Drug delivery technology increases drug availability

Drug delivery technology has developed considerably in recent years, such as: intestinal retention technology developed by ZuMax in the US near AvMax, and nanocrystalline drug delivery technology (DDT) from Elan, USA, which contains a kind of prevention of aggregation and further improvement of dissolution. Patented excipients) and a new peptide-like delivery agent being developed by Emé„„ishpere. These unique technologies have provided strong research and development for a variety of new drug delivery products, making up for the bioavailability defects of new drugs due to their chemical structure.

The research on drug delivery technology has gone through 30 years. The focus of early research is mainly on the improvement of oral delivery products. Among them, Zui is also typical of Zui. The successful example is to change the oral preparations administered three times a day to daily. 1 time controlled release product. The emergence of controlled release products not only revitalized many old products, but also extended their patent protection period.

The data show that the total transit time of the controlled release product in the intestine is about 24 hours, but most of the time is in the colon, not the small intestine. The results of drug absorption studies in healthy people showed that the relative bioavailability of the proximal small intestine was about 70%, followed by the small intestine (30%) and the small intestine (20%), while the ascending colon was only about 10%. Poor absorption in the distal area of ​​the intestine will affect the successful development of the product once a day. Therefore, before looking for a suitable delivery method for a certain drug, the capsule technology should be used to study the absorption of the person. Recent studies by zui have shown that more than 40% of new molecular drugs are poorly water-soluble. In order to solve the supply of drugs in the intestinal lumen, research on sustained-release materials has focused on the use of non-aqueous solvents and/or microemulsifications to improve compounds. In vivo solubility. The classic way is to reduce the particle size of the drug to increase the rate of dissolution.

With the advancement of combinatorial chemistry and high-throughput screening technology, coupled with the development of bioinformatics, a large number of new drug candidates have entered the all-round development stage. The next goal of drug delivery technology research is to develop newer controlled release products to enable A small number of these candidate drugs have biopharmaceutical properties suitable for oral delivery. Therefore, the development of current controlled release products is mainly focused on the update and upgrade of "controlled release technology for certain new drugs".

Nowadays, more and more biotech drugs are entering the development stage. These peptides and proteins are usually rapidly degraded in the intestinal tract (large molecular weight and low permeability). Although the new peptide-like transport agent can improve its bioavailability, this change is large. Studies of molecularly permeable cell-enhanced chemical enhancers and studies that specifically alter cell-to-cell tight binding to facilitate cell-side uptake have led to controversy over regulatory management as it is unclear about the potential adverse effects of altered intestinal barrier permeability. For biotech drugs, if the results of human intestinal absorption studies are not ideal, then in most cases it is necessary to consider whether to change the delivery route, such as by pulmonary, nasal or traditional parenteral administration.

In recent years, more and more new molecular entities (NMEs) are not only chemically complex, but more importantly, have low pharmacokinetic properties after oral administration. Highly complex intestinal wall processes and/or outflows are a major challenge for developing such new molecular entity drugs. It has been reported that studies of intestinal retention techniques have completed relevant experiments and are preparing for entry into clinical trials. This technology allows the drug to stay in the upper intestinal tract, thereby maintaining its local action on H. pylori to treat peptic ulcers, and this area is also the best intestinal site for bioavailability. At present, many large pharmaceutical companies in the world are very active in this field.

In addition, in order to maintain a 24-hour balanced blood drug level, drug delivery is well synchronized with the natural biological rhythm of the human body (ie, selective drug delivery therapy), and the development of advanced technology has made it a reality, such as the development of Alza Corporation of the United States. CoveraHS" has shown remarkable results for the treatment of hypertension.

Although there are not many new products registered with unique drug delivery technologies, the development prospects in this field will be broad with the deepening of the understanding of the basic disease processes affected by the natural rhythm of the human body.

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