Residence Time Of Dosage Form Research Articles

Review on a Oral Mucoadhesive Drug Delivery System

Since the previous four decades, the idea of mucoadhesion has attracted significant interest across a range of pharmaceutics domains.Because mucosal membranes are relatively permeable, the mucoadhesive drug delivery system is a well-liked innovative drug delivery technique, allowing for the rapid uptake of a medication into the systemic circulation and avoiding the first pass metabolism. Recent years have seen the development of a number of mucoadhesive drug delivery systems for nasal, buccal, oral, vaginal, and rectal routes for both local and systemic effects.The mucus membrane, which covers the mucin molecules and the mucosal epithelial surface, can interact with mucoadhesive drug delivery systems. This interaction increases the dosage form's residence time at the site of absorption, increasing medication bioavailability and effectiveness while also enhancing therapeutic results.

Design and Evaluation of Gastroretentive Multiple Units of Dipyridamole: in-vitro and in-vivo human studies

Objective: The pH dependent solubility of Dipyridamole was made to select as a model drug for the formulation of gastroretentive drug delivery system. Dipyridamole is highly soluble in acidic pH and as the pH increases the solubility of the drug decreases. The study was planned to formulate, characterize with in-vitro and in-vivo evaluation in human volunteers.
 Method: In this study floating mini matrix tablets of Dipyridamole was formulated using HPMC grade polymers by wet granulation method and prepared multiple units equivalent to one dose were filled in one 000 size empty gelatin capsule. The prepared multiple units were subjected to physical evaluation, in-vitro drug release, and stability studies as per ICH guidelines. The in-vivo radiographic studies were conducted for determining the residence time of dosage form in human subjects.
 Results: All the prepared batches showed good physical properties and in-vitro buoyancy. The optimized FD7 formulation remained buoyant for more than 12 h with drug release of more than 90% in 12 h. The drug release kinetics for optimized formulation FD7 followed a first order kinetics with non fickian mechanism. Formulation FD7 was selected as the best formulation based on the in-vitro characteristics and subjected for stability and in-vivo radiographic studies. These studies revealed that the multiple units were stable during the stability period and remained in the stomach for upto 6 h in human subjects.
 Conclusion: Based on in-vitro characteristics and in-vivo radiographic studies, formulation FD7 was concluded as the best formulation among others. Due to increase in gastric retention time, by choosing floating mini matrix tablets we can improve patient compliance and ensure better disease management.
 Keywords: Dipyridamole, Mini matrix tablets, In-vitro buoyancy, Stability studies Radiographic Studies

A Survey on Mucoadhesive Thermoreversible Drug Delivery System with special Emphasis on Recto-Anal Region for the Treatment of Internal Hemorrhoids

The concept of combination of thermo reversibility and mucoadhesion has achieved a much valuable interest in various fields of pharmaceutics. Mucoadhesive drug delivery systems interact with the mucus layer covering the mucosal epithelial surface, and mucin molecules and increase the residence time of the dosage form at the site of absorption. Thermoreversible gels are the hydrogels that are liquids at room temperature but undergo gelation when in contact with body fluids or change in pH. A major problem faced by conventional formulation in various routes of administration viz. nasal, ocular, vaginal, rectal, etc is drainage of instilled formulation, poor patient compliance as in the case of vaginal and rectal delivery system. Also, blurred vision and irritation to mucosa is observed in the case of ocular and nasal delivery respectively. The drainage of the formulation results in inaccurate dose delivery thus decreasing the bioavailability of the drug which demands an increase in the frequency of the administration. To overcome these limitations, there is need of novel delivery system such as thermoreversible mucoadhesive insitu gel which provides an ease of administration and improved patient compliance as these smart delivery system is free flowing liquid at ambient temperature and gels at physiological temperature which is higher than the LCST (low critical solution temperature) of thermoreversible polymer. The combined effect of mucoadhesion and thermoreversible property will enhance prolongation of residence time of dosage form and the accuracy of the dose in body cavity respectively, leading to increased bioavailability of the drug. This review focuses on benefits of mucoadhesive thermoreversible system of drug delivery through rectum for the treatment of internal hemorrhoids.

