Hydroxypropyl Methylcellulose Concentration Research Articles

3D printing of extended-release tablets of theophylline using hydroxypropyl methylcellulose (HPMC) hydrogels.

An extrusion based 3D printer was used to prepare the semi-solid tablets with different drug loading dosages (75, 100, 125mg) under ambient temperature. The active pharmaceutical ingredient, theophylline, was uploaded within the hydrogels prepared of hydroxypropyl methylcellulose (HPMC) K4M or E4M. The HPMC concentrations were adjusted to different levels (10 and 12% w/w) to fulfill the requirements for 3D printing. Rheological and textural properties, as well as release profiles, were significantly affected by the type and concentration of excipient regardless of theophylline doses used. The printing material should exhibit shear-thinning behavior, keeping yield stress less than 4000Pa and a loss factor (tanδ=G''/G') between 0.2 and 0.7, especially for 3D printing purposes using the current platform. The SEM images demonstrated that the hydrogel matrix exhibited a porous structure, which had the potential to encapsulate the theophylline clusters within its microstructure. The in vitro dissolution test showed that the release of all tablets was extended over 12h, and the calculation of drug release kinetic models revealed that the 3D printed HPMC matrices release the theophylline by diffusion and erosion mechanisms. The excipient HPMC K4M 12% w/w hydrogel was optimal to load the theophylline with flexible dosage combinations due to the great extrudability and shape retention ability. The exploration of rheological properties was investigated in this study, and the results revealed that it is a feasible method to predict the SSE 3D printability and quality of hydrogel-API blend materials for the drug delivery system.

Design, Characterization, and Application of a pH-Triggered In Situ Gel for Ocular Delivery of Vinpocetine.

We developed a pH-triggered in situ gel (ISG) for ocular delivery of vinpocetine to achieve systemic absorption and a brain-targeting effect in rats. Carbopol acted as a gelling agent combined with hydroxypropyl methylcellulose (HPMC) as a viscosity-enhancing agent. The concentration of Carbopol (0.2%, w/v) and HPMC (1.5%, w/v) was optimized for the ISG system. The optimized formulation was evaluated for studies on release in vitro, rheology, differential scanning calorimetry, ocular irritation, residence time, and in vivo pharmacokinetics. The vinpocetine ISG stayed longer in rabbit eyes than vinpocetine ointment. In vivo pharmacokinetics showed that compared with vinpocetine ointment, vinpocetine ISG attained a peak plasma concentration and area under the curve that was 1-2 folds greater in rat plasma. The Drug Targeting Index (DTI) was 1.06 and 1.26 for vinpocetine ointment and vinpocetine ISG, respectively, after ocular administration, showing that vinpocetine ISG had better distribution in rat brain. These results revealed that a pH-triggered ISG system via ocular administration could be an alternative approach compared with traditional ophthalmic formulations.

Transition from binder to matrix-forming: The effect of hydroxypropylmethylcellulose concentration on the properties of starch/hydroxypropylmethylcellulose granules prepared in a high shear granulator

The effects of the hydroxypropylmethylcellulose (HPMC) concentration and the operation parameters on the starch/HPMC granule properties prepared in a high shear granulator are investigated. At a lower concentration of 3.8% or 4.9%, HPMC acts as an intergranule binder. At a higher concentration of 7.2%, HPMC acts as an intragranule matrix-forming polymer. At the intermediate HPMC concentration of 6.1%, HPMC shows dual roles as a binder and as matrices. At the intermediate HPMC concentration, a new granule oscillating growth profile is observed. The impeller rotational speed has a more pronounced effect on the granule size distribution at the intermediate HPMC concentrations. The prepared granules are rounder and have narrow size distributions. The granules also show the highest compaction loading of 140 N and the highest tablet crushing force of 39.95 N.

A novel temperature-sensitive cationic hydrophobic cellulose ether: preparation and characterization

