Controlled-release Tablets Research Articles

Development of the novel formulations of perospirone for the treatment of schizophrenia.

Schizophrenia is a severe mental illness. Its clinical features include positive symptoms (hallucinations, delusions, thought disorders), negative symptoms (avolition, anhedonia, poverty of thought, social withdrawal), and cognitive dysfunction. A large number of antipsychotic drugs with traditional dosage forms are available to mitigate the symptoms of schizophrenia but the duration of action is commonly short, often requiring frequent administration. The perospirone hydrochloride hydrate (PER), as a second-generation antipsychotic drug, shows therapeutic effects on both positive and negative symptoms of schizophrenia, with less impact on cognitive function. However, it suffers from a short half-life, fluctuating blood concentration, instability in the circulating leading to peak-trough fluctuations, and poor patient compliance due to the required frequent administration. Based on the hydrophilic matrix, we developed novel formulations of PER, including the extended-release and the controlled-release tablets of PER. The resulting formulations delayed the drug release and prolonged the persistence of PER, leading to an extended half-life and reduced fluctuations in blood concentration with stable therapeutic levels and an improved absorption with higher bioavailability, thus reducing dosing frequency. These oral extended-release and controlled-release tablets promise to alleviate patients' medication discomfort and provide long-term sustained drug release. They would provide a platform with broad prospects for the clinical treatment of schizophrenia.

Formulation and Evaluation of Controlled Release Tablet Using Thyme and Rosemary for Osteoporosis

Osteoporosis is a common public health problem which currently affected millions of people worldwide. Osteoporosis is mainly associated with Ovarian hormone deficiency following menopause is till now a most common reason of age-related bone loss. There are tablets that are available in the market, which shows the side effect such as nausea, heart burn, gastric problem after the continuous use of medicine. These side effects led to the avoidance of such medicine. Using herbal plant such as thyme and rosemary as an alternative of those drug will help to reduce these effects. Hence, selected to develop a Controlled Release Tablet of Rosemary and Thyme. Tablet is the most popular among all dosage forms existing today because of its convenience of self-administration, compactness and easy manufacturing. Developing the tablet using thyme and rosemary in the form of controlled release drug will help to prolonged the effect of the medicine. As precision of dosing, to improve the bioavailability of the drug and to maintain the constant level of drug in the plasma become important to provide the long-term effect to the patient. It will also provide the patience compliance as well as prolonged the effect of drug in the patient’s body.

Development and In vitro Evaluation of Pantoprazole-Sustained Release Effervescent Floating Tablets for Effective Management of Ulcer

Introduction: Pantoprazole is a very suitable drug for the treatment of numerous acid-related conditions in humans and mammals. Owing to its short half-life (0.9 – 1.9 h), it is ideal for sustained release formulation. Methods: This study was aimed at developing pantoprazole gastroretentive (GR) controlledrelease tablets and to determine the effects of this formulation and processing parameters on drug release and other critical quality attributes of directly compressed tablets produced using different matrix-forming polymers, namely, Hydroxypropyl methylcellulose (HPMC), chitosan, sodium alginate, maize starch, kappa- carrageenan, and propyl vinyl pyrrolidine PVP K30 when formulated into effervescent Floating Drug Delivery Systems (FDDS). Results: The buoyancy lag time of less than 5 seconds and a total floating time of more than 12 hours for all batches is a good indication of achieved floatation for FDDS. Conclusion: Validation processes initiated with the five batches indicated that the polymer blends had the potential for the formulation of pantoprazole FDDS and, hence, could enhance patient compliance and better treatment outcomes due to their sustained release potentials.

Effects of intravenous nicardipine followed by oral labetalol in combination with nifedipine controlled-release tablet on severe peripartum hypertension.

