Sustained-release Tablets Research Articles

Formulation, Development and Investigation of Matrix Type Sustained Release Tablet of Antiulcer Drug by Using Soluble Polymer as a Drug Release Retarding Agent

The main goals of sustained release drug delivery are to modify the medication's biopharmaceutical, pharmacokinetic, and pharmacodynamic properties in order to lessen adverse effects, increase patient compliance, and treat the illness. The current work set out to create sustained release tablets of nizatidine (220 mg) using a wet granulation process and different concentrations of polymers such as chitosan, Kollidon SR, and HPMC K100M. Pre-formulation characteristics were examined, including medication DSC analysis and FTIR research. We assessed a number of post-compression characteristics, including content homogeneity, thickness, hardness, friability, and weight uniformity. This study demonstrated how the post-compression characteristics of the drug formulation are influenced by the concentration of polymers.

Effects of Citric Acid and Sodium Alginate on the Stability and Dissolution of Clarithromycin Extended-Release Tablet

The pharmacokinetics of clarithromycin (CLR) conventional tablets (T1/2: 5-7 h) demand 2 or 3 doses per day, which is inconvenient for patients. Therefore, a sustained-release CLR tablet is necessary. Based on Klacid MR tablets (AbbVie) composed of citric acid and sodium alginate (Na-ALG), we developed a 24-hour extended-release CLR tablet. Although citric acid had a significant effect on the CLR release profile, the incompatibility of citric acid and CLR was reported (via FT-IR and stability study). Based on the function of Na-ALG in controlling the release and reducing the incompatibility of citric acid and CLR, a process (CLR and citric acid were granulated separately) was proposed. The final tablet formulation showed 1-month stability and dissolution similarity to standard tablets in pH 6.8 medium (f2 > 50).

Enteral Nutrition Intervention Enhances Analgesic Effect of Morphine Hydrochloride Sustained Release Tablets in Alleviating Cancer Pain

We have explored the effects of enteral nutrition interventions on the analgesic effect of morphine hydrochloride sustained-release tablets in cancer pain therapy. Patients in the control group were monitored in real time, and analgesics were given as needed to improve the pain. Patients in the treatment group received both morphine hydrochloride sustained-release tablets and enteral nutrition interventions. After treatment, the Visual Analogue Scale score, unified Parkinson’s disease rating scale, and Pittsburgh sleep quality index scores in the treatment group were reduced relative to the control group, and Parkinson’s disease sleep scale scores and nutritional indexes were elevated. Levels of interferon-γ and interleukin-2 in the treatment group were elevated relative to the control group, while the levels of interleukin-4 were reduced. The incidence of adverse reactions in the treatment group was 15.79% (21/133), which was lower relative to the control group (31.58%, 42/133). Levels of 5-hydroxytryptamine and brain-derived neurotrophic factor in the treatment group were elevated relative to the control group, while the levels of dopamine declined. To sum up, morphine hydrochloride sustained-release tablets combined with enteral nutrition interventions can decrease the inflammatory response of patients and promote sleep quality

Comparing the Performance of Raman and Near-Infrared Imaging in the Prediction of the In Vitro Dissolution Profile of Extended-Release Tablets Based on Artificial Neural Networks.

In this work, the performance of two fast chemical imaging techniques, Raman and near-infrared (NIR) imaging is compared by utilizing these methods to predict the rate of drug release from sustained-release tablets. Sustained release is provided by adding hydroxypropyl methylcellulose (HPMC), as its concentration and particle size determine the dissolution rate of the drug. The chemical images were processed using classical least squares; afterwards, a convolutional neural network was applied to extract information regarding the particle size of HPMC. The chemical images were reduced to an average HPMC concentration and a predicted particle size value; these were used as inputs in an artificial neural network with a single hidden layer to predict the dissolution profile of the tablets. Both NIR and Raman imaging yielded accurate predictions. As the instrumentation of NIR imaging allows faster measurements than Raman imaging, this technique is a better candidate for implementing a real-time technique. The introduction of chemical imaging in the routine quality control of pharmaceutical products would profoundly change quality assurance in the pharmaceutical industry.

Formulation and Evaluation of Cola acuminata Gum-based Mucoadhesive Sustained-release Matrix Tablets of Diclofenac Sodium.

