Avicel PH Research Articles

Water interaction with MCC powder exposed to wetting–drying cycles: Comparison of capillary imbibition techniques

We investigate how wetting-and-drying (WD) cycles change the properties of microcrystalline cellulose (MCC) powder (Avicel PH101), due to hornification, by performing the following experiments: (i) drop absorption in a slightly compressed powder bed, (ii) capillary imbibition in a packed powder column, and (iii) drop absorption into tablets obtained by direct compression. We use the MCC powder as received, as well as the powder obtained after one or more WD cycles. In each case, the powder is sieved and fractionated into two samples, with different particle size distribution. First, we perform drop absorption experiments using both water and silicone oil (Polydimethylsiloxane - PDMS) drops. We observe that WD cycles increase the absorption time for water, a particularly marked effect after the first cycle, for both particle size distributions. Comparing the absorption times of water and oil drops we obtain a parameter β that characterizes the water-MCC interaction in lieu of the contact angle, and accounts for both capillary and swelling phenomena. We observed that the main effect is produced after the first WD cycle exhibited by a large (more than 50%) reduction in the β value. Column imbibition experiments performed using water and PDMS show that, initially, water penetrates at a larger rate than PDMS. This initialing faster water uptake is more significant for larger particles and fewer WD cycles. A power law regime is obtained in each case with a ζ exponent. In particular, a Washburn-like imbibition regime with ζ=0.5 is recovered at long times for both liquids. In the last experimental technique, we study the absorption of water drops deposited on tablets obtained by direct compression of the full distribution of powder particle sizes. We observe that absorption time increases with increasing number of WD cycles of the MCC powder. This is quantified by the 30% reduction of the ζ exponent that models the penetration rate of the drop.In summary, we use three kinds of experiments that cover a wide range of characteristic time scales to quantify the effect of WD cycles on the interaction of water with a swelling powder like MCC. The importance of comparing responses under different timescales is that the swelling phenomenon modifies the properties of the material in time, while imbibition happens. It is shown by this study that in some cases, the phenomena can be decoupled (droplet absorption in porous media) while in other cases it cannot be (droplet on tablets and intermediate times in capillary rise). Finally, at long times in capillary rise, even when the swelling and imbibition effects are not decoupled, it is possible to estimate the permeability ratio, χ, and its dependence with the WD cycles when the results are used in combination with the ones from the droplet absorption on powder test. The permeability decreased about 8 times for no WD cycles, and it decreased much less (2 and 3 for small and large particles respectively) for one and two WD cycles. We were able to quantitative characterize the effects of water-MCC interaction and this is important in order to predict how some pharmaceutical processes, like wet granulation, will be affected.

Enhancement of Solubility and Dissolution Rate of Simvastatin Tablets by Liquisolid Compact Approach

The aim of the current work was to improve the solubility and dissolution rate of poorly water-soluble drug, simvastatin (SM) by using the liquisolid compact technique (LS; SM-LS). Liquid load factors, and excipient ratios were used to calculate the required amounts of excipients necessary to prepare the SM-LS and compressed to tablets according to mathematical models. Avicel PH102, Aerosil 200 and Crosspovidone (CP) was used as carrier, coating material and disintegrant, respectively. Drug-excipient mixtures were evaluated compatibility by Attenuated total reflectance (ATR) and differential scanning calorimetry (DSC). Prepared SM-LS formulations were evaluated for various pre-compression and post-compressional parameters, in-vitro dissolution, and stability studies (40 ± 2°C / 75 ± 5% RH) for 3 months. Among the different formulations, LS10 formulation which contains 30% drug, 5% CP, Avicel pH 102: Aerosil 200 (1:10) showed 14-folds increase in dissolution rate when compared with pure SM powder. FTIR-ATR and DSC studies confirmed that there was no interaction between the drug and excipients. Further, the LS10 formulation had shown comparable dissolution profile with commercially available tablet formulation. The LS10 formulation showed no significant changes in the physicochemical properties over 3 months during stability studies. Therefore, the SM loaded LS formulation could be considered as an alternative approach to enhance the solubility and dissolution for commercial formulations. Keywords: Liquisolids compacts, solubility, dissolution, carrier, coating material, stability.

