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Objective: To optimize the formula of bromhexine hydrochloride dry powder inhalations (BH DPIs). Methods: BH DPIs were prepared by freezing-drying combined with an air-jet milling method. Three factors, including the weights of mannitol (X1), leucine (X2) and poloxamer 188 (X3) in the formula were known to be associated with the quality of BH DPIs. A central composite design was used to investigate the effects of the three factors on the response angle (Y1), fine particle fraction (FPF, Y3) and aerody-namic diameter (Y4). Response surface and overlay contour plot were delineated according to the best-fit mathematic models. Opti-mum formula was selected by overlay contour plot. Results: The quantitative relationships between the three factors and the three re-sponses were obtained. The optimal formula was mannitol﹕leucine﹕poloxamer 188 (2. 4: 2. 22: 0. 05) in the excipients. The pre-dicted and observed values of the optimum formula were similar. Conclusion: The multi-objective simultaneous optimization of the for-mula of BH DPIs is achieved by central composite design-response surface methodology.
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Objective:To explore the effects and mechanism of liraglutide on nitrogen monoxide (NO) release in human umbilical vein endothelial cells in the state of hypoxia and high glucose.Methods:A model of hypoxia and high glucose was established by using isolation and culture of primary human umbilical vein endothelial cells (HUVECs) in vitro.HUVECs were incubated with liraglutide and/or exendin (9-39) for 4 h.The metabolic ability of cells was detected by MTT assay,the activity of lactate dehydrogenase (LDH) was measured by a colorimetric method,and the levels of extracellular NO were measured by a nitrate reductive enzymatic method.The endothelial nitric oxide synthase (eNOS) mRNA expression was detected by reverse transcription-polymerase chain reaction (RT-PCR).Results:Compared with the model group,liraglutide could significantly increase cell metabolic ability,reduce LDH release,increase NO release and eNOS mRNA expression (P<0.05 or P<0.01).The above effects of liraglutide were partly inhibited by glucagon like peptide-1 (GLP-1) receptor antagonist exendin (9-39)(P<0.05).Conclusion:Liraglutide can improve endothelial relaxation function in HUVECs in the state of hypoxia and high glucose in vitro.The effect might be related to up-regulating eNOS mRNA expression and promoting NO release.
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Objective:To establish an analytical method for the determination of furazolidone and indometacin in furazolidone, in-dometacin and cuscohygrinolis α-acetylbenzoacetate suppositories by HPLC. Methods: The separation was performed on a ZORBAX Extend-C18 (250 mm × 4. 6 mm,5μm) column. The mobile phase was acetonitrile and 0. 035 mol·L-1 potassium phosphate monobas-ic aqueous solution (adjusting pH to 3. 0 with acetic acid) with gradient elution. The flow rate was 1. 0 ml·min-1, and the detection wavelengths were set at 364 nm and 318 nm. The column temperature was 30℃ and the injection volume was 20 μl. Results:Under the selected chromatographic conditions, the two components showed good linearity within the range of 0.005-0.05 mg·ml-1(r=0. 9999). The limit of detection was 20 ng·ml-1 and 26 ng·ml-1, respectively. The limit of quantitation was 70 ng·ml-1 and 90 ng·ml-1, respectively. The average recovery was 99. 4％(RSD=0. 6％, n=9)and 99. 4％(RSD=0. 3％,n=9),respectively. Conclusion:The method is simple, rapid and specific, and the results are accurate and reliable. The method can be used for the de-termination of the two components in furazolidone, indometacin and cuscohygrinolis α-acetylbenzoacetate suppositories.
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Objective To prepare vinorelbine bitartrate long-circulation liposomes by pH gradient loading methods and make characterization. Methods The impact of hydration temperature and extrusion times on the blank liposome particle size was investigated;and the incubation temperature and in duration on size and encapsulation percentage of drug loading liposome particle was tested. The vinorelbine bitartrate long-circulation liposome was characterized for particle size,polydispersion index, Zeta potential,morphology,and was studied for long term stability. Results The particle size,Zeta potential,polydispersion in-dex of long-circulation liposomes were (96. 4±27. 2) nm,(0. 162±0. 042),(-26. 7±3. 5) mV,respectively. The liposomes were small,unilamellar and spherical with smooth surface under transmission electron microscopy. Long term stability studies showed that the liposomes were stable for up to 3 months after storage at 5 ℃ . Conclusion The preparation technology for the vinorel-bine bitartrate long-circulation liposome by pH gradient loading methods is feasible.
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Objective:To establish a method to determine the content of lidocaine hydrochloride in buccal adhesive tablets contai-ning carbomer as an excipient by HPLC. Methods:Calcium chloride was used to precipitate carbomer in buccal adhesive tablets. The HPLC analysis was performed on a Welch C18 column(250 mm × 4. 6 mm,5 μm)with the column temperature of 40℃. The mobile phase was the mixture of 0. 05% sodium acetate solution(added 50 ml acetic acid into 930 ml distilled water,adjusting pH to 3. 40 with 1 ml·min-1 sodium hydroxide solution)and acetonitrile(70:30). The flow rate was 1. 0 ml·min-1 ,the detection wavelength was at 254 nm and the injection volume was 20 μl. Results:Within the range of 0. 10-2. 00 mg·ml-1 ,there was a good linear rela-tionship between the concentration and the peak area of lidocaine hydrochloride(r=0. 999 9). The average recovery was 100. 2%( RSD=1. 4%,n=9). Conclusion:The established method is simple,accurate and reproducible,which can be applied to determine the content of lidocaine hydrochloride in buccal adhesive tablets.
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Objective:To optimize the formula of mirtazapine orally disintegrating tablets by orthogonal experiment and determine the stability preliminarily. Methods:The formula was optimized by orthogonal experiment based on 4 impacting factors:the amount of mannotil (A), microcrystalline mellulose (B), low substituted hydroxypropyl cellulose (C) and cross-linked polyvinylpyrrolidone ( D) , respectively with 2 indices of disintegration time and dissolution. The release rate of the orally disintegrating tablets and the ref-erence tablets was studied by similarity factors. The stability was respectively studied by high temperature test, high humidity test and photostability test. Results:The optimum formula of the tablets was as follows:the amount of A, B, C and D was 70, 20, 2. 5 and 10 mg, respectively. The f2 for the orally disintegrating tablets and the reference tablets in the dissolution medium was 63. 38. Conclu-sion:The formula is reasonable, the preparation process is feasible and the quality is stable.
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Objective: To optimize the formula of compound asiaticoside gel plasters, and determine the optimal preparation process. Methods:Using the initial adhesion, viscosity and appearance as the indices, the gel plasters were evaluated by orthogonal design in order to study the effects of various base ratios on the preparation and screen the optimal formula and preparation process. Re-sults:The optimal formula was dihydroxyaluminium aminoacetate∶EDTA∶glycerol∶CMC-Na of 0. 25∶0. 05∶45∶1. Conclusion: Com-pound asiaticoside gel plasters with the optimal formula and preparation technique show good adhesion and uniformity, which can meet the need of large-scale production.