Mucoadhesive Drug Delivery Systems: A Review of Recent Developments

Purpose: The aim of this article is to present a review of mucoadhesion drug delivery systems. The review covers the mucoadhesive concepts, polymers used, theories and mechanisms of mucoadhesion, and factors affecting the mucoadhesive dosage forms. Study Design: An extensive review was carried out on mucoadhesion formulations, applications, mechanisms, theories, and polymers used in these dosage forms. Results: Mucoadhesive drug delivery system can interact with the mucus membrane, which covers the mucin molecules and mucosal epithelial surface. This interaction leads to an increment of the dosage form residence time at the site of absorption and hence increasing the bioavailability, efficacy of drugs, and improving therapeutic outcomes. Polymers are used to provide muco-adhesion of the dosage form, enhancing drug release pattern, solubility and dissolution of inadequately soluble drugs. Conclusion: Mucoadhesive drug delivery systems were found to be the best alternative approaches for the traditional dosage forms to enhance bioavailability of poorly soluble drugs and to avoid GIT degradation and first pass metabolism of some drugs.

Development and Evaluation of Amoxicillin Loaded Carbopol 934P Mucoadhesive Microcapsules for Sustained Drug Release for H. pylori Treatment

Amoxicillin (α-amino-p-hydroxybenzyl-penicillin) is a semi-synthetic, orally absorbed and widely prescribed β-lactam antibiotic. It is now widely used for eradication of gastric Helicobacter pylori infection combined with a second antibiotic and an acid‐suppressing agent despite its short elimination half-life of one hour. The purpose of this study was to develop and evaluate amoxicillin loaded carbopol 934P mucoadhesive microcapsules for sustained drug release at the gastric mucosa to prolong the residence time of dosage form in the stomach and to achieve controlled drug release for more effective H. pylori eradication. Amoxicillin mucoadhesive microcapsules were formulated by ion gelation technique using 32 factorial designs. A 32 full factorial design was used to derive the statistical equation, ANOVA analysis, contour plots and 3D response surface plots. FT- IR (4000 cm-1- 450 cm-1) analysis of amoxicillin and with polymers was performed by using potassium bromide pellet method. Different polymer ratios of carbopol 934P and sodium alginate were used to formulate by nine formulations (F1 to F9) amoxicillin mucoadhesive microcapsules. The prepared formulations were characterized by determining their percentage of yield, particle size, percentage of entrapment efficiency, swelling index, percentage of mucoadhesion and percentage of drug release. Amoxicillin and used polymers are found to be compatible with no interaction reported by FTIR analysis. The optimized formulation (F9) exhibited a high drug entrapment efficiency of 96.04±0.03%, particle size of 847.2518±0.06 μm, yield of 98.86±0.01%, swelling index of 120.09±0.06%, and mucoadhesion of 67.00±0.02 after 8 h. A successful sustained drug release was achieved for more than 14 h. In-vitro dissolution test for optimized formulation (F9) demonstrated a slower release behavior in 0.1N hydrochloric acid followed by linear release profile in pH 7.4 phosphate buffer. The drug-to-polymer-to-polymer ratio had a more significant effect on the dependent variables. The release kinetic study of optimized formulation (F9) displayed a good fitting with zero order behavior and Korsmeyer-Peppas model has confirmed a non-Fickian release. The developed mucoadhesive amoxicillin microcapsules were observed to have adhered strongly with gastric mucosa with approximately 14 h of prolonged stay expecting improved bioavailability and reduced dosing frequency and subsequently improving patient’s compliance. The concentration of carbopol 934P and sodium alginate had highly significant effects on depended variables. The present study concludes that amoxicillin mucoadhesive microcapsules can be effectively used for the more effective treatment of H. pylori infection.