Unveiling the Preparation and Characterization of Lercanidipine Hydrochloride in an Oral Solid Self-Nanoemulsion for Enhancing Oral Delivery.

Chronic kidney disease (CKD) is becoming increasingly prevalent worldwide, particularly among the elderly, along with an increase in the incidence of hypertension and cardiovascular disorders. Developing lipid-based oral dosage forms with a higher expected bioavailability of antihypertensive drugs with nephroprotective effects poses a challenge. Lercanidipine hydrochloride (LRCH) is a newer type of third-generation dihydropyridine calcium channel blocker that functions as an antihypertensive and has significant nephroprotective effects. Due to its extensive first-pass metabolism, its bioavailability is about 10% and increases to 3-4 times when taken with a high-fat meal. Targeting this drug to the lymphatic system using the solid self-nano-emulsifying drug delivery system (SSNEDDS) is a promising approach for improving LRCH's bioavailability and dispersion rate. SSNEDDS combines the benefits of both liquid self-emulsifying and solid dosage forms, improving drug stability and extending storage time. In this study, liquid SNEDDS composed of 10% peppermint oil, 67% Tween 20, and 22.5% propylene glycolwas solidified using two adsorbent agent mixtures (SSNEDDS1: Avicel PH 101 and Aerosil 200) and (SSNEDDS2: Avicel PH 102 and Aerosil 200) separately. The prepared formulations were evaluated for powder flow, drug content, and an in-vitro dispersion test in comparison to the brand-marketed tablet as a standard or pure drug. DSC and X-ray diffraction analysis were also used. The SSNEDDS2 shows excellent flowability, a higher drug content (99.761%), and a significantly higher and faster dispersion rate of 100% within 10 minutes compared to 92% of the marketed LRCH tablet and 18.1% of the pure drug for 60 minutes. The solid-state characterization of the formulation composed of SSNEDDS2 confirmed that the LRCH was in an amorphous form inside the solidified nano system without interacting with the excipient. This study successfully prepared LRCH using the promising strategy of SSNEDDS as a hard gelatin capsule with a higher dispersion rate. It improved its stability and expected bioavailability compared to the brand-marketed tablet as the standard.

An Effective Approach to Enhance the Dissolution Profile of Curcumin and Quercetin: Liquisolid Compacts

Background: The drugs categorized under BCS class II and IV are poorly water-soluble, which in turn affects their dissolution and bioavailability. To overcome these limitations, namely, poor solubility and bioavailability, several approaches have been tried so far, like, co-solvency, size reduction or micronization, complexation, adsorption on high surface area carriers, etc. Objective: The present article aims to explore the utilization of the liquisolid technique to improve the dissolution profile of curcumin and quercetin, used as a combination in a solid dosage form. It covers the study of the impact of various carriers employed in liquisolid technology on drug dissolution profiles; Avicel pH 101, Fujicalin and Neusilin were used as carriers in this study. Methods: The solubility of the drugs was evaluated in various non-volatile solvents except water to select the vehicle having maximum solubility. All formulations were then prepared using curcumin and quercetin in a ratio of 2:1 (150 mg curcumin : 75 mg Quercetin), comprising a proportion of 40-60% w/w of the total mass of the formulation and were estimated for post-compression parameters. During the final processing of the liquisolid compacts, the carrier is to coating material ratio was kept consistent, i.e., 20:1. Results: Powder X-ray Diffraction (PXRD) and Fourier Transform Infrared Spectroscopy (FTIR) were utilized to analyze drug-excipient interaction; these studies stated no evidence of any physical or chemical interaction between drug(s) and the excipients. The final product was then evaluated for the liquid adsorption capacity and in vitro release of the drugs as a combination, and it was observed that these two properties were found to be significantly improved in the liquisolid compacts. Conclusion: The outcomes indicated that the combination of Neusilin as the carrier and castor oil as a non-volatile solvent was the best-performing formulation appropriate for targeting an improved dissolution profile.

