Current Issue : January - March Volume : 2018 Issue Number : 1 Articles : 6 Articles
In the present study, an attempt was made to develop floating microspheres for trimebutine maleate using different viscosity grades of ethyl cellulose as a release retarded material by solvent evaporation technique. The full 24 factorial design was followed, the study design involved the investigation of the effect of four independent factors, namely the polymer type (ethylcellulose 50, ethylcellulose 200), the drug/polymer (weight ratio at two levels (1:1 and 1:2), two types of external phase (methylene chloride and isopropyl alcohol) and stirring rate at two levels (500 rpm and 1000 rpm) leading to 16 formulae. The microspheres were characterized for yield, drug entrapment efficiency and particle size analysis. It was observed the four factors have significant effect on drug entrapment efficiency, yield and particle size analysis, but the stirring rate has non-significant effect on drug entrapment efficiency. The effect of polymer concentration on the in-vitro release of trimebutine maleate from the microspheres was also studied. It can be seen that by increasing the polymer concentration, decreases the rate of drug release from the microspheres dramatically. The best microspheres formulation was selected based on the characterization of microspheres and on the in-vitro release profile....
Various approaches have been used to retain the dosage form in the stomach as a way of increasing the gastric residence time, including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible or swellable systems and superporous hydrogel systems. Trimebutine maleate has a short elimination half-life and is mainly absorbed in proximal areas of GIT. The purpose of this study was to develop a gastroretentive controlled release drug delivery system for the drug. Tablet formulations were designed using Hydroxypropylmethylcellulose (HPMC K15M) or Hydroxypropylmethylcellulose (HPMC K100M) as release-retarding polymers and sodium bicarbonate (NaHCO3) and citric acid as a gas former. Floating behavior and drug release studies were conducted in 0.1 N HCl (pH 1.2) at 37±0.5˚C. The tablets showed acceptable physicochemical properties. Drug release profiles of all formulae followed non-Fickian diffusion. Statistical analyses of data revealed that tablets containing HPMC K100 (1:0.75), citric acid (4%, w/w) and NaHCO3 (3.5%, w/w) were promising systems exhibiting were promising systems exhibiting excellent floating properties and sustained drug release characteristics. The formulae were stored at 40 ˚C/75% RH for 3 months according to ICH guidelines. Formula F23 showed better physical stability....
To improve the transdermal bioavailability and safety of alendronate (ALN), a nitrogencontaining\nbisphosphonate, we developed self-dissolving microneedle arrays (MNs), in which ALN\nis loaded only at the tip portion of micron-scale needles by a dip-coating method (ALN(TIP)ââ?¬â??MN).\nWe observed micron-scale pores in rat skin just after application of ALN(TIP)ââ?¬â??MN, indicating that\ntransdermal pathways for ALN were created by MN. ALN was rapidly released from the tip of MNs\nas observed in an in vitro release study. The tip portions of MNs completely dissolved in the rat\nskin within 5 min after application in vivo. After application of ALN(TIP)ââ?¬â??MN in mice, the plasma\nconcentration of ALN rapidly increased, and the bioavailability of ALN was approximately 96%.\nIn addition, the decrease in growth plate was effectively suppressed by this efficient delivery of\nALN in a rat model of osteoporosis. Furthermore, no skin irritation was observed after application\nof ALN(TIP)ââ?¬â??MN and subcutaneous injection of ALN, while mild skin irritation was induced by\nwhole-ALN-loaded MN (ALNââ?¬â??MN)ââ?¬â?in which ALN is contained in the whole of the micron-scale\nneedles fabricated from hyaluronic acidââ?¬â?and intradermal injection of ALN. These findings indicate\nthat ALN(TIP)ââ?¬â??MN is a promising transdermal formulation for the treatment of osteoporosis without\nskin irritation....
