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Tytuł pozycji:

Tolmetin sodium-loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks.

Tytuł :
Tolmetin sodium-loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks.
Autorzy :
Akl MA; a Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys) , Al-Azhar University , Nasr City , Cairo , Egypt.
Ismael HR; a Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys) , Al-Azhar University , Nasr City , Cairo , Egypt.
Abd Allah FI; a Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys) , Al-Azhar University , Nasr City , Cairo , Egypt.; b Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy , Egyptian Russian University , Bader City , Cairo , Egypt.
Kassem AA; a Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys) , Al-Azhar University , Nasr City , Cairo , Egypt.
Samy AM; a Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys) , Al-Azhar University , Nasr City , Cairo , Egypt.
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Źródło :
Drug development and industrial pharmacy [Drug Dev Ind Pharm] 2019 Feb; Vol. 45 (2), pp. 252-264. Date of Electronic Publication: 2018 Oct 31.
Typ publikacji :
Journal Article
Język :
English
Imprint Name(s) :
Publication: London : Informa Healthcare
Original Publication: New York, Dekker.
MeSH Terms :
Anti-Inflammatory Agents, Non-Steroidal/*administration & dosage
Tolmetin/*administration & dosage
Administration, Oral ; Administration, Rectal ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics ; Anti-Inflammatory Agents, Non-Steroidal/toxicity ; Biological Availability ; Capsules ; Chemical and Drug Induced Liver Injury/metabolism ; Drug Compounding ; Gels ; Humans ; Male ; Poloxamer ; Rabbits ; Rats, Sprague-Dawley ; Suppositories ; Temperature ; Tissue Adhesives ; Tolmetin/pharmacokinetics ; Tolmetin/toxicity
Contributed Indexing :
Keywords: Tolmetin Sodium; bioavailability; mucoadhesive; pharmacodynamics effects; rectal delivery; thermosensitive liquid suppository
Substance Nomenclature :
0 (Anti-Inflammatory Agents, Non-Steroidal)
0 (Capsules)
0 (Gels)
0 (Suppositories)
0 (Tissue Adhesives)
106392-12-5 (Poloxamer)
D8K2JPN18B (Tolmetin)
Entry Date(s) :
Date Created: 20181011 Date Completed: 20190701 Latest Revision: 20190701
Update Code :
20210301
DOI :
10.1080/03639045.2018.1534858
PMID :
30303407
Czasopismo naukowe
Tolmetin sodium (TS) is a nonsteroidal anti-inflammatory drug (NSAID) indicated for treatment of musculoskeletal issues. As other NSAID, TS displays a marked side effects on the gastro-intestinal (GI) tract after oral administration. Traditional solid suppositories can cause pain and discomfort for patients, may reach the end of the colon; consequently, the drug can undergo the first-pass effect. TS liquid suppository (TS- LS ) was developed to enhance patient compliance and rectal mucosal safety in high-risk patients receiving highly NSAID therapy. This work was conducted to optimize and evaluate Poloxamer P407/P188-based thermoresponsive TS- LS by using mucoadhesive polymers such as methylcellulose (MC). TS- LS was prepared by cold method and characterized their in vitro physicochemical properties as gelation temperature (GT), gel strength, bioadhesive properties, and in vitro release. The safety of the prepared suppository on rectum, stomach, and liver was evaluated histologically. Pharmacokinetic analyses were performed to compare rectal TS- LS to orally Rhumtol ® capsules. The results showed that the optimized TS- LS ; composed of P407/P188/MC (21/9/0.5% w/w) displayed gelation at rectum temperature ∼32.90 °C, gel strength of 21.35 s and rectal retention force at the administration site of 24.25 × 10 2  dyne/cm 2 . Moreover, TS- LS did not cause any morphological damage to the rectal tissues. Pharmacokinetic parameters of optimized TS- LS formulation revealed 4.6 fold increase in bioavailability as compared to Rhumtol ® capsules. Taken together, the results demonstrated that liquid suppository is a potential and physically safe rectal delivery carrier for improvement rectal bioavailability and in vivo safety of TS.
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