Analysis of Three Factors Affecting Solubility

Dissolution test is an important indicator for evaluating traditional Chinese medicine preparations, production processes, and bioavailability. The preparation, dosage form, excipients, and preparation process of solid oral preparations of traditional Chinese medicine are directly related to the dissolution of the drug, as they are made from powder or extract raw materials. By selecting appropriate excipients and preparations to improve the dissolution, release, and elution of drugs, the absorption of drugs in the body can be increased.

Factors, preparation and process affecting the solubility of traditional Chinese medicine preparations

1. There is a close relationship between dosage form and drug solubility

Researchers measured the solubility of Niuhuangjie tablets and Niuhuangjiedu tablets using baicalin, berberine, chlorogenic acid, and total anthraquinone as indicators. The results indicate that the dissolution rate of tablets is 2/3 slower than that of sugar coated tablets. Obviously, converting bezoar toxin tablets into bezoar detoxification tablets is beneficial for drug release. But not all tablets have lower solubility than tablets. For example, after being converted into tablets, the release rate of Yinqiao Jiedu and Huanglian Shangqing tablets decreased by 2/3. The release of Mao Dongqing root dried capsules within two minutes is equivalent to the release of sugar coated tablets within 30 minutes. After 50 minutes, the release amount of the capsule exceeded that of the sugar coated tablet by 5 times. The effect of T50 is twice as fast as that of Guanxin Suhe Wan, with significant clinical efficacy and better biological parameters than Guanxin Suhe Wan. Therefore, in vitro solubility determination can be used to select the ideal dosage form. When treating acute diseases, large dosage forms should be chosen to ensure rapid drug efficacy. When treating chronic diseases, small dosage forms can be chosen, and drugs can slowly take effect.

2. The preparation of prescription drugs and additives includes two parts

The release and dissolution of active ingredients in solid pharmaceutical preparations are related to the properties of the drug (solubility, crystal form, particle size, etc.) as well as the type and dosage of the material. In the traditional Chinese medicine Qinglan, flavonoids such as Pueraria lobata and Rutin are made into tablets with different excipients. As a result, different excipients have a significant impact on the solubility of different flavonoid drugs. Aluminum hydroxide, sodium carbonate, Pueraria lobata tablets, and Yunpian in the blue tablets all use aluminum oxide as an auxiliary material. The research conducted by Shanghai Institute of Traditional Chinese Medicine shows that the dissolution rate of Su Bing Drop Pills with added magnesium stearate is significantly lower than that of Su Bing Drop Pills without magnesium stearate.