Effective method for improving bioavailability of powder drugs

The principle and technical characteristics of supersonic airflow crushing and grading system. For some insoluble powdery drug materials, if the "micronized" treatment, the specific surface area is doubled, the activity is high, and the adsorption performance, surface charge and surface adhesion are all wonderfully changed. Undoubtedly, the improvement of the therapeutic time and the improvement of bioavailability are beneficial.

This paper expounds the application of modern ultrafine pulverization technology in the modernization of Chinese and Western medicine, veterinary medicine and pesticide production, which makes the reform of Chinese medicine type, the saving of Chinese medicine resources, and the possibility of Chinese medicine going global; the suspension rate of pesticide wettable powder is over 95%. It greatly improves the control effect of pesticides on diseases, insects, grasses and other harmful organisms, and at the same time reduces the residual surface pollution of pesticides in agricultural and sideline products and the environment, and improves the safety of pesticide use.

First, the question raised For powder drugs, no matter whether it is Western medicine, Chinese medicine or pesticides, veterinary drugs, in order to improve the bioavailability, the "micronized" treatment of drugs is a good solution; Chinese medicine modernization, the preferred process is also Superfinely crushed,

However, in the "micronization" process of powder medicine, you will definitely encounter such problems:

1. How the particle size of the drug is thinner;

2. How to avoid pollution during the crushing process;

3, how to avoid the smashing process caused by excessive temperature and change the chemical composition of the drug;

4. The drug can be accurately and timely separated and collected after crushing.

To this end, pharmaceutical manufacturers have taken many methods, from traditional rolling to mechanical ball milling, from dry crushing to water flying, all kinds of, it is difficult to solve the above problems in one time.

In view of the above situation, our company has been researching for many years, and has developed a new generation of TC series medicinal ultrafine pulverizing and grading system with high starting point and high level. The device combines supersonic nozzle technology, fluidized bed diversion technology, and grading technology. Crushing----grading----collection once completed. The pulverization fineness can reach 0.3 micrometers (> 10000 mesh) and can be arbitrarily adjusted between 0.3 and 40 (350 mesh) micrometers.

Second, the process principle of medicinal ultrafine pulverization and grading technology, the characteristics of medicinal ultrafine pulverization and classification technology is realized by fluidized bed supersonic airflow pulverizing classifier. She uses aerodynamics as a theory to supersonic nozzle technology. The fluidized bed diversion technology and the classification technology are integrated into one, forming a set of TC series superfine pulverization-classification system.

The supersonic airflow crushing and grading system usually consists of a gas source, a feeding system, a supersonic airflow nozzle, a crushing chamber, a classification chamber, a cyclone collection, and a bag collection. (see process schematic)

The pulverization fineness of the TC system can reach 0.3 micron (> 10000 mesh) and can be arbitrarily adjusted. The system has obtained the national patent (patent number 02263987X). From the example of our company successfully smashing nearly one thousand kinds of Chinese and Western medicine raw materials, the technical performance of this equipment has reached the domestic and foreign advanced level.

2.1 Principle of Airflow Crushing Purified and dried compressed air is introduced into nozzles at several opposite positions to form a supersonic flow into the crushing chamber. The material is sent from the hopper to the crushing chamber and accelerated by the supersonic airflow, which becomes a high-speed moving jet, which collides with each other at the intersection; because the high-speed multi-phase fluidized bed is formed in the crushing chamber, the crushing strength and efficiency are greatly improved, thereby achieving super Micro-grinding. The principle and technical characteristics of supersonic airflow crushing and grading system. For some insoluble powdery drug materials, if the "micronized" treatment, the specific surface area is doubled, the activity is high, and the adsorption performance, surface charge and surface adhesion are all wonderfully changed. Undoubtedly, the improvement of the therapeutic time and the improvement of bioavailability are beneficial.

This paper expounds the application of modern ultrafine pulverization technology in the modernization of Chinese and Western medicine, veterinary medicine and pesticide production, which makes the reform of Chinese medicine type, the saving of Chinese medicine resources, and the possibility of Chinese medicine going global; the suspension rate of pesticide wettable powder is over 95%. It greatly improves the control effect of pesticides on diseases, insects, grasses and other harmful organisms, and at the same time reduces the residual surface pollution of pesticides in agricultural and sideline products and the environment, and improves the safety of pesticide use.

First, the question raised For powder drugs, no matter whether it is Western medicine, Chinese medicine or pesticides, veterinary drugs, in order to improve the bioavailability, the "micronized" treatment of drugs is a good solution; Chinese medicine modernization, the preferred process is also Superfinely crushed,

However, in the "micronization" process of powder medicine, you will definitely encounter such problems:

1. How the particle size of the drug is thinner;

2. How to avoid pollution during the crushing process;

3, how to avoid the smashing process caused by excessive temperature and change the chemical composition of the drug;

4. The drug can be accurately and timely separated and collected after crushing.

To this end, pharmaceutical manufacturers have taken many methods, from traditional rolling to mechanical ball milling, from dry crushing to water flying, all kinds of, it is difficult to solve the above problems in one time.

