Characterization of solid dispersions of piroxicam/polyethylene glycol 4000

Fernández, María Tomé; Rodríguez, Inés Carmen; Margarit, María Victoria; Cerezo, Antonio Castilla

doi:10.1016/0378-5173(92)90060-f

Cited by 42 publications

(19 citation statements)

References 4 publications

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“…Vera et al 19 dissolved 1 g of oxodipine per 150 mL of ethanol before mixing the solution with melted PEG 6000. In the preparation of piroxicam-PEG 4000 solid dispersion, Fernandez et al 20 dissolved the drug in chloroform and then mixed the solution with the melt of PEG 4000 at 70°C…”

Section: Limitations Of Solid Dispersion Systemsmentioning

confidence: 99%

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Serajuddin

1999

Journal of Pharmaceutical Sciences

1,431

780

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Although there was a great interest in solid dispersion systems during the past four decades to increase dissolution rate and bioavailability of poorly water-soluble drugs, their commercial use has been very limited, primarily because of manufacturing difficulties and stability problems. Solid dispersions of drugs were generally produced by melt or solvent evaporation methods. The materials, which were usually semisolid and waxy in nature, were hardened by cooling to very low temperatures. They were then pulverized, sieved, mixed with relatively large amounts of excipients, and encapsulated into hard gelatin capsules or compressed into tablets. These operations were difficult to scale up for the manufacture of dosage forms. The situation has, however, been changing in recent years because of the availability of surface-active and self-emulsifying carriers and the development of technologies to encapsulate solid dispersions directly into hard gelatin capsules as melts. Solid plugs are formed inside the capsules when the melts are cooled to room temperature. Because of surface activity of carriers used, complete dissolution of drug from such solid dispersions can be obtained without the need for pulverization, sieving, mixing with excipients, etc. Equipment is available for large-scale manufacturing of such capsules. Some practical limitations of dosage form development might be the inadequate solubility of drugs in carriers and the instability of drugs and carriers at elevated temperatures necessary to manufacture capsules.

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Section: Limitations Of Solid Dispersion Systemsmentioning

confidence: 99%

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Serajuddin

1999

Journal of Pharmaceutical Sciences

1,431

780

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“…It was found that the newly developed crystals had a higher dissolution rate than the pure drug. According to other published studies, polymers such as polyethylene glycol (PEG) and polyvinylpyrrolidone (PVP) have been used as excipients for the purpose of improving the dissolution rate of many poorly water-soluble drugs such as NSAIDs (4,5).…”

mentioning

confidence: 99%

Crystal modifications and dissolution rate of piroxicam

Lyn¹,

Sze²,

Rajendran³

et al. 2011

Acta Pharmaceutica

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Crystal modifications and dissolution rate of piroxicam Piroxicam is a nonsteroidal anti-inflammatory drug with low aqueous solubility which exhibits polymorphism. The present study was carried out to develop polymorphs of piroxicam with enhanced solubility and dissolution rate by the crystal modification technique using different solvent mixtures prepared with PEG 4000 and PVP K30. Physicochemical characteristics of the modified crystal forms of piroxicam were investigated by X-ray powder diffractometry, FT-IR spectrophotometry and differential scanning calorimetry. Dissolution and solubility profiles of each modified crystal form were studied and compared with pure piroxicam. Solvent evaporation method (method I) produced both needle and cubic shaped crystals. Slow crystallization from ethanol with addition of PEG 4000 or PVP K30 at room temperature (method II) produced cubic crystal forms. Needle forms produced by method I improved dissolution but not solubility. Cubic crystals produced by method I had a dissolution profile similar to that of untreated piroxicam but showed better solubility than untreated piroxicam. Cubic shaped crystals produced by method II showed improved dissolution, without a significant change in solubility. Based on the XRPD results, modified piroxicam crystals obtained by method I from acetone/benzene were cube shaped, which correlates well with the FTIR spectrum; modified needle forms obtained from ethanol/methanol and ethanol/acetone showed a slight shift of FTIR peak that may be attributed to differences in the internal structure or conformation.

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“…Minimizing the temperature and volume of organic solvent is necessary to obtain a productive SD. Other approaches based on those two basic methods have been suggested: gentle heating can be used to increase the solubility of components in the solvent method (126), or only the drug can be dissolved in the organic solvent, followed by adding the solutions to the melted carriers (127). Although the SD technique is commonly used to enhance the dissolution properties of poorly water-soluble drugs using hydrophilic polymeric carriers as dispersing agents (7), several studies on SDs have referred to "CR-SDs" using water-insoluble carriers such as EC (128), Eudragit (129), and Compritol (74) to produce sustained-release pharmaceutical forms of highly water-soluble drugs.…”

Section: Traditional Methodsmentioning

confidence: 99%

Controlled Release Systems Containing Solid Dispersions: Strategies and Mechanisms

Tran

Park

et al. 2011

Pharm Res

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In addition to a number of highly soluble drugs, most new chemical entities under development are poorly water-soluble drugs generally characterized by an insufficient dissolution rate and a small absorption window, leading to the low bioavailability. Controlled-release (CR) formulations have several potential advantages over conventional dosage forms, such as providing a uniform and prolonged therapeutic effect to improve patient compliance, reducing the frequency of dosing, minimizing the number of side effects, and reducing the strength of the required dose while increasing the effectiveness of the drug. Solid dispersions (SD) can be used to enhance the dissolution rate of poorly water-soluble drugs and to sustain the drug release by choosing an appropriate carrier. Thus, a CR-SD comprises both functions of SD and CR for poorly water-soluble drugs. Such CR dosage forms containing SD provide an immediately available dose for an immediate action followed by a gradual and continuous release of subsequent doses to maintain the plasma concentration of poorly water-soluble drugs over an extended period of time. This review aims to summarize all currently known aspects of controlled release systems containing solid dispersions, focusing on the preparation methods, mechanisms of action and characterization of physicochemical properties of the system.

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Characterization of solid dispersions of piroxicam/polyethylene glycol 4000

Cited by 42 publications

References 4 publications

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Crystal modifications and dissolution rate of piroxicam

Controlled Release Systems Containing Solid Dispersions: Strategies and Mechanisms

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