Preparation and characterization of emulsified solid dispersions containing docetaxel

Chen, Ying; Shi, Qiongzhi; Chen, Zhiyu; Zheng, Jianling; Xu, Hengjun; Li, Jiazhi; Hong, Liu

doi:10.1007/s12272-011-1111-2

Cited by 14 publications

(14 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The temperatures ranged from 2°C to 60°C and the relative humidity varied between 0% and 100%. The duration also varied significantly, with stability studies lasting from 24 h to two years (73,74,81,82,84,86,88,92,93,104,105,109,110,113,115,116,118,120,123,124,126,127,129,130,132,134,135,139,143,146,149,153,158,166,169,172,175,176). While most of the studies did not mention the container used for the physical stability test, a few specified, for example, whether a closed or open container was used (88,92,113,123,132,146).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

“…Ninety-two of the 101 studies reported solubility and dissolution studies (71–74,77–79,81–92,95,97–107,109–111,113–119,121,123,124,126–133,135–139,141–154,156,157,160,161,166,168–176). The USP in vitro dissolution type II apparatus was the most commonly used instrument (67%), followed by the USP type I apparatus (6%), while the remaining 27% used various other apparatuses, including modified versions of the USP type I only (148) or paired with confocal Raman microscopy (98), USP types I and II apparatus (72), USP type IV (152), closed loop of USP types II and IV (152), a perspex flow cell (73,142), a rotary mixer (131), a Chinese pharmacopoeia type III apparatus (118), an in-house miniaturized USP type II apparatus (175), Sirius T3 apparatus (146), μFLUX dissolution-permeation apparatus (141), Raman UV-Vis flow cell system (99), a centrifuge (88), high throughput screening using a 96-well plate (82,115,157), Wood’s apparatus (99,137), an orbital shaking incubator (156), and another shake-flask method (171) (Fig. 6).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

See 1 more Smart Citation

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

View full text Add to dashboard Cite

The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

show abstract

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

View full text Add to dashboard Cite

show abstract

“…The results showed a 134-fold increase in dissolution rate for SD containing 30/70 w / w fenofibrate/ poloxamer 407. Surfactants are also used in preparation of SD of poorly soluble anticancer drugs such as docetaxel [76], flutamide [77], and lapatinib [78].…”

Section: Solid Dispersionsmentioning

confidence: 99%

“…In vitro release of the drug from the SD was 4.35-fold greater than that of the pure drug after 2.5 h. In addition, the oral BA of the drug from the SD was higher than that of the conventional drug as determined by AUC (4.8-fold) and C max (13.1-fold). The solvent evaporation method has often been used to improve solubility of poorly water-soluble anticancer drugs such as paclitaxel [133], docetaxel [76], and others (Table 3). For example, the solubility and dissolution of emulsified SD of docetaxel at 2 h were 34.2- and 12.7-fold greater, respectively, compared to those of the conventional drug [76].…”

Section: Solid Dispersionsmentioning

confidence: 99%

Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

et al. 2019

View full text Add to dashboard Cite

Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic anticancer drugs) based on effectiveness and safety profile. Biologic drugs are administered by intravenous (IV) injection due to their large molecular weight, while small molecule drugs are preferentially administered by gastrointestinal route. Even though IV injection is the fastest route of administration and ensures complete bioavailability, this route of administration causes patient inconvenience to visit a hospital for anticancer treatments. In addition, IV administration can cause several side effects such as severe hypersensitivity, myelosuppression, neutropenia, and neurotoxicity. Oral administration is the preferred route for drug delivery due to several advantages such as low cost, pain avoidance, and safety. The main problem of NCEs is a limited aqueous solubility, resulting in poor absorption and low bioavailability. Therefore, improving oral bioavailability of poorly water-soluble drugs is a great challenge in the development of pharmaceutical dosage forms. Several methods such as solid dispersion, complexation, lipid-based systems, micronization, nanonization, and co-crystals were developed to improve the solubility of hydrophobic drugs. Recently, solid dispersion is one of the most widely used and successful techniques in formulation development. This review mainly discusses classification, methods for preparation of solid dispersions, and use of solid dispersion for improving solubility of poorly soluble anticancer drugs.

show abstract

“…However, it also requires the therapeutic dose of API to be low. For instance, Chen et al prepared emulsified SDs containing docetaxel by three approaches, i.e., melting method, solvent-melting method and solvent method [ 71 ]. It was shown that the dissolution of docetaxel from SDs prepared by the solvent-melting method was higher than that prepared by the melting method.…”

Section: Solid Dispersion Techniquementioning

confidence: 99%

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

et al. 2018

View full text Add to dashboard Cite

Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

show abstract

Preparation and characterization of emulsified solid dispersions containing docetaxel

Cited by 14 publications

References 33 publications

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

Overview of the Manufacturing Methods of Solid Dispersion Technology for Improving the Solubility of Poorly Water-Soluble Drugs and Application to Anticancer Drugs

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

Contact Info

Product

Resources

About