No positive livestock or feces were found. Conclusions The schistosomiasis epidemic situation is stabilized in Yunnan Province in 2016. However,the area with snails and the number of living snails are increasing,and therefore,the schis-tosomiasis epidemic risk still exists. So,the comprehensive control measures should be strengthened continuously.

The patients with severe traumatic brain injury(sTBI)have a higher incidence of epilepsy.It's controversial whether prophylactic antiepileptic drugs(AEDs)are needed to prevent epilepsy in sTBI.Patients with sTBI do not need prophylactic AEDs on the basis of analgesic and sedative treatment in the early stage(within 7 days),and prophylactic AEDs are also not needed in late stage.Patients diagnosed with epilepsy need to take AEDs.

OBJECTIVETo explore the prevalence of vision, mental, audibility, language, psychiatry, extremity, and influence factors in the 0 - 7 year olds.

METHODSA total number of 77,727 0 - 7 year old children living in Shenzhen city were tested with tree phase screening under the Chinese standard of evaluation in disabilities.

RESULTSThe prevalence of all disabilities was 5.59 per thousand (adjusted rate was 8.49 per thousand with a false negative of 3.1 per thousand ). The prevalence of mental disease was the highest (1.88 per thousand, with adjusted rate 3.43 per thousand ), the prevalence of language disability was 1.88 per thousand (including retarded language development, with adjusted rate 3.43 per thousand ). The prevalence rates of psychiatry, extremity and audibility disability were 1.59 per thousand, 1.56 per thousand, 1.11 per thousand respectively with of vision the lowest (0.37 per thousand ). The prevalence of all disabilities, audibility, language and mental was on the increase with age. The difference was statistically significant. Among all different age groups regarding psychiatric disease, the highest fell in the 2 - 4 year olds. The prevalence of extremity was not statistically different among age groups. The suspected agents of disease which occurred before or during pregnancy took up 45.7%.

CONCLUSIONThe prevalence of six kinds disabilities in Shenzhen was about 10 per thousand lower than that of the samples of the nation in 1989, but two times higher than that of similar studies in Japan. The prevalence rates of language and psychiatric disease were higher than that of the nation in 1989. The causation should be further studied.

Age Factors ; Child ; Child, Preschool ; China ; epidemiology ; Cross-Sectional Studies ; Disabled Children ; Female ; Humans ; Infant ; Infant, Newborn ; Language Disorders ; epidemiology ; Male ; Mental Disorders ; epidemiology ; Prevalence ; Vision Disorders ; epidemiology

OBJECTIVETo compare the clinical effectiveness of percutaneous US- or CT-guided drainage and laparotomy for patients with infective pancreatic necrosis.

METHODSData of 90 infective pancreatic necrosis patients admitted from January 2008 to December 2009 were included. They were divided into two groups by the different treatment choices. Twenty-seven patients in the percutaneous group received percutaneous US- or CT-guided drainage as first choice. After that a sump suction apparatus was applied for controlled drainage. If no improvement was achieved after 3 days, they would received operation soon. While patients in the laparotomy group received surgical drainage at the time when the diagnosis of infected pancreatic necrosis was confirmed. Continuous drainage was also applied for these ones.

RESULTSThe percutaneous group had a significant low rate of reoperation (7.1% vs. 14.3%, P < 0.05) and postoperative residual abscesses (7.1% vs. 28.6%, P < 0.05). Furthermore, 48.1% of patients in percutaneous group successfully avoid laparotomy. In the regard of complications, the percutaneous group presented lower incidence of both single organ dysfunction (7.4% vs. 28.6%, P < 0.05), intestinal fistula (7.4% vs. 27.0%, P < 0.05) and long-term complications (3.7% vs. 22.2%, P < 0.05). In addition, the percutaneous group costed less medical resources as evidenced by shorter ICU duration (21.2 ± 9.7 vs. 28.7 ± 12.1, P < 0.01), shorter hospital duration (48.2 ± 12.5 vs. 59.6 ± 17.5, P < 0.05) and less expenditure (191 762 ± 5892 vs. 341 689 ± 10 854, P < 0.05).

CONCLUSIONSPercutaneous drainage can effectively lower the surgical rates and the rates of complications and reoperations in patients with infective pancreatic necrosis. Besides that, it could also reduce the cost of medical resources.

Adult ; Drainage ; methods ; Female ; Humans ; Laparotomy ; Male ; Middle Aged ; Pancreatitis, Acute Necrotizing ; surgery ; Retrospective Studies ; Treatment Outcome

This study was purposed to investigate whether phenylhexyl isothiocyanate (PHI) can reduce p16 gene methylation level or not. The myeloma U226 cell line was cultured with PHI of 0, 5, 10 micromol/L for 72 hours, then DNA was extracted. Hydrosulfite was used to treat the genome DNA of healthy adult, PCR amplification was carried out by using this DNA as template. The gene chip detecting methylation changes of 3 CpG in promoter region of p16 gene was constructed by designing a pair of probes which contain one methylated and one unmethylated probes. This pair of probes was used to detect 3 consecutive sites of CpG island in p16 gene. The standard curve was constructed by using gene chip after the methylated and unmethylated DNA were mixed at different ratio. Then treated samples of U266 cells were dotted on gene chip, obtained results were compared with standard curve to get the quantitative results. The results indicated that the probes on chip had excellent reproducible ability and precision, the methylation level of p16 gene in U266 cells treated with 0, 5 and 10 micromol/L of PHI was determined as 78.2%, 61.7% and 54.8%, respectively. It is concluded that the PHI can reduce the methylation level of p16 gene in U266 cells.
Cell Line, Tumor ; CpG Islands ; DNA Methylation ; Down-Regulation ; Genes, p16 ; Humans ; Isothiocyanates ; pharmacology ; Oligonucleotide Array Sequence Analysis