Oral Controlled Release Research Articles

FORMULATION AND EVALUATION OF LOSARTAN POTASSIUM MATRIX TABLETS BY USING DIFFERENT POLYMERS

The study aims to create a sustained release matrix tablet for Losartan potassium, an angiotensin II receptor antagonist, to improve patient compliance and maintain therapeutic blood or tissue levels for extended periods. The research investigates the role of novel semi-synthetic polymers and natural polymers in comparison to well-known release retarding agents. Gastroretentive drug delivery systems (GRDDS) are unique technologies designed to improve drug bioavailability and absorption by avoiding the first-pass effect. Losartan potassium, an angiotensin II receptor antagonist, has a bioavailability of 32% and a low elimination half-life, making it suitable for oral controlled release. The study utilized natural and synthetic polymers in matrix tablet preparation, concentration, drug particles size, additives, and excipients to modify drug release. The powder mixtures were tested for pre-compression parameters and post-compression parameters, and in-vitro dissolution studies showed good dissolution profiles for drug release. Formulations with higher concentrations and polymers sustained drug release for 24 hours. FT-IR Spectroscopy confirmed drug compatibility with polymers and other excipients KEYWORDS: matrix tablets, Losartan Potassium, flow properties, pre compression parameters post compression parameters, In-vitro dissolution.

An emerging terpolymeric nanoparticle pore former as an internal recrystallization inhibitor of celecoxib in controlled release amorphous solid dispersion beads: Experimental studies and molecular dynamics analysis

Solid oral controlled release formulations feature numerous clinical advantages for drug candidates with adequate solubility and dissolution rate. However, most new chemical entities exhibit poor water solubility, and hence are exempt from such benefits. Although combining drug amorphization with controlled release formulation is promising to elevate drug solubility, like other supersaturating systems, the problem of drug recrystallization has yet to be resolved, particularly within the dosage form. Here, we explored the potential of an emerging, non-leachable terpolymer nanoparticle (TPN) pore former as an internal recrystallization inhibitor within controlled release amorphous solid dispersion (CRASD) beads comprising a poorly soluble drug (celecoxib) reservoir and insoluble polymer (ethylcellulose) membrane. Compared to conventional pore former, polyvinylpyrrolidone (PVP), TPN-containing membranes exhibited superior structural integrity, less crystal formation at the CRASD bead surface, and greater extent of celecoxib release. All-atom molecular dynamics analyses revealed that in the presence of TPN, intra-molecular bonding, crystal formation tendency, diffusion coefficient, and molecular flexibility of celecoxib were reduced, while intermolecular H-bonding was increased as compared to PVP. This work suggests that selection of a pore former that promotes prolonged molecular separation within a nanoporous controlled release membrane structure may serve as an effective strategy to enhance amorphicity preservation inside CRASD.

Agarose as a tunable platform for oral drug delivery: Controlled release of a highly soluble drug, theophylline, within a sequentially-changing-pH medium

The purpose of this study was to expand the use of freeze-dried agarose-based systems for the oral controlled release of highly water-soluble drugs. Three additives (Eudragit S-100 and RL-PO and Labrafac) were included within these systems together with Theophylline. The release of this drug from the rehydrated systems was evaluated in deionized water and in a sequentially-changing-pH medium that simulated the conditions under oral administration. Considering the results obtained in the preliminary release test in water, only the Eudragit-containing compositions were further characterized. The theophylline release in a sequentially-changing-pH medium showed two different patterns that mainly depend on the additive nature: those systems containing Eudragit S-100 showed a similar behaviour to that observed in the absence of additives while the presence of Eudragit RL-PO yields a progressive and pH-independent release. Agarose-based systems were capable of accommodating additives that allows tailoring a controlled release of theophylline, a highly soluble drug.

Multifunctional Pomegranate Peel Microparticles with Health-Promoting Effects for the Sustainable Development of Novel Nutraceuticals and Pharmaceuticals.