Oromucosal delivery especially that utilizing the buccal and sublingual mucosa as the absorption site, is a promising drug delivery route which promotes rapid absorption and high bioavailability, with subsequent almost immediate onset of pharmacological effect. These advantages are the result of the highly vascularized oral mucosa through which drugs enter the systemic circulation directly, thus bypassing the gastrointestinal tract and the first pass effect in the liver. Tablets are the most common solid dosage form, administered orally, but many patients specially children, mentally ill patients and geriatrics have problem in swallowing the tablets. Mouth dissolving tablets (MDT) have advantage of ease of administration and rapid onset of action. Further there is advantage of rapid disintegration without use of water in oral cavity. When MDT is kept in oral cavity then saliva quickly penetrates into tablet pores and causes rapid disintegration. To mask the bitterness of drug various techniques are available, among those taste masking by use of ion exchange resin is most commonly used commercially. Ion exchange resins (IERs) are used to mask bitter taste of drug. They are solid and insoluble high molecular weight poly electrolytes capable of exchange of their ions with the counter ion in the surrounding medium. In present study an attempt was made to mask the taste of tenoxicam with formulation of mouth dissolving tablet having desired good characteristics of MDT so as to give pleasant taste and good bioavailability. Complexation with cation-exchange resin, Indion 204 resemblance to taste masking of tenoxicam. The drug resin complexes (DRC) were prepared by batch process and efficient drug loading was obtained by using inactivated form of resin in the drug-resin ratio 1:3.3 with 30 min swelling time of resin in 25 ml of water with 5 min stirring time. Drug-resin complexes were characterized for dissolution studies. Drug release from drug-resin complex in salivary pH was insufficient to impart bitter taste. The new sublingual tablet concept presented is based on interactive mixtures consisting of a water-soluble carrier covered with fine drug particles and a bioadhesive component. With this approach, it is possible to obtain rapid dissolution in combination with bioadhesive retention of the drug in the oral cavity. Optimized orally disintegrating tablets (ODTs) containing tenoxicam) were prepared by direct compression method. And characterized for hardness, disintegration time, friability and wetting time. Box-Behnken statistically designed with 3 factors, 3 levels and 15 run was selected to statistically optimized the formulation parameters and evaluate the main, quadratic and interaction effects of the preparations. The manufactured ODTs were complying with the pharmacopeia guidelines regarding hardness, friability, weight variation and content....
Sufficient aqueous solubility is an important criterion for a drug candidate for further development. Poor aqueous solubility is usually associated with erratic and low bioavailability. Enhancing aqueous solubility an essential task during the development process of such compounds. Different formulation approaches have been utilized to overcome this obstacle. Solid dispersions, cyclodextrin complexation, self-emulsifying drug delivery systems, size reduction and mesoporous inorganic carriers are discussed in this review....
The crystallization of mefenamic acid in transdermal patch is a major problem that makes the patch unstable and decreases\nthe drug release. The additive was used to inhibit crystallization of a mefenamic acid. Among the different types of additives,\npolyvinylpyrrolidone (PVP) K30 and PVP K90 were studied and found to be highly effective in inhibiting the crystallization of\nthe drug. The PVP presented as a solubilizer agent for mefenamic acid in matrix patches at the different ratio between drug : PVP,\n1 : 2 and 1 : 2.5 for using PVP K30 and 1 : 1.5 and 1 : 2 for using PVP K90. The characterizations showed the homogeneous patches\nwithout the crystal formof the mefenamic acid in matrix patches. The release profiles of the mefenamic acid fromthe patches were\ninvestigated by Franz diffusion cells. Over the first 1 h, the release behavior of mefenamic acid fromthe patches obviously increased\nwhen PVP was used as a crystallization inhibitor. However, the ratio between drug : PVP K90 at 1 : 2 was found to be the most\neffective in increasing the drug release from patch.Thus, the PVP could be used as a crystallization inhibitor for mefenamic acid\nin matrix patches which will increase the drug release....
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