Comparative Dissolution Study Research Articles

Comparative Dissolution Study Between Resveratrol Nanocream Formula and Conventional Resveratrol Cream with Dimethylsulfoxide Addition

Resveratrol has potential activity as an antioxidant. Several studies have formulated resveratrol into topical preparations, but the low solubility of resveratrol causes low release of the active substance. Dimethylsulfoxide is a widely used ingredient in topical preparations, which can be used to increase the solubility of poorly soluble substances Nanocream is a nanoparticle-based topical drug delivery. The globule size is nanoscale, which can help improve drug solubility. The aim of the research was to conduct a comparative dissolution study between resveratrol nanocream formula and resveratrol conventional cream preparation with the addition of dimethylsulfoxide at various concentrations of 3%, 5% and 7%. The research method began with formulating resveratrol nanocream preparation. The preparation consisted of lipid components dispersed into a cream base. The lipids consisted of VCO, tween 80 and propylenglycol. Loading drug of resveratrol lipid was 300 mg, then tested for transimtance value and globule size. Conventional resveratrol cream formula was made into FI, FII and FIII, where each formula used different concentration of DMSO. Physical characteristics testing was conducted on nanocream and conventional resveratrol cream.Analysis of dissolution test results was observed among FI, FII and FIII in conventional cream formulas. The dissolution test results of these three formulas were also compared with the resveratrol nanocream preparation. Observation of dissolution results was assessed from the percentage of active substance released at minutes 5, 10, 15, 30, 45, 60.The dissolution test results showed that there was no significant difference in the percentage of active substance released between the conventional resveratrol cream preparation formulas, but there was a significant difference between the three conventional resveratrol cream preparation formulas and the resveratrol nanocream preparation.

The Influence of the coating on the release of Ibuprofen from the Tablet: Comparative Dissolution Study of the different types of coating

Ibuprofen is a non-steroidal anti-inflammatory drug known for its remarkable therapeutic effects. It can be available in different forms among which are coated and sugar-coated tablets.The objective of this study was to compare the dissolution profile between these two forms. The study was conducted with 5 ibuprofen drugs: 3 generics and one reference drug based on coated tablets, and one drug containing the coated tablets.The parameters used to evaluate and compare the dissolution profiles were the similarity (f2) and difference (f1) factors.The results obtained showed similar dissolution profiles for the two types of coating, with a more significant release for the sugar-coated tabletsduring the first 30 minutes.Dissolution studies are important studies to establish equivalence between generic and brand name drugs, and also to predict the release of the AP.

INVESTIGATION OF SOLID DISPERSION APPROACH FOR THE IMPROVEMENT OF PHARMACEUTICAL CHARACTERISTICS OF TELMISARTAN USING A CENTRAL COMPOSITE DESIGN

Objective: The goal of this study was to use a solid dispersion approach to improve the aqueous solubility and dissolution rate of Telmisartan. Methods: Design of experiment trials was conducted following a central composite design with different combinations of polymers and stirrer rpm and the selected responses (drug release, entrapment efficiency) were determined. The selected optimized formulation was characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, and X-ray diffraction, which reflected the changes that occurred in API and excipients after conversion in to the formulation. Results: In the design of experiments, central composite design was implemented and it was observed that polymers concentration (polyvinyl pyrrolidine K25, polyethylene glycol 4000) and stirrer rpm were having a significant impact on the responses (drug release, entrapment efficiency), and variables were having p-value<0.05 which reflected the significant impact. The results of stability study showed a significant no decrease in drug assay values, which reflected the stability behavior of the formulation. The results of comparative dissolution studies revealed that the optimized formulation have improved the drug solubility and dissolution rate. Conclusion: It can be concluded that optimized telmisartan-loaded solid dispersion improved the solubility and dissolution rate of Telmisartan. The optimized formulation was having release>85% release within 30 min. Further, the stability of the formulation was also assessed under the accelerated condition as per ICH which reflected their stability. So, this approach can be employed for improving dissolution rate of other BCS II class drugs.

