Drug-excipient compatibility assessment of solid formulations containing meloxicam

Silveira, Lucas Melo da; Fiorot, Ariadne Botto; Xavier, Thiago Padovani; Yoshida, María Irene; Oliveira, Marcos Antônio de

doi:10.1016/j.ejps.2017.11.015

Cited by 25 publications

(18 citation statements)

References 13 publications

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“…Solid-state reactions can occur in drugs and formulations, possibly initiating alterations in their stability, solubility, dissolution rates and bioavailability. Therefore, compatibility studies are necessary to ensure that potential physical and chemical interactions between API and excipient do not compromise drug stability [5].…”

Section: Resultsmentioning

confidence: 99%

“…Furthermore, after the binary mixing of two ingredients, shifts in the transition temperature and peak shape and area invariably occur without necessarily representing a harmful interaction, so these changes need to be carefully evaluated [5]. Moreover, in the case of APIs that decompose without melting, omeprazole sodium for example, the search for incompatibility is problematic [6].…”

Section: Introductionmentioning

confidence: 99%

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DSC supported by factor analysis as a reliable tool for compatibility study in pharmaceutical mixtures

Rojek

Wesołowski

2019

J Therm Anal Calorim

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A chemometrically optimized DSC interpretation was developed for the identification of compatibility/incompatibility between active pharmaceutical ingredients (APIs) and excipients in pharmaceutical preparations. The chemometric approach based on factor analysis (FA) can be used as a supplementary tool for incompatibility detection in theophylline mixtures with excipients. The FA results expose the formation of two distinctly separate clusters on the FA score scatter plots-in the case of mixtures with compatible ingredients, one cluster was formed by theophylline and mixtures with high API content, the second by excipient and mixtures with high excipient content. In the event of incompatibility, the DSC curves of binary mixtures differ from those of ingredients, and the FA score scatter plot displays one cluster consisting of some mixtures at different ratios and the other of remaining mixtures and both ingredients. In brief, FA proved the incompatibility of theophylline mixtures with arabic gum, glucose, sorbitol and sucrose. The application of FA can help to circumvent the misinterpretation of DSC data.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

DSC supported by factor analysis as a reliable tool for compatibility study in pharmaceutical mixtures

Rojek

Wesołowski

2019

J Therm Anal Calorim

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“…A p < 0.05 was accepted as significant.3 | RESULTS AND DISCUSSION3.1 | Differential scanning calorimetry analysisAny possible interactions or incompatibilities among IMA, DEX, and excipients were investigated using DSC. There were no differences in melting point between separate substances and their mixtures (DSC thermograms are shown as(Da Silveira, Fiorot, Xavier, Yoshida, & de Oliveira, 2018) indicating no interactions.…”

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confidence: 99%

Efficacy of targeted liposomes and nanocochleates containing imatinib plus dexketoprofen against fibrosarcoma

Çoban

Değim

Yılmaz³

et al. 2019

Drug Development Research

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The main challenges in treating cancer using chemotherapeutics are insufficient dose at the target site and the development of drug resistance, while higher doses can induce side effects by damaging nontarget tissues. Combinatorial drug therapy may overcome these limitations by permitting lower doses and more specific targeting, thereby mitigating drug resistance and nontarget side effects. Recent reports indicate that nonsteroidal anti-inflammatory drugs (NSAIDs) have anticancer potential and can be used together with conventional chemotherapeutics to improve efficacy and safety. In the present study, imatinib mesylate and dexketoprofen trometamol were selected as model drugs to develop targeted surface-modified liposome and nanocochleate formulations for fibrosarcoma treatment. The physicochemical properties and in vitro efficacy of various formulations were evaluated by measurement of particle size distribution, polydispersity index, zeta potential, encapsulation efficiency, diffusion through Caco-2 cells, and toxicity in culture. Selected formulations were then evaluated in fibrosarcoma-bearing model mice by histopathological observations and tyrosine kinase receptor inhibition assays.The most effective formulation on the fibrosarcoma model was a PEGylated nanocochleate formulation. These findings provide a foundation for developing more effective formulations and chemotherapeutic strategies for the treatment of fibrosarcoma and other types of cancer.