Formulation and In-Vitro Evaluation of Amoxicillin Mucoadhesive Microcapsules for the Treatment of Helicobacter pylori Infection

Event Abstract Back to Event Formulation and In-Vitro Evaluation of Amoxicillin Mucoadhesive Microcapsules for the Treatment of Helicobacter pylori Infection Senthil Adimoolam1*, Bolai Paul1 and Mohd Javed Quereshi1 1 Mahsa University, Malaysia Background Amoxicillin (α-amino-p-hydroxybenzyl-penicillin) is a semi-synthetic, orally absorbed and widely prescribed β-lactam antibiotic. It is widely used for eradication of gastric Helicobacter pylori infection combined with a second antibiotic and an acid‐suppressing agent despite its short elimination half-life of one hour. The purpose of this study was to develop and evaluate amoxicillin loaded HPMC K15M mucoadhesive microcapsules for sustained drug release at the gastric mucosa to prolong residence time of dosage form in stomach to achieve more effective H. pylori eradication. Methods Amoxicillin mucoadhesive microcapsules were formulated by ion gelation technique by using different mucoadhesive polymers HPMC K15M and sodium alginate with varying concentration. A 32 full factorial design was applied to derive statistical equation, ANOVA analysis, contour plots and 3D response surface plots. The nine formulations were subjected to evaluation of percentage yield, entrapment efficiency, swelling index, mucoadhesion and in vitro drug release. Results Among nine formulations (F1 – F9), F9 exhibited a promising drug entrapment efficiency (92.50±0.03%), percentage yield (97.50±0.02%), percentage mucoadhesion (65±0.03 after 8 h) and in vitro drug release more than 14 h. The kinetics of the drug release of microcapsules (F9) showed good fitting with zero order and Korsmeyer-Peppas model followed by a non-Fickian release. The ANOVA analysis shows highly significant effects on depended variable. Conclusion Therefore, amoxicillin mucoadhesive microcapsules can be effectively used in the treatment of H. pyloriinfection. Acknowledgements Authour would like to thank MAHSA University Management for financial support fro this research Keywords: microcapsule, Amoxicillin, mucoadhesion, Entrapment efficiency, Percentage yield Conference: International Conference on Drug Discovery and Translational Medicine 2018 (ICDDTM '18) “Seizing Opportunities and Addressing Challenges of Precision Medicine”, Putrajaya, Malaysia, 3 Dec - 5 Feb, 2019. Presentation Type: Poster Presentation Topic: Miscellaneous Citation: Adimoolam S, Paul B and Quereshi M (2019). Formulation and In-Vitro Evaluation of Amoxicillin Mucoadhesive Microcapsules for the Treatment of Helicobacter pylori Infection. Front. Pharmacol. Conference Abstract: International Conference on Drug Discovery and Translational Medicine 2018 (ICDDTM '18) “Seizing Opportunities and Addressing Challenges of Precision Medicine”. doi: 10.3389/conf.fphar.2018.63.00075 Copyright: The abstracts in this collection have not been subject to any Frontiers peer review or checks, and are not endorsed by Frontiers. They are made available through the Frontiers publishing platform as a service to conference organizers and presenters. The copyright in the individual abstracts is owned by the author of each abstract or his/her employer unless otherwise stated. Each abstract, as well as the collection of abstracts, are published under a Creative Commons CC-BY 4.0 (attribution) licence (https://creativecommons.org/licenses/by/4.0/) and may thus be reproduced, translated, adapted and be the subject of derivative works provided the authors and Frontiers are attributed. For Frontiers’ terms and conditions please see https://www.frontiersin.org/legal/terms-and-conditions. Received: 26 Oct 2018; Published Online: 17 Jan 2019. * Correspondence: Dr. Senthil Adimoolam, Mahsa University, Kuala Lumpur, Malaysia, senthil@mahsa.edu.my Login Required This action requires you to be registered with Frontiers and logged in. To register or login click here. Abstract Info Abstract The Authors in Frontiers Senthil Adimoolam Bolai Paul Mohd Javed Quereshi Google Senthil Adimoolam Bolai Paul Mohd Javed Quereshi Google Scholar Senthil Adimoolam Bolai Paul Mohd Javed Quereshi PubMed Senthil Adimoolam Bolai Paul Mohd Javed Quereshi Related Article in Frontiers Google Scholar PubMed Abstract Close Back to top Javascript is disabled. Please enable Javascript in your browser settings in order to see all the content on this page.

