Innovative Dosage Form Research Articles

Анализ номенклатуры трансдермальных терапевтических систем в аптечной сети ОАО «Смоленск-фармация»

Use of transdermal therapeutic systems - innovative dosage form - especially for the treatment of chronic diseases is a promising direction in medicine and pharmacy. Transdermal therapeutic systems have modified release according to the principle of regulation, which in cutaneous application allow to provide sys- temic therapeutic effects hundred-stably maintain a constant concentration of active substance in the blood plas- ma, which is close to the minimal therapeutic concentrations, and so as to reduce the effect of first pass metabol- ism in the liver. As part of this work we conducted content analysis, studied range of tera-apeutic transdermal systems that are registered in the State Register of pharmaceuticals-governmental funds of the Russian Federa- tion for 2014. To study the Sun-requirements are available in the pharmaceutical market assortment pe-de-listing study group medicines studied nomenclature of transdermal therapeutic systems, implemented in 2014 through a network of up-technuyu OAO Smolensk-Pharmacy (Smolensk), which includes more than 50 pharmacies or- ganizations located in Smolensk, regional centers and other towns in the area. It was revealed that the range of transdermal-governmental therapeutic systems in the pharmacy network is not wide enough, the leader of sales in 2014 was Voltaren (diclofenac) from Novartis, pain-PWM demand as Nicorette (Nicotine) - Johnson & John- son, Nikvitin (Nicotine) - GlaxoSmithKline.

Study of sodium hyaluronate-based intranasal formulations containing micro- or nanosized meloxicam particles

This article reports on the micro- and nanonization of meloxicam (MEL) with the aim of developing pre-dispersions as intermediates for the design of intranasal formulations. As a new approach, combined wet milling technology was developed in order to reduce the particle size of the MEL. Different milling times resulted in micro- or nanosized MEL in the pre-dispersions with polyvinyl alcohol as stabilizer agent, which were directly used for preparing intranasal liquid formulations with the addition of sodium hyaluronate as mucoadhesive agent. Reduction of the MEL particle size into the nano range led to increased saturation solubility and dissolution velocities, and increased adhesiveness to surfaces as compared with microsized MEL particles. A linear correlation was demonstrated between the specific surface area of MEL and the AUC. The in vitro and in vivo studies indicated that the longer residence time and the uniform distribution of nano MEL spray throughout an artificial membrane and the nasal mucosa resulted in better diffusion and a higher AUC. Nanosized MEL may be suggested for the development of an innovative dosage form with a different dose of the drug, as a possible administration route for pain management.

Modern evaluation of liquisolid systems with varying amounts of liquid phase prepared using two different methods.

Liquisolid systems are an innovative dosage form used for enhancing dissolution rate and improving in vivo bioavailability of poorly soluble drugs. These formulations require specific evaluation methods for their quality assurance (e.g., evaluation of angle of slide, contact angle, or water absorption ratio). The presented study is focused on the preparation, modern in vitro testing, and evaluation of differences of liquisolid systems containing varying amounts of a drug in liquid state (polyethylene glycol 400 solution of rosuvastatin) in relation to an aluminometasilicate carrier (Neusilin US2). Liquisolid powders used for the formulation of final tablets were prepared using two different methods: simple blending and spraying of drug solution onto a carrier in fluid bed equipment. The obtained results imply that the amount of liquid phase in relation to carrier material had an effect on the hardness, friability, and disintegration of tablets, as well as their height. The use of spraying technique enhanced flow properties of the prepared mixtures, increased hardness values, decreased friability, and improved homogeneity of the final dosage form.

