Study on shedding particles from Chuanping Sustained-release Tablets based on multi-marker components balanced release / 中草药

Objective: To study on the changes of shedding particles, drug loading and release of Chuanping Sustained-release Tablets (CST) which were made by the different sustained-release excipients in vitro, so as to elucidate the mechanism about balanced release of multi-marker components on Chinese materia medica compound sustained-release preparation. Methods: Using Chuanping Prescription (Ephedra Herba and Datura Flos) as model drug, improved Peach Gum and HPMC was used as sustained release materials, the release test combinied with underwater video observation were applied to shot external forms at different time point, and the laser particle sizer was applied to determinate particle size, and HPLC was applied to determine the accumulated release rate of the index components (ephedrine, pseudoephedrine, and scopolamine) to calculate the cumulative release curve slope K value, and to evaluate the balance release of the different components. Results: CST which were made by the improved peach gum and HPMC sustained-release excipient, which particles were dropped at 0.5 h after contacting the dissolution medium. At the same time, the particles were obviously shedding with the passage of time. In contrast, CST that was made by the improved peach gum, its balanced release of multi-marker components was better (K of ephedrine was 12.18, K of pseudoephedrine was 12.30, and K of scopolamine was 12.40), and particles dropped faster (it was significantly at 1 h), and particle size was bigger (D50 was 53.37—70.33 μm and D90 was 100.3—196.5 μm), and drug loading was more (ephedrine 30.63%, pseudoephedrine 32.97%, and scopolamine 31.67%), and release time of drug was longer (60—120 min). Conclusion: The shedding particles were important part of balance release of multi-marker components about CST which was made by the improved peach gum sustained-release excipient, and also was the embodiment of the drug release mode of “corrosion-dissolution”.

Changes of polysaccharide content, functional properties and in vitro release of peach gum before and after improvement / 中草药

Objective To analyze the difference of polysaccharides content, property characterization, and in vitro release between the original peach gum and improved peach gum, and to find the change rule, so as to provide the basis for its further application as the new delivery material. Methods The content of polysaccharides was measured by the phenol-sulfuric acid method combined with ultraviolet spectrophotometry. The pH value of liquid cement was measured by pH meter. The dynamic viscosity of liquid cement was measured by the Brookfield DV-Ⅱ Pro viscometer. The solubility and swelling ratio of rubber powder were measured by the weighing method. The moisture-absorption rate at different relative humidity of rubber powder was measured by the method of controlling humidity with the desiccator. With three index components (ephedrine, pseudoephedrine, and scopolamine) as the standards, HPLC and the release test were applied to determine the accumulated release rate of Chuanping adhesive tablets (CAT). Results Original peach gum: In the three producing areas of Xishui in Guizhou Province, Xinfeng in Jiangxi Province, and Suixian in Hubei Province, the content of polysaccharides respectively was 84.30%, 81.52%, and 77.84%. The pH value of 1% liquid cement was 5.63, 5.60, and 5.88. The dynamic viscosity of 1% liquid cement was 30.8, 28.5, and 25.9 mPa∙s. The solubility of rubber powder was 6.08%, 5.75%, and 5.12%. The swelling ratio of rubber powder was 34.22%, 29.66%, and 26.25%. The 12 h moisture-absorption rate of the improved peach gum polysaccharose at RH of 43% was 28.19%, 27.02%, and 26.44%; and at RH of 81% was 38.22%, 35.26%, and 34.64%. The 2 h cumulative release amount in vitro of methamphetamine, pseudoephedrine, and scopolamine of Chuanping adhesive tablets were 95.41%—98.84%, 96.05%—97.11%, and 96.35%—98.21%. Improved peach gum: In the three producing areas of Xishui, Xinfeng, and Suixian, the content of polysaccharides respectively was 96.92%, 94.76%, and 93.35%. The pH of 1% liquid cement was 7.10, 7.08, and 7.12. The dynamic viscosity of 1% liquid cement was 318.4, 289.6, and 266.4 mPa∙s. The solubility of rubber powder was 17.82, 16.73, and 16.38 g. The swelling ratio of rubber powder was 84.98%, 81.55%, and 79.82%. The 12 h moisture-absorption rate of the improved peach gum polysaccharose at RH of 43% was 41.22%, 39.93%, and 39.20%; and at RH of 81% was 60.88%, 58.48%, and 57.17%. The 12 h cumulative release amount in vitro of methamphetamine, pseudoephedrine, and scopolamine of CAT were 97.88%—98.36%, 97.59%—98.56%, and 97.72%—98.12%. Conclusion Compared with the original peach each gum, the content of polysaccharides, dynamic viscosity, solubility, swelling ratio, and moisture-absorption rate, and sustained release property of the improved peach gum were all improved remarkably, and the solution was also neutral. These results show that the improved peach gum can be further developed and applied as a new sustained release material.

