Establishment of new preparation method for solid dispersion formulation of tacrolimus

Yamashita, Kazunari; Nakate, Toshiomi; Okimoto, Kazuto; Ohike, Atsuo; Tokunaga, Yuji; Ibuki, Rinta; Higaki, Kazutaka; Kimura, Takeshi

doi:10.1016/j.ijpharm.2003.07.010

Cited by 303 publications

(208 citation statements)

References 26 publications

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“…Numerous technologies have been widely attempted to prepare SDs, such as melting method, solvent-evaporation method and solvent-wetting method (Yamashita et al, 2003;Miller et al, 2007;Joe et al, 2010). However, there are some limitations of using these methods such as the degradation of drug due to the requirement of relatively high preparation temperatures, and the toxicity associated with the use of organic solvents.…”

Section: Introductionmentioning

confidence: 99%

Enhanced dissolution and oral bioavailability of valsartan solid dispersions prepared by a freeze-drying technique using hydrophilic polymers

Xie

Cao

et al. 2014

Drug Delivery

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This study aimed to improve the dissolution rate and oral bioavailability of valsartan (VAL), a poorly soluble drug using solid dispersions (SDs). The SDs were prepared by a freeze-drying technique with polyethylene glycol 6000 (PEG6000) and hydroxypropylmethylcellulose (HPMC 100KV) as hydrophilic polymers, sodium hydroxide (NaOH) as an alkalizer, and poloxamer 188 as a surfactant without using any organic solvents. In vitro dissolution rate and physicochemical properties of the SDs were characterized using the USP paddle method, differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and Fourier transform-infrared (FT-IR) spectroscopy, respectively. In addition, the oral bioavailability of SDs in rats was evaluated by using VAL (pure drug) as a reference. The dissolution rates of the SDs were significantly improved at pH 1.2 and pH 6.8 compared to those of the pure drug. The results from DSC, XRD showed that VAL was molecularly dispersed in the SDs as an amorphous form. The FT-IR results suggested that intermolecular hydrogen bonding had formed between VAL and its carriers. The SDs exhibited significantly higher values of AUC 0-24 h and C max in comparison with the pure drug. In conclusion, hydrophilic polymer-based SDs prepared by a freeze-drying technique can be a promising method to enhance dissolution rate and oral bioavailability of VAL.

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Section: Introductionmentioning

confidence: 99%

Enhanced dissolution and oral bioavailability of valsartan solid dispersions prepared by a freeze-drying technique using hydrophilic polymers

Xie

Cao

et al. 2014

Drug Delivery

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“…26 Amounts of drug compositions were weighed out corresponding to~25 times the aqueous solubility of repaglinide (~53 mg repaglinide in each sample). The dissolution medium was the same as described above (eg, 50 mM citric acid/100 mM sodium phosphate dibasic pH 4.5), using 100 mL of medium for this procedure.…”

Section: Dissolution Performed Under Supersaturation Conditionsmentioning

confidence: 99%

Rapidly dissolving repaglinide powders produced by the ultra-rapid freezing process

et al. 2007

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The objective of the study was to produce rapidly dissolving formulations of the poorly water-soluble drug repaglinide using an innovative new technology, ultra-rapid freezing (URF), and to investigate the influence of excipient type on repaglinide stability. Repaglinide compositions containing different types and levels of excipients and different drug potencies (50%-86%) were produced by the URF technology. Repaglinide/excipient solutions were frozen on a cryogenic substrate, collected, and lyophilized to form a dry powder. Surfactants, including sodium dodecyl sulfate, and alkalizing agents such as diethanolamine (DEA) and tromethamine (TRIS) were incorporated into the compositions. Forced degradation of repaglinide was conducted under stressed conditions (eg, elevated temperature, exposure to peroxide) to determine the stability of the drug in such environments. The solubility of repaglinide increased as a function of increasing pH; therefore, incorporation of an alkalizing agent into the URF formulations increased the drug's solubility. Drug instability resulted when the drug was exposed to pH values above 9.0. URF formulations containing alkalizing agents showed no degradation or spontaneous recrystallization in the formulation, indicating that increased stability was afforded by processing. URF processing created nanostructured drug/excipient particles with higher dissolution rates than were achieved for unprocessed drug. Alkalizing agents such as TRIS and DEA, present at levels of 25% to 33% wt/wt in the formulations, did not cause degradation of the drug when processed using URF. URF processing, therefore, yielded fast-dissolving formulations that were physically and chemically stable, resistant to alkali degradation or spontaneous recrystallization in the formulation.

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“…Furthermore, no energy is required to break up the crystal lattice of a drug during dissolution process (Taylor and Zografi, 1997), and drug solubility and wettability may be increased by surrounding hydrophilic carriers (Craig, 2002). The methods used to prepare solid dispersions include the melting method, the solvent method and the solvent wetting method (Leuner and Dressman, 2000;Yamashita et al, 2003). However, the melting method and the solvent method have some limitations.…”

Section: Introductionmentioning

confidence: 99%

Physicochemical Characterization of Physical Mixture and Solid Dispersion of Diclofenac Potassium with Mannitol.

Han¹,

Faudone²,

Zitto³

et al. 2017

J App Pharm Sci

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Diclofenac potassium is an anti-inflammatory agent classified as a class II drug as per the biopharmaceutical classification system (BCS). The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. There are several techniques to enhance the dissolution of poorly soluble drugs. Methods available include salt formation, micronization and addition of solvent or surface active agents. The objective of the present work is to improve the dissolution profile of diclofenac potassium by formation of a physical mixture and a solid dispersion with mannitol. The solid dispersion was prepared by solvent method using ethanol/water. As diclofenac potassium melts with decomposition, the compatibility study with mannitol was done with the acid form by differential scanning calorimetry (DSC). The dissolution properties and physicochemical properties of diclofenac potassium:mannitol physical mixture and solid dispersion were investigated by Powder X-ray Diffraction (PXRD), Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and dissolution test. This study shows that the dissolution rate of diclofenac potassium can be enhanced considerably by formulating it with mannitol, as a physical mixture or as a solid dispersion although crystallinity was maintained.

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Establishment of new preparation method for solid dispersion formulation of tacrolimus

Cited by 303 publications

References 26 publications

Enhanced dissolution and oral bioavailability of valsartan solid dispersions prepared by a freeze-drying technique using hydrophilic polymers

Enhanced dissolution and oral bioavailability of valsartan solid dispersions prepared by a freeze-drying technique using hydrophilic polymers

Rapidly dissolving repaglinide powders produced by the ultra-rapid freezing process

Physicochemical Characterization of Physical Mixture and Solid Dispersion of Diclofenac Potassium with Mannitol.

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