Formulation and Quality Control of Orally Disintegrating Tablets (ODTs): Recent Advances and Perspectives

Orally disintegrating tablets (ODTs) rapidly disintegrate or dissolve in the oral cavity without using water. Demand for ODTs has increased, and the field has overgrown in the pharmaceutical industry and academia. It is reported that ODTs have several advantages over other conventional tablets. Since some of them are absorbed from the mouth, pharynx, and esophagus as the saliva passes down into the stomach, in such cases, the bioavailability of the drug improves meaningfully. Furthermore, the immediate release property of ODTs makes them a popular oral dosage form in patients with swallowing challenges, children, and for cases with a need for rapid onset of action. The current review article explains the features of active ingredients and excipients used in the formulation of ODTs, discusses multiple ODT formulation and preparation techniques with their merits and demerits, and also, offers remedies for problems associated with ODTs. Moreover, quality control steps and required considerations are presented.

Formulation, Characterization and Release Behaviour of Metformin Hydrochloride Modified Release Tablet by Using Hydrophilic Polymers

Amongst the many public health problems, the diabetes mellitus is considered as a chronic life-style related disease which is now growing as an epidemic in both developed as well as developing countries. The current study is about formulation of metformin hydrochloride tablet to confirm their sustained release property by using various polymers. The tablets are prepared by granulation techniques using binding solution containing polyvinyl pyrolline K30. The possible interaction between the pure metformin hydrochloride and polymers are identified by Fourier transform-infrared spectroscopy. Tablets were formulated with different polymers like Hydroxy propyl methyl cellulose K100 and sodium carboxymethyl cellulose. Matrix prepared with high concentration of HPMC K100 polymer retards the drug release up to 6 h at 59 %, but the formulation 2 (F2) showed 72.72% of drug release in 6 h. The release of drug from the F2 formulation was found to be prolonged drug release when compared to other formulations. Hence our study conclude that the HPMC K100 polymer containing formulation showed good sustained release property owing to the high gel strength and well high viscosity nature of the polymer.

One-Pot Fabrication Cellulose/Silica Composite Microcapsules and Their Application in Cotton Fabrics

Research on multi-functional fabrics is an inevitable trend in the future development of textile field. Nevertheless, the key to the development of multifunctional fabric is how to solve the problem of contradictory function combination and how to achieve the multifunctions. In this work, a novel multifunctional fabric based on cellulose/silica microcapsules was developed by using green, facile and economical methods. Owing to the loaded essence and hydrophobic coupling reagent and UV absorber modified silica of microcapsules, the coated fabric not only exhibited slow-release property of fragrance, but also had excellent superhydrophobicity and ultraviolet (UV) protection. Furthermore, multifunctional fabric also displayed the durable superhydrophobicity and UV protection even after chemically or mechanically damaged. The development of mulfunctional fabrics largely depends on the development of textile functional finishing agent and finishing technology. Therefore, it is very important to develop new functional micrcapsules or finishing agent.

Termination of Dollateralized Obligations as an Illegal Action in Case of Bankruptcy: Problems of Criminal Law Assessment

There is a general rule according to which if the claims of some creditors on the debtor’s property are knowingly satisfied to the detriment of other creditors, it constitutes an illegal action in case of bankruptcy provided that such an action inflicted major damage. In its turn, the size of the inflicted damage coincides with the size of satisfied claims minus the share that would have been due to the creditors who satisfied their claims this way if the insolvency estate has been distributed according to the insolvency law. At the same time, the corresponding crime may be committed not only through the due performance of an obligation, but also through the termination of bail bonds on other grounds. When the authors analyze illegal actions in cases of bankruptcy committed through the provision of release property, they conclude that if the market value of the release property exceeds the size of terminated obligations by the sum equaling major damage, the actions should be classified as multiple offences under Parts 1, 2, Art. 195 of the Criminal Code of the Russian Federation. As for the order of determining the size of damage when satisfying claims secured by the debtor’s property, the authors pay attention to the privileged status of the pledge holder: a part of proceeds from the sale of pledged property must be used to satisfy their claims on the principal plus interest. Thus, for the corresponding part of the value of the object of pledge, no damage is inflicted on other creditors in connection with satisfying the claims of the pledgee. In some circumstances, the claims of the pledge holder are satisfied by a part of the proceeds from the sale of the object of pledge designated for the satisfaction of other claims, which cannot be overlooked when determining the size of the inflicted damage. The exceptions are the cases when, as a result of satisfying the claims of the pledgee, their claims on compensating damages and (or) paying financial sanctions were also satisfied. The satisfaction of the abovementioned claims in the size equaling major damage constitutes a crime under Part 2, Art. 195 of the Criminal Code of the Russian Federation. At the same time, if the difference between the size of pledge requirements terminated by the provision of release property, and the value of the transferred assets equals major damage, the actions must be classified as multiple offences under Parts 1, 2, Art. 195 of the Criminal Code of the Russian Federation.

