Bioavailability Of Medications Research Articles

Gastroretentive Drug Delivery Systems with improved Floating and Swelling Capabilities

For medications with an absorption window in the stomach and upper part of small intestine, a controlled drug delivery system with a longer stomach residence duration can be particularly useful. Rapid gastrointestinal transit may cause drug delivery system above the absorption zone to only partially release drug, which would reduce the supplied dose's effectiveness. The main drawbacks are linked to the non-uniformity of drug absorption across the alimentary canal and the inter- and intra-subject variability of gastro-intestinal transit time. The bioavailability of medications is predicted to be improved by floating delivery systems, which are designed to stay buoyant on the gastric contents for an extended period of time. Floating in combination with swellable system gaining attention due to their wide applicability in the targeting of drugs to stomach. These floating and swellable tablet have the advantage that they remain buoyant and swells to 2-3 folds in gastric fluid.

Quality by Design Approach: Progress in Pharmaceutical method Development and Validation

Pharmaceutical analysis plays a significant role in pharmaceutical formulation quality assurance and control. Due to the pharmaceutical industries' rapid expansion and the production of pharmaceuticals all over the world, there is a greater need for novel analytical procedures in this sector. Establishing the identification, purity, physical properties, and potency of medications as well as the medication's bioavailability and stability is the goal of analytical method development. A few new drug applications were recently given regulatory flexibility by the Food and Drug Administration for an analytical method based on quality by design. With Quality by design, product design and development are performed methodically. Analytical methodologies have similar opportunities for implementing Quality by design as production procedures do. It consequently enhances formulation design, development efficiency, and capacity. The underpinnings of the QbD approach have been explored in this article due to their use in the creation and validation of analytical procedures. Additionally, a summary of experimental studies reporting the application of the QbD methodology to method development is included.

REVIEW ON COMPREHENSIVE DESCRIPTION OF DEVELOPMENT AND ASSESSMENT OF CO-CRYSTAL DRUG DELIVERY SYSTEM

Over the past few decades, co-crystal Drug Delivery System (DDS) has attracted interest due to their potential to increase the solubility, stability, and bioavailability of medications that aren't sufficiently soluble. In this study, we factualized to develop a co-crystal chemical delivery system utilizing an experimental model. We utilized caffeine and succinic acid as model chemicals and prepared co-crystals utilizing different methods, including solvent evaporation, grinding, and spray drying. The co-crystals have been characterized utilizing X-ray powder diffraction, Fourier-transform infrared spectroscopy, and differential scanning calorimetry. The solubility and dissolution rate of the co-crystals has been evaluated in simulated digestive and intestinal juices. The outcomes showed that when compared to co-crystals made utilizing the solvent evaporation and spray drying procedures, those organized utilizing the grinding approach exhibited the maximum solubility and dissolution rate. This study underlines the potential of co-crystals as a workable method for enhancing the administration of pharmaceuticals that are not adequately soluble and provides a helpful experimental paradigm for the development of co-crystal chemical delivery systems.

Formulation and Evaluation of Mouth Dissolving Film of Imipramine HCL

The main objective of the present study outlines a systematic approach for Design and Evaluation of Fast Dissolving Oral Films of Imipramine HCl to enhance the therapeutic efficacy and provide rapid onset of action in patients suffering from depression Because of patient may have trouble in swallowing a tablet or capsules. Mouth dissolving film is the most advanced oral solid dosage form due to its flexibility and comfort in use. Mouth dissolving films are oral solid dosage form that disintegrate and dissolve within a minute when placed in mouth without taking water or chewing. This dosage form allows the medication to bypass the first pass metabolism so bioavailability of medication may be improved. Fast dissolving Oral film of Imipramine Hydrochloride was formulated by using solvent casting method with different concentrations of HPMC-E3. Film forming property of various grades of HPMC was investigated based on preliminary characteristics of various batches of FDOFs.

