Rheological and Mechanical Analyses of Felbinac Cataplasms by Using Box–Behnken Design

Yang, Jianqun; Zhu, Yishen; Diao, Yongqin; Yin, Caiyun

doi:10.3390/pharmaceutics10030088

Cited by 7 publications

(3 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As shown in Figure 1e, the strain of the cataplasm increased rapidly to a plateau under stress, and after the stress was removed, the strain could not return to the zero-stress state. This creep-recovery characteristic showed similar features to the Kelvin-Voigt model [20], which also reflected the presence of a cross-linked structure within the cataplasm. According to the shear rate, from high to low, the trends in stress and viscosity of the cataplasm were investigated.…”

Section: Characterization Of Ketorolac Tromethamine Cataplasmsupporting

confidence: 59%

See 1 more Smart Citation

Topical Delivery of Ketorolac Tromethamine via Cataplasm for Inflammatory Pain Therapy

et al. 2023

View full text Add to dashboard Cite

Nonsteroidal anti-inflammatory drugs (NSAIDs) have been widely used in the treatment of inflammatory pain, such as in osteoarthritis. Ketorolac tromethamine is considered to be an NSAID with strong anti-inflammatory and analgesic potency, however, traditional applications, such as oral administration and injections, often induce high systemic exposure, leading to adverse events such as gastric ulceration and bleeding. To address this key limitation, herein we designed and fabricated a topical delivery system for ketorolac tromethamine via cataplasm, which is based on a three-dimensional mesh structure formed by the cross-linking of dihydroxyaluminum aminoacetate (DAAA) and sodium polyacrylate. The viscoelasticity of the cataplasm was characterized by rheological methods and exhibited a “gel-like” elastic property. The release behavior showed a Higuchi model characteristic with a dose dependence. To enhance the skin permeation, permeation enhancers were added and screened utilizing ex vivo pig skin, in which 1,2-propanediol was found to have the optimal permeation-promoting effect. The cataplasm was further applied to a rat carrageenan-induced inflammatory pain model, which showed comparable anti-inflammatory and analgesic effects with oral administration. Finally, the biosafety of the cataplasm was tested in healthy human volunteers, and reduced side effects were achieved as compared to the tablet formulation, which can be ascribed to less systemic drug exposure and lower blood drug concentrations. Therefore, the constructed cataplasm can reduce the risk of adverse events while maintaining efficacy, thus serving as a better alternative for the treatment of inflammatory pain, including osteoarthritis.

show abstract

Section: Characterization Of Ketorolac Tromethamine Cataplasmsupporting

confidence: 59%

“…PSTC 1 standard test method evaluated peel strength at a peel angle of 180° using an electronic peel-strength test device (Sumspring Co., Ltd., Jinan, China) [ 20 ]. The backing membrane side of the cataplasm was fixed on a stainless-steel plate (length: 125 mm, width: 50 mm, and thickness: 2 mm).…”

Section: Methodsmentioning

confidence: 99%

Topical Delivery of Ketorolac Tromethamine via Cataplasm for Inflammatory Pain Therapy

et al. 2023

View full text Add to dashboard Cite

show abstract

“…Compared with the patch, the cataplasm has the advantages of high drug loading, moisture retention and good air permeability, which is a kind of topical preparations with good development prospect. The cataplasm containing felbinac is developed as a new route of administration to deliver high concentration of the drug to the sites of in ammation for the treatment of arthritis [18][19][20][21].…”

Section: Introductionmentioning

confidence: 99%

Design of a novel felbinac cataplasm with high permeability for the treatment of arthritis

Liu

Bai

Zhao

et al. 2023

Preprint

View full text Add to dashboard Cite

The purpose of this study was to design a novel felbinac cataplasm with higher permeability than commercial product SELTOUCH® through using chemical enhancer strategy to reduce the times of administration and improve the compliance of patients. The novel felbinac cataplasm with high adhesion and good biocompatibility was prepared by calendar coating method. On the basis of previous research, the high-performance liquid chromatography (HPLC) analytical method of felbinac was established. According to 2020 Chinese pharmacopoeia (Ch. P), the paddle plate method was used to study the in vitro dissolution. The results showed the release of drug from self-made felbinac cataplasm could reach 90%. Subsequently, the effects of different kinds of penetration enhancers (N-methylpyrrolidone (NMP), isopropyl myristate (IPM) and propylene glycol (PG)) with the same percentage on the penetration of felbinac cataplasm were investigated. Propylene glycol (PG) was proved to be the most effective permeation enhancer among them. After screening different percentages of PG, 1% was added as the amount of permeation enhancer and the 12 h cumulative permeation amount was 189.03 µg/cm2 which was two times of the reference cataplasm (94.44 µg/cm2). The self-made felbinac cataplasm also had good stable permeability after placing at room temperature for 4 months. Finally, the tissue distribution study showed no matter in plasma, skin or muscle, the drug concentration of self-made cataplasm group was higher than reference cataplasm group. These data indicated that the self-made cataplasm provided a new reference for the development of felbinac dosage forms and promising alternative strategy for arthritis therapy.

show abstract

A two-step design of experiments approach to investigate the simultaneous effects of ion-pairing and chemical enhancers to improve the permeability of lornoxicam in a topical hydrogel patch

Nguyen,

Duong,

Nguyen

et al. 2024

J. Pharm. Investig.

View full text Add to dashboard Cite

Rheological and Mechanical Analyses of Felbinac Cataplasms by Using Box–Behnken Design

Cited by 7 publications

References 18 publications

Topical Delivery of Ketorolac Tromethamine via Cataplasm for Inflammatory Pain Therapy

Topical Delivery of Ketorolac Tromethamine via Cataplasm for Inflammatory Pain Therapy

Design of a novel felbinac cataplasm with high permeability for the treatment of arthritis

A two-step design of experiments approach to investigate the simultaneous effects of ion-pairing and chemical enhancers to improve the permeability of lornoxicam in a topical hydrogel patch

Contact Info

Product

Resources

About