Advances in coamorphous drug delivery systems

Shi, Qin; Moinuddin, Sakib M.; Cai, Ting

doi:10.1016/j.apsb.2018.08.002

Cited by 128 publications

(77 citation statements)

References 124 publications

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“…The high internal energy of amorphous solids, which, on the one hand, is the reason for their high solubility, on the other hand, makes amorphous materials thermodynamically unstable [10][11][12][13][14]. Thus, currently, much effort is being made to (i) investigate physical stability of amorphous form of pharmaceuticals [15][16][17], (ii) find effective methods leading to their stabilization [18][19][20], and (iii) discover the molecular mechanisms responsible for the observed recrystallization inhibition [16,[21][22][23][24][25].…”

Section: Introductionmentioning

confidence: 99%

Importance of Mesoporous Silica Particle Size in the Stabilization of Amorphous Pharmaceuticals—The Case of Simvastatin

et al. 2020

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In this paper, the role of mesoporous silica (MS) particle size in the stabilization of amorphous simvastatin (SVT) is revealed. For inhibiting recrystallization of the supercooled drug, the two MS materials (Syloid® XDP 3050 and Syloid® 244 FP) were employed. The crystallization tendency of SVT alone and in mixture with the MS materials was investigated by Differential Scanning Calorimetry (DSC) and Broadband Dielectric Spectroscopy (BDS). Neither confinement of the SVT molecules inside the MS pores nor molecular interactions between functional groups of the SVT molecules and the surface of the stabilizing excipient could explain the observed stabilization effect. The stabilization effect might be correlated with diffusion length of the SVT molecules in the MS materials that depended on the particle size. Moreover, MS materials possessing different particle sizes could offer free spaces with different sizes, which might influence crystal growth of SVT. All of these factors must be considered when mesoporous materials are used for stabilizing pharmaceutical glasses.

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Section: Introductionmentioning

confidence: 99%

Importance of Mesoporous Silica Particle Size in the Stabilization of Amorphous Pharmaceuticals—The Case of Simvastatin

et al. 2020

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“…A co-amorphous system has shown some promising results for solubility enhancement in the delivery of poorly water-soluble drugs. A co-amorphous system can be defined as a single phase system made up of a crystalline API and a co-former of low molecular weight molecules which could be either relevant APIs or excipients (104). Some examples of the co-former include urea, sugar, amino acids and carboxylic acids, which are known to be able to enhance the stability and solubility in a co-amorphous system (105).…”

Section: Other Recent Innovation Formulations Via Hot-melt Extrusionmentioning

confidence: 99%

“…Some of the most commonly used PAT tools include UV-Vis ( 139 , 140 ), Fourier transform near-infrared (FT-NIR) ( 104 , 119 ), and Raman ( 141 , 142 ) spectroscopy techniques. These techniques are simple, fast, and non-destructive to the samples during the HME process.…”

Section: Recent Innovations In Hot-melt Extrusion To Prevent Thermal mentioning

confidence: 99%

Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing

Tan

Davis

Miller³

et al. 2020

AAPS PharmSciTech

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Thermal processing has gained much interest in the pharmaceutical industry, particularly for the enhancement of solubility, bioavailability, and dissolution of active pharmaceutical ingredients (APIs) with poor aqueous solubility. Formulation scientists have developed various techniques which may include physical and chemical modifications to achieve solubility enhancement. One of the most commonly used methods for solubility enhancement is through the use of amorphous solid dispersions (ASDs). Examples of commercialized ASDs include Kaletra®, Kalydeco®, and Onmel®. Various technologies produce ASDs; some of the approaches, such as spray-drying, solvent evaporation, and lyophilization, involve the use of solvents, whereas thermal approaches often do not require solvents. Processes that do not require solvents are usually preferred, as some solvents may induce toxicity due to residual solvents and are often considered to be damaging to the environment. The purpose of this review is to provide an update on recent innovations reported for using hot-melt extrusion and KinetiSol® Dispersing technologies to formulate poorly water-soluble APIs in amorphous solid dispersions. We will address development challenges for poorly water-soluble APIs and how these two processes meet these challenges.

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“…However, it is not an uncommon problem that the inherent higher apparent solubility of an amorphous material is offset by poor dispersibility or wettability (Gniado et al, 2016). Furthermore, so far little attention has been paid to the design of drug-drug coamorphous systems with a pharmacologically relevant dose ratio (Shi et al, 2018). When drug complementarity is taken into accountboth in terms of indication and relative dosethe development of viable coamorphous formulations has remained a challenging task.…”

Section: Introductionmentioning

confidence: 99%

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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Advances in coamorphous drug delivery systems

Cited by 128 publications

References 124 publications

Importance of Mesoporous Silica Particle Size in the Stabilization of Amorphous Pharmaceuticals—The Case of Simvastatin

Importance of Mesoporous Silica Particle Size in the Stabilization of Amorphous Pharmaceuticals—The Case of Simvastatin

Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing

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

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