A temperature-sensitive polymer—hydroxyl isopropoxy triethyl ammonium chloride cellulose ether—was prepared from hydroxypropyl methyl cellulose (HPMC) and with epoxypropyl triethyl ammonium chloride as the hydrophobization reagent. Then, the reaction conditions of etherification reaction time, mass ratio of the etherifying agent to HPMC, molar ratio of alkali to etherifying agent, and concentration of HPMC were optimized. The structures of the products were characterized via nuclear magnetic resonance and infrared spectrum, and the temperature sensitivity was analyzed via ultraviolet spectrophotometry. It was found that the degree of substitution significantly affected the temperature sensitivity and lowest inversion temperature of the hydroxyl isopropoxy triethyl ammonium chloride cellulose ether. The effects of the substitution degree rising from 0.19 to 0.50 on the water retention value were explored. When the molar ratio of alkali to HPMC was constant, the water retention value declined with the increased substitution degree of cationic cellulose ether. The temperature rise of phase transformation in this process was fully reversible and nonhysteretic. Since the polymer variation originated from the change of intramolecular and intermolecular forces during the heating process, here the effects of addictive micromolecules on the regulator solution were further studied. As the NaOH concentration rose, the substitution degree and water retention value both first increased and then declined and both maximized at the NaOH concentration of 20.7%.

Comparative Two-Photon Fluorescence Microscopy Analysis of Riboflavin Penetration in Two Different Solutions: Dextran and Hydroxypropyl Methylcellulose.

PurposeThis study compared riboflavin penetration in porcine corneas using two different solutions: dextran and hydroxypropyl methylcellulose (HPMC).MethodsPorcine corneas were de-swollen and after prepared in an artificial anterior chamber with balanced saline solution. The pressure was checked with a portable tonometer. We used 0.1% riboflavin in 20% dextran for 30 min or 0.1% riboflavin in 1% HPMC for 10 min. The fluorescence intensity in multiphoton microscopy was used to evaluate concentration into the cornea, and ultrasonic pachymetry was performed before and after using riboflavin.ResultsRiboflavin concentration up to 340 μm was higher in the HPMC group (p 0.146). From 340 microns to 500 μm, the concentration was higher in the dextran group (p 0.248). There was no statistically significant difference between the groups when considering all the corneal thickness studied (p 0.528). Pachymetric measurements in the group with dextran showed a 12.9% corneal thickness decrease after 30 min, while the HPMC group showed a 9.1% increase after 10 min.ConclusionWe concluded that 1% HPMC riboflavin for 10 min had the same level of safety when compared to the Dresden protocol with dextran riboflavin for 30 min. Ultrasonic pachymetry during corneal crosslinking has fundamental importance in controlling corneal hydration due to changes in thickness caused by different types of riboflavin. This study used different methods than previous studies to better simulate corneal physiological conditions and used 1% HPMC concentration which differs from previous studies performed with 1.1% HPMC.

FORMULASI DAN UJI FISIK GEL EKSTRAK DAUN SALAM (Syzygium poliyantum (Wight) Walp) DENGAN GELLING AGENT HPMC (Hydroxypropyl Methylcellulose)

Nowdays, medical plants have been widely used for overcome health problem. One of the nutritious plants is Bay Plant (Syzygium poliyantum (Wight) Walp) which contains flavonoid active compound, saponin which contains flavonoid compounds, saponins, which are used as antibacterial. This study aims to determine the gel formulation and evaluation as well as the effect of differences in the concentration of HPMC (Hydroxypropyl Methylcellulose) on the physical properties og the gel. In this study used variations in the HPMC concentrations of 4%, 5% and 6% with bay leaf extract concentrations of 5%. Bay leaves extracted by maceration for 7 days, then will be remacerated for 2 days to find the compouds that were still left with 70% ethanol solvent. Gel evaluation includes organoleptic, spread power, adhesion, pH, homogeneity, and protection. The evaluation result showed that at a concentration of HPMC 4%, 5% and 6% each had a distinctive odor of bay leaf extract and brown colored in an organoleptic test, produced homogeneus preparations, had a pH value of 6,16; 5,82; and 5,73; spread power 6,2 cm; 5,8 cm; and 5,1 cm; Stickness 5,75 sec; 7,46 sec; and 9.35 sec; and protective power 6,57 sec; 6,87 sec; 6.89 sec. The results of pH test, spreadability, and stickness using Kruskal Wallis showed an Asymp.Sig < 0.05% that is 0.000, which indicates that there are significant difference between the concentration of HPMC with ph test, spreadability and stickness. The result of protective power test showed an Asymp.Sig > 0.05 that is 0.497 and there is no significant difference between the concentration of HPMC with the protective power. The result of testing all three formulas meet the requirements except for protective power.

