Oral solid preparations are the preferred dosage form in clinical use, including oral powders, granules, tablets, capsules and dripping pills. They have good physical and chemical stability, low production and manufacturing costs, and are more convenient to take and carry. Features. In the research and development of solid preparations, the formulation of dosage forms and the preparation process are the main links.
Active pharmaceutical ingredients and pharmaceutical excipients are composed together. The interaction between pharmaceutical excipients and active pharmaceutical ingredients is a double-edged sword. It can develop in both beneficial and harmful directions. Therefore, we need to pay attention to the formulation of the formulation.
The prescription composition of oral solid preparations:
(1) Main medicine: (API) active pharmaceutical ingredients
The biologically active ingredients in medicines such as tablets and capsules-active ingredients of medicines are the most important kind of medicines, and their properties must be safe. Solid preparations are also composed of active pharmaceutical ingredients and excipients, so excipients are an indispensable and important part of the development and production of solid preparations. The use of excipients in the development of solid drug formulations is beneficial to the formation of the formulation, improving the stability of the drug, adjusting the effect of the active ingredients or improving the physiological requirements, and smoothing the preparation process.
Medicilon provides R&D and production services for pharmaceutical preparations. According to the characteristics of the dosage form, combined with the physical and chemical properties and stability of the drug, the production conditions and equipment are considered, process research is carried out, the preparation process of laboratory samples is initially determined, and the corresponding Process control indicators.
(2) Excipients: no physiological activity, no reaction with the main drug, and non-toxic and harmless. mainly include:
1) Thinner (filler) and absorbent
Fillers are generally used for materials that have insufficient API content to compress tablets or fill capsules. It can not only make the size of the dosage form moderate, but also can impart suitable hardness to the preparation by providing viscosity. In addition, the diluent affects the friability, content uniformity, solubility, stability, and processability of the formulation through its own fluidity, compressibility and other properties.
2) Wetting agent and adhesive
Binders mainly provide cohesive auxiliary materials for the raw and auxiliary materials in oral solid preparations, which not only contribute to the formation and fluidity of particles during the manufacturing process, but also contribute to the integrity of the tablets when the particles are compressed.
3) Disintegrant
Disintegrants are excipients that can promote the rapid fragmentation of tablets into fine particles in the gastrointestinal fluid. The main function is to eliminate the binding force generated by the binder or high compression, so that the tablet can be completed in water. The disintegrants currently used in solid oral preparations are mainly three super disintegrants: sodium carboxymethyl starch (SSG), croscarmellose sodium (CCS) and crospovidone (PVPP)
4) Lubricant
Lubricant is an important part of solid preparations such as tablets and capsules. Its main function is to reduce the friction between materials, between materials and equipment, between products and equipment, improve the fluidity between materials, and ensure the consistency of tablet weight and filling volume. .
5) Coloring agent
Food coloring makes the tablet beautiful and easy to identify. The coloring agent should be light and beautiful, and dark spots are likely to appear.
6) Flavoring agent
According to needs, aromatics and sweeteners can be added, including aromatic oils, stevioside, aspartame sweeteners, etc., to improve patient compliance.
3. Preparation process of oral solid preparation
The basic process of the preparation of oral solid preparations is: medicine→crushing→sieving→mixing→granulation→tabletting.
(1) After the powder is sieved, if it is evenly mixed with other components, it can be directly divided into powders;
(2) If the uniformly mixed materials are granulated, dried, and then packed, granules can be obtained;
(3) If the prepared particles are compressed and formed, they can be prepared into tablets;
(4) If the mixed powder or granules are divided into capsules, they can be prepared into capsules.
For solid preparations, the degree of mixing, fluidity, and filling of materials are very important, because crushing, sieving, and mixing can ensure the uniformity of the drug content. The good fluidity and filling of solid materials can fully guarantee the accurate dosage of the product. Among them, the addition of glidant is one of the main measures to improve fluidity and filling.
After oral administration of the solid preparation, the drug is dissolved and then absorbed into the blood circulation through the gastrointestinal epithelial cell membrane to exert its therapeutic effect. For some poorly soluble drugs, the dissolution process of the drug will become the rate-limiting process of drug absorption. If the dissolution rate is small and the absorption is slow, the blood drug concentration is difficult to reach the therapeutically effective concentration. Therefore, in the development of new drug solid preparations, it is necessary to improve the solubility of the drug to increase the dissolution rate of the drug and quickly reach the effective concentration of the drug treatment.
