ABSTRACT
Chloral hydrate is a commonly used central sedative drug before pediatric clinical examination, but its clinical safety and medication adherence are needed to focus on normally because of its poor stability and palatability. Under the premise of investigating the stability of different formulations, their palatability were also screened by using both human sensory and electronic tongue evaluation techniques. Human sensory evaluation has been conducted with the informed consent of all participants in accordance with the ethical requirements of the Good Clinical Practice for Drug Trials. The results showed that the addition of sorbitol and sucralose could effectively ensure the stability of the oral solution. Sorbitol is the main taste-masking component, and the ratio of 40% sorbitol and 0.5% sucralose can effectively mask the bitterness, astringency and spicy taste of 10% chloral hydrate oral solution. The results detected by human sensory and electronic tongue have good correlation and complementarity, and the combination of these two methods is more conducive to getting objective and reasonable conclusions.
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Texture analyzer is a multifunctional physical property analyzer. Through a variety of test modes such as compression， puncture， shearing and stretching， hardness， adhesion， elasticity， cohesiveness and other physical property parameters are characterized. The results are objective， sensitive， and accurate， which can provide theoretical basis and reference for interpretation of basic theoretical， optimization of prescription technology and quality control research of pharmaceutical preparations. Firstly， the principles， test modes， measurement indexes and measurement data analysis methods of texture analyzer were summarized in this paper. Secondly， the application progress of texture analyzer in solid preparations， semi-solid preparations， liquid preparations， traditional Chinese medicine decoction pieces and their intermediates was described in detail， and compared with the commonly used measurement methods of physical property indicators. Finally， the application prospects of texture analyzer and its research contents to be improved were reviewed， so as to facilitate the use of texture analyzer by pharmaceutical researchers to promote the development of related fields of pharmaceutics， and to provide new ideas and methods for the research and development of pharmaceutical preparations.
ABSTRACT
OBJECTIVE：To optimi ze the ratio of four comp onents of Compound renshen jianti formulation （Panax ginseng ， Dioscorea oppositifolia ，Lycium barbarum fruit，Alpinia oxyphylla ），and to investigate its anti-fatigue activity and acute toxicity. METHODS：The water extract of Compound renshen jianti formulation was prepared by water extraction ，concentration and decompression drying. By single factor tests ，using weight-bearing swimming time as index ，the effects of four factors were investigated，such as the amount of P. ginseng ，D. oppositifolia ，L. barbarum fruit，A. oxyphylla . On the basis of single factor tests，using comprehensive score of weight-bearing swimming time ，serum urea nitrogen content ，liver glycogen content and AUC of blood lactate after exercise as index ，the formulation was optimized by Box-Behnken response surface method. The mice was divided into blank control group （water），positive control group （Renshen hongjingtian capsules ，0.135 g/kg）and compound low-dose，medium-dose and high-dose groups [the optimal ratio of Compound renshen jianti formulation extract （called“optimal compound formulation ”for short ）4.08，8.16，12.24 g/kg，by crude drug] ，intragastric administration of drug or distilled water 20 mL/kg，once a day ，for consecutive 30 d. The weight-bearing swimming time ，the contents of serum urea nitrogen ，liver glycogen and blood lactate AUC after exercise were used to optimize its anti-fatigue activity of optimal compound formulation. The comprehensive score was calculated based on the measured data of mice in the compound formulation middle-dose group ， and the difference between it and the theoretical prediction value was compared. The mice were given optimal compound formulation intragastrically （total dose 16.00 g/kg， by extract）. The general state ， body mass change ， toxic characteristics and death of mice were observed and recorded for 14 days. Median lethal dose （LD50）and maximum tolerated dose （MTD）were measured. RESULTS ：The optimal formulation ratio of Compound renshen jianti formulation included that P. ginseng 1.5 g，D. oppositifolia 10 g，L. barbarum fruit 10 g，A. oxyphylla 3 g. Results of anti-fatigue activity validation test showed that the optimal compound formulation could significantly prolonged weight-bearing swimming time ，reduced serum content of urea nitrogen ，blood lactate content and its AUC （except for low-dose group ），while significantly increased the content of liver glycogen （P＜0.05 or P＜0.01）. Average comprehensive score of medium-dose group was 96.95，which was only 0.06％ different from the theoretical prediction value of 97.01. The results of acute toxicity test showed that there was no death in mice. The oral MTD of the optimal compound formulation was more than 15 g/kg，which was non-toxic. CONCLUSIONS ：The optimal Compound renshen jianti formulation has effective anti-fatigue activity of mice ，and has no significant toxic effect.