Recovering the bioactive components from pomegranate peel (PP) in the fruit-processing industry has attracted great attention in terms of minimizing the waste burden, as well as providing a new source of a multitude of functional compounds. The present study aimed to develop a feasible microencapsulation process of PP extract by using pectin and a pectin/2-hydroxypropyl-β-cyclodextrin (HP-β-CD) blend as coating materials. Microsized powders obtained by a spray drying technique were examined in terms of technological characteristics, exhibiting high powder yield and desirable moisture content, flowability, and cohesive properties. Assuming that the interactions with the used biopolymers occur on the surface hydrophobic domain, their presence significantly improved the thermal stability of the microencapsulated powders up to 200 °C. The health-promoting effects of PP have been associated with its high content in ellagitannins, particularly punicalagin. The obtained PP powders exhibited strong antioxidant and hypoglycemic potential, while an antimicrobial assay revealed their potent activity against Gram-positive bacteria. Additionally, an in vitro release study suggested that the used biopolymers can modify the release of target bioactive compounds, thus establishing a basis for developing an oral-controlled release system. Altogether, biowaste valorization from PP by the production of effective multifunctional microsized powders represents a sustainable way to obtain novel nutraceuticals and/or pharmaceuticals.

A brief review on basic fundamentals of nanoparticle (NPs)

According to studies made by previous researchers there are various technical problems associated with liposomes which can be avoided by designing colloidal drugs carrier like nanoparticles with nanotechnology. Now a days they are beneficial in the field of agriculture, veterinary, pharmaceutical, textile technologies. Site specific delivery of encapsulated drugs can be formulated with a nanometer size range which can be injected into the general circulation. The objective of this review is to explain the potential of NPs and nanotechnology associated with their characters and classifications, synthesis and application as the emerging scopes for NPs, rather will attract everyone’s attention. The aim of the present work is to characterize biodegradable nanoparticulate systems for oral controlled release, while numerous publications have appeared on this by international research teams, the research on polymeric nanoparticles has been primarily performed by a few research groups in Europe. Nanoparticles are being investigated as an alternative colloidal drug delivery system that could potentially avoid some of the technical problems observed with other drug delivery system.

Formulation of chitosan based lipid polymer hybrid nanocarrier system for oral delivery of tamoxifen citrate: Toxicological and hemocompatibility evaluation

The objective of the current work was to develop chitosan based lipid nanocarriers for the oral controlled release of tamoxifen citrate (TC). The ionic gelation method was used to develop various formulations with altered ratios of polymer, lipid, and emulsifier. The developed lipid hybrid nanoparticles (LHNPs) were characterized for particle size, polydispersity index, zeta potential, entrapment efficiency, SEM, DSC, FTIR, PXRD, in vitro release studies, stability studies, kinetic modeling, toxicity studies, and hemocompatibility assay. Particle size and entrapment efficiency of the developed formulations varied between 138.2 ± 4.2 nm to 281.8 ± 63.1 nm and 70.94 ± 0.29 % to 82.23 ± 0.02 %, respectively. The polydispersity index and zeta potential ranged from 0.199 ± 0.03 to 0.555 ± 0.01 and 17.9 ± 0.62 to 32.3 ± 0.36, respectively. Nano-sized, spherical in shape surfaces of developed particles were depicted by SEM. While removal of TC melting endotherm revealed by DSC analysis, suggested good thermal stability of LHNPs. FTIR verified that the components of the formulation do not interact chemically. PXRD depicted that the developed formulation has been successfully amorphized. In vitro release study revealed drug release, an initial burst drug release followed by the controlled release up to 72 h. Kinetic modeling exposed that all developed formulations showed a non-Fickian diffusion profile and were best fitted into Higuchi's square root and Korsmeyer-Peppas models. Toxicity investigations on female albino rabbits provided evidence for the compatibility and non-toxicity of developed particles with biological systems. Hemocompatibility assay showed that the developed system is compatible with blood and nontoxic. These investigations demonstrate the potential of developed LHNPs as a vehicle, aimed at controlled oral delivery of TC for better therapeutic applications in breast cancer.

Cydonia oblonga-Seed-Mucilage-Based pH-Sensitive Graft Copolymer for Controlled Drug Delivery-In Vitro and In Vivo Evaluation.