Optimizing Seaweed Capsule Shell Formula with Multiple Disintegrants to Accelerate Disintegration Time

Abstract Seaweed-based capsule shells are gaining popularity due to their animal-free sourcing and guaranteed quality. However, these shells often suffer from prolonged disintegration. Various studies have explored formulations with additional disintegrants like polyvinylpyrrolidone (PVP) K-30, yet results have fallen short of pharmacopeia standards. In this research, multiple disintegrants and formulations were tested to develop seaweed capsule shells with rapid disintegration times. The variation in composition of disintegrants was determined using Simplex Lattice Design (SLD) in Design Expert® 13.0.12. By altering the variables in the form of concentrations of PVP K-30, Avicel PH 101, Primogel, Amylum Manihot, Carrageenan, Tween 80, and Aquadest. Primary targets were to identify disintegrants that can significantly reduce disintegration time while maintaining adherence to pharmacopeia standards. Using primogel can fully produce a capsule shell with a promising disintegration time of around 17 minutes, thereby achieving the objective of expediting the disintegration process. Primogel also reduces the critical gel point to 48.23°C when completely replacing PVP K-30. However, balancing desirability proved challenging, as reducing PVP K-30 led to increased disintegration time. Other disintegrants, like Avicel PH 101 or amylum manihot, had no significant impact on disintegration time or gel point. These findings contribute to understanding the complex relationship between disintegrants and their effects on seaweed capsule shell properties, advancing the objectives in optimizing formulation for improved pharmaceutical applications.

Design Formulation and Evaluation of Anti Migraine Mouth Dissolving Tablets Using Different Super Disintegrants

The main objective of this research was to create and evaluate the efficacy of orally disintegrating tablets containing sumatriptan succinate at a dosage of 25 milligrammes, a medicine commonly prescribed for the treatment of migraines. The tablets are made using the direct compression method. In order to achieve best results, the formulations were enriched with microcrystalline cellulose of varying composition (Avicel PH 102), mannitol as a diluent, crospovidone, croscaramellose, and sodium starch glycollate as superdisintegrants. Carbomer (carbopol 940), Sodium CMC, and Sodium Alginate were among the other excipients that were used. When used at varying doses, these excipients act as disintegrants. In addition, magnesium stearate was used as a substance to reduce friction, while talc was used as a substance to improve flow. We assessed each of the excipients to ascertain their compatibility with the model drug. The findings revealed no occurrence of any physical or chemical interaction. Before compression, the preformulation features of the tablet blend were examined. The criteria considered were bulk density, tapped density, compressibility index, and hausner ratio. An assessment was carried out on central tablets to ascertain their dimensions, firmness, tendency to crumble, variability in weight, rate of disintegration, and uniformity of drug content properties. Furthermore, an investigation was conducted to examine the impact of these variables on the release of the drug. The drug release studies were performed in vitro using the USP dissolving apparatus-II (paddle type) with a phosphate buffer solution at a pH of 6.8. The experiments were conducted at a speed of 50 revolutions per minute at a temperature of 37 degrees Celsius, with a standard deviation of 5 degrees Celsius. The sampling was conducted at consistent intervals of 2, 4, 6, 8, and 10 minutes. After each withdrawal, an equivalent volume of dissolving medium was replaced with the sample. The ultraviolet (UV) method is employed to evaluate the cumulative quantity of medications that have been discharged at different time intervals. Based on the evaluation results, the F-3 trial formulation, which included 6% crospovidone, was selected as the superior formulation among the superdisintegrants. Conversely, the F-10 trial formulation, which included 2% carbopol 940p, was selected as the superior formulation compared to other basic disintegrants.

Formulation and evaluation of immediate-release capsules of pregabalin

The aim is to develop and evaluate capsules with various excipient compositions that satisfy the reference product's specifications to achieve an in-vitro correlation with the reference product after that. Pregabalin I.R. capsules were formulated using Corn starch, Dibasic calcium phosphate, Lactose anhydrous, and Avicel pH 102(Microcrystalline cellulose). After compatibility studies for the capsule blend were completed, the Drug was determined to be compatible with all excipients used in various formulations. After the blend was put into capsules, several metrics were examined, including average weight, disintegration, and assay. The formulation containing D.C.P. disintegrates at a faster rate than other formulations. It was discovered that the percentage of drug release in the F7 invitro dissolving profile was equal to that of the innovator product. Finally, it was concluded that the F7 formulation is better and similar to the innovator product.