Formulation Development of Tolperisone Hydrochloride Film Coated Tablet

Among all the different routes of administration, oral route of administration continues to be the most preferred route due to various advantages including ease of ingestion, avoidance of pain, versatility and most importantly patient compliance. Likewise, among all dosage forms tablet is the most popular dosage form existing today because of its convenience of self-administration, compactness and easy manufacturing. Sometimes immediate onset of action is considered obligatory immediate release tablets are the final option. Recently immediate release tablets have started gaining popularity and acceptance as a drug delivery system, mainly because they are easy to administer and lead to better patient compliance. In the present work, we engage in discussion about formulation, development, and evaluation of immediate release tablets. An immediate release dosage form allows a manufacturer to extend market exclusivity. They are also a tool for expanding markets, extending product life cycles and generating opportunities. pharmaceutical products designed for oral delivery and currently available on the prescription and over-the-counter markets are mostly the immediate release type, which are designed for immediate release of drug for rapid absorption. Tolperisone Hydrochloride Film Coated Tablets 50 mg was prepared using various excipients listed as in formula. The tablets were prepared by wet granulation method using concave plane punch on multi-station compression machine. The formulations were evaluated for their physical characteristics like thickness, hardness and friability, weight variation, content uniformity study was carried out. Evaluated for chemical analysis like Assay, disintegration and dissolution. In-vitro comparative dissolution study was performed with the help of U.S.P dissolution test apparatus-II with 900 ml of 0.1 N HCL, Acetate buffer pH 4.5 & 0.1 M HCL Acid at the 75 rpm for 45min.

Comparative Dissolution Study of Various Brands of Valsartan Tablets Marketed in Pakistan

Comparative Dissolution Study of Various Brands of Valsartan Tablets Marketed in Pakistan

Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations.

Nanocrystals are carrier-free, submicron-sized, colloidal drug delivery systems with particle sizes in the mean nanometer range. Nanocrystals have high bioavailability and fast absorption because of their high dissolution velocity and enhanced adhesiveness to cell membranes. Loxoprofen, a nonsteroidal anti-inflammatory drug belonging to the Biopharmaceutical Classification System (BCS) II drug class, was selected as the model drug. The aim of this study was to formulate nanocrystals of loxoprofen. A total of 12 formulations (F1 to F12) were prepared. An antisolvent technique was used to determine the effects of various stabilizers and processing conditions on the optimization of formulations. The various stabilizers used were hydroxypropyl methylcellulose (0.5%), polyvinylpyrrolidone (0.5%), and sodium lauryl sulfate (0.1%). The various characterizations conducted for this research included stability studies at 25 °C and 4 °C, scanning electron microscopy, transmission electron microscopy (TEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), zeta potentials, polydispersity indexes, and dissolution studies. F10 was the optimized formulation that showed stability at room temperature, as well as at a refrigerated temperature, for 30 days. A high dissolution rate (100% within the first 10 min) was shown by comparative dissolution studies of nano-suspensions with the micro-suspension and raw loxoprofen. F10 formulation had a non-porous and crystalline morphology on evaluation by TEM and XRPD, respectively, and the average particle size was 300 ± 0.3 nm as confirmed by TEM. DSC recorded a reduction in the melting point (180 °C processed and 200 °C unprocessed melting points). The dissolution rate and solubility of the formulated loxoprofen nanocrystals were significantly enhanced. It can be concluded that selecting suitable stabilizers (i.e., polymers and surfactants) can produce stable nanocrystals, and this can potentially lead to a scaling up of the process for commercialization.

