scholarly journals DEVELOPMENT OF THE COMPOSITION AND TECHNOLOGY FOR THE PRODUCTION OF ENCAPSULATED DRUGS BASED ON 3,7-DIAZABICYCLO[3.3.1]NONANE

2020 ◽  
Vol 17 (34) ◽  
pp. 502-511
Author(s):  
Galina Eduardovna BRKICH ◽  
Natalia Valeryevna PYATIGORSKAYA ◽  
Natalya Borisovna DEMINA ◽  
Elena Olegovna BAKHRUSHINA ◽  
Mstislav Igorevich LAVROV
Keyword(s):  
Dosage Form ◽  
Dissolution Kinetics ◽  
Biological Properties ◽  
Oral Dosage ◽  
Lag Phase ◽  
Technological Parameters ◽  
Pharmaceutical Substance ◽  
Key Indicators ◽  
Oral Dosage Forms ◽  
Pharmacopoeial Requirements

The following biological and pharmaceutical factors influence the therapeutic efficacy and bioequivalence of drugs: physicochemical properties of a pharmaceutical substance, bioavailability, type of dosage form, route of administration, nature of excipients, their compatibility, as well as technological conditions of production, including the preparation of drugs forms. Before mass production of a drug, the technological parameters and characteristics of the pharmaceutical substance must be carefully studied and scientifically substantiated. This work is devoted to the study of the technological properties of an original pharmaceutical substance based on the derivative of 3.7-diazabicyclo[3.3.1]nonane with the chemical name IUPAC 6-[4methoxy-3- (1H-pyrazol-1-ylmethyl) benzyl] -1,11dimethyl-3,6,9-triazatricyclo[7.3.1.1]tetradecane-4,8,12-trion, used as an active substance for the development of the composition and technology for the preparation of oral dosage forms in capsule form. The article presents the results of the development and testing of a drug in the form of capsules of the original pharmaceutical substance of the nootropic action of 3,7-diazabicyclo[3.3.1]nonanane, which is practically insoluble in water. The study identified and evaluated the technological and biological properties of a pharmaceutical substance that can affect the pharmacological activity in the production of a dosage form. The study examined the key indicators: solubility, particle size, flowability, bulk density. The technological characteristics of the pharmaceutical substance are studied not only by certain values of the indicated characteristics but also by the values of the Hausner and Carr indices. The data obtained suggest the content and progress of further stages of pharmaceutical development. The presence of the lag phase when dissolving hypromellose capsules in a medium with a pH of 1,2 and relatively low disintegration rates in media with a pH of 1,2, pH 4,5, and pH 6,8 served as the basis for the choice of gelatin capsules. The developed dosage form meets modern pharmacopoeial requirements, including the dissolution kinetics: according to the results obtained, in 45 minutes (77,6 ± 2,5)% of the substance passes into the dissolution medium with a pH of 4,5. The results of the study are used to develop a technological scheme for obtaining the dosage form of 3,7-diazabicyclo[3.3.1]nonane, its indicators, and quality standards.

scholarly journals Multiple Unite Pellet Systems (MUPS) as Drug Delivery model

2020 ◽  
Vol 10 (6) ◽  
pp. 231-235
Author(s):  
Saad M. Majeed ◽  
Mohammed K. Al-Shaheen ◽  
Radhwan Nidal Al-Zidan ◽  
Sameer M. Mahmood
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Oral Dosage ◽  
Drug Bioavailability ◽  
Physicochemical Stability ◽  
Key Variables ◽  
High Flexibility ◽  
Gastro Intestinal Tract ◽  
Oral Dosage Forms ◽  
Different Characteristics

Multiparticulate drug delivery systems are mainly oral dosage form, consist of small discrete units that exhibit different characteristics especially in release pattern and drug bioavailability. These systems are represented by granules, pellets, microspheres, microcapsules, and minitablets. Pellets offer high flexibility in the design, formulation, and development of oral dosage forms such as sachet, suspension, capsule, and tablet. Multiparticulate tablets manufactured by compaction of multiple unite pellets is one of the latest and, yet, challenging technologies. Multiparticulate tablets combine the benefits of both a tablet and a pellet-filled capsule in one dosage form but their manufacturing experience many difficulties. The oral multiparticulate products consist of polymer-coated subunits or pellets, which are embedded in an inert excipients’ matrix, formulated to overcome the difficulty in administering capsules and improve the physicochemical stability of suspension and offer predictable release and uniform distribution in the gastro-intestinal tract compared to the plain tablet. This review discusses the advantages and drawbacks of MUPS, the properties of an ideal MUPS, various pharmaceutical applications of MUPS, the challenges and key variables that to be considered in the tableting process for successful production of MUPS Keywords: MUPS®, Pellets, Multiparticulate tablets.

