Formulation and evaluation of fexofenadine hydrochloride orally disintegrating tablets for pediatric use

WOS: 000428979600026Allergic rhinitis is a common disease in children which has considerable negative effects on the quality of life. Fexofenadine hydrochloride (FFH) is a second-generation oral antihistamine which has been widely perscribed for alleviating symptoms of AR in children. The aim of this study was to take the advantage of convenient direct compression method for preparation of Orally Disintegrating Tablets (ODTs) containing 30 mg FFH per tablet. Six ready-to-use commercial tablet excipients (F-Melt (R), Pearlitol (R) Flash, Pharmaburst (R) 500, Prosolv (R) Easytab SP, Ludiflash (R), Parteck (R) ODT (R)) were used for direct compression and suitability of these excipients were evaluated. ODTs could be successfully compressed with all the investigated excipients and all of the formulations exhibited acceptable crushing stregth, low friability and remarkably short disintegration time. The ODTs which were able to possess a disintegration time below 30 s were considered eligible for further studies. In vitro dissolution studies showed a complete release of the drug from ODTs made from Pharmaburst (R) 500 within 15 min. Short term stability results exhibited no significant change of the drug in tested formulations. In conclusion, FFH containing ODTs formulated with Pharmaburst (R) 500 were determined explicitly the most promising formulation when compressed at a force of 1000 kg.Yuzuncu Yil University FoundationYuzuncu Yil University [2013-SBE YL 049]; TR Prime Ministry State Planning Organization FoundationTurkiye Cumhuriyeti Kalkinma Bakanligi [09/DPT/001]The authors would like to thank Prof. Dr. Idris Turel from Adiyaman University, Faculty of Pharmacy, Department of Pharmacology. This study was supported by Yuzuncu Yil University Foundation (Project Number: 2013-SBE YL 049). The authors would also like to thank to the TR Prime Ministry State Planning Organization Foundation (Project Number 09/DPT/001)

EVALUATION OF MICROEMULSION FORMULATIONS FOR PARENTERAL DRUG DELIVERY OF APROTININ: FORMULATION, DESIGN AND STABILITY STUDIES

WOS: 00020934590008

A comprehensive in vitro and in vivo evaluation of thiolated matrix tablets as a gastroretentive delivery system

WOS: 000292878600003PubMed ID: 21463156The aim of this study was to investigate the potential of thiolated matrix tablets for gastroretentive delivery systems. Poly(acrylic acid)-cysteine (PAA-Cys) and chitosan-4-thiobuthylamidine (chitosan-TBA) were evaluated as anionic and cationic thiolated polymers and riboflavin was used as a model drug. Tablets were prepared by direct compression and each formulation was characterized in terms of disintegration, swelling, mucoadhesion, and drug release properties. Thereafter, the gastric residence times of tablets were determined with in vivo study in rats. The resulting PAA-Cys and chitosan-TBA conjugates displayed 172.80 +/- 30.33 and 371.11 +/- 72.74 mu mol free thiol groups, respectively. Disintegration studies demonstrated the stability of thiolated tablets up to 24 h, whereas tablets prepared with unmodified PAA and chitosan disintegrated within a time period of 1 h. Mucoadhesion studies showed that mucoadhesion work of PAA-Cys and chitosan-TBA tablets were 1.341- and 2.139-times higher than unmodified ones. The mucoadhesion times of PAA, PAA-Cys, chitosan, and chitosan-TBA tablets were 1.5 +/- 0.5, 21 +/- 1, 1 +/- 0.5, 17 +/- 1 h, respectively. These results confirm the theory that thiol groups react with mucin glycoproteins and form covalent bonds to the mucus layer. Release studies indicated that a controlled release was provided with thiolated tablets up to 24 h. These promising in vitro results of thiolated tablets were proved with in vivo studies. The thiolated tablets showed a gastroretention time up to 6 h, whereas unmodified tablets completely disintegrated within 1 h in rat stomach. Consequently, the study suggests that thiolated matrix tablets might be promising formulations for gastroretentive delivery systems.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK); Ege UniversityEge University [08/ECZ/010]The scholarship for this work was financed by The Scientific and Technological Research Council of Turkey (TUBITAK). Also this work was supported by Ege University (Project no: 08/ECZ/010)