This study aimed to evaluate Cola acuminata gum (CAG) for the formulation of mucoadhesive sustained-release matrix tablets of diclofenac sodium. Different batches of granules containing CAG and 100 mg of DS in ratios 0.5:1, 1:1, 2:1, and 3:1 were prepared, compressed into tablets, and evaluated for mucoadhesive strength, swelling index, and drug release in SGF (pH 1.2) and SIF (pH 7.4). Swelling indices and mucoadhesive strengths of the tablets were pH-dependent. Swelling indices of 56 ± 2.03 to 121 ± 2.19% and mucoadhesive strengths of 7.25 ± 1.45 to 15.43 ± 2.71 g/cm2 obtained at pH 7.4 were significantly higher (p<0.05) than swelling indices of 25 ± 2.43 to 47 ± 3.15% and mucoadhesive strengths of 5.52 ± 0.76 to 9.22 ± 1.95 g/cm2 obtained at pH 1.2. The percentage release of DS from the matrix tablets at pH 1.2 after 2 h (T2h) was insignificant. However, the percentage of drug release at pH 7.4 was significant for all the batches and dependent on the CAG concentration. The drug release was in the order of batches containing 3 g (80.44 ± 7.75) < 2 g (86.35 ± 5.65) < 1 g (90.08 ± 6.14) < 0.5 g (99.70 ± 3.90). The time for maximum drug release was 7 h (T7h) for CAG containing 0.5 g and 10 h (T10h) for other batches. This study showed that CAG could be useful for mucoadhesive sustained drug delivery.

Application of a novel Revolver apparatus for a biorelevant dissolution test of ropinirole sustained release tablets

Application of a novel Revolver apparatus for a biorelevant dissolution test of ropinirole sustained release tablets

FORMULATION, DEVELOPMENT AND EVALUATION OF SUSTAINED RELEASE TABLET OF ACECLOFENAC

In this study, sustained-release (SR) tablets of Aceclofenac were developed using acrypol 971Pas polymers. The tablets were prepared by mixing the active drug (Aceclofenac) with the polymer and other excipients, and then compressing the mixture into tablets using a tablet press.The release profile of the SR tablets was optimized by adjusting the ratios of the polymers and other excipients. The optimized formulation showed sustained release of the drug up to 16 hours, and the release kinetics followed first-order models. The tablets were stored under various conditions (e.g., at different temperatures and humidity levels) for a set period of time. The results showed that there were no significant changes in the drug content, physiochemical parameters. This suggests that the optimized SR tablets of Aceclofenac are stable and may be suitable for use as a sustained-release formulation of the drug.

Effect of compression process parameters on the physical properties and in vitro release mechanism of the press-coated nifedipine matrix sustained-release tablets

We aim to clarify the influence of compression process parameters on the physical properties and release kinetics of the dual-reservoir press-coated tablets (PCTs). The critical compression force from plastic deformation to elastic deformation was 12.15 and 20.08 kN for core tablets and coat layer powder, respectively. Below 12.15 kN, the core tablets underwent flattening, further compression and surface area changing during the compression process of the coat layer, which in turn made the coat layer further compressed in both axial and radial space, resulting in reduced porosity and increased tensile strength. The release testing revealed that PCTs exhibited a dual-reservoir sequence release mechanism of super case II transport in the coat layer and irregular transport in the core tablets, with compression force of the core tablets as a crucial process parameter. In brief, release profiles could be designed by adjusting drug distribution in dual-reservoir and process parameter of PCTs.

Design and evaluation of gastro-swelling/gastro-floating sustained-release tablets of brivaracetam for epilepsy therapy

To prolong the absorption of the drug and achieve the effect of gastric retention, new brivaracetam tablets together with the characteristics of rapid swelling and sustained floating have been developed here. The tablets were optimized and prepared by direct compression techniques using Kollidon® SR and cross-linked polyvinylpyrrolidone (PVPP) XL as the matrix and disintegrant respectively, and carbomer 71G NF and polyethylene oxide (PEO) N60K as the gel materials to achieve sustained release effect. The characteristics of static expansion, floating time, drug release and dynamic swelling performance in vitro of the tablets were evaluated. The optimized formulations (F5 and F10) exhibited satisfactory swelling and floating properties, mechanical strength, and in vitro sustained-release characteristic with diffusion and matrix erosion mechanisms. X-ray images of beagle dogs showed that the tablet F5 could be retained in the stomach for more than 6 h. Furthermore, the pharmacokinetic studies in volunteers exhibited that the bioavailability of F5 and F10 was 95.70% (90% CI, 83.80%-109.28%) and 103.39% (90% CI, 87.61%-122.01%), respectively, relative to commercial tablets, with Tmax prolonged, demonstrating an excellent sustained-release effect. Therefore, the present system can reduce dosing frequency and improve patient compliance, which is expected to be a promising treatment option for epilepsy patients.

