Recently, the fast disintegrating tablet (FDT) has started gaining popularity and acceptance as a new drug delivery system. Lubricants could influence on disintegration time (DT), hardness, wetting time (WT) and dissolution of FDT. This study investigated the effects of amount and type of lubricants (magnesium stearate and sodium stearyl fumarate) as well as compression force on characteristics of the cetirizine dihydrochloride (CD) FDT. The spatial distribution of lubricants in tablets had been analyzed using Raman mapping and scanning electron microscopy–energy dispersive X-ray spectroscopy. The more concentration of lubricants or higher compression force resulted in more distribution of lubricant therefore hindering water penetration into the tablet. In addition, CD FDT was prepared by direct compression method. A 32 full factorial design was applied for the optimization of CD FDT. By adopting a systematic formulation approach, the closeness between predicted and observed values (DT, WT, contact angle, surface free energy, hardness) indicated the validity of derived equations for the dependent variables. Sodium stearyl fumarate had less impact on hardness and disintegration time than magnesium stearate. Therefore, FDT containing sodium stearyl fumarate as lubricant showed higher drug release than that containing magnesium stearate.
Cetirizine dihydrochloride has a very unpleasant bitter taste. To mask the bitter taste, complexation with beta-cyclodextrin using ethanol as a kneading solvent was investigated and evaluated by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, thermogravimetric analysis, simultaneous X-ray diffractometry-differential scanning calorimetry measurement and H-1-nuclear magnetic resonance spectroscopy. Taste was evaluated by human volunteers using an unstructured line scale. The basic characterization of the prepared tablets including in vivo disintegration time and drug dissolution was studied. Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffractometry data confirmed the inclusion complex formation. Thermogravimetric analysis, simultaneous X-ray diffractometry-differential scanning calorimetry measurements revealed the reduction of crystalline beta-cyclodextrin due to the displacement of water molecules from complex formation. Proton nuclear magnetic resonance spectroscopy indicated an intermolecular interaction between protons of cetirizine dihydrochloride with the cavity of beta-cyclodextrin. The prepared complex showed an unstructured line scale with apparent low average rating of 1.70. The inclusion complex-loaded fast disintegrating tablet prepared with direct compression had short disintegration time and good taste with an unstructured line scale with average rating of 0.28. Cetirizine dihydrochloride, beta-cyclodextrin inclusion complex was successfully prepared by kneading method using ethanol as solvent. The inclusion complex-loaded fast disintegrating tablet had good taste and good perception in the mouth.
ปรัชญา เกตวุงศา*, ธวชัชยั แพชมัด และ ลาวัลย ์ศรัทธาพุทธ Prachya Katewongsa*, Thawatchai Phaechamud and Lawan Sratthaphut 1 ภาควชิาเทคโนโลยเีภสชักรรม คณะเภสชัศาสตร ์มหาวทิยาลยัศลิปากร นครปฐม 1 ภาควชิาสารสนเทศสขุภาพ คณะเภสชัศาสตร ์มหาวทิยาลยัศลิปากร นครปฐม Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand Department of Health-Related Informatics, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand
Recently, the fast disintegrating tablet (FDT) has started gaining popularity and acceptance as new drug delivery system. Cetirizine dihydrochloride (CD) is the selective histamine (H-1)-receptor antagonist that is demonstrated to treat the symptoms associated with seasonal and perennial allergic rhinitis which this drug nowadays was prepared in form of FDT. Lubricant typically influences on tablet disintegration time (DT) and wetting time (WT). Therefore, it is important for optimizing the lubricant amount in this dosage form. The purpose of this study was to evaluate the effect of the lubricants (magnesium stearate (Mg-st) and sodium stearyl fumarate (SSF)) on the CD tablet containing highly loaded colloidal silicon dioxide. Mg-St was well known as a high hydrophobic lubricant and that sodium stearyl fumarate (SSF) is less hydrophobic than Mg-St. Therefore, the DT and WT of tablets containing Mg-St increased as the amount of Mg-st increased. However, the DT and WT of FDT were influenced not only by lubricant properties, but by hardness. The polarity of the surface tablets was remarkably decreased by increased the amount of Mg-st which related to the WT of FDT. Therefore, the contact angle of tablets increased and SFE decreased. On the other hand, the polarity of the surface tablets was remarkably increased by increased the amount of SSF.