To investigate the effects of intravenous nicardipine as initial therapy and oral labetalol combined with nifedipine controlled-release tablet as subsequent treatment of severe peripartum hypertension. Intravenous nicardipine was delivered as the initial treatment, after the target blood pressure (BP) had been achieved, oral labetalol was used to maintain the target BP. If oral labetalol failed to maintain the target BP, oral labetalol combined with nifedipine controlled-release tablet was used. A total number of 131 patients were enrolled. The target BP (BP < 140/90 mmHg) was achieved in all patients within 60 minutes by intravenous nicardipine. After receiving labetalol orally, the target BP was maintained in nine patients. However, in 104 patients, we had to combine oral labetalol and nifedipine controlled-release tablet due to re-elevation of their systolic BP to 140-159 mmHg. In 18 patients, we restarted intravenous nicardipine because their systolic BP re-elevated above 160 mm Hg. Among the 104 patients who received oral labetalol and nifedipine controlled-release tablet, the target BP was achieved and maintained in 96 patients, and eight patients had to restart nicardipine. Of the total number of 26 patients in whom intravenous nicardipine was resumed, the target BP was successfully maintained in 22 patients with oral labetalol combined with nifedipine controlled-release tablet. Intravenous nicardipine rapidly and safely lowered severe peripartum hypertension. As subsequent therapy, oral labetalol combined with nifedipine controlled-release tablet protocol may be applied to effectively maintain a target BP.

Intestinal Absorption Site-Guided Development and Evaluation of Oral Disintegrating Controlled Release Tablets of Mirabegron

The aim was to employ site-dependent absorption of mirabegron (MB) as a guide for fabrication of oral disintegrating controlled release tablet (ODCRT) which undergoes instantaneous release of loading fraction followed by delayed release of the rest of MB. The goal was to release MB in a manner consistent with the chronobiology of overactive bladder (OAB) syndrome. In situ rabbit intestinal permeability of MB was adopted to assess absorption sites. MB was subjected to dry co-grinding with citric acid to develop the fast-dissolving fraction in the mouth. Delayed release fraction was formulated by ethanol-assisted co-processing with increasing proportions of Eudragit polymer (S100) as pH responsive polymer. The developed dry mixtures underwent thermal (DSC) and physical (X-ray diffraction) characterization, in addition to in vitro release behavior. Optimized fast dissolving and delayed release formulations were mixed with tablet excipient before compression in ODCRT which was assessed for release profile using continuous pH variation. MB underwent preferential permeation through ileum and colon. Co-grinding with citric acid provided co-amorphous powder with fast dissolution. Co-amorphization of MB with Eudragit S100 (1:5) showed pH-dependent release to release most of the dose at pH 7.4. The developed ODCRT released 43.5% of MB in the buccal environment and retained MB at acidic pH to start release at pH 7.4. The study successfully fabricated ODCRT guided by site-dependent absorption. The ODCRT instantaneously released loading fraction to support the patient after administration with delayed fraction to sustain the effect.Graphical

Controlled Release Lercanidipine Tablets: A Study on Formulation and Evaluation by Wet Granulation

Lercanidipine blocks the entry of extracellular calcium into vascular and cardiac muscle cells, preventing myocardial smooth muscle contraction due to decreased intracellular calcium. This results in the dilation of coronary and systemic arteries, reducing blood pressure. This study aimed to develop and evaluate lercanidipine controlled-release tablets for oral administration using polymers like HPMC K 100M, sodium alginate, and guar gum. Lercanidipine, polymers, and diluents were sieved and mixed for 10 minutes. Granules were formed using isopropyl alcohol, dried at 60°C for one hour, and sieved. The granules were lubricated with colloidal silicon dioxide (Aerosil-200) and magnesium stearate, blended for 5 minutes, and compressed using a rotary machine (average weight: 500 mg; hardness: 5-6 kg/cm²). Bulk and tapped densities were nearly identical for all formulations. Compressibility index and Hausner ratio ranged from ?18 to 1.09-1.21, indicating good flow properties. Tablet thickness ranged from 5.82 to 5.91 mm, hardness from 5.9 to 6.3 kg/cm², and friability was less than 1.0 %W/W. Drug content was between 98-102%. The controlled-release order from dissolution data was F9 &gt; F7 &gt; F8, showing optimal release with a combination of HPMC and two natural polymers.

Structural and Release Properties of Combined Curcumin Controlled-Release Tablets Formulated with Chitosan/Sodium Alginate/HPMC.

