Drug solid-state screening
Rapid and precise deciphering of complex formulations
In-depth analysis of
solid-state properties
Development and Industrialization of Solid State
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第一行主标题 请输入要描述的内容进行内容补充请输入 - Salt and Solid State Screening 第一行主标题 请输入要描述的内容进行内容补充请输入 - Evaluation of drug efficacy 第一行主标题 请输入要描述的内容进行内容补充请输入 - Assessment of Drug Efficacy 第一行主标题 请输入要描述的内容进行内容补充请输入 - Stable amorphous development |
Intellectual Property Breakthrough Originator pharmaceutical companies often establish barriers through layered patent protection to extend the lifecycle of their drugs. Even after the compound patent for an originator drug expires, the crystalline form patent may still be in effect, creating a patent barrier that delays the market entry of other improved drugs or generics. New Yang Weikang's technical team can assist you in developing superior new crystal forms to break through the patent blockade of originator crystal forms and related delivery systems, seizing market opportunities swiftly after the compound patent expires. Our company's technical team achieves this by modifying molecules in terms of crystalline aspects, enhancing API dissolution rates while maintaining certain physical stability, and continuously improving its formulation properties. We have successfully developed dozens of new crystal forms through screening and obtained patents. These new crystal forms address shortcomings of originator crystal forms, such as faster dissolution rates that aid absorption in the gastrointestinal tract, thereby enhancing drug bioavailability. Case Patent Display A Patent display of new drug crystal forms (partial patents) Baloxavirmarboxil (trade name: Xofluza) is a novel anti influenza drug developed by Shionogi, a Japanese pharmaceutical company, and jointly researched with Roche, Switzerland, targeting influenza A and B viruses. In February 2018, Baloxavir received accelerated approval and was approved for market launch in Japan. In October 2018, the US Food and Drug Administration (FDA) accepted a new drug application for Baloxavir axetil and granted it priority review qualifications. This drug is the first approved anti influenza drug with a novel mechanism of action in the United States in nearly 20 years. In April 2021, Baloxavir tablets were approved by the National Medical Products Administration (NMPA) of China for domestic marketing, with the marketed drug name being Mabaloxavir tablets. Baloxavir ester is a precursor drug that hydrolyzes into the active substance Baloxavir in the body, exerting anti influenza virus activity. The original research patent WO2018030463A1 (Japanese patent JP6249434B1) reported Baloxavir Form I, Form II, and Form III. Form I is crystallized from a mixture of dimethyl sulfoxide/water, Form II is crystallized from acetonitrile/water, and Form III is crystallized from methyl acetate. Among them, Type I crystallization is the crystal form used in the preparation of solid formulations in patent JP 6590436 B1 and its related patents, which has been proven to be stable when stored at room temperature. According to reports, the solubility of the API in aqueous solutions between pH 1 and 7 at 37 ° C is 18-21 μ g/mL. Figure: PXRD pattern of the original crystal structure Our technical team has modified the crystalline structure of baloxavir marboxil molecules to enhance the dissolution rate of the active pharmaceutical ingredient (API), while maintaining adequate physical stability and continuously improving its formulation properties. Through screening and preparation, they have developed a new crystal form of baloxavir marboxil. Studies indicate that this new crystal form exhibits faster dissolution rates, facilitating better absorption in the gastrointestinal tract and thereby enhancing the drug's bioavailability. Patent Showcase B. Levomilnacipran (brand name Fetzima) is the levorotatory enantiomer of milnacipran, developed jointly by Forest Laboratories, Inc. (now Allergan) from the United States and Pierre Fabre Pharmaceuticals from France. Due to the high therapeutic value of levomilnacipran, research on existing crystalline forms of levomilnacipran can lead to the development of superior new crystal forms, breaking through the original research's crystalline form patents. Obtaining advantages such as high purity, crystal stability, and reproducible preparation methods with a new crystal form is highly significant for pharmaceutical companies. The new crystal form can improve upon deficiencies in the original product while providing formulation advantages, such as long-term stability under varied environmental conditions without strict requirements for temperature, light, or humidity. The original research worldwide patent WO2011/057176A1 discloses a crystalline form (Form A) of levomilnacipran hydrochloride. The preparation method of Form A primarily involves crystallization using water or alcohols as solvents. Research literature indicates that the dissolution rate of the original research's levomilnacipran hydrochloride may decrease with extended storage time, potentially affecting its efficacy in the body. Figure: PXRD Pattern of the new crystalline form (Form B) of Levomilnacipran hydrochloride By creatively avoiding the use of water or alcoholic solvents traditionally used in the dissolution of levomilnacipran molecules, and instead opting for solvents with slightly lower limits but still possessing adequate solubility characteristics, along with the addition of other solvents or polymers, a new crystal form has been obtained through expedited solvent removal techniques. This new crystal form enhances the pharmaceutical properties of the drug, including but not limited to improved dissolution rates, high crystallinity, stability of crystalline structure, good flow properties, excellent solubility, and ease of preparation. Additionally, leveraging the obtained crystal form can provide advantages in formulation. |
Solid State Research
Improving drug absorption through solid-state technology is the foundation of all innovative technologies at Xinyang Weikang.
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Innovative Improved Drugs
Our company strategically focuses on developing high-end formulations, successfully completing numerous advanced oral film formulations, and establishing a systematic approach to formulation development.
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CDMO
We are the only integrated domestic platform specializing in crystalline formulation production, strictly adhering to GMP standards. We specialize in scaling up research and commercial production of various dosage forms including oral films, topical formulations, and solid formulations.
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Nycrist Phamatech Co.,Ltd
Tel：19129598229
19129598368（Mr.Lee）
19926561149（Mrs.Chen）
19926414326（Mr.Liu）
Headquarters Address: Building A3, Guanming Technology Park, No. 3009 Guangming Avenue, Fenghuang Community, Fenghuang Street, Guangming District, Shenzhen
Production Base Address: Weiguang Life Science Park, Guangming District, Shenzhen
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