Effect of solubility enhancement on nasal absorption of meloxicam

Besides the opioids the standard management of the World Health Organization suggests NSAIDs (non-steroidal anti-inflammatory drugs) alone or in combination to enhance analgesia in malignant and non-malignant pain therapy. The applicability of NSAIDs in a nasal formulation is a new approach in pharm...

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Elmentve itt :
Bibliográfiai részletek
Szerzők: Horváth Tamás
Ambrus Rita
Völgyi Gergely
Budai-Szűcs Mária
Márki Árpád
Sipos Péter
Bartos Csilla
Seres Adrienn
Sztojkov-Ivanov Anita
Takács-Novák Krisztina
Csányi Erzsébet
Gáspár Róbert
Szabó-Révész Piroska
Dokumentumtípus: Cikk
Megjelent: Elsevier 2016
Sorozat:EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES 95
doi:10.1016/j.ejps.2016.05.031

mtmt:3076538
Online Access:http://publicatio.bibl.u-szeged.hu/8156
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520 3 |a Besides the opioids the standard management of the World Health Organization suggests NSAIDs (non-steroidal anti-inflammatory drugs) alone or in combination to enhance analgesia in malignant and non-malignant pain therapy. The applicability of NSAIDs in a nasal formulation is a new approach in pharmaceutical technology. In order to enhance the nasal absorption of meloxicam (MX) as an NSAID, its salt form, meloxicam potassium monohydrate (MXP), registered by Egis Plc., was investigated in comparison with MX. The physico-chemical properties of the drugs (structural analysis, solubility and dissolution rate) and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out to determine the nasal applicability of MXP as a drug candidate in pain therapy. It can be concluded that MX and MXP demonstrated the same equilibrium solubility at the pH5.60 of the nasal mucosa (0.017mg/ml); nonetheless, MXP indicated faster dissolution and a higher permeability through the synthetic membrane. The animal studies justified the short Tmax value (15min) and the high AUC of MXP, which is important in acute pain therapy. It can be assumed that the low mucoadhesivity of MXP spray did not increase the residence time in the nasal cavity, and the elimination from the nasal mucosa was therefore faster than in the case of MX. Further experiments are necessary to prove the therapeutic relevance of this MXP-containing innovative intranasal formulation. 
700 0 1 |a Ambrus Rita  |e aut 
700 0 1 |a Völgyi Gergely  |e aut 
700 0 2 |a Budai-Szűcs Mária  |e aut 
700 0 2 |a Márki Árpád  |e aut 
700 0 2 |a Sipos Péter  |e aut 
700 0 2 |a Bartos Csilla  |e aut 
700 0 2 |a Seres Adrienn  |e aut 
700 0 2 |a Sztojkov-Ivanov Anita  |e aut 
700 0 2 |a Takács-Novák Krisztina  |e aut 
700 0 2 |a Csányi Erzsébet  |e aut 
700 0 2 |a Gáspár Róbert  |e aut 
700 0 2 |a Szabó-Révész Piroska  |e aut 
856 4 0 |u http://publicatio.bibl.u-szeged.hu/8156/1/Effect_of_solubility_enhancement_on_nasal_absorption_of_meloxicam_u.pdf  |z Dokumentum-elérés