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“…Meloxicam (MEL) [4‐hydroxy‐2‐methyl‐N‐(5‐methyl‐2‐thiomethyl)‐2H‐1,2‐benzothiazide‐3‐formamide‐1,1‐dioxide], a new NSAID of enolamide class, which has remarkable analgesic and anti‐inflammatory effects (Adawaren, Mukandiwa, Mukandiwa, Chipangura, Wolter, & Naidoo, ; Haiting Wang & Tan, ; Naidu et al, ). It is a preferably cyclooxygenase‐2 (COX‐2) inhibitor with a lower incidence of gastrointestinal side effects and a faster onset effect compared with COX‐nonselective NSAIDs or COX‐1‐selective NSAIDs (El‐Awdan, Al‐Shafeey, Al‐Shafeey, Salam, El‐Iraqy, & Kenawy, ; Khan, Paulson, Paulson, Verburg, Lefkowith, & Maziasz, ; Lihua Cao, ; Louder et al, ; da Silveira, Fiorot, Fiorot, Xavier, Yoshida, & Oliveira, ; Urayama et al, ). Approved formulations include MEL oral suspension, injectable solution, and transmucosal oral spray.…”

Section: Introductionmentioning

confidence: 99%

“…. It is a preferably cyclooxygenase-2 (COX-2) inhibitor with a lower incidence of gastrointestinal side effects and a faster onset effect compared with COXnonselective NSAIDs or COX-1-selective NSAIDs (El-Awdan, Al-Shafeey, Al-Shafeey, Salam, El-Iraqy, & Kenawy, 2015;Khan, Paulson, Paulson, Verburg, Lefkowith, & Maziasz, 2002;Lihua Cao, 2011;Louder et al, 2011;da Silveira, Fiorot, Fiorot, Xavier, Yoshida, & Oliveira, 2018;Urayama et al, 2019). Approved formulations include MEL oral suspension, injectable solution, and transmucosal oral spray.…”

mentioning

confidence: 99%

Pharmacokinetics and relative bioavailability of meloxicam oil suspension in pigs after intramuscular administration

Liu

Guo

Jiang

et al. 2019

Vet Pharm & Therapeutics

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This study aimed to develop one novel meloxicam (MEL) oil suspension for sustained‐release and compare the pharmacokinetic characteristics of it with MEL conventional formulation in pigs after a single intramuscular administration. Six healthy pigs were used for the study by a crossover design in two periods with a withdrawal interval of 14 days. Plasma concentrations of MEL were measured by ultra‐performance liquid chromatography–tandem mass spectrometry (UPLC‐MS/MS). Pharmacokinetic parameters were calculated by noncompartmental methods. The difference was statistically significant (p < .05) between MEL oil suspension and MEL conventional formulation in pharmacokinetic parameters of mean residence time (6.16 ± 4.04) hr versus (2.66 ± 0.55) hr, peak plasma concentration (Cmax) (0.82 ± 0.12) µg/ml versus (1.12 ± 0.22) µg/ml, time needed to reach Cmax (Tmax) (2.33 ± 0.82) hr versus (0.59 ± 0.18) hr, and terminal elimination half‐life (t1/2λz) (3.74 ± 2.66) hr versus (1.55 ± 0.37) hr. The mean area under the concentration–time curve (AUC0–∝) of MEL oil suspension and MEL conventional formulation was 5.35 and 3.43 hr µg/ml, respectively, with a relative bioavailability of 155.98%. Results of the present study demonstrated that the MEL oil suspension could prolong the effective time of drugs in blood, thereby reducing the frequency of administration on a course of treatment. Therefore, the novel MEL oil suspension seems to be of great value in veterinary clinical application.

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Drug-excipient compatibility assessment of solid formulations containing meloxicam

Cited by 25 publications

References 13 publications

DSC supported by factor analysis as a reliable tool for compatibility study in pharmaceutical mixtures

DSC supported by factor analysis as a reliable tool for compatibility study in pharmaceutical mixtures

Efficacy of targeted liposomes and nanocochleates containing imatinib plus dexketoprofen against fibrosarcoma

Pharmacokinetics and relative bioavailability of meloxicam oil suspension in pigs after intramuscular administration

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