The primary objective of this study was to assess the potential utility of quince seed mucilage as an excipient within a graft copolymer for the development of an oral-controlled drug delivery system. The Cydonia oblonga-mucilage-based graft copolymer was synthesized via a free radical polymerization method, employing potassium per sulfate (KPS) as the initiator and N, N-methylene bisacrylamide (MBA) as the crosslinker. Various concentrations of monomers, namely acrylic acid (AA) and methacrylic acid (MAA), were used in the graft copolymerization process. Metoprolol tartarate was then incorporated into this graft copolymer matrix, and the resultant drug delivery system was subjected to comprehensive characterization using techniques such as Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The swelling behavior of the drug delivery system was evaluated under different pH conditions, and in vitro drug release studies were conducted. Furthermore, pharmacokinetic parameters including the area under the curve (AUC), maximum plasma concentration (Cmax), time to reach Cmax (Tmax), and half-life (t1/2) were determined for metoprolol-loaded hydrogel formulations in rabbit plasma, and these results were compared with those obtained from a commercially available product. The key findings from the study include observations that higher concentrations of acrylic acid (AA) and Cydonia oblonga mucilage (CM) in the graft copolymer enhanced swelling, while the opposite trend was noted at elevated concentrations of methacrylic acid (MAA) and N, N-methylene bisacrylamide (MBA). FTIR analysis confirmed the formation of the graft copolymer and established the compatibility between the drug and the polymer. SEM imaging revealed a porous structure in the prepared formulations. Additionally, the swelling behavior and drug release profiles indicated a pH-sensitive pattern. The pharmacokinetic assessment revealed sustained release patterns of metoprolol from the hydrogel network system. Notably, the drug-loaded formulation exhibited a higher Cmax (156.48 ng/mL) compared to the marketed metoprolol product (96 ng/mL), and the AUC of the hydrogel-loaded metoprolol was 2.3 times greater than that of the marketed formulation. In conclusion, this study underscores the potential of quince seed mucilage as an intelligent material for graft-copolymer-based oral-controlled release drug delivery systems.

Practical Application of 3D Printing for Pharmaceuticals in Hospitals and Pharmacies.

Three-dimensional (3D) printing is an unrivaled technique that uses computer-aided design and programming to create 3D products by stacking materials on a substrate. Today, 3D printing technology is used in the whole drug development process, from preclinical research to clinical trials to frontline medical treatment. From 2009 to 2020, the number of research articles on 3D printing in healthcare applications surged from around 10 to 2000. Three-dimensional printing technology has been applied to several kinds of drug delivery systems, such as oral controlled release systems, micropills, microchips, implants, microneedles, rapid dissolving tablets, and multiphase release dosage forms. Compared with conventional manufacturing methods of pharmaceutical products, 3D printing has many advantages, including high production rates due to the flexible operating systems and high drug loading with the desired precision and accuracy for potent drugs administered in small doses. The cost of production via 3D printing can be decreased by reducing material wastage, and the process can be adapted to multiple classes of pharmaceutically active ingredients, including those with poor solubility. Although several studies have addressed the benefits of 3D printing technology, hospitals and pharmacies have only implemented this process for a small number of practical applications. This article discusses recent 3D printing applications in hospitals and pharmacies for medicinal preparation. The article also covers the potential future applications of 3D printing in pharmaceuticals.

Physicochemical and Pharmacokinetic Studies of Metformin for Development of Controlled Release Matrix Tablet: Formulation Optimization Using in silico Tools

Metformin, taken by nearly 120 million people across the world as a treatment for type 2 diabetes, has a relatively short plasma half-life and low absolute bioavailability. In this study, physicochemical and pharmacokinetics properties of metformin have been thoroughly assayed using ADMETLab, SwissADME, SmartCYP, LigandScout web-servers and software to evaluate the effectiveness of its formulation as controlledrelease matrix tablets. The objective of the present work was to develop a formulation of an oral controlled-release (CR) metformin tablet, using hydrophilic hydroxylpropylmethylcellulose (HPMC) grades K4M and K100M polymers at different concentrations utilizing computational simulatory tools. Intestinal membrane permeability of the drug has been assayed using 2 hours simulation run with MembranePlus Software. Simulated environment generated for in silico dissolution study, using DDDPlus software, of the prepared formulations used USP Apparatus Type 2 rotating at 100 rpm. The simulation run was for 2 hours using 0.1N HCl phase followed by 8 hours with 6.8 USP Phosphate buffer phase. The results showed that drug release from the higher viscosity grade, K100M was slower as compared to the lower viscosity grade K4M at a fixed polymer concentration level. Furthermore, plasma concentration-time curves for the formulations have been generated using GastroPlus software. Dhaka Univ. J. Pharm. Sci. 22(1): 29-42, 2023 (June)

