ABSTRACT
The powder modification technology was used to improve the powder properties and microstructure of Dioscoreae Rhizoma extract powder, thereby solving the problem of poor solubility of Dioscoreae Rhizoma formula granules. The influence of modifier dosage and grinding time on the solubility of Dioscoreae Rhizoma extract powder was investigated with the solubility as the evaluation index, and the optimal modification process was selected. The particle size, fluidity, specific surface area, and other powder properties of Dioscoreae Rhizoma extract powder before and after modification were compared. At the same time, the changes in the microstructure before and after modification was observed by scanning electron microscope, and the modification principle was explored by combining with multi-light scatterer. The results showed that after adding lactose for powder modification, the solubility of Dioscoreae Rhizoma extract powder was significantly improved. The volume of insoluble substance in the liquid of modified Dioscoreae Rhizoma extract powder obtained by the optimal modification process was reduced from 3.8 mL to 0 mL, and the particles obtained by dry granulation of the modified powder could be completely dissolved within 2 min after being exposed to water, without affecting the content of its indicator components adenosine and allantoin. After modification, the particle size of Dioscoreae Rhizoma extract powder decreased significantly, d_(0.9) decreased from(77.55±4.57) μm to(37.91±0.42) μm, the specific surface area and porosity increased, and the hydrophilicity improved. The main mechanism of improving the solubility of Dioscoreae Rhizoma formula granules was the destruction of the "coating membrane" structure on the surface of starch granules and the dispersion of water-soluble excipients. This study introduced powder modification technology to solve the solubility problem of Dioscoreae Rhizoma formula granules, which provided data support for the improvement of product quality and technical references for the improvement of solubility of other similar varieties.
Subject(s)
Powders , Solubility , Technology, Pharmaceutical , Technology , Plant Extracts , Particle SizeABSTRACT
Dioscoreae Rhizoma formula granules are made from decoction pieces by decocting， extracting， separating， concentrating， drying and granulating， which have the advantages of simple dispensing， convenient use and easy to take without decoction. However， because Dioscoreae Rhizoma is rich in starch and mucus components， its extract powder and formula granules are poorly soluble and difficult to dissolve or disperse completely within 5 min， and the insoluble material is difficult to dissolve completely even after 24 h in water， which affects the quality evaluation of the formula granules and medication psychology of patients. Therefore， by studying the dissolution process and mechanism of Dioscoreae Rhizoma extract and its formula granules， it was found that the special chemical composition of Dioscoreae Rhizoma， the denaturation of starch and its compounding with protein and other substances during the high temperature extraction process， and the contraction of coating membrane during the spray drying process were combined to form the special microstructure of coating membrane covering starch granules， and it is the root cause of poor solubility of Dioscoreae Rhizoma formula granules. Based on the research on the structure， property and function of the powder， this paper proposed a technical strategy to improve the solubility of Dioscoreae Rhizoma formula granules by powder modification process， and experimentally demonstrated that the modified Dioscoreae Rhizoma formula granules could completely dissolve within 2 min， which solved the technical problem and could provide reference for the improvement of solubility of other similar varieties， and promote the high-quality development of traditional Chinese medicine formula granule industry.
ABSTRACT
After more than 100 years of development， spray drying technology has become more mature and widely used， and it is of great importance in the field of traditional Chinese medicine （TCM）. TCM powders prepared by spray drying is the raw material of dispensing granules， and the powder properties have an important influence on subsequent molding process and product quality. As a new form of TCM， dispensing granules have been included in the management category of TCM decoction pieces， indicating a broader application market， and a consensus has also been reached on the importance of TCM powder research. Based on this， the author summarized the application progress of spray drying in the study of TCM powders， including the factors affecting spray drying process， such as liquid properties， process parameters and equipment factors， as well as the application of computational fluid dynamics （CFD） and thermodynamic model in spray drying process simulation. Moreover， some commonly used pharmaceutical excipients for the modification of TCM powders were also introduced such as maltodextrin， microcrystalline cellulose and povidone. In addition， spray drying technology can also be used as a preparation technology for new drug delivery systems such as microcapsules and solid dispersions. Through the summary of this paper， the author suggests that the future research direction of spray drying of TCM can be carried out from the aspects of application rule of the coprocessing auxiliary materials based on the "unification of medicines and excipients"， the "structure-property" relationship of spray-dried powders and the application of computer simulation and design， so as to further enrich the application of spray drying in the field of TCM powders.
