OBJECTIVE: To explore the characteristics of crystallization inhibition by cellulose polymers against supersaturated drugs. METHODS: The biopharmaceutics classification system(BCS) II class drug indometacin was selected as the model drug.Supersaturated amorphous drug solid was prepared and the solubility of indometacin was measured. The types, added amounts, ionic intensity and viscosity of cellulose polymers were employed as influential factors to assess the crystallization inhibition effect of polymers against indometacin. RESULTS: HPMC E15 displayed the strongest crystallization inhibition effect. The crystallization inhibition was enhanced by adding larger amount of polymers, decreasing the viscosity of polymers and increasing the ionic intensity. CONCLUSION: The study is helpful to clarify the profiles that cellulose polymers inhibit the crystallization of drugs in supersaturated states. This research may provide scientific guide for the practical application of cellulose polymers for drug crystallization.

OBJECTIVE: To prepare curcumin solid dispersions by different preparation technologies and compare their properties. METHODS: Curcumin/poloxamer 407 solid dispersions were prepared by freeze-drying, co-precipitation and microwave/quench cooling methods, respectively. Internal properties of obtained solid dispersion were analyzed by SEM, DSC, XRD and FT-IR. The improvement effect on the insolubility of curcumin by making it into solid dispersions by different technologies was characterized by dissolution and solubility experiments. RESULTS: Curcumin was dispersed in solid dispersions in micro-crystal form. Compared with other technologies, microwave/quench cooling method could significantly improve the solubility and dissolution of insoluble curcumin. CONCLUSION: The study provides reference for choice of applicable production technology for solid dispersions of insoluble Chinese traditional medicine curcumin.

Low back pain is an important cause of disability worldwide. It has a high incidence rate and brings a huge burden to families and society. Intervertebral disc degeneration (IDD) is one of the leading factors causing low back pain and the pathological basis of degenerative disc diseases, such as intervertebral disc herniation and spinal stenosis. However, the etiology of IDD is complex, and the risk factors and specific mechanisms behind remain unclear. Some controversial views have also been observed. Surgery is often considered for patients with severe intervertebral disc diseases, but there is no effective treatment for IDD at the early and middle stages. It will be of great significance to in-depth explore the molecular biological mechanisms and related risk factors, which can bring benefits to the prevention, accurate diagnosis, early treatment, and rehabilitation of degenerative disc diseases. Refer to the literatures published in the past ten years, this paper describes the latest research progress on risk factors related to IDD in terms of aging, genetics, mechanical loading, low-grade infection, biological rhythms, smoking, metabolic disease, estrogen, and nutrition. The results show that IDD is affected by multiple risk factors. These factors can interact with each other, and lead to death, phenotypic transformation, and metabolic disorder of disc cells, leading to a reduction of extracellular matrix and an unbalanced microenvironment and eventually loss of structural integrity of intervertebral disc tissue and IDD. A good body clock, a controlled weight, an appropriate blood glucose level, adequate nutrition, no smoking, a good hormone level, moderate exercise, avoiding injury, and strict aseptic techniques in the clinic will bring benefits to the progress of IDD.

Microwaves can be directly transformed into heat inside materials because of their ability of penetrating into any substance. The degree that materials are heated depends on their dielectric properties. Materials with high dielectric loss are more easily to reach a resonant state by microwaves field, then microwaves can be absorbed efficiently. Microwave irradiation technique with the unique heating mechanisms could induce drug-polymer interaction and change the properties of dissolution. Many benefits such as improving product quality, increasing energy efficiency and reducing times can be obtained by microwaves. This paper summarized characteristics of the microwave irradiation technique, new preparation techniques and formulation process in pharmaceutical industry by microwave irradiation technology. The microwave technology provides a new clue for heating and drying in the field of pharmaceutics.
Chemistry, Pharmaceutical ; methods ; Drug Discovery ; instrumentation ; methods ; Microwaves ; Pharmaceutical Preparations ; administration & dosage ; chemistry ; Technology, Pharmaceutical ; methods

Converting two poorly water-soluble crystalline drugs to co-amorphous drug systems by ball milling, quench-cooling, or cryo-milling method can improve stability of the drug, enhance dissolution rates, and reduce adverse reactions of the single drug. Co-amorphous system has been used to solve problems of co-administration of medicines. Formation and intermolecular interactions of co-amorphous drug systems may be verified by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Raman spectroscopy (RS) and Fourier transform infrared spectroscopy (FT-IR). Stability of co-amorphous drug systems is influenced by their glass transition temperature (Tg) and intermolecular interactions. The theoretical Tg values and the interaction parameter x are calculated by Gordon-Taylor equation and the Flory-Huggins equation, respectively. Thus, co-amorphous drug systems are analyzed theoretically at molecular level. Co-amorphous drug systems provide a new sight for the co-administration of medicines.
Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; methods ; Cimetidine ; chemistry ; Drug Combinations ; Drug Compounding ; Drug Stability ; Glipizide ; chemistry ; Indomethacin ; chemistry ; Naproxen ; chemistry ; Ranitidine ; chemistry ; Simvastatin ; chemistry ; Solubility ; Spectroscopy, Fourier Transform Infrared ; Spectrum Analysis, Raman ; Technology, Pharmaceutical ; methods ; Temperature ; X-Ray Diffraction