Controlled-release tablets offer several benefits, such as controlled release, odor masking, ease of use, stability, extended shelf life, and reduced production costs. This study developed combined curcumin controlled-release tablets (CCCTs) to increase the bioavailability of curcumin with hydroxypropyl methylcellulose (HPMC), chitosan, and sodium alginate. The hardness of the CCCTs was 5.63-1.98 kgf, friability was 0.00-1.22%, and disintegration time was 0.00-401.25 min. Differential scanning calorimetry and Fourier-transform infrared spectroscopy indicated a high compatibility between the excipients and curcumin. CCCTs with chitosan formed a gel structure, impeded disintegration, and reduced the release rate to 72.5% in simulated gastric fluid. In simulated intestinal fluid, CCCT with the HPMC-sodium alginate group formed a polyelectrolyte membrane hydrogel to prolong release from 6 to 12 h. This study developed various CCCT formulations that can be delivered through the gastric or intestinal tracts, using chitosan and HPMC-sodium alginate as excipients, respectively. CCCT can be used as a reference strategy for controlled-release curcumin delivery in the functional and healthcare supplement development.

Development of single layer osmotic controlled release tablet for low soluble drug: Single Core Osmotic Pump (SCOP)

A novel Single Core Osmotic Pump (SCOP) pill has been created to administer high doses of the low solubility medication Rifaximin using osmosis. The formulations were evaluated using six comparative parameters: Q24 (total release after 24 hours), Q12 (total release after 12 hours), TL (lag time), RSQzero12 (R square of the zero-order equation for drug release in 12 hours), RR12 (in vitro release rate for 12 hours), and T80% (time required to deliver 80% of the drug). The drug release profile from osmotic devices shows that the choice of polymer and its concentration in the core formulation can significantly impact the release of the drug. Augmenting the osmogent quantity to an optimal level resulted in a substantial enhancement of Q12 and a notable improvement in the zero-order release pattern of rifaximin. In order to improve the bioavailability of the core formulation, an additive called citric acid was included. Citric acid has several properties that contribute to this enhancement, such as increased solubility of the active ingredient, the creation of a difference in osmotic pressure, regulation of the flow of the active ingredient, and making the composition containing the active ingredient more water-loving. Consequently, TL and T80% experienced a decline, whereas Q12 and RR12 saw a rise. The concentration of PEG 4000 in the semipermeable membrane of the SCOP was found to have a significant impact on TL, T80%, Q12, Q24, and RR12. Specifically, increasing the concentration of PEG 4000 led to a decrease in TL and T80%, while increasing Q12, Q24, and RR12. The optimal aperture diameter for achieving a zero-order release pattern was found to be 850 μm. This study also demonstrated that optimizing the thickness of SPM is crucial for achieving zero order kinetics. The invented SCOP technology has the potential to create a single layer osmotic controlled release tablet of a water insoluble medication with a high dosage.

Comparison of Clinical Effects of Sacubitril Valsartan Sodium Tablets and Nifedipine Controlled-Release Tablets in the Treatment of Chronic Renal Insufficiency Complicated with Hypertension

Objective: To compare the clinical effects of using sacubitril valsartan sodium tablets with nifedipine controlled-release tablets in patients with chronic renal insufficiency combined with hypertension. Methods: 110 patients with chronic renal insufficiency combined with hypertension treated in our hospital from April 2023 to February 2024 were taken as the study subjects. They were divided into the test group (n = 55) and the comparison group (n = 55) by randomized numerical table method. The test group was provided with sacubitril valsartan sodium tablets and the comparison group was treated with nifedipine controlled-release tablets. The urine excretion rate of albumin and blood urea nitrogen levels as well as adverse effects were compared before and after treatment in both groups. Results: In the test group, the urinary albumin excretion rate was 101.77 ± 7.42 μg/min and the blood urea nitrogen level was 15.81 ± 1.76 mmol/L, which was much lower than that of the comparison group; the total rate of adverse reactions in the test group was 1.82%, which was significantly lower than that of the comparison group, the difference between the data of the test group and the comparison group after treatment is statistically significant (P &lt; 0.05). Conclusion: By providing treatment with sacubitril valsartan sodium tablets for patients with chronic renal insufficiency combined with hypertension, their urinary albumin excretion rate and blood urea nitrogen level are significantly improved, and the total occurrence rate of adverse reactions is low.

Comparative Bioequivalence and Food Effect of Two Formulations of 30-mg Nifedipine Controlled-Release Tablets in Healthy Chinese Adults.

