Avicel PH Research Articles

Material-Sparing and Expedited Development of a Tablet Formulation of Carbamazepine Glutaric Acid Cocrystal- a QbD Approach.

To efficiently develop a tablet formulation of carbamazepine using a soluble cocrystal with excess coformer to maintain phase stability during dissolution. The carbamazepine - glutaric acid cocrystal (CBZ-GLA, 1:1) and excess glutaric acid (GLA) were mixed with suitable tablet excipients, which were selected to address powder flowability and tabletability deficiencies specifically. Tablet friability and dissolution profiles were evaluated to guide formulation optimization. Dry granules were prepared by milling simulated ribbons. A binary blend of CBZ-GLA and GLA had poor flowability and marginal tabletability. Therefore, silica coated Avicel PH-102 (sMCC) was applied as a binder to improve the flow property and tabletability. A formulation consisting of sMCC, CBZ-GLA, and GLA exhibited good manufacturability but did not show improved dissolution because of rapid precipitation of CBZ dihydrate when CBZ-GLA came in contact with water. Dry granulation of CBZ-GLA and GLA dramatically improved dissolution profile due to the intimate contact between CBZ-GLA and GLA. Such cocrystal - coformer granules also led to much improved tablet manufacturability and dissolution. The successful tablet development of CBZ-GLA, using < 3 g of the cocrystal in <3 weeks, demonstrates an efficient workflow for tablet formulation development based on material-sparing and predictive powder characterization techniques. This workflow is useful for early tablet development using enabling solid form, such as cocrystal, when only a small amount of material is available.

Optimasi Formula Tablet Piroksikam Menggunakan Eksipien Laktosa, Avicel pH-101, dan Amprotab dengan Metode Simplex Lattice Design

Piroxicam solubility in water is very small this cause problem in the process of absorption so that it’s required an optimal formula to establish the physical properties of tablet quality for piroxicam tablets. The purpose of this research was creating formulas with the optimal combination of excipients lactose, Avicel pH 101, and piroxicam amprotab to obtain tablets with good physical properties and disolution. Seven piroxicam tablet formulas were made with a combination of lactose, avicel PH-101, and Amprotab on 2 batches. Method for making tablets piroxicam was established by direct compression. Tests included were the physical properties of piroxicam tablets tablets weight uniformity, uniformity of size, hardness, brittleness, disintegration test, as well as dissolution test, and content uniformity. Based on the simplex lattice design method, lactose is a dominant factor to improved the uniformity of tablet’s concentartions. Interaction of two components avicel PH-101 and amprotab is a dominant factor to reduced vulnerability. Interaction of three components lactose, avicel PH-101 and amprotab is a dominant factor to lowered the value coefisien variation of weight uniformity, increased hardness, decreased the disintegration, and improved dissolution of tablets. Selection of the optimum formula was determined by the method of simplex lattice design through diagrams superimposed contour plots and contour plots for obtaining the optimal proportions of each ingredient as follows: lactose (85,154–100%), avicel PH-101 (0–12,437%), and amprotab (0–5,425%).

INFLUENCE OF CELLULOSE AND ACETATE-BASED POLYMERS ON THE RELEASE OF CIPROFLOXACIN HCL FROM EXTENDED RELEASE MATRIX TABLETS PREPARED BY DIRECT COMPRESSION TECHNIQUE

The objectives of the current study were to investigate the influence of different types and concentration of polymers on release of ciprofloxacin HCl as well as to formulate an extended release tablets of ciprofloxacin hydrochloride by direct compression method. Twelve formulations (F1–F12) were manually designed using different proportions (10–30%) of Hydroxypropyl methylcellulose (HPMC), Ethylcellulose (EC) and Kollidon SR polymers. Avicel PH101, talc and magnesium stearate were used in a constant quantity of 2% in all the formulations. Multiple point dissolution was carried out in different media. Dissolution profiles indicated that formulations F1, F4, F8 and F11, extended the drug release up to 12 hrs, while, other formulations failed to retard the drug release up to desired period. DDSolver software was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Korsmeyer–Peppas and Higuchi models. Drug polymers compatibility was assessed using Fourier Transformed Infrared (FTIR) spectroscopy. Selected formulations were placed in the stability chamber at accelerated temperature (40±2°C and RH 75±5%) for six months and re-evaluated after 3 and 6 months as per ICH guidelines. The present study accomplished that ethylcellulose alone or in combination with HPMC was found to be an excellent rate controlling agent for ciprofloxacin and may be used successfully to develop extended release tablet formulations.