HPMC-co-acrylic acid dexibuprofen once-daily oral hydrogels

The study aimed to synthesize dexibuprofen (DXIBN) solid dispersions (SDS)-loaded hydroxypropylmethylcellulose (HPMC) and co-acrylic acid (AA)-based oral hydrogels via a modest solvent evaporation technique. Free radical polymerization technique was used to prepare HPMC-co-AA hydrogels using EGDMA as cross-linker and ammonium per sulfate as initiator. SDS of DXIBN were prepared using Soluplus® (SLPS®) as a solubilizing agent. The solubility of pure DXIBN and the respective SDS was analyzed in phosphate buffer solutions (PBS) at varying pH (1.2, 6.8 and 7.4 pH) at temperatures (25 and 37 °C). The physiochemical characterizations: swelling analysis, diffusion co-efficient, porosity and sol-gel analysis, Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC), swelling behavior and release studies (at pH 1.2 and 7.4) were steered. The solubility was found to be significantly (p < .05) improved up to twofolds as compared to pure DXIBN. The hydrogels with higher concentrations of HPMC and AA showed significant (p < .05) increase in swelling, whereas there was a significant (p < .05) decrease with higher concentration of cross-linker EGDMA. The release kinetics applied trailed overall the non-Fickian release mechanism. The existing work exhibited was found to be improved DXIBN solubility using Soluplus via SDS technique and a stable HPMC-co-AA DXIBN release retardant hydrogel as an exceptional safer tool for the treatment of rheumatoid arthritis.

Oleogel Fabrication Based on Sodium Caseinate, Hydroxypropyl Methylcellulose, and Beeswax: Effect of Concentration, Oleogelation Method, and Their Optimization

AbstractIn the present study, the oleogel preparation with hydroxypropyl methylcellulose (HPMC) (0–2 g/100 g), sodium caseinate (CN) (0–4 g/100 g), beeswax (0–5 g/100 g), and oleogelation method (foam and emulsion template) was optimized using response surface methodology (RSM) to attain the desirable oil retaining ability, rheological, and textural characteristics. For all the chosen responses, the quadratic model was the best‐fitting model with a determination coefficient of R2 &gt; 0.91. Results exhibited that the HPMC and CN concentrations were the most influential tested factors on the oil binding capacity, textural, and rheological characteristics of the oleogels due to the formation of more complex and strong network. There was a significant improvement in oil binding capacity and structure recovery of samples by beeswax addition. To produce oleogel similar to industrial shortening, the optimization method was done based on maximum oil binding capacity and thixotropic recovery and other responses were chosen equal to those of shortening values (ɳa = 330 Pa.s, G′ = 276,543 Pa, A value = 164,308 Pa s rad−1, and firmness = 44.99 g). As regards the optimized level of structuring agents and responses (ɳa = 317 and 329 Pa.s, G′ = 249,782 and 260,997 Pa, A value = 180,022 and 180,373 Pa s rad−1, and firmness = 44.37 and 36.98 g corresponding to Optimization 1 and Optimization 2, respectively), fabrication of oleogels with at least 90 g/100 g trans‐free and low saturated oil and attributes close to industrial shortening is possible.

Investigation into hydroxypropyl-methylcellulose-reinforced polylactide composites for fused deposition modelling

Polylactide (PLA) is an aliphatic polyester biopolymer that can be derived from renewable agricultural products, such as corn, potatoes, rice, tapioca, and cane sugar. In this study, hydroxypropyl methylcellulose (HPMC)/PLA composite filaments with up to 7 % HPMC were prepared and used to produce parts via fused deposition modelling (FDM). The effect of the HPMC content on the microstructure, chemical structure, thermal properties, mechanical properties, and water contact angle (CA) was investigated. A uniform dispersion of HPMC within the PLA matrix was obtained. The incorporation of HPMC had no effect on the PLA chemical structure. Additionally, the cold crystallisation temperature decreased from 111 °C for the neat PLA filament to 104 °C for the composite filament with 7 % HPMC. The strengths of the composite filaments with 5 % and 7 % HPMC (51 MPa and 49 MPa, respectively) were maintained at a level comparable to that of their neat PLA counterpart (53 MPa). However, the tensile and impact strengths of the printed samples both decreased with the addition of HPMC, owing to the increased porosity. The hydrophilicity of the composites was significantly enhanced with the addition of HPMC, and the water contact angle of the sample with 7 % HPMC was reduced by approximately 30°.This work represents a step towards a simple but promising way to prepare biocompatible HPMC/PLA composites for FDM.

