FORMULATION, EVALUATION AND OPTIMIZATION OF RANITIDINE HYDROCHLORIDE FLOATING TABLETS WITH IMPROVED GI ABSORPTION

This study is an attempt to create floating tablets of paracetamol, which, when taken orally, extend the drug's duration of stomach residency and boost its bioavailability. The optimal combination was chosen from preliminary testing batches based on the floating behavior (floating lag time, total floating time). Various grades of polymers, including HPMC K4M, HPMC K15 M, and HPMC K100 M, as well as guar gum, chitosan, and sodium bicarbonate, a gas-generating agent, were used to create the tablet batches. To examine the impact of these polymers on both floating and releasing behaviors, the formulations were created utilizing the direct compression technique. Analgesic Antipyretic medication aims to either stimulate the control of fever and pain management.t he development of floating drug delivery system for paracetamol aims to enhance its therapeutic effectiveness by sustained drug released. Reducing discomfort, manage pain, and preventing recurrence are the objectives of treatment. One of the key components of a continuous medication delivery system is an oral regimen. Drug delivery systems that can float in the stomach for a prolonged amount of time are related to the oral sustained drug delivery system group. Paracetamol in soluble in both acid and alkaline condition it remain adequate in stomach acidic condition. Its solubility influence by PH levels

The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core containing the drug. The findings of the study indicated that all systems demonstrated sustained release. The properties of the polymer used and the structure of each formulation appear to considerably affect drug release and its release rate. The three-layer formulations exhibit lower drug release compared to the matrices. This was due to the fact that the barrier-layers hindered the penetration of liquid into the core and modified drug dissolution and release. The geometrical characteristics/structure of the tablets as well as the weight/thickness of the barriers-layers considerably influence the rate of drug release and the release mechanisms. Kinetic analysis of the data indicated that drug release from matrices was mainly attributed to Fickian diffusion while three-layer tablets exhibited either anomalous diffusion or erosion/relaxation mechanisms. The advantage of Carbopol formulations is that a range of release profiles can easily be obtained through variations in tablet structure and thus Carbopols are appropriate carriers of oral sustained drug delivery systems for soluble drugs such as the isosorbite mononitrate.

Plants and their derivatives have contributed immensely to drug development for their application as medicinal agents or as excipients in preparation of new drug delivery systems. Their use keeps increasing by the day. The rich, yet-to-be fully tapped vegetation available in the African sub-region puts it with great potential to be the next global destination as sources for pharmaceutical excipient. This work reviews published articles on plants and derivatives that have been employed so far in modifying drug delivery. Published articles from databases of PubMed, science direct and google scholar were sourced. Obtained manuscripts were screened for relevance to the topic and currency from reading through the abstract and scanning the body of the work. Gums and mucilages as plant derivatives in their natural form or as changed forms have been well investigated for use in controlled drug delivery. Some of these have been as functional in modifying drug release as many commercially employed excipients in drug delivery. Many plants and plant-derived polymers are generally regarded as safe, easily cultivated, show good functionality as drug additives and can be modified to improve on any less desirable property. Taking advantage of these positive factors will open doors for optimal use of these naturally endowed pharmaceutical excipients

Natural polymer-based plant polysaccharides and proteins have been most widely explored as an adjuvant in the dosage form formulation. Here we design a novel gastro-retentive floating tablet, based on a polysaccharide material from Flaxseed (Linum usitatissimum L.) for Domperidone. After oral administration; Domperidone showed good solubility in acidic pH but significantly reduced solubility in alkaline medium. So that to increase the absorption and bioavailability of Domperidone, it is necessary to increase the retention time in the upper part of the Gastrointestinal tract (GIT) by developing a floating sustained drug delivery system. The directly compressible floating tablets of domperidone were formulated using varying amount of hydroxypropyl methylcellulose K 100 M (HPMC K100 M), Carbopol 934 and Flaxseed mucilage. Hardness, friability, weight variation, thickness, disintegration time of tablet formulations were within acceptable limits. The overall results explained that the optimized formulation F5 prepared by the exact ratio of Flaxseed mucilage, HPMC K100 M, Carbopol, could be more efficient on floating and sustained release of Domperidone in the upper part of GIT as compared to the tablets prepared by using HPMC K100 M and Carbopol 934 only. These findings indicated that Flaxseed can be used to develop novel gastro-retentive sustained release drug delivery system with the double advantage of sustained drug release at the upper part of GIT.

