Tablet Formula Research Articles

Formulation and Evaluation of Immediate-Release Oral Tablets Containing Magnesium Aluminum Silicate-Loaded Simvastatin

Background: Simvastatin (SIM) is a lipid-lowering agent to prevent disorders caused by clogged blood vessels. Because of its low solubility, it has low bioavailability. The adsorption technique is effective in improving drug solubility and dissolution rate. Objective: To use magnesium aluminum silicate (MAS) as an adsorbent in combination with Soluplus® as a hydrophilic polymer to formulate SIM as immediate-release tablets (IRTs). Methods: We used the solvent evaporation method to make MAS-loaded SIM in the presence of Soluplus®, making sure that the ratio of SIM to MAS to SOLU was 1:6:3. We then used this mixture to make IRTs. Using the direct compression method, we made all of the SIM-IRT formulas. We used diluents like Avicel®PH102, Avicel®PH101, and starch, as well as super disintegrants like Crospovidone (CP), Croscarmellose sodium (CCS), and sodium starch glycolate (SSG). We evaluated these formulas for their weight variation, hardness, friability, disintegration time, drug content, and dissolution profile. Results: We prepared the tablet formula (T5) using MAS-loaded SIM, Avicel®PH102 as a diluent, and CCS 3% as a super disintegrant. This formula showed the shortest disintegration time (0.61 min) and best drug release in phosphate buffer pH 7.0, releasing more than 80% of the drug within 30 minutes. Conclusion: Using suitable excipients, adsorption was an efficient method to enhance the solubility of SIM for preparation as IRTs.

Characterization of 2-((4-(chloromethyl)benzoyl)oxy)benzoate acid for analgesic tablet dosage form formulation

The 2-((4-(chloromethyl)benzoyl)oxy)benzoic acid (4CH2Cl) is a potential analgesic compound derived from salicylic acid and 4-chloromethyl benzoyl chloride. Characterization required 4CH2Cl for the formulation of tablet dosage forms. This study aims investigate the effect of SSG, PVP-K30, and the combination of SSG*PVP K-30 on the formulation of 4CH2Cl tablets. Additionally, this study aimed to obtain the optimum 4CH2Cl tablet composition. The experiment followed the two-factor simplex lattice design and direct compression method. The analgesic activity of 4CH2Cl in the optimal tablet was investigated using the hot-plate methods. The ANOVA of linear models is acceptable and the polynomial coefficients of quadratic models are similar to those of linear models. The coefficient of the linear model shows that SSG and PVP K-30 increase the Carr index (16.26; 20.61), Hausner ratio (1.19; 1.29), hardness (4.19; 9.39), friability (0.48; 0.67), disintegration time (0.34; 7.50), and drug release (85.29; 97.69). The coefficient of the quadratic model shows that SSG*PVP K-30 increased the Carr index (1.90), Hausner ratio (0.04), hardness (1.88), friability (0.06), and drug release (4.56), and decreased disintegration time (−0.30). SSG and PVP K-30 increased Carr index, Hausner ratio, hardness, friability, disintegration time, and drug release. The combination of SSG*PVP K-30 has the same effect, except that the disintegration time decreased. The optimum tablet formula is 4CH2Cl (300 mg), Ne (75 mg), SSG (33.60 mg), PVP K-30 (22.40 mg), MCC (40 mg), and SDL (up to 800 mg). 4CH2Cl tablets can be a candidate and choice for new analgesic drugs in the future.