Formulasi dan Evaluasi Sediaan Tablet Nanopartikel Ekstrak Daun Salam (Syzygium Polyanthum) dengan Variasi Konsentrasi Na Alginat dan Avicel PH 102

The use of traditional medicines is an alternative treatment which is considered safer in terms of side effects and toxicity. One of the herbal plants that have properties that can reduce blood pressure is bay leaf (Syzigium polyanthum) because it contains essential oils (citral, eugenol), tannin, and flavonoids. Ethanol extract of bay leaves (Syzigium polyanthum) with antihypertensive potential needs to be made into dosage forms. This study aimed to determine the optimal formula of the preparation of bay leaf (Syzigium polyanthum) nanoparticles tablet with variations in the concentration of Na alginate and Avicel PH 102. Salam leaf extract was made using maceration method using ethanol 96%, followed by evaporation until thick extract was formed. Colloidal nanoparticles were prepared by mixing bay leaf extract into technical ethanol 96% and aquadest, chitosan solution in acetic acid and NaTTP solution. Further, it was measured using PSA (Particle Size Analyzer) to determine the particle size. Tablets were prepared using 4 formulas with variations in the concentration of sodium alginate and avicel PH 102 using the direct pressing method. The results of this study indicate that variations in the concentration of Na alginate and Avicel PH 102 affect the physical properties of tablets. The addition of Avicel PH 102 can increase the hardness and disintegration time of the tablet. While the addition of Na alginate can increase the fragility of tablets. Based on the evaluation results, the optimum formulation of tablet formulas is formula 4.

Fine grade engineered microcrystalline cellulose excipients for direct compaction: Assessing suitability of different dry coating processes

Recent work showed that contrary to conventional wisdom, fine surface engineered excipients outperform their larger counterparts in blends of highly loaded blends of cohesive drug powders in terms of their packing, flowability and tablet tensile strength. Here, two continuous devices, fluid-energy mill (FEM) and conical mill (Comil), are compared with LabRAM, a batch device used in previous work, for nano-silica dry coating of microcrystalline cellulose (MCC) excipients, 20 and 30 μm. Coated MCCs from all three devices had higher bulk densities and flow function coefficients (FFCs) compared with Avicel PH-102. Silica coating quality was best with LabRAM, but also good with FEM and Comil, although Comil was less effective for the finer MCC. However, the better coating quality of LabRAM had a downside of having poorer compaction properties. The most surprising outcome was that multi-component blends of 17 wt% coated MCC with 60 wt % Ibuprofen 50 had higher bulk density, higher or similar flowability, higher tablet tensile strength, and comparable Ibuprofen dissolution from tablets, compared to those with Prosolv 50, a silicified excipient. The FEM dry coated MCC blends, having only 0.17 wt% silica, performed the best, having desirable bulk density, FFC, and tensile strength that could facilitate high-speed direct compression tableting. In summary, considering that achieving best coating quality need not be the primary objective, FEM may be the best option for producing desired sized dry coated fine excipients.

