Lactose as a Low Molecular Weight Carrier of Solid Dispersions for Carbamazepine and Ethenzamide.

Hirasawa, Noriyuki; Okamoto, Hirokazu; Danjo, Kazumi

doi:10.1248/cpb.47.417

Cited by 44 publications

(16 citation statements)

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“…For other co-crystals of ethenzamide, see: Aitipamula et al (2009b); Moribe et al (2004). For related information on the drug activity of ethenzamide, see: Hirasawa et al (1999). For the crystal structure of ethenzamide, see: Pagola & Stephens (2009).…”

Section: Related Literaturementioning

confidence: 99%

Bis[2-(cyclopropyliminomethyl)-5-methoxyphenolato]zinc(II)

Bai¹

2010

Acta Cryst E

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Section: Related Literaturementioning

confidence: 99%

Bis[2-(cyclopropyliminomethyl)-5-methoxyphenolato]zinc(II)

Bai¹

2010

Acta Cryst E

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“…Yamashita et al 11) prepared the solid dispersion of tacrolimus using PEG, PVP, and hydroxypropylmethylcellulose (HPMC). We reported that naproxen-a-lactose monohydrate solid dispersions, 12,13) prepared using melting methods, supported the existence of a high-energy amorphous drug phase in systems containing more than 50% alactose monohydrate. The dissolution data suggested that the dissolution rate of this phase was 7-20-fold greater than the crystalline drug.…”

mentioning

confidence: 94%

Particle Design of Three-Component System for Sustained Release Using a 4-Fluid Nozzle Spray-Drying Technique

Chen

Takahashi

Okamoto

et al. 2006

CHEMICAL & PHARMACEUTICAL BULLETIN

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Various methods to improve the dissolution of poor watersoluble drugs have been reported. 1,2) The formation of solid dispersion using a carrier is one such method. Some researchers have proposed that increased drug dissolution rates reflect the formation of a high-energy amorphous drug phase.3) Several water-soluble polymer carrier systems, such as polyethylene glycol (PEG), [4][5][6] polyvinylpyrrolidone (PVP), 7) and hydroxypropylcellulose (HPC), 8) have been used in fast-release preparations. The mechanisms of interaction between drug and carrier in solid dispersions have also been studied. Solid dispersions of nifedipine and a carrier polymer such as hydroxypropylmethylcellulose acetate succinate (HPMCAS) were prepared by a solvent method. 9) Emara et al. 10) improved the dissolution of nifedipine prepared by a fusion method. Yamashita et al. 11) prepared the solid dispersion of tacrolimus using PEG, PVP, and hydroxypropylmethylcellulose (HPMC). We reported that naproxen-a-lactose monohydrate solid dispersions, 12,13) prepared using melting methods, supported the existence of a high-energy amorphous drug phase in systems containing more than 50% alactose monohydrate. The dissolution data suggested that the dissolution rate of this phase was 7-20-fold greater than the crystalline drug.Recently, a spray-drying technique yielded an amorphous form of crystalline drugs, such as cimetidine, that becomes amorphous when spray-dried with Cht, as reported by He et al. 14) This indicates that solid dispersion was formed when cimetidine was dispersed in Cht molecules by spray-drying. Corrigan et al. 15) tried to make an amorphous drug by spraydrying using PVP as a carrier. The dissolution rate of the drug commonly quickens when a solid dispersion is formed by using a polymer as a carrier. However, few studies have investigated the slow release of the drug after the formation of a solid dispersion using spray-drying. Shaikh et al. 16) performed a spray-drying technique using Act and ethylcellulose (EC) and tried to achieve a sustained release of Act. Their results demonstrated the possibility of forming solid dispersion by dispersing Act with a spray-drying technique with EC molecules in a molecular state. They concluded that the sustained release of Act in this solid dispersion was caused by an increase in EC viscosity.In this study, we designed composite particles to the sustained release of Act by changing the mixture ratio of Act and carriers (Cht and HPMCP). Sustained release in the digestive tract was attempted in this formation by using Cht and HPMCP as carriers and solid dispersions between the carriers and drugs. Cht dissolved after it formed a gel 17,18) in the acid solution, and HPMCP was insoluble in the acid solution. However, HPMCP dissolved in the alkaline solution, and Cht was insoluble. Sustained release of the drug was tried using such dissolution properties as the pH of the carrier. Then the particle design of a three-component system for the sustained release of the drug was tried by forming s...

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“…[1][2][3][4][5] Phosphatidylcholine and lactose have been tested as carriers, 6,7 and the twinscrew extruder method has been studied as a new technique for solid dispersion. 8 Solid dispersion has also been applied for the controlled release of drugs.…”

Section: Introductionmentioning

confidence: 99%

Controlled release of drug via methylcellulose-carboxyvinylpolymer interpolymer complex solid dispersion

2005

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The purpose of this research was to examine the controlled release of phenacetin (PHE) from solid dispersion by the formation of an interpolymer complex between methylcellulose (MC) and carboxyvinylpolymer (CP). The PHE/ polymer composition ratio was fixed at 20:80 (w/w) in the solid dispersion. The effect of the MC/CP ratio and molecular weight of MC on the PHE release was studied. The release of PHE from the solid-dispersion granules depended on the MC/CP ratio, with a ratio of 50:50 giving the lowest rate of release. In aqueous solution, this MC/CP ratio resulted in the lowest transmittance, suggesting a maximal extent of interpolymer complex formation between MC and CP. Furthermore, at a MC/CP ratio of 50:50, the release of PHE from the solid dispersion granules decreased as the molecular weight of the MC increased, reaching a plateau at molecular weights 180,000. The contributions of diffusion and polymer relaxation to PHE release increased as the molecular weight of the MC increased. This study shows that it is feasible to control the release of PHE from MC-CP solid dispersion granules by modulating complex formation between MC and CP, which can be accomplished by altering the MC/CP ratio and the molecular weight of MC.

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Lactose as a Low Molecular Weight Carrier of Solid Dispersions for Carbamazepine and Ethenzamide.

Cited by 44 publications

References 1 publication

Bis[2-(cyclopropyliminomethyl)-5-methoxyphenolato]zinc(II)

Bis[2-(cyclopropyliminomethyl)-5-methoxyphenolato]zinc(II)

Particle Design of Three-Component System for Sustained Release Using a 4-Fluid Nozzle Spray-Drying Technique

Controlled release of drug via methylcellulose-carboxyvinylpolymer interpolymer complex solid dispersion

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