Objective:To research the best processing method for Bupleurum chinense DC.by orthogonal tests.Methods:With the contents of saikosaponin a and saikosaponin d as the indices,the L9(34) orthogonal table was used to study three factors including the amount of wheat bran,pot temperature before heating and processing time.The orthogonal design was applied to study the processing technology of Bupleurum chinense DC.fried with wheat bran.Results:The best processing method was as follows:100 g Bupleurum chinense DC.was mixed with 10 g wheat bran and fried at 290 ℃ for 80 seconds.Conclusion:The optimized processing technology is reasonable,reliable and highly reproducible,which provide reference for the processing of Bupleurum chinense DC.with wheat bran.

Objective To investigate and analyze the epidemiological characteristics of eye injury among military inpatients. Methods Data of eye injury among military inpatients from 15 military general hospitals during 2001 --2005 were recorded and statistically analyzed. Results There were 716 military inpatients with eye injuries, taking up 7.41% of the whole ocular trauma inpatients in corresponding time period. Military inpatients with eye injuries were admitted more in spring and summer; with sex ratio as 46.73:1 ; mean age as (24.99±8.40) years and 82.27% in 17-29 years while 7.82% were binocular injuries. A certain proportion of the complication appeared after the myoporthosis operations. Mechanical and non-mechanical eye injuries took up 92.49% and 7.51% respectively. Sports (17.62%), explosion (11.92%) and fighting (11.40%) related factors were the main causes of injuries. 51.55% of the accidents took place during working or training processes and 30.31% was on military training sites. At discharge, 22 eyeballs were removed mainly due to open globe injuries, 9 eyes with no light perception but vision acuity equalled to or more than 0.5 in 62.16% of the patients. Conclusion Of those eye injury inpatients, military training and construction for defense were the main causes related to occupational eye injuries among soldiers. Mutilation power of eye injury should not be ignored and epidemiological survey on military eye injuries need to be carried out more extensively.

OBJECTIVETo investigate the function of POLH(polymerase eta) through establishment of the POLH gene-blocked cell line FL-POLH(-).

METHODSA mammalian expression vector expressing antisense POLH gene fragment pMAMneo-amp-POLHA (-) was constructed by cloning the 1473 - 2131 fragment of POLH gene into the mammalian expression vector pMAMneo-amp(-) in antisense orientation. The FL cells were transfected with this antisense RNA expressing vector and selected by G418. The mutation assay was conducted using the shuttle plasmid pZ189.

RESULTThe spontaneous mutation frequency of SupF tRNA gene in the plasmid replicated in the FL-POLH(-) was 13.5 x 10(-4), while it was 4.9x10(-4) and 3.7x10(-4) in the control cells FL and FL-M, respectively. The nontargeted mutation frequency of SupF tRNA gene decreased in the plasmid replicated in these cell lines pretreated with MNNG.

CONCLUSIONPOLH plays an important role in maintenance of genetic stability and genesis of nontargeted mutation.

Antisense Elements (Genetics) ; pharmacology ; Cell Line ; DNA-Directed DNA Polymerase ; genetics ; physiology ; Methylnitronitrosoguanidine ; toxicity ; Mutagenesis

Adolescent ; Brain Neoplasms ; metabolism ; pathology ; Diagnosis, Differential ; Female ; Humans ; Melanoma ; metabolism ; pathology ; Melanoma-Specific Antigens ; metabolism ; Neurilemmoma ; metabolism ; pathology ; S100 Proteins ; metabolism ; Vimentin ; metabolism

AIMTo study the effect of experimental left varicocele (ELV) on epididymal structure and function in adolescent Sprague-Dawley rats.

METHODSELV was induced by partial ligation of the left renal vein. Sham-operated animals served as the controls. Four and 8 weeks after the operation, the histological, ultrastructural and biochemical (alpha-glucosidase activity and carnitine content) changes in different segments of the epididymis were observed.

RESULTSIn the treated animals, there were degeneration of the epididymal epithelium and edema of the interstitial tissue; numerous shedding cells, residual bodies, deformed sperm and macrophages appeared in the epididymal lumen. Morphometric measurement indicated a significant reduction in the epididymal tubular diameter (P<0.05) and a significant increase in the epididymal interstitial area (P<0.05) compared with the controls. Ultrastructural study showed sparse microvilli of the columnar epithelium, increased and enlarged lysosomes in the principal cells with defected organelles and the presence of large cytoplasmic vacuoles. The protein and carnitine contents and the alpha-glucosidase activity in the caput, corpus and cauda epididymis of the ELV rats were lower than those of the controls (P<0.05).

CONCLUSIONThere were structural and functional changes in the epididymis of adolescent ELV rats, which may contribute to the infertility caused by varicocele.

Animals ; Carnitine ; metabolism ; Epididymis ; enzymology ; pathology ; physiopathology ; ultrastructure ; Male ; Microscopy, Electron ; Rats ; Rats, Sprague-Dawley ; Varicocele ; enzymology ; pathology ; physiopathology ; alpha-Glucosidases ; metabolism