Preparation of Single Garlic, Red Ginger, Lemon and Apple Vinegar Combination Tablets By Wet Granulation Method

Garlic, red ginger, lemon, and apple cider vinegar are spices in Indonesia that can be useful for increasing the body's resistance and preventing degenerative diseases. Tablet preparations are preferred because they are practical, easy to use, and easy to carry anywhere. The aim of this research is to see the effect of differences in the concentration of internal and external disintegrants, binders, gliders, and lubricants in each formula. Tablets are made with the single active ingredients of garlic, red ginger, apple cider vinegar, and lemon. The wet granulation method was chosen because natural materials have poor flow properties, so by using the wet granulation method, the flow rate, compressibility, and binding capacity of the granules can be improved for the better so that they can be molded into tablet preparations. The research results showed that all tablet formulas met the tablet evaluation requirements. The concentration of external and internal disintegrants, binders, gliders, and anti-adherents does not make a difference in flow time or angle of repose but provides different water content values in formula 3.There is an influence of differences in the concentration of additional ingredients on the quality of the tablets produced. The greater the concentration, the better the weight uniformity, the harder the resulting tablet, and the longer the disintegration time. Tablet fragility on F2 is high than formula 1 and 3, but still meets tablet quality requirements.

DEVELOPMENT OF ORODISPERSIBLE TABLETS OF LORATADINE CONTAINING AN AMORPHOUS SOLID DISPERSION OF THE DRUG IN SOLUPLUS® USING DESIGN OF EXPERIMENTS

Objective: The objective of the present work was to develop an orodispersible tablet of loratadine, an orally active, non-sedating anti-histaminic, belonging to BCS Class II. The drug was prepared as a solid dispersion using Soluplus® as carrier and formulated into an optimal tablet using Design of Experiments. Methods: Solid dispersions of loratadine with varying ratios of Soluplus® were prepared by solvent evaporation and subjected to solubility study in simulated salivary fluid. Selected composition was characterized by differential scanning calorimetry and X-ray diffraction and formulated into an orodispersible tablet by direct compression after addition of suitable excipients. DOE based on a full factorial design was used to optimize the product using a trial version of JMP software, so as to obtain a tablet with low friability, rapid disintegration and maximal drug dissolution within 5 min. The optimized tablet was prepared and evaluated for several attributes, including in vivo disintegration and palatability. Results: A solid dispersion prepared with a 1: 4 ratio of loratadine: Soluplus® was found to show a 130-fold increase in drug solubility in the simulated salivary fluid. X-ray diffraction revealed loratadine in amorphous form. The exercise using DOE for optimization of the orodispersible tablet formula served to balance the proportion of crospovidone as super disintegrant and PVP as dry binder and yielded a formulation with good mechanical strength, rapid in vitro disintegration (39 sec) and dissolution of 93.78% of the drug within 5 min. When evaluated in vivo, the tablets were found to disintegrate in about 60 secs and were reported to be palatable. Conclusion: A patient-friendly dosage form containing a highly soluble form of loratadine was prepared and could be of potential benefit in offering quick relief from allergic conditions.

Identification and Separation of the Degradation Products of Vildagliptin Tablets and Raw Material using LC-MS and NMR, and then Exploration of the Corresponding Degradation Pathways

A gradient high performance liquid chromatography (HPLC) method has been developed for the qualitative and quantitative analyses of vildagliptin related substances. This method is based on using of RP-C18 (250 × 4.6 mm×5µm) and gradient elution with phosphate buffer and methanol as mobile phase. Various forced degradation studies were conducted to establish an impurity profile for vildagliptin in the tablet formula. Three degradation products were produced upon exposing vildagliptin to different degradation conditions (acidic, basic, oxidative, photolytic, aqueous and thermal); their structures were characterized using LC-MS and NMR (1H NMR, 13C NMR and DEPT) techniques. Some excipient components, examined in this study, had major effect towards producing any extra new degradation products.

The predictive power of biphasic dissolution approach using Class IV model drug

This study was aimed to evaluate biphasic dissolution system and its applicability to discriminate between different formulas. Two different tablet formulas of furosemide were prepared using dry compression (F1) and wet granulation (F2). The prepared formulas were evaluated for hardness,
 friability and disintegration. Thereafter, monophasic and biphasic dissolution systems were used to compare the dissolution profiles of the prepared formulas with a commercially available tablet. The results of the physical properties of the prepared tablets were within acceptable values. Moreover, there were insignificant differences (P>0.05) between generic product and the prepared formulations. The similarity and difference factors were > 58 and <10, respectively. On the other hand, the biphasic dissolution system results showed significant difference regarding dissolution profiles for all items under investigation. In conclusion, biphasic dissolution system could be a viable tool in assessment in-vitro drug performance as a result of its good discriminatory power.

