The Preparation Of Paediatric Oral Dry Emulsion And Taste-masking Effect Evaluation

Children are extremely sensitive to the bitter taste of medicine,which affects the amount of the drug taken on time.In this study,paracetamol,ibuprofen,and amoxicillin were used as model drugs in children,and they were prepared as taste-masking dry emulsions by spray drying and freeze drying.The best prescription and preparation process were selected respectively,and their taste-masking effect was evaluated to provide a experimental basis for the development and application of taste-masking dry emulsion.Part One Investigation of prescription process of Dry EmulsionObjective: Screen out the optimal prescription and preparation process of three model drug dry emulsions.Methods: Choose different oil phases and drying methods according to the properties of the drug.The ratio and amount of emulsifier were screened separately through single factor exploration.Orthogonal experimental design was used to further optimize the emulsifier ratio,dosage and solid carrier dosage.Emulsions were prepared by high-speed dispersion,and the emulsification process conditions and different dry emulsion process conditions were screened by single factor investigation.Results:1.According to the prescription and process screening,the best formula for paracetamol dry emulsion was determined as:AAP The drug loading is about 50 mg/gOlive oil 16%Gum Arabic 10.8%Gum tragacanth 1.2%Maltodextrin 12%Water 25 m LThe best technical parameters as: 10000 r/min high speed homogenizer 1 min to produce coarse emulsion.After adding the remaining aqueous phase,high speed homogenizer 5 min to obtain a stable emulsion.The operation parameters of the spray dryer were as follows: inlet temperature of 150?;feeding rate of 20 r/min,Compressed air of 0.2 MPa,air flow rate of 34.2.the best prescription for ibuprofen dry emulsion was determined as:IBU The drug loading is about 40 mg/gOrange oil 4.8%Corn oil 11.2%Gum Arabic 9.6%Gum tragacanth 2.4%Maltodextrin 12%Water 25 m LThe best technical parameters as: 10000 r/min high speed homogenizer 5 min to produce coarse emulsion.After adding the remaining aqueous phase,high speed homogenizer 5 min to obtain a stable emulsion.The operation parameters of the spray dryer were as follows: inlet temperature of 130?;feeding rate of 20 r/min,Compressed air of 0.2 MPa,air flow rate of 34.3.the best prescription for amoxicillin dry emulsion was determined as:AMX The drug loading is about 50 mg/gCorn oil 20%Gum Arabic 16%Gum tragacanth 4%Maltodextrin 15%Water 20 m LThe best technical parameters as: 10000 r/min high speed homogeni zer 3 min to produce coarse emulsion.After adding the remaining aque ous phase,high speed homogenizer 5 min to obtain a stable emulsion.Then transferred to a freezer at-70°C and kept for 6 h.Conclusions: paracetamol,ibuprofen,and amoxicillin dry emulsionswere prepared respectively.Part Two Study on quality of Dry Emulsion.Objective: Respectively to establish methods for determining the content of paracetamol,ibuprofen and amoxicillin.The three dry emulsions were evaluated to investigate the preliminary stability of the dry emulsions.Methods: The content of drugs was determined by high performance liquid chromatography.The specificity,accuracy,precision,stability and recovery of the chromatographic conditions were investigated.Physical chemical property and dissolution of dry emulsions are detected.Including the distribution of particle size before and after Spray Drying,surface structure,drug loading,dissolution in vitro of dry emulsions.The stability of the dry emulsion was investigated by the influence factor test on the appearance of the preparation and the drug content.Results: The established conditions of high performance liquid chromatography were characterized by high specificity,precision,stability,and recovery.AAP,IBU,AMX emulsions have same appearance before and after Spray Drying.The particle size of the redispersible emulsion is 1.91?5.04?4.17 ?m,The surface of AAP and IBU dry emulsions are smooth and round,and the AMX dry emulsion has pore structure inside,the drug loads of the three dry emulsions are 47.94,36.52,47.77 mg/g,which can release more than 80% accumulatively within 30 min.The experimental results of influencing factors show that AAP and IBU dry emulsions have good stability to high temperature,high humidity and illumination,while AMX dry emulsions are sensitive to high temperature and high humidity.Conclusions: The Established chromatographic conditions meet the methodological requirements and can be used to determine the content of drugs.The dry emulsion has good redispersibility,complete appearance and its dissolution meets the requirements of pharmacopoeia for quick release;The effects of temperature and humidity on the preparation,storage and transportation of AMX dry emulsion should be paid attention to.Part Three Taste evaluation of Dry EmulsionObjective: The taste masking effects of three model drugs dry emulsions were investigated separately.Methods: Evaluation of taste masking effect selected scriptures group by taste,two-bottle preference test and brief-exposure tests.Results: The results of the classical mouth-tasting method showed that the dry emulsion had a taste-masking effect;in the animal experiment,the preference index for the emulsion in the two-bottle preference method was greater than 0.5;in the results of the Brief-exposure tests,the frequency of licking of the emulsion was higher than Drug suspensions and commercially available formulations.Conclusions: Preparation of the drug as a dry emulsion has a better taste-masking effect.