Production of Micro Crystalline Cellulose from Tapioca Solid Waste: Effect of Acid Concentration on its Physico-chemical Properties

This study was aimed to examine the production of microcrystalline cellulose (MCC) from tapioca solid waste (TSW), using HCl hydrolysis with various concentrations, i.e., 2 N, 2.5 N, 3 N, and 3.5 N. MCC was produced by delignifying the TSW with NaOH 20%, and bleaching with NaOCl 3.5% to produce α-cellulose, and subsequently hydrolyzing α-cellulose with three different HCl concentrations to produce MCC. The physicochemical properties of MCC were then analyzed, including Scanning Electron Micrograph (SEM), X-ray diffraction (XRD), and FTIR spectra. The results showed that hydrolysis with 2.0 N HCl resulted in a higher yield of 61.28%, α-cellulose content of 56.33%, moisture 6.25%, pH of 6.54; ash 0.23%, and water solubility 0.34%. SEM analysis showed the morphology and size of the MCC produced were like those of a commercial MCC (Avicel PH101), while the XRD analysis showed the higher concentration of HCl gave rise to an increased crystalline index. FT-IR spectrum analysis indicated that TSW, MCC produced, and commercial MCC had similar functional groups.

Colon targeted bioadhesive pellets of curcumin and cyclosporine for improved management of inflammatory bowel disease.

The objective of the present work was to develop and optimize multiparticulate pH-dependent bioadhesive pellets of curcumin and cyclosporine for the management of intestinal bowel disease (IBD). The bioadhesive sustained release pellets were intended for targeting the affected site for an improved therapeutic effect. Bioadhesive pellet cores of curcumin and cyclosporine were formulated using Carbopol 940 (CP940) and hydroxypropyl cellulose (HPC-H) by the extrusion/spheronization method, and drug delivery to the colon was controlled by the pH-sensitive polymer Eudragit® S100. Microcrystalline cellulose (Avicel PH101) was found to be the best forming agent for pellet core. The ratio of CP940 to HPC-H was kept at 1:1 to achieve 100% bioadhesion. The in vitro dissolution profiles of coated pellets depicted that 12.327 ± 0.342% of curcumin and 14.751 ± 0.112% of cyclosporine were released at the end of 6h (at pH6.8), whereas 71.278 ± 0.100% of curcumin and 76.76 ± 0.195% of cyclosporine were released at the end of 24h (at pH7.4). The drug release profile was found to follow zero-order kinetics for both drugs. The selected formulation was evaluated on an acetic acid-induced ulcerative colitis in the rat model to evaluate the efficiency of drug-loaded pellets coated with Eudragit®S100. The pharmacodynamic study revealed the therapeutic efficacy of Eudragit®S100-coated pellets of curcumin and cyclosporine in alleviating the conditions of the acetic acid-induced colitis model as reflected by weight gain as well as improvement of clinical, macroscopic and microscopic parameters of induced colitis, as compared with free curcumin and cyclosporine. The combination of curcumin and cyclosporine has been proven to have a synergistic effect for the successful management of IBD when used in a low dose as compared with individual drugs with high doses. Hence, curcumin- and cyclosporine-loaded bioadhesive pellets may act as a promising targeted drug delivery system in the management of IBD. Graphical abstract.

Formulation and evaluation of self nano-emulsifying drug delivery system of ezetimibe for dissolution rate enhancement

The present study was aimed to develop a Self Nano Emulsifying Delivery System of Ezetimibe (EZM) for enhancing its dissolution rate. Ezetimibe is a cholesterol absorption inhibitor, being a lipophilic drug due to its low solubility EZM shows a low dissolution profile. The SNEDDS formulation consisted of excipients Cinnamon oil, Tween 80, PEG 400 as the Oil, Surfactant and Co-surfactant. Twelve formulations with different ratios of Oil, Surfactant and Co-surfactant were prepared. The liquid SNEDDS were then converted into Solid form by adsorption technique using Avicel PH 101 and Aerosil 200 as adsorbents. The liquid SNEDDS was characterised for Particle size, Emulsification time, Dispersibility, percentage transmittance, PCM, Centrifugation, Cloud Point and Freeze thaw cycle. The solid form was characterized for the flow property, SEM, Drug content and in-vitro dissolution. Among the twelve formulations F6 formulation was found to have a particle size of 196 nm and PDI of 0.123. F6 formulation was selected as the best and it was made into solid by adsorption onto solid carriers. The F6 formulation consisted of the 25% Cinnamon oil, 50% tween 80 and 25% PEG 400. The in-vitro dissolution rate of the prepared formulation was compared with the marketed formulation. The in-vitro dissolution data showed that the drug release at the end of 60 mins from marketed formulation was 63.75 % and from SNEDDS formulation was 90.62 %. The dissolution rate of the prepared SNEDDS was increased by 1.42 times than the marketed formulation. The increase in the dissolution rate shows that SNEDDS is a suitable drug delivery system to enhance the rate of dissolution of Ezetimibe.

