A Practical Method to Predict Physical Stability of Amorphous Solid Dispersions

Greco, Stéphanie; Authelin, Jean‐René; Leveder, Caroline; Segalini, Audrey

doi:10.1007/s11095-012-0717-5

Cited by 62 publications

(60 citation statements)

References 36 publications

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“…The high energy state of the amorphous form confers higher solubility and improves bioavailability through increasing dissolution. Thus, the application of amorphous phases has been the subject of very intensive investigations in the pharmaceutical field [16,17,18]. However, the thermodynamic instability of this amorphous state is generally associated with the high energy state and may lead to unacceptable physical changes, such as recrystallization during storage [19,20].…”

Section: Introductionmentioning

confidence: 99%

Characterization and Stability of Tanshinone IIA Solid Dispersions with Hydroxyapatite

Wang

Huo

et al. 2013

Materials

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Solid dispersions of tanshinone IIA (TanIIA) using hydroxyapatite (HAp) as the dispersing carrier (TanIIA-HAp SDs) were prepared by the solvent evaporation method. The formed solid dispersions were characterized by scanning electron microscopy (SEM), differential scanning calorimetry analysis (DSC), X-ray powder diffraction (XRPD) and Fourier transforms infrared (FTIR) spectroscopy. The in vitro dissolution rate and the stability of TanIIA-HAp SDs were also evaluated. DSC and XRPD showed that TanIIA was changed from a crystalline to an amorphous form. FTIR suggested the presence of interactions between TanIIA and HAp in solid dispersions. The result of an in vitro dissolution study showed that the dissolution rate of TanIIA-HAp SDs was nearly 7.11-folds faster than free TanIIA. Data from stability studies for over one year of TanIIA-HAp SDs performed under room temperature revealed no significant differences in drug content and dissolution behavior. All these results indicated that HAp may be a promising carrier for improving the oral absorption of TanIIA.

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Section: Introductionmentioning

confidence: 99%

Characterization and Stability of Tanshinone IIA Solid Dispersions with Hydroxyapatite

Wang

Huo

et al. 2013

Materials

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“…[4041] Amorphous drugs formulated as SDs have a tendency to recrystallize during long-term storage, eventually resulting in impaired dissolution profiles. Temperature and humidity during storage have been reported to influence the stability of the amorphous forms of drugs.…”

Section: Resultsmentioning

confidence: 99%

Enhanced dissolution and stability of Tanshinone IIA base by solid dispersion system with nano-hydroxyapatite

Jiang¹,

Zhang²,

Saiyan³

et al. 2014

Phcog Mag

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Background:Tanshinone IIA (TSIIA) exhibits a variety of cardiovascular effects; however, it has low solubility in water. The preparation of poorly soluble drugs for oral delivery is one of the greatest challenges in the field of formulation research. Among the approaches available, solid dispersion (SD) technique has proven to be one of the most commonly used these methods for improving dissolution and bioavailability of drugs, because of its relative simplicity and economy in terms of both preparation and evaluation.Objective:This study was aimed at investigating the dissolution behavior and physical stability of SDs of TSIIA by employing nano-hydroxyapatite (n-HAp).Materials and Methods:The TSIIA SDs was prepared to use a spray-drying method. First, an in vitro dissolution test was performed to assess dissolution characteristics. Next, a set of complementary techniques (differential scanning calorimetry, scanning electron microscopy, X-ray powder diffraction, and Fourier transform infrared spectroscopy) was used to monitor the physicochemical properties of the SDs. The SDs was stored at 40°C/75% relative humidity for 6 months, after which their stability was assessed.Results:TSIIA dissolution remarkably improved because of the formulation of the SDs with n-HAp particles. Comparisons with the corresponding physical mixtures revealed changes in the SDs and explained the formation of the amorphous phase. In the stability test, virtually no time-dependent decrease was observed in either in vitro drug dissolution or drug content.Conclusion:SD formulation with n-HAp may be a promising approach for enhancing the dissolution and stability of TSIIA.

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“…If T g ≥ T s , it is presumed that the sample can be stored stably at T s for a long period of time [21]. Note that the T g of a sample depends on its composition and water content, as well as the glass-forming characteristics of the cryo-/lyoprotectant agents added to the sample.…”

Section: Resultsmentioning

confidence: 99%

Isothermal vitrification methodology development for non-cryogenic storage of archival human sera

et al. 2013

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Biorepositories worldwide collect human serum samples and store them for future research. Currently, hundreds of biorepositories across the world store human serum samples in refrigerators, freezers, or liquid nitrogen without following any specific cryopreservation protocol. This method of storage is both expensive and potentially detrimental to the biospecimens. To decrease both cost of storage and the freeze/thaw stresses, we explored the feasibility of storing archival human serum samples at non-cryogenic temperatures using isothermal vitrification. When biospecimens are vitrified, biochemical reactions can be stopped, the specimen ceases to degrade, and macromolecules can be stabilized without requiring cryogenic storage. In this study, 0.2, 0.4, or 0.8 M trehalose; 0, 0.005 or 0.01 M dextran; and 0 or 10% (v/v) glycerol was added to human serum samples. The samples were either dried diffusively as sessile droplets or desiccated under vacuum after they are adsorbed onto glass microfiber filters. The glass transition temperatures (Tg) of the desiccated samples were measured by temperature-ramp Fourier Transform Infrared (FTIR) spectroscopy. Sera samples vitrified at 4 ± 2 °C when 0.8 M trehalose and 0.01 M dextran were added and the samples were vacuum dried for two hours. Western immunoblotting showed that vitrified serum proteins were minimally degraded when stored for up to one month at 4 °C. About 80% of all proteins were recovered after storage at 4 °C on glass microfiber filters, and recovery did not decrease with storage time. These results demonstrated the feasibility of long-term storage of vitrified serum at hypothermic (and non-cryogenic) temperatures.

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A Practical Method to Predict Physical Stability of Amorphous Solid Dispersions

Abstract: The proposed methodology can be used as a stress program to predict long-term stability from a relatively short observation period and to design appropriate temperature and humidity conditions for long-term storage to prevent crystallization.

Cited by 62 publications

References 36 publications

Characterization and Stability of Tanshinone IIA Solid Dispersions with Hydroxyapatite

Characterization and Stability of Tanshinone IIA Solid Dispersions with Hydroxyapatite

Enhanced dissolution and stability of Tanshinone IIA base by solid dispersion system with nano-hydroxyapatite

Isothermal vitrification methodology development for non-cryogenic storage of archival human sera

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