Quality control and physico-chemical properties of vitamin K1 self-nanoemulsifying drug delivery systems / 国际药学研究杂志

Objective To establish assay methods for the determination of dissolution,content and related substances of vita-min K1 self-nanoemulsifying drug delivery system(VK1-SNEDDS),and investigate the physico-chemical properties of the preparation. Methods The UV method was established to determine the dissolution of VK1-SNEDDS. The content and related substances were de-termined by HPLC. The appearance,self-emulsification time,micro-morphology,droplet size and zeta potential were also investigat-ed. Results The linearity range of established UV and HPLC methods was 0.85-20.4 and 2.16-216μg/ml,respectively,and all the recovery,precision,specificity and sensitivity met requirements. VK1-SNEDDS could disperse quickly after dilution. The transmission electron microscope(TEM)image of the optimized liquid SNEDDS showed that most of the emulsion droplets were of uniform size with no signs of coalescence. Droplet size of optimal formulation was revealed as 47.74 nm with polydispersibility index(PDI)of 0.248,and zeta potential was found to be-20.53 mV. Conclusion VK1-SNEDDS could form homogeneous and stable nanoemulsion when dilut-ed with aqueous phase and increase the dissolution of lipophilic drug. The methods are reliable,accurate and suitable for quality con-trol of VK1-SNEDDS.

Nanodrug delivery systems based on drug-phospholipid complex:research advances / 国际药学研究杂志

Phospholipids are the major components of the biomembrane. Combining the phospholipids and the drugs to form drug-phospholipid complex can improve the solubility,stability and bioavailability of the drugs. On this basis,the nanodrug delivery system,which is constructed with the drug-phospholipid complex as an intermediate carrier,has become a research hot spot in the field of pharmaceutics. This kind of nanodrug delivery system can not only improve the solubility,stability and bioavailability of drugs,but also carry out the targeted drug delivery,decrease the drug dose and reduce the side effects,thereby it is very promising. In this review,we describe the structural composition,characteristics,forming mechanism of the drug-phospholipid complex and the research progresses in a variety of nanodrug delivery systems based on drug-phospholipid complex.

Preformulation study on anti-smallpox drug tecovirimat / 国际药学研究杂志

[Abstact] Objective To study the preformulation properties of tecovirimat for formulation design. Methods The appear?ance,crystal structure,solubility and permeability of the drug were investigated. The UV method was established to determine the con?tent of tecovirimat in vitro. The solubilization experiment was also conducted. Results Tecovirimat is white and odorless powder with crystalline hydrate structure and low water-solubility with high permeability. The morphology of tecovirimat is six-prismatic-shape. The linearity range of established UV method was 4.14-24.83μg/ml(r=0.9996). The 1∶1 soluble complex was formed with tecovirimat and hydroxypropyl-β-cyclodextrin. Conclusion Tecovirimat is poorly water-soluble drug with high permeability and the established meth?od could be used to determine the content of the drug. Hydroxypropyl-β-cyclodextrin could be used for the solubilization of tecovirimat.

Developing specific drug/device combination products improves the treatment level of the acute chemical injury / 国际药学研究杂志

To deal with effectively acute chemical injury events,the service ability of protective medicine against chemical weapons has being widened from dealing with traditional chemical warfare to public chemical accident or chemical terrorist attack. Fo?cusing on the important researching and developing of medicine for chemical defense use only,the novel drug/device combination products should be vigorously promoted including the new mechanism,good curative effect and high safety of detoxification drugs such as hydroxycobalamin used in the treatment of known or suspected cyanide poisoning in both adults and the pediatric population ,and the convenient and quick drug delivering technologies such as auto-injectors with a retreat hidden needle and a smart remindful injec?tion,which could improve greatly the emergency medical rescue ability of chemical accidents.

A retrospective study on deep lobe tumor parotidectomy with preservation of the superficial lobe / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To study our experiences on deep lobe tumor parotidectomy with preservation of the superficial lobe of the parotid gland.@*METHOD@#Eleven cases of benign tumor in the deep lobe of the parotid gland were analyzed restrospectively. Tumour recurrence, Frey's syndrome, paralysis of facial nerve, salivary fistula, dry mouth and feeling around the auricular lobule were evaluated.@*RESULT@#Numbness around the auricular lobule appeared in 2 cases and salivary fistula appeared in 1 case, transient facial paralysis in 1 case. There were no patients appeared Frey's syndrome, dry mouth, permanent facial paralysis and recurrence in the 1-3 years followed up time.@*CONCLUSION@#Deep lobe tumor parotidectomy with preservation of the superficial lobe improves the cosmetics and the feeling around the auricular lobule, reduces the incidence rate of Frey's syndrome, facial paralysis and dry mouth.