Strategies to Prolong the Intravaginal Residence Time of Drug Delivery Systems

WOS: 000272231000007PubMed ID: 20067707The vagina has been studied as a suitable site for local and systemic delivery of drugs. There are a large number of vaginal medications on the market. Most of them, however, require frequent applications due to their short vaginal residence time. A prolonged vaginal residence time of formulations is therefore a key parameter for improved therapeutic efficacy. Promising approaches for prolonging the residence time base on mucoadhesion, were in- situ sol-to-gel transition and mechanical fixation. Mucoadhesive drug delivery systems can be tailored to adhere to the vaginal tissue. In-situ gelling systems offer the advantage of increased viscosity in vaginal cavity and consequently reduce outflow from the vagina. Mechanical fixation needs specially shaped drug delivery systems and reduce the frequency of administration significantly. In this review, an overview on these different strategies and systems is provided. Furthermore, the techniques to evaluate the potential of these systems for prolonged vaginal residence time are described

Gastroretentive particles formulated with thiomers: development and in vitro evaluation

WOS: 000277364900004PubMed ID: 20021230Permeation studies were performed with freshly excised stomach mucosa from rats. Polymers and combination with glutathione were evaluated for permeation enhancing properties. Furthermore, particles were prepared by air jet milling and characterized. Permeation studies showed that the apparent permeability coefficients for RF5'PNa with thiomers and glutathione are 1.511-fold and 2.354-fold higher than control, respectively. It can be seen from the results glutathione in combination with thiomers has a significant influence for increasing permeation. Poly(acrylic acid)-cysteine and chitosan-4-thiobuthylamidine particles demonstrated a mean diameter of 336.5 +/- 16.5 and 396.3 +/- 17.0 nm and zeta potential of -19.98 +/- 1.015 and 27.15 +/- 0.500 mV, respectively. The drug loading of Poly(acrylic acid) particles was significantly higher than chitosan particles. The release rate of RF5'PNa from the thiolated particles was slower compared with unmodified particles. Moreover, thiolated particles showed higher mucoadhesive properties compared to unmodified particles. Overall, thiolated particles of both anionic and cationic polymers had improved mucoadhesive and controlled release properties. Therefore, they could be promising for gastroretentive delivery systems.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK)The scholarship for this work was financed by The Scientific and Technological Research Council of Turkey (TUBITAK)

Evaluation of chitosan based vaginal bioadhesive gel formulations for antifungal drugs

WOS: 000337705100001PubMed ID: 24914716The aim of the present study was to evaluate chitosan as a vaginal mucoadhesive gel base for econazole nitrate and miconazole nitrate. To this aim, different types of chitosan with different molecular masses and viscosity properties [low molecular mass chitosan (viscosity: 20,000 mPa s), medium molecular mass chitosan (viscosity: 200,000 mPa s), high molecular mass chitosan (viscosity: 800,000 mPa s)] have been used. First, rheological studies were conducted on chitosan gels. Mechanical, syringeability and mucoadhesive properties of chitosan gels were determined. Release profiles of econazole nitrate and miconazole nitrate from chitosan gels were obtained and evaluated kinetically. In addition, anticandidal activities of formulations were determined. Finally, vaginal retention of chitosan gels in rats was evaluated by in vivo distribution studies. Based on the results, it can be concluded that gels prepared with medium molecular mass chitosan might be effectively used for different antifungal agents in the treatment of vaginal candidiosis, since it has high mucoadhesiveness, suitable mechanical and release properties with good vaginal retention.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [106/S/196]This work is a part of the authors' research project (No. 106/S/196) supported by the Scientific and Technological Research Council of Turkey (TUBITAK)