Formulation and Evaluation of Anti-Diabetic Tablet from Insulin Plant (Costus Igneus)

In this research article we prepare tablet formulation of Costus igneus plant i.e., Insulin plant by its ethanolic leaves extract and mixing with suitable excipients. Extract was prepared by collecting Costus igneus plant leaves and go for shade drying for 4-7 days, after drying its crushed by mill to form powder and taken for extraction. After extraction we prepare powder for taking different chemical qualitative test and laboratory flow properties such as; (Angle of repose, Loose bulk density, Tapped bulk density , Compressibility index) and after checking flow properties and then punch tablet by direct compression method we take two forms of tablet formula changes in main API one is extract and other is only powder and go for evaluation study such as; ( Color ,Weight variation Test ,Hardness, Friability, Disintegration Time, Thickness)

FORMULASI TABLET PARASETAMOL DENGAN KOMBINASI PVP DAN AMILUM UMBI PORANG (Amorphopallus onchopyllus) SEBAGAI BAHAN PENGIKAT TERHADAP SIFAT FISIK TABLET

Tablets are the most widely used preparations, this is because tablets have advantages that other pharmaceutical preparations do not have, both in terms of production, storage, distribution, and use. This study aims to determine the concentration of PVP and starch from porang tubers which can be used as a binder in the preparation of paracetamol tablets and to determine the combination of PVP and starch from porang tubers as a binder to the physical properties of paracetamol tablets. In this study, 4 paracetamol tablet formulas with PVP binder were made combined with porang tuber starch with a weight of 650 mg per tablet. The binder used was PVP in each formula, namely F1 0%, F2 1%, F3 3%, and F4 5%, and porang tuber starch in each formula was F1 5%, F2 0%, F3 6%, and F4 7%. Tablets were made using wet granulation, the granules obtained were tested for their physical properties. including moisture content, flow time, angle of repose, and compressibility. After the powder mixture was compressed with a hardness between 4-8 kg, the resulting tablets were then tested for their physical properties including weight uniformity, size uniformity, friability, hardness, and disintegration time. The tablets produced from all formulas met the uniformity of weight, uniformity of size, and friability, the hardness that met the physical properties of the tablets was only found in formula I, which was 7.30 kg, and the fastest disintegration time in formula I was 9.6 minutes.

Hydroxypropyl Methylcellulose as Hydrogel Matrix and Citric Acid-Locust Bean Gum as Negative Matrix for Controlled Release Tablet.

Purpose: This study aimed at determining the optimum concentration of hydroxypropyl methylcellulose (HPMC) as hydrogel matrix and citric acid-locust bean gum (CA-LBG) as negative matrix for controlled release tablet formulation. In addition, the study was to determine the effect of CA-LBG and HPMC. CA-LBG accelerates the disintegration of tablets into granules so that the HPMC granule matrix swells immediately and controls drug release. The advantage of this method is that the tablets do not produce large HPMC gel lumps without drug (ghost matrix) but form HPMC gel granules, which can be rapidly degraded after all of the drug is released. Methods : The experiment followed the simplex lattice design to obtain the optimum tablet formula with CA-LBG and HPMC concentrations as optimization factors. Tablet production by the wet granulation method and ketoprofen is the model of the active ingredient. The kinetics of ketoprofen release was studied using several models. Results : Based on the coefficients of each polynomial equation that HPMC and CA-LBG increased the value of angle of repose (29.91:27.87), tap index (18.99:18.77), hardness (13.60:13.32), friability (0.41:0.73), and release of ketoprofen (52.48:99.44). Interaction of HPMC and CA-LBG increased the value of angle of repose (3.25), tap index (5.64), and hardness (2.42). Interaction of HPMC and CA-LBG too decreased the friability value (-1.10) and release of ketoprofen (-26.36). The Higuchi, Korsmeyer-Peppas, and Hixson-Crowell model is the kinetics of eight experimental tablet formulas. Conclusions : The optimum concentrations of HPMC and CA-LBG for controlled release tablets are 32.97 and 17.03%, respectively. HPMC, CA-LBG, and a combination of both affect the physical quality of tablet and tablet mass. CA-LBG is a new excipient candidate that can control drug release from tablets by the matrix disintegration mechanism on the tablet.

