Melting Process of the Peritectic Mixture of Lidocaine and Ibuprofen Interpreted by Site Percolation Theory Model

Kataoka, Hikaru; Sakaki, Yoshinori; Komatsu, Kazushi; Shimada, Yohsuke; Goto, Satoru

doi:10.1016/j.xphs.2017.04.010

Cited by 15 publications

(22 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A phase diagram for ibuprofen (IBP; T m = 329 K) and LDC at various ratios indicated that the mixtures are peritectic with two phase transition temperatures (293 and 310 K), suggesting the presence of heterogeneous intermediate states at these temperatures. 19) The tendency to form a heterogeneous amorphous phase has been kinetically observed, particularly in IBP-rich mixtures. As illustrated by these examples, the individual behaviors of components are determined by the component with the lower fusion temperature.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Enthalpy–Entropy Compensation in the Structure-Dependent Effect of Nonsteroidal Anti-inflammatory Drugs on the Aqueous Solubility of Diltiazem

et al. 2022

Self Cite

View full text Add to dashboard Cite

Certain combinations of acidic and basic drugs can cause significant changes in physicochemical properties through the formation of ionic liquids, eutectic mixtures, or deep eutectic solvents. In particular, combining indomethacin and lidocaine is known to result in apparent increases in both the partition coefficients (hydrophobicity) and aqueous solubilities (hydrophilicity). The physicochemical interactions between drugs change the water solubility of the drugs and affect the bio-availability of active pharmaceutical ingredients. Therefore, we need to clarify the mechanism of changes of water solubility of drugs through the physicochemical interactions. In the present study, we identified a thermodynamic factor that regulates the dissolution of a basic drug, in the presence of various acidic nonsteroidal anti-inflammatory drugs. The results demonstrated that enthalpy-entropy compensation plays a key role in the dissolution of drug mixtures and that relevant thermodynamic conditions should be considered.

show abstract

Section: Introductionmentioning

confidence: 99%

“…20,21) Thus, the water-soluble amorphous states of IDM/LDC, IBP/LDC, and other mixtures have been investigated because LDC has a lower fusion temperature. 18,19) Although the hydrochloride salt of LDC (T m = 347 K) also exhibits an amorphous state when mixed with IDM, the glass transition occurs at any ratio with-out anisotropy.…”

Section: Introductionmentioning

confidence: 99%

Enthalpy–Entropy Compensation in the Structure-Dependent Effect of Nonsteroidal Anti-inflammatory Drugs on the Aqueous Solubility of Diltiazem

et al. 2022

Self Cite

View full text Add to dashboard Cite

show abstract

“…34 Combined with this fact, OXY is thought to exhibit a parachute effect on the supersaturated state of PX-AH by modifying the interface to the solution of anhydrate crystal and monohydrate crystal. 37 The results shown in Fig. 3a cannot enable us to predict how long the parachute effect of OXY continues depending on the concentration.…”

Section: Discussionmentioning

confidence: 95%

“…S8 and S9 †). [37][38][39][40][41] From these results, it is considered that the parachute effect of OXY against the PX-AH's supersaturated state is not a simple system that interacts 1 : 1, but more intricate interactions among PX, OXY, and water molecules occur. However, since OXY molecules are smaller and simpler than the polymers, we can contribute to the elucidation of the mechanism of the parachute effect on the supersaturated state.…”

Section: Discussionmentioning

confidence: 99%

The function of oxybuprocaine: aparachuteeffect that sustains the supersaturated state of anhydrous piroxicam crystals

et al. 2020

Self Cite

View full text Add to dashboard Cite

show abstract

“…Subsequently, the remnant water added to yield the final lidocaine loaded microemulsions. It has been reported that the eutectic mixture, due to the decreased melting points and enthalpy, would have the potential to improve the solubility of the drugs and subsequently be favorable for oral administration and higher transdermal efficiency into the skin as topical drugs (15,16).…”

Section: Preparation Of Lidocaine Microemulsionsmentioning

confidence: 99%

Design and Development of Lidocaine Microemulsions for Transdermal Delivery

Wang

et al. 2019

AAPS PharmSciTech

View full text Add to dashboard Cite

Topical administration is a preferable choice for local anesthetic delivery. Microemulsions have shown great effectiveness for transdermal transport of lidocaine. However, fabrication of microemulsions containing highly concentrated lidocaine (10%) to provide an extended local anesthetic effect is still a challenge. This study investigated the feasibility of using microemulsions for transdermal delivery of a high dosage of lidocaine (10%). At first, eutectic mixtures by kneading lidocaine with thymol were tailored to form a lipophilic solution, then the mixtures were readily incorporated into the oil phase of microemulsions after addition of proper surfactants and cosurfactants. The physicochemical properties, the skin permeation, local anesthetic efficacy, and the irritation experiment of the developed microemulsions were evaluated. The optimum composition was as follows: 12% of ethyl oleate as oil phase, 28% of the mixed surfactant, and cosurfactant (polyoxyl 15 hydroxystearate and ethanol) and 60% of the aqueous phase. The average particle size was about 13 nm. The transmission electron microscope (TEM) studies revealed almost homogeneous spherical globules without aggregation. The Fourier-transform infrared spectroscopy (FTIR) results highlighted the drugs homogeneously dispersed in the microemulsions. In vitro skin permeation and in vivo anesthesia effect evaluation indicated that microemulsions can enhance and extend the anesthetic effect of lidocaine. The irritable results indicated that the microemulsions had the better biocompatibility and the negligible influence on the dermal. Therefore, incorporating the eutectic mixtures into microemulsions could be proposed as an attractive choice and a promising transdermal delivery strategy for the future topical anesthetic therapy.

show abstract

Melting Process of the Peritectic Mixture of Lidocaine and Ibuprofen Interpreted by Site Percolation Theory Model

Cited by 15 publications

References 23 publications

Enthalpy–Entropy Compensation in the Structure-Dependent Effect of Nonsteroidal Anti-inflammatory Drugs on the Aqueous Solubility of Diltiazem

Enthalpy–Entropy Compensation in the Structure-Dependent Effect of Nonsteroidal Anti-inflammatory Drugs on the Aqueous Solubility of Diltiazem

The function of oxybuprocaine: aparachuteeffect that sustains the supersaturated state of anhydrous piroxicam crystals

Design and Development of Lidocaine Microemulsions for Transdermal Delivery

Contact Info

Product

Resources

About