ABSTRACT
Traditional Chinese medicine （TCM） effervescent tablets have the characteristics of rapid disintegration， good taste， and convenient taking， but there are some technical difficulties in the preparation and storage process， which are mainly reflected in the sticking， easy moisture absorption， poor compressibility， and poor stability. The basic physical properties of TCM powder （extract powder， raw powder） are the main cause of these technical problems， and also the key to control the quality of TCM effervescent tablets. Powder modification technology has shown good effects in solving the above problems. The author intended to review the research in the above aspects in recent years， and proposed the following strategies for applying powder modification technology to solve the problems in the production process of TCM effervescent tablets from the three aspects of raw materials， excipients and preparation intermediates：①The application of co-processing technology to the treatment of raw materials and auxiliary materials can solve the problems of sticking， poor compressibility， delayed disintegration， and poor stability. ②Using surface coating technology to treat raw materials and preparation intermediates can improve poor fluidity， poor compressibility and delayed disintegration. ③The hygroscopicity of the preparation can be reduced by using microencapsulation technology to treat the raw material. ④The inclusion technology can improve the clarity and stability of the preparation.
ABSTRACT
Particle design, based on the concept of "quality by design", combines the elements of microbiology, formulation science, heat and mass transfer, solid state physics, powder science, and nanotechnology. It is widely used to develop particles with excellent functional properties. Without affecting the active ingredients, the modification technology of traditional Chinese medicine (TCM) powder based on particle design theory, could improve the flowability, tabletability, disintegration and dissolution behavior, hygroscopicity, wettability, and other functional properties at the physical structure level. This greatly promotes the development of solid preparations of TCM. The present review aims to summarize and discuss the research progress of powder modification of TCM from the perspective of the theory of particle design, powder modification technology, equipment used for powder modification, application in TCM and modification mechanism mainly based on researches published in recent ten years. This review could provide ideas and theory basis for the development of particle design.
ABSTRACT
Based on the defects in powder properties of the contents of Ziyin Yiwei Capsules, this study screened out the main medicinal slice powders causing the poor powdery properties, and introduced the powder modification process to improve the powdery properties of these slice powders, the pharmaceutical properties of the capsule contents, and the content uniformity of Ziyin Yiwei Capsules, so as to provide a demonstration for the application of powder modification technology to the preparation of Chinese medicinal solid preparations. Through the investigation on the powder properties of the contents of Ziyin Yiwei Capsules, it was clarified that the pulverized particle size of the capsule contents had a good correlation with the pulverization time. According to the measurement results of the powder fluidity and wettability, the quality defects of the capsule contents were caused by the fine powders of Taraxaci Herba and Lungwortlike Herba. "Core-shell" composite particles were prepared from medicinal excipients magnesium stearate and fine powders of Taraxaci Herba and Lungwortlike Herba slices after ultra-fine pulverization to improve the powder properties of the problematic fine powders. Powder characterization data including fluidity and wettability were measured, followed by scanning electron microscopy(SEM) and infrared ray(IR) detection. It was determined that the optimal dosage of magnesium stearate was 2%, and the compositing time was 3 min. The composite particles were then used as content components of the Ziyin Yiwei Capsules. The powder characteristics between the original capsule and the modified composite capsule including the particle size, fluidity, wettability, uniformity of bulk density, and uniformity of chromatism as well as the content uniformity and in vitro dissolution were compared. The results showed that the powder characteristics and content uniformity of the prepared composite capsule were significantly improved, while the material basis of the preparation was not changed before and after modification. The preparation process was proved to be stable and feasible. The powder modification technology solved the pharmaceutical defects that were easy to appear in the preparation of traditional capsules, which has provided experimental evidence for the use of powder modification technology for improving the quality of Chinese medicinal solid preparations and promoting the secondary development and upgrading of traditional Chinese medicinal dosage forms such as capsules.