Nifedipine is a potent antihypertensive medication classified as a dihydropyridine calcium channel blocker. The objective of this trial was to assess the bioequivalence of a 30-mg nifedipine controlled-release tablet and a reference drug in a cohort of healthy Chinese individuals. Two independent open-label, randomized, single-dose, crossover studies were conducted, 1 under fasting conditions (N = 44, with 1 participant dropping out midway) and the other under fed conditions (N = 44, with 4 participants dropping out midway). Plasma concentrations of nifedipine were determined using liquid chromatography-mass spectrometry, and pharmacokinetic (PK) parameters were calculated using noncompartmental analysis with Phoenix WinNonlin 8.0 software. In both fasting and fed studies, reasonable bioequivalence was observed for the PK parameters of both the test product and the reference drug. A good safety profile was demonstrated for both the test product and reference drug, with no serious adverse events reported, and both were similarly well tolerated. An important observation with food coadministration was that systemic exposure to nifedipine (based on area under the curve, AUC0-∞) was reduced by approximately 12%. The bioequivalence of the test product and reference drug under fasting/fed conditions in healthy subjects in China was demonstrated by the study results.

Economic evaluation of Annao Pills combined with antihypertensive drugs in treatment of primary hypertension: a study based on decision tree model

The purpose of this study was to evaluate the economics of Annao Pills combined with antihypertensive drugs in the treatment of primary hypertension in the Chinese medical setting. TreeAge pro 2018 was used for cost-effect analysis and sensitivity analysis of the two treatment regimens. The intervention time of the simulation model was 2 weeks. The cost parameters were derived from Yaozhi.com, and the effect parameters were based on Meta-analysis of randomized controlled trial(RCT) involving Annao Pills. The experimental group was treated with Annao Pills combined with anti-hypertensive drugs(nifedipine controlled-release tablets + losartan potassium tablets), and the control group was treated with anti-hypertensive drugs(nifedipine controlled-release tablets + losartan potassium tablets). The basic analysis showed that the incremental cost-effect ratio(ICER) of the two groups was 2 678.67 yuan, which was less than 7.26% of the per capita disposable income in 2022. That is, compared with anti-hypertensive drugs alone, Annao Pills combined with antihypertensive drugs cost 2 678.67 yuan more for each additional patient with primary hypertension. The results of sensitivity analysis verified the robustness of the basic analysis results. The probability sensitivity results showed that when the patient's personal willingness to pay the price was higher than 2 650 yuan, the probability of the regimen in the experimental group was higher, which was consistent with the results of the basic analysis. In conclusion, when the price was higher than 2 650 yuan, Annao Pills combined with anti-hypertensive drugs was more economical than anti-hypertensive drugs alone in terms of improving the response rate of the patients with primary hypertension.

Effect of Hydration Forms and Polymer Grades on Theophylline Controlled-Release Tablet: An Assessment and Evaluation.

Drug release from controlled release delivery systems is influenced by various factors, including the polymer's grade and the drug's hydration form. This study aimed to investigate the impact of these factors on the controlled release of theophylline (THN). This research compares the monohydrate form found in branded products with the anhydrous form in generic equivalents, each formulated with different polymer grades. Quality control assessment was conducted alongside in vitro evaluation, complemented by various analytical techniques such as X-ray diffraction (XRD) and scanning electron microscopy (SEM). Additionally, thermal analyses using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were employed. Quality control assessments demonstrated that the generic tablets exhibited lower average weight and resistance force compared to the branded ones. In vitro tests revealed that generic tablets released contents within 120 min, compared to 720 min for the branded counterpart. Characterization using XRD and SEM identified disparities in crystallinity and particle distribution between the three samples. Additionally, the thermal analysis indicated consistent endothermic peaks across all samples, albeit with minor variations in heat flow and decomposition temperatures between the two products. This study demonstrated that variations in polymer grade and hydration form significantly impact THN release.

Physiologically based pharmacokinetic modeling of ritonavir-oxycodone drug interactions and its implication for dosing strategy