DISSOLUTION ENHANCEMENT AND FORMULATION OF FILM COATED TABLETS OF LORNOXICAM BY PHASE TRANSITION METHOD: IN VITRO AND IN VIVO EVALUATION

Objective: This study aimed to enhance the oral solubility and dissolution of poorly soluble lornoxicam by anti-solvent precipitation, and the manufacture of oral tablets by the phase transition method. &#x0D; Methods: The solvent was mixture of polyethylene glycol 400 and absolute ethanol. Three stabilizers Inutec SP1, Pluronic F127, Sucrose ester S1670 at two concentrations and two matrix formers Mannitol, and Avicel PH102 were used to obtain 12 formulae. The formulae were characterized regarding their infrared spectroscopy (IR), differential scanning calorimetry (DSC), particle size (PS) measurement, drug content and dissolution. Further characterizations were done for the optimum formula by scanning electron microscopy (SEM) and X-ray diffraction (XRD). Four tablet formulae were manufactured by phase transition method. The optimum tablets (T3) were evaluated through hardness, drug content, disintegration, dissolution, IR, and stability studies. Finally, (T3) was compared to conventional tablets in New Zealand rabbits using crossover design.&#x0D; Results: The dissolution rate for the prepared formulae was enhanced, from 3.44 to 5.96 folds. Statistical significance was obtained using one and two way ANOVA among formulae. The optimum tablet formula (T3) had hardness 5.637±1.57 kg, drug content 90.424±1.19%, disintegration time 341.5±9.62 s and the drug dissolved 72.107±0.0025%. Stability, after one month storage of the selected tablets at (25 °c/60% relative humidity), was satisfactory. The absorption extent of lornoxicam from (T3) compared to the conventional tablets was higher.&#x0D; Conclusion: Taken together, the obtained results confirmed successfully the potential of the promising formula (T3), over the conventional tablets of lornoxicam.

INFLUENCE OF CELLULOSE AND ACETATE-BASED POLYMERS ON THE RELEASE OF CIPROFLOXACIN HCL FROM EXTENDED RELEASE MATRIX TABLETS PREPARED BY DIRECT COMPRESSION TECHNIQUE

The objectives of the current study were to investigate the influence of different types and concentration of polymers on release of ciprofloxacin HCl as well as to formulate an extended release tablets of ciprofloxacin hydrochloride by direct compression method. Twelve formulations (F1–F12) were manually designed using different proportions (10–30%) of Hydroxypropyl methylcellulose (HPMC), Ethylcellulose (EC) and Kollidon SR polymers. Avicel PH101, talc and magnesium stearate were used in a constant quantity of 2% in all the formulations. Multiple point dissolution was carried out in different media. Dissolution profiles indicated that formulations F1, F4, F8 and F11, extended the drug release up to 12 hrs, while, other formulations failed to retard the drug release up to desired period. DDSolver software was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Korsmeyer–Peppas and Higuchi models. Drug polymers compatibility was assessed using Fourier Transformed Infrared (FTIR) spectroscopy. Selected formulations were placed in the stability chamber at accelerated temperature (40±2°C and RH 75±5%) for six months and re-evaluated after 3 and 6 months as per ICH guidelines. The present study accomplished that ethylcellulose alone or in combination with HPMC was found to be an excellent rate controlling agent for ciprofloxacin and may be used successfully to develop extended release tablet formulations.