Comparative dissolution studies of 3D-printed inserts in a novel biopharmaceutical bladder model

Urinary tract disorders come at great discomfort to the patients suffering from them. To treat them, several potent drug substances are available but unfortunately, systemic drug therapy often comes along with undesired adverse effects. Previous work has therefore been conducted aiming at a local drug release in the urinary bladder. However, whether a therapeutically relevant drug concentration may be reached at the target site is not easy to determine when applying common compendial dissolution methods. Therefore, the aim of this study was to develop a biorelevant dissolution model able to take physiological conditions into consideration, i.e. urine flow rates, urination intervals and movement patterns during day- and nighttime. The newly developed bladder model was tested with 3D-printed intravesical inserts containing three different APIs (lidocaine hydrochloride, trospium chloride and hydrochlorothiazide) and varying the operating conditions. Although the cumulative drug release was similar to the compendial method in most cases, notable differences became apparent in the corresponding concentration profiles of all APIs. It revealed periodic concentration fluctuations in 24 h intervals due to the constantly changing volume and agitation in the bladder model. The model furthermore allowed investigating the influence of varying physiological and pathophysiological conditions on local drug release.

Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment.

The current study was designed to prepare the inclusion complex Genistein (GS) using Hydroxypropyl β cyclodextrin (HP β CD) and poloxamer 188 (PL 188). The binary inclusion complex (GS BC) and ternary inclusion complex (GS TC) were developed by microwave irradiation technique and evaluated for a comparative dissolution study. Further, the samples were assessed for FTIR, DSC, XRD, and NMR for the confirmation of complex formation. Finally, antioxidant and antimicrobial studies and cytotoxicity studies on a breast cancer (MCF-7) cell line were conducted. The dissolution study result showed a marked increment in GS dissolution/release after incorporation in binary (GS: HP β CD, 1:1) and ternary (GS: HP β CD: PL 188; 1:1:0.5) inclusion complexes. Moreover, the ternary complex exhibited a significant enhancement (p < 0.05) in dissolution than did the binary complexes. This might be due to the presence of PL 188, which helps in solubility enhancement of GS. DSC, XRD and SEM evaluation confirmed the modification in the structure of GS. FTIR and NMR results indicated the formation of an inclusion complex. The antioxidant and antimicrobial activity results revealed that GS TC has shown significant (p < 0.05) higher activity than pure GS. The cytotoxicity study results also depicted concentration-dependent cytotoxicity. GS TC exhibited significantly (p < 0.05) high cytotoxicity to cancer cells (IC50 = 225 µg/mL) than pure GS (IC50 = 480 µg/mL). Finally, it was concluded that a remarkable enhancement in the dissolution was observed after the inclusion of GS in the ternary complex and it therefore has significant potential for the treatment of breast cancer.

Azithromycin Nanosuspension Preparation using Evaporative Precipitation into the Aqueous Solution (EPAS) Method and its Comparative Dissolution Study

Aim: EPAS (evaporative precipitation into aqueous solution) was used in the current studies to prepare azithromycin nanosuspensions and investigate the physicochemical characteristics for the nanosuspension batches with the aim of enhancing the dissolution rate of the nanopreparation to improve bioavailability. Methods: EPAS method used in this study for preparing azithromycin nanosuspension was achieved through developing an in-house instrumentation method. Particle size distribution was measured using Zetasizer Nano S without sample dilution. Dissolved azithromycin nanosuspensions were also compared with raw azithromycin powder and commercially available products. The total drug content of nanosuspension batches was measured using an Ultra-Performance Liquid Chromatography (UPLC) system with Photodiode Array (PDA) detector while residual solvent was measured using Gas Chromatography (GC). Results: The average particle size of azithromycin nanosuspension was 447.2 nm and total drug content was measured to be 97.81% upon recovery. Dissolution study data showed a significant increase in the dissolution rate for nanosuspension batch when compared to raw azithromycin and commercial version (microsuspension). The residual solvent found for azithromycin nanosuspension is 0.000098023 mg/mL or 98.023 ppb. Conclusion: EPAS was successfully used to prepare azithromycin nanoparticles that exhibited a significantly enhanced dissolution rate. Further studies are required to scale up the process and determine long term stability of the nanoparticles.

Design and Evaluation of Press Coated Formulation of Aceclofenac and Comparison with Marketed Preparations.