Formulasi Spray Gel Ekstrak Daun Pandan Wangi Sebagai Antiseptik Tangan

Spray gel as an alternative to hand washing soap. Pandan wangi leaves are efficacious as antiseptics. This study aimed to obtain a good formulation of spray gel pandan wangi leaves extract and efficacious as an antiseptic. The method used in this study was to compare the concentration of Hydroxypropyl methylcellulose (HPMC) on three formulas including 0,5%; 1,5%; and 2,5%. The formulas was tested for their physical properties to determine the best formula and will be tested for physical stability at room temperature (28 o ±2 o C) for 4 weeks and followed by testing the effectiveness of antibacterials. The result showed that formula I (0,5% HPMC concentration) was the best formula. This formula fulfills all the criteria for good physical properties. The formula I was stable at room temperature and has effectiveness against Staphylococcus aureus. This study is the basic experiment for development of spray gel prparations with active substances derived from natural ingredients Keywords : m spray gel, Pandanus amaryllifolius, Roxb. extract, anseptic

Formulation and In vitro Release Behavior of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Containing Poorly Soluble Fenofibrate

Fenofibrate, a water insoluble drug was used to prepare matrix tablet with four different viscosity grades of Hydroxypropyl Methylcellulose (HPMC) which were Methocel K4M CR, Methocel K15M CR, Methocel K100M CR and Methocel K100LV CR. The concentration of those excipients was 5, 10, 20, and 40% (w/w), respectively. The content of drug in a fixed quantity of powder in every formulation was ranged between 96.47 to 104.78 %. The dissolution study was done by using USP dissolution apparatus II. The kinetics of release was analyzed by using zero-order, first order, Korsmeyer-Peppas, Higuchi and Hixon-crowell equations to explain the drug release mechanism from the matrix tablets. In-vitro dissolution profile of matrix tablets were dependent upon the HPMC concentration and dissolution was rapid for tablets containing lower polymer proportion i.e. 5,10, and 20% Percentage (w/w) HPMC than those containing 40% (w/w) HPMC. Bangladesh Pharmaceutical Journal 23(1): 10-16, 2020

Formulation and Evaluation of Fast Dissolving Oral Films of Cetirizine Hydrochloride

Introduction: Fast-dissolving oral delivery system is a solid dosage form, which is used as a novel approach, as it dissolves rapidly in the mouth and directly reaches the systemic circulation. This facilitates rapid absorption and reduces first-pass effects. These films provide better utilization without the need to chew and do not require the need of water for administration. Fast-dissolving oral films might be useful in special patients like those with swallowing difficulties and in that in chemotherapy. This study was aimed to formulate and evaluate the fast dissolving oral films of Cetirizine Hydrochloride.&#x0D; Methods: Oral films of Cetirizine Hydrochloride were prepared using Hydroxy Propyl Methyl Cellulose (HPMC), Polyvinyl alcohol, glycerol, aspartame in different concentrations by the solvent casting method. Films were evaluated for different physical Films were subjected to USP dissolution studies.&#x0D; Results: The drug content of the nine formulations was found to be in the range as per Indian Pharmacopeia. In vitro release studies indicated 60-91% release within 30 min in the formulated oral films. The best release was found to be 91.58% of formulation F7, having a minimum concentration of HPMC alone as a polymer along with other common ingredients and minimum release was found to be 60.01% of formulation F1. Surface pH was found to be near to neutral (pH 7) which was good for buccal mucosa.&#x0D; Conclusion: Increasing the concentration of polymer (PVA and HPMC) while keeping the plasticizer ratio constant showed enhanced folding endurance. The dissolution rates were also increased with the increase in the concentration of the polymers. The high concentration of polymers decreased the release rate of cetirizine while a low concentration of polymers causes an increment in the release rate of cetirizine.

Development of a topical tissue cross-linking solution using sodium hydroxymethylglycinate (SMG): viscosity effect.

Hyperviscosity agents are commonly used in ophthalmic formulations for improving corneal drug penetration by increasing tissue contact time. One such viscosity agent is hydroxypropyl methylcellulose (HPMC). HPMC has been used in riboflavin solutions for photochemical UVA cross-linking (CXL). Sodium hydroxymethylglycinate (SMG) is a small molecule formaldehyde releaser that can function as a therapeutic tissue cross-linker for corneal and scleral applications. The present study was undertaken in order to study formulation factors using HPMC and SMG that could positively influence the cross-linking effect in these ocular tissues. Formulations containing 10 mM SMG and 100 mM sodium bicarbonate were prepared with varying HPMC concentrations from 0 to 4.4%. Their cross-linking effects on porcine and rabbit eyes were measured using differential scanning calorimetry (DSC), expressed as the change/difference in melting temperature (ΔTm) compared with the control. SMG in 4.4% HPMC solution resulted in ΔTm of 6.3 ± 1.21, while other concentration showed no differences in Tm shift on porcine cornea. In ex vivo rabbit cornea, there was a trend toward an increasing cross-linking effect with higher viscosity albeit mild differences. While a significant Tm shift was observed in porcine and rabbit sclera, there was no difference in effect of cross-linking between four HPMC concentrations. Increasing the HPMC concentration does not negatively affect the cross-linking efficacy attributed by SMG and could still be a positive cross-linking enhancer by virtue of increasing tissue contact time in a dynamic biological system. This information will be useful for planning further animal and human studies.