Recent Advancement in Self Emulsifing Drug Delivery System

Every day, researchers make new attempts to identify neurotherapeutics, but few of them make it to clinical trials. The main cause is their low bioavailability, which is connected to low water solubility, low permeability through biological membranes, and the hepatic first-pass metabolism. However, the most significant challenge in administering drugs to the brain is overcoming the blood-brain barrier. In order to get around it, intranasal administration has become more popular, sometimes even more so than oral administration. Because of its structure, the nasal cavity can bypass the blood-brain barrier and transport drugs to the brain directly. Nasal absorption increases the systemic bioavailability of highly processed substances because they bypass the hepatic first-pass metabolism. However, due to their unique physicochemical properties, most neurotherapeutics must be synthesized in lipidic nanosystems as self-emulsifying drug delivery systems (SEDDS). To load large quantities of lipophilic medicines into micro or nanoemulsions, these isotropic mixes of oils, surfactants, and co-surfactants are diluted in water. The goal of SEDDS is to increase the stability of labile pharmaceuticals against enzymatic activity, boost drug penetration through absorptive membranes, and reduce the likelihood of drug precipitation at absorption sites. Therefore, improved brain targeting and bioavailability of medications might be anticipated by combining the benefits of SEDDS with those of the intranasal route for brain delivery. In order to better understand the mechanisms involved in the intranasal administration of pharmaceuticals loaded in SEDDS, this paper provides a comprehensive characterization of SEDDS as a lipidic nanosystem. Finally, the in vivo effects of intranasal or oral delivery of SEDDS, showing their superiority over standard solutions or suspensions, are described.

Formulation and evaluation of mouth dissolving film of antihypertensive agentFormulation and evaluation of mouth dissolving film of antihypertensive agent

Mouth dissolving film is the one of the most advanced oral solid dosage form because of its flexibility and comfort in use. Mouth dissolving films are oral solid dosage form that disintegrate and dissolve within a minute when placed in mouth without taking water or chewing. This dosage form allows the medication to bypass the first pass metabolism so bioavailability of medication may be improved .Mouth dissolving film has potential to improve onset of action lower the dosing and eliminate the fear of chocking. Formulation of mouth dissolving films involves both the visual and performance characteristics as plasticized hydrocolloids, API taste masking agents are being laminated by solvent casting and semisolid casting method. Solvent casting method being the most preferred method over other methods because it offers great uniformity of thickness and films prepared having fine glossy look and better physical properties. Mouth dissolving films are evaluated for its various parameters like thickness, physical property like folding endurance, disintegration and dissolution time. This review gives an idea about formulation techniques, evaluation parameters, overview on packaging and some available marketed products of mouth dissolving films.

Methods for Improving the Solubility of Water-Insoluble Drugs: A Comprehensive Review

Orally directed medications totally ingest just when they show reasonable dissolvability in gastric medium and such medications shows great bioavailability. The solvency and disintegration properties of medications assume a significant part during the formulation development. Greater part of the disappointments in the new medication improvement have been credited to poor water dissolvability of medication. It is widely accepted that poor water dissolvability is quite possibly the most every now and again experienced troubles in the field of pharmaceutics. Low solvency and ensuing unacceptable disintegration rate regularly bargain oral bioavailability. There are most remedial specialists used to create fundamental impacts by oral course that are the favored method of organization inferable from its few benefits and high quiet consistence contrasted with different courses. Thusly the current methodologies being utilized for BCS class II medications, along with retention enhancers, can be applied to detail class IV compound. Effervescent Assisted Fusion Technique, Solvent Evaporation method, Microemulsion, Liposomes are some imperative methodologies regularly utilized to improve the dissolvability of ineffectively water dissolvable medications. Determination of technique for solvency upgrade relies on drug qualities like dissolvability, substance nature, melting point, retention site, actual nature, pharmacokinetic conduct, etc, measurement structure necessity like tablet or capsule formulation, strength, quick or modified release. This review features the novel strategies accessible for improving solvency, disintegration and bioavailability of medications with poor fluid dissolvability.