Preparation and impregnation of deep eutectic solvents containing zileuton onto adsorbents to elicit the biopharmaceutical attributes

Deep eutectic solvent (DES) is a contemporary and eco-friendly solvent recently exploited to modulate the solubility of drugs. Herein, we developed DESs for an increment of solubility and bioavailability of zileuton (ZLT). ZLT is an anti-inflammatory drug categorized as an inhibitor of the enzyme 5-lipoxygenase commonly prescribed for treating chronic bronchial asthma. However, its therapeutic uses are limited owing to its poor water solubility. Several stable DESs were developed and assessed for viscosity, pH, and solubility. The DES comprising ChCl: EG (1:3) exhibits an excellent ZLT solubility (57.27 ± 0.14 mg/mL). The molecular and electrostatic interaction was assessed through a conductor-like screening model for real solvents (COSMO-RS). Further, 1H NMR analysis, FTIR, and digital microscopy were used to investigate the molecular transition in the chosen DES-ZLT. The DES in a liquid state possesses several drawbacks, such as instability, volatility, and dose precision. Therefore, a wet impregnation approach utilizing inert carriers such as Aerosil-200 and Avicel PH-102 was performed for the solidification of liquid DES. The solidified DES-ZLT was characterized by DSC and PXRD techniques and indicated the existence of ZLT in a highly dissolved state. Furthermore, solid DES-ZLT showed a significant increment in the dissolution studies, resulting in a 2.91 fold rise in oral bioavailability of ZLT. Hence, the presented study proves a well-organized and proficient development of a solid DES system to ameliorate the solubility and stability aspects of ZLT, which could provide the template for promising drugs that lack therapeutic effectiveness owing to solubility issues.

DEVELOPMENT OF MYCROCRYSTALLINE CELLULOSE ORIGINATE FROM SAGO (METROXYLON SAGU) STEM BARK BY HYDROLISIS METHODE USING NITRIC ACID

Objective: Microcrystalline cellulose (MCC) is an essential excipient in tablet formulation. Mostly MCC was obtained from wooden conifer stem fiber, therefore environment issues had been came up. Alternative sources for MCC which offer friendly conifer wood need to be explored. This study aimed to isolate and determine the characteristics of MCC originated from Sago (Metroxylon sago Rottb.) stem fibers as an promising alternative of MCC. Methods: MCC was prepared through pre-hydrolysis using an acetic acid solution, alkali heating using NaOH solution, and acid hydrolysis using nitric acid 0.3 N using three variations of heating temperature, namely 90, 95 and 100 °C. The characterization carried out were pharmaceutical grade, powder properties, FTIR analysis and powder morphology by SEM. Results: The yields obtained were 66.02; 65.53 and 65.08%, respectively. The characteristics of the MCC sample based on pharmaceutical grade quality were white to yellowish white powder, odorless, tasteless, insoluble in: ether, 96% alcohol, HCl 2N and NaOH 1N. The pH of the MCC suspension were 5.07-5.12, while moisture content were 3.67-4.17%, with loss on drying value as much as 0.37-0.4%, and ash content 1-2.17%. The value of permanganate number were 0.09-0.11, Hausner factor was between 1.05-1.25, and angle of repose were between 11.4-24.8°. Conclusion: Based on the results, it can be concluded that Sago is potent natural resource for MCC. The resulting MCC revealed physicochemical and characteristic of MCC, which almost similar to Avicel PH 102 as standard.