The primary objective of the studies is to investigate whether compression coating could be used to produce tablets providing maximum drug plasma concentration 6 to 8 hours after an evening dose taken at approximately 22:00. Fast Dispersible core tablets containing Aceclofenac were prepared using super disintegrants like Ac-Di-Sol, Crospovidone, and Sodium starch glycolate through wet granulation method and evaluated for various parameters. Prepared press-coated tablets were characterized for physical parameters, drug content, lag time, in vitro drug release characteristics. Aceclofenac formulation tablets of batch F4 containing combination Methocel K4M and Methocel K100M showed desired lag time along with drug release as compared to other formulations. The Comparative dissolution study of an optimized formulation containing Aceclofenac was carried with marketed preparations also showed good results.

Evaluation of Dissolution Profiles of a Newly Developed Solid Oral Immediate-Release Formula Containing Alpha-Lipoic Acid

Alpha-lipoic acid (ALA, thioctic acid), a naturally-occurring essential dithiol compound, has become a common ingredient in many pharmaceutical and food supplement products (FSP), used in oxidative stress-dependent pathologies; oral bioavailability of ALA is limited by pharmacokinetic particularities that reduce its therapeutic efficacy-reduced solubility, lack of gastric stability and hepatic degradation, doubled by formulation hinders. The objectives were to develop a solid oral 600 mg ALA FSP to obtain an optimal pharmaceutical profile compared to a reference listed drug (RLD) with a similarity factor f2 50. A comparative dissolution study was performed; an HPLC method was used for ALA quantification. After planning combinatory simulations (formulation stage), two prototype formulas (#1 and #2) were manufactured and further optimized by adjusting ALA physical characteristics and the excipients quantities (#3 and #4) in order to achieve the Quality Target Product Profile. A misshapen of ALA’s in vitro release was observed for #3 Formula (f2 = 31.6); the optimal profile was obtained for Formula #4 (f2 = 58.5). A simple quantitative formula is not enough to assure good ALA bioavailability; the formulation needs multiple compounding modulations under physicochemical compatibility algorithms, with multiple dissolution profiles testing back-ups. It is essential to ensure a formulation with an in vitro dissolution comparable with the RLD, allowing the compound to reach its target level to assure the optimum claimed antioxidant activity of ALA at the cellular level, even for food supplement formulations.

COMPARATIVE DISSOLUTION STUDIES OF WARFARIN SODIUM TABLETS: INFLUENCE OF AGITATION RATE, DISSOLUTION MEDIUM, AND USP APPARATUS

Objective: The aim of this study was to carry out comparative dissolution studies with warfarin sodium reference tablets under the hydrodynamic environments generated by the USP basket and paddle apparatus and flow-through cell using different agitation rates and dissolution media.&#x0D; Methods: Dissolution profiles were obtained with the USP basket and paddle apparatus at 50, 75, and 100 rpm and 900 ml of water as dissolution medium. After this, dissolution profiles of warfarin sodium were obtained with the USP paddle apparatus and flow-through cell method using 0.1 N hydrochloric acid, acetate buffer pH 4.5, phosphate buffer pH 6.8, and water. Spectrophotometric determination at 308 nm was carried out during 30 min. Dissolution profiles were compared with model-independent and model-dependent approaches.&#x0D; Results: Significant differences were found with mean dissolution time and dissolution efficiency at 50 and 75 rpm (*P&lt;0.05). Makoid-Banakar was the best-fit model used to describe the in vitro release performance of warfarin sodium with 50-100 rpm and the USP basket and paddle apparatuses. Significant differences in all calculated parameters were found (*P&lt;0.05) excepting percent dissolved at 30 min with 0.1 N hydrochloric acid and phosphate buffer pH 6.8.&#x0D; Conclusion: More research is necessary to identify the in vitro release performance of poorly soluble drugs under available USP apparatuses considering factors as agitation rate and kind of dissolution media. The knowledge of the in vitro release performance of reference drug products is important for the design of better generic formulations

Comparative dissolution and polymorphism study of clopidogrel bisulfate tablets available in Argentine

Comparative dissolution and polymorphism study of clopidogrel bisulfate tablets available in Argentine

In Vitro Dissolution and In Vivo Bioequivalence Evaluation of Two Metformin Extended‐Release Tablets