Aceclofenac fast dispersible tablet formulations: Effect of different concentration levels of Avicel PH102 on the compactional, mechanical and drug release characteristics

The objective of this study was based on the formulation development of fast dispersible Aceclofenac tablets (100 mg) and to evaluate the influence of pharmaceutical mixtures of directly compressible Avicel PH102 with Mannitol and Ac-di-sol on the compressional, mechanical characteristics and drug release properties. Fast dispersible Aceclofenac formulations were developed by central composite design (CCD). Among them the best possible formulation was selected on the basis of micromeritic properties, appropriate tablet weight and disintegration time for further study. Tablets were directly compressed using manual hydraulic press with a compressional force ranging from 7.2 to 77.2 MN/m2. Pre and post compression studies were performed and the compressed formulations (FA-FF) were assessed for different quality tests. The Heckel and Kawakita equations were applied for determination of compressional behavior of formulations. The quality attributes suggested that formulation (FB) containing avicel PH 102 (20%), mannitol (25%) and ac-di-sol (3%) as best optimized formulation showing better mechanical strength i.e. hardness 35.40 ± 6.93N, tensile strength 0.963 MN/m2, and friability 0.68%. Furthermore, compressional analysis of FB showed lowest PY value 59.520 MN/m2 and Pk value 1.040 MN/m2 indicating plasticity of the material. Formulation FB disintegrated rapidly within 21 seconds and released 99.92% drug after 45 min in phosphate buffer pH 6.8. Results of drug release kinetics showed that all formulations followed Weibull and First-order models in three different dissolution media. Avicel PH102 based formulation mixture exhibit excellent compactional strength with rapid disintegration and quick drug release.

CHARACTERIZATION OF KAPOK PERICARPIUM MICROCRYSTALLINE CELLULOSE PRODUCED OF ENZYMATIC HYDROLYSIS USING PURIFIED CELLULASE FROM TERMITE (MACROTERMES GILVUS)

Objective: This study aimed to increase the yield of microcrystalline cellulose (MCC) from kapok pericarpium alpha-cellulose produced by enzymatic hydrolysis using purified cellulase from Termites (Macrotermes gilvus) and to compare the characteristics with the reference product.&#x0D; Methods: In this research, MCC was prepared from kapok pericarpium powder through the chemical isolation process of alpha-cellulose, followed by enzymatic hydrolysis with purified cellulase from Macrotermes gilvus. The yield was improved by using purified cellulase in optimized temperature, pH, and hydrolysis time. Identification was carried out by using ZnCl and infrared spectrophotometry, followed by characterization of MCC include particle size analysis (PSA) and diffracto­gram pattern (X-Ray Diffraction). The results were compared with Avicel PH 101 as the reference product.&#x0D; Results: Purified cellulase from Macrotermes gilvus showed high cellulose activity. Cellulose in the concentration of 11.743 U/ml formed 49 mm clear zone area with cellulolytic index 7.16 that similar to the formed clear zone area of Trichoderma reesei (50 mm), the optimum hydrolysis condition was achieved at 50 °C, pH 6.0, in 2 h, which produced 80% yield of MCC. Produced MCC was analyzed with ZnCl and FTIR spectrum resulting in positive results, similar to reference. The results of the organoleptic test, particle size analysis, and diffracto­gram pattern (X-Ray Diffraction) showed crystalline characteristics of MCC is similar to the reference (Avicel PH 101).&#x0D; Conclusion: Cellulase Macrotermes gilvus yielded 80% MCC and higher enzymatic activity than Trichoderma reesei. Based on the organoleptic test, particle size analysis, and diffracto­gram pattern observation, MCC from kapok pericarpium has shown similar characteristics to reference (Avicel pH 101) and might be potential to be further developed.

Mesoporous silica pellets – A promising oral drug delivery system?