Study on balanced release of Chuanping extract sustained-release tablets combined with different accessories / 中草药

Objective: To study the balanced release of complex components of Chuanping extract sustained-release tablets combined with different accessories. Methods: With methamphetamine, pseudoephedrine, and scopolamine as indexes, HPLC and the in vitro release test were applied to determining the accumulated release rate of the complex components in nine sustained-release Chuanping extract preparations (Q1-Q9), and to evaluating the influences of different accessories to the release behaviors of complex components in vitro. Results: The differences about dissolutions of four single modern materials in Chuanping extract sustained-release tablets Q1-Q3 were significant, and Q4 released fast. All of them were not balanced release. The differences about dissolutions of single improved Chinese materia medica (CMM) sustained-release accessories made Chuanping extract sustained-release tablets Q5 were significant, and Q6 was balanced release. The difference about dissolutions of complex improved CMM sustained release excipients made Chuanping extract sustained-release tablets Q9 was incomplete, the balanced release of Q8 was not well. The balanced-release of complex components of Q7 was well. Conclusion: Different accessories would affect the balanced release of sustained-released Chuanping extract tablet in vitro. The modern sustained-release accessories are hard to achieve the balanced release of complex components of CMM compound sustained-release preparations, but the improved traditional sustained-release accessories could be achieved well.

Correlation between dissolution in vitro and absorption in vivo of chuanping sustained release tablets / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the correlation between dissolution in vitro and absorption in vivo of Chuanping sustained release tablets.</p><p><b>METHOD</b>The ephedrine, pseudoephedrine were chosen as marker components, dissolution in vitro of Chuanping sustained release tablets in the different pH were tested by the rotating basket method and HPLC; urine drug levels were determined by HPLC and absorption fractions were calculated according to Wagner-Nelson's formula and deconvolution technique.</p><p><b>RESULT</b>The linear regressive equation between the absorption percentage in vivo F and accumulative release percentage in vitro of Chuanping sustained release tablets was established as F(ephedrine) = 1.572 5f-20. 729 (R2 = 0.974 5); F(pseudoephedrine) = 1.237f-0.147 6 (R2 = 0.959 5).</p><p><b>CONCLUSION</b>The results suggested that there was fine correlation between the absorption percentage in vivo and the accumulative release percentage in vitro of Chuanping sustained release tablets.</p>

Evaluation of balanced release of complex components of Chuanping sustained tablets based on fingerprint / 中国中药杂志

To combine fingerprint and drug release rate in vitro, in order to study in vitro release of complex components of Chuanping sustained tablets, compound traditional Chinese medicine preparation. A qualitative determination of the characteristic peaks of the compound preparations were conducted by the fingerprint. The results of the dissolution rate determination under different release conditions showed that the release of three index components (methamphetamine, pseudoephedrine and scopolamine) of Chuanping sustained tablets was less affected by gastrointestinal factors, with similarity factors being more than 80 with unknown component release curves of three major characteristic peaks in the fingerprint. The qualitative determination proved that multiple components of the compound traditional Chinese medicine preparation was dissolved in vitro at similar rates, realizing the balanced release of complex components of the compound traditional Chinese medicine preparation. This study layed a theoretical and experimental basis for quality evaluation for the compound traditional Chinese medicine preparation.