Floating drug delivery systems (FDDS) are controlled release drug delivery systems, which get retained in the stomach for longer periods, thus helping in absorption of drug for the intended duration of time. Gastricretentive drug delivery devices can be useful for the spatial and temporal delivery of many drugs. In general, drugs with narrow therapeutic window and prone to degradation in intestine and colon along with drugs having low retention time in gastrointestinal tract (GIT) are selected for FDDS which helps drugs to stay long time in stomach thus increasing gastric residence time and reduces dosing frequency. The present review article shows the various methods of FDDS for increasing retention time of drugs in GIT. Key words: Dosing frequency, floating drug delivery systems, gastric

The purpose of writing this review on floating drug delivery systems attempts to compile the recent literature with special focus on various floating drug delivery systems approaches that have recently become leading methodologies in the field of site-specific orally administered controlled release drug delivery. In recent years scientific and technological advancements have been made in the research and development of controlled release oral drug delivery systems by overcoming physiological adversities like short gastric residence times and unpredictable gastric emptying times. So generally floating dosage systems form important technological drug delivery systems with gastric retentive behavior and offer several advantages in drug delivery. In this review current and recent development of floating drug delivery system is discussed

Design and Invitro Evaluation of Olmesartan Medoxomil Floating Tablets

Conventional immediate release dosage forms does not control the drug release which leads to low oral bioavailability and more toxic effects. This happens due to multiple dosing and fluctuations in the plasma drug concentrations. Retention of the dosage forms in a specific region of the GIT provides more benefits, for those drugs which have poor absorption in stomach, low solubility and degradation in alkaline pH. FDDS is one among the important system with gastric retention properties. Formulations designed as FDDS, controls the rate of drug release by prolonging the gastric retention for extended hours and improves the absorption as well as bioavailability. This article provides information on recent trends of research and development in FDDS with a special emphasis on its importance for oral controlled drug delivery system. This review article also provides information on category of drugs and different polymers used for FDDS.

Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention

Orally-administered controlled-release drug delivery systems are associated with the shortcomings of relatively short residence times in the human stomach as well as highly variable gastrointestinal (GI) transit times. Thus, considerable intra-individual and inter-individual differences in the bioavailability of drugs are observable. There are numerous drug substances which may benefit from prolonged and controlled GI passage times. As a solution to the problem, gastroretentive drug delivery systems (GRDDS), which feature an enhanced gastric residence time (GRT), were developed. Several approaches are currently used including Floating Drug Delivery System (FDDS), swelling and expanding system, polymeric bioadhesive systems, modified-shape systems, high density system and other delayed gastric emptying devices. The drugs having absorption window in the upper part of Gastro Intestinal Tract (GIT) have enhanced bioavailability when formulated through these techniques. The recent technological development for enhancing GRT including the physiological and formulation variables affecting gastric retention, patented delivery systems, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Despite the extensive research performed in the field of GRDDS, the development, the production, and the evaluation of floating devices are still challenging. The purpose of writing this review was to compile recent literature on pharmaceutical approaches used in enhancing the Gastric Residence Time (GRT). Enhancing the GRT may explore new potentials of stomach as drug-absorbing organ. © 2020 iGlobal Research and Publishing Foundation. All rights reserved.

Background: Medicine is a substance that through its chemical effects brings about changes in biological functions. The GRDDS delivery system is a sustained drug delivery system that can hold drugs back in the stomach for a longer time. The advantages of GRDDS include being able to increase bioavailability, increase the solubility of drugs that are poorly soluble in high pH, can control of therapeutic levels to reduce the occurrence of fluctuations, can extend the half-life so that the frequency of drug administration can be reduced.
 
 Objectives: This study aims to describe the types of GRDDS preparations. The variation is due to a combination of differences in mechanisms and technology.
 
 Method: The design in this study uses a systematic review of the review process that identifies, assesses, and interprets all findings on a research topic.
 
 Result: Floating systems can use expandable polymeric materials such as HPMC and chitosan. The floating mechanism begins with the contact of gastric juices with tablets which causes the polymer to hydrate to form a gel layer that can withstand CO2 gas formed due to the interaction of sodium bicarbonate with citric acid so that the tablets can expand and can float. The oral drug delivery route is the most preferred because it is easy to use. Absorption of oral drugs mostly occurs in the stomach and the intestines.
 
 Conclusion: Therefore, it is necessary to have a drug delivery system that can extend the contact time with the stomach, namely the Gastroretentive Drug Delivery System (GRDDS).

