Formulation and evaluation of co-prodrug of flurbiprofen and methocarbamol

Bhatia, Neela M.; Katkar, Kiran; Ashtekar, Snehal S.

doi:10.1016/j.ajps.2015.10.031

Cited by 11 publications

(7 citation statements)

References 16 publications

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“…The main reason for this fact can be, for example, the different adsorbing properties of applied stationary phases or eluents such as their elution strength or surface tension, which show an influence on the results of the R M parameter. As was confirmed in previous studies, the pH value of distilled water used as a mobile phase component also has a large impact on the value of both the chromatographic lipophilicity parameters and the experimental partition coefficients [8,11,18,31].…”

Section: Resultssupporting

confidence: 53%

“…Because the pH value of distilled water used to determine the partition coefficient in an n -octanol-water system may cause the differences in logP exp values for the abovementioned compounds, the partition coefficient of the synthesized co-prodrug of flurbiprofen and methocarbamol was determined in the three mobile phases, namely: water, n -octanol-water (pH = 1.2) and n -octanol-phosphate buffer (pH = 7.4). Under these conditions the logP o/w values equal to 5.13; 1.32 and 4.72 were observed [31].…”

Section: Resultsmentioning

confidence: 99%

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Comparison of the Utility of RP-TLC Technique and Different Computational Methods to Assess the Lipophilicity of Selected Antiparasitic, Antihypertensive, and Anti-inflammatory Drugs

2019

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The aim of this study was to assess the lipophilicity of selected antiparasitic, antihypertensive and non-steroidal anti-inflammatory drugs (NSAIDs) by means of reversed phase–thin layer chromatography (RP-TLC) as well by using Soczewiński–Wachtmeister’s and J. Ościk’s equations. The lipophilicity parameters of all examined compounds obtained under various chromatographic systems (i.e., methanol-water and acetone-water, respectively) and those determined on the basis of Soczewiński-Wachtmeister’s and Ościk’s equations (i.e., RMWS and RMWO) were compared with the theoretical ones (e.g., AlogPs, AClogP, milogP, AlogP, MlogP, XlogP2, XlogP3) and the experimental value of the partition coefficient (logPexp). It was found that the RMWS parameter may be a good alternative tool in describing the lipophilic nature of biologically active compounds with a high and low lipophilicity (i.e., antihypertensive and antiparasitic drugs). Meanwhile, the RMWO was more suitable for compounds with a medium lipophilicity (i.e., non-steroidal anti-inflammatory drugs). The chromatographic parameter 0(a) can be helpful for the prediction of partition coefficients, i.e., AClogP, XlogP3, as well as logPexp of examined compounds.

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Section: Resultssupporting

confidence: 53%

Section: Resultsmentioning

confidence: 99%

Comparison of the Utility of RP-TLC Technique and Different Computational Methods to Assess the Lipophilicity of Selected Antiparasitic, Antihypertensive, and Anti-inflammatory Drugs

2019

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“…with stomach ulcer such as relaxation of muscle and dopamine secretion [16]. For clarifying the target genes of FLD, ANOVA of gene expression level in different groups was carried out and eighteen ones were deduced.…”

Section: Discussionmentioning

confidence: 99%

Transcriptomic Analysis of Fuzi Lizhong Decoction for the Treatment of Stomach Ulcers

Yang

Wang

2020

Evidence-Based Complementary and Alternative Medicine

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This study aims to understand the treatment of stomach ulcers with FLD and to identify its potential target genes as well as related pathways by transcriptomic analysis. Rat stomach mRNA from a blank group (BG), a model group (MG), an untreated-model group (u-MG), and a treated group (TG) was sequenced. A partial least-squares discriminant analysis (PLS-DA) was used to differentiate the MG from the BG, and the Deseq2 R Package was used to identify differentially expressed genes between these groups. Furthermore, t-tests based on transcripts per million (TPM) were used to select different genes between MG and BG and significantly retrieved genes in TG, except for self-retrieved genes in u-MG. Finally, pathways regulated by retrieved genes were analyzed with KEGG database. Results showed that 327 of the 32,623 total detected genes were different (p<0.05) between the MG and BG. Among these genes, eighteen genes were significantly retrieved after rats were treated with FLD in TG, and they were considered as target genes on which FLD acted. In conclusion, FLD was deduced to cure stomach ulcers by affecting glycerolipid metabolism, fatty acid degradation, circadian entrainment, circadian rhythm, and dopaminergic synapse.

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“…The long exposure to DC inhibits prostaglandin formation which causes gastric irritation, bleeding, and ulcers [ 2 ]. These side effects can be minimized by reducing direct contact of drug with GIT [ 3 ].…”

Section: Introductionmentioning

confidence: 99%

Development and Optimization of Nanolipid-Based Formulation of Diclofenac Sodium: In Vitro Characterization and Preclinical Evaluation

et al. 2022

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In the present research study, we formulate bilosomes (BMs) of diclofenac (DC) for oral delivery for enhancement of therapeutic efficacy (anti-inflammatory disease). The BMS were prepared by thin film hydration method and optimized by Box–Behnken design (BBD) using cholesterol (A), lipid (B), surfactant (C), and bile salt (D) as formulation factors. Their effects were evaluated on vesicle size (Y1) and entrapment efficacy (Y2). The optimized DC-BMs-opt showed a vesicle size of 270.21 ± 3.76 nm, PDI of 0.265 ± 0.03, and entrapment efficiency of 79.01 ± 2.54%. DSC study result revealed that DC-BMs-opt exhibited complete entrapment of DC in BM matrix. It also depicted significant enhancement (p < 0.05) in release (91.82 ± 4.65%) as compared to pure DC (36.32 ± 4.23%) and DC-liposomes (74.54 ± 4.76%). A higher apparent permeability coefficient (2.08 × 10−3 cm/s) was also achieved compared to pure DC (6.6 × 10−4 cm/s) and DC-liposomes (1.33 × 10−3 cm/s). A 5.21-fold and 1.43-fold enhancement in relative bioavailability was found relative to pure DC and DC liposomes (DC-LP). The anti-inflammatory activity result showed a significant (p < 0.05) reduction of paw edema swelling compared to pure DC and DC-LP. Our findings revealed that encapsulation of DC in BMs matrix is a good alternative for improvement of therapeutic efficacy.

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Formulation and evaluation of co-prodrug of flurbiprofen and methocarbamol

Cited by 11 publications

References 16 publications

Comparison of the Utility of RP-TLC Technique and Different Computational Methods to Assess the Lipophilicity of Selected Antiparasitic, Antihypertensive, and Anti-inflammatory Drugs

Comparison of the Utility of RP-TLC Technique and Different Computational Methods to Assess the Lipophilicity of Selected Antiparasitic, Antihypertensive, and Anti-inflammatory Drugs

Transcriptomic Analysis of Fuzi Lizhong Decoction for the Treatment of Stomach Ulcers

Development and Optimization of Nanolipid-Based Formulation of Diclofenac Sodium: In Vitro Characterization and Preclinical Evaluation

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