Formulation and Evaluation of Acyclovir Orodispersible Tablets Using Sublimation Method

Difficulty in swallowing (dysphagia) is common among all age groups, especially for geriatric and paediatric patients. Oral dispersible tablets (ODT) constitute an innovative dosage form that overcome the problems of swallowing and provides a quick onset of action. The aim of the present research was to prepare oral dispersible tablets by sublimation method. The technique is to increase the porosity of the tablet whereby subliming material was sublimed from the tablets by exposing the tablets to vacuum and to investigate the effects of super disintergrants (Kollidon & Ac-Di-Sol). Acyclovir is an antiviral drug used for the treatment of herpes simplex virus (HSV), mainly HSV-1 and HSV-2 and varicella zoster virus. It is a BCS class III drug. Hence an orally disintegrating tablet formulation of acyclovir was prepared by direct compression,which was taken as the model drug for the study.The drug and finalized formulation were characterized using FTIR studies revelled that there is no interaction between drug and excipients. The powder blend was examined for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio and prepared tablets were evaluated for general appearance, content uniformity, hardness, friability, wetting time, In-vitro disintegration and dissolution studies were found to be acceptable according to standard limits, In-vitro release studies were performed using USP apparatus-II (paddle method) in 500 ml of distilled water at 50rpm. The highest drug dissolved was obtained from SF4 (100.2%). Tablet with 5% of camphor 5% Crospovidone 4% Croscarmellose sodium shows quick dissolution, disintegration, and good dispersion pattern. It is concluded that Oral disintegrating acyclovir tablets could be prepared by direct compression using sublimation method.

Delivery of Drugs from Laminar Co-Extrudates Manufactured by a Solvent-Free Process at Room Temperature

This work aims to design and manufacture laminar co-extrudates as a new dosage form for the delivery of drugs. Co-extrudates made of lipid-based materials with a laminar shape were manufactured at room temperature in the absence of solvents and assessed over time for their mechanical properties (bending strength, deformation, stiffness, and elasticity), density, porosity, thermal behavior and main mechanism of drug release. The study has shown that the extrusion force at steady state increased with the extrusion rate and with the number of layers. The bending strength and stiffness of extrudates increased over time. Laminar co-extrudates with higher number of layers presented a decreasing dissolution efficiency of 38.3 ± 0.6%, 23.0 ± 0.2%, and 12.3 ± 0.2%, for mono-, bi-, and trilayer, respectively. After 90 days, the density, the deformation, and elasticity decreased: trilayer extrudates were the denser and the ones to present the lowest ability to deform and the highest elasticity, whereas monolayer extrudates were the less dense presenting the highest ability to deform. Changes were more evident in the first days after manufacture leading to stabilization over time. Laminar (co-)extrudates have been confirmed as an innovative dosage form for tailored delivery of drugs made without solvents at room temperature.

Drug delivery from injectable calcium phosphate foams by tailoring the macroporosity–drug interaction

In this work, novel injectable calcium phosphate foams (CPFs) were combined with an antibiotic (doxycycline) to design an innovative dosage form for bone regeneration. The material structure, its drug release profile and antibiotic activity were investigated, while its clinical applicability was assessed through cohesion and injectability tests. Doxycycline had a clear effect on both the micro and macro structure of the CPFs, owing to its role as a nucleating agent of hydroxyapatite and to a drying effect on the paste. Doxycycline-loaded CPFs presented interconnected macroporosity, which increased drug availability compared with calcium phosphate cements, and was a critical parameter controlling the release kinetics which followed a non-Fickian diffusion model. Up to 55% (1mg) of the drug was released progressively in 5days, the percentage released being proportional to the macroporosity of the CPFs. All doxycycline-containing foams had immediate cohesion and were injectable. Moreover, antibacterial activity was observed against Staphylococcus aureus and Escherichia coli. Thus, in addition to enhancing osteoconduction and material resorption, macroporosity enables tuning of the local delivery of drugs from injectable calcium phosphates.

Recent patents survey on self emulsifying drug delivery system.