Recent Approaches of Matrix Release Tablet in NDDS System

The purpose of this analysis is to categorize matrix tablets according to the kind of polymer they are made of as well as the rate at which they release their contents. When it came to medicinal applications, the matrix system was the very first oral extended release platform ever developed. The utilization of matrix tablets enables the modification of drug release characteristics. They are highly favored for this kind of treatment because of the benefits they give for the patient in terms of better adherence to the treatment, more stable medication levels, decreased dose and bad effects, and a bigger safety margin for highly potent medications. Because of their versatility in delivering a desired drug release profile, cheap cost, and general regulatory acceptability, hydrophilic polymer matrix systems are frequently used in oral controlled drug delivery dosage forms. Because of the rapid diffusion of the dissolved medication via the hydrophilic gel network, the use of hydrophilic matrix alone for delayed drug release is not possible for medicines that are very water soluble. It is now generally accepted that the formulation of such drugs requires the use of matrix systems that incorporate hydrophobic polymers. It would appear that the most successful strategy would be to create a formulation for oral controlled release by employing matrix tablets.

The role of matrix tablet in controlled release drug delivery system

The purpose of this review article is to characterize all of the parameters regarding the types, polymers used, and release kinetics of matrix tablets. Matrix system was the earliest oral extended-release platform for medicinal use. Matrix tablets are most commonly used methods to modulate the release profile of drugs. They are much desirable and preferred for such therapy because they offer better patient compliance, maintain uniform drug levels, reduce dose and side effects, and increase safety margin for high potency drugs. Hydrophilic polymer matrix systems are widely used for designing oral controlled drug delivery dosage forms because of their flexibility to provide a desirable drug release profile, cost effectiveness, and broad regulatory acceptance. However, the use of hydrophilic matrix alone for extending drug release for highly water-soluble drugs is restricted due to rapid diffusion of the dissolved drug through the hydrophilic gel network. For such drugs it becomes essential to include hydrophobic polymers in the matrix system. This leads to the conclusion that matrix tablets seem to be most promising when developing an oral controlled release formulation.

Pluronic F-68 Montmorillonite As A Drug Delivery Vehicle For Extended Release Of Venlafaxine Hydrochloride.

Short half-life and low bioavailability of Venlafaxine hydrochloride (VF), an antidepressant drug, necessitates the frequent administration of VF tablets in a day in order to maintain adequate drug concentration in blood plasma. This generates the need for the development of formulations which could prolong the release of VF and reduce the multiple dosages. The present work explores the combination of Montmorillonite (Mt) with Pluronic F-68 (PF-68) (OrganoMT) for oral delivery of VF. The effect of various parameters including pH of aqueous drug solution, contact time and initial drug concentration on drug loading capacity of OrganoMT has been studied. The synthesized OrganoMT-VF complexes were characterized by various suitable techniques. XRD studies indicated that the VF molecules were intercalated within the OrganoMT layers. In vitro release behavior of VF from OrganoMT-VF complexes shows an extended-release pattern for a period of 30 h and reaches upto 70% and 60% compared to pure VF having complete release time of 5.5 h and 3.5 h in simulated gastric and intestinal fluid respectively. Various kinetic models were employed to elucidate the drug release mechanism where the best fitting was obtained with Korsmeyer Peppas model. The results suggest the possibility of designing an oral extended controlled release formulation for VF to minimize its administration frequency thereby increasing the effectiveness of drug. This improves patient compliance by reducing the dose from 4 times in 24 h to once in 24 h.

Understanding Degradation Pathway of Poorly Stable Diltiazem Hydrochloride and Development of its Stabilized Controlled-release Tablets

Diltiazem hydrochloride is a class -1 drug, as per the breast-conserving surgery (BCS) classification system, which is highly soluble and highly permeable. It is a poorly stable drug that poses many problems during formulation preparation. The stability of the final product is quite challenging. The API undergoes hydrolysis to form desacetyl-diltiazem. It is the major degradation impurity. Desacetyl-diltiazem exhibits only a quarter to half of the pharmacological activity as compared to diltiazem HCl. A correct understanding of the degradation pathway and usage of suitable excipients can provide a stable product with improved shelf life. During the course of various trials and application of factorial designing, an optimized composition for oral controlled release tablets of diltiazem HCl has arrived, suggesting that exposure to an aqueous medium for tablets granulation and eliminating the polyvinylpyrrolidone from the composition significantly improved the product stability and final tablets shelf life by not only maintaining the desired in-vitro drug release profile but also keeping the related substances (impurities level) at very low levels throughout the entire shelf life.

