Impact of Inter- and Intramolecular Interactions on the Physical Stability of Indomethacin Dispersed in Acetylated Saccharides

Kamińska, Ewa; Adrjanowicz, Karolina; Tarnacka, Magdalena; Kołodziejczyk, K.; Dulski, Mateusz; Mapesa, Emmanuel Urandu; Żakowiecki, Daniel; Hawełek, ᴌ.; Kaczmarczyk-Sedlak, Ilona; Kamiński, Kamil

doi:10.1021/mp500286b

Cited by 27 publications

(31 citation statements)

References 52 publications

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“…IR and Raman spectroscopy are also important tools to study changes in intermolecular interactions upon amorphization and the presence of drug-polymer or drugcoformer interactions that stabilize the system [202][203][204][205][206][207][208]287]. H bonding between the drug and the polymer or coformer can affect the molecular mobility of the API, inhibit H bonding between two API molecules and can impact on the crystallization driving force due to the relative strength of API-polymer/coformer and API-API H bonds.…”

Section: Savolainen Et Al Reported An Example Where In Situmentioning

confidence: 99%

Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals

Erxleben

2016

CPD

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Understanding the properties, stability and transformations of the solid-state forms of an active pharmaceutical ingredient (API) in the development pipeline is of crucial importance for process-development, formulation development and FDA approval. Investigation of the polymorphism and polymorphic stability is a routine part of the preformulation studies. Vibrational spectroscopy allows the real-time in situ monitoring of phase transformations and probes intermolecular interactions between API molecules, between API and polymer in amorphous solid dispersions or between API and coformer in cocrystals or coamorphous systems and thus plays a major role in efforts to gain a predictive understanding of the relative stability of solid-state forms and formulations. Infrared (IR), near-infrared (NIR) and Raman spectroscopies, alone or in combination with other analytical methods, are important tools for studying transformations between different crystalline forms, between the crystalline and amorphous form, between hydrate and anhydrous form and for investigating solid-state cocrystal formation. The development of simple-to-use and cost-effective instruments on the one hand and recent technological advances such as access to the low-frequency Raman range down to 5 cm-1, on the other, have led to an exponential growth of the literature in the field. This review discusses the application of IR, NIR and Raman spectroscopies in the study of solid-state transformations with a focus on the literature published over the last eight years.

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Section: Savolainen Et Al Reported An Example Where In Situmentioning

confidence: 99%

Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals

Erxleben

2016

CPD

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“…[21][22] Studies have shown that small molecules like amino acids, sugar, urea, citric acid, kaolin, aluminium hydroxide 23 or other API can improve physical stability of the amorphous drugs more effectively than polymers. [24][25][26] The main reason for the stability of the co-amorphous system was attributed to molecular interactions between the drugs/excipient in the system. It was reported that unstable drug like Naproxen could be stabilized by Indomethacin and Cimetidine, and dissolution rates of these systems were also enhanced.…”

Section: Introductionmentioning

confidence: 99%

Co-Amorphization of Ibuprofen by Paracetamol for Improved Processability, Solubility, and In vitro Dissolution

Bhandari

Wairkar

Patil

et al. 2018

ACSi

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Co-amorphous (COAM) systems of ibuprofen (IB) and paracetamol (PA), in clinical dose ratios, were prepared by ball milling to enhance solubility and dissolution of IB. Subsequently, COAM were characterized by solubility, processability, XRPD, DSC, ATR-FTIR, SEM, in-vitro dissolution and accelerated stability studies. Maximum increase in aqueous solubility of IB was seen in 500:200 mg dose ratio (COAM 1) with 6.7 fold rise from 78.3 ± 1.1 to 522.6 ± 1.29 µg/ml. COAM 1 exhibited 99.80 ± 0.58% dissolution of IB at 20 min in phosphate buffer, significantly high (P < 0.05) compared to plain IB. Thus saturation solubility and dissolution rate of IB was found significantly improved unlike PA. The flowability/processability of COAM system was remarkably improved compared to pure IB, speculated due to as formation of miniscular forms of PA-IB, having strong adhesive interactions. XRPD and DSC results confirmed amorphization of IB. ATR-FTIR results evidenced hydrogen bonding interactions between both the drugs. In accelerated stability studies, flowability, XRPD, DSC and in-vitro dissolution studies demonstrated insignificant changes, thus confirming successful stabilisation of IB by PA.

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“…Acetylated starch is classified by the Food and Drug Administration (FDA) as a Generally Recognized as Safe (GRAS) material. Numerous investigations regarding the use of various sugar derivatives, i.e., acetylated sucrose, glucose, maltose, galactose, to stabilize amorphous forms of drugs, such as indomethacin, itraconazole, and nifedipine have been published (6,17,18). Solid dispersions composed of amorphous APIs have been obtained by melting with appropriate ratios of active substances and modified saccharides followed by rapid cooling.…”

Section: Introductionmentioning

confidence: 99%

“…Moreover, it has been found that the amorphous form of API remained stable even after 1 year of storage under room conditions (22). In this context, application of acetylated saccharides in the formulation seems to be a promising option (11,17,18).…”

Section: Introductionmentioning

confidence: 99%

Melts of Octaacetyl Sucrose as Oral-Modified Release Dosage Forms for Delivery of Poorly Soluble Compound in Stable Amorphous Form

Haznar-Garbacz

Kamińska

Żakowiecki³

et al. 2017

AAPS PharmSciTech

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Abstract. The presented work describes the formulation and characterization of modified release glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model BCS (Biopharmaceutical Classification System) class II drug. The GSDFs were prepared by melting nifedipine together with octaacetyl sucrose. Dissolution profiles, measured under standard and biorelevant conditions, were compared to those obtained from commercially available formulations containing nifedipine such as modified release (MR) tablets and osmotic release oral system (OROS). The results indicate that the dissolution profiles of the GSDFs with nifedipine are neither affected by the pH of the dissolution media, type and concentration of surfactants, nor by simulated mechanical stress of biorelevant intensity. Furthermore, it was found that the dissolution profiles of the novel dosage forms were similar to the profiles obtained from the nifedipine OROS. The formulation of GSDFs is relatively simple, and the dosage forms were found to have favorable dissolution characteristics.

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Impact of Inter- and Intramolecular Interactions on the Physical Stability of Indomethacin Dispersed in Acetylated Saccharides

Cited by 27 publications

References 52 publications

Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals

Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals

Co-Amorphization of Ibuprofen by Paracetamol for Improved Processability, Solubility, and In vitro Dissolution

Melts of Octaacetyl Sucrose as Oral-Modified Release Dosage Forms for Delivery of Poorly Soluble Compound in Stable Amorphous Form

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