In this study we investigated the application potential of ordered mesoporous silica SBA-15 powders as an excipient in development of prolonged release pellets for doxycycline.The doxycycline adsorption onto the SBA-15 powders was performed using adsorption from a concentrated solution. The pellets were obtained via wet granulation, extrusion and spheronization method. The pellets were composed of drug-loaded SBA-15, microcrystalline cellulose (Avicel PH 101), ethylcellulose (22 cP) and magnesium stearate. The 5 wt% polyvinylpyrrolidone (PVP K30) ethanolic solution (96% v/v) was used as a binder. The yield, drug content, size analysis, hardness, friability, disintegration time and pharmaceutical availability tests were carried out. The classic doxycycline pellets based on microcrystalline cellulose were prepared and investigated in the same manner for comparative purposes.The SBA-15 powders were characterized by efficient adsorption of doxycycline (103.5 ± 3.1 mg/g equal to 9.4% drug loading). The SBA-15 pellets were successfully obtained in laboratory scale. The prolonged 12 h drug release in phosphate buffer solution (pH = 6.8) was observed for SBA-15 pellets which was 2 times longer compared to drug release profile of microcrystalline cellulose-based pellets. The obtained mesoporous silica pellets may represent a novel solution in the development of prolonged release formulations for water soluble drugs.

FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLET OF MELOXICAM USING NATURAL SUPERDISINTEGRANTS

Objective: The objective of the present work was the preparation and evaluation of mouth dissolving tablets (MDTs) of meloxicam using natural superdisintegrants.&#x0D; Methods: Meloxicam is BCS Class II (low soluble, and high permeable) drug increasing the dissolution properties of the poorly water-soluble drug meloxicam using a solid dispersion method (solvent evaporation method). Solvent evaporation method using drug and carrier as polyethylene glycol (PEG)-6000 and PEG-15,000 the ratio of 1:1, 1:2 (drug:carrier), and acetone as solvent. In house prepared banana powder were used as natural superdisintegrant. Manufacturing of MDT was done by the direct compression method. In this MDTs, various excipients were used such as mannitol used as the diluent, sodium saccharin used as a sweetening agent, Avicel pH-102 used as a binding agent, and talc and sodium lauryl sulfate (SLS) used as lubricant and glidant. The best formula of the tablet was selected according to the disintegration time (DT) and friability tests.&#x0D; Results: The results have shown that an increase in the meloxicam solubility was obtained using solid dispersion with the solvent evaporation method using PEG-15000 as a carrier in the ratio of 1:2 (drug:carrier). Taste masking was also done by a solid dispersion method. Tablet prepared with in house prepared banana powder gave less DT (70 s) as compared to tablet prepared with branded banana powder (80 s), but formulation F5 failed in friability testing. Improved strength of tablet obtained using SLS (&lt;1%) also showed an increase in the dissolution performance of the tablet in formulation F6. This F6 formulation having 10% natural super disintegrating agent (in house prepared banana powder) has shown 99% cumulative drug release within 18 min. It also passed the friability test.&#x0D; Conclusion: Accordingly, the solubility of meloxicam was successfully enhanced through solid dispersion with carrier PEG-15,000 and formulated as a MDT to improve its oral absorption. PEG has also been used as a taste masking agent in these formulations. It was concluded that in house banana powder had excellent DT as compared to branded banana powder. Banana powder is “economical” and “easily available” than other commonly used synthetic superdisintegrants. The process of banana powder preparation is eco friendly. The meloxicam MDT formulated with natural superdisintegrant in house prepared banana powder found to pass all pharmacopeial tests.

Preparation of Microcrystalline Cellulose from Cotton Yarn Spinning Mills Wastes: Effect of Pretreatment and Hydrolysis Reaction Condition on the Product Characteristics