Formulation and optimization of a single-layer coat for targeting budesonide pellets to the descending Colon

The current budesonide formulations are inadequate for addressing left-sided colitis, and patients might hesitate to use an enema for a prolonged time. This study focuses on developing a single-layer coating for budesonide pellets targeting the descending colon. Pellets containing budesonide (1.5%w/w), PVP K30 (5%w/w), lactose monohydrate (25%w/w) and Avicel pH 102 (68.5%w/w) were prepared using extrusion spheronization technique. Coating formulations were designed using response surface methodology with pH and time-dependent Eudragits. Dissolution tests were conducted at different pH levels (1.2, 6.5, 6.8, and 7.2). Optimal coating formulation, considering coating level and the Eudragit (S + L) ratio to the total coating weight, was determined. Budesonide pellets were coated with the optimized composition and subjected to continuous dissolution testing simulating the gastrointestinal tract. The coating, with 48% S, 12% L, and 40% RS at a 10% coating level, demonstrated superior budesonide delivery to the descending colon. Coated pellets had a spherical shape with a uniform 30 µm thickness coating, exhibiting pH and time-dependent release. Notably, zero-order release kinetics was observed for the last 9 h in colonic conditions. The study suggests that an optimized single-layer coating, incorporating pH and time-dependent polymers, holds promise for consistently delivering budesonide to the descending colon.

ISOLASI ALFA SELULOSA DAN PEMBUATAN SERTA KARAKTERISASI MIKROKRISTALIN SELULOSA DARI KULIT BUAH LIMPASU (Baccaurea lanceolata Muell)

Indonesia is rich in biological natural resources and has diversity spread throughout Indonesia. One of the typical Indonesian plants, especially in Kalimantan, is Limpasu. Limpasu is a typical Kalimantan plant, where this plant has many nutritious contents such as antioxidants and has high potential to be used as a raw material for making microcrystalline cellulose. Microcrystalline Cellulose (MCC) is cellulose that is partially purified, then processed with ɑ-cellulose preparations. The aim of this research is to obtain microcrystalline cellulose from Limpasu fruit peel waste. The research method used in this research is chemical delignification, followed by hydrolysis using dilute acid to produce MCC, then characterized with Avicel PH 102 as a commercial comparison. Based on the research results, the yield of α-cellulose was 14.14% for simplicia powder, the MCC yield was 11.48% for α-cellulose and the characterization of MCCKBL powder showed similar characteristics to Avicel® PH 102 as a comparison.

Characterizations of Swelling Granule of Clove Leaf (Syzygium aromaticum L.) Ethanol Extract

Cloves, scientifically known as Syzygium aromaticum L., hold promise as a potential antiulcer remedy due to their rich composition of compounds, including high levels of phenolic compounds such as eugenol, eugenol acetate, and gallic acid. To improve bioavailability in the gastric environment, this study focuses on optimizing and evaluating a swelling granule system derived from clove leaf extract. The granules were produced using wet granulation with Carbopol, HPMC, and their combination as polymer matrices. Results indicated favorable properties in the swelling granules, with the optimal composition of 210 mg Carbopol, 36 mg PVP, and 404 mg Avicel pH 101. These granules exhibited a uniform particle size distribution, with 90.1% below 149 µm and 9.9% distributed across mesh numbers 100, 80, and 40. The formula with Carbopol polymer showed superior flow rate, compressibility, and swelling capacity compared to other formulations. The interaction between Carbopol's C=O groups and HPMC's hydroxyl groups significantly influenced parameters, especially swelling capacity. Thus, when combining polymers, potential chemical or physical reactions should be considered. The wet granulation process effectively preserved secondary metabolite levels from clove leaf. Further tests are recommended to evaluate the granulation's effectiveness as a delivery system for clove leaf extract.