In view of the above situation, our company has been researching for many years, and has developed a new generation of TC series medicinal ultrafine pulverizing and grading system with high starting point and high level. The device combines supersonic nozzle technology, fluidized bed diversion technology, and grading technology. Crushing----grading----collection once completed. The pulverization fineness can reach 0.3 micrometers (> 10000 mesh) and can be arbitrarily adjusted between 0.3 and 40 (350 mesh) micrometers.

Second, the process principle of medicinal ultrafine pulverization and grading technology, the characteristics of medicinal ultrafine pulverization and classification technology is realized by fluidized bed supersonic airflow pulverizing classifier. She uses aerodynamics as a theory to supersonic nozzle technology. The fluidized bed diversion technology and the classification technology are integrated into one, forming a set of TC series superfine pulverization-classification system.

The supersonic airflow crushing and grading system usually consists of a gas source, a feeding system, a supersonic airflow nozzle, a crushing chamber, a classification chamber, a cyclone collection, and a bag collection. (see process schematic)

The pulverization fineness of the TC system can reach 0.3 micron (> 10000 mesh) and can be arbitrarily adjusted. The system has obtained the national patent (patent number 02263987X). From the example of our company successfully smashing nearly one thousand kinds of Chinese and Western medicine raw materials, the technical performance of this equipment has reached the domestic and foreign advanced level.

2.1 Principle of Airflow Crushing Purified and dried compressed air is introduced into nozzles at several opposite positions to form a supersonic flow into the crushing chamber. The material is sent from the hopper to the crushing chamber and accelerated by the supersonic airflow, which becomes a high-speed moving jet, which collides with each other at the intersection; because the high-speed multi-phase fluidized bed is formed in the crushing chamber, the crushing strength and efficiency are greatly improved, thereby achieving super Micro-grinding.

The role and characteristics of ultrafine pulverization are:

1. Improve bioavailability: In the pharmacopoeia or general standard, the fine powder of the medicine directly used for medicine is 80 mesh (180 μm) or 100 mesh (150 μm). In the ideal cell disruption model, the 180μm particles composed of 10μm cells have a ratio of particle size to cell diameter n=18, and the cell breaking rate η is only 15.77%. If the powder reaches 1250 mesh (10μm) n≥1, η≤100% . Therefore, after taking the ultrafine powder of the traditional Chinese medicine, the active ingredient in the cell does not need to pass through the cell wall and the barrier established by several layers or dozens of cell membranes to be absorbed by the administration site, but directly in contact with the administration site; The ultrafine powder of traditional Chinese medicine has a large specific surface area, a large contact area with the administration site, and its adhesive property prolongs the time of the drug at the absorption site, thereby greatly increasing the absorption rate and absorption degree of the active ingredient, thereby achieving quick effect. Efficient, long-lasting therapeutic effect. In addition, since the ultrafine pulverization technology adopts supersonic airflow pulverization, freeze pulverization, etc., unlike the conventional pure mechanical pulverization method, local overheating does not occur during the pulverization process, and the pulverization speed is fast, and the pulverization speed is fast. To preserve the biologically active substances and various nutrients in traditional Chinese medicines. Therefore, the ultrafine powder of traditional Chinese medicine is of great significance for improving the efficacy of traditional Chinese medicine, reducing toxic side effects and reducing the dosage.

2. There is homogenization in the compound pulverization: the cell breaks the wall, the water and oil in the cell migrate out, so that the surface of the particle is semi-moist, and a stable particle group is formed between the particle and the particle, and the mixing ratio of each particle group is the same. The traditional Chinese medicine ingredient can achieve a uniform effect and can increase the absorption effect.

3. Increasing the industrial extraction rate of active ingredients can increase by more than 22.5%.

4, pulverization can be fully enclosed, the comminution rate is 100%, no loss, no dust pollution, because the material is stainless steel, the structure is simple, can meet the sanitary requirements of GMP corrosion resistance, easy to clean, and because of the low pulverization temperature, suitable for crushing Heat sensitive material.

5. Make full use of the production and circulation conditions before the original decoction pieces to save investment costs.

6, saving medicines, reducing costs, and benefiting consumers.

After obtaining the clinical effect, the dosage of the prescription can be changed. The micro-powder decoction can be decoctioned, and the blistering can reduce the dosage of the prescription, which can reduce the medical expenses and save the resources of the medicine, and benefit the country and the people.

We know that ultrafine pulverization technology is one of the advanced technologies for the modernization of traditional Chinese medicine. In recent years, we have used supersonic airflow pulverization technology to superfinely smash various types of Chinese herbal medicines for pharmaceutical companies, Chinese medicine universities, and Chinese medicine research institutes. (See Schedule). Relevant experts will also let them accumulate Chinese medicine prescriptions for many years. They conducted a comparative study on pharmacodynamics, biopharmaceutics, and pharmacokinetics of single and compound drugs, and found that the preparations prepared by the ultrafine powder technique have significantly higher pharmacological effects than those prepared by conventional pulverization techniques. Experts have found that general Chinese medicine: one gram of ultrafine powder is equivalent to the active ingredient of five grams of extract.