Subject(s)
Capsules , Excipients , Particle Size , Powders , WettabilityABSTRACT
Polyethylene glycol (PEG) surface film-forming method was used to prepare hydrophilic Indigo Naturalis decoction pieces with stable effect.The preparation process of modified Indigo Naturalis was optimized and its microscopic properties,hydrophilicity,antipyretic efficacy,and safety were systematically evaluated.With equilibrium contact angle as assessment index,the influence of modifier type,modifier dosage,dispersant dosage,and co-grinding time on water solubility of Indigo Naturalis was investigated by single factor test.The results showed that the optimal preparation process was as follows.The 6%PEG6000 is dissolved in 10%anhydrous ethanol solution by sonification and then the mixture is ground with Indigo Naturalis for 2 min.The resultant product is dried on a square tray in an oven at 60℃to remove ethanol and thereby the PEG-modified hydrophilic Indigo Naturalis decoction pieces are yielded.The morphological observation under scanning electron microscope (SEM) indicated that the modified Indigo Naturalis had smoother surface than Indigo Naturalis,and energy spectrometer measurement showed that the nitrogen (N),calcium(Ca),oxygen (O),and silicon (Si) on the surface of modified Indigo Naturalis powder were less than those of Indigo Naturalis powder.Modified Indigo Naturalis had the equilibrium contact angle 18.96°smaller,polar component 22.222 m J·m~(-2)more,and nonpolar component 7.277 m J·m~(-2)smaller than the Indigo Naturalis powder.Multiple light scattering technique was employed to evaluate the dispersion in water and the result demonstrated that the transmittance of Indigo Naturalis and modified Indigo Naturalis was about85%and 75%,respectively,suggesting the higher dispersity of modified Indigo Naturalis.The suspension rate of modified Indigo Naturalis in water was determined by reflux treatment.The result showed that 57%of Indigo Naturalis was not wetted after refluxing for1 h,while the modified Indigo Naturalis was all wetted and dispersed into water.The dissolution of indigo and indirubin of modified Indigo Naturalis increased and the process was more stable.Then,rats were randomized into the blank group,model group,acetaminophen group,Indigo Naturalis group,and hydrophilic Indigo Naturalis group.The temperature changes of rats were observed after administration and the concentration of IL-1βand TNF-αin serum and IL-1βand PGE_2in hypothalamus was measured.The results indicated that the temperature of Indigo Naturalis group and hydrophilic Indigo Naturalis group dropped and the IL-1βlevel of the hydrophilic Indigo Naturalis group decreased (P<0.05) as compared with those in the model group.Thus,both Indigo Naturalis and hydrophilic Indigo Naturalis had antipyretic effect,particularly the hydrophilic Indigo Naturalis.The acute toxicity test of hydrophilic Indigo Naturalis verified that it had no toxicity to rats.In this study,the hydrophilic Indigo Naturalis decoction pieces were prepared with the PEG surface film-forming method,and the antipyretic efficacy and safety were evaluated,which expanded the technological means of powder modification for Chinese medicine and provided a method for clinical use of Chinese medicine.
Subject(s)
Animals , Rats , Drugs, Chinese Herbal , Hydrophobic and Hydrophilic Interactions , Indigo Carmine , Indigofera , Polyethylene GlycolsABSTRACT
Excellent taste is of great significance to ensure the clinical efficacy of traditional Chinese medicine. Aiming at the deficiency of traditional Chinese medicine powder preparation and the demand of children and elderly people with insufficient swallowing function, a novel dosage form called Chinese medicine oral instant powders was proposed. The introduction of this concept was inspired by the characteristics of ancient Jujube Instant Beverage, Longjiao Powders from Japan and freeze-dried tablets. It was also based on the understanding of the structure-property-function of traditional Chinese medicine powder, and integrated powder modification technology, taste masking technology, and the pretreatment technology of raw materials. In this manuscript, the concept, basic characteristics, composition of raw materials and accessories, design principle, process route, core equipment, quality evaluation methods and technical advantages of Chinese medicine oral instant powders were introduced in detail. It is hoped that the development of Chinese medicine oral instant powders will help to meet the needs of special population. Meanwhile, it will provide new ideas and technologies for the innovation of powder decoctions, hospital preparations and Chinese patent medicine powders in new era.