The main goal of an oral controlled drug delivery system is to maximise bioavailability, which should be predictable and repeatable, by administering medications over extended periods of time. Patients choose this approach for a number of reasons, including as affordability, ease of transportation, efficacy, perceived safety, and patient acceptability. The gastrointestinal system's variety results in several physiological limitations for oral delivery. Additionally, a number of variables alter along the gastrointestinal system, all of which affect how well drugs are absorbed. The most crucial factors are surface area, pH, commensal bacteria, gastrointestinal transit time, and enzyme activity. An ideal medication delivery system should have two basic characteristics: one, it should be a single dose for the duration of the therapy, and two, the active medicine should be delivered directly to the site of action. To provide drug delivery systems that, by releasing the medicine in a regulated and predictable way, may reduce side effects, dosage frequency, and changes in plasma drug concentration while remaining in the stomach for an extended amount of time and maintaining active plasma drug concentration. One of the special characteristics of the system is the gastroretentive drug delivery mechanism (GRDDS). New medication delivery techniques continue to spark interest even though oral controlled release dose forms are the most often manufactured. Drugs are rapidly removed from the systemic circulation due to their short half-life and ease of absorption from the GI tract. For these medications to have sufficient therapeutic effectiveness, frequent dosing is required.

Current innovation in pharmaceuticals determine the merits of mucoadhesive drug delivery system is particularly relevant than oral control release, for getting local systematic drugs distribution in GIT for a prolong period of time at a predetermined rate. The demerits relative with the oral drug delivery system is the extensive presystemic metabolism, degrade in acidic medium as a result insufficient absorption of the drugs. However parental drug delivery system may beat the downside related with oral drug delivery system but parental drug delivery system has significant expense, least patient compliance and supervision is required. By the buccal drug delivery system the medication are directly pass via into systemic circulation, easy administration without pain, brief enzymatic activity, less hepatic metabolism and excessive bioavailability. This review article is an outline of buccal dosage form, mechanism of mucoadhesion, in-vitro and in-vivo mucoadhesion testing technique.

Diabetes mellitus (DM) is a metabolic disease characterized by increased blood sugar levels (hyperglycemia) and is associated with impaired function of β cells. The uncontrolled and prolonged hyperglycemia in DM can cause complications. One of the most common is diabetic non-healing wounds, the leading cause of disability in people with diabetes, therefore adjuvant therapy is needed. Compounds from natural ingredients are currently getting the spotlight in recent studies conducted to prove their effect on non-healing wounds, such as Resveratrol (RSV). This review aims to discuss the potential of RSV as a novel adjuvant therapy and its delivery system strategy in the case of diabetic non-healing wounds. We conducted an extensive search from three online scientific databases such as ScienceDirect, ResearchGate, and PubMed on February-March 2023. Keywords used are "resveratrol", "diabetic wound healing", and "diabetes mellitus". As a result, 86 studies were reviewed, and only 79 selected studies met all inclusion criteria. The formulation of RSV nanoparticles in oral drug delivery systems and topical administration has shown promise to overcome the limitations of RSV as adjuvant therapy in diabetic non-healing wounds. The best option that we found through this literature review is the nano-oral drug delivery system as it could minimize drug metabolism in the gastrointestinal tract, therefore the drug bioavailability and drug concentration on the target site could be maximized, even though the systemic side effects might occur.

Colorectal cancer (CRC) is the second global cause of cancer morbidity. Often, potent CRC drugs fail to reach the market, due to the molecule having low solubility levels. Therefore, there is a need to develop a viable, targeted delivery system for hydrophobic drugs. Whey protein isolate (WPI), in the form of hydrogels, has demonstrated loadability with hydrophobic molecules. Hydrophobic cannabidiol (CBD) has demonstrated potential in inhibiting and suppressing CRC tumour growth. Therefore, in this study, WPI hydrogels were assessed as a novel oral hydrophobic drug delivery vehicle, using CBD as a model drug. The hydrogels were analysed in conditions consistent with the alimentary tract. The investigation was performed at pH 2 (stomach), pH 7 (small intestines) and pH 9 (large intestines) and using the enzymes pepsin (stomach) and protease (small and large intestines) to simulate the digestive environment. Polymer swelling assays demonstrated that the swelling potential of the hydrogels was strongly dependent on pH. At pH 2, hydrogels decreased in mass, losing around 10% of their initial mass, while hydrogels in a pH 9 environment increased in mass by approximately 50%. However, the enzymatic degradation of the hydrogels at pH 2 (pepsin, stomach), pH 7 (protease, small intestines) and pH 9 (protease, large intestines) was more pronounced in the neutral-alkaline pH range. Pepsin at pH 2 had no significant effect on the hydrogels. In contrast, protease at pH 9 significantly degraded the hydrogels, resulting in a mass loss of 30-40% from the initial mass. The results suggesting a higher rate of degradation in the intestines rather than in the stomach. Furthermore, CBD release, analysed with U.V. spectroscopy, demonstrated a higher release rate in pH conditions associated with the intestines (pH 7 and pH 9) rather than the stomach (pH 2), suggesting a higher rate of CBD release in regions of the digestive tract affected by CRC. Significantly, the hydrogels significantly reduced the viability of HT29 CRC cells. This study demonstrates the potential of the utilisation of WPI hydrogels as an oral hydrophobic drug delivery system.