scholarly journals Dry syrup: An overview

2018 ◽  
Vol 6 (03) ◽  
pp. 30-38
Author(s):  
M. Ola ◽  
R. Bhaskar ◽  
Priya Patil
Keyword(s):  
Gastrointestinal Tract ◽  
Dosage Form ◽  
Drug Stability ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Technological Advancement ◽  
Ich Guidelines ◽  
Reconstituted System ◽  
Oral Dosage Forms ◽  
High Bioavailability

The advantages of oral dosage form that are responsible for its popularity are its ease of administration, patient compliance and stability of formulation. The most popular oral dosage forms beings tablets and capsules, but one important drawback of the dosage forms however is the difficulty to swallow especially when a dosage form is developed for pediatric and geriatric patient. The modern scientific and technological advancement in the pharmaceutical field had created bank of interest in reconstitutable oral suspension dosage form in the recent year. The reconstituted system is the formulation of choice when the drug stability is a major concern. Reconstitutable oral systems show the adequate chemical stability of the drug during shelf life and also reduce the weight of the final product. Dry syrup form of the drug is also useful in case of bioavailability as it has high bioavailability rather than tablets and capsules as it disintegrates in water outside of the oral cavity and directly the suspension is gone through the gastrointestinal tract. So the suspension easily absorbs in the GIT. The present review gives an account of the excipients used, methods of preparation of dry syrups along with their evaluations, their packaging, ICH guidelines.

scholarly journals A Review Extended Release Oral Drug Delivery System and Multiparticulate Drug Delivery Systems (MDDS)

2020 ◽  
pp. 84-92
Author(s):  
Swapnil B. Khambat ◽  
Shubham A. Kale.
Keyword(s):  
Drug Delivery ◽  
Dosage Form ◽  
Extended Release ◽  
Oral Drug Delivery ◽  
Oral Dosage ◽  
Oral Drug ◽  
Solid Dosage ◽  
Oral Formulations ◽  
Oral Drug Delivery System ◽  
Oral Dosage Forms

The extended release product will optimize therapeutic effect and safety of a drug at the same time improving the patient convenience and compliance. By incorporating the dose for 24 hrs into one tablet/capsule from which the drug is released slowly. The concept of multiple unit dosage form was initially introduced in the early 1950’s.These forms play a major role in the design of solid dosage form processes because of their unique properties and the flexibility found in their manufacture. These forms can be defined as oral dosage forms consisting of a multiplicity of small discrete units, each exhibiting some desired characteristics. The release of drug from pellets depends on a variety of factors including the carrier used to form pellets and the amount of drug contained in them. Consequently, pellets provide tremendous opportunities for designing new controlled and extended release oral formulations, thus extending the frontier of future pharmaceutical development. The possible mechanism for drug release includes solution/diffusion through the continuous polymer phase or plasticizer channels, diffusion through aqueous pores and osmotically driven release through aqueous pores. To distinguish between these mechanisms, the release rate was studied as a function of coating thickness, plasticizer content and osmotic pressure in the dissolution medium.

scholarly journals AN OVERVIEW ABOUT NOVEL FAST DISSOLVING ORAL FILMS

2018 ◽  
Vol 6 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Pravin Kumar Sharma ◽  
Pankaj Kumar Sharma ◽  
Gajanan N Darwhekar ◽  
Birendra Shrivastava
Keyword(s):  
Dosage Form ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Drug Dissolution ◽  
Solid Dosage Forms ◽  
Onset Of Action ◽  
Cold Sore ◽  
Solid Dosage ◽  
Oral Films ◽  
Oral Dosage Forms

