Formulation and optimization of carbamazepine floating tablets by 23 - factorial design employing Starch-Urea-Borate: A new floating polymer

Several approaches are currently used to retain the dosage form in the stomach. These include bioadhesive systems, swelling and expanding systems, floating systems   and other delayed gastric emptying devices. The principle of floating tablets offers a simple and practical approach to achieve increased gastric residence time to enhance the bioavailability and to obtain controlled release. Floating tablets are designed based on gas generating principle. Design of floating tablets needs a strong matrix forming polymer. Though several polymers are available for floating tablets, there is a continued need to develop new, effective and efficient polymers for controlled release floating tablets. The major objective of the investigation is to evaluate starch-urea-borate, a new modified starch as a floating matrix former in the design of controlled release floating tablets. Keywords: Optimisation, Carbamazepine, Starch-Urea-Borate, Floating Tablet

Preparation and characterization of Starch–Urea–Borate: A new floating polymer

In recent years considerable attention has been focused on the development of new drug delivery systems known as controlled release drug delivery systems. Such interest is based largely on the fact that the controlled release products have established and retained place in the market based on their uniqueness and their clinical advantages in the practices of medicine. The major types of controlled release systems include matrix tablets, floating tablets, swellable tablets,  coated beads, microcapsules and microspheres, mucoadhesive systems, ion exchange resin complexes, osmotic pressure controlled release systems, transdermal systems etc. The principle of floating tablets offers a simple and practical approach to achieve increased gastric residence time to enhance the bioavailability and to obtain controlled release. Floating tablets are designed based on gas generating principle. Design of floating tablets needs a strong matrix forming polymer. Several polymers such as various viscosity grades of hydroxypropylmethyl cellulose (HPMC), Carbopol 934P, Eudragit RL, calcium alginate, chitosan, xanthan gum, guar gum, ethyl cellulose etc., have been used in the design of floating tablets of various active pharmaceutical ingredients (APIs). Though these polymers are available for floating tablets, there is a continued need to develop new, effective and efficient polymers for controlled release floating tablets.The overall objective of the investigation is to develop new, efficient and safe polymer as floating matrix former for floating systems. Keywords: Floating, Matrix, Polymers, Starch-urea-borate

Effects of nanosuspension and inclusion complex techniques on the in vitro protease inhibitory activity of naproxen

This study investigated the effects of nanosuspension and inclusion complex techniques on in vitro trypsin inhibitory activity of naproxen—a member of the propionic acid derivatives, which are a group of antipyretic, analgesic, and non-steroidal anti-inflammatory drugs. Nanosuspension and inclusion complex techniques were used to increase the solubility and anti-inflammatory efficacy of naproxen. The evaporative precipitation into aqueous solution (EPAS) technique and the kneading methods were used to prepare the nanosuspension and inclusion complex of naproxen, respectively. We also used an in vitro protease inhibitory assay to investigate the anti-inflammatory effect of modified naproxen formulations. Physiochemical properties of modified naproxen formulations were analyzed using UV, IR spectra, and solubility studies. Beta-cyclodextrin inclusion complex of naproxen was found to have a lower percentage of antitryptic activity than a pure nanosuspension of naproxen did. In conclusion, nanosuspension of naproxen has a greater anti-inflammatory effect than the other two tested formulations. This is because the nanosuspension formulation reduces the particle size of naproxen. Based on these results, the antitryptic activity of naproxen nanosuspension was noteworthy; therefore, this formulation can be used for the management of inflammatory disorders

Formulation and evaluation of carvedilol microcapsules using Eudragit NE30D and sodium alginate

Inclusion complexes of carvedilol(CR) with hydroxyl propyl beta-cyclodextrin (HPBCD) was prepared using co-grinding technique. Then, the inclusion complex was microencapsulated using combinations of Eudragit NE30D (EU) and sodium alginate (SA) utilizing orifice gelation technique. The formulations were analysed by using Scanning electron microscopy (SEM), Fourier Transform Infrared spectroscopy (FTIR), Differential scanning Calorimetry (DSC) and X-ray diffractometer (XRD) and also evaluated for particle size, encapsulation efficiency, production yield, swelling capacity, mucoadhesive properties, zeta potential and drug release. The microcapsules were smooth and showed no visible cracks and extended drug release of 55.2006% up to 12 hours in phosphate buffer of pH 6.8, showing particle size within the range of 264.5-358.5 µm, and encapsulation efficiency of 99.337±0.0100-66.2753±0.0014%.The in vitro release data of optimized batch of microcapsules were plotted in various kinetic equations to understand the mechanisms and kinetics of drug release, which followed first order kinetics, value of "n" is calculated to be 0.459 and drug release was diffusion controlled. The mice were fed with diet for inducing high blood pressure and the in vivo antihypertensive activity of formulations was carried out administering the optimized formulations and pure drug separately by oral feeding and measured by B.P Monwin IITC Life Science instrument and the results indicated that the bioavailability of carvedilol was increased both in vitro and in vivo with the mucoadhesive polymers showing primary role in retarding the drug release

