Solid dispersions: a strategy for poorly aqueous soluble drugs and technology updates

Alam, Mohammad Mumtaz; Ali, Raisuddin; Al-Jenoobi, Fahad I.; Al-Mohizea, Abdullah M.

doi:10.1517/17425247.2012.732064

Cited by 103 publications

(54 citation statements)

References 117 publications

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“…According to the biopharmaceutics classification system (BCS) classification, the drugs of class II and IV have low solubility (1). The solubility and bioavailability of poorly soluble drugs has been improved by several techniques including particle size reduction, complex formation, nanotechnologies, solid dispersion, polymeric micelle, salt formation, prodrugs, polymorphs, and solvates (2)(3)(4). Each of these techniques has its pros and cons.…”

Section: Introductionmentioning

confidence: 99%

“…Each of these techniques has its pros and cons. Different solubilization techniques may have different influence on the solubility and other physicochemical characteristics of the same drug molecule (3,4). So, there is no universal technology which can be used in all cases of solubility enhancement, while preserving the safety and efficacy of drugs.…”

Section: Introductionmentioning

confidence: 99%

“…Among these techniques of solubility enhancement, solid dispersion seems to be an easy and simple technique. In solid dispersion, a poorly soluble drug substance is dispersed in a quickly water soluble solid carrier matrix (4). These water soluble carriers include mannitol, lactose, urea, polyethylene glycol, Gelucire, poloxamer 127, etc.…”

Section: Introductionmentioning

confidence: 99%

“…Binary or ternary solid dispersions have been reported to be more successful since they provide physical stability and prevents recrystallization of drug (4,(6)(7)(8)(9). Use of surfactant with carrier enhances the wettability and solubilization of the drug and also assists in drug release (10)(11)(12).…”

Section: Introductionmentioning

confidence: 99%

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Effervescence Assisted Fusion Technique to Enhance the Solubility of Drugs

et al. 2015

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Abstract. The solubility of five poorly soluble drugs was enhanced by using an effervescence assisted solid dispersion (EASD) technique. EASDs were prepared by using modified fusion method. Drug and hydrophilic carrier were melted, and in this molten mixture, effervescence was generated by adding effervescence couple comprising organic acid (citric acid) and carbonic base (sodium bicarbonate). Solubility of drug powders, solid dispersions, and EASDs was determined at 25°C using shake flask method. Atorvastatin calcium, cefuroxime axetil, clotrimazole, ketoconazole, and metronidazole benzoate were estimated using a spectrophotometer at 246, 280, 260, 230, and 232 nm (λ max ), respectively. Solubility of atorvastatin calcium (from 100 to 345 μg/ml), cefuroxime axetil (from 441 to 1948 μg/ml), clotrimazole (from 63 to 677 μg/ml), ketoconazole (from 16 to 500 μg/ml), and metronidazole benzoate (from 112 to 208 μg/ml) in EASDs was enhanced by 3.45-, 4.4-, 10.7-, 31.2-, and 1.8-fold, respectively. Scanning electron micrographs of drug powder, solid dispersion, and EASDs were compared. Scanning electron micrographs of EASDs showed a uniform distribution of drug particles in the carrier matrix. Morphology (size and shape) of cefuroxime axetil particles was altered in solid dispersion as well as in EASD. EASDs showed better solubility enhancement than conventional solid dispersions. The present technique is better suitable for drugs having a low melting point or melt without charring. Effervescence assisted fusion technique of preparing solid dispersions can be employed for enhancing solubility, dissolution, and bioavailability of poorly soluble drugs.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Effervescence Assisted Fusion Technique to Enhance the Solubility of Drugs

et al. 2015

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“…Soluplus ® has excellent potential to form solid solutions. [15][16][17][18][19] In this study, we examined whether the water solubility and the antitumor activity of sapacitabine both in vitro and in vivo increased on using Soluplus ® .…”

Section: Improvement Of the Antitumor Activity Of Poorly Soluble Sapamentioning

confidence: 99%

Improvement of the Antitumor Activity of Poorly Soluble Sapacitabine (CS-682) by Using Soluplus® as a Surfactant

Obata

Suzuki

Ogawa

et al. 2014

Biological & Pharmaceutical Bulletin

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Sapacitabine (CS-682 or CYC682; 1-[2-C-cyano-2-deoxy-β-D-arabino-pentfuranosyl]N4-palmitoyl cytosine), a novel antitumor 2′-deoxycytidine analogue, shows a marked reduction in the water solubility because of the fatty acid side chain on the N4 group of the cytosine moiety. Poor water solubility is one of the important reasons why sapacitabine does not exert maximum antitumor activity. Therefore, we attempted to improve the water solubility of sapacitabine using a novel surfactant, Soluplus ® , which consisted of a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. In this study, we examined whether Soluplus ® increased the water solubility and an antitumor activity of sapacitabine. The cytotoxicity of Soluplus ® alone was lower than that of Tween 80 and Kolliphor ® D-α-tocopherylpolyethylene glycol 1000 succinate (TPGS). The water solubility and the chemosensitivity of sapacitabine against several tumor cell lines to sapacitabine markedly increased upon using Soluplus ® . In addition, the potential of Soluplus ® including sapacitabine in increasing the antitumor activity was compared with sapacitabine alone in vivo. Although the total dose in the experimental period was considerably lower than the effective dose of sapacitabine alone, the life span of mice treated with sapacitabine containing 40 mg/mL Soluplus ® increased by 150%. If Soluplus ® was used as the solubilizing agent in clinical trials of sapacitabine, a low administration dose was appeared to require, and thus side effects might be prevented.

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