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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Co-crystal Advantages of Co-crystals: Improvement of Physicochemical Properties: Co-crystals significantly enhance the physicochemical properties of active pharmaceutical ingredients (APIs) without disrupting covalent bonds. This improvement includes aspects such as melting point, solubility, permeability, stability, bioavailability, and mechanical properties. Co-crystals enrich the solid-state forms of drugs, particularly beneficial for amorphous, non-dissociating, or low pKa active pharmaceutical ingredients, thereby serving as a crucial means to alter the solid-state form of drugs. Establishing Intellectual Property Protection: Co-crystals offer substantial potential in establishing intellectual property protection and extending the lifecycle of APIs. Masking Techniques / Formulation Production: Co-crystals find excellent applications in masking the taste of drugs, improving tabletting performance, and expanding production capabilities. Methods for preparing co-crystals The methods for preparing co-crystals are mainly divided into two categories: solution methods (including solution evaporation, reaction crystallization, and cooling crystallization) and grinding methods (dry grinding and wet grinding). There are also some less common methods for preparing co-crystals, such as gel method, hot melt extrusion, spray drying, hot stage microscopy, and supercritical fluid method. Preparation method of eutectic It is mainly divided into two categories: solution method (solution evaporation method, reaction crystallization method, and cooling crystallization method) and grinding method (dry grinding, wet grinding) There are also some rare methods to prepare eutectic, such as gel method, hot melt extrusion method, spray drying method, thermal microscope method and supercritical fluid method. Co-crystal screening Co-crystal screening is the experimental process of determining whether candidates for co-crystal formers (CCFs) can crystallize with known active pharmaceutical ingredients (APIs). There are various technical methods used in pharmaceutical co-crystal screening, including high-throughput crystallization screening, supercritical fluid enhanced spray technology, solution methods, and grinding methods. Additionally, screening methods based on the Cambridge Structural Database, thermodynamic approaches (such as hot-stage microscopy and differential scanning calorimetry), and slurry crystallization screening are also employed. Co-crystals possess a unique potential to enhance drug characteristics and therapeutic effects without altering the chemical properties and biological activity of active pharmaceutical ingredients. This characteristic has made co-crystals a significant branch in pharmaceutical development. By selecting suitable co-crystal formers and screening for new co-crystals that can improve the physicochemical properties of APIs, changes in solid-state structures can be achieved, thus allowing for patent protection. Since there is currently no method to predict co-crystal formation accurately, discovery often relies on iterative experimentation. Consequently, co-crystals do not exhibit obviousness, and newly discovered, previously unreported co-crystals typically qualify for patent protection. Research in the preparation, cultivation, screening, and characterization of co-crystals is expected to expand significantly in the future. Case Study - Entresto Entresto, also known as sacubitril/valsartan, is a novel co-crystal medication developed by Novartis. It combines sacubitril, an inhibitor of neprilysin (a peptidase enzyme involved in regulating blood pressure), with valsartan, an angiotensin II receptor blocker (ARB). Approved by the FDA in July 2015, six weeks ahead of schedule as a combination therapy for heart failure, Entresto's co-crystal structure ensures similar absorption and elimination rates for both active ingredients. This synchronicity optimizes their therapeutic effects concurrently. The co-crystal formulation offers advantages over independent formulations, notably enhancing the bioavailability of valsartan, which allows for corresponding dose reduction. Entresto has become a leading cardiovascular medication for chronic heart failure, with sales reaching approximately $1.73 billion in 2019, marking a 68% increase from 2018. Sacubitril exhibits an oral bioavailability of ≥60%, while valsartan's oral bioavailability is enhanced by 50%, with no significant food effects observed.
Some representative co-crystal drugs already on the market |
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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