HPLC methods for analysis of related substances and their content in dexmethyl-phenidate hydrochloride sustained-release pellets / 军事医学

Objective To establish an HPLC method for determination of related substances of dexmethylphenidate hydrochloride and their content .Methods The HPLC method was used on an Agilent ZORBAX SB-C18 column with a mo-bile phase of methanol-0.2%triethyl citrate in 25 mmol/L potassium dihydrogen phosphate ( pH was adjusted to 3.5 with phosphoric acid) (35∶65) at a flow rate of 1.0 ml/min.The detection wavelength was 209 nm and column temperature was 40℃.Results Under the selected chromatographic condition , dexmethylphenidate hydrochloride was completely separated from impurity.The limit of detection was 81.12 ng/ml.The calibration curve was linear in the range of 2-30 μg/ml ( r=0.9995).The average recovery of the method was 100.83%, and the stability of the working solution was acceptable in 12 h(RSD=0.10%).Conclusion This method is simple,specific,accurate and suitable for analyzing the related substances and their content in dexmethylphenidate hydrochloride .

Development of chemical defense medicine driven by biotechnology / 国际药学研究杂志

The health service of chemical defense medicine is an important guarantee for national security, which has been expanded from dealing with traditional pure chemical warfare to current medical treatment of poisoning caused by public chemical accident, chemical terrorist attack, or future potential toxic agents at the boundary of chemistry and biology. The most recent scientific and technical disciplines, such as synthetic biology, pharmaceutical bioinformatics, nanotechnology, or drug/device combinatorial technology, should be utilized greatly to enhance the ability of the health service of the chemical defense medicine. And it is also important to establish and improve such management practice of emergence medicine as shelf life extension program or emergency use authorization.

Expression of serum YKL-40 in anaphylactic rhinitis patients and association of serum YKL-40 with serum IL-4 and IFN-γ / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#This study intends to preliminarily discuss the expression and the clinical meaning of serum YKL-40 in anaphylactic rhinitis by comparing the different expressions of serum YKL-40 in types of anaphylactic rhinitis, and to preliminarily discuss possible mechanism of having anaphylactic rhinitis involved with serum YKL-40 by associating it with serum IL-4 and IFN-γ in anaphylactic rhinitis.@*METHOD@#Firstly, each select 20 people in our hospital who have anaphylactic rhinitis respectively according to different levels--mild intermittent, mild persistent, moderate-severe interminttent, moderate-severe persistent as the experimental groups, while 20 healthy people as the nomal control. Secondly, test the levels of serum YKL-40, IL-4 and IFN-γ respectively in each group by the ELISA method. Thirdly, statistically analyze and discuss the collected data.@*RESULT@#(1) There was a rise in the expression of serum YKL-40 between the experimental groups and the nomal control group, which contained a statistical significance (P 0.05). (2) There was a rise in the expression of serum IL-4 between the experimental groups and the nomal control group, which contained a statistical significance (P 0.05). (3) There was a reduction in the expression of serum IL-4 be- tween the experimental groups and the nomal control group, which contained a statistical significance (P 0.05). (4) The corelation between serum YKL-40 and IL-4 in anaphylactic rhinitis was positive, while the corelation between serum YKL-40 and IFN-γ was negative.@*CONCLUSION@#(1) Allergic rhinitis serum YKL-40 expression was increased. The corelation between serum YKL-40 and IL-4 in anaphylactic rhinitis was positive, while the corelation between serum YKL-40 and IFN-γ was negative,suggesting that YKL-40 may regulate the differentiation of Th cells, Promote Th1 to Th2 immune shift, through this mechanism involved in the pathogenesis of allergic rhinitis. (2) Compared with patients with intermittent allergic rhinitis, persistent allergic rhinitis serum YKL-40 expression was increased, suggesting that YKL-40 may promote the continuous attacks of the symptoms of allergic rhinitis.

Expression of phosphofructokinase 1 protein and it's enzyme activity on nasopharyngeal carcinoma / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#The aim of this study is to investigate the expression of phosphofructokinase 1 and it's enzyme activity in nasopharyngeal carcinoma biopsy samples.@*METHOD@#Sixty-one biopsy samples were detected, including 41 tissues from patients with nasopharyngeal carcinoma as experimental group and 20 tissues from patients with chronic nasopharyngitis as control group. Phosphofructokinase 1 protein was detected by Western blot and it's enzyme activity was detected.@*RESULT@#It was observed that the expression levels of phosphofructokinase 1 protein and it's enzyme activities in the experimental group were higher than that in the control group (P < 0.01). In the experimental group, the expression levels of phosphofructokinase 1 protein and it's enzyme activities in patients with lymph node metastasis were higher than that in patients without lymph node metastasis (P < 0.01).@*CONCLUSION@#Phosphofructokinase 1 may be a marker in occurrence and metastasis of nasopharyngeal carcinoma.

