Development of sustained-release microspheres for injection

Shijiazhuang Four Medicines Co., Ltd. was founded in 1948 and has undergone more than 70 years of historical changes. It has now developed into a large comprehensive pharmaceutical group, forming a new industrial development pattern with a relatively complete industrial chain, mainly consisting of chemical preparations, raw materials, traditional Chinese medicine preparations, and medical packaging materials. The enterprise has multiple high-level innovation platforms such as the National Enterprise Technology Center, and leads the annual production of 3 billion bottles (bags) of large-capacity injections. It is an important leading enterprise in injection production, research and development, and export in China, and has become one of the top 100 enterprises in the Chinese pharmaceutical industry and one of the outstanding export-oriented enterprises in the Chinese chemical pharmaceutical industry. In 2007, the company was listed in Hong Kong.
Project introduction: 
Microspheres are a typical innovative preparation, which refers to small spherical entities formed by drug dissolution or dispersion in a polymer material matrix. The particle size is relatively small, usually ranging from 1 to 500 μ Between m, it belongs to matrix type skeleton particles. Microspheres can not only protect drugs from damage, but also have special affinity with some cell tissues. They can be swallowed (swallowed, pinocytosis) by the reticuloendothelial system of organs and tissues or fused by Cell fusion, concentrated in the target area and gradually diffused to release drugs or degraded by enzymes in Lysosome to release drugs. Microspheres have the advantages of long-term efficacy, safety, targeting, and increased bioavailability, among which the long-term advantage is obvious, with a maximum duration of up to six months, which can greatly improve patient medication compliance.
The complexity and cost control of the production process of microsphere products, the quality control of microsphere products, and the stability of drugs are all technical barriers. The core technology has long been monopolized by drug manufacturers in developed countries, so the development of microsphere in China is relatively slow. At present, the microsphere products sold in the Chinese market include Octreotide, leuprorelin, triptorelin, risperidone, etc.
There are high barriers to microsphere research and industrialization. Currently, there are relatively few companies and varieties of microsphere formulations in China. With the advancement of microsphere technology research and development in China, companies such as Green Leaf Pharmaceutical, Lizhu, Qilu, and Hengrui have successively laid out and listed their products. However, overall, there are few companies with independent research and development capabilities, and they are still in the stage of oligopoly competition.
Intended countries: Germany and France 
plan to solve the main problem through the project: the
research and development cycle of microsphere formulations is relatively long. As the microspheres are long-acting preparations, each test lasts for 1-3 months, which takes a long time. At the same time, the linear amplification problem also leads to a small magnification, which can only be 3-5 times, slowing down the progress of Drug development to a certain extent. The main barrier to microsphere formulations lies in industrial production, where production equipment does not have universal equipment and needs to be customized and improved by oneself; The production end is affected by the complex process of drug prescription, which makes it difficult to industrialize linear amplification production and requires exploring appropriate parameters; In addition, in terms of microsphere quality control, it is also necessary to maintain the encapsulation rate and uniformity of microsphere particle size, and Aseptic technique throughout the process;
Technical indicators: Solve technical difficulties encountered in the preparation method, surface treatment, delivery technology, and production of microspheres;
Technical maturity: This type of technology product has been approved and preliminary pilot studies are underway.