Nowadays, novel fast dissolving oral films (FDF) have come in existence as an alternative dosage form in comparison with tablet, capsules, syrup and other oral dosage forms with respect to patient convenience and compliance. Fast dissolving oral films are helpful to paediatric and geriatric patients who experience difficulties in swallowing traditional oral solid-dosage forms. The FDF drug delivery systems are solid dosage form which disintegrate or dissolve within seconds when placed in the mouth cavity without need of water or chewing. FDF provide better drug dissolution, faster onset of action, bypassing the first pass metabolism of drugs and thus enhance their oral bioavailability with reduced dosing frequency. These formulations are suitable for cough, cold, sore throat, allergenic conditions, nausea, pain, hypertension and CNS disorders. The present review provides the details about the recent advancement in design and development of oral fast dissolving film.

scholarly journals Formulation and evaluation of effervescent tablets: a review

2018 ◽  
Vol 8 (6) ◽  
pp. 296-303 ◽  
Author(s):  
Salim G Patel ◽  
M Siddaiah
Keyword(s):  
Drug Delivery Systems ◽  
Dosage Form ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Liquid Form ◽  
Pulsatile Drug Delivery ◽  
Oral Dosage Forms ◽  
Effervescent Tablet ◽  
Liquid Dosage Form ◽  
Slow Absorption

Oral dosage forms are the most popular way of taking medication, despite having some disadvantages compared with other methods like risk of slow absorption of the medicament, which can be overcome by administering the drug in liquid form, therefore, possibly allowing the use of a lower dosage. However, instability of many drugs in liquid dosage form limits its use. Effervescent technique can be used as alternate to develop a dosage form which can accelerate drug disintegration and dissolution, is usually applied in quick release preparations. Along with the development of new pharmaceutical technique, effervescent tablet are more and more extensively to adjust the behaviour of drug release, such as in sustained and controlled release preparations, pulsatile drug delivery systems, and so on. This review demonstrated the new applying of effervescent technique in effervescent tablets. Keywords: Effervescent Tablet, Sustained release, Floating Delivery System

scholarly journals A comprehensive review on pharmaceutical mini tablets

2018 ◽  
Vol 8 (6) ◽  
pp. 382-390 ◽  
Author(s):  
Priyanka Priyanka ◽  
Kapil Kumar ◽  
Deepak Teotia
Keyword(s):  
Dosage Form ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Formulation Development ◽  
Coating Materials ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Therapeutic Benefits ◽  
Form Design ◽  
Oral Dosage Forms

Mini-tablets represent a new trend in solid dosage form design, with the main goal of overcoming some therapeutic obstacles. Mini tablets are multiple unit dosage forms and are advantageous than pellets or any other oral dosage forms as they are easy to manufacture and stability problems are less. Offering some therapeutic benefits such as dose flexibility and combined release patterns. They do not require any solvent for their production and also local irritation can be avoided by the use of mini tablet Mini tablet offer several advantages like they can be manufactured relatively easily, They are not require less coating materials and also there is a great flexibility during their formulation development. Mini tablet are more acceptable in children and elderly people as they are easy to swallow. The objective of controlled drug delivery systems is to reduce the frequency of the dosing and to increase the effectiveness of the drug by localization. Keywords: Mini-tablets, solid dosage form, oral dosage forms.

scholarly journals AN OVERVIEW ABOUT NOVEL FAST DISSOLVING ORAL FILMS

2018 ◽  
Vol 6 (1) ◽  
pp. 1-7
Author(s):  
Pravin Kumar Sharma ◽  
Pankaj Kumar Sharma ◽  
Gajanan N Darwhekar ◽  
Birendra Shrivastava
Keyword(s):  
Dosage Form ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Drug Dissolution ◽  
Solid Dosage Forms ◽  
Onset Of Action ◽  
Cold Sore ◽  
Solid Dosage ◽  
Oral Films ◽  
Oral Dosage Forms

Nowadays, novel fast dissolving oral films (FDF) have come in existence as an alternative dosage form in comparison with tablet, capsules, syrup and other oral dosage forms with respect to patient convenience and compliance. Fast dissolving oral films are helpful to paediatric and geriatric patients who experience difficulties in swallowing traditional oral solid-dosage forms. The FDF drug delivery systems are solid dosage form which disintegrate or dissolve within seconds when placed in the mouth cavity without need of water or chewing. FDF provide better drug dissolution, faster onset of action, bypassing the first pass metabolism of drugs and thus enhance their oral bioavailability with reduced dosing frequency. These formulations are suitable for cough, cold, sore throat, allergenic conditions, nausea, pain, hypertension and CNS disorders. The present review provides the details about the recent advancement in design and development of oral fast dissolving film.