Expression and clinical significance of 6-phosphofructo-1-kinase in nasopharyngeal carcinoma / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#The aim of this study is to investigate the expression and clinical significance of 6-phosphofructo-1-kinase in nasopharyngeal carcinoma biopsy samples.@*METHOD@#Sixty-one biopsy samples were detected, including 41 tissues samples from patients with nasopharyngeal carcinoma and 20 tissues samples from patients with chronic nasopharyngitis as control group. 6-phosphofructo 1 kinase mRNA expression was detected by RTPCR.@*RESULT@#It was observed that the expression levels of 6 phosphofructo-1-kinase mRNA in nasopharyngeal carcinoma tissues were higher than in the chronic inflammatory tissues. And the expression levels in patients with lymph node metastasis were higher than without lymph nod metastasis.@*CONCLUSION@#6-phosphofructo-1-kinase may be a marker in occurrence and metastasis of nasopharyngeal carcinoma.

Anatomy of marginal mandibular branch of facial nerve in partial parotidectomy / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To study our experiences in anatomy of marginal mandibular branch of facial never in partial parotidectomy.@*METHOD@#Thirty-eight cases receiving partial parotidectomy were analyzed retrospectively, and marginal mandibular branch of facial nerve were separated in all cases.@*RESULT@#Temporary facial paralysis appeared in 2 cases and Frey's syndrome appeared in 2 cases. There was no patient appeared the recurrence in the 1-3 years followed up time.@*CONCLUSION@#Partial parotidectomy with anatomy of marginal mandibular branch of facial nerve is a safe, effective and minimally invasive therapeutic method for benign tumor on parotid gland (<5 cm).

Combination therapy of plasma radiofrequency ablation at low temperature and nasal endoscopy for chronic na-sal sinusitis / 局解手术学杂志

Objective To explore the curative effect of combination therapy of low-temperature plasma radiofrequency ablation and nasal endoscopy for chronic nasal sinusitis. Methods From January 2010 to January 2012,98 patients with chronic nasal sinusitis in our hospital were ramdomly divided into observation group and control group. The observation group (49 cases) received plasma radiofrequency ablation at low temperature combined nasal endoscopic treatment. The control group (49 cases) were performed only nasal endoscopic treatment. The curative effect of the 2 groups were compared. Results After 1 month and 1 year, the total effective rate of the observation group were 91. 84% and 89. 80%, the total effective rate of the control group were 77. 55% and 73. 47% respectively. To compare the total effective rate of 2 groups were compared,there were statistically significant differences(P<0. 05). Conclusion Curative effect of plasma radiofrequency ablation at low temperature and nasal endoscopy is distinct,it is worthy of being widely applied in clinic.

Auto-injector:a supporting approach of emergency medicine for the first-aid / 国际药学研究杂志

Auto-injector, a spring-driven drug-device based combination production that automatically injects the drug into the skin via a pre-filled syringe or cartridge, allows minimally trained individuals to self-inject potentially life-saving medication when e-mergency medical care may be absent or remote, and thus has been becoming a supporting approach of emergency medicine for the first-aid. The auto-injector was developed originally by the United State of America, and experienced the three outstanding states in-cluding syrettes, single chamber auto-injectors and dual chamber auto-injectors from the battlefield to the civilianization. The current auto-injector devices have five different types named as ACE (AtroPen), ComboPen, Binaject, Soluject and Truject, respectively. The applied drugs to the systems for military use have atropine, pralidoxime chloride, obidoxime, diazepam and morphine sulfate. The oth-er drugs for emergency medical use such as epinephrine, lidocaine hydrochloride and sumatriptan have been also applied to. All of the auto-injector based combination production have been twined with a simulator in order to conduct a training schedule before use. Importantly, the needle hidden or the device-status notification technique after injection has been becoming a trend in the technology advances of the auto-injectors.