Evaluation of the efficacy and safety of conversion from the tacrolimus capsule to tablet in stable liver transplant recipients with maintenance therapy: a 24-week, open-label, single-center, phase IV exploratory clinical study.

The tablet form of tacrolimus is more convenient for drug ingestion than the capsule form. We examined the efficacy and safety of tacrolimus tablets and a satisfaction survey after formula conversion in liver transplant (LT) recipients. This study was an open-label, prospective clinical trial for tacrolimus formula 1:1 conversion from capsule to tablet in 41 adult LT recipients with tacrolimus maintenance therapy of more than 1 month. The primary endpoint was incidence of biopsy-proven acute rejection (BPAR) within 24 weeks. Surveys 1 week before and 4 weeks after formula conversion were conducted for total daily dose of medication, number, scale of discomfort and satisfaction. The overall incidence of BPAR was 0% and there was no graft loss or patient death. The incidence of adverse effects was 34.1% (n = 14) after formula conversion. The most common severe adverse effect was abnormal liver function test (n = 5): biliary complications (n = 4) and alcoholic recidivism (n = 1). Total daily dose and number of tacrolimus doses were significantly lower after formula conversion (P < 0.05) without changes in trough level. According to survey analysis, there was no significant difference in discomfort and satisfaction scales from capsule to tablet conversion (P < 0.05). The present study suggests that the new tablet formula can be a useful treatment option to maintain a consistent level of tacrolimus with a lower total daily dose and number in adult LT recipients.

Formulasi Tablet Effervescent Ekstrak Sirih Cina (Peperomia pellucida L.) Dan Uji Aktivitas Terhadap Antibakteri Staphylococcus aureus

Chinese Betel herb (Peperomia pellucida L.) has flavonoid and saponin content compounds that can inhibit bacterial growth. The innovation of effervescent tablets used as disinfectants is not widely known in the Indonesian market. This preparation has the advantage of being easy to manufacture as a disinfectant. Chinese betel herb extract is formulated into an effervescent tablet preparation. This study aims to determine the influence on variations in the levels of binders and fillers in the physical properties of effervescent tablet preparations and determine the activity in the effervescent tablet formula of Chinese betel extract (Peperomia pellucida L.) in inhibiting the growth of Staphylococcus aureus bacteria. Chinese betel herb extract is obtained through a maceration extraction process using methanol solvent for 5 days. The preparation of effervescent tablets is made 3 formulas, namely the concentration of binding substances 10%, 13%, 15%. Physical tests of tablet preparations include organoleptic tests, tablet hardness tests, tablet soluble time tests, size uniformity tests, weight uniformity tests,, fragility tests and antibacterial activity tests against Staphylococcus aureus with disc paper diffusion methods.The best formula tablets are formula I (PEG 10%) with uniformity of weight 525±17,014, tablet hardness 3,452±1,172, tablet fragility 0.264%, soluble time 1 minute 6 seconds, uniformity size 3.33±0.06. The results of antibacterial activity tests showed weak inhibitory power with an average formula value of 4.51±0.02.