Cyclodextrins and ternary complexes: technology to improve solubility of poorly soluble drugs

Cyclodextrins (CDs) are cyclic oligosaccharides composed of D-glucopyranoside units linked by glycosidic bonds. Their main property is the ability to modify the physicochemical and biological characteristics of low-soluble drugs through the formation of drug:CD inclusion complexes. Inclusion complexation requires that host molecules fit completely or partially within the CD cavity. This adjustment is directly related to the physicochemical properties of the guest and host molecules, easy accommodation of guest molecules within the CD cavity, stoichiometry, therapeutic dose, and toxicity. However, dosage forms may achieve a high volume, depending on the amount of CD required. Thus, it is necessary to increase solubilization efficiency in order to use smaller amounts of CD. This can be achieved by adding small amounts of water-soluble polymers to the system. This review addresses aspects related to drug complexation with CDs using water-soluble polymers to optimize the amount of CD used in the formulation in order to increase drug solubility and reduce dosage form volume.Ciclodextrinas (CDs) são oligossacarídeos cíclicos, compostos por unidades D-glicopiranosídicas ligadas entre si por meio de ligações glicosídicas e sua principal propriedade está na capacidade de alterar as características físico-químicas e biológicas de fármacos com baixa solubilidade por meio da formação de complexos de inclusão fármaco:CD. Para a formação dos complexos de inclusão a molécula hospedeira necessita ajustar-se total ou parcialmente no interior da cavidade da CD, onde este ajuste está diretamente ligado a propriedades físico-químicas da molécula hóspede e hospedeira, facilidade de alojamento da molécula hóspede no interior da cavidade da CD, estequiometria, dose terapêutica e toxicidade. No entanto, as formas farmacêuticas podem atingir um elevado volume, em função da quantidade de CD requerida, sendo necessário aumentar sua eficiência de solubilização para que seja possível utilizar menores quantidades das mesmas. Isso pode ser obtido com a inclusão de pequenas quantidades de polímeros hidrossolúveis ao sistema. Nessa revisão, são abordados aspectos relacionados à complexação de fármacos com ciclodextrinas empregando-se polímeros hidrossolúveis para otimização da quantidade de CD utilizada na formulação, com a finalidade de aumentar a solubilidade do fármaco e reduzir o volume das preparações

Preparation and characterization of Starch–Urea–Borate: A new floating polymer

In recent years considerable attention has been focused on the development of new drug delivery systems known as controlled release drug delivery systems. Such interest is based largely on the fact that the controlled release products have established and retained place in the market based on their uniqueness and their clinical advantages in the practices of medicine. The major types of controlled release systems include matrix tablets, floating tablets, swellable tablets,  coated beads, microcapsules and microspheres, mucoadhesive systems, ion exchange resin complexes, osmotic pressure controlled release systems, transdermal systems etc. The principle of floating tablets offers a simple and practical approach to achieve increased gastric residence time to enhance the bioavailability and to obtain controlled release. Floating tablets are designed based on gas generating principle. Design of floating tablets needs a strong matrix forming polymer. Several polymers such as various viscosity grades of hydroxypropylmethyl cellulose (HPMC), Carbopol 934P, Eudragit RL, calcium alginate, chitosan, xanthan gum, guar gum, ethyl cellulose etc., have been used in the design of floating tablets of various active pharmaceutical ingredients (APIs). Though these polymers are available for floating tablets, there is a continued need to develop new, effective and efficient polymers for controlled release floating tablets.The overall objective of the investigation is to develop new, efficient and safe polymer as floating matrix former for floating systems.&#x0D; Keywords: Floating, Matrix, Polymers, Starch-urea-borate.</jats:p

Formulation and optimization of carbamazepine floating tablets by 23 - factorial design employing Starch-Urea-Borate: A new floating polymer

Several approaches are currently used to retain the dosage form in the stomach. These include bioadhesive systems, swelling and expanding systems, floating systems   and other delayed gastric emptying devices. The principle of floating tablets offers a simple and practical approach to achieve increased gastric residence time to enhance the bioavailability and to obtain controlled release. Floating tablets are designed based on gas generating principle. Design of floating tablets needs a strong matrix forming polymer. Though several polymers are available for floating tablets, there is a continued need to develop new, effective and efficient polymers for controlled release floating tablets. The major objective of the investigation is to evaluate starch-urea-borate, a new modified starch as a floating matrix former in the design of controlled release floating tablets.&#x0D; Keywords: Optimisation, Carbamazepine, Starch-Urea-Borate, Floating Tablets</jats:p