Manufacture of High-Purity Meloxicam via Its Novel Potassium Salt Monohydrate

Mezei, Tibor; Mesterházy, Norbert; Bakó, Tibor; Porcs-Makkay, Márta; Simig, Gyula; Volk, Balázs

doi:10.1021/op900031h

Cited by 37 publications

(31 citation statements)

References 18 publications

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“…Another option for the inhalable microcomposite preparation is the use of MX potassium salt form and additional excipients (Poly-vinyl alcohol, leucine) (Chvatal et al, 2017). Due to the water solubility of the MX salt (Mezei et al, 2009), an easier feed stock preparation and spray drying conditions could be developed, leading to amorphous MX (Chvatal et al, 2017).…”

Section: Introductionmentioning

confidence: 99%

Formulation and comparison of spray dried non-porous and large porous particles containing meloxicam for pulmonary drug delivery

Chvatal

Ambrus

Party

et al. 2019

International Journal of Pharmaceutics

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Meloxicam is an anti-inflammatory drug that could be interesting to deliver locally to the lungs to treat inflammation occurring in cystic fibrosis or chronic obstructive pulmonary disease (COPD). Spray drying conditions were optimized to prepare inhalable dry powders, from meloxicam aqueous solution with pH adjustment. A comparison study between non-porous and large porous particles (LPPs) was carried out to demonstrate the relevance of the aimed large size (>5 µm) and low density (<0.2 mg/cm 3) formulations. With the appropriate amount of porogen agent, ammonium bicarbonate, LPPs exhibited the same aerodynamic diameter and a higher deposited fraction than smaller but dense particles. The aerodynamic evaluation of LPPs showed that the fine particle fraction (FPF) reached up to 65.8%, while the emitted fraction (EF) reached 85.4%, both higher than for the non-porous particles. Stability tests demonstrated that, after 10 weeks of storage, no significant difference could be detected in the aerodynamic behaviour of the formulations. To the best of our knowledge this is the first time large porous particles, with enhanced aerodynamic properties, from an aqueous solution of meloxicam are reported.

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Section: Introductionmentioning

confidence: 99%

Formulation and comparison of spray dried non-porous and large porous particles containing meloxicam for pulmonary drug delivery

Chvatal

Ambrus

Party

et al. 2019

International Journal of Pharmaceutics

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“…To decrease the time to reach the therapeutic concentration and accelerate the onset of action, numerous meloxicam-based formulations have been prepared and evaluated with respect to aqueous solubility. [28][29][30][31] In spite of all the efforts that were taken, a faster onset oral dosage form of meloxicam remains absent to date. Given the fact that pharmaceutical cocrystals can influence the physicochemical properties of APIs including solubility, a study was designed and performed to explore their effect on improving the solubility and subsequently the onset of action of meloxicam.…”

Section: Introductionmentioning

confidence: 99%

Coformer Selection in Pharmaceutical Cocrystal Development: a Case Study of a Meloxicam Aspirin Cocrystal That Exhibits Enhanced Solubility and Pharmacokinetics

Cheney

Weyna

Shan³

et al. 2011

Journal of Pharmaceutical Sciences

219

151

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“…In vitro and in vivo investigations of micro- and nanonized MEL-containing IN formulations, prepared with combined wet milling, were performed, which showed better diffusion and a higher plasma AUC of the nanosized MEL-containing formulation compared to the raw or micronized drug [ 24 ]. The bioavailability of the salt form of MEL (meloxicam potassium monohydrate—MELP) [ 25 , 26 ] was also investigated [ 27 ]. MELP revealed a higher permeability through the synthetic membrane and a higher plasma concentration compared to the MEL-containing formulation.…”

Section: Introductionmentioning

confidence: 99%

Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems

et al. 2018

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The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with nanonized meloxicam (nano MEL spray) and its salt form known as meloxicam potassium monohydrate (MELP spray). The physicochemical properties and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out. These forms were first investigated in “nose-to-brain” relation. It was found that the in vitro study and in vivo study did not show any significant correlation. In vitro experiments demonstrated faster dissolution rate and higher diffusion of MELP from the spray compared with the nano MEL spray. The administration of the nano MEL spray resulted in faster absorption and constant plasma concentration of the drug after five minutes of administration as compared to MELP. The axonal transport of the drug was justified. MEL appeared in the brain tissues after the first five minutes of administration in the case of both spray forms, but its amount was too small in comparison with the total plasma concentration. The application of the nano MEL spray resulted in the same AUC in the brain as the intravenous injection. The “nose-to-blood” results predicted the nasal applicability of MEL and MELP in pain management. The “nose-to-brain” pathway requires further study.

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Manufacture of High-Purity Meloxicam via Its Novel Potassium Salt Monohydrate

Cited by 37 publications

References 18 publications

Formulation and comparison of spray dried non-porous and large porous particles containing meloxicam for pulmonary drug delivery

Formulation and comparison of spray dried non-porous and large porous particles containing meloxicam for pulmonary drug delivery

Coformer Selection in Pharmaceutical Cocrystal Development: a Case Study of a Meloxicam Aspirin Cocrystal That Exhibits Enhanced Solubility and Pharmacokinetics

Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems

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