A REVIEW ON MOUTH DISSOLVING FILM

Oral route of Mouth dissolving film is the most advanced oral solid dosage form due which it is very much in use now a day because of it’s flexibility and comfort. Mouth dissolving films are oral solid dosage form that disintegrate and dissolve within few minutes when placed in tongue without taking water. This dosage form allows the medication to bypass the first pass metabolism, so that the bioavailability of medication can be improved .Mouth dissolving film has potential to improve onset of action lower the dosing and eliminate the fear of chocking. Formulation of mouth dissolving films involves both the visual and performance characteristics as plasticized hydrocolloids, API’s taste masking agents are being laminated by solvent casting and semisolid casting method. Solvent casting method being the most preferred method over other methods because it offers great uniformity of thickness and films prepared having fine glossy look and gives them the better physical properties. Mouth dissolving films are evaluated for its various parameters like dissolution time, disintegration thickness, physical property like folding endurance. This review gives an idea about formulation techniques, evaluation parameters, overview on packaging and some available marketed products of mouth dissolving films.

Novel Methods to Enhance Solubility of Water Insoluble Drugs

Orally directed medications totally ingest just when they show reasonable dissolvability in gastric medium and such medications shows great bioavailability. The solvency and disintegration properties of medications assume a significant part during the formulation development. Greater part of the disappointments in the new medication improvement have been credited to poor water dissolvability of medication. It is widely accepted that poor water dissolvability is quite possibly the most every now and again experienced troubles in the field of pharmaceutics. Low solvency and ensuing unacceptable disintegration rate regularly bargain oral bioavailability. There are most remedial specialists used to create fundamental impacts by oral course that are the favored method of organization inferable from its few benefits and high quiet consistence contrasted with different courses. Thusly the current methodologies being utilized for BCS class II medications, along with retention enhancers, can be applied to detail class IV compound. Effervescent Assisted Fusion Technique, Solvent Evaporation method, Microemulsion, Liposomes are some imperative methodologies regularly utilized to improve the dissolvability of ineffectively water dissolvable medications. Determination of technique for solvency upgrade relies on drug qualities like dissolvability, substance nature, melting point, retention site, actual nature, pharmacokinetic conduct, etc, measurement structure necessity like tablet or capsule formulation, strength, quick or modified release. This review features the novel strategies accessible for improving solvency, disintegration and bioavailability of medications with poor fluid dissolvability.

The Impact of Microsponge and Microsphere on Improving Oral Bioavailability of Medications: A Short Review

While many diseases require an efficient drug delivery technology that has the ability to improve bioavailability and alleviate side effects, various types of gastroretentive drug delivery systems (GRDDS) have been developed in order to overcome the obstacles, which are related to a narrow absorption window, instability, site of action, side effects, and dosing frequency. In this context, microsponge and microsphere systems depict two different types of GRDDS, aiming to provide adequate time for active ingredients to be absorbed in the stomach despite the variation in releasing mechanisms of the entrapped ingredients. For the successful designing of these systems, it is essential to optimize the characterizations of the formulated microparticles by considering physiological, pharmaceutical, and patient-related factors, which have a dramatic impact on the efficacy. Consequently, they will demonstrate different behaviors at the desired site of action, determining which systems are showing superiority compared to others. However, each microparticle system has some advantages over the others, providing more options for researchers to ease the difficulties that exist with conventional oral dosage forms. Therefore, this review aims to shed the light on critical factors that have significant impacts on microsponge and microsphere systems and addresses their advantages and disadvantages, providing an understanding of these criteria in order to optimize the drug systems.

Formulation and evaluation of gastro-retentive floating tablets of terbinafine

Gastro-retentive dosage forms enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal tract and improve the bioavailability of medications those are characterized by a narrow absorption window. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of terbinafine were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of terbinafine were evaluated tablet hardness, uniformity of weight, friability, uniformity of content, in vitro buoyancy test, swelling index, in vitro dissolution study and stability study. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of terbinafine shown that the formulation F5 was found to be the best formulation as it releases 96.22% terbinafine in a controlled manner for an extended period of time (up to 480 min). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. Prepared floating tablets of terbinafine may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.

Intranasal Local Anaesthesia:A Recent Advancement in Pediatric Dentistry

Intranasal local anaesthesia is a recent advancement in pediatric dentistry. Here we try to give a better and comfortable mode of administration of local anaesthesia for kids for their better cooperation. Intranasal anaesthesia in other words needle free anaesthesia has rapid onset, ease of delivery, painless administration, high medication bio availability as its advantages. Kovacaine mist is a spray type of intranasal local anaesthesia that is effective only on permanent and primary anteriors, primary molars, permanent premolars.