Microencapsulation: A Promising Technique for Controlling Drug Delivery

Microencapsulation is a well-established process of enveloping or surrounding one substance into another substance which gives capsules having range from less than one micron to several hundred microns in size. One of the highly efficiently method is micro encapsulation, micro particles or microspheres rely upon various factors like solubility of polymer in solvent, concentration of polymer, solubility of organic solvent in water, rate of solvent removal etc. Microparticulate drug delivery systems are an interesting and promising option when developing an oral controlled release system. The objective of this paper is to take a closer look at microparticles as drug delivery devices for increasing efficiency of drug delivery, improving the release profile and drug targeting. In order to appreciate the application possibilities of microcapsules in drug delivery, some fundamental aspects are briefly reviewed. The controlled release drug delivery system, releases the active drug or medicament at a predetermined rate targeting to specific site over a prolonged period of time.

A Review on Techniques and Applications of Gastroretentive Drug Delivery System

A Controlled release dose forms have been widely utilized to enhance treatment with a number of significant medications. However, a number of physiological challenges, including the inability to control and localize the system within the target region of the gastrointestinal tract and the extremely changeable nature of the gastric emptying process, pose challenges to the development processes. The bioavailability and periods needed to reach peak plasma levels may be unpredictable as a result of this diversity. The goal of this review on gastro retentive drug delivery systems was to gather the most recent research with a special emphasis on the numerous gastro retentive technologies that have lately emerged as leading approaches in the area of site-specific oral controlled release drug delivery. We have included crucial elements in order to comprehend numerous physiological challenges to achieve stomach retention.

Development and Evaluation of Etodolac Osmotic Capsule

controlled release formulations have been developed based on their significant advantages over conventional immediate release dosage forms, such as the decrease of dosing frequency, the increase of patient compliance, better dosing patterns, the reduction of side effects, or the maintenance of the drug concentration within a desired range, i.e., an overall improved therapeutic benefit. However, oral controlled release formulations are exposed to changing environment during transit through the GI-tract which may affect their performances e.g. physiological factors such as patient age or food-intake. Reported as releasing drug independently of these factors, oral osmotically-driven systems (OODS) have taken an integral place in the pharmaceutical field. The dissolution profile of orally delivered drugs can be controlled through the use of osmotically controlled drug delivery devices. The most commonly used device is the osmotic tablet/Capsule, which is essentially a tablet/Capsule core that is coated with a rate-limiting semipermiable membrane. Using osmotic pressure as driving force, various OCODDS design and compositions have been developed. Numerous products are launched based on these systems. In present investigation attempts are taken to formulate, optimize and develop an economic osmotically controlled Capsule containing drugs belonging to non steroidal anti-inflammatory category to release the drug in controlled manner. Such formulations are most beneficial for the patients shifted on long term pain management therapy(e.g. in arthritis) in view to reduce the associated side effects of these drugs.

ONE FACTOR RESPONSE SURFACE METHODOLOGY (RSM) FOR THE OPTIMIZATION OF ORAL VENLAFAXINE HCL CONTROLLED RELEASE ORGANOGEL

Objective: The aim of this study was to develop the oral Venlafaxine HCl controlled-release organogel (organogel–CR) by using one-factor response surface methodology (RSM). Methods: In this study, Drug-excipient compatibility was evaluated by FT-IR. A total of 14 experimental runs were carried out employing the detailed conditions designed by a single factor completely randomized design based on the response surface methodology was used to check the concentration effect of 12-Hydroxy stearic acid (12-HSA) at different cooling rates on drug release at 10 h (Q10) and after 12 h (Q12). Multiple linear regression analysis, analysis of variance (ANOVA) and graphical representation of the influence factor were performed by using design expert 12. The developed organogel was also evaluated for viscosity, strength, transition temperature, diffusivity and Scanning electron microscopy (SEM). Prepared organogel was filled in the capsule and investigated for weight variation, drug content, erosion of organogel and In vitro drug release study. Results: FT-IR results showed that there was no chemical interaction between the drug and excipients. The SEM photograph indicates that the developed organogel was highly viscous with 3D network structure. The experimental confirmation tests showed a correlation between the predicted and experimental responses (R2 = 0.9937 and 0.9709). The results of ANOVA suggested that calculated F values of all dependent variables are greater than tabulated values. The optimal point obtained was located in the valid region and the optimum in vitro release of the predicted batch containing 7.9% concentration of 12-HSA with gradual cooling rate. To validate the evolved mathematical models, a checkpoint was selected and its desirability value was found to be 0.866. Conclusion: Oral controlled release Venlafaxine HCl organogel fix the problem of repeated dosing and patient noncompliance.

