制药性晶体:设计,制备,应用和挑战的回顾
Suvarna Jagannath Shelke1, Dhanashri Haushiram Bhangare1, Mayuri Deepak Patil1
1Department of Pharmaceutics, SMBT College Of Pharmacy, Nashik, Maharashtra, India.
概括
药物共结晶,多组分固体, 增强药物的溶解性和生物可用性. 这一审查涵盖了它们的设计,制备和应用,提供了新的配方可能性.
科学领域:
- 材料科学
- 制药科学
- 水晶工程
背景情况:
- 药用共晶体是多元晶体固体,增强活性药物成分 (API) 的物理化学特性.
- 它们可以提高溶解度,生物可用性,稳定性和溶解率,而不会改变药理活性.
- 晶是通过非离子相互作用形成的,例如键和π-π堆叠.
研究的目的:
- 审查药用共晶体的演变,设计,制备和应用.
- 突出其在改善药物性能,实现受控释放和创造知识产权方面的潜力.
- 讨论共同晶体发展的挑战和监管考虑.
主要方法:
- 探索各种制备技术,包括基于溶剂 (例如,溶剂蒸发,冷却结晶) 和基于固体 (例如,研磨,液体辅助研磨) 的方法.
- 设计策略的讨论,重点是结倾向和超分子合成方法.
- 分析诸如分子兼容性,热力学障碍和监管障碍等挑战.
主要成果:
- 制药类晶为优化药物输送和配方提供了一种多功能平台.
- 通过成功应用cocrystal技术,可以提高药物的有效性和患者的服药性.
- 晶体工程的进步和监管的接受正在为商业化铺平道路.
结论:
- 制药性共晶体代表了药物开发的重大进步,提供了增强的物理化学和药物动力学特征.
- 进一步的研究对于克服现有挑战和充分利用cocrystal技术的商业潜力至关重要.
- 这项审查强调了可晶体在优化药物输送和配方方面具有有意义的治疗效益.
相关概念视频
01:25Crystal Growth: Principles of Crystallization
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Crystallization is a phase transformation process in which crystals are precipitated from a supersaturated solution or formed from other sources. During crystallization, atoms or molecules arrange themselves into a well-defined, rigid crystal lattice to minimize energy.
Initiating crystallization involves manipulating the concentration of the solute and the temperature of the solution. Since crystal growth occurs when the ratio of concentration and solubility of the solute in the solvent...
Initiating crystallization involves manipulating the concentration of the solute and the temperature of the solution. Since crystal growth occurs when the ratio of concentration and solubility of the solute in the solvent...
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01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
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Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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01:22Biopharmaceutical Factors Influencing Drug Product Design: Overview
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Rational drug product design integrates knowledge of the drug’s physicochemical properties, formulation components, manufacturing techniques, and intended route of administration. Each factor influences the drug’s performance, including how it is released, absorbed, and eliminated in the body.The physicochemical properties of a drug—such as solubility, stability, and particle size—affect its compatibility with excipients and the choice of dosage form. Excipients, though...
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01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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