APPLICATION OF A HYDROPHILIC BIOPOLYMER OBTAINED FROM PENNISETUM GLAUCUM SEED FIBRE AS BINDER IN ALBENDAZOLE CHEWABLE TABLET FORMULATION

Natural polymers with enhanced binding properties in tablet formulation continue to be highly sought over synthetic materials. This study aims to evaluate the binding properties of a hydrophilic biopolymer derived from the modification of the seed fibre of Pennisetum glaucum (TP) in the manufacture of albendazole chewable tablets. Dry TP seeds were steeped in water for 24h, washed, wet milled, and the fibre separated from the starch by washing slurry with water through a muslin cloth. Fibre of TP was dried at 60°C, screened through 180µm sieve (TP-NF). An 800 g of TP-NF was dispersed in 3.0L of 3.5% w/v sodium hypochlorite for 30 min, washed with distilled water to neutral pH, dispersed in 90% v/v ethanol for 10 min and dried at 60°C (TP-MC). The fibre was classified (180µm) and characterised using standard methods. Albendazole tablets were formulated using 5, 7.5, 10 and 15% w/w of the biopolymers by wet granulation. Avicel PH 101 was used as comparing standard binder. The dried albendazole granules were micromeritically evaluated while tablets made from the granules were evaluated for their physical properties, assay and dissolution studies. TP-MC powder flowed and compressed better than TP-NF, while albendazole granules had better flow and compressibility than TP-NF and TP-MC. The albendazole tablets were fairly strong and varied minimally in weight. Friability was <1%, and > 80% of albendazole was released from the tablets within 15 min. TP-MC served more effectively than TP-NF and compared favourably with Avicel PH 101 as binder in the formulation of albendazole tablets.

Ethanol Extract Dry Syrup Granulation Formulation Dayak Onion Bulb (Eleutherine bulbosa (Mill.) Urb.)

Background: Dayak onion (Eleutherine bulbosa (Mill.) Urb.) is one kind of medicinal plant native to East Kalimantan that has antioxidant activity. The dosage form that can be developed is dry syrup granules which become one of the most simple dosage forms in preparation, easy to use, storage-stable and can cover the bitter taste of the drug. The goal of this study was to find the best mix of Avicel PH 101 and Na CMC to make dry syrup granules that meet the requirements for physical properties. Methods: Research was carried out experimentally using three formulas with combinations of Avicel PH 101 and Na-CMC. The ratios of Avicel PH 101 and Na-CMC were (1:0); (0.5:0.5) and (0:1). The evaluation of dry syrup granules included organoleptic observations, a moisture content test, a flowability test, a reconstitution time test, pH test, viscosity test and a hygroscopic test. Result: dry syrup granules with variation 1:0 of Avicel PH 101 and Na-CMC have the best requirements for physical properties, i.e. moisture content of 2.47%, the flow time of 0.91 seconds, an angle of repose 25.19 ° and tap index of 10.67%. Conclusion: Dry syrup granules with a ratio of Avicel PH 101 and Na CMC (1:0) are preparations that best meet the physical properties requirements, namely moisture content of 2.47%, flow time of 0.91 seconds, angle of repose 25, 19° and a fixing index of 10.67%.

Direct compression of diclofenac sodium tablet using modified Musa paradisiaca pseudostem cellulose-corn starch polymer alloy

Background: Biomaterials exhibit different functional properties. The aim of this study is to formulate direct compressible diclofenac sodium tablet using modified pseudostem cellulose and starch complex. Methods: Cellulose was extracted from Musa paradisiaca pseudostem and modified using acid-hydrolysis and fermentation techniques. The modified cellulose was evaluated using FT-IR analysis. Avicel pH-101 was used as control cellulose. Micromeritic properties of the modified cellulose were evaluated using tapped consolidation technique. Co-milling heat technique was used to produce polymer-alloy of 21.7, 43.4 or 87.0% of modified cellulose and 78.3, 56.6, or 13.0% dried corn starch respectively. The dried starch or polymer-alloy was blended with diclofenac sodium, co-povidone and magnesium stearate to produce batches A - G. The blends were analyzed for Kawakita densification properties before being compressed to tablets. The physicochemical and drug-release properties of the tablets were evaluated. Results: Of the dried pseudostem mass, 52.01% and 48.04% of extracted and modified celluloses respectively were obtained. The FTIR study showed presence of cellulose in the pseudostem extract and no interaction between the cellulose and diclofenac sodium. The celluloses had Hausner’s ratios < 1.32 and Carr’s indices < 23.54%. The polymer-alloy blends showed Kawakita compressibility < 16.34 and compactibility > 489.30. The control tablets passed physicochemical properties tests. The test tablets had hardness > 12.34 KgF, disintegration time > 144.67 min, and released 7.64 - 77.59% drug in acidic to basic medium over 240 min. The result indicates that the pseudostem-cellulose was flow-able, and produced compactible polymer alloys and extended drug-release tablets. Conclusion: Direct compression of diclofenac sodium with Musa paradisiaca pseudostem cellulose-corn starch polymer-alloy produced compact tablets with extended drug release. Keywords: Acid-hydrolysis, co-milling, compressibility, drug release