ABSTRACT
Objective: To explore the key factors affecting the low wettability of Indigo Naturalis by using “knockout” method combined with surface element analysis, so as to provide scientific basis for regulating and changing the wettability of Indigo Naturalis. Methods: Using N,N-dimethylformamide as solvent, six Indigo Naturalis powders were prepared by ultrasonic extraction for 0-5 times, 30 min for each time, filtration and drying process. The contents of indigo and indirubin in six kinds of Indigo Naturalis were determined by HPLC. The contact angle, surface free energy and its components, particle size, surface morphology, surface element analysis and infrared spectroscopy were determined. The relationship between the content of organic matter and wettability of Indigo Naturalis was discussed by correlation analysis. Results: With the increase of extraction times, the content of indigo decreased from 3.320% to 0.112%, the content of indirubin decreased from 0.120% to 0.006%, the contact angle in pure water decreased from 53.56 degrees to 34.84 degrees, the polar component of surface free energy increased from 24.880 to 38.701 mJ/m2, the non-polar component changed little, and the total surface free energy increased from 46.523 to 62.240 mJ/m2. Scanning electron microscopy (SEM) showed that the particulate matter on the surface of Indigo Naturalis was gradually disappeared, and the surface became smooth; Mapping scanning by energy spectrometer showed that N element was gradually decreased, Ca and Si element were increased slightly; Particle size distribution and infrared spectrum changed little; Correlation analysis showed that the content of indigo, indigo and indirubin was positively correlated with the contact angle, and the higher the content, the worse the wettability. Conclusion: The contact angle, polar component of surface free energy and total surface free energy of Indigo Natural was significantly increased after knockout, and the wettability was increased. Organic substances adhering to the surface of Indigo Naturalis were the key factors leading to its low wettability. To improve the hydrophilicity of Indigo Naturalis by powder surface modification technology, it is necessary to focus on organic substances.
ABSTRACT
Objective: To discuss the interaction between modifier and Indigo Naturalis by selecting the modifier that enhancing the superficial hydrophilicity of I. naturalis, then the best powder modification technique was selected to prepare the hydrophilic decoction pieces of I. naturalis, which can suit for decoction. Methods: In this paper, the contact angle was used to select the modifier, thermal stability was studied by different drying temperatures; Mechanism and thermal stability were studied according to the microstructure of alcohols, I. naturalis, and indirrubin preliminarily. Best technique was chosen by single factor experiment and uniform design. Results: Alcohols could enhance the superficial hydrophilicity of I. naturalis comparing to the normal one, the acts of -OH and -CH3 were different, and generally, the modifying effect of longer carbochain and polyhydroxy-alcohol was better. The best modifier was ethanol, the optimum modifying technique was 19% ethanol and grinding for 23 min. Conclusion: Above all, alcohols can enhance the superficial hydrophilicity of I. naturalis, the use of ethanol as modifier and the modifying process are reliable and suitable, and hydrophilic decoction pieces of I. naturalis can be prepared successfully.
ABSTRACT
Objective: The purpose of this paper is to verify the key role of water absorption in the process of disintegration of Chinese materia medica (CMM) dispersible tablets, so as to provide the solution idea for slow disintegration of CMM dispersible tablets. Methods: In this paper, the influence of water absorption of raw materials and auxiliary materials on disintegration process was verified using oily Jianghuang Qingzhi Tablets (JQT) as research object. The water absorption and disintegrating process of different drugs, JQT with different materials, and modified dispersible tablet were determined. Results: The water absorption of JQT was lower than that of lactose tablets, and the disintegrating process was slower. The water absorption of different materials prescription of JQT was: CMS-Na-PVPP (1∶1) > PVPP > CMS-Na, and disintegrating process is the same as the former order. The water absorption of JQT after modification enhanced, and disintegration time was significantly shortened. It indicated that the water absorption of raw materials and excipients was stronger, the disintegration was faster. Conclusion: The study proves that water absorption is a key role in the disintegration of CMM dispersible tablets. And co-grinding of silica powder and raw materials is important technology to solve the problem of slow disintegration of CMM dispersible tablets.
ABSTRACT
Powder is the basis of solid preparation in Chinese materia medica (CMM), its properties have a great effect on the following preparation technology and its quality evaluation. Exploring the method for the powder modification technology is the key issues in pharmaceutics, due to the complicated and unusual physicochemical properties of CMM powder. Nearly ten years, tough and fruitful work has been carried out in this field. On the basis of other experts' achievements and their work experience, this paper reviews the modification technology for CMM powder initially, so as to promote the development of powder modification technology for CMM.