The objective of the present study was to evaluate the bioequivalence between generic and branded metformin extended-release (ER) tablets in Chinese subjects. We tested bioequivalence in vitro and in vivo using a comparative dissolution study and a comparative pharmacokinetic trial. Safety assessments were conducted throughout the entire trial period. The dissolution profiles of the generic formulation expressed obvious extended-release properties, similar to those of the branded formulation (f2 > 60.0%). Consistent with the result of the in vitro study, no remarkable differences were found in terms of pharmacokinetic profiles between generic and branded formulations. The 90% confidence intervals of Ln AUC0-36h , Ln AUC0-∞ , and Ln Cmax from generic formulation versus branded formulation were 91.4% to 105.0%, 91.3% to 104.7%, and 101.2% to 119.4%, respectively. During the entire trial period, 4 subjects experienced 11 adverse events. All these were mild and spontaneously resolved. The results obtained from the present study suggest that the generic and branded metformin ER tablets were bioequivalent in Chinese subjects.

MODULATORY EFFECT OF POLYMER TYPE AND CONCENTRATION ON DRUG RELEASE FROM SUSTAINED RELEASE MATRIX TABLETS OF RANOLAZINE: A COMPARATIVE RELEASE KINETIC STUDY

Objective: Ranolazine (RZ), antianginal drug indicated for the treatment of chronic stable angina pectoris, was formulated into sustained-release matrix tablets and optimized to improve patient compliance and achieve controlled release over a certain period.&#x0D; Methods: Different formulations were prepared by wet- and melt-granulation techniques. Excipients at different ratios as Eudragit® L100-55, Methocel™ E5, Avicel® PH-101, and carnauba wax powder were used to develop a ternary polymeric matrix system for the controlled delivery of RZ. The prepared formulations were subjected to granulometric and characteristic studies. Comparative dissolution and release kinetic studies of the selected formulation and the reference product, Ranexa® extended-release film-coated tablets, Gilead Sciences, Inc., USA, were further carried out to ensure product similarity.&#x0D; Results: The optimum pH-dependent to pH-independent polymers ratio was 1:1.3 (w/w). Extragranular carnauba wax in a concentration of 32.50 mg/tablet (2.50 gm% w/w) was the key excipient in controlling drug release kinetics by forming waxy matrix granules which prevent rapid dissolution. Modulation of the microenvironmental pH using a potent alkalinizing agent was very effective for controlling drug release patterns in different dissolution media from pH 1.2–6.8.&#x0D; Conclusion: The release of RZ from the matrix tablets was controlled for a period of 24 h, and thereby expected to provide patient compliance with minimal side effects.

Comparative dissolution studies on granules with acetaminophen and caffeine using the basket and paddle methods with simultaneous spectrophotometric determination of active substances

Abstract Acetaminophen and caffeine, popular therapeutic substances used to relieve pain or alleviate the symptoms of cold. The aims of the study were the comparison of granules, in terms of dissolution rate and moreover the development of spectrophotometric method to the simultaneous determination of both active pharmaceutical ingredients (APIs) in granules. The granules were tested by two pharmacopoeial methods of dissolution for solid dosage forms, and the dissolution profiles for each formulation were compared. A method of simultaneous determination of two medicinal substances by the double calibration method using derivative spectrophotometry was used. Considering the dissolution process carried out in the paddle apparatus, it was shown that more than 80% of acetaminophen and caffeine were released from each of the preparations in a clearly shorter time than 10 minutes. Carrying out the basket test, substances dissolved gradually, much slower than in the paddle method. The time required to release 80% of both active substances from majority of tested preparations was from 30 to 45 minutes. Application of the first derivative spectrophotometric method allows simultaneous determination of acetaminophen and caffeine in the mixture, without the need to separate them first.