Formulation of Pectin-Based Double Layer-Coated Tablets Containing Dexamethasone and Probiotics for Inflammatory Bowel Disease

Inflammatory Bowel Disease (IBD) is a chronic inflammatory condition in the colon that includes ulcerative colitis and Crohn’s disease. Dexamethasone is a steroid anti-inflammatory drug that can be used in IBD therapy. This study aims to obtain an optimum formulation of a dexamethasone drug delivery system for IBD treatment and to investigate its release profile based on an in vitro dissolution test. Dexamethasone was formulated as a double-coated tablet in combination with a probiotic L. acidophilus and B. longum mixture (1:1). The core tablets were produced using the wet granulation method, after which they were coated with pectin 4% b/v on the inner coat and a mixture of Eudragit L100 and S100 (1:4) on the outer coat. Three different core tablet formulas were prepared by varying the concentration of probiotics at 0%, 16% and 40% (F1, F2, and F3, respectively). The cumulative drug release of F1, F2 and F3 in HCl 0.1 N pH 1.2 for 2 hours were 42.92 ± 1.55%, 39.41 ± 4.10%, and 39.39 ± 1.63%, respectively, while in the phosphate buffer pH 6.8 they were 102.83 ± 1.56%, 105.08 ± 1.70%, and 98.81 ± 3.37% respectively, after 12 hours. From the results, we conclude that all formulas could be promising candidates for developing colon-targeted drug delivery.

Tablet Formulation of 2-((3-(Chloromethyl)benzoyl)oxy)benzoic Acid by Linear and Quadratic Models.

Purpose: This research determines the effect of sodium lauryl sulfate (SLS) as a surfactant, croscarmellose sodium (CS) as a disintegrating agent, and SLS–CS combinations on 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CH2Cl) (log P = 3.73) tablet formulations. In addition, this study aims to determine the optimum of the 3CH2Cl tablet formula. Methods: The tablets are manufactured through direct compression according to the simplex lattice design. The optimal SLS and CS concentration was determined in vitro using linear and quadratic models to achieve better tablet disintegration and dissolution. Results: The same linear and quadratic coefficient profiles of SLS and CS indicate that the combined coefficient of SLS–CS with a quadratic model can be used to predict the effect of the SLS–CS combination. Based on the linear model coefficients, SLS and CS increase the value of flow time (9.35; 7.65), Carr index (26.17; 21.17), hardness (9.84; 7.44), friability (0.38; 0.31), disintegrating time (5.74; 2.62), and drug release (84.28; 58.65). The quadratic model coefficient shows that SLS–CS combinations increase flow time (0.60), Carr index (2.00), hardness (1.00), and disintegrating time (1.04). Meanwhile, they decrease friability (−0.02) and drug release (−9.10). Conclusions: SLS, CS, and SLS–CS combinations affect the quality of tablet mass and tablets. The optimum tablet formula was 3CH2Cl (300 mg), Ne (9.38%), SLS (0.92%), CS (2.33%), MCC (5%), and SDL (ad 800 mg). 3CH2Cl has analgesic activity despite the presence of tablet excipients. The 3CH2Cl tablet is an innovative formulation and a new alternative for future analgesic drugs.

Pengaruh Kombinasi Matriks terhadap Karakter Tablet Metformin HCl Lepas Lambat Sistem Floating Effervescent

The research aimed to prepare and evaluate of sustained release metformin HCl tablet with floating system. The tablets were prepared by wet granulation using HPMC K4M and chitosan as matrixes with proportions (w/w) 17.78%:4.44%; 14.44%:7.78%; 11.11%:11.11% ;7.78%;14.44%; 4.44%:17.78%. The tablets were evaluated of weight variation, drug content, hardness, friability, and in vitro floating and drug release studies. The dissolution study had been carried out for 6 hours using USP dissolution apparatus II (paddle) in 900 ml HCl pH 3.0 media at 37±0.50C. All tablet formulas showed closed similarity with the requirement physical tablet of United State Pharmacopea (USP) and Farmakope Indonesia reference. The matrixes containing higher HPMC K4M, and lower chitosan showed floating lag time decreased and duration time increased. Meanwhile, tablet disintegration was the lowest. The release test showed that all formulas did not meet the requirements dissolution metformin HCl sustained release tablet. The result of this study is sustained release tablet metformin HCl with matrixes HPMC K4M and chitosan able to float, but it did not form sustained release.