A Review on Mouth Dissolving Film

Mouth dissolving film is the most advanced oral solid dosage form due to its flexibility and comfort in use. Mouth dissolving films are oral solid dosage form that disintegrate and dissolve within a minute when placed in mouth without taking water or chewing. This dosage form allows the medication to bypass the first pass metabolism so bioavailability of medication may be improved .Mouth dissolving film has potential to improve onset of action lower the dosing and eliminate the fear of chocking. Formulation of mouth dissolving films involves both the visual and performance characteristics as plasticized hydrocolloids, API taste masking agents are being laminated by solvent casting and semisolid casting method. Solvent casting method being the most preferred method over other methods because it offers great uniformity of thickness and films prepared having fine glossy look and better physical properties. Mouth dissolving films are evaluated for its various parameters like thickness, physical property like folding endurance, disintegration and dissolution time. This review gives an idea about formulation techniques, evaluation parameters, overview on packaging and some available marketed products of mouth dissolving films.
 Keywords: Mouth dissolving film, solvent casting, fast disintegration

Evaluation of the anticancer activity of sprout extract-loaded nanoemulsion of N. sativa against hepatocellular carcinoma

Nigella sativa L. belonging to Ranunculaceae family is an important medicinal spice which has been utilised to treat various chronic diseases. Lipid nanoemulsions containing oil from medicinal plants have shown to enhance drug dissolvability, diminish symptoms of different powerful medications and enhance the bioavailability of medications, in contrast with conventional formulations. In the present study, aqueous titration method was used to prepare nanoemulsion. The optimised formulation (NE11) with the mean particle size of 37.47 nm showed a minimum viscosity of 0.547 cps and maximum drug release (98.2%) in 24 h. The stability study showed considerably stable formulations at refrigerator temperature as compared to room temperature. The cancer cell line studies confirmed that 5d sprout extract of N. sativa nanoemulsion reduced the cell viability (p < .05) and increased colony formation, ROS intensity and chromatin condensation. All data such as colony formation, ROS intensity and chromatin condensation are represented as mean ± SD (p < .001) treated cells for 48 hours. Our results concluded that the development of nanoemulsion could be an efficient carrier for drug delivery.

Sometimes Treatment Is Hard To Swallow

Sometimes Treatment Is Hard To Swallow

Thickening agents used for dysphagia management: effect on bioavailability of water, medication and feelings of satiety

Dysphagia is the medical term for difficulty swallowing. Thickened liquids are often used in the management of dysphagia to improve bolus control and to help prevent aspiration. A range of starches and gums has historically been used to thicken liquids. Although thickened liquids improve swallow safety, they appear to have a great potential for unintended physiological consequences. Initial concerns were raised about the impact of thickeners on water binding due to the high prevalence of dehydration amongst individuals with dysphagia. Thankfully, regardless of thickening agent, thickeners do not affect water bioavailability. This effect holds true even for extremely thick fluids. However, bioavailability of medication is impaired with viscous substances. Liquids thickened to as little as 150 mPa.s retards drug release. In addition, feelings of satiety and thirst increase with increasingly viscous fluids. Flavour deteriorates with increasing thickness regardless of thickening agent. Therapeutically clinicians often prescribe small volumes of thickened liquids, consumed often. Yet small volumes of thick substances consumed with a long oral processing time, which is common for individuals with dysphagia, reduces the amount consumed. A combination of poor flavour, and increasing feelings of fullness result in little motivation and poor physiologic drive to consume thickened liquids.This review provides evidence from the dysphagia, pharmaceutical and food technology literature to show unintended side effects of thickened liquids that contribute to dehydration and potential sub-theraputic medication levels for individuals with dysphagia. The physical property of viscosity rather than a particular thickening agent appears to be key. Provision of “spoon-thick” or “extremely thick liquids” is particularly likely to contribute to dehydration and poor bioavailability of solid dose medication. Clinicians are encouraged to prescribe the minimal level of thickness needed for swallowing safety. Consultation with pharmacy and dietetic staff is essential for optimum management of individuals with dysphagia. Given the aged population forecasts for the year 2050, improved dysphagia management should be a high priority.

