Ruilin-like peptide drug innovative dosage form attribute July 22, 2016 Source: admin01 Growth Promtor,Growth Promoter For Poultry,Growth Promoter Hormone,Growth Promoter For Cattle Sichuan Aibang Weiye Biological Engineering Co., Ltd. , https://www.aibangpharm.com
Ruilin-like peptide drug innovative dosage form attribute
Ruilin drugs refer to a large class of synthetic peptide drugs based on the structure of gonadotropin releasing hormone (GnRH), also known as luteinizing hormone releasing hormone (LHRH). When exogenous GnRH or its analog is administered in short-term low dose at physiological pulse frequency (every 90 min), it promotes the pituitary gland system and is used clinically for the treatment of sexual dysfunction, anovulation, and puberty delay. When administered at a non-physiological pulse frequency for a long-term large dose, it can inhibit the secretion of LH and FSH from the pituitary gland, resulting in decreased gonad-secreting hormone capacity and atrophy of the sexual organs. It is clinically used to treat some hormone-dependent diseases such as prostate cancer and uterine fibroids. Breast cancer, endometriosis and adolescent precocious puberty.
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In 1971, humans discovered and elucidated the structure of LHRH, and then people began to synthesize more active LHRH analogues, and made breakthroughs in the short term. Then, Goserelin and Buscherin appeared like mushrooms, which drove the prosperity of such drugs. The FDA currently approves eight types of Ruilin products, including a variety of specifications and dosage forms.
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FDA approved relin drugs
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Of course, there are also the early-developed alanurin in China, the buserelin developed by West Germany, and the products such as Tallinn and leuprolide developed by Japanese companies . At present, there are six varieties commonly used in the domestic market, including the two types of troprelin and leuprolide produced by both imported and state-owned enterprises, as well as the exclusive AstraZeneca Goserelin, the state-owned Prolin, Gona Relin and Alanine. The best sellers are Goserelin, Triptorelin and Leuprolin.
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It is impressive that most of these products are eligible for priority review or have orphan drug status. For example, Shire's group Aurora Lin SUPPRELIN LA has both of these identities; while Gona Relin, Kelly Relin, etc. Orphan drug identity. Many of them are the first drugs of a certain disease, such as the Merck subsidiary EMD Serono's product, which is the FDA approved for abnormal HIV caused by lipodystrophy in HIV-infected patients. This is the first one. The only drug approved for the treatment of the disease.
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Although the relin drugs can effectively promote the release of gonadotropins, they are easily degraded by gastrointestinal peptidase, making them orally ineffective, and most of them require injection. Because some diseases require long-term administration, this provides an opportunity for innovative dosage forms.
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For example, the first time in the world was the Triptorel sustained-release microsphere developed by the French company Ipsen, which was launched in 1986. The sustained-release microsphere technology encapsulates the drug in a microsphere carrier and delivers it slowly or subcutaneously or intramuscularly, thereby slowly releasing the drug, changing the process of transport in the body, and prolonging the action time. The leuprolide and the like also adopt the sustained release microsphere technology.
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The long-acting effect of sustained release of the implant not only reduces the trouble of continuous medication, but also facilitates the use of Ruilin drugs for contraception or treatment of cancer and chronic diseases. The implant is divided into a non-injectable implant and an injectable implant. The non-injectable implant is surgically implanted into the human body, and then the drug can be slowly and uniformly released over a long period of time. Currently, contraceptives are commonly used. This method. Injectable implants are prepared by mixing and melting the drug with PLGA, then extruding it into strips through a porous device, cutting it to a certain length, and sterilizing it into a special disposable syringe. Direct clinical or subcutaneous injection, the drug is released with the degradation of the matrix material to play a long-lasting effect. The injection type implant does not need to be surgically implanted or taken out like a non-injection type implant, and is convenient to use and simple to prepare. The computer-controlled infusion pump delivery system can achieve long-term, precise administration, and is a safe and effective route for the treatment of chronic diseases.
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ENDO's treatment of prostate cancer drug group Aminocillin VANTAS, the use of subcutaneous implantation once a year, can stably inhibit testosterone for a long time, so that it maintains castration level, so that palliative treatment of advanced prostate cancer can be achieved. It uses Valera's patented Hydron (water-absorbing acrylic polymer) implant technology to allow continuous administration of histamine for 12 months. Another group of the aminosulinin drug Supprelin LA approved in ENDO in 2007 is clinically used to treat central precocious puberty in children . It can slowly release histamine from subcutaneously implanted microplates for 1 year to inhibit pituitary secretion of gonadotropin and temporarily inhibit puberty development. The test results show that the subcutaneous implantation of 50 mg of histamine in the arm of the child is very effective for the treatment of central precocious puberty, and has the advantages of avoiding repeated drug injection and dose adjustment. Of course, AstraZeneca's Goserelin implant ZOLADEX, which is made in China, contains 3.6mg once a month and 10.8mg every three months. In 2015, its global sales were 8.16. One hundred million U.S. dollars.
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Due to its unique physical and chemical properties, LHRH drugs are destined to innovate in the development of such drugs, and enable new dosage forms and new technologies to develop rapidly. New technologies, etc., while attenuating and increasing efficiency and increasing patient compliance, have undoubtedly achieved the legend of Ruilin-like peptide drugs.
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