Formulation Development of Solid Dispersions of Bosentan using Gelucire 50/13 and Poloxamer 188

Panda, Tapan Kumar; Das, Debajyoti; Panigrahi, Lalatendu

doi:10.7324/japs.2016.60904

Cited by 22 publications

(9 citation statements)

References 18 publications

(17 reference statements)

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“…Several surfactants such as Inulin [69,70], inutec [70], poloxamer 407 [71], Gelucire 44/14 [72], and Compritol 888 ATO [73] are used in preparation of SD. In a study by Panda et al [74], Gelucire 50/13 and poloxamer 188 were used in the development of a bosentan SD formulation to improve the solubility and dissolution of this drug. The results showed that the solubility of bosentan from the SD formulation increased 8- and 10-fold when using Gelucire 50/13- and poloxamer 188-based SDs, respectively, in comparison with that of the pure drug.…”

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

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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.

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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

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“…As a result, they tend to have a poor flow, poor compressibility, and hard to pulverize [99,100]. To resolve these problems, inert material with good flow and compressibility should be used to absorb the dispersion on its surface [101]. Moreover, adsorption carriers not only prevent the crystal growth due to confined space within the pores of carriers but also stabilize the drug in the TSD by various chemical interactions [102].…”

Section: Adsorbentsmentioning

confidence: 99%

Fundamental Aspects of a Third Component Used in Ternary Solid Dispersion: A Review

Varshini

Rajesh

2021

Int J App Pharm

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Ternary solid dispersion (TSD) is one of the promising approaches used in recent studies to address the issues encountered by poorly water-soluble drugs. The binary solid dispersion (BSD) with the drug and the single polymer is not sufficient to satisfy all the criteria such as improved solubility, dissolution, stability, supersaturation, and recrystallization inhibition. Hence, the TSD with the third component/ternary agent aids in overcoming the limitations, thereby enhancing the solubility and bioavailability to a greater extent when compared to the BSD. Excipients that can be used as a third component includes surfactants, pH modulator, polymer and adsorbents. All these excipients have distinct benefits in improving the efficiency of the final dosage form. However, care must be taken in selecting suitable excipients for the research. This review highlights the impact of these excipients in improving the formulation complications and the therapeutic potential of the TSD.

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“…Poloxamers are nonionic surfactant, polyoxyethylenepolypropylene block copolymer consists of hydrophilic core (ethylene oxide) and hydrophobic core (polypropylene oxide) blocks arranged in a triblock structure resulting in an amphiphilic copolymer 17 . Poloxamers are hydrophilic non-ionic surfactant used mainly as solubilizing agents, wetting agents and used for enhancing the solubility and bioavailability of poorly soluble drugs [18][19] .…”

Section: Introductionmentioning

confidence: 99%

Preparation, Characterization and Dissolution Enhancement of Dihydroartemisinin Microparticles

Pm¹,

Ss²,

Naikwade³

2019

Int Res J Pharm

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The objective of the present study was to prepare a Dihydroartemisinin microparticles using spray drying method to enhance the solubility and dissolution rate which will help for improvement of oral bioavailability. Dihydroartemisinin is the active metabolite of artemisinin compound and a drug of choice for treatment of malaria. Dihydroartemisinin has poor aqueous solubility, incompletely absorbed after oral intake due to poor dissolution characteristics in the intestinal fluid which limits its application. To address these issues, spray dried microparticles of Dihydroartemisinin were prepared using Poloxamer 188, non-ionic surfactant with different ratios of drug and carrier. Based on results of solubility study, spray dried microparticles formulation with highest aqueous solubility was analyzed for Fourier transform infrared spectroscopy, X-ray powder diffraction and Differential scanning calorimetry study. Spray dried microparticles evaluated for determination of percent yield, solubility, drug content, encapsulation efficiency, micromeritic properties and in vitro dissolution parameters. Surface morphology study by Scanning electron microscopy revealed spherical shape of microparticles. Prepared microparticles showed good flow property, improved aqueous solubility and faster in vitro dissolution rate compared with pure drug. The spray dried microparticles of Dihydroartemisinin with Poloxamer 188 in a ratio of 1:4 w/w showed 2.5 times enhancement of aqueous solubility and > 95 % drug release in 120 min when compared with pure drug alone. Thus from the result it can be concluded that spray dried microparticles of Dihydroartemisinin using Poloxamer 188 is useful technique to enhance the solubility and dissolution rate that will help to improve oral bioavailability.

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Formulation Development of Solid Dispersions of Bosentan using Gelucire 50/13 and Poloxamer 188

Cited by 22 publications

References 18 publications

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

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

Fundamental Aspects of a Third Component Used in Ternary Solid Dispersion: A Review

Preparation, Characterization and Dissolution Enhancement of Dihydroartemisinin Microparticles

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