Self-Emulsifying Drug Delivery System is a unique feasible approach to overcome low oral bioavailability problem which is associated with the hydrophobic drugs due to their unparalleled potential as a drug delivery with the broad range of application. The estimated 40% of active pharmaceuticals are poorly water soluble. Now recently, formulation containing oral SEDDS has received much interest as it solve problems related to oral bioavailability, intra and inter-subject variability and lack of dose proportionality of hydrophobic drugs. Now a days, it is the first way to investigate the development of any kind of innovative dosage forms. Many important in-vitro characteristics such as surfactant concentration, oil/surfactant ratio, emulsion polarity, droplet size and zeta potential play an important role in oral absorption of drug from SEEDS. It can be orally administered in the form of SGC or HGC and also enhances bioavailability of drugs to increase solubility and minimizes the gastric irritation. After administration the drug remains entrapped in the oily droplets (inside the droplet or in the surfactant`s film at the interface) of the emulsion that are formed in the GIT upon self-emulsification process. It is also a bit problematic to say that the drug is being released from SMEDDS, it would be more precise to say that it diffuses out of oily droplets into the GIT media resulting in the formation of an equilibrium between the drug dissolved in oily droplets and the outer dispersed media (e.g. GIT fluids). Many of the application and preparation methods of SEDDS are reported by research articles and patents in different countries. We present an exhaustive and updated account of numerous literature reports and more than 150 patents published on SEDDS in the recent period. This current patent review is useful in knowledge of SEDDS for its preparations and patents in different countries with emphasis on their formulation, characterization and systematic optimization strategies, thus paving the way for accelerated progress into the SEDDS application in pharmaceutical research as well as patents on SEDDS methods.

Comparative study on novel test systems to determine disintegration time of orodispersible films

Orodispersible films (ODFs) are a promising innovative dosage form enabling drug administration without the need for water and minimizing danger of aspiration due to their fast disintegration in small amounts of liquid. This study focuses on the development of a disintegration test system for ODFs. Two systems were developed and investigated: one provides an electronic end-point, and the other shows a transferable setup of the existing disintegration tester for orodispersible tablets. Different ODF preparations were investigated to determine the suitability of the disintegration test systems. The use of different test media and the impact of different storage conditions of ODFs on their disintegration time were additionally investigated. The experiments showed acceptable reproducibility (low deviations within sample replicates due to a clear determination of the measurement end-point). High temperatures and high humidity affected some of the investigated ODFs, resulting in higher disintegration time or even no disintegration within the tested time period. The methods provided clear end-point detection and were applicable for different types of ODFs. By the modification of a conventional test system to enable application for films, a standard method could be presented to ensure uniformity in current quality control settings.

A new deferiprone controlled release system obtained by ultrasound-assisted compression

Objectives: This study implements the design of an innovative dosage form using ultrasound-assisted compression of thermoplastic polymers and the development of controlled release tablets for the oral administration of deferiprone in two doses per day.Methods: Binary matrix tablets containing deferiprone and thermoplastic polymers have been prepared using an ultrasound-assisted tableting machine. Scanning electron microscopy has been employed to determine a sintering phenomenon of the excipients. Water uptake and drug release studies have been carried out to evaluate the ability of the polymers to control the drug release.Results: SEM micrographs showed that some polymers underwent the sintering process and the in vitro dissolution test showed good fit of the release data from these tablets to the zero-order kinetic model.Conclusions: Carbopol 974P and 971P have been selected as matrix forming polymers for the final formulation. The polymer percolation threshold has been exceeded with 15% w/w of polymer. Therefore, sustained release tablets have been developed with only 15% of excipient. This implies that matrix tablets containing 750 mg of API, intended for two administrations a day, can be obtained with a similar weight to those existing in the market containing 500 mg of API for three administrations a day.

