Microscopic and dissolution characteristics of Tianma ultrafine powder

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Microscopic and dissolution characteristics of Tianma ultrafine powder
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Chen Changzhou, Sun Dongmei, Zhang Xiaojuan, Tu Yaosheng, Cui Jingchao (Guangdong Institute of Traditional Chinese Medicine, Guangzhou 510095, China)
Abstract: Objective ultrafine powder technology Gastrodiae ultrafine grinding, in order to improve the dissolution gastrodin.
Methods Ultrasonic extraction was carried out by micro-powder, and the content and dissolution of gastrodin were determined by high performance liquid chromatography.
Through a 400 mesh screen results Gastrodia micropowder T 50 is 9.2min, 100 ~ 120 mesh micropowder T 50 is 44.4min.
Conclusion: After ultrafine pulverization of Tianma, the dissolution of gastrodin of 400 mesh fine powder is obviously higher than that of 100~120 mesh, and the dissolution rate after powder granulation is still better than 100~120 mesh.
Key words: Gastrodia elata/chemistry; Gastrodin/Analysis; Chinese medicine ultrafine powder technology/instrument and equipment
CLC number: R284.1    Document identification code: A     Article ID:1003-9783 (2002 )04-0251-02
Ultra-fine powder technology is a multi-disciplinary modern comprehensive science and technology, which has been successfully applied in materials, chemicals, metallurgy, electronics, medicine and food industries. The ultra-fine powder technology refines the material and increases the specific surface area. For the drug, the dissolution and release of the solid drug are improved, thereby improving the bioavailability of the drug. Traditional Chinese medicine has been used as a powder since ancient times. It has similarities with ultra-fine powder technology, and it is necessary to smash the original medicine. In other words, the ultra-fine powder technology is to refine the traditional powder, which suggests that we can use the powder as the ultra-fine powder technology in the application of Chinese medicine, to better improve the bioavailability of the powder. According to this idea, we have carried out research on a series of traditional Chinese medicine varieties. The research report of Tianma ultrafine powder is as follows.
1 Materials and methods
1, 1 medicinal materials and reagents    Gastrodia medicine is provided by a pharmaceutical factory in Guangdong. The gastrodia elata powder is made into 100-120 mesh, 250-300 mesh, and 400 mesh powder, respectively. A pharmaceutical factory Tianma formula particles, batch number 010434. A company full Tianma capsule, batch number 2001101, go to the capsule shell, mix and use. The gastrodin standard is provided by the China National Institute for the Control of Pharmaceutical Sciences. Methanol, analytically pure.
1, 2 instruments Standard sieve set, Sanqing micro-powder, OLYMPMSBH microscope. High Performance Liquid Chromatograph Agilent 1100 Series.
1,3 Method (1) After being coarsely pulverized, the gastrodia elata is put into the micro-powder machine, crushed at -10~-15 °C for 15 min, and 100~120 mesh, 250~300 mesh are prepared with special sieves of different specifications. Three fine-grain samples of 400 mesh were observed microscopically to observe the microscopic characteristics of each fineness sample. (2) Then, three kinds of fineness powders were respectively made into three kinds of particles of 100-120 mesh, 250-300 mesh and 400 mesh, and the gastrodin content was 0.1%. Weigh accurately 2.5g of each of the three kinds of samples, placed in a 250ml conical flask and accurately add 25ml of methanol, placed in an ultrasonic washer, adjust the water temperature of 40~45°C, and use a 0.45μm microfiltration syringe for 5min respectively. Samples were taken at 15 min, 30 min, 45 min, 60 min, and the gastrodin content was determined according to the literature [1] . Calculate the cumulative dissolution rate of gastrodin, refer to the literature [1] Weibull function calculation method to find its linear equation, the slope is m, and calculate the gastrodin gas dissolution 50% (T 50 ) and dissolution of 63.2% (T d ) time. The dissolution parameters were based on the "NDST New Drug Statistics Program" software, and the q test was used to compare the two.
2 results
2.1 Ultrafine powder microscopic characteristics    See Table 1.
2.3 The comparison results of the dissolution of Tianma particles are shown in Table 3.
Table 1             Microscopic characteristics of three kinds of fineness powder of Gastrodia elata
Fineness              Powder uniform state             Cells and catheters                  Needle crystal state
100~120 mesh          Uneven size,             More complete                  Suffocation
40×40?m, 160 ×160?m                     
250~300 mesh         More uniform size,            Cell wall and catheter             Not in bundle
40 × 40?m, 80 × 80?m         Fragments scattered                    
Passing 400 mesh       The size is quite uniform,         Almost seeing intact cells and catheters,     Needle crystal broken
10~40?m                 Polysaccharide particles
2.2 Dissolution of ultrafine powder gastrodin    The results are shown in Table 2.
Table 2 Dissolution parameters of three kinds of fine gastrodia elata powder gastrodin (N=3)
Sample fineness m T 50 /min T d /min
100~120 mesh 0.645 44.4 78.5
250~300 mesh 0.640 22.6 39.9
Pass 400 mesh 0.972 9.2 13.4


2.3 The comparison results of the dissolution of Tianma particles are shown in Table 3.
table 3     Comparison of gastrodin release parameters of different samples (χ± s )
Sample fineness N/ batch m T d /min T 50 /min
100~120 mesh fine powder particles 5 0.549 ±0.22 63.84 ±22.95** 30.98 ±8.26**
400 mesh fine powder particles 5 0.702 ±0.11 10.66 ±1.60 6.33 ±1.42
Tianma Formula Granules 4 0.863 ±0.10 35.55 ±4.06* 23.15 ±2.40**
Whole Tianma Capsule 5 0.578 ±0.56 18.92 ±4.09 10.00 ±2.14
Note: *p<0.05, **p<0.01 compared to 400 mesh fine powder particles.
3 discussion
3, 1 research using ultra-fine pulverization technology to smash Tianma, with the increase of fineness, cell, catheter, needle crystal fragmentation degree increased, the fineness of 250~300 mesh, most cells have broken, to pass 400 mesh Almost all of the rupture, the polysaccharide particles are exposed, which is conducive to the dissolution and diffusion of the active ingredients. The dissolution test showed that the time required for gastrodin to dissolve 50% was shortened as the fineness was increased.
3, 2 Ultra-fine powder technology application of one of the big problems of Zui is that the powder is easy to adsorb and agglomerate each other, which brings a series of difficulties for the packaging, transportation and storage of drugs. In this study, the granulation method was used. The time required for the dissolution of 400 mesh granule gastrodin 50% was less than 100-200 mesh particles (p<0.05=, indicating that the granulation method was reasonable and feasible. The results of this study are available for Tianma formula granules. Manufacturer's reference.
Reference party:
[1] National Pharmacopoeia Commission, Pharmacopoeia of the People's Republic of China (2000 edition) [S], Beijing: Chemical Industry Press, 2000.453.
[2] Yu Xiangan, Cai Huaiyou, using the calculator to calculate the tablet dissolution parameter calculation procedure [J], Chinese pharmacy, 1995, 6 (4): 21.
 

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