Cotton wastes from cotton yarn spinning mills has been utilized as an alternative resource for the production of Microcrystalline Cellulose (MCC), an important ingredient in food, cosmetic, pharmaceutical industries, etc. The main processes conducted including cotton wastes sorting, cotton lint pretreatment, and alpha cellulose hydrolysis. In this study, several parameters on pretreatment and hydrolysis were varied in order to produce MCC which characteristics were evaluated comparing to Avicel PH-101, a commercial MCC product. Pretreatment was carried out using 17.5% alkali (w/v) at temperature 80°C for 30 minutes, followed by a bleaching process at 5-30% H2O2 (v/v). The hydrolysis reaction was done using 1.25 M sulfuric acid, at temperature 80°C and 96°C for 2-4 hours. Results showed that pretreatment process with alkali for 30 minutes followed by a bleaching process with 5% H2O2 (v/v) was able to isolate 87% alpha cellulose with 99.98% of purity. The yields of MCC powders produced from acid hydrolysis of alpha cellulose at 96°C for 2, 3, and 4 hours were 74.6%, 70.2%, and 42.8%, respectively. According to the SEM, infrared spectra, and XRD results, the process conducted was applicable to produce MCC that physically and chemically similar to the characteristics of Avicel PH-101.

Development, evaluation and optimization of solid self emulsifying drug delivery system (s-sedds) of lercanidipine hydrochloride

The objective of the study is to formulate Solid Self Emulsifying Drug Delivery System (SEDDS) for improvement of solubility and dissolution of poorly water-soluble drug Lercanidipine Hydrochloride which has very less water solubility (0.000165mg/mL) and absolute bioavailability of 10%. The Liquid Self Emulsifying Drug Delivery System concentrate was prepared using different oils, surfactants and cosurfactants which were screened based on saturation solubility studies. The SEDDS prepared using oil like peppermint oil, surfactant as propylene glycol, cosurfactant as PEG 400 showed very good self-emulsification property. The prepared SEDDS were subjected for evaluation of various parameters like self-emulsification property, FTIR studies, DSC studies, viscosity, globule size determination, zeta potential determination, robustness to dilution, thermodynamic stability studies. Liquid SEDDS showed good emulsification with globule size 357.2 nm and PDI 0.491. The optimized SEDDS formulation with 20% peppermint oil, 7% propylene glycol surfactant, 63% PEG 400 cosurfactant and 10% drug was used for the preparation of Solid SEDDS following physical adsorbent technique using Avicel PH 101 as an inert solid adsorbent in 1:4 ratio. The prepared solid SEDDS with free-flowing property were compressed as tablets and evaluated for hardness, friability, drug content, disintegration and dissolution studies. The results of our study conclude that the Avicel PH 101 can be used for the preparation of solid SEDDS to improve the solubility and dissolution of poorly water-soluble drug Lercanidipine Hydrochloride.

Formulation and Evaluation of Acetazolamide Tablet by Liquisolid Technique

A novel concept of liquisolid technique is where a liquid is converted to dry flow able and compressible powder by mixing with appropriate carrier and coating material. Improved in-vitro dissolution property of partially soluble Acetazolamide was explored by possible liquisolid technique. Liquisolid formulations were prepared by suspending Acetazolamide in PEG 400Tween 80propylene glycol with Avicel PH 102 and HPMC K4M Aerosil 200 and Sodium starch glycolateas carrier coating material and disintegrating agent respectively. Drug excipients interactions were studied by FT-IR Spetroscopy. Solubility of the drug in the solvent was determined as showed PEG400 86.4mgmlPG 66.6mgml and Tween 8034.2mgml. Disintegration between 80 ndash 95 Sec. Dissolution profile percentage of F1 98.21 within 20 min showed is better than the formulations prepared by direct compression which increased surface area and wetting properties through liquisolid method. Itrsquos a determinative move to improve dissolution by liquisolid method of partially water soluble drug

Effect of Oily Ingredients and Solid Adsorbents on the Chemical Stability of a Solid Dosage Form of Lubiprostone

