A systematic evaluation of dual functionality of sodium lauryl sulfate as a tablet lubricant and wetting enhancer

Dun, Jiangnan; Osei-Yeboah, Frederick; Boulas, Pierre; Lin, Yiqing; Sun, Changquan Calvin

doi:10.1016/j.ijpharm.2018.09.056

Cited by 36 publications

(15 citation statements)

References 57 publications

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“…Therefore, replacing MgSt with SLS in an otherwise identical RTV tablet formulation may be expected to improve drug release. 11 However, concentration-time profile in ASD stomach chamber surprisingly exhibited lower C max and slower initial release than the MgSt-containing tablet (Fig. 2).…”

Section: Retarded Release Of Rtv In Sls-contained Tabletmentioning

confidence: 91%

“…[5][6][7] It has been used as an emulsifier, solubilizer, tablet lubricant, and wetting agent. 5,[8][9][10][11] When applied as a wetting agent, SLS could reduce the surface tension between hydrophobic drugs and aqueous media to prevent the self-aggregation of drug particles, thus increase the effective surface area of dissolution. 8 Above the critical micelle concentration (CMC), SLS monomers aggregate to form micelles that can solubilize hydrophobic drugs.…”

Section: Introductionmentioning

confidence: 99%

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Mechanism for the Reduced Dissolution of Ritonavir Tablets by Sodium Lauryl Sulfate

Guo

Wang

Dun

et al. 2019

Journal of Pharmaceutical Sciences

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Sodium lauryl sulfate (SLS) is an anionic surfactant widely used in pharmaceutical research as a dissolution enhancer for poorly soluble drugs. When SLS was used in ritonavir (RTV) tablet formulation to improve wetting, dissolution of RTV was surprisingly deteriorated in acidic media. To understand this unexpected phenomenon, a systematic investigation, including solubility determination, intrinsic dissolution rate measurement, dissolution in an artificial stomach and duodenum apparatus, and solidstate characterization, revealed the formation of a poorly soluble salt, [RTV 2þ ][LS À ] 2 , in an acidic environment. Solubilization of the poorly soluble RTV salt was observed when the concentration of SLS exceeded the critical micelle concentration. Thus, precipitation of [RTV 2þ ][LS À ] 2 at a low pH and in presence of a low SLS concentration can lead to deteriorated bioavailability. This unintended negative effect on dissolution should be carefully considered when using SLS in a tablet formulation of a basic drug that can be ionized in gastric fluid.

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Section: Retarded Release Of Rtv In Sls-contained Tabletmentioning

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Mechanism for the Reduced Dissolution of Ritonavir Tablets by Sodium Lauryl Sulfate

Guo

Wang

Dun

et al. 2019

Journal of Pharmaceutical Sciences

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“…Surfactants are included in solid oral dosage forms to reduce the interface energy barrier between the dissolution medium and the API, which will allow for more efficient wettability. Surfactants are amphiphilic substances that contain both hydrophobic (non-polar) and hydrophilic (polar) functional groups in their molecular structures [43,44].…”

Section: Surfactantsmentioning

confidence: 99%

“…Surfactants are able to form micelles above the critical micelle concentration (CMC) in aqueous liquids such as the fluids found in the gastro-intestinal tract. These micelles can increase the solubility of poorly water-soluble active ingredients by incorporating these molecules in the lipophilic cores of the micelles [43].…”

Section: Surfactantsmentioning

confidence: 99%

The Role of Functional Excipients in Solid Oral Dosage Forms to Overcome Poor Drug Dissolution and Bioavailability

et al. 2020

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Many active pharmaceutical ingredients (APIs) exhibit poor solubility and low dissolution rates in aqueous environments such as the luminal fluids of the gastrointestinal tract. The oral bioavailability of these compounds is usually very low as a result of their poor solubility properties. In order to improve the bioavailability of these poorly soluble drugs, formulation strategies have been applied as a means to improve their aqueous solubility and dissolution rates. With respect to formulation approaches, excipients can be incorporated in the formulation to assist in the dissolution process of the drug, or specialized dosage forms can be formulated that improve dissolution rate through various mechanisms. This paper provides an overview of selected excipients (e.g., alkalinizing agents, surfactants and sugars) that can be used in formulations to increase the dissolution rate as well as specialized dosage forms such as self-emulsifying delivery systems and formulation techniques such as inclusion complexes and solid dispersions. These formulation approaches are discussed with available examples with specific reference to positive outcomes in terms of drug solubility and bioavailability enhancement.

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“…Garam mandi (61)(62)(63)(64) Kapasitas Kalor (72)(73)(74)(75) Sintesis organik (16; 76-78) Pengering (34)(35)(36)(37) Pertanian (38)(39)(40) Farmasi (18)(19)(20)(21) Elektrolit pada sintesis (85)(86)(87) Koagulan (31)(32)(33) Mobilitas Ion (65)(66)(67) Bentuk dan struktur (11; 46; 80; 81) MgSO4 umumnya dapat dijumpai dalam garam epsomite yakni MgSO4.7H2O. Di alam senyawa ini terdapat dalam bentuk mineral sulfat.…”

Section: Sifat Fisikaunclassified

Analisis Termodinamika Molekul Magnesium Sulphate (MgSO4)

Yuliani¹,

Zainul²

2018

Preprint

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Magnesium sulfat merupakan salah satu garam anorganik dengan rumus kimia MgSO4. Magnesium sulfat ini termasuk senyawa ionik karena terdapat ikatan antara logam magnesium dengan spesi non logam sulfat. Magnesium sulfat bersifat polar, bentuk anhidratnya sangat higroskopik dan mudah memiliki koordinasi dengan air. Umumnya magnesium sulfat terbentuk dalam formasi hidrat MgSO4.xH2O. Penelitian ini bertujuan untuk menganalisis pengaruh sifat termodinamika molekul MgSO4 terhadap interaksi molekuler di dalam senyawa tersebut. Metode yang digunakan ialah pemodelan dengan aplikasi ChemOffice 15.0. Sedangkan untuk data mobilitas ion, konduktivitas, viskositas, kecepatan hanyut dengan menggunakan perhitungan dan data dari hasil review beberapa jurnal penelitian yang berkaitan dengan magnesium sulfat sesuai tahapan yang tertera pada fishbond. Magnesium sulfat memiliki sifat termokimia dalam fasa solid dengan ∆𝐻𝑓,∆𝐺𝑓,𝑆°, 𝑑𝑎𝑛 𝐶𝑝 pada tekanan 1 atm dan suhu 25°C yang masing-masing mempunyai nilai -1284,9 kJ/mol, -1170,7 kJ/mol, 91,6 J/molK dan 96,48 J/molK. Mobilitas ion Mg2+dan SO42- adalah 5,50.10-8m2s-1V-1 dan 8,29.108m2s-1V-1. Panas reaksi standar (ΔHr°) MgSO4 bernilai negatif maka reaksi bersifat eksotermis

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A systematic evaluation of dual functionality of sodium lauryl sulfate as a tablet lubricant and wetting enhancer

Cited by 36 publications

References 57 publications

Mechanism for the Reduced Dissolution of Ritonavir Tablets by Sodium Lauryl Sulfate

Mechanism for the Reduced Dissolution of Ritonavir Tablets by Sodium Lauryl Sulfate

The Role of Functional Excipients in Solid Oral Dosage Forms to Overcome Poor Drug Dissolution and Bioavailability

Analisis Termodinamika Molekul Magnesium Sulphate (MgSO4)

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