ABSTRACT
Objective To screen prescriptions for moxifloxacin hydrochloride tablets and optimize its preparation technology. Methods Taking the angle of repose,tap density,hardness,friability,disintegration time,tablet weight difference,and dissolution rate as indexes,the amount of each component,binder solvent,amount of binder,size of the mesh for granulation and particle drying process were investigated. The optimal formulation and process were determined based on the above results. Results With water as the binder solvent,binder volume of 6 ml,screen mesh number of 26 mesh,and finally drying 1 h at 50℃,the indicators of the tablet prepared met the quality requirements of tablet in the second part of the Pharmacopoeia of People′s Republic of China the 2015 ver-sion. And the dissolution profile was in good agreement with the commercially available preparation. Conclusion The quality of moxi-floxacin hydrochloride tablets prepared by the optimal formulation and process in this study is in accordance with the standard. The pre-scription and process can be used for the preparation of generic drugs of moxifloxacin hydrochloride tablets.
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OBJECTIVE:To study the formulation of Xiqingguo buccal tablet,optimize the proportion and quantity of main materials. METHODS:Using appearance,hardness,dissolution and taste as investigation indexes,orthogonal design was adopted to optimize the proportion and quantity of main thinner(lactose,mannitol),wetting agent(ethanol),lubricant(magnesium stea-rate),flavoring agent(aspartame),and critical relative humidity was detected. RESULTS:By wet granulation,the optimal formu-lation were as follows as the ratio of lactose and mannitol was 1:3,ethanol volume fraction was 60%,the dosage of menthol, magnesium stearate,aspartame and orange essence was 0.4%,0.9%,2.0%,0.4%;it was proven that the total score of 3 batches of samples were 2.67,2.67,2.70 (RSD=0.65%,n=3),respectively. The critical relative humidity of granule was 60%. CON-CLUSIONS:The Xiqingguo buccal tablet prepared by optimal prescription meets the requirements.
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OBJECTIVE:To optimize the formulation of Budesonide sustained-release tablet. METHODS:Using the cumula-tive releases in 2,4,8 h as investigation indexes,central composite design-response surface method was used to optimize the amount of hydroxypropylcellulose L(HPC-L),amount of soybean phosphatides,and filler(fixed total 200 mg)lactose- micro-crystalline cellulose mass ratio in the formulation of Budesonide sustained-release tablet,and the verification test was conducted. The release behaviors of prepared sustained-release tablet and original preparation in pH 7.2,7.0,6.8 phosphate buffer were com-pared. RESULTS:The optimal formulation was as follow as budesonide of 9 mg,HPC-L of 46.49 mg,soybean phosphatides of 9.23 mg,filler lactose-microcrystalline cellulose mass ratio of 1:2.9;the cumulative releases in 2,4,8 h were 21.9%,50.1%, 99.5%,the relative errors with predicted values (22.0%,50.0%,98.5%) were 0.45%,0.20%,1.02%(n=3),respectively. Compared with cumulative release of original preparation,the f2 was higher than 50. CONCLUSIONS:Budesonide sustained-re-lease tablet is successfully prepared,which shows similar release behavior to original preparations.
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Aim: To study the hydrofluoroalkane-driven(HFA-134a) salbutamol sulfate (SS) MDI formulation compositions and the respiratory tract absorption in rats. Methods: Solubility determination and orthogonal design were used to aid the screening of non-CFC SS MDI formulations. Rats were exposed to SS MDI via intubation inhalation. Fluorescent HPLC detection was developed to determine plasma SS concentration in rats given the selected SS MDI formulations. Analysis of the plasma drug level-time profiles was performed by the statistical moment approach. Results: Stable and homogeneous non-CFC SS MDI formulations were obtained. The developed HPLC method was validated and used to assay SS levels in the rats after inhalation of the MDI. AUC ratios of the SS/HFA-134a-driven MDI formulation to the reference SS MDI and CFC SS MDI formulation were 109. 86% and 135. 54%, respectively. Conclusion: It is proven that the absorption of the HFA-134a SS MDI formulation in rats is equivalent to the simulant formulation commercially available oversea and better than CFC formulation.