Lubiprostone (LPT), a novel laxative, is commercially available as a soft gelatin capsule with oily ingredient, complementing its poor water‐solubility and oxygen‐labile property. In the present study, in order to address drawbacks associated with soft capsule formulations such as difficulty in process control or high production costs, conversion of the drug‐loaded oil solution into powder dosage form was attempted using several oily ingredients and porous solid carriers. Drug solubilization in medium chain triglycerides (MCT) drastically improved the drug stability compared to that in powder or other oily ingredients, exhibiting over 95% of the drug remaining after 5 days of storage at 60 °C. However, conversion of drug‐loaded MCT into a free‐flowing powder using porous carriers markedly deteriorated drug stability. Although the drug stability in the solidified formulations prepared using Avicel PH 102 or Aerosil 200 were relatively higher than those prepared using metallic adsorbents (Florite, DCP A/T, and Neusilin US2), they were less stable than in the intact oil solution under stress and accelerated condition. This implied that the decreased thickness of the oily barrier in the solidified formula failed to inhibit the exposure of the labile compound to oxygen and/or moisture, thereby accelerating drug degradation. In vitro drug release from the adsorbent progressed rapidly, providing complete drug release within 15 min, under sink condition. This study suggests that the kind of oily vehicle and the thickness of the barrier are important factors for ensuring the stability of LPT, an oxygen‐labile compound, and additional pharmaceutical approaches are required for the construction of stable solid preparations.

New Formulation Technique for Solubility and Dissolution Rate Enhancement of Poorly Soluble Drugs

Ebastine (EBS) is a second-generation non-sedating antihistamine used for the prevention and treatment of allergic rhinitis and chronic idiopathic urticaria. It is BCS class II drug exhibiting low aqueous solubility and poor oral bioavailability. The present work was aimed at enhancing the dissolution rate of EBS by formulating it in the form of a liquisolid (LS) system using Tween 20 (non-volatile solvent), Avicel PH 102 (carrier material) and Aerosil 200 (coating material). Various batches of LS powder system were formulated by adopting a mathematical model for calculating required quantities of excipients. The absence of interaction between drug and excipients was checked by Fourier transform IR spectroscopy and differential scanning calorimetry studies. Formulated EBS tablets were evaluated for post compression parameters. X-ray powder diffraction studies and scanning electron microscopy showed the loss of EBS crystallinity in LS formulations. Formulation F9 was considered as optimum, showing a higher drug release of up to 99.06% in comparison to marketed tablet formulations. Stability of the optimized formulation was confirmed by results of the accelerated aging study. Thus, it is concluded that LS formulation is a favorable method of EBS solubility enhancement.

Effects of Surfactants on Itraconazole-Hydroxypropyl Methylcellulose Acetate Succinate Solid Dispersion Prepared by Hot Melt Extrusion III: Tableting of Extrudates and Drug Release From Tablets

Hydroxypropyl methylcellulose acetate succinate (HPMCAS) has gained popularity as a carrier for amorphous solid dispersion because of its ability to maintain drugs in supersaturated state after dissolution in aqueous media. In part I and II of this series of articles, we have demonstrated that amorphous solid dispersions containing HPMCAS may be prepared using surfactants as plasticizers to reduce processing temperature (Solanki et al., J Pharm Sci. 2019; 108:1453-65), where surfactants also increase dissolution rate and degree of supersaturation (Solanki et al., J Pharm Sci. 2019; 108: 3063-73). The present investigation was undertaken to develop melt extrudates of itraconazole-HPMCAS and itraconazole-surfactant-HPMCAS mixtures into tablets having tensile strength ≥2 MPa, where poloxamer 407 and d-α-tocopherol polyethylene glycol 1000 succinate were used as surfactants. Milled filaments were sieved to collect <212-μm particles, which were then compressed into tablets with different excipients (silicified microcrystalline cellulose [MCC], Avicel PH-102, dicalcium phosphate, lactose, and Starch 1500). Initial screening of various diluents showed that only silicified MCC and Avicel PH-102 could provide the target tensile strength of ≥2 MPa. Tabletability (tensile strength vs. compaction pressure), compressibility (porosity vs. compaction pressure), and compactibility (tensile strength vs. porosity) were then studied for tablet formulations. The desired tensile strength could be obtained at the diluent level of 50%-70%, where silicified MCC provided better hardness than Avicel PH-102. Tablets disintegrated in <2 min, and drug release from tablets was comparable to that of milled filaments.