Simultaneous Analysis of Indapamide and Related Impurities in Sustained-Release Tablets by a Single-Run HPLC-PDA Method

The contents of indapamide and related impurities in generic indapamide sustained-release tablets were simultaneously detected by a single-run high performance liquid chromatography equipped with photodiode array detector (HPLC-PDA) method for the quality control in this paper. The results showed the method had a good selectivity and was validated through linearity, limits of detection and quantification, recovery, and precision. The linear ranges of indapamide, 2-methyl-1-nitroso-2,3-dihydro-1H-indole (impurity A, ImA), 4-chloro-N-(2-methyl-1H-indol-1-yl)-3-sulphamoyl-benzamide (impurity B, ImB) and 4-chloro-3-sulfamoylbenzoic acid (impurity 1, Im1) were 0.028-1.80 μg/mL (R=0.999 95), 0.060-1.20 μg/mL (R=0.999 6), 0.032 4-1.20 μg/mL (R=0.999 85) and 0.060-1.20 μg/mL (R=0.999 7) with detection limits of 0.009 3, 0.012, 0.012 and 0.006 μg/mL, respectively. ImA and Im1 were not detectable in the generic drug. The content of indapamide was 96.7% of the labeled amount with a relative standard deviation (RSD) of 1.30%, and the percentage of ImB relative to the labeled amounts of indapamide was 0.106% with an RSD of 1.82%. The content of other unspecified impurities all met the reference quality standards. The results provided references for the quality control and the quality standard study of generic indapamide sustained-release tablets.

Integration of artificial neural network and physiologically based biopharmaceutic models in the development of sustained-release formulations.

Model-informed drug development is an important area recognized by regulatory authorities and is gaining increasing interest from the generic drug industry. Physiologically based biopharmaceutics modeling (PBBM) is a valuable tool to support drug development and bioequivalence assessments. This study aimed to utilize an artificial neural network (ANN) with a multilayer perceptron (MLP) model to develop a sustained-release matrix tablet of metformin HCl 500mg, and to test the likelihood of the prototype formulation being bioequivalent to Glucophage® XR, using PBBM modeling and virtual bioequivalence (vBE). The ANN with MLP model was used to simultaneously optimize 735 formulations to determine the optimal formulation for Glucophage® XR release. The optimized formulation was evaluated and compared to Glucophage® XR using PBBM modeling and vBE. The optimized formulation consisted of 228mg of hydroxypropyl methylcellulose (HPMC) and 151mg of PVP, and exhibited an observed release rate of 42% at 1h, 47% at 2h, 55% at 4h, and 58% at 8h. The PBBM modeling was effective in assessing the bioequivalence of two formulations of metformin, and the vBE evaluation demonstrated the utility and relevance of translational modeling for bioequivalence assessments. The study demonstrated the effectiveness of using PBBM modeling and model-informed drug development methodologies, such as ANN and MLP, to optimize drug formulations and evaluate bioequivalence. These tools can be utilized by the generic drug industry to support drug development and biopharmaceutics assessments.

Preparation and Evaluation of Polymer Fused Metformin Hydrochloride Sustained Release Tablet

Preparation and Evaluation of Polymer Fused Metformin Hydrochloride Sustained Release Tablet

Impact of Raman mapping area and intra-tablet homogeneity on the accuracy of sustained-release tablet dissolution prediction

This exploratory study investigated the minimum required Raman mapping area for predicting sustained-release tablet dissolution profiles based on intra-tablet homogeneity. The aim was to minimize scanning time while achieving reliable dissolution profile predictions. To construct the sample set, we controlled the blending time to introduce variability in the homogeneity of the tablets. The dissolution prediction models were established using the partial least squares regression under different Raman mapping area. The accuracies of the prediction results were evaluated according to the difference factor f1 and Intersection–Union two one-sided t-tests (IU TOST) methods, and the implications conveyed by the results were discussed. The results showed that the homogeneity of sustained-release tablet affects the minimum required mapping area, and the tablets with higher homogeneity show higher prediction accuracy when using the same mapping area to model the dissolution profiles of tablets.