FORMULATION AND EVALUATION ORAL DISPERSIBLE TABLET OF CINNARIZINE

Oral Dispersible tablets (ODTs) constitute an innovative dosage form, which overcomes the problem of swallowing and provides a quick onset of action. The aim of the proposed work is to formulate fast dissolving tablets of Cinnarizine for rapid dissolution of drug and absorption, which may produce rapid onset of action in the treatment of motion sickness. For this purpose the tablets of Cinnarizine were prepared by Effervescent method, Super disintegrants addition method and Sublimation method. Cinnarizine is an Antihistamines drug has been used for the treatment of motion sickness. Cinnarizine is poorly soluble in water making it a potent candidate fast-dissolving drug delivery system. Key word: ODT, Cinnarizine, Granules, Superdisintegrants,

Improvement and enhancement of traditional Chinese medicine injections

Compared to oral administrations, traditional Chinese medicine (TCM) injections act more rapidly and stronger, which is good for the treatment of acute or complicated diseases and makes up for the deficiencies of the oral ways. As an innovative dosage form which combines the modern pharmaceutical technology with the TCM, it represents the spirit of improvement and enhancement. With the expansion of clinical applications and adverse reactions or even death caused by individual dosages, TCM injections are receiving concerns from all fields of society and facing tremendous challenges and pressures. Some even suggested the cancellation. This study discussed the background, current situation and the reasons for the occurrence of adverse reactions. Taking Houttuynia injection as an example, it introduced the principle of improvement and described in detail the ideas and methods for it, which provided some reference for the improvement and enhancement of the TCM injections and reduced the safety risks of TCM injections to minimum.

A progressive review of Sandhana kalpana (Biomedical fermentation): An advanced innovative dosage form of Ayurveda

Sandhana kalpana (biomedical fermented formulations) are one of the best dosage forms of Ayurveda in practice since thousands of years. In order to prepare these medicaments, certain sets of conditions are prearranged, which lead to fermentation. Thus, products bequeath with self-generated ethyl alcohol, which potentiate these preparations (Asava–Arishta), pharmaceutically and therapeutically. Commonly, medicinal and commercial components of these formulations are prompting many researchers to contribute in manufacturing, quality control, safety, and efficacy of these formulations. To cope up with this, literature related to Asava–Arishta has been surveyed from the Vedic period to recent publications of Government of India, ie, Ayurvedic Formulary of India, and presented briefly here. In this review paper, we have discussed pioneering facts such as nature and amount of carbohydrate, type of containers, optimum temperature, variety and relevance of initiator of fermentation, manufacturing, regulatory rules, and business aspects of Asava-Arishta. After going through this basic information, any academician or researcher may show a way to further strengthen this dosage form.

Development of mouth dissolving tablets of clozapine using two different techniques

Mouth dissolving tablets constitute an innovative dosage form that overcomes the problems of swallowing and provides a quick onset of action. In view of enhancing bioavailability an attempt has been made to study two different methods direct compression and sublimation in formulation of mouth dissolving tablets of clozapine. Total four formulations using various superdisintegrants and subliming agents were prepared. All prepared formulations were evaluated for physico-chemical parameters. The formulations exhibited good disintegration properties with total disintegration time in the range of 25 to 35 s. Comparative evaluation of two methods showed direct compression method is a better alternative to sublimation method as its formulations rapidly disintegrate in oral cavity. In vitro cumulative percentage drug release for formulations prepared by direct compression with explotab superdisintegrants shows 99.79 while sublimation method using camphor 93.58 release in 12 min. Kinetic studies indicated that all the formulations followed first order release with diffusion mechanism.

Benefits of different drug formulations in psychopharmacology

Adequate dosage forms are essential for achieving successful pharmacotherapy. Innovative dosage forms or delivery systems may direct a drug to its specific site of action, optimize the timing of the drug release, or increase comfort or convenience for the patient. Thus, such innovations may improve efficacy and tolerability and lead to improvements in health-related quality of life. Specialized dosage forms (e.g., depot injections, extended-release formulations) of several psychiatric agents have been extensively used. The latest addition is an orally disintegrating formulation of the antidepressant mirtazapine. This dosage form dissolves rapidly in the mouth and is convenient for the large proportion of patients who have difficulty in swallowing tablets.