The concomitant administration of ritonavir and oxycodone may significantly increase the plasma concentrations of oxycodone. This study was aimed to simulate DDI between ritonavir and oxycodone, a widely used opioid, and to formulate dosing protocols for oxycodone by using physiologically based pharmacokinetic (PBPK) modeling. We developed a ritonavir PBPK model incorporating induction and competitive and time-dependent inhibition of CYP3A4 and competitive inhibition of CYP2D6. The ritonavir model was evaluated with observed clinical pharmacokinetic data and validated for its CYP3A4 inhibition potency. We then used the model to simulate drug interactions between oxycodone and ritonavir under various dosing scenarios. The developed model captured the pharmacokinetic characteristics of ritonavir from clinical studies. The model also accurately predicts exposure changes of midazolam, triazolam, and oxycodone in the presence of ritonavir. According to model simulations, the steady-state maximum, minimum and average concentrations of oxycodone increased by up to 166% after co-administration with ritonavir, and the total exposure increased by approximately 120%. To achieve similar steady-state concentrations, halving the dose with an unchanged dosing interval or doubling the dosing interval with an unaltered single dose should be practical for oxycodone, whether formulated in uncoated or controlled-release tablets during long-term co-medication with ritonavir. The results revealed exposure-related risks of oxycodone-ritonavir interactions that have not been studied clinically and emphasized PBPK as a workable method to direct judicious dosage.

DEVELOPMENT OF CONTROLLED RELEASE FORMULATIONS OF DEXLANSOPRAZOLE TO IMPROVE BIOAVAILABILITY

The present work was aimed to development of controlled release formulations of Dexlansoprazole to improve bioavailability. Dexlansoprazole is the proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Dexlansoprazole blocks the final step in acid production, thus reducing gastric acidity. Construction of calibration curve of Dexlansoprazole and to investigate the drug and polymer interaction studies by FTIR and DSC. To prepare the different controlled release formulations of Dexlansoprazole tablets with different polymers such as acrylic acid polymer such as Carbopol-974P, HPMC grades for prevalence HPMC-K4M, HPMC-K15M, HPMCK100M, Natural Polymers akin to Xanthan gum, Guar gum, Sodium Carboxy Methyl Cellulose, and Pectin by Direct Compression method. Evaluation of Dexlansoprazole pre compression parameters such as Bulk density, Tapped density, Hausner’s ratio, Carr’s index, Angle of repose. Evaluation of post-compression parameters of Dexlansoprazole controlled release tablets such as Weight variation, Hardness, Friability test, Thickness, Drug Content and In-vitro dissolution studies. Evaluation of in-vitro dissolution uniqueness of all the formulations of Dexlansoprazole by using USP dissolution apparatus type-II (paddle). To study the mechanism of drug dissolution by applying kinetic parameters. To perform the stability studies of optimized formulations of Dexlansoprazole as per ICH guidelines.

Formulation and Evaluation of Losartan Potassium Controlled Release Tablets Using Starch Based Polymers

Formulation and Evaluation of Losartan Potassium Controlled Release Tablets Using Starch Based Polymers

Tongue Edema Caused by Taking Nifedipine Controlled-Release Tablets.

Tongue Edema Caused by Taking Nifedipine Controlled-Release Tablets.

Design and Evaluation of Ginkgolides Gastric Floating Controlled Release Tablets Based on Solid Supersaturated Self-nanoemulsifying.

Ginkgolides are receptor antagonist of platelet activating factor with great clinical prospect, but its application is limited by its low solubility, short half-life and poor alkaline environment stability. It is difficult to solve these problems with a single drug delivery system. In this study, supersaturated self-nanoemulsifying gastric floating tablets of ginkgolides were developed through the combination of solid supersaturated self-nanoemulsifying drug delivery system (solid S-SNEDDS) and gastric retentive floating drug delivery system (GFDDS) to solve these problems of ginkgolides. Solid S-SNEDDS was prepared by D-optimal mixture design, normalization method and single factor experiment. The properties of solid-S-SNEDDS were studied by TEM, PXRD, FT-IR, SEM and in vitro drug release profile. Then, the optimal formulation of stomach floating tablet was obtained through single factor experiment and center composite design, followed by the study of in vitro release, model and mechanism of release, in vitro buoyancy and kinetics of erosion and swelling. PXRD and FT-IR showed that the drug in solid S-SNEDDS existed in an amorphous manner and formed hydrogen bond with excipients. The results showed that the cumulative release of GA and GB in the optimal tablets was 96.12% and 92.57% higher than the simple tablets within 12 h. The release mechanism of the tablet was skeleton erosion and drug diffusion. In 12 h, the optimal tablets can float stably in vitro and release the drug at a constant rate, with a cumulative release of more than 80%. In summary, the combination of SNEDDS and GFDDS is a promising means to solve the problems of ginkgolides.

