Oral is the most commonly used route of administration. After oral administration, the drug particles are absorbed through the gastrointestinal mucosa, but before the gastrointestinal mucosa is absorbed, the drug particles need to be dissolved in the digestive juice of the gastrointestinal tract. In the pharmaceutical industry, about 90% of the active ingredients of drugs are contained in solid particles, and about one-third of these solid drug compounds are insoluble in water. Water-insoluble drugs cannot be effectively dissolved in the gastrointestinal juice, which limits their effects in the human body. Therefore, drugs need to have a certain degree of solubility and dissolution rate (called dissolution) in order to have better efficacy. And drug micronization is another technology that changes the structure and increases the specific surface area of the drug by reducing the particle size of the drug crystal, thereby improving the water solubility and bioavailability of the drug. Compared with before micronization, the particle size of the drug particles after micronization is obviously reduced, so that the dissolution rate is increased, the effective ingredients are more fully entered into the blood, and the drug effect is improved. At the same time, the mixing uniformity of the various ingredients in the suspension and solid preparations is also closely related to the particle size, and the micronized medicine is conducive to the uniform mixing of the ingredients.
Fig.1 Micronization of pharmaceutical ingredients
At present, the drug micronization technology commonly used in the pharmaceutical industry mainly includes mechanical grinding, recrystallization, freeze drying and spray drying. Roughly classified into two methods: (1) physical grinding of raw materials under dry or wet conditions; (2) solution-based deposition process. During the mechanical grinding process, the loss of medicine is serious. Long-term contact between the grinding medium and the medicine may also cause the pollution of the medicine. For heat-sensitive medicines, it will also cause the decomposition and loss of the active ingredients of the medicine. At present, the pharmaceutical industry needs to use a large amount of organic solvents. Today, with the increasingly stringent requirements for the discharge of toxic chemicals, the pharmaceutical industry still needs to face tremendous pressure on environmental protection.
CD Formulation provides customers with very professional technical guidance and product solutions for the development of pharmaceutical preparations. The currently developed drug micronization technology effectively improves the bioavailability of drugs. The current specific preparation methods of micronization are divided into the following contents:
CD Formulation has professional experience and technical personnel in the technical aspect of drug micronization. If you have an insoluble API, please contact us in time to learn how drug micronization can help solve your formulation challenges, and let us take your product from concept to commercialization.
If you have a requirement about our services, please contact us by phone or email, our colleagues will reply to you within three working days.