Permeation Efficacy of a Transdermal Vehicle with Steroidal Hormones and Nonsteroidal Anti-inflammatory Agents as Model Drugs

2018 ◽  
Vol 16 (2) ◽  
pp. 136-141
Author(s):  
Laura A. Junqueira ◽  
Hudson Polonini ◽  
Sharlene Loures ◽  
Nádia R.B. Raposo ◽  
Anderson O. Ferreira ◽  
...  

Background: Transdermal delivery is an alternative route for the administration of drugs. However, it requires the development of vehicles that allow the drugs to cross the layers of the skin and reach the systemic circulation. Objective: In this study, a new transdermal vehicle was evaluated using progesterone, estradiol, estradiol + estriol (Biest) and ketoprofen administered as model drugs. </P><P> Methods: To evaluate the ex vivo permeation of the drugs, the Franz vertical diffusion cell with human skin was used. Results: After 24 h, the vehicle was able to deliver 18.32 &#181;g/cm2 of progesterone and 92.07 &#181;g/cm2 of ketoprofen through the skin to the receptor medium. The permeation percentages were 91%, 78.8%, 48.5%, 73.2%, and 63.6%, respectively, for estradiol, estradiol (Biest), estriol (Biest), progesterone and ketoprofen. For all drugs, sufficient amounts were delivered to achieve a systemic effect, and it was also possible to decrease the amount of emulsion applied. Thus, the vehicle demonstrated a high performance and the possibility of it being used for drugs that present difficulties in regards to administration by the transdermal route.

1999 ◽  
Vol 179 (1) ◽  
pp. 129-134 ◽  
Author(s):  
Jagdish Jaiswal ◽  
Ramarao Poduri ◽  
Ramesh Panchagnula

Author(s):  
Harmanpreet Singh ◽  
Pooja Jaiswal ◽  
Suksham Gupta ◽  
Simerjit Singh

  Objective: The current investigation deals with formulation and evaluation of fast disintegrating sublingual tablets of rizatriptan benzoate (RTB) to produce its intended therapeutic effect for acute treatment of migraine. When the drug is given by sublingual route, it overcomes the first pass metabolism and quick entry of drug in systemic circulation is obtained. It would result in fast pharmacological response hence faster relief from migraine which is an important criterion in migraine therapy.Methods: In this study, RTB sublingual tablets were prepared using direct compression process using various bioadhesive polymers such as sodium carboxymethyl cellulose, hydroxyl propyl methyl cellulose-K4M, and chitosan at various concentration ranging 0.5-5% w/w along with sodium starch glycolate (SSG) or cross carmellose sodium (CCS) as super disintegrants at different concentration ranging 2-8% w/w.Results: The tablets disintegrated quickly and dissolution tests conclude that RTB was released from the formulation within the compendial limits. The formulations batches (A8 and B8) containing 2% w/w chitosan along with 2% w/w SSG or CCS which disintegrate rapidly and show high dissolution and ex vivo permeation were selected as optimized formulations.Conclusion: The results obtained from the study showed that the bioavailability problem of the drug has been solved as the drug is given by sublingual route and it directly enters into systemic circulation. Furthermore, the formulation overcomes the problems associated with migraine attack as fast disintegrating technology is used.


2017 ◽  
Vol 38 ◽  
pp. 59-71 ◽  
Author(s):  
Biswarup Das ◽  
Suma Oomen Sen ◽  
Ruma Maji ◽  
Amit Kumar Nayak ◽  
Kalyan Kumar Sen

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