Effects of increasing compaction temperature on tablet strength

Over time, a standard tablet press heats up during use. This investigation aims to explore heat effects at a small scale in the laboratory.  The effects of heat on compression have been studied using a Compaction Simulator fitted with a temperature controlled die. Placebo formulation blends composed of Avicel PH102, Lactose Fast Flo 316, Sodium Starch Glycolate and Magnesium Stearate was compressed using a hydraulic Compaction Simulator. To assess the manufacturability of the formulations a Korsch XL100 profile at 30 rpm was chosen using 10 mm flat faced tooling. A jacketed die was connected to a water-bath, heated to a set temperature. The temperatures assessed were: 20oC, 30oC, 40oC, 50oC and 60oC and any effects on the tabletability of the formulation was assessed. The tensile strength at 100 MPa compaction pressure for each temperature was determined using trend line equations. Increasing temperature changes the tensile strength of the formulation. The highest tensile strength was recorded at 50oC with no further increase for this formulation blend above this temperature.

LOZENGES FORMULATION OF CIPLUKAN (PHYSALIS ANGULATA L.) FRUIT EXTRACT AS AN ANTIOXIDANT WITH COMBINATION OF FILLER AGENTS AVICEL PH 102–LUDIPRESS

Objective: This research aimed to determine the effect of variations in the concentration of filler agents Avicel PH 102-Ludipress on the evaluation results of granules and tablets and to determine the antioxidant activity of ciplukan (Physalis angulata L.) fruit extract lozenges.
 Methods: The extract was obtained by the soxhletation method using ethanol 96%. The lozenges were made by direct compression, and the formula was divided into 3 concentration variations of Avicel PH 102 and Ludipress, namely F1 (1:2), F2 (1:1), and F3 (2:1). The best lozenges were tested for their antioxidant activity using the DPPH method.
 Results: The results of statistical analysis using the One Way Anova test formulation of ciplukan fruit extract lozenges with variations in concentrations of Avicel PH 102 and Ludipress had a significant effect (p<0.05) on the angle of repose, bulk density, tapped density, Carr's index, Hausner's ratio, thickness, friability, and disintegration time, but no significant effect (p>0.05) on diameter, weight variation, and hardness. The best ciplukan fruit extract (F1) lozenge formula has a concentration ratio of Avicel PH 102 and Ludipress (1:2) with an IC50 value of 28.46 ppm and is classified as a very strong antioxidant.
 Conclusion: Ciplukan fruit extract formulated in the form of lozenges with varying concentrations of the filler Avicel PH 102: Ludipress (1:2) has very strong antioxidant activity.

Solubility and Bioavailability Enhancement of a Novel Liquisolid Compact of Gliclazide

The study investigates the use of liquisolid compacts, a revolutionary pharmaceutical formulation technique, to improve the dissolution rate of weakly water-soluble medicines, with gliclazide as a case study. Nonvolatile solvents such as polyethylene glycol (PEG) 400, tween 80, and propylene glycol were used to make liquidsolid tablets, together with carrier ingredients such as Avicel PH102, starch, or HPMC, and Aerosil 200 as a coating material. The drug-excipient interaction was studied utilizing techniques such as differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The produced tablets were tested for appearance, weight fluctuation, hardness, friability, drug content, and in-vitro drug release before being compared to traditional tablets (control) to determine the improvement in dissolution rate. The optimum formulation was subjected to stability tests. FTIR and DSC investigations revealed no significant drug-excipient interactions. All pill formulations met the requirements. Liquisolid tablets significantly increased gliclazide dissolving when compared to conventional tablets, which was ascribed to improved wetting qualities and particle effective surface area. According to the study, the liquisolid technique is a potential approach for increasing the dissolving rate of poorly soluble pharmaceuticals. The tablets remained stable at accelerated settings for three months, demonstrating the efficacy and feasibility of the liquisolid approach in increasing gliclazide dissolving rates.