Physicochemical and antimicrobial properties of in situ crosslinked alginate/hydroxypropyl methylcellulose/ε‐polylysine films

ABSTRACTIn the present study, in situ crosslinked films were easily prepared by the spray deposition of Phase A, composed by sodium alginate (Alg), hydroxypropyl methylcellulose (HPMC), ε‐polylysine (ε‐PL), and plasticizers, followed by the spray deposition of Phase B (Ca2+ ions) on polystyrene dishes. The effect of the amount of plasticizer, HPMC, and ε‐PL in Phase A on the films properties was explored in a set of 12 systems. Fourier transform infrared vibrational spectroscopy in the attenuated total reflectance mode revealed that plasticizers compete with Ca2+ ions for complexation with Alg. Films with high HPMC content and low content of plasticizer and ε‐PL presented the best mechanical properties. The best system presented Young modulus of 0.76 ± 0.10 GPa, water vapor transmission of 5.35 ± 0.28 mg cm−2 h−1, swelling ratio of 1374 ± 97%, 99.99% reduction against Gram‐negative Escherichia coli bacteria, and 99.9% reduction against Gram‐positive Staphylococcus aureus bacteria. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020, 137, 48832.

Fabrication of Muco-Adhesive Oral Films by the 3D Printing of Hydroxypropyl Methylcellulose-Based Catechin-Loaded Formulations.

Pharmaceutical applications of three dimensional (3D) printing technology are increasing following the approval of 3D-printed tablets by the U.S. Food and Drug Administration. Semi-solid extrusion-type 3D printers are used to 3D print hydrogel- and paste-based materials. We previously developed tablet formulations for semi-solid extrusion-type 3D bioprinters. In the present study, we extended our study to the preparation of muco-adhesive oral film formulations to 3D bioprint mouth ulcer pharmaceuticals. We focused on hydroxypropyl methylcellulose (HPMC)-based catechin (model drug)-loaded hydrogel formulations and found that the viscosity of a hydrogel formulation is dependent on the HPMC concentration, and that viscosity is important for facile 3D printing. HPMC-based films were prepared using two different drying methods (air drying and freeze drying). The films exhibited different drug dissolution profiles, and increasing the amount of HPMC in the film delayed drug dissolution. The fabrication of HPMC-based catechin-loaded films with different shapes provides a model of individualized, on-demand pharmaceuticals. Our results support the flexible application of 3D bioprinters (semi-solid extrusion-type 3D printers) for preparing film formulations.

The Effect of Different Ratios of the Hydrophilic Polymers Sodium Al-ginate 20cP and Hydroxy Propyl Methyl Cellulose E15 on the Physicochemical Characteristics of Meloxicam Patch

Meloxicam is one of the Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) often used for osteoarthritis treatment. However, long-term use of meloxicam can cause side effects within the digestive tract, such as ulceration of the gastric mucosa. Transdermal patches offer an alternative route to reduce the side effects of meloxicam. This study aimed to determine the effect that different ratios of hydrophilic polymers had on the physicochemical characteristics of meloxicam patches. The hydrophilic polymers used were Sodium alginate 20 cP and Hydroxy Propyl Methyl Cellulose (HPMC) E15. Several comparisons were made between the hydrophobic polymer Ethyl Cellulose (EC) N22 including F1 (4:6:1), F2 (4,5:5:1,5), F3 (5:5:1) and F4 (5:4,5:1,5) which were made by a solvent evaporation method. Patches were then evaluated for their physicochemical properties, including organoleptic characteristics, moisture content, surface homogeneity, drug homogeneity, and assay testing. The results showed that increases in HPMC concentration can increase the results obtained. Based on statistical analysis results, no significant differences between the four formulas were found. In conclusion, a combination of HPMC E15, sodium alginate 20cP, and EC N22 with the most HPMC E15 produced the highest physicochemical characteristics.

Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline.&#x0D; Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.

Fast, Spectroscopy-Based Prediction of In Vitro Dissolution Profile of Extended Release Tablets Using Artificial Neural Networks.

The pharmaceutical industry has never seen such a vast development in process analytical methods as in the last decade. The application of near-infrared (NIR) and Raman spectroscopy in monitoring production lines has also become widespread. This work aims to utilize the large amount of information collected by these methods by building an artificial neural network (ANN) model that can predict the dissolution profile of the scanned tablets. An extended release formulation containing drotaverine (DR) as a model drug was developed and tablets were produced with 37 different settings, with the variables being the DR content, the hydroxypropyl methylcellulose (HPMC) content and compression force. NIR and Raman spectra of the tablets were recorded in both the transmission and reflection method. The spectra were used to build a partial least squares prediction model for the DR and HPMC content. The ANN model used these predicted values, along with the measured compression force, as input data. It was found that models based on both NIR and Raman spectra were capable of predicting the dissolution profile of the test tablets within the acceptance limit of the f2 difference factor. The performance of these ANN models was compared to PLS models using the same data as input, and the prediction of the ANN models was found to be more accurate. The proposed method accomplishes the prediction of the dissolution profile of extended release tablets using either NIR or Raman spectra.

FORMULATION DEVELOPMENT AND EVALUATION OF SUSTAINED RELEASE GASTRORETENTIVE TABLET OF EMTRICITABINE

Objective: The study aims for the design and evaluation of floating tablets of emtricitabine (EMT), post oral administration to sustain the release and enhance gastric residence time (GRT).&#x0D; Methods: EMT is a nucleoside reverse-transcriptase inhibitor for the prevention and treatment of human immunodeficiency virus (HIV) infection. The investigation was considered to formulate a floating tablet of EMT with various agents. The formulation included with various concentrations of hydroxypropyl methylcellulose (HPMC) k4m, ethylcellulose, microcrystalline cellulose, polyvinylpyrrolidone (PVP) by wet granulation method. Various parameters for the prepared formulations were evaluated for weight variation, thickness, hardness, friability, floating lag time (FLT), total floating time (TFT), swelling index, in vitro drug release, and fourier-transform infrared spectroscopy (FTIR) studies.&#x0D; Results: The best formulation F1 exhibited 88.28% release in 24 h duration, with a floating lag time of 7 min and swelling index of 52.1% and drug content was determined to be 98.27%. The release mechanism was determined to be first order with higuchi release kinetics displaying diffusion along with the dissolution of the EMT from the tablet by non fickian mechanism.&#x0D; Conclusion: EMT tablets showed an increased GRT with a sustained release for 24 h thereby allowing a better window for absorption consequently improve the therapeutic effect of the drug.

Development of sorafenib loaded nanoparticles to improve oral bioavailability using a quality by design approach

Sorafenib, a potent anticancer drug, has low absorption in the gastrointestinal tract due to its poor aqueous solubility. The main purpose of this investigation was to design sorafenib nanoparticle using a newly developed technique, nanoparticulation using fat and supercritical fluid (NUFS™) to improve the absorption of sorafenib. The quality by design (QbD) tool was adopted to define the optimal formulation variables: hydroxypropyl methyl cellulose (HPMC), polyvinyl pyrrolidone K30 (PVP), and poloxamer. The studied response variables were particle size of nanoparticle, dissolution (5, 60, and 180 min), drug concentration time profile of nanoparticle formulations, and maximum drug concentration. The result of particle size revealed that an increase in concentration of poloxamer and HPMC decreased the particle size of nanoparticles (p < 0.05). Likewise, the concentration of drug release at different time point (5, 60, and 180 min) showed HPMC and poloxamer had positive effects on drug dissolution while PVP had negative effects on it. The design space was built in accordance with the particle size of nanoparticle (target < 500 nm) and dissolution of sorafenib (target > 7 µm/mL), following failure probability analysis using Monte Carlo simulations. In vivo pharmacokinetics studies in beagle dogs demonstrated that optimized formulation of sorafenib (F3 and F4 tablets) exhibited higher blood drug profiles indicating better absorption compared to the reference tablet (Nexavar®). In conclusion, this study showed the importance of systematic formulation design for understanding the effect of formulation variables on the characteristics of nanoparticles of the poorly soluble drug.