Recent advances in improving oral drug bioavailability by cocrystals

Emami, Shahram; Siahi‐Shadbad, Mohammadreza; Adibkia, Khosro; Barzegar-Jalali, Mohammad

doi:10.15171/bi.2018.33

Cited by 99 publications

(85 citation statements)

References 133 publications

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“…34 But the preparation of nano co-crystals are challenging due to their phase instability of co-crystals in aqueous medium. 68 Recently multi-drug co-crystal (MDC) is also gaining attraction among pharmaceutical scientists. 69 MDC have synergistic effects, increased solubility, bioavailability, and potential to stabilize unstable components via intermolecular interactions.…”

Section: Applications Of Co-crystals In Pharmaceutical Industrymentioning

confidence: 99%

Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

et al. 2020

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Pharmaceutical co-crystals are novel class of pharmaceutical substances, which possess an apparent probability of advancement of polished physical properties offering stable and patentable solid forms. These multi-component crystalline forms influence pertinent physicochemical parameters like solubility, dissolution rate, chemical stability, physical stability, etc. which in turn result in the materials with superior properties to those of the free drug. Co-crystallization is a process by which the molecular interactions can be altered to optimize the drug properties. Co-crystals comprise a multicomponent system of active pharmaceutical ingredient (API) with a stoichiometric amount of a pharmaceutically acceptable coformer incorporated in the crystal lattice. By manufacturing pharmaceutical co-crystals, the physicochemical properties of a drug can be improved thus multicomponent crystalline materials have received renewed interest in the current scenario due to the easy administration in the pharmaceutical industry. There is an immense amount of literature available on co-crystals. However, there is a lack of an exhaustive review on a selection of coformers and regulations on co-crystals. The review has made an attempt to bridge this gap. The review also describes the methods used to prepare co-crystals with their characterization. Brief description on the pharmaceutical applications of co-crystals has also been incorporated here. Efforts are made to include reported works on co-crystals, which further help to understand the concept of co-crystals in depth.

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Section: Applications Of Co-crystals In Pharmaceutical Industrymentioning

confidence: 99%

Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

et al. 2020

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“…Poznanie mechanizmu rozpuszczania i procesów poprzedzających absorpcję substancji czynnej jest konieczne, aby zaprojektować odpowiednią postać leku wykorzystującą potencjał zwiększonej rozpuszczalności API ko-krystalizowanej z substancją obojętną. Proponowany w literaturze mechanizm zwiększenia rozpuszczalności substancji czynnej w formie ko-kryształu w stosunku do substancji macierzystej polega na utworzeniu przejściowego roztworu przesyconego podczas rozpuszczania ko--kryształów [6]. Mechanizm ten jest charakterystyczny dla postaci amorficznych oraz soli.…”

Section: Rozpuszczanie Ko-kryształów In Vivounclassified

“…Powyższą właściwość nazwano efektem spadochronu (ang. parachute) (rycina 1) [6,7]. Dodanie inhibitora wytrącania może prowadzić do zwiększonej biodostępności substancji czynnej w formie ko-kryształów w porównaniu do biodostępności ko-kryształów bez dodatku substancji hamujących wytrącanie API.…”

Section: Rozpuszczanie Ko-kryształów In Vivounclassified

“…Dodanie inhibitora wytrącania może prowadzić do zwiększonej biodostępności substancji czynnej w formie ko-kryształów w porównaniu do biodostępności ko-kryształów bez dodatku substancji hamujących wytrącanie API. Jednak przeprowadzone do tej pory badania rozpuszczania in vitro ko-kryształów nie zawsze uwzględniały 3) co-crystals dissolution in the presence of crystallization inhibitor which acts as parachute [6]. efekt przesycenia i następującego po nim wytrącania, a badania farmakokinetyczne przeprowadzono dla prostych dyspersji ko-kryształów bez etapu formulacji.…”

Section: Rozpuszczanie Ko-kryształów In Vivounclassified

“…Kluczowe czynniki, które należy wziąć pod uwagę przy opracowywaniu układów przesyconych ko-kryształów, to: -zdolność do generowania i utrzymywania wysokiego stopnia przesycenia, -szybkość przemiany fazowej, -wyższa rozpuszczalność i szybkość rozpuszczania utworzonego osadu [6]. Wpływy inhibitora krystalizacji na biodostępność substancji zilustrowano na przykładzie ko--kryształów dihydromirycetyny (flawonoid należący do IV klasy BCS) z mocznikiem lub kofeiną [8].…”

Section: Rozpuszczanie Ko-kryształów In Vivounclassified

See 2 more Smart Citations

Influence of co-crystallization on bioavailability of drug substances

Kozłowska¹,

Garbacz²,

Wesołowski³

2019

Farm Pol.

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Influence of co-crystallization on bioavailability of drug substances • The majority of drug substances are poorly water-soluble compounds. Thus, the development of new approaches improving water solubility of drug substances is the most challenging issue to overcome. Co-crystallization is one of the way that is used in the pharmaceutical technology to enhance the solubility of water-insoluble compounds. For this reason, the paper deals with a short characteristic of co-crystals and their role as a new method employed for improving the solubility and permeability of active pharmaceutical ingredients. The paper focused especially on the recent advances that have been made for enhancing bioavailability of new solid forms of drug substance.

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Deep Eutectic Solvents: An Eco‐friendly Design for Drug Engineering

et al. 2023

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In the spirit of circular economy and sustainable chemistry, the use of environmentally friendly chemical products in pharmacy has become a hot topic. In recent years, organic solvents have been the subject of a great range of restriction policies due to their harmful effects on the environment and toxicity to human health. In parallel, deep eutectic solvents (DESs) have emerged as suitable greener solvents with beneficial environmental impacts and a rich palette of physico‐chemical advantages related to their low cost and biocompatibility. Additionally, DESs can be accompanied by a remarkable solubilizing effect for several active pharmaceutical ingredients (APIs), thus forming therapeutic DESs (TheDESs). In this work, special attention is paid to DESs, presenting a precise definition, classification, methods of preparation, and characterization. A description of natural DESs (NaDESs), i.e., eutectic solvents present in natural sources, is also reported. Moreover, the present review article is the first one to detail the different approaches for judiciously selecting the constituents of DESs in order to minimize the number of experiments. The role of DESs in the biomedical and pharmaceutical sectors and their impact on the development of successful therapies are also discussed.

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Recent advances in improving oral drug bioavailability by cocrystals

Cited by 99 publications

References 133 publications

Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

Pharmaceutical Co-Crystallization: Regulatory Aspects, Design, Characterization, and Applications

Influence of co-crystallization on bioavailability of drug substances

Deep Eutectic Solvents: An Eco‐friendly Design for Drug Engineering

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