Effect of Characteristics of Compounds on Maintenance of an Amorphous State in Solid Dispersion with Crospovidone

Shibata, Yusuke; Fujii, Makiko; Kokudai, Makiko; Noda, Shinobu; Okada, Hideko; Kondoh, Masuo; Watanabe, Yoshihisa

doi:10.1002/jps.20794

Cited by 31 publications

(16 citation statements)

References 22 publications

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“…These results are in agreement with previous reports. [4][5][6] In the case of IM-Pmix-sieved, the heat of fusion was almost the same as for IM-Pmix. After 120 min, however, the heat of fusion was slightly smaller than that of IM-Pmix, indicating that more IM crystals had become amorphous.…”

Section: Resultsmentioning

confidence: 77%

“…When preparing SDs by these methods, difficulties can arise with obtaining the appropriate dosage forms and maintaining the amorphous state. 3) To solve these problems, Fujii et al 4) and Shibata et al 5,6) studied preparation of SDs using crospovidone as a carrier. Crospovidone is an insoluble polymer which does not melt upon heating, allowing it to remain a powder during the SD preparation process.…”

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confidence: 99%

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Effect of Particle Size of Drug on Conversion of Crystals to an Amorphous State in a Solid Dispersion with Crospovidone

Sugamura

Fujii

Nakanishi

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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The effect of particle size on amorphization of drugs in a solid dispersion (SD) was investigated for two drugs, indomethacin (IM) and nifedipine (NP). The SD of drugs were prepared in a mixture with crospovidone by a variety of mechanical methods, and their properties investigated by particle sizing, thermal analysis, and powder X-ray diffraction. IM, which had an initial particle size of 1 m mm and tends to aggregate, was forced through a sieve to break up the particles. NP, which had a large initial particle size, was jet-milled. In both cases, reduction of the particle size of the drugs enabled transition to an amorphous state below the melting point of the drug. The reduction in particle size is considered to enable increased contact between the crospovidone and drug particles, increasing interactions between the two compounds.

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Section: Resultsmentioning

confidence: 77%

mentioning

confidence: 99%

Effect of Particle Size of Drug on Conversion of Crystals to an Amorphous State in a Solid Dispersion with Crospovidone

Sugamura

Fujii

Nakanishi

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…It should be also noted that several studies on SDs of this antibiotic have previously been reported in literature (17)(18)(19)(20) and in addition, a commercially available SD example of this drug is known [Gris-polyethylene glycol (PEG), 125 or 250 mg of active ingredient, Pedinol Pharmacal Inc (7)]. In particular, in these works, the following aspects have been investigated: the factors influencing "solid solubility" and phase separation kinetics of Gris-PVP SD (17), the factors influencing the stability and dissolution properties of Gris-PVP SD (19) and the effect of hydrogen bonding properties on the maintenance of an amorphous state of Gris-CrosPVP SD (18).…”

Section: Introductionmentioning

confidence: 95%

Griseofulvin/Carrier Blends: Application of Partial Least Squares (PLS) Regression Analysis for Estimating the Factors Affecting the Dissolution Efficiency

et al. 2011

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Abstract. The main aim of the present study was to estimate the carrier characteristics affecting the dissolution efficiency of Griseofulvin (Gris) containing blends (BLs) using partial least squares (PLS) regression analysis. These systems were prepared at three different drug/carrier weight ratios (1/5, 1/10, and 1/20) by the solvent evaporation method, a well-established method for preparing solid dispersions (SDs). The carriers used were structurally different including polymers, a polyol, acids, bases and sugars. The BLs were characterised at the solid-state by spectroscopic (Fourier transform infrared spectroscopy), thermoanalytical (differential scanning calorimetry) and X-ray diffraction studies and their dissolution behaviours were quantified in terms of dissolution efficiencies (log DE/DE Gris ). The correlation between the selected descriptors, including parameters for size, lipophilicity, cohesive energy density, and hydrogen bonding capacity and log DE/DE Gris (i.e., DE and DE Gris are the dissolution efficiencies of the BLs and the pure drug, respectively) was established by PLS regression analysis. Thus two models characterised by satisfactory coefficient of determination were derived. The generated equations point out that aqueous solubility, density, lipophilic/hydrophilic character, dispersive/polar forces and hydrogen bonding acceptor/donor ability of the carrier are important features for dissolution efficiency enhancement. Finally, it could be concluded that the correlations developed may be used to predict at a semiquantitative level the dissolution behaviour of BLs of other essentially neutral drugs possessing hydrogen bonding acceptor groups only.

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“…[27] Shibata et al reported that all compounds containing hydrogen bond donor functional group interacted with amide carbonyl group of crospovidone and were shown to be stable for 6 months. [28] Compounds without H-bond donor group could not maintain amorphous state and underwent recrystallization. Another factor that affect the release of drug from the system is the ratio of drug to polymer in the solid dispersion.…”

Section: Interaction Between Drug and Polymermentioning

confidence: 99%

“…While those without hydrogen bond donor groups could not maintain an amorphous state and underwent recrystallization within 1 month. [28] In another study by Dhumal et al, compression stabilizer such as carrageenan was used. Solid dispersion of celecoxib prepared as co-precipitate with PVP was found to be stable for 3 years using carrageenan.…”

Section: Polymorph and Soluble Prodrugsmentioning

confidence: 99%

Solid Dispersion: An Alternative Technique for Bioavailability Enhancement of Poorly Soluble Drugs

Sinha

Baboota

Ali

et al. 2009

Journal of Dispersion Science and Technology

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Formulation of solid dispersion in water-soluble carriers has been widely researched over the past four decades for solubility and related bioavailability enhancement. Despite 40 years of active research, there has not been much products in market based on this technique. The main reason for this being stability and scale up problems associated with this method, as reported by several authors. Strategies used for overcoming these problems and factors affecting formation of solid dispersion such as glass transition temperature and interaction of drug with polymer have been dealt conceptually in this review. The advent of surface-active carriers such as Gelucires, Poloxamers, and lipid-based carriers has given a new dimension for the successful development of solid dispersions by combating the problems associated with stability and also giving products with enhanced dissolution rate. Therefore, the article also discusses properties of such carriers that are being unraveled lately for formulation of solid dispersion. Characterization of solid dispersion to detect the change from crystalline to amorphous states and vice versa is an important tool for its formulation and determination of stability; thus, all the methods that are available for characterizations are discussed in this article with emphasis on the principle of the technique and its application.

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Effect of Characteristics of Compounds on Maintenance of an Amorphous State in Solid Dispersion with Crospovidone

Cited by 31 publications

References 22 publications

Effect of Particle Size of Drug on Conversion of Crystals to an Amorphous State in a Solid Dispersion with Crospovidone

Effect of Particle Size of Drug on Conversion of Crystals to an Amorphous State in a Solid Dispersion with Crospovidone

Griseofulvin/Carrier Blends: Application of Partial Least Squares (PLS) Regression Analysis for Estimating the Factors Affecting the Dissolution Efficiency

Solid Dispersion: An Alternative Technique for Bioavailability Enhancement of Poorly Soluble Drugs

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