Current Approaches and Pharmaceutical Applications of Colloidosome Drug Delivery Systems

Recently a number of lipid based systems like lipospheres, liposomes, niosomes, ethosomes, and transferosomes have been developed. The purpose of this review article on colloidosome drug delivery was to compile the focus on the types, properties, fabrication techniques, characterization and stability of colloidosomes. This system also solves the problem of insolubility, instability, rapid degradation and is widely used in specialized areas like protein delivery, gene delivery, targeting to the brain and tumor targeting. In a series of vascular systems, colloidosome represents an advanced tool in drug delivery. Colloidosomes are an emerging vesicular system in drug delivery. Vesicular drug delivery reduces the cost of therapy by improved bioavailability of medication, especially in the case of poorly soluble drugs. Colloidosomes have a great encapsulation efficacy with a wide control over size, permeability, mechanical strength and compatibility.

Unpredictable Absorption of Oral Opioid Medications in a Quadriplegic Patient With Chronic Enterocutaneous Fistulas

ABSTRACTAlthough there is an abundance of literature on the acute management of enterocutaneous fistulas, there is a paucity of data on the chronic management of enterocutaneous fistulas. Their impact on oral pharmacotherapy, including their effect on the bioavailability of oral medications, is poorly understood. This case describes a 23-year-old quadriplegic male with a complex history of multiple abdominal surgeries presented with three persistent enterocutaneous fistulas. Diazepam and furosemide were among the patient's oral medications and had sufficient bioavailability to show efficacy on anxiety and pedal edema, respectively. Conversely, oral oxycodone and methadone were ineffective in controlling chronic pain despite high doses and aggressive titration. Due to inadequate pain control, the patient supplemented opioid medications with high doses of lorazepam and diazepam to augment psychological comfort. A trial of subcutaneous morphine successfully produced immediate analgesia, causing a marked reduction in benzodiazepine use. Enterocutaneous fistulas may reduce the bioavailability of oral medications to various degrees depending upon the medication. Further research is needed to elucidate the effect chronic enterocutaneous fistulas have on the bioavailability of oral medications. It is therefore important for clinicians to question the bioavailability of medications in the setting of enterocutaneous fistulas and poor clinical response.

Identifying Clinically Questionable Psychotropic Prescribing Practices for Medicaid Recipients in New York State

This study sought to identify and characterize rates of clinically questionable prescribing in New York State. As part of a quality improvement initiative, 34 national psychopharmacology experts identified a set of questionable prescribing practices recognizable from pharmacy claims data. Indicators of such practices were applied to Medicaid claims data for 217,216 beneficiaries in New York State who had an active psychotropic prescription on April 1, 2008. A total of 156,103 (72%) of these beneficiaries had one or more continuing (>90 days) prescriptions for a psychotropic. About 10% of adults were prescribed four or more psychotropics concurrently, and 13% of children and 2% of older adults were prescribed three or more concurrently. Prescribing an antipsychotic with a moderate-to-high risk of causing metabolic abnormalities approached 50% (46%) among individuals who had existing cardiometabolic conditions. Among beneficiaries prescribed second-generation antipsychotics with a moderate-to-high risk of causing metabolic abnormalities, over half (60%) had not received a metabolic screening test in the past year. Among women of reproductive age prescribed mood stabilizers, over one-quarter (30%) were prescribed a valproic acid-based formulation despite its potential for teratogenicity. Only 2% of youths under age 18 were prescribed benzodiazepines; however, about half (48%) had trials over 90 days' duration. Examination of pharmacy claims from Medicaid beneficiaries in New York State indicated that prescribing practices deemed clinically questionable by pharmacology experts are common. Aggregated pharmacy claims data can identify such practices, and reviews of these data can be a core component of efforts to improve prescribing practices.

Identifying Clinically Questionable Psychotropic Prescribing Practices for Medicaid Recipients in New York State

Identifying Clinically Questionable Psychotropic Prescribing Practices for Medicaid Recipients in New York State