Solubility enhancement of desloratadine by solid dispersion in poloxamers

Kolašinac, Nemanja; Kachrimanis, Kyriakos; Homšek, Irena; Grujić, Branka; Đurić, Zorica; Ibrić, Svetlana

doi:10.1016/j.ijpharm.2012.06.060

Cited by 97 publications

(49 citation statements)

References 29 publications

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“…The 8-mm IDM showed a faster drug release for the L inner tablet whereas the IDM using a 7:3 inner tablet showed a slower drug release. This was due to the rapid erosion of the hydrophilic matrix of L (25,26). In the case of the 7:3 outer layer, the release was sustained but still faster than the S outer layer because 7:3 lowered the drug release owing to the apparently strengthened gel as previously reported (7).…”

Section: Discussionmentioning

confidence: 57%

Double-Layered Matrix of Shellac Wax-Lutrol in Controlled Dual Drug Release

Phaechamud

Choncheewa

2015

AAPS PharmSciTech

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Abstract. Double-layered matrix tablets prepared from shellac wax-lutrol were fabricated using a molding technique, and the release of hydrochlorothiazide and propranolol HCl from the inner tablet or outer layer was studied. The simultaneous determination of dual drug release was measured with first derivative UV spectrophotometry. The tablet containing shellac wax as the outer tablet and lutrol as the inner tablet showed more appropriate drug release and the size of the inner layer influenced the rate of drug release. In addition, the aqueous solubility of the drug and the components of the inner tablet or outer layer affected the drug release behavior. Most of the double-layered tablets exhibited the drug-release pattern which fitted well with zero-order kinetic due to the restriction of the release surface. Biphasic drug release pattern was found in the tablet of which the outer layer rapidly eroded. The drug dissolution data from drug-loaded-outer layer could predict the dissolution time for the outer layer of drug-loaded inner part of double-layered matrix tablet. Incorporation of lutrol increased the drug release from shellac wax matrix, and the zero-order release was attained by fabricating it into a double-layered tablet.

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Section: Discussionmentioning

confidence: 57%

Double-Layered Matrix of Shellac Wax-Lutrol in Controlled Dual Drug Release

Phaechamud

Choncheewa

2015

AAPS PharmSciTech

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“…The reviewed publications showed that different grades of water were used as media to determine the solubility of drug substance: double-distilled water (6)(7)(8); double deionized water (9), Milli-Q® purified water (10), 18.2 MΩ.cm/ 0.22 μm (11); Milli-Q®ultrapure water, conductivity less than 0.1 μS cm (12,13); ultrapure water Elix® Millipore (14); distilled water (5,15-21) deionized water (22)(23)(24)(25)(26); distilled, deionized, and filtered water (27); purified water (28)(29)(30)(31)(32)(33)(34)(35)(36); demineralized water (37). The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

“…In the last decade, biorelevant media have been extensively used to determine drug solubility and as dissolution media, especially for BCS class II compounds (14 studies or 25.0%) (8,9,13,22,27,33,35,42,44,45,47,51,54,55) as well as for BCS class I (4 studies or 7.1%) (33,34,49,51), class III (2 or 3.6%) (33,51), and class IV (2 or 3.6%) (33,51). As mentioned, biorelevant media contain generally components which are likely present in the human GI tract such as bile salts and lecithin aiming to mimic the physiological conditions in specific segments of the GI tract; thus, in these media, pH, osmolality, and surface tension are adapted to physiological values (75).…”

Section: Biorelevant Mediamentioning

confidence: 99%

“…Deaerated water is mentioned in USP chapter 1092 (102); the suggested methods for deaerating include warming the dissolution media to 41°C, followed by vacuum filtration through a 0.45-μm pore-size-rated membrane, and vigorously stirring the filtrate while maintaining vacuum. This review showed that 6 of 20 studies (9,14,16,22,23,34) used water as dissolution medium. Only one study mentioned the degassing procedure (14).…”

Section: Watermentioning

confidence: 99%

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Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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“…26 Currently, the typical carriers widely used for the formulation of SDs consist of organic materials that are highly water soluble and/or polymeric in nature. [27][28][29][30] In addition to these carriers, inert hydrophilic carriers, such as inorganic silica-based materials 31,32 which have relatively large specific surface areas, and thus produce powders in which the drug may be highly dispersed, are receiving increasing attention. Takeuchi et al [33][34][35] reported that SDs with porous silica or colloidal silica prepared using the spray-drying method can improve the dissolution property of tolbutamide and indomethacin.…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles

Jiang¹,

Zhang²,

Liu³

et al. 2013

IJN

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Abstract:We prepared solid dispersions (SDs) of tanshinone IIA (TSIIA) with silica nanoparticles, which function as dispersing carriers, using a spray-drying method and evaluated their in vitro dissolution and in vivo performance. The extent of TSIIA dissolution in the silica nanoparticles/TSIIA system (weight ratio, 5:1) was approximately 92% higher than that of the pure drug after 60 minutes. However, increasing the content of silica nanoparticles from 5:1 to 7:1 in this system did not significantly increase the rate or extent of TSIIA dissolution. The physicochemical properties of SDs were investigated using scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and Fourier transforms infrared spectroscopy. Studying the stability of the SDs of TSIIA revealed that the drug content of the formulation and dissolution behavior was unchanged under the applied storage conditions. In vivo tests showed that SDs of the silica nanoparticles/TSIIA had a significantly larger area under the concentration-time curve, which was 1.27 times more than that of TSIIA (P , 0.01). Additionally, the values of maximum plasma concentration and the time to reach maximum plasma concentration of the SDs were higher than those of TSIIA and the physical mixing system. Based on these results, we conclude that the silica nanoparticle based SDs achieved complete dissolution, increased absorption rate, maintained drug stability, and showed improved oral bioavailability compared to TSIIA alone.

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Solubility enhancement of desloratadine by solid dispersion in poloxamers

Cited by 97 publications

References 29 publications

Double-Layered Matrix of Shellac Wax-Lutrol in Controlled Dual Drug Release

Double-Layered Matrix of Shellac Wax-Lutrol in Controlled Dual Drug Release

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles

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