Formulation and Acute Toxicity, Anti-Inflammatory, Analgesic Effects of Hard Capsules of Herba Siegesbeckiae Orientalis Dry Extract in Experimental Animals

This study aimed to investigate the acute toxicity, analgesic and anti-inflammatory effects of hard capsules containing dry extract from Siegesbeckia orientalis L. (CKHT) in animal models. Hard capsules were prepared using the volumetric method, with Avicel PH 102 as the diluent excipient and magnesium carbonate as the adsorbent excipient. The acute toxicity of CKHT was assessed on white mice at a dose of 2,400 mg/kg body weight. The anti-inflammatory effect was evaluated using a carrageenan-induced paw edema model in rats, while the analgesic effect was tested using an acetic acid-induced writhing model in mice. The results showed that CKHT administered at the doses of 102.2 mg/kg/day, 204.4 mg/kg/day, and 408.8 mg/kg/day had significant anti-inflammatory effect on the carrageenan-induced rat paw edema model by reducing the paw volume and increasing the percentage of edema inhibition compared to the untreated group (p < 0.001). The dose of CKHT 408.8 mg/kg/day showed anti-inflammatory effects that similar to aspirin at the dose level of 200 mg/kg/day (p > 0.05). In the analgesic study, mice treated with CKHT at the doses of 188.7 mg/kg/day, 377.4 mg/kg/day, and 754.8 mg/kg/day had significant reduction in acetic acid-induced writhing within 30 minutes compared to the untreated group (p < 0.001). Furthermore, CKHT did not show acute toxicity (no LD50) at the dose of 2,400 mg/kg body weight. These results suggested that CKHT exhibited acute analgesic and anti-inflammatory effects in animal models.
 Keywords: Dried extract from Siegesbeckia orientalis L.; capsules; anti-inflammatory; analgesic. 
 

FORMULASI KAPSUL ANTIDIABETES EKSTRAK UMBI BAWANG DAYAK (Eleuhterine palmifolia (L) Merr.) DENGAN VARIASI KONSENTRASI AVICEL 101 DAN PREGELATINIZED STARCH

Diabetes Mellitus is a heterogeneous disease characterized by improvement glucose levels in the blood. Several studies have shown that Dayak onions have hypoglycemic activity or lowering blood glucose levels which may be very useful for treatment of diabetes mellitus. Flavonoids contained in Dayak onions are in position to restore the characteristics of pancreatic tissue by increasing insulin release through β cells, so that it can lower blood sugar levels and can also increase sensitivity peripheral cells to insulin. Given the great potential of Dayak onions as antidiabetic, it is very important to develop more practical preparations that can carrying out weight uniform measurements of the products used, of course, one of them is in pharmaceutical preparations capsule form. This examination aims to determine the physical properties and antioxidant activity of Dayak onion extract capsules in large quantities concentration of Avicel PH 101 and pregelatinized starch as fillers. Look was carried out experimentally using three formulas with various concentrations fillers with a ratio between Avicel PH 101 and pregelatinized starch, in particular formula I (1:0), formulation II (0.5:0.5) and method III (0:1). body residence and drug stability is checked and then tested for antioxidant hobby spectrophotometric use. The research results show that the formula with the composition of Avicel PH 101 and pregelatinized starch in the ratio (0:1) is given the best wet house physical test results were 3.4%, sliding houses 12.82 gram/second, angle of repose 29.85⁰, compressibility 8%, density 0.544 and destroyed time 3 minutes 37 seconds. along with antioxidant effects activity examination showed that the drug Dayak onion extract proved to be moderate antioxidant activity, specifically 228.78 ppm.