Formulation optimization of metoprolol succinate sustained release pellets using central composite design-response surface methodology / 军事医学

Objective To optimize the formulation of metoprolol succinate ( MS) controlled release pellets by central composite design-response surface methodology .Methods MS sustained-release pellets were prepared using sugar pellet cores as starter beads , ethyl cellulose as coating materials and MS itself as a pore former .The formulation of MS sustained-release pellets was optimized by a central composite design with two factors at five levels .These two factors ( two independ-ent variables) were the pore former level and coating level , and the evaluated indexes ( namely dependent variables ) included the in vitro cumulative release percentages of MS at 1, 4, 8, 12 and 16 h, respectively.Results and Conclusion The results of mathematical equation fitting suggested that the second-order quadratic model was the optimal fitting equa-tion.According to the response surfaces , the optimum values at the pore former level and coating level weve ranged from 16%to 18%and 20% to 25%, respectively .The in vitro cumulative release percentage of MS from the pellets at 1 h reached 9.15%,which consequently eliminated the lag phase in the initial release period and exhibited a good sustained-release effect.Central composite design-response surface methodology can be applied to optimizing the coating formulation for MS sustained release pellets .

Selection of surfactants and dissolution profiles of nimesulide sustained-release tablets / 军事医学

Objective To study the effect of surfactants on the dissolution profiles of poorly water-soluble acidic drug nimesulide from sustained-release tablets.Methods The anionic surfactant sodium dodecyl sulfate (SDS), cationic sur-factant cetyltrimethyl ammonium bromide (CTAB) and nonionic surfactant polysorbate 80 (Tween 80) were used to prepare nimesulide micelles .The effect of the buffer , surfactant and ionic strength on the equilibrium solubility of the drug and the in vitro release of sustained-release tablets was studied .Results and Conclusion In pH 1.2 HCl solution, water and pH 6.8 phosphate buffer, the solubilization capacity of CTAB was the highest.However, in pH 9.0 Tris buffer, when CTAB concen-tration was at about 1%, the equilibrium solubility of nimesulide was at the trough value .The in vitro release results were similar to those of equilibrium solubility and the kinetic pattern conformed to the first order equation according to the coefficient R .

Coated pellets:the emerging direction of oral modified-release solid dosage forms / 国际药学研究杂志

Oral modified-release multiple-unit dosa ge forms such as coated pellets have always been more effective therapeutic alternative to conventional single-unit dosage forms. Coated pellets ranging in size,typically,between 0.5-1.0 mm,are produced primarily for the purpose of oral controlled-release dosage forms having gastro-resistant or sustained-release properties or the capability of site-specific drug delivery. With regards to the final dosage form,the multi-particulates are usually formulated into single-unit dosage forms such as filling them into hard gelatin capsules or compressing them into tablets. As drug-delivery systems become more sophisticated,the role of pellets in the design and development of dosage forms is increasing. The safety and efficacy of the formulation is higher than that of other dosage forms. This review provides an update on this research area and discusses the phenomena and mechanisms of the multi-particulate system concluding multiple-unit pellet system and pellet-containing tablets.

Intralesional bleomycin-A5 with dexamethasone injection under pedestal laryngoscope for huge laryngopharyngeal and laryngeal hemangiomas / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To investigate the therapeutic effect of intralesional bleomycin-A5 with dexamethasone injection under pedestal laryngoscope for huge laryngopharyngeal and laryngeal hemangiomas.@*METHOD@#Intralesional bleomycin-A5 with dexamethasone injection under pedestal laryngoscope was performed in huge laryngopharyngeal and laryngeal hemangiomas.@*RESULT@#The injection frequencies were 3 times in 4 cases, 4 times in 3 cases, and 5 times in 9 cases. Twelve cases (75%) were cured, and 4 cases (25%) were improved.@*CONCLUSION@#Intralesional bleomycin-A5 with dexamethasone injection under pedestal laryngoscope is a safe, effective and minimally invasive therapeutic method for huge laryngopharyngeal and laryngeal hemangiomas.

Epidemiological investigation on relativity of allergic rhinitis and recurring respiratory infection of preschool children in Shenzhen / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To understand the prevalence rate and the relativity of allergic rhinitis and recurring respiratory infection of preschool children in Shenzhen, and to investigate and analyse the prevalence rate, predisposing factor, allergen, therapy, turnover on allergic rhinitis and recurring respiratory infection of preschool children.@*METHOD@#The ENT doctors examined the investigated children and recorded them, then delivered questionnaires to the children's parents and explained to them. The result was analyzed statistically.@*RESULT@#The prevalence rate of allergic rhinitis of preschool children in Shenzhen was 20.1%, the prevalence rate of recurring respiratory infection was 13.7%, the prevalence rate (18.0%) of allergic rhinitis combined recurring respiratory infection was higher than that (7.80) of cases with non-allergic rhinitis combined recurring respiratory infection. The difference had a statistical significance (P < 0.05).@*CONCLUSION@#We initially understood the epidemiologic situation of allergic rhinitis and recurring respiratory infection of preschool children in Shenzhen, providing epidemiologic datas for the standardization of prevention and cure for allergic rhinitis.