Cork tree (Sonneratia caseolaris (L.) Engl., family Sonneratiaceae) found in estuarine and tidal creek landscape and mangrove area. Cork tree extract has antioxidant and antimicrobial activity. The aim of this research was to develop liquid soap base containing cork tree extract prepared by beaker method using Cocamide DEA and Cocamidopropyl betaine as foam booster, Texapon N70 and Empigen OB as surface active agent and Eumulgin E033 as viscosity inducing agent as well as solubilizer. The most appropriate formula consisted of Cocamide DEA 2 %w/w, Cocamidopropyl betaine 5 % w/w, propylene glycol 2%w/w, Empigen OB 20%, Eumulgin E033 3 %w/w, Nmethyl pyrrolidone 5 %w/w and cork tree extract 1 %w/w. Liquid soap represented the rheological behavior as newtonian flow. The antimicrobial activity of liquid soap containing NMP against S. aureus was shown in this research.
Virgin coconut oil (VCO) is gaining wide popularity in the scientic eld and among the public. The purpose of this research was to develop the non-aqueous hair gel by dispersing hydrophilic colloidal silicon dioxide (Aerosil 200) or hydrophobic colloidal silicon dioxide (Aerosil R 972) into virgin coconut oil and to determine the effect of Aerosil type on physical properties of prepared hair gel. Texture analysis and satisfied evaluation of prepared system were also conducted. At a suitable amount of Aerosil 200 and Aerosil R 972, the three-dimensional network led to the immobilization of a dispersing medium. The viscosity of the prepared gel was increased as the amount of Aerosil 200 or Aerosil R 972 was increased. However, the viscosity of gel containing Aerosil 200 was apparently higher than system prepared from Aerosil R 972. The rheological behavior of these gels depended on type and concentration of colloidal silicon dioxide. From texture analysis, the hardness and adhesion of systems comprising Aerosil 200 were higher than that containing Aerosil R 972 with concentration dependence. Satisfied evaluation by a panel consisting of human volunteers demonstrated that the developed non-aqueous virgin coconut oil gel could be used as the hair setting gel.
Disintegrants had influence on disintegration time and dissolution for fast disintegrating tablet (FDTs). Therefore, the purpose of this study was to evaluate the effect of disintegrant type on the characteristics of FDTs. In this research, the tablets were fabricated by direct compression with the compression force of 1.5 tons and using the different disintegrants components (chitin, chitosan, xylitol, microcrystalline celluloses, white bentonite and magnabite F). The physical properties of these tablets were determined. The xylitol tablets were rapidly disintegrated within 7 +/- 1 s, whereas that of the others was longer than 30 mins The tablets containing the mixture of xylitol and other materials were subsequently fabricated since the hardness of the xylitol tablet was very poor. The disintegration time and wetting time of tablets containing 9:1 xylitol:Avicel PH101 was shorter than that of the others. The contact angle of tablets containing xylitol and Avicel PH101 at the ratio of 9:1 was lowest and surface free energy (SFE) of them was highest compared with the other formula. Moreover, scanning electron microscope (SEM) displayed that xylitol and tablets containing 9:1 xylitol:Avicel PH101 had no disordered arrangement, therefore it could promote the disintegrating property effectiently.
The aim of our study was to evaluate the applicability of yam (Dioscorea sp.) starch and arrowroot (Maranta arundinacea) starch as suspending agents in suspension. Paracetamol was used as a model drug because of its low solubility. It was found that the optimal concentration as suspending agent in paracetamol suspension was in the range of 7-8% for yam starch and 5-6% for arrowroot starch. All formulations were stable within the period of study with pH of 5.4-6.9. These results were comparable to those obtained from the sodium carboxymethyl cellulose (sodium CMC) which is a common suspending agent. It could be concluded that yam starch and arrowroot starch showed suspending activity in paracetamol suspension and could be applied as commercial suspending agent.