Pharmaceutical characterization and pharmacokinetics of florfenicol-loaded alginate dried beads in rabbits

The pharmacokinetic variables of a new formulation of florfenicol included in dried bean of alginate (FADBs), its acceptance as in food medication, and its relationship with theoretical minimum inhibitory concentration (MIC) values of the main pathogens in rabbits, are presented. FADBs sought to mask the unpleasant taste of florfenicol while enhancing sustained absorption in a day to facilitate and optimise its dosage in this species. The entrapment efficiency was determined to be 94-98% and 73.56±3.26% of drug loading. No reduction in food consumption was detected, nor selectivity when choosing from their usual food. The elimination half-life was 1.23 to 2.4 h slower than the one previously reported in the literature. Possible flip-flop pharmacokinetics is proposed for FADBs in rabbits, thus complying better with the key pharmacokinetics/pharmacodynamics (PK/PD) ratio of t≥MIC. Also, if a MIC2.0 μg/mL is taken as the cut-off point for florfenicol in rabbits, then ad libitum intake of FADBs in their standard diet is sufficient to maintain plasma concentrations of florfenicol above this level during the whole dosing interval of 24 h. Additionally, FADBs are a low-cost and attractive drug delivery system for the oral controlled release of florfenicol in rabbits.

Development of Mucoadhesive Microsphere of Quinapril Hydrochloride for Treatment of Hypertension

Mucoadhesive drug delivery systems are very widely functional approach for delivery of system within the lumen of GIT to enhance drug absorption through the part of stomach with specific manner. Quinapril hydrochloride is the hydrochloride salt of quinapril, the ethyl ester of a non-sulfhydryl, angiotensin-converting enzyme (ACE) inhibitor, quinaprilat. The quinapril hydrochloride microspheres was prepared with a coat consisting of alginate polymer i.e. sodium alginate in combination of mucoadhesive polymer chitosan/ guargum by an ionic gelation process. The microspheres were evaluated for morphological character, particle size, micromeritic properties, percentage entrapment efficiency, in-vitro wash-off test and in-vitro release studies. The drug quinapril hydrochloride was study for the release over 24 h duration. The retarding nature of system maximizing the medication discharge rate at the appropriate site within specified time period for enhancing the bioavailability of drug at desired site of action to give successful treatment to the patients experiencing hypertension The drug release of the microspheres (QLMM1 – QLMM10) was slow, extended and dependent on the composition of galactomannan concentration of polymer and stirring speed during formulation used. The mucoadhesive microspheres were adhered at intestinal pH due to highly swelling nature of composition of polymers at this pH. So, increase the adhesive strength and retarded the drug release of best composition of CH:GG in the ratio of 1:3 (QLMM6). Guargum is a highly viscous material having a property of more swelling nature due to presence of galactommannan constituent. Thus, drug release from QLMM6 was slow and extended over a period of 24 h and these microcapsules were found suitable for oral controlled release formulations.
 Keywords: Gastro-retentive drug delivery, Mucoadhesive microsphere, Quinapril hydrochloride, Pulsatile drug delivery system, Treatment of hypertension, Natural polymers

Quantitative chemical profiling of cellulose acetate excipient via 13C NMR spectroscopy in controlled release formulations

Cellulose acetate (CA) is the main component of controlled-release (CR) coating of formulations such as osmotic-controlled release oral delivery system (OROS) and CR microspheres. Despite multiple applications, there are limited or no reports dealing with the characterization and quantification of CA in the formulated systems. Thus, the present investigation deals with the development of the Quantitative Carbon-13 Nuclear Magnetic Resonance (q13CNMR) spectroscopy method for the determination of CA amount in the CR microsphere formulations. The developed q13CNMR method was also verified using control CA samples from marketed OROS formulation. Thereafter, the concentration of CA in the microspheres was calculated. Furthermore, the impact of different concentrations of CA on the critical quality attributes such as the drug release profile from the formulation was investigated. The study demonstrated the CA coating levels to be inversely proportional to the extent and rate of release of API. The developed q13CNMR method was found to be accurate and precise and can be explored further to investigate the effect of different stability conditions on the degree of polymerization and degradation of CA resulting in altered quality of pharmaceutical products.