Optimization of ibuprofen hydrogel-based Matrix tablet formulation for oral delivery

Objective. Ibuprofen, a nonsteroidal anti-inflammatory drug, is poorly soluble leading to its slow systemic absorption. This study aimed to optimize the formulation of an ibuprofen hydrogel-based matrix tablet to improve its dissolution for better oral bioavailability.&#x0D; Methods. Raw material of ibuprofen was subjected to quality control test and compatibility test with the excipients. Six trial formulations were performed, with polyethylene glycol (PEG) 6000 as the matrix for the first three trial formulations and carbopol for the remaining trial formulations. Finished product quality control (FPQC) tests were conducted to choose the best formulations to be compared against the marketed products using comparative dissolution and stability studies.&#x0D; Results. Among the trial formulations, Formulation 3 and Formulation 4 displayed highly satisfactory results from FPQC. The results of disintegration tests, comparative dissolution, and stability studies suggested carbopol as the better polymer over PEG 6000 which made Formulation 4 as the best.&#x0D; Conclusion. Based on the percent drug release and similarity factor, it was concluded that the formulation optimized in this study was considered to be similar with the standard liquigel.

Preparation and Optimization of Fast-Disintegrating Tablet Containing Naratriptan Hydrochloride Using D-Optimal Mixture Design.

Optimization of a lyophilized fast-disintegrating tablet (LFDT) formulation containing naratriptan hydrochloride, an antimigraine drug, was the foremost objective of the study, aiming in achieving fast headache pain relief. The Design-Expert® v10 software was used to generate formulations using D-optimal mixture design with four components: gelatin (X1), hydrolyzed gelatin (X2), glycine (X3), and mannitol (X4) of total solid material (TSM) w/w. The effect of the relative proportion of each component was determined on friability (Y1), hardness (Y2), and in vitro disintegration time (Y3), which was then applied for formulation optimization. In addition, their effect on tablet porosity was determined via scanning electron microscopy (SEM). Drug-excipient interaction was evaluated using differential scanning calorimetry (DSC). A comparative dissolution study against the conventional tablets was studied. Accelerated stability study was carried out in (Al/Al) and (Al/PVC) blister packs. An in vivo pharmacokinetic study was carried out to compare the optimized formulation and the conventional tablets. The optimized formulation's responses were 0.30%, 3.4kg, and 6.12s for Y1, Y2, and Y3, respectively. No drug-excipient interaction was specified via DSC. The optimized formulation exhibited porous structure as determined via SEM. Dissolution study demonstrated complete dissolution within 1.5min. Study indicated stability for 78months in (Al/Al) blister packs. In vivo pharmacokinetic study demonstrated that Cmax, AUClast, and AUCinf were significantly higher for the developed formulation. As well, the Tmax was 1h earlier than that of convenient tablet. An LFDT would achieve a faster onset of action for naratriptan compared to other formulations.

Comparative In-Vitro Dissolution Studies for Determination of Cefixime in an Innovator Product of Suprax Powder for Oral Suspension Dosage form Using Rp-Hplc Method

Comparative In-Vitro Dissolution Studies for Determination of Cefixime in an Innovator Product of Suprax Powder for Oral Suspension Dosage form Using Rp-Hplc Method

Comparative Dissolution and Disintegration Study of Different Brands of Linezolid 600 mg Tablets Available in Karachi, Pakistan

The dissolution and disintegration tests (USP) are extensively useful for the determination of the safe and effective drugs as well as used for the stability and quality of the drug product. The purpose of the study was to observe the disintegration and dissolution profile (UV spectrophotometer), and estimation of the quality through weight variation and hardness test of different brands of Linezolid 600 mg tablets from Karachi, Pakistan. The weight variation test for all the brands was found to be under normal limits and the hardness of all the brands was also within normal limits. The tablet disintegration time was as per the specifications and all the tablets were disintegrated within 30 minutes except for brand C3, which disintegrates within 3.98 minutes and provided better disintegration time. Although, all the brands showed better dissolution rate, but the percent drug release of C1 was found to be the best, i.e. 100% drug was dissolved in 30 minutes in contrast to the different brands. Dissolution test is comparatively an efficient and cost effective in vitro approach that can be helpful in the assessment of the release attributes of formulation. It was found that brand C1 and C2 exhibited better dissolution profile as compared to other brands. Although, C3 and C4 were also found to be under the limits i.e. 80 % of the label amount of the drug.