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1.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-1006277

ABSTRACT

ObjectiveTo prepare oral nanoemulsions encapsulating essential oil from Alpinia zerumbet fructus(EOFAZ) and to investigate its pro-absorption effect in vitro and distribution in vivo. MethodThe proteoglycan conjugate polysaccharides of vinegar-processed Bupleuri Radix-bovine serum albumin(VBCP-BSA) was prepared by Maillard reaction of VBCP and BSA. Taking VBCP-BSA as emulsifier, vitamin B12(VB12) as absorption enhancer, and medium chain triglycerides mixed with EOFAZ as oil phase, the nanoemulsions loaded with EOFAZ was prepared by high energy emulsification method. The particle size, particle size distribution, surface Zeta potential, EOFAZ content and appearance and morphology of the nanoemulsions were characterized, and fluorescein tracer method was used to investigate the absorption effect of fluorescein-labeled EOFAZ nanoemulsions in vitro and their distribution in vivo. ResultVBCP-BSA was formed by Maillard reaction for 48 h with high grafting rate. Using VBCP-BSA as emulsifier, the homogeneous pink nanoemulsions was prepared and denoted as EOFAZ@VBCP-BSA/VB12. The particle size of the nanoemulsions was less than 100 nm and the particle size distribution was uniform. The surface of the nanoemulsions was a weak negative charge, and the shape was spherical. The encapsulation rate of the nanoemulsions for EOFAZ was greater than 80%, which had a good absorption effect in vitro and could enhance liver accumulation after oral administration. ConclusionThe designed proteoglycan nanoemulsions can effectively load EOFAZ, promote oral absorption and enhance liver distribution, which can provide experimental basis for the development of oral EOFAZ liver protection preparations.

2.
Zhongguo Zhong Yao Za Zhi ; 47(2): 358-366, 2022 Jan.
Article in Chinese | MEDLINE | ID: mdl-35178977

ABSTRACT

Taste is an important factor affecting the medicinal properties of oral preparations and patient compliance with medication, and also an important evaluation index for oral preparation design and clinical application. How to characterize the taste objectively, accurately, simply, and efficiently is a bottleneck problem that restricts the taste design, development, and utilization of oral preparations. At present, the commonly used taste assessment methods for oral preparations are traditional human taste panel, electronic tongue, animal preference test, in vitro release study, and electrophysiological test. The traditional human taste panel is the first choice for taste evaluation, but it is limited by poor subjectivity and reproducibility. Therefore, despite some limitations, the other four taste assessment methods have been applied in the pharmaceutical industry as auxiliary methods. This study reviewed the detection principles, applicability, advantages, and disadvantages of the above methods to provide references for the taste correction research and taste assessment of oral preparations, improve patient compliance and the competitiveness of oral preparation products in the industry, and promote the development of oral preparation technologies.


Subject(s)
Pharmaceutical Preparations , Taste , Administration, Oral , Animals , Electronic Nose , Humans , Reproducibility of Results
3.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-927977

ABSTRACT

Taste is an important factor affecting the medicinal properties of oral preparations and patient compliance with medication, and also an important evaluation index for oral preparation design and clinical application. How to characterize the taste objectively, accurately, simply, and efficiently is a bottleneck problem that restricts the taste design, development, and utilization of oral preparations. At present, the commonly used taste assessment methods for oral preparations are traditional human taste panel, electronic tongue, animal preference test, in vitro release study, and electrophysiological test. The traditional human taste panel is the first choice for taste evaluation, but it is limited by poor subjectivity and reproducibility. Therefore, despite some limitations, the other four taste assessment methods have been applied in the pharmaceutical industry as auxiliary methods. This study reviewed the detection principles, applicability, advantages, and disadvantages of the above methods to provide references for the taste correction research and taste assessment of oral preparations, improve patient compliance and the competitiveness of oral preparation products in the industry, and promote the development of oral preparation technologies.