Formulation and Evaluation of Gastro Retentive Floating Tablet of Cetirizine Hydrochloride using Linseed Mucilageas Polymer

This study’s objectives were to create and assess gastric-floating controlled release tablets employing flaxseed mucilage as polymer. Linseed mucilage was isolated from Linum usitatissum seeds. Compatibility studies were performed on drug and other excipients. This study employed individual and mixed polymers to manufacture floating CH tablets. The polymers HPMC, MCC, and linseed mucilage were utilized in various ratios. Five distinct formulae were created (F1-F5 by powder a direct compression method. Formulations was tested for various parameters including in-vitro drug release and floating ability. The findings of all evaluation parameters are substantial. With an 8-hour floating time and a medicine release rate of 98.4% at end of the 24 hours, the formulation (F3), including hydroxyl propylmethyl cellulose and Linseed mucilage was shown to be the best. The current study focuses on the formulation of floating tablets using a natural polymer as a binder (Linseed mucilage). However, in-vivo experiments are still needed to establish the efficacy of the manufactured CH floating tablets.

Late-onset non-obstructive mesenteric ischemia (NOMI) resulting from delayed absorption of overdosed antihypertensive drugs: An autopsy case report.

Non-obstructive mesenteric ischemia (NOMI) is caused by reduced blood flow to the intestines without physical occlusion in the mesenteric artery. Previous reports show that drug overdose occasionally induces late-onset NOMI; however, in most cases, the reason for the delayed onset is unclear. Here, we present an autopsy case of late-onset NOMI that was induced by a drug overdose. An 80-year-old man was admitted to the intensive care unit because of severe hypotension after an overdose of antihypertensive drugs. He received vasopressor therapy and continuous hemodiafiltration dialysis; however, gastrointestinal decontamination was not performed. He began to recover but developed acute mesenteric ischemia on the evening of day 4 and died on day 5. Autopsy showed discontinuous submucosal bleeding from the duodenum to the colon; there was no thrombus in the mesenteric artery, which led to a diagnosis of NOMI. In the stomach, there was 250mL of reddish-brown fluid with a muddy brown substance. Histologic examination revealed ischemic necrosis in the small intestine. Quantitative analysis of serum collected during hospitalization revealed that nifedipine and cilostazol levels had peaked on day 3 of hospitalization. The formulation of nifedipine was a controlled-release tablet, and the low water solubility of cilostazol may have caused the tablets to adhere and remain in the stomach. Therefore, the drugs had been released into the blood stream several days after hospitalization, leading to delayed-onset NOMI. In cases of overdose, it is crucial to consider the formulation and properties of the involved drugs when determining medical treatment.

Population pharmacokinetic modeling of levodropropizine: extended application to comparative analysis between commercial formulations and exploration of pharmacokinetic effects of diet.

Levodropropizine, a nonopioid antitussive agent, is being increasingly used in clinical practice with the development of several formulations for symptomatic relief of acute and chronic bronchitis. However, scientific and quantitative population pharmacokinetic analyses of levodropropizine are lacking. Moreover, no integrated quantitative comparison has been performed between formulations. This study quantitatively evaluated and predicted pharmacokinetic properties of formulations through population pharmacokinetic model-based comparisons of commercially available formulations. Plasma concentration profile results from bioequivalence studies of 60-mg immediate release (IR) levodropropizine tablets in 40 healthy Korean males were used as population pharmacokinetic modeling data. For interindividual variability in levodropropizine pharmacokinetics, body surface area was identified as an effective covariate that was positively correlated with peripheral compartment distribution volume. Population pharmacokinetic model for IR tablets well-described the levodropropizine syrup and capsule datasets, suggesting no significant differences in pharmacokinetics among IR tablets, syrups, and capsules of levodropropizine. In contrast, pharmacokinetic profiles differed between 90-mg controlled release (CR) and IR levodropropizine tablets; however, separate parameter estimation was possible by applying the same model structure. In terms of pharmacokinetics, twice-daily regimen of 90-mg CR tablets was equivalent to thrice-daily regimen of 60-mg IR tablets. However, at steady-state, interindividual plasma concentration variability within population was reduced by approximately 36.71-83.18%. For levodropropizine CR tablets, a high-fat diet significantly delayed gastrointestinal absorption but maintained overall plasma exposure equivalent. This study provides useful quantitative judgment data for precision medicine of levodropropizine and can be helpful in predicting the pharmacokinetics of levodropropizine based on commercialized formulation switching.