Synthesis of Hybrid Organic-Inorganic Hydrotalcite-Like Materials Intercalated with Duplex Herbicides: The Characterization and Simultaneous Release Properties

In this study, a controlled-release formulation of duplex herbicides, namely, 2,4,5-trichlorophenoxybutyric acid (TBA) and 3,4-dichlorophenoxy-acetic acid (3,4D), was simultaneously embedded into Zn-Al-layered double hydroxides (LDHs). The resulting nanohybrid Zinc-Aluminium-3,4D-TBA (ZADTX) was composed of a well-ordered crystalline layered structure with increasing basal spacing from 8.9 Å to 20.0 Å in the Powder X-ray Diffraction (PXRD) with 3,4D and TBA anions located in the gallery of LDHs with bilayer arrangement. The release of 3,4D and TBA fit the pseudo-second-order model. This duplex nanohybrid possessed a well-controlled release property (53.4% release from TBA and 27.8% release from 3,4D), which was highly effective, requiring the use of a small quantity and, hence, environmentally safer.

Formulation and Evaluation of Transdermal Patches of Benidipine Hydrochloride

The present research was designed to evaluate matrix type Benidipine Hydrochloride transdermal patches. So, the present work is an attempt to study effect of variation in Methocel E15LV concentration and study effect of hydrophilic and hydrophobic Methocel E15LV and Eudragit RL100 combination on release profile of Benidipine Hydrochloride. All prepared formulations were evaluated for physical and mechanical properties like thickness, moisture uptake, percent flatness, tensile strength, and percent elongation. An attempt was made to get a patch with suitable drug release property as well as physical and mechanical properties. A formulation containing Methocel E15LV 2% has shown good physical, mechanical and in-vitro drug release properties. It also showed good diffusion of Benidipine Hydrochloride across goat skin.

Targeted drug delivery using Beeswax derived Albendazole-Loaded Solid Lipid Nanoparticles in Haemonchus contortus, an albendazole tolerant nematode.

Targeted delivery has not been achieved for anthelmintic treatment, leading to excess drugs and side effects for therapeutics. For that, drug-loaded, biocompatible nanoparticles were made using lipids that helminths uptake as a food source. The formulation showed excellent drug (albendazole) loading efficiency of ~83.3 mg/g with sustained-release properties and showed ~86.4 % of drug release within 24 h. Furthermore, upon ingestion of Rhodamine B loaded particles by Haemonchus contortus, a time-dependent release of dye was observed in the alimentary canal followed by dissemination in the whole worm. The intestinal sustained-release property was shown by the particles that caused enhancement of albendazole potency for up to 50 folds. Therefore, this formulation has immense potential as an anthelminthic drug delivery vehicle that will not only be able to reduce the dose but will also reduce the drug-induced side effects by enhancing the bioavailability of the drug.

Controlled Release of Curcumin from HPMC (Hydroxypropyl Methyl Cellulose) Co-Spray-Dried Materials

In order to achieve the controlled release of curcumin, HPMC (hydroxypropyl methyl cellulose) was spray dried with curcumin and lactose. The spray-dried materials were pressed into tablets with a diameter of 8 mm, and their release characteristics in vitro were measured. In vitro experiments showed that the release of curcumin from the HPMC mixture was significantly slower due to the sustained-release property of HPMC as a typical excipient. The release profile of curcumin from the HPMC mixture was relatively stable for a controlled release. SEM images show that the HPMC co-spray-dried powders have crumpled surfaces due to the large molecular weight of HPMC. DSC, XRD, FTIR, N2 adsorption, and TGA have been measured for the spray-dried curcumin materials. This work indicates that HPMC can be used as a controlled-release excipient for curcumin preparations.

Doxorubicin Loaded Dextran-coated Superparamagnetic Iron Oxide Nanoparticles with Sustained Release Property: Intracellular Uptake, Pharmacokinetics, and Biodistribution Study

Background: Due to the short biological half-life and serious side effects (especially for heart and kidney), the application of Doxorubicin (Dox) in clinical therapy is strictly limited. To overcome these shortcomings, a novel sustained release formulation of doxorubicin-loaded dextran-coated superparamagnetic iron oxide nanoparticles (Dox-DSPIONs) was prepared. Objective: The purpose of this study was to evaluate the intracellular uptake behavior of Dox-DSPIONs and to investigate their pharmacokinetics and biodistribution properties. Method: Confocal laser scanning microscopy was employed to study the intracellular uptake and release properties of Dox from Dox-DSPIONs in SMMC-7721 cells. Simple high-performance liquid chromatography with fluorescence detection (HPLC-FLD) method was established to study the pharmacokinetics and biodistribution properties of Dox-DSPIONs in vivo after intravenous administration and compared with free Dox. Results: Intracellular uptake experiment indicated that Dox could be released sustainedly from Dox-DSPIONs over time. The pharmacokinetics parameters displayed that the T1/2and AUC0-24h of Dox-DSPIONs were higher than those of free Dox, while the Cmax of Dox-DSPIONs was significantly lower than that of free drug. The biodistribution behaviors of the drug were altered by Dox-DSPIONs in mice, which showed obvious liver targeting, and significantly reduced the distribution of the drug in the heart and kidney. Conclusion: Dox-DSPIONs have the sustained-release property in vitro and in vivo, which could significantly prolong blood circulation time, improve bioavailability, and reduce the side effects of Dox. Therefore, the novel formulation of the Dox-DSPIONs has the potential as a promising drug delivery system in cancer therapy.