Subject(s)
Animals , Humans , Administration, Oral , Electronic Nose , Pharmaceutical Preparations , Reproducibility of Results , Taste
4.
Drug Dev Ind Pharm ; 47(8): 1318-1325, 2021 Aug.
Article in English | MEDLINE | ID: mdl-34605349

ABSTRACT

OBJECTIVE: The aim of this study was to develop a pediatric oral preparation for ibuprofen. SIGNIFICANCE: Ibuprofen is widely used for defervescence in children, but medication compliance is poor due to its bitter taste. Dry emulsions possess good stability and can be transported and stored in solid form; they can be dispersed into liquid emulsions with water and easily administered to children. METHODS: In this study, a dry emulsion excipient was prepared by spray drying: a mixture of orange peel and corn oils (3:7, w/w) was used as the oil phase and solvent for ibuprofen; gum arabic and gum tragacanth were chosen as emulsifiers; and maltodextrin was used as a solid carrier. RESULTS: The particle sizes of the liquid and reconstituted emulsions were 5.75 µm and 6.11 µm, respectively; the average particle size distribution of the dry emulsion powder was 8.13 µm; scanning electron microscopy showed that the dry emulsion powder was composed of evenly distributed smooth spheres. At a drug loading of 36.52 ± 1.15 mg/g, 90% of ibuprofen was released from the dry emulsion excipient within 30 min. Sensory evaluations using human volunteers, rats, and an electronic tongue demonstrated that the emulsion had a taste-masking effect on ibuprofen. It was further corroborated by in vivo studies using a rat model that highlighted a 1.76-fold increase in ibuprofen absorption when the drug was administered as an emulsion compared with granules. CONCLUSIONS: These results indicate that the dry emulsion for taste-masking is promising and valuable in the development of ibuprofen for pediatrics.


Subject(s)
Ibuprofen , Taste , Animals , Child , Emulsions/pharmacology , Excipients/pharmacology , Humans , Ibuprofen/pharmacology , Oils/pharmacology , Particle Size , Powders/pharmacology , Rats
5.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-802086

ABSTRACT

Objective: To explore drug utilizing regularity of traditional Chinese medicine(TCM) in treating and preventing asthenopia by analyzing the patent status of TCM in the field of asthenopia control for nearly 20 years. Method: Global patents about TCM in treating and preventing asthenopia were systematic searched in IncoPat platform.The application trend,legal status and categories of patents were analyzed.Meanwhile,the oral prescriptions and external prescriptions were performed correlation index analysis by IBM SPSS Modeler 18.0,respectively;the difference of compatibility rules between them was compared. Result: The number of global patents in treating and preventing asthenopia gradually increased,and the proportion of patents from China was more than 99%.The main patent applications were pharmaceutical composition,oral preparation,external eye patch and so on,but the ratio of licensed patents in total patents was low.In term of drug utilizing regularity,the oral prescriptions paid much attention to using TCM for nourishing the liver and kidney,while external prescriptions highlighted relieving sickness heat and detoxification. Conclusion: Patents of TCM in treating and preventing asthenopia has been kept increasing in recent years,but the authorization rate is low.Formulation based on TCM theory can be statistically summarized,which can be helpful for the development of anti-asthenopia products.

6.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-696439

ABSTRACT

The role and potential function of oral vancomycin in regulating intestinal microflora and prospect of alleviating function of vancomycin in primary sclerosing cholangitis were reviewed,based on domestic and abroad clinical researches and experiments.Through this review,it can provide new ideas for clinical treatment of primary sclerosing cholangitis and to fill vacancies in oral administration of vancomycin in domestic:oral vancomycin play a consi-derable role in the improvement of clinical indicators and clinical manifestations of the primary sclerosing cholangitis patients,affecting the immune response and the release of related cytokines.Based on this,it has the potential to play a role in alleviating the disease in children with primary sclerosing cholangitis.In addition,through the problems remain resolved in this review,we provides a new research direction for future clinical research.

7.
China Pharmacist ; (12): 1312-1314,1315, 2015.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-671160

ABSTRACT

To establish a method for the simultaneous determination of the active ingredients ( codeine phosphate, brompheniramine maleate, chlorpheniramine maleate, ephedrine hydrochloride and guaifenesin) in compound codeine phosphate oral preparations by capillary electrophoresis ( CE) . Methods:The method employed an uncoated capillary column ( eCAPTM ) from Beck-mann company (50 cm × 75 μm);the electrophoresis voltage was at 10 kV;20 mmol·L-1 phosphate buffer solution (pH 7. 5) was used;the UV measurement was at the wavelength of 214 nm. Results: The studied components had good linear ranges (r≥0. 995) within the range of the investigated concentrations. The recovery was no less than 96%. Conclusion:The presented method can be ap-plied in the content determination of active ingredients in compound codeine phosphate oral preparations from different enterprises. It is simple, efficient and universal, which facilitates the market supervision in a fast and valid manner.

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