Formulasi dan Evaluasi Granul Gastroretentive Mukoadhesif Amoksisilin

Amoxicillin is a semisynthetic antibiotic, belonging to the β-Lactam family, which is effective for bacterial infection treatment, especially for Helicobacter pylori infection. In this research, Amoxicillin was formulated as mucoadhesive granules dosage form to improve their effectivenesses by increasing the residence time of dosage form in the stomach. Mucoadhesive granules were prepared by wet granulation method in ten formulas using HidroxypropylMethyl cellulose, Methyl cellulose and Ethyl cellulose as mucoadhesive polymers. Granules were evaluated for moisture content, flow rate, angle of repose, density, mucoadhesive strength with wash off test, and dissolution. The results of this researchshowed that formula IB with 50% HPMC has best mucoadhesive strength with percentage of mucoadhesion 20% in 90 minutes of wash off test, and also formula IB is slowest formula in releasing of drug, with percentage of drug released is 55,76% in 15 minutes and 104,01% in 180 minutes.

Gastroretentive Controlled Release Glibenclamide Oral Tablet Formulation

Hydroxypropyl methylcellulose (HPMC-4000cps, fixed amount), various contents of calcium hydroxide, stearyl alcohol, magnesium stearate, different drug: PVP ratios and altered tablet hardness were used to design floating tablet formulation capable to deliver glibenclamide in a sustained manner. Both full factorial and Box-Wilson designs, in consecutive manner, were used to investigate for the influences of these formulation variables on the developed dosage form performance and drug release. Tablet hardness has revealed an influential effect on tablet onset of floating, and drug release was shown to be more evident in the initial phase (p<0.05). Loading level of calcium hydroxide, stearyl alcohol and tablet swellability all have showed profound enhancing effects on duration of tablet buoyancy and drug release. Glibenclamide release from tablets of the invention was shown to follow the anomalous type (n=0.8212-1.0244). Application of statistical and mathematical modeling has enabled the optimization of the developed tablet formulation to meet selective constraints for floating, hardness and drug release. The optimized buoyant tablet formulation with highest CI revealed hardness of 50 N, immediate onset of floating and floating duration >6 hours. Concerning drug release, the formula showed evidence of 25 and 84% drug release after 1 and 6 hours, respectively, with T50% of 3 hours. Moreover, release kinetics of the drug from the optimized formula was shown to be near the desired zero order type of release (n=0.8897 or 0.0132; r2=0.9993). The in vivo dosage form residence time study in six human subjects demonstrated that the developed tablet formulation retained in the stomach for more than four hours under fasting conditions. Comparative bioavailability study revealed that floating tablets showed 2-2.5 times increase in AUC (p≤ 0.1) indicating the sustained release tendency of the drug from the floating tablet formulation. The three months based stability study indicated that the drug and the dosage form retained their initial physical characters in both accelerated and normal conditions for the test duration as far as blister pack is considered.

Formulation and Development of In Situ Nasal Gelling Systems for Quetiapine Fumarate-Loaded Mucoadhesive Microemulsion

Purpose Quetiapine fumarate (QF), a novel antipsychotic agent, has got poor brain uptake because of its poor oral bioavailability (9 %) due to extensive first-pass metabolism. The aim of this study was to develop QF microemulsion formulation to enhance the bioavailability and to accomplish the intranasal delivery of the drug to the brain. Mucoadhesive in situ gelling systems of QF were formulated to increase the residence time of dosage form and provide sustained release of the drug.

