Innovation of pharmaceutical enterprises: new technology makes the legend of raylin peptide medicine

Long term demand for drugs leads to new dosage forms Although raylin can effectively promote the release of gonadal hormone, it is easy to be degraded by gastrointestinal peptidase, which makes it ineffective in oral administration Most of the clinical drugs need to be injected Because some diseases require long-term administration, this provides opportunities for innovative dosage forms Such as the sustained-release microspheres, the triptorelin sustained-release microspheres developed by Ipsen company in France, which was first listed in the world, were listed in 1986 Sustained release microsphere technology is to encapsulate the drug in the microsphere carrier, through subcutaneous or intramuscular administration, make the drug release slowly, change the process of transport in vivo, and extend the action time The sustained-release microsphere technology was also used by leuprorelin The sustained-release and long-term effects of implants not only reduce the trouble of continuous medication, but also provide convenience for the use of Rayleigh drugs in contraception or treatment of cancer and chronic diseases Implants are divided into non injectable implants and injectable implants Non injectable implants are implanted into the human body through surgery, and then the drugs can be released slowly and evenly in a long time At present, this method is commonly used in contraceptives Injectable implant is to mix and melt the drug and PLGA, then extrude them into strips by porous device, cut them into a certain length, sterilize them and put them into a special disposable syringe In the clinical direct subcutaneous or intramuscular injection, the drug will play a long-term role with the degradation of the skeleton material Injectable implants do not need to be implanted or taken out like non injectable implants, so they are easy to use and simple to prepare The computer-controlled infusion pump delivery system can achieve long-term and accurate drug delivery, which is a safe and effective way to treat chronic diseases   A long-term preparation from wind and water The treatment group of prostate cancer drug of Endo company, amrelin vantas, is administered subcutaneously once a year, which can stably inhibit testosterone for a long time and keep castration level, so as to realize palliative treatment of advanced prostate cancer It uses Valera's hydron (water absorbing acrylic polymer) implant patent technology, so that histamine can be administered for 12 months In 2007, another group of amrelin drug, supplelinla, approved by Endo, was used to treat central precocious puberty in children It can release amrelin and inhibit the secretion of gonadotropin by subcutaneous implantation of microplate for one year, and temporarily inhibit the development of puberty The results showed that the implantation of 50mg histamine in the arm subcutaneously for one year was very effective in the treatment of central precocious puberty, and had the advantages of avoiding repeated drug injection and dose adjustment Of course, there are also Zoladex, AstraZeneca's goserellin implant, which is well developed in China It has two specifications: 3.6mg once a month and 10.8mg once a month In 2015, its global sales reached 816 million US dollars Due to its unique physical and chemical properties, LHRH drugs are bound to be innovated throughout the development of this kind of drugs, as well as new dosage forms and new technologies At the same time of reducing toxicity and increasing patients' compliance, new technology has undoubtedly made the legend of Rayleigh peptide drugs   Top 4 sales volume of domestic raylin drugs Light prolin Leuprorelin is a nine peptide analogue of GnRH, which is used in endometriosis, prostate cancer and breast cancer With a total domestic sales volume of 1.213 billion yuan, the market is divided into three parts: Takeda, Beijing Bonte and Shanghai Lizhu Takeda is slightly dominant, and the three products are slow-release microsphere powder Qu Puruilin Triptorelin is a ten peptide synthesized by triptorelin, which is a GnRH analogue It is clinically used for prostate cancer and precocious puberty The total domestic sales volume is 1.067 billion yuan French Yipu Sheng and Huiling account for more than 90% of the market, and the share of domestic enterprises is less than 10% Gore Sherry Lin Goserellin is a synthetic decapeptide, a GnRH analog, which is used in prostate cancer and breast cancer The total domestic sales amount is 1.029 billion yuan The market is exclusively owned by AstraZeneca, and the product is injection implant Alapril Alarelin is a nine peptide analogue of GnRH, which is used in endometriosis The total domestic sales volume is nearly 3 million yuan, and the market is Ma'anshan Fengyuan (Reprint) July 25, 2019