Effect of Glipizide on non-insulin-dependent diabetes mellitus

Type 2 diabetes mellitus, sometimes referred to as non-insulin-dependent diabetes, (NIDDM). The patient was unable to secrete enough insulin, resulting in elevated blood glucose. Complications during a patient's diseases are common in type 2 diabetes patients. Common type 2 diabetes does not have an age or gender difference. Patients with type 2 diabetes or those under treatment are frequently fat and sedentary. Glipizide, a sulfonylurea medication, is prescribed to people with non-insulin-dependent diabetic mellitus. (type 2 diabetes). There are two common types, oral tablets and sustained-release tablets. The common type of oral tablets is fast-acting tablets. Absorption is rapid and the effect is rapid, because oral tablets have a significant effect and may cause short-term hypoglycemia. The body disintegrates the medication and release it. A contributing factor to type 2 diabetes is having high blood glucose levels, as the pancreas produces less insulin, resulting in a residual overall glucose in the blood. These disorders are often caused by genetics or overweight/physical inactivity . The blood glucose levels of patients with type 2 diabetes are greater than those of ordinary healthy individuals since the condition is a chronic metabolic disorder. Glipizide can be used as an insulin secretagogue to stimulate islet β cells to release insulin, thereby increasing plasma insulin concentration. It also serves as an auxiliary hand in diet and exercise. Different regions have different laws for the use of glipizide. Glipizide can be used in combination with other NIDDM drugs in the United States. It can only be used alone or not in the United Kingdom because of the high risk of aggravating hypoglycemia in patients. Patients who have any cardiovascular or renal disease or have a long history do not mind using these drugs. Such agents are likely to worsen the hypoglycemia associated with the disease. Among many drugs, glipizide is one of the most common sulfonylureas and has a moderate price.

Construction and properties of venlafaxine hydrochloride sustained release system based on hollow mesoporous silica microspheres

The aim of this work is to develop a venlafaxine hydrochloride sustained release system based on hollow mesoporous silica microspheres (HMSMs). HMSMs were innovatively prepared with tetraethyl silicate (TEOS) as the precursor and volatile n-heptane as a soft template. The obtained HMSMs show a well-defined hollow structure with an average size of 967 nm and pore volume of 0.85 cm3/g, implying it is a potential drug carrier. Subsequently, venlafaxine hydrochloride (VF) was absorbed in the HMSMs with a content of 37.67% or so. The sustained release effect is further measured by the dissolution instrument at 37 °C and 50 rpm in ultrapure water. The results showed that the HMSMs/VF system shows good sustained release properties compared with sustained release tablets with hydroxypropyl methylcellulose as the main component. This HMSMs sustained release system appears to be a promising candidate for a sustained drug release.

Network Meta-analysis of Chinese patent medicines in treatment of idiopathic membranous nephropathy

This study aimed to systematically evaluate the efficacy and safety of different Chinese patent medicines in the treatment of idiopathic membranous nephropathy. The relevant randomized controlled trial(RCT) was retrieved from PubMed, EMbase, Cochrane Library, CNKI, SinoMed, Wanfang, and VIP with the time interval from database inception to December 2022. The Cochrane risk of bias assessment tool was employed to evaluate the quality of the included RCT, and Stata 15.0 and GEMTC to perform the Bayesian network Meta-analysis. Finally, 51 RCTs were included, involving 9 Chinese patent medicines and 3 591 patients. The results of network Meta-analysis showed that in terms of the total effective rate and the increase in plasma albumin, the top three interventions were Zhengqing Fengtongning Sustained Release Tablets + conventional western medicine, Bailing Capsules + conventional western medicine, and Tripterygium Glycosides Tablets + conventional western medicine. In terms of reducing 24-hour urine total protein, the top three interventions were Zhengqing Fengtongning Sustained Release Tablets + conventional western medicine, Shenfukang Capsules +conventional western medicine, and Huangkui Capsules + conventional western medicine. In terms of reducing serum creatinine, the top three interventions were Shenfukang Capsules + conventional western medicine, Bailing Capsules + conventional western medicine, and Zhengqing Fengtongning Sustained Release Tablets + conventional western medicine. In terms of safety, Chinese patent medicines combined with conventional western medicine had fewer adverse reactions than the control group. The results suggest that Chinese patent medicines combined with conventional western medicine can improve the therapeutic effect on idiopathic membranous nephropathy, and differentiated medications can be adopted according to the specific symptoms of patients in clinical treatment. Further validation needs to be carried out in the future with multi-center, large-sample, and high-quality RCT.

