Injection research and development progress scan old preparation "old appearance" for "new face"

Althoughinjection is not a new formulation, there have been some important research progress in the variety and packaging type in recent yearsSuch as in the variety has appeared in the lipid injection, therapeutic mono-anti-injection, long-acting biodegradable micro-ball injection, nanoparticle injection, storage-type controlled release injection, gene therapy drug injection, gel type injection, etc., while in the injection device and packaging, there have been single-dose / multi-dose needle-free injections, powder-liquid syringes, subcutaneous injections, etcMicrosphere injectioncombined the drug in the microsphere carrier through subcutaneous or muscle administration, can make the drug release slowly, change its internal transport process, extend the action time in the body (up to 1 to 3 months), greatly reduce the number of medications, significantly improve the patient's compliance with the drugCurrently used in the preparation of slow-release microspheres of skeleton materials are mainly polylactic acid-
polyhydroxyacetic acid (PLGA) and polylactic acid (PLA) - is approved by the United States FDA can be used in the human biodegradability materials, which in turn is more commonly used in PLGAIn addition to good biocompatibility, non-immune response, high safety, but also more rare is by changing the proportion of the two monomers and polymerization conditions to adjust the rate of polymer degradation in the bodyMicrosphere injections of protein and polypeptide drugs should be selected for small daily doses due to the limited dose of microsphere injectionProteins and polypeptides are generally in small doses and require long-term useMicrosphere release mode and the clinical needs of the drug should be basically consistent, microspheres in the drug encapsulation rate is high, the sudden release effect when the release of drugs to be small, the release mode to be stable, the release time to meet the requirementsIn addition, there are many factors affecting microsphere release, including the type and proportion of the skeleton material, the preparation process, microsphere morphology, structure, particle size and distribution, the encapsulation rate and load of microsphere drugs, the state of microsphere drugs and the interaction between carriers and so onGenerally used to compound milk-
in the drying method, low-temperature spray solvent extraction method and other preparation microspheresThere are a number of related products on the market, and many more products (including microspheres of macromolecules and small molecule drugs) are being developed or approvedMicrosphere injections of the vaccine have been paid more and more attention because of the advantages of good biocompatibility and easy regulation of the rate of releaseAt present, the World Health Organization (WHO) led the research team has submitted tetanus totoxin microsphere injection formula and animal experiment resultsThe long-acting formulation consists of two microspheres, one with a smaller particle size and a high content, a ratio of 50 50 in the PLGA, a larger particle size, a lower content, a ratio of 75 25 in the two monomers in the PLGA; When the microsphere preparation is administered, higher levels of antibody levels can be produced in mice than the solution agentLilipid injectionsliposomes have been paid attention to because of their good biocompatibilityAfter more than 20 years of research, researchers have overcome the quality of lipid materials, large-scale production preparation process problems, encapsulation and stability problemsFollowing the first productthe sexmycin lipidbody listed abroad, there are amycin, erythromycin and other approved for the market, nitric acid proconaziagliolipid gel is also in EuropeSo far, the FDA registered lipid products are cisplatin, interleukin-
2, insulin-like growth factor, prostaglandin E1, Changchun new alkali and so onDomestic in the State FoodDrug
administration registered with hydroxyl hi-tree alkali lipids, ribavirin lipids and nitric acid isazole lipids registeredWith the improvement of carrier materials and surface modification of lipids, a number of types of lipid regime agents have appeared, such as immunolipids, long-cycle lipids, guided peptide coupled lipids, pH sensitive lipids and thermally sensitive lipids, magnetic lipids and so on Long-cycle lipids will be hydrophilic macromolecules such as polyethyl glycol (PEG) and its derivatives through the lipid anchor embedded on the lipid body film, in the lipid surface and form a hydrophilic layer, thereby reducing the mesh endothelial system identification and absorption, increase the circulation of lipids in the body, prolong the drug action time Such as amycin common preparations need to be administered 3 times a week, and the chloricacid amycin lipidbody (Caelyx) through the novel polyethyl glycol to contain amycin, can make its retention time in the body than the ordinary preparation of amycin extended, conducive to the effect of the drug, and more convenient to use (once a month) Now the third generation liposomes (targeted long-cycle lipids) are being studied and developed Nanoparticle injection
January 2005, the United States FDA approved the whiteprotein-combined yewol nanoparticle injection suspension market, for metastatic breast cancer after the failure of combination chemotherapy or secondary chemotherapy within 6 months of recurrence of breast cancer This indicates that a new class of "protein binding particles" drug can be prepared using ABI patented nanoparticle albumin binding technology This product is composed of albumin-bound yewol nanoparticles, which do not contain adverse reactions severe surfactants Thanks to nanoparticle technology, the therapeutic dose and even more yew alcohol can be released into the body via a regular intravenous tube for 30 minutes Taxol, a sequoia-based agent with Cremophor -
EL as a surfactant, requires the use of steroid hormones and antihistamines for preventive treatment before use, and the infusion time is up to 3 hours Magnetic nanoparticle injections for diagnosis have also been used clinically The patented technology of vault foam-type long-acting release
drug developed by Skyepharma has been successfully applied to the aglycosine slow-release injection, consisting of dispersed water-filled chamber lipids in the matrix Lipid particle size is 10 to 30 microns, suspended in physiological saline, mixed suspension like skimmed milk, can be injected with fine needles The water-filled chamber contains drugs and is the main body of lipids Lipids use natural substances such as phospholipids and triglycerides, which can be controlled in the time of release from 1 to 30 days After injection, the drug-containing particles gradually degrade, prolonging the release time of the drug, can be injected once in two weeks, thus greatly reducing the disturbance of patients' lives, reducing the risk of frequent injections, but also reduce medical costs And most importantly, slow release allows asugarcyscosides to maintain high concentrations in cerebrospinal fluid, and can also delay the of disease Recently, the U.S FDA also approved the listing of a foam-type injection for morphine storage sulfate storage to treat pain after major surgery The principle of release of a needle-free injection release system a needle-free release system is the use of a powder/liquid injection handheld device that uses a transdermal release drug, which uses high-pressure gas (helium, etc.) to instantly accelerate the drug powder/droplet to 750 m/s and enter the skin cell through the skin cells It controls the depth of the release and releases macromolecules (such as antigens) directly into the epidermis, whereas regular needle injections are difficult to handle If the vaccine is applied in the combination of the epidermis and the dermis, a strong immune response can be produced Bioject has listed needle-free drug deliverers for the release of pediatric human growth hormone (produced by Serono) Medical House PLC has also sold the innovative Mhi -
500 insulin needle-free injection system in more than 30 countries, including the UK, France, Germany, Ireland and Italy, which releases up to 70 units of up to 100 units of insulin in a single dose, replacing syringes or pen syringes for insulin injections (reproduced from China Medical Daily)