STUDI PREFORMULASI TABLET EFFERVESCENT DAUN TORBANGUN (Coleus Amboinucus L) SEBAGAI ALTERNATIF PENINGKATAN PRODUKSI ASI

The prevalence of exclusive breastfeeding coverage is still far from the national target. The lack of utilization torbangun leaves an excellent opportunity for the development of science and technology. This study aims to determine the optimum formulation of torbangun leaf effervescent tablets (Coleus Amboinicus L) as an alternative to increasing breast milk production. The research method used was an experimental post-experimental design, with the stages of processing simplicia, extracting torbangun leaves, making effervescent tablet formulas, evaluating granules, and evaluating tablet preparations. The difference in the dose variation of each ingredient used in the manufacture of the torbangun leaf effervescent tablet formula greatly affects the quality which is reviewed based on the moisture test of the formulation and the physical properties of the torbangun leaf granules. The results shown in table 2, obtained the formulation of torbangun leaf effervescent tablets made with a variety of ingredients with 4 formulas with a weight of 100 grams each, from the 4 formulas arranged, the results obtained that the best effervescent tablet formula was found in formula 4. A good formula was then tested for granule moisture, flow properties test for an angle of repose and compressibility index as an effervescent tablet in increasing breast milk production, the Na Bicarbonate content in formula 4 which was 26.56 grams gave an excellent solubility effect in water, with this the galactagogue content in Torbangun extract is more free and effective for breast milk production. Meanwhile, based on the physical properties of the granules, the best granule physical properties is formula 2 with a good flow rate, which is more than 10g/second. The flow rate of a granule is influenced by the shape of the granule and the size of the granule.

Development of Herbal Ayurvedic Formulation as Digestive Tablets, Evaluation of it’s Pharmaceutical, Pharmacognostic Parameters and Screening of its Antioxidant Potential

Herbal digestive tablets are meant for treating indigestion problems. The indigestion problem is one of the major problems of all (the) ages of human beings. As trends for eating fast foods is increasing, simultaneously the improper digestion also tends to increase. There are a number of digestive tablets in the market but in attempt to improve their taste the actual motto behind their use is masked. To combat the indigestion problems, in the present study an attempt has been made to formulate, develop and evaluate herbal digestive tablets. The formula of the digestive tablet has been decided after deep review of Ayurvedic formulary of India. The ingredients of this formulation have been procured from authentic sources. The wet granulation method was used to prepare the granules for punching the tablets. After preparation, the herbal digestive tablets were subjected to various pharmaceutical evaluations and quality control evaluations as per the guidelines from World Health Organization (WHO). The formulation was also subjected to antioxidant screening using Phosphomolybdenum method. The digestive tablets are obtained as light brown-colored round tablets with pleasant odour and spicy taste with an average size of 8mm and smooth edges. Maximum extractive value was observed as 34% in methanol with a total ash value of 10.16%. Other parameters reported as bitterness value- 0.69 units, volatile oil content-8%, loss on drying- 12.3%, swelling and foaming index of 0.27 and less than 100 respectively. The tablets showed a total antioxidant potential of 0.51mg/mg as Ascorbic acid equivalent. Tablets also pass various pharmaceutical evaluation parameters like hardness, friability, weight variation, and disintegration test. Herbal digestive tablets have very excellent taste due to less bitter drugs. The tablet formula can be applied to prepare large scale production of digestive tablets.

Physical characteristics of effervescent tablet probiotics in various concentration of tapioca coatings

RICA (Research Institute for Coastal Aquaculture) Maros in South Sulawesi has developed 5 probiotic preparations, namely RICA-1, RICA-2, Rica-3, RICA-4 and RICA-5 in liquid form to improve shrimp farming in ponds. In practice, the use of liquid probiotics has been very