The Hunan Academy of Traditional Chinese Medicine has used the TC-10, TC-20B and TC-30 equipment developed by our company to develop the ultra-fine decoction pieces of four hundred flavors of Chinese medicine, which has been registered as “super micro-drinking tablets”. Beijing Keyifeng Biotechnology Development Co., Ltd. (three productions of Beijing Sanyin Factory) is processed by our company to export estradiol, estriol and diketone ultrafine powder. The crushing particle size is 95% less than 5um. The added value is greatly improved. Progesterone produced by Hangzhou Aisheng Pharmaceutical, Guilong Kechuanning produced by Shanxi Guilong Pharmaceutical, Shouwu Tianma produced by Hunan Guohua, Ejiao of Jiuzhitang, Wuji Baifeng of Jiangxi Huiren, Yujiang Pharmaceutical Factory In the summer, Xuzhou Pharmaceutical Factory's non-Lobert, Jilin Yatai, Amendment Pharmaceutical, Taitai Pharmaceutical |, Health Pharmaceutical, Jiangsu Provincial Hospital, etc., research institutes and pharmaceutical factories all went to our company to process products and Purchase TC series medicinal ultrafine crushing classifier produced by our company.

Shandong Xinde Pharmaceutical Co., Ltd. has used the TC series fluidized bed supersonic airflow crushing and classifying machine produced by our company to produce “intestinal music” and “ball elimination” micro-powder products, which have been put into the market and won the favor of the majority of farmers.

In summary, the development of new products and new dosage forms of traditional Chinese medicines with better curative effect and better variety will have far-reaching theoretical and practical significance. The State Science and Technology Commission and the State Administration of Traditional Chinese Medicine have listed it as one of the "21st Century Chinese Medicine Modernization Development Strategy".

4. Ultra-micro wettable powder is an effective method to improve the suspension rate. The ultra-fine powder technology is available. It can disperse and dissolve pesticides and surfactants from 150~200 mesh particle size (75μm or more) obtained from traditional crushing process. Increase to 5~10μm or less. Under the fineness condition, the suspensibility of the wettable powder reaches 95%, and the ultra-wet wettable powder is hardly precipitated in water, and becomes a viscous and flowable uniform suspension. The advantages are as follows:

1. The particle size of the ultrafine powder is extremely small (5~10μm or less), the uniformity and dispersibility are good, and the contact area of ​​the drug is large. Therefore, the sterilization, insecticidal and herbicidal effects are greatly increased. If the pesticide is a plant growth regulator, the time and extent of plant uptake is greatly increased and the amount of pesticide used can be reduced.

2, ultra-fine powder has a large specific surface area, strong adsorption capacity, and is resistant to rain, thus maintaining the long-term effect of pesticides.

3. Ultra-fine powder has strong surface activity, and the rate of decomposition in agricultural and sideline products and environment is accelerated, so the pesticide residue is reduced and pollution is reduced.

In summary, the pesticide wettable powder adopts the supersonic airflow pulverization method, which further strengthens the effect of high efficiency, long-lasting effect, low toxicity and safety of the pesticide.

In recent years, some of the pesticide products that have been entrusted to our company to process and export such as: thiophanate-methyl, carbendazim, glucosinolate, bactericidal, chlorophyll, imidacloprid and other wettable powders are required to be below 5 microns. This fully illustrates this problem.

We use supersonic jet milling technology to superfinely crush various types of pesticides for pesticide factories and pesticide research institutes. They conducted a comparative study on pharmacodynamics, biopharmaceutics, and pharmacokinetics of this part of the pesticide, and found that the pharmacological action intensity of the pesticide prepared by the ultrafine powder technology was significantly higher than that prepared by the conventional pulverization technique.

In summary, new ultra-fine powder products and new dosage forms with better development effects and higher formulation technical standards will have far-reaching theoretical and practical significance. The National Development Planning Commission and the State Science and Technology Commission have included this in the Agriculture section of the “Guidelines for Priority Development of High-tech Industrialization Key Areas”.

V. Conclusions From the example of our company successfully smashing nearly one thousand kinds of Chinese and Western medicine raw materials, and comparing with the same type of equipment in Japan and Germany, the system has obtained national patent (patent number 02263987X). The technical performance of the equipment has reached the domestic and foreign advanced level.

Practice has stated and will continue to confirm that this ultra-fine pulverization technology is used in the fields of Chinese and Western medicine, pesticides and veterinary drugs, and it is an ideal method in the pharmaceutical pulverization process. As one of the ways to reform the medicinal type, it enriches the traditional processing. The content can bring new vitality to the production and application of traditional Chinese medicine, and become a new growth point of the Chinese medicine industry.

Our company welcomes you to test and process, in order to increase our understanding of us, so that the technology that our company has been studying for many years can help the major factories to rise steadily in the pharmaceutical industry.


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