SITE SPECIFIC DRUG DELIVERY THROUGH NASAL ROUTE USING BIOADHESIVE POLYMERS

This review explains some aspects of mucoadhesion related to the nasal drug delivery system. On the first count, the theories of the adhesion of mucoadhesive polymers to the mucosa epithelium are described. Secondly, the characteristics and application of several widely used mucoadhesive polymers in nasal drug delivery are presented. The nasal mucosa provides a potentially good route for systemic drug delivery. One of the most important features of the nasal route is that it avoids first-pass hepatic metabolism, thereby reducing metabolism. The application of mucoadhesive polymers in nasal drug delivery systems has gained to promote dosage form residence time in the nasal cavity as well as improving intimacy of contact with absorptive membranes of the biological system. The aspiration of any drug delivery system is to endow with a therapeutic amount of drug to the proper site in the body to achieve promptly &amp; then uphold the desired drug concentration. That is why the drug delivery system should deliver drug at a state dictated by the needs of the body over a specified period of treatment. This idealized objective points to the two aspects most important to drug delivery, namely, spatial placement relates to targeting a drug to a specific organ or tissue while temporal delivery refers to the control of rate of drug delivery to the target tissue. Over the last few decades, the relevance of mucoadhesive polymers in nasal drug delivery systems has gained significance among pharmaceutical scientists as a means of promoting dosage form residence time in the nasal cavity as well as for improving intimacy of contact with absorptive membranes of the biological system. In addition, the improved paracellular absorption subsequent the swelling of the mucoadhesive polymers on the nasal membranes provides an important way for the absorption of the macromolecules through the nasal cavity. Keywords: Nasal route, Mucoadhesive polymers, Paracellular absorption,

Formulasi Sediaan Granul Mukoadhesif Kombinasi Ekstrak Kulit Batang Mimba (Azadirachta indica A. Juss) dan Kunyit (Curcuma domestica val.)

Neem bark (Azadirachta indica A.Juss) and turmeric (Curcuma domestica Val.) extracts have been found posses gastroprotective effect so that they are used in the treatment of gastric ulcer. Administration of combination of both extracts can give synergistic effect so that the administration dose can be reduced. In this research, combination of neem bark and turmeric extracts were formulated as mucoadhesive granules to improve their effectivenesses by increasing the residence time of dosage form in the stomach. Mucoadhesive granuleswere prepared by wet granulation method in six formulas using HPMC, Carbopol, and combination of HPMC and Carbopol as mucoadhesive polymers. Granules were evaluated for particle size distribution, swelling, mucoadhesive strength with bioadhesive in vitro test and wash off test, and dissolution. Bioadhesive in vitro test showed that all formulas have goodmucoadhesive strength.Wash off test showed that combination of HPMC and Carbopol can improve mucoadhesive strength of formulas. Mucoadhesive strength increased with the increasing of HPMC. The result of this research indicated that formula with combination ofHPMCand Carbopol (2:1) showed best mucoadhesive strength with percentage of mucoadhesion 98.67%in bioadhesive in vitro test and 38.00% in wash off test.

A review on mucoadhesive polymer used in nasal drug delivery system

This update review is on mucoadhesive polymers used in nasal dosage forms. The nasal mucosa provides a potentially good route for systemic drug delivery. One of the most important features of the nasal route is that it avoids first-pass hepatic metabolism, thereby reducing metabolism. The application of mucoadhesive polymers in nasal drug delivery systems has gained to promote dosage form residence time in the nasal cavity as well as improving intimacy of contact with absorptive membranes of the biological system. The various new technology uses in development of nasal drug delivery dosage forms are discussed. The various dosage forms are vesicular carriers (liposome, noisome), nanostructured particles, prodrugs, in situ gelling system with special attention to in vivo studies.

