Multi-unit Controlled Release Systems of Nifedipine and Nifedipine:Pluronic® F-68 Solid Dispersions: Characterization of Release Mechanisms

Mehta, Ketan A.; Kislalioglu, M. Serpil; Phuapradit, Wantanee; Malick, A. Waseem; Shah, Navnit

doi:10.1081/ddc-120002843

Cited by 22 publications

(11 citation statements)

References 22 publications

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“…15 Recently, poloxamers, a group of block copolymer nonionic surfactants, have attracted considerable attention for application in preparation of solid dispersions. [16][17][18] These polymers are widely used as emulsifiers, solubilizing agents, and suspension stabilizers in liquid, oral, topical, and parenteral dosage forms and also act as wetting agents and plasticizers, and have been reported for enhancing the solubility and bioavailability of sparingly soluble drugs in solid dosage forms. 19,20 Nine grades of poloxamers have been evaluated by Saettone and coworkers 21 as solubilizers for tropicamide, a poorly water-soluble drug.…”

Section: Introductionmentioning

confidence: 99%

Process optimization and characterization of poloxamer solid dispersions of a poorly water-soluble drug

Shah

Amin

Parikh³

et al. 2007

AAPS PharmSciTech

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The objective of the present investigation was to improve the dissolution rate of Rofecoxib (RXB), a poorly water-soluble drug by solid dispersion technique using a water-soluble carrier, Poloxamer 188 (PXM). The melting method was used to prepare solid dispersions. A 3 2 full factorial design approach was used for optimization wherein the temperature to which the melt-drug mixture cooled (X 1 ) and the drug-to-polymer ratio (X 2 ) were selected as independent variables and the time required for 90% drug dissolution (t 90 ) was selected as the dependent variable. Multiple linear regression analysis revealed that for obtaining higher dissolution of RXB from PXM solid dispersions, a low level of X 1 and a high level of X 2 were suitable. The differential scanning calorimetry and x-ray diffraction studies demonstrated that enhanced dissolution of RXB from solid dispersion might be due to a decrease in the crystallinity of RXB and PXM and dissolution of RXB in molten PXM during solid dispersion preparation. In conclusion, dissolution enhancement of RXB was obtained by preparing its solid dispersions in PXM using melting technique. The use of a factorial design approach helped in identifying the critical factors in the preparation and formulation of solid dispersion.

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Section: Introductionmentioning

confidence: 99%

Process optimization and characterization of poloxamer solid dispersions of a poorly water-soluble drug

Shah

Amin

Parikh³

et al. 2007

AAPS PharmSciTech

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“…Therefore, multiple mechanisms control the rate of drug release from the formulations. Mehta et al demonstrated that drug release systems governed by multiple mechanisms, such as diffusion and erosion, can exhibit pseudosteady state approaching zero-order release rates (44,46). A zero-order release is observed when the diffusion rate of the dissolution media into the matrix and the polymer dissolution rate are equal, resulting in a synchronized or constant drug-depleted layer (47).…”

Section: Discussionmentioning

confidence: 99%

Development of Novel Oral Formulations Prepared via Hot Melt Extrusion for Targeted Delivery of Photosensitizer to the Colon

Cassidy

Tunney

Caldwell

et al. 2011

Photochem & Photobiology

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Colon-residing bacteria, such as vancomycin-resistant Enterococcus faecalis and Bacteroides fragilis, can cause a range of serious clinical infections. Photodynamic antimicrobial chemotherapy (PACT) may be a novel treatment option for these multidrug resistant organisms. The aim of this study was to formulate a Eudragit®-based drug delivery system, via hot melt extrusion (HME), for targeting colonic release of photosensitizer. The susceptibility of E. faecalis and B. fragilis to PACT mediated by methylene blue (MB), meso-tetra(N-methyl-4-pyridyl)porphine tetra-tosylate (TMP), or 5-aminolevulinic acid hexyl-ester (h-ALA) was determined, with tetrachlorodecaoxide (TCDO), an oxygen-releasing compound, added in some studies. Results show that, for MB, an average of 30% of the total drug load was released over a 6-h period. For TMP and h-ALA, these values were 50% and 16% respectively. No drug was released in the acidic media. Levels of E. faecalis and B. fragilis were reduced by up to 4.67 and 7.73 logs, respectively, on PACT exposure under anaerobic conditions, with increased kill associated with TCDO. With these formulations, photosensitizer release could potentially be targeted to the colon, and colon-residing pathogens killed by PACT. TCDO could be used in vivo to generate oxygen, which could significantly impact on the success of PACT in the clinic.

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“…[14] Recently, poloxamers, a group of block copolymer nonionic surfactants, have attracted considerable attention for application in preparation of SDs. [15][16][17] These polymers are widely used as emulsifiers, solubilizing agents, and suspension stabilizers in liquid, oral, topical, and parenteral dosage forms and also act as wetting agents and plasticizers, and have been reported for enhancing the solubility and bioavailability of sparingly soluble drugs in solid dosage forms. [18,19] Nine grades of poloxamers have been evaluated by Saettone et al [20] as solubilizers for tropicamide, a poorly water-soluble drug.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of glimepiride solid dispersion tablets

Gill¹,

Kaur²,

Kumar³

et al. 2010

Asian J Pharm

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The poor dissolution rate of water-insoluble drugs is still a major problem conforming the pharmaceutical industry. The most common method for improving the solubility is by increasing the surface area of the drug through micronization. But, in practice the effect of micronization is often disappointing, especially when the drugs are encapsulated or tablet. It is generally recognized that low solubility or dissolution rate often becomes a rate-limiting step in absorption of poorly water soluble drugs. Therefore, the enhancement of the dissolution rate of poorly water-soluble drugs after oral administration is one of the most challenging aspects of modern pharmaceutics. Olanzepine (2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno [2, b] [1, 5]benzodiazepine possess antipsychotic activity and exhibits very slight solubility in water and as a consequence it exhibit low bioavailability after oral administration Therefore, the improvement of olanzepine dissolution from its oral solid dosage forms is an important issue for enhancing its bioavailability and therapeutic efficacy. The purpose of present work is to improve the solubility of Olanzepine by preparing its dispersion with polymer PEG (Poly Ethylene Glycol) using solvent evaporation technique.

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Multi-unit Controlled Release Systems of Nifedipine and Nifedipine:Pluronic® F-68 Solid Dispersions: Characterization of Release Mechanisms

Cited by 22 publications

References 22 publications

Process optimization and characterization of poloxamer solid dispersions of a poorly water-soluble drug

Process optimization and characterization of poloxamer solid dispersions of a poorly water-soluble drug

Development of Novel Oral Formulations Prepared via Hot Melt Extrusion for Targeted Delivery of Photosensitizer to the Colon

Formulation and evaluation of glimepiride solid dispersion tablets

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