scholarly journals Technologic Considerations of Creation Dosage Form of Original Substance 3,7-diazabicyclo[3.3.1]nonane

2020 ◽  
Vol 9 (4) ◽  
pp. 44-52
Author(s):  
G. E. Brkich ◽  
N. V. Pyatigorskaya ◽  
O. A. Zyryanov ◽  
N. B. Demina ◽  
E. O. Bakhrushina ◽  
...  
Keyword(s):  
Ampa Receptors ◽  
High Performance ◽  
Dosage Form ◽  
Oral Dosage ◽  
Pharmaceutical Substance ◽  
Oral Dosage Form ◽  
Nonane Derivative ◽  
Pass Through ◽  
Ph Range

Introduction. An innovative pharmaceutical substance based on the 3,7-diazabicyclo[3.3.1]nonane derivative provides long-term activation of AMPA receptors and the production of neurotrophic factors, which makes it possible to use it for the treatment of cognitive impairments and rehabilitation of patients who have undergone acute brain hypoxia. Given that this substance is able to be absorbed through the walls of the gastrointestinal tract and pass through the blood-brain barrier, there are no restrictions on the development of an oral dosage form. In addition, the oral dosage form has significant advantages when used in geriatric and pediatric practice.Aim. The aim of the work was to carry out a comparative study of the possibility of using gelatin and hypromellose capsules for the development of the composition and technology for obtaining a dosage form containing a pharmaceutical substance based on a 3,7-diazabicyclo[3.3.1]nonane derivative.Materials and methods. The study of the «Dissolution» test of gelatinous and hypromellose capsules was carried out on an ERWEKA DT 720 «Paddle stirrer» apparatus at a stirrer rotation speed of 50 rpm in three media: pH 1.2, pH 4.5 and pH 6.8. The content of the substance in each sample was determined by high performance liquid chromatography with UV detection.Results and discussion. The results of the development and testing of capsules containing an original pharmaceutical substance of nootropic action based on a derivative of 3,7-diazabicyclo[3.3.1]nonane, which has low pharmaceutical and technological characteristics and is practically insoluble in water, are presented. The D/S value was ≥250.00 ml in each physiological pH range. The results of determining the dissolution of the developed dosage form in three media at pH values of 1.2, 4.5 and 6.8 showed a positive effect of the technology used on the solubility of the substance.Conclusion. A significant increase in the solubility of the practically insoluble substance of the 3,7-diazabicyclo[3.3.1]nonane derivative in the developed dosage form was shown, which is the result of the use of a well-founded complex of excipients and the technology of moisture-activated granulation. According to the results obtained, (77.60 ± 2.50) % of the substance passes into the dissolution medium with a pH of 4.5 in 45 minutes. The research results are used to develop a technological scheme for obtaining a finished dosage form, its indicators and quality standards.

scholarly journals Formulation and Evaluation of Pediatric Paracetamol Elixir Using Natural Colorant

2020 ◽  
Vol 13 (3) ◽  
pp. 180-185
Author(s):  
Mamatha Tirunagari ◽  
Nagadivya Nerella ◽  
Anupama Koneru ◽  
Madihah ◽  
Syed Sarfaraz ◽  
...  
Keyword(s):  
Dosage Form ◽  
Cost Effective ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Physical Parameters ◽  
Natural Colorant ◽  
Solid Dosage ◽  
Pediatric Age Group ◽  
Wide Range ◽  
Oral Dosage Forms

Oral dosage forms are most popular among other dosage forms. In terms of bioavailability liquid dosage form is better than that of solid dosage form. In the present scenario monophagic liquid dosage forms such as syrups, elixirs, throat paints, mouth washes, gargles have gained huge popularity. These are very basic preparations which involve brief processes, machineries and are cost effective also. They come in wide range colours and flavors so as to attract the pediatric age group. Currently colors derived from natural sources are given priority compared to synthetic ones. In this study we formulated paracetamol which is a bitter drug as an elixir using natural colorant from annatto seeds at three different concentrations in F1, F2, and F3. Ethanol. Propylene glycol, mixed fruit juice, chloroform spirit, sucrose syrup and glycerin were also used. These formulations were evaluated for different physical parameters and it showed good results.

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

Sign in / Sign up

Export Citation Format

Share Document