Salbutaml Sulfate Lipid Powder Preparation And Quality Evaluation Of Mist

Salbutamol sulfate is a specific and highly selective β2-receptor agonists, are widely used in the treatment of bronchial asthma, wheezing bronchitis and pneumonia and other respiratory diseases, is considered to be the first selection medicine of prevention and treatment of bronchial asthma. Since the effect of these drugs fast, short half-life, efficacy lasted 4-6 hours, frequent dosing, inconvenient to the patient, the current common market salbutamol sulfate aerosols(such as Glaxo Smith Kline Chongqing Co. salbutamol aerosol drug generally used as a temporary treatment for acute asthmatic airway, bronchitis) in acute onset to relieve asthma good curative effect, can quickly relieve symptoms, quick action, but both immediate-release and sustained-release long-lasting effect of combining aerosol also rarely reported. Therefore, this study design first film dispersion method SAL wrapped in liposomes, then spray-dried liposomes prepared SAL lung powder for inhalation, to inspect its quality and stability, while moving its pharmacokinetics Studies conducted a preliminary evaluation. The main contents and results are as follows:First, to establish the HPLC determination of SAL in vitro drug content, determine to determine the wavelength of 276 nm, the linear equation A=3.3601C-1.6750, r=0.9998, salbutamol sulfate in 7.54μg.ml-1~128.18μg.ml-1 a linear good range.Study of methodology, low, medium and high concentration recovery RSD values are less than 1.79%; day and inter-day precision are good precision, RSD values were less than 0.22%, accessories for the determination without interference, specific, comply with the requirements of methodology. The constant temperature water bath-dialysis method is used for the encapsulation efficiency of liposome SAL.Secondly, the encapsulation efficiency screening of preparation methods, finally select liposome membrane dispersion method to the preparation of SAL. Orthogonal design by water/oil phase, volume, drug/lipid mass than, phospholipids/cholesterol ratios to screen the best prescription; To the hydration temperature, hydration time, ultrasonic time for study factors, the encapsulation efficiency as index, screening the best preparation technology. Ultimately determine the best prescription: phospholipids and cholesterol mass ratio of 6:1, the quality of the drug and phospholipid ratio of 1:10, the water phase and oil phase volume ratio of 3:1; best preparation process: hydration temperature 60℃, hydration time 60 min, ultrasonic time 6min, ultrasonic power 300 w. Optimize the prescription and preparation process of three groups of liposome SAL, measuring the average particle size of 109.7 nm; the encapsulation efficiency was 79.4%.By spray-drying technique SAL lipid suspension prepared powders for inhalation lung. Through the multi-index comprehensive evaluation method to select the optimal prescription: liposome/accessories(proportion of lactose 70% + leucine accounted for 30%) mass ratio of 1:5. Process for the preparation of lipid dry powder inhaler orthogonal optimized to Z points method to evaluate the results and chooses the optimum process conditions, inlet air temperature 150℃, the injection rate 4ml/min, wind speed 4.3m/s, needle frequency for slow. SAL lipid formulation prepared using the best technology and the best preparation of powders for inhalation, particle size and entrapment efficiency of inhalation SAL lipids were investigated after reconstitution, the measured average particle size(118.9±0.31)nm, the entrapment efficiency of 78.20%±1.30%, entrapment rate decreased slightly but not significantly; According to the powder quality evaluation index of its investigation, the results showed that the prepared dry powder inhaler drug SAL lipid content, grain Quality Drive, morphology, atomization and effective lung deposition rates and other indicators are in line with pulmonary administration of dry powder inhaler requirements; and the cumulative release in vitro, the results show: the cumulative release curve is slightly convex, although preliminary However, since the whole is relatively flat, the lipid membrane may be unencapsulated drug rapid release, slow seeping from the latter part of the drug in the lipid backbone, it has immediate release and extend the action time of the combination of effects.