Bilayer Tablet a Dual Released, an Emerging Trend for Novel Drug Delivery System

Bilayer tablets are a kind of medication that effectively treats illness by combining two pharmaceuticals, either the same or different ones, in a single dosage. Physically separating active pharmaceutical ingredients (API) may prevent chemical incompatibilities, and bilayer tablets can pave the way for the creation of various drug release profiles, such as immediate and prolonged release. Analgesic and anti-inflammatory bilayer tablets are significantly different. Two medications may be sequentially released from a bi-layer tablet, making it ideal for sustained-release tablets. One layer can be immediate-release for the first dosage, while the other can be a maintenance dose. The purpose of this review is to identify problems with bilayer tablet preparation and to suggest ways to fix them. To further aid comprehension, the article goes on to list the many kinds of bilayer tablets, including single-side presses, double-side presses, and bilayer tablet displacement presses, as well as their uses, advantages, and disadvantages. In addition, the review paper discusses the several ways and procedures used to manufacture bilayer tablets, so readers may have a comprehensive understanding of these tablets. In the last paragraph, the whole essay is evaluated critically.

Formulation Studies and Application of Their Experimental Techniques to Drug Discoveries

In my first experience as a researcher, I isolated and performed structural predictions of the novel compounds, cis- and trans-palythenic acids, from Noctiluca milialis. I then worked for a pharmaceutical company in a research laboratory of pharmaceutics. I examined an inclusion complex of cinnarizine with β-cyclodextrin, and found that the inclusion complex did not improve the oral bioavailability of cinnarizine. However, the bioavailability of the inclusion complex after its oral administration was improved by a competing agent. This was the first study to show the potential of a competing agent to improve bioavailability. I subsequently joined a laboratory performing drug discovery research and used experimental techniques from pre-formulation studies. A screening system of solubility for drug design and discovery was constructed to increase the solubilities of compounds synthesized in the laboratory. This screening system contributed to the discovery of a phosphodiesterase type 5 inhibitor with sufficient solubility. As a visiting lecturer at a university, I prepared amoxicillin intragastric buoyant sustained-release tablets for the eradication of Helicobacter pylori and applied cinnarizine as a competing agent. I established a laboratory of pharmaceutics at a university in Tochigi. To develop an enema with fluticasone propionate for ulcerative colitis, I investigated its physicochemical properties and methods to improve its solubility. After moving to another university in Kagawa, I developed a method to reduce the amount of drugs remaining on the surfaces of a pestle and mortar following the grinding of tablets, and new cleaning agents for an automatic dividing packaging machine were discovered.

An Overview Onsustained Release Formulations Using Solid Dispersion as Solubility Enhancement Technique.

Biopharmaceutical classification system is important for determining the bioavailability of the drug. Drugs that dissolve slowly in water can be effectively solid-dispersed to increase their bioavailability. The bioavailability issue can be due to insufficient solubility of permeability. The poorly water-soluble medication dissolves more quickly when combined with the water-soluble carriers used to make solid dispersion. The review paper concentrates on the preparation techniques, benefits, drawbacks, and characterization of solid dispersion. Pharmaceuticals with sustained release have recently emerged as a very practical tool in medical practise, providing patients with a variety of real and perceived benefits. By minimising fluctuations in Using the therapeutic dose of the medicine in the body, sustained release is another promising reduction technique side effects. The major methods for creating tablets with a sustained release matrix are wet granulation, direct compression, or dispersion. In this review paper got the information about various polymers and different methods which are used for the formulate the sustained release tablet.&#x0D;

Adjustment of Analgesic in a Patient with Pain and Renal Dysfunction

Opioid drugs are widely used in the treatment of cancer pain. Renal dysfunction slows down the clearance of opioids, which can easily lead to drug accumulation and overdose, posing a challenge to safe medication. This article takes a patient with cancerous abdominal pain and chronic low back pain combined with severe renal function damage as an example. This patient experienced central inhibitory, such as somnolence, hypoxemia, and needle like pupil contraction during the use of oxycodone sustained-release tablets for pain treatment. Clinical pharmacist conducted a comprehensive pain assessment of patient and adjusted oxycodone sustained-release tablets to tramadol capsules. The physician followed the pharmacist's advice and the patient's pain was satisfactorily controlled without obvious adverse effects. This article discusses the pharmacological and pharmacokinetic characteristics of commonly used opioid drugs in clinical practice, as well as their application in patients with renal function impairment. This article also provides an in-depth analysis of the application of oxycodone and tramadol in patients with cancer pain, chronic low back pain, and renal function damage, based on case studies. This case suggests that for patients with severe renal dysfunction and opioid intolerance, it is not only necessary to choose drugs that are less reliance on renal clearance and short acting formulations, but also to gradually titrate from a small dose to an appropriate dose; For pain patients with complex clinical conditions, physicians should focus on collaborating with pharmacists to develop personalized and refined medication plans for patients, in order to achieve satisfactory pain control and ensure patient medication safety.