In vivo evaluation of rapid release and sustained release Gelucire capsule formulations

Dennis, Andrew B.; Farr, Stephen J.; Kellaway, I.W.; Taylor, Glyn; Davidson, R. D.

doi:10.1016/0378-5173(90)90013-t

Cited by 53 publications

(31 citation statements)

References 43 publications

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“…PEGs are widely used due to their low melting point, low toxicity, wide drug compatibility and hydrophilicity. [9] Solubility of PEGs in water is generally good, but it decreases with increase in their molecular weight. [10] PEGs have the ability to solubilize poorly water soluble compounds by improving their wettability.…”

Section: Introductionmentioning

confidence: 99%

Improvement in Micromeritic Properties and Dissolution Rate of Glimepiride

Sahoo¹

2017

WJPR

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Section: Introductionmentioning

confidence: 99%

Improvement in Micromeritic Properties and Dissolution Rate of Glimepiride

Sahoo¹

2017

WJPR

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“…Even though the composition of formulation D1, D2, and D3 was similar except the presence or absence of amorphous state of CIL, still the extent of drug release in D1 and D2 formulations was just around 30%. This aspect for poor drug release from these matrices may be correlated with the importance of wettability (35)(36)(37). Since the crystalline form is poorly water soluble and formulating this form into wax-based matrix does not allow the drug to get wet and available for diffusion through the insoluble wax matrix.…”

Section: Design and Development Of 12-h Release Profilementioning

confidence: 99%

Disintegration Mediated Controlled Release Supersaturating Solid Dispersion Formulation of an Insoluble Drug: Design, Development, Optimization, and In Vitro Evaluation

Verma

Rudraraju²

2014

AAPS PharmSciTech

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Abstract. The objective of this study was to develop a solid dispersion based controlled release system for drug substances that are poorly soluble in water. A wax-based disintegration mediated controlled release system was designed based on the fact that an amorphous drug can crystallize out from hydrophilic matrices. For this study, cilostazol (CIL) was selected as the model drug, as it exhibits poor aqueous solubility. An amorphous solid dispersion was prepared to assist the drug to attain a supersaturated state. Povidone was used as carrier for solid dispersion (spray drying technique), hydrogenated vegetable oil (HVO) as wax matrix former, and sodium carboxymethyl cellulose (NaCMC) as a disintegrant. The extreme vertices mixture design (EVMD) was applied to optimize the designed and developed composition. The optimized formulation provided a dissolution pattern which was equivalent to the predicted curve, ascertaining that the optimal formulation could be accomplished with EVMD. The release profile of CIL was described by the Higuchi's model better than zero-order, first-order, and Hixson-Crowell's model, which indicated that the supersaturation state of CIL dominated to allow drug release by diffusion rather than disintegration regulated release as is generally observed by Hixson-Crowell's model. The optimized composition was evaluated for disintegration, dissolution, XRD, and stability studies. It was found that the amorphous state as well as the dissolution profile of CIL was maintained under the accelerated conditions of 40°C/75% RH for 6 months.

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“…Gelucire44/14 has commonly been used in solid dispersion for the bioavailability enhancement of drugs. A commonly used surfactant, Polysorbate 80, when mixed with solid PEG, has also been reported to be an alternative surface-active carrier 67,68,69 .…”

Section: Direct Capsule Fillingmentioning

confidence: 99%

Untitled

2010

IJPSR

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The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.

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In vivo evaluation of rapid release and sustained release Gelucire capsule formulations

Cited by 53 publications

References 43 publications

Improvement in Micromeritic Properties and Dissolution Rate of Glimepiride

Improvement in Micromeritic Properties and Dissolution Rate of Glimepiride

Disintegration Mediated Controlled Release Supersaturating Solid Dispersion Formulation of an Insoluble Drug: Design, Development, Optimization, and In Vitro Evaluation

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