The application of mucoadhesive polymers in nasal drug delivery

Background: Over the last decades, the application of mucoadhesive polymers in nasal drug delivery systems has gained interest among pharmaceutical scientists as a means of promoting dosage form residence time in the nasal cavity as well as improving intimacy of contact with absorptive membranes of the biological system. In addition, the enhanced paracellular absorption following the swelling of the mucoadhesive polymers on the nasal membranes provides an important way for the absorption of the macromolecules through the nasal cavity. Method: This paper describes some aspects of mucoadhesion related to the nasal drug delivery system. First the theories of the adhesion of mucoadhesive polymers to the mucosa epithelium are described. Then the characteristics and application of several widely used polymers in nasal drug delivery are presented. Finally, the influences of dosage form on the nasal absorption of drugs in the mucoadhesive polymer-based formulations are discussed. Conclusion: The mucoadhesive polymers have enormous potential for the delivery of therapeutic macromolecules, genes, and vaccines through the nasal cavity with high drug bioavailability.

The application of mucoadhesive polymers in nasal drug delivery.

Over the last decades, the application of mucoadhesive polymers in nasal drug delivery systems has gained interest among pharmaceutical scientists as a means of promoting dosage form residence time in the nasal cavity as well as improving intimacy of contact with absorptive membranes of the biological system. In addition, the enhanced paracellular absorption following the swelling of the mucoadhesive polymers on the nasal membranes provides an important way for the absorption of the macromolecules through the nasal cavity. This paper describes some aspects of mucoadhesion related to the nasal drug delivery system. First the theories of the adhesion of mucoadhesive polymers to the mucosa epithelium are described. Then the characteristics and application of several widely used polymers in nasal drug delivery are presented. Finally, the influences of dosage form on the nasal absorption of drugs in the mucoadhesive polymer-based formulations are discussed. The mucoadhesive polymers have enormous potential for the delivery of therapeutic macromolecules, genes, and vaccines through the nasal cavity with high drug bioavailability.

Mucoadhesive Drug Delivery Systems

Mucoadhesion in drug delivery systems has recently gained interest among pharmaceutical scientists as a means of promoting dosage form residence time as well as improving intimacy of contact with various absorptive membranes of the biological system. Besides acting as platforms for sustained-release dosage forms, bioadhesive polymers can themselves exert some control over the rate and amount of drug release, and thus contribute to the therapeutic advantage of such systems. This paper describes some aspects of bioadhesion such as mucus layer, mucoadhesion, and theories of bioadhesion to explain the adhesion mechanism. The factors important to mucoadhesion, the methods used to study bioadhesion, and bioadhesive polymers are described. The methods that evaluate the mucoadhesive dosage forms and finally the bioadhesive drug delivery systems designed for several therapeutic purposes are presented.

Polymers and Permeation Enhancers: Specialized Components of Mucoadhesives

Mucoadhesive polymers have recently gained interest among pharmaceutical scientists as a means of improving drug delivery by promoting dosage form residence time and contact time with the mucous membranes. Mucoadhesion occurs between two surfaces, one of which is a mucous membrane and another is drug delivery system. Pharmaceutical aspects of mucoadhesion have been the subject of great interest during recent years because mucoadhesion could be a solution for bioavailability problems that result from a too short length of stay of the pharmaceutical dosage form at the absorption site within the gastro-intestinal tract. It has been a great challenge to the pharmaceutical sciences in order to enhance localised drug delivery or to deliver ‘difficult’ molecules (proteins and oligonucleotides) into the systemic circulation. Mucoadhesive systems remain in close contact with the absorption tissue, the mucous membrane, releasing the drug at the site of action leading to increase in bioavailability (both local and systemic effects). Extending the residence time of a dosage form at a particular site and controlling the release of drug from the dosage form are useful especially for achieving controlled plasma level of the drug as well as improving bioavailability. The present review describes mucoadhesion, mucoadhesive polymers and use of these polymers in designing different types of mucoadhesive drug delivery systems. Key words: Mucoadhesion; Mucoadhesive polymers; Mucoadhesive force; Bioadhesive property. DOI: http://dx.doi.org/10.3329/sjps.v4i1.8878 SJPS 2011; 4(1): 91-95