Co amorphous systems: A product development perspective

Chavan, Rahul B.; Thipparaboina, Rajesh; Kumar, Dinesh; Shastri, Nalini R.

doi:10.1016/j.ijpharm.2016.10.043

Cited by 152 publications

(109 citation statements)

References 64 publications

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“…Coamorphous systems and cocrystals can be prepared by various methods (Chavan et al, 2016). In this work, ball-milling and liquid-assisted grinding, i.e.…”

Section: Resultsmentioning

confidence: 99%

“…The coformer stabilizes the (thermodynamically unstable) amorphous phase towards recrystallization by physically separating the API molecules and/or preventing the reorientation of the API molecules through the formation of API-coformer intermolecular interactions. Coamorphization becomes an even more powerful approach, when the inactive coformer is replaced with a complementary drug (Laitinen et al, 2013;Chavan et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

“…Besides overcoming dissolution and bioavailability issues, a pharmaceutically appropriate coamorphous system reduces the number of medications a patient has to take, thus improving patient compliance and quality of life. While a number of drug-drug coamorphous systems have been developed (Chavan et al, 2016), the focus has been on preparation, characterization and stabilization of the amorphous phase. Significant progress has been made on the selection of suitable coformers in this regard.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Investigation of the formation of drug-drug cocrystals and coamorphous systems of the antidiabetic drug gliclazide

Aljohani

MacFhionnghaile

McArdle

et al. 2019

International Journal of Pharmaceutics

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The antidiabetic drug gliclazide (GLZ) has a slow absorption rate and a low bioavailability due to its poor solubility. GLZ is often prescribed along with an antihypertensive, as many diabetic patients have coexistent hypertension. Cocrystallization and coamorphization are attractive strategies to enhance dissolution rates and to reduce the number of medications a patient has to take. In this work the formation of cocrystals and coamorphous systems of GLZ with various antihypertensive drugs was studied, namely chlorothiazide (CTZ), hydrochlorothiazide (HTZ), indapamide (IND), triamterene (TRI) and nifedipine (NIF) as well as benzamidine (BZA) as a model for the amidine pharmacophore. TRI, IND and HTZ were found to form coamorphous systems with GLZ that are stable for at least six months at 22  2 C and 56 % relative humidity. Coamorphous GLZ-TRI is also stable in dissolution medium. Coamorphization of GLZ-TRI with 15 % sodium taurocholate gave a viable coamorphous formulation with an enhanced dissolution rate. Comilling of GLZ with BZA and cocrystallization from solution gave the amorphous and crystalline salt, respectively and the X-ray structure is reported. During attempts to obtain X-ray suitable cocrystals crystals of 2 Na + GLZand IND . 0.5H2O were obtained. Redetermination of the published structure of IND . 0.5H2O revealed a unit cell with the length of the a axis doubled, a different space group and no disorder. Liquid-assisted grinding of a 1:1 mixture of GLZ and IND indicated the transformation of IND to a new solid-state form, while GLZ remained unaltered. Milling-and heating-induced solid-state transformations of IND are discussed.

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“…Coamorphous systems and cocrystals can be prepared by various methods (Chavan et al, 2016). In this work, ball-milling and liquid-assisted grinding, i.e.…”

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Investigation of the formation of drug-drug cocrystals and coamorphous systems of the antidiabetic drug gliclazide

Aljohani

MacFhionnghaile

McArdle

et al. 2019

International Journal of Pharmaceutics

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show abstract

“…Approximately 90% of new chemical entities (NCE) and 40% of drugs on the market are poorly water soluble [1,2]. Low-solubility drugs are characterised by slow dissolution rates and slow drug adsorption which lead to inadequate bioavailability and gastrointestinal toxicity [3].…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, amorphous materials are more hygroscopic than crystalline materials and the glass-transition temperature of most amorphous drugs is lowered, even with only very small water content [15][16][17][18]. Therefore, the phase change of an amorphous active ingredient dispersed in a polymer is facilitated by the hygroscopic nature of the polymer adopted, which has caused the recall of many products by the FDA [1].…”

Section: Introductionmentioning

confidence: 99%

Physico-chemical characterisation of three-component co-amorphous systems generated by a melt-quench method

D’Angelo

Edgar

Hurt

et al. 2018

J Therm Anal Calorim

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The purpose of this work was to evaluate the possibility of creating a ternary co-amorphous system and to determine how the properties of a co-amorphous material are altered by the addition of a selected third component. Piroxicam and indomethacin form a stable co-amorphous with the T g above room temperature. The third component added was selected based on tendency to crystallise (benzamide, caffeine) or form amorphous (acetaminophen, clotrimazole) on cooling. Generated co-amorphous systems were characterised with TGA, HSM, DSC, FTIR and XRD. Stable ternary co-amorphous systems were successfully generated, which were confirmed using XRD, DSC and FTIR analysis. In all cases, T g of the ternary system was lower than the T g of the binary system, although higher than that of the individual third component. Upon storage for 4 weeks, all created ternary systems showed significantly smaller variation in T g compared to the binary system. Stable three-component co-amorphous systems can be generated via melt-quench method using either a crystalline or an amorphous third component. Addition of third component can alter the T g of co-amorphous system and in all cases created more stable co-amorphous system upon storage. Physical parameters may not be sufficient in predicting the resulting T g ; therefore, knowledge of chemical interaction must be brought into equation as well.

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Cocrystals, Coamorphous Phases and Coordination Complexes of γ‐ andε‐Lactams

Hall

Chambers

Musa

et al. 2021

Handbook of Pyrrolidone and Caprolactam Based Materials

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The strongly interacting lactam functional group in both γand ε-lactams makes them of considerable interest in the formation of multicomponent solids including a hugely diverse range of cocrystals, coordination complexes with lactam ligands and coamorphous phases. Cocrystals are structurally homogenous crystalline substances that are comprised of two or more chemically different neutral molecules generally in stoichiometric amounts that are connected by non-ionic and non-covalent interactions [1]. The Food and Drug Administration (FDA) classifies cocrystals as crystalline materials composed of two or more different molecules, typically Active Pharmaceutical Ingredients (API) and approved, non-toxic cocrystal former (coformer), in the same crystal lattice [2].Cocrystals fall under the umbrella of multi-component molecular solids, which encompasses crystalline forms such as solvates, hydrates, and lattice inclusion compounds as well as coamorphous materials. The relationships between these various solid forms are illustrated in Figure 1. Also included under multi-component crystalline solids are solid solutions in which one component is randomly distributed in a crystal of another [4]. Salts are also multi-component molecular solids, with the main difference between a salt and a cocrystal often being proton transfer from an acid to a base that occurs to give a salt in contrast to neutral molecule cocrystals. However, the distinction is a fine one since, depending on the temperature, salts and cocrystals can interconvert [5]. Generally, true cocrystals are regarded as being formed from components that are solids at room temperature, a definition which excludes solvates and hydrates. However, this narrowing would mean that some materials involving low melting solids might be regarded as cocrystals in some labs and not others despite that fact that there is no fundamental structural difference between a cocrystal and a solvate [1,6,7].

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Co amorphous systems: A product development perspective

Cited by 152 publications

References 64 publications

Investigation of the formation of drug-drug cocrystals and coamorphous systems of the antidiabetic drug gliclazide

Investigation of the formation of drug-drug cocrystals and coamorphous systems of the antidiabetic drug gliclazide

Physico-chemical characterisation of three-component co-amorphous systems generated by a melt-quench method

Cocrystals, Coamorphous Phases and Coordination Complexes of γ‐ andε‐Lactams

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