Development Of Controlled Release Formulations Research Articles

Bilayer Tablets: A Promising Novel Drug Delivery System

The bilayer tablet heralds a new chapter in the development of controlled-release formulations with a wide range of properties that result in an effective drug delivery technique. Controlled release dosage forms have been commonly used to increase the treatment of a variety of important drugs. Uses of bilayer tablets for anti-inflammatory and analgesic purposes are a unique feature. Bilayer tablets are useful for releasing two medications in sequence, separating two incompatible chemicals, and creating a sustained-release tablet with the first layer of immediate-release as the initial dose and the second layer as the maintenance dose. The bilayer tablet is a more modern technology that corrects the flaws of single-layer tablets. The objective of this paper is to highlight the obstacles that arise during the preparation of bilayer tablets, as well as to suggest solutions to these issues. To better comprehend bilayer tablets, kinds such as single side press, double side press, and bilayer tablet displacement press are discussed, as well as uses, pros, and disadvantages. Its drug companies have become more interested in mixing two or more APIs (active pharmaceutical ingredients) in a single dosage form to improve patient convenience and compliance throughout the last decade. Many pharmaceutical industries are now working on bi-layer tablets for a variety of purposes, including patent extension, therapeutics, and advertising. This article provides an introduction of bilayer tablet technology, highlighting the key benefits of this type of oral dosage form while also describing current issues and developments in production techniques and the quality of products. The current report covers a variety of elements of bilayer tablets.

Advances in Controlled-Release Pesticide Formulations with Improved Efficacy and Targetability.

Pesticides are commonly used in modern agriculture and are important for global food security. However, postapplication losses due to degradation, photolysis, evaporation, leaching, surface runoff, and other processes may substantially reduce their efficacy. Controlled-release formulations can achieve the permeation-regulated transfer of an active ingredient from a reservoir to a target surface. Thus, they can maintain an active ingredient at a predetermined concentration for a specified period. This can reduce degradation and dissipation and other losses and has the potential to improve efficacy. Recent developments in controlled-release technology have adapted the concepts of intelligence and precision from the pharmaceutical industry. In this review, we present recent advances in the development of controlled-release formulations and discuss details of the preparation methods, material improvements, and application technologies.

Evaluation of Pharmaceutical Compatibility between Acarbose and Common Excipients Used in the Development of Controlled Release Formulations

Background: Excipients are used in the formulation of pharmaceutical dosage forms, but mayinteract with active pharmaceutical ingredients (APIs). Some of these interactions could alterthe physicochemical properties of the APIs which can affect the therapeutic efficacy and safety.Acarbose is an anti-diabetic drug used in this study as an API to investigate its compatibility withcommon excipients in order to development of pharmaceutical controlled release formulations. Methods: For this purpose, 15 different excipients were selected. Binary mixtures of drug witheach of the excipients (1:1 mass ratio) were prepared. Mixtures were analyzed immediately aftermixing and also after incubation at stress conditions (adding 20% water and incubated at 40°Cfor 2 months). The thermal analytical investigation like differential scanning calorimetry (DSC),Fourier transform infra-red spectroscopy (FTIR) and high-performance liquid chromatography(HPLC) were employed for physicochemical evaluations of the possible incompatibility.Photodiode-array (PDA) and mass studies were performed to ensure the peak purity of theHPLC peaks of API in stressed samples. Results: Incompatible excipients with acarbose were determined as EC (ethyl cellulose),Carbopol 934, Hydroxypropyl cellulose, PEG2000 (Polyethylene Glycol 2000), Mg Stearate, NaAlginate and Poloxamer. Conclusion: Results of this study would be used for the development of controlled releaseformulation of acarbose. It is recommended to avoid the use of incompatible excipients.

Evaluation and Use of Opioid Analgesics in Pediatric Cancer Pain

Morphine is the preferred opioid analgesic in pediatric cancer pain due to extensive clinical experience with it, significant pharmacokinetic and pharmacodynamic data following oral and parenteral administration, global availability, and the development of controlled-release formulations. Randomized clinical trials are needed to fully evaluate the pharmacokinetics, dose equivalence, clinical efficacy, and safety of other opioid analgesics in cancer pain. Clinical trials are also needed to evaluate the efficacy and safety of adjuvant analgesics in children, including tricyclic antidepressants, anticonvulsants, and antiarrhythmics for neuropathic pain and corticosteroids and diphosphonates for bone pain. Unfortunately, the number of children with cancer pain and stable analgesic requirements is usually not large enough to support well-controlled clinical trials at a single institution. Consequently, multicentre and perhaps multinational efforts are necessary to fully evaluate opioid pharmacokinetics, pharmacodynamics, and dosage guidelines in children with cancer.

Pharmacokinetic characterization of controlled-release formulations

The development of controlled-release formulations should be based on a clinico-pharmacological rationale such as increased compliance, reduced side effects and improved efficacy. The pharmacokinetic profile of a controlled-release formulation and its dose regimen should be compared under steady-state conditions with that of an immediate-release formulation or that of another controlled-release formulation. Apart from conventional characteristics such as AUC, tmax and Cmax, alternative characteristics are suggested such as residual concentration at the end of the dose interval, peak-through fluctuation in steady state, plateau time, statistical moments, in vivo input functions and intravenous infusion schemes which mimic the concentration/time profile after oral administration of the controlled-release formulation. The pharmacokinetic steady-state profile should be reproduced with and without food, from day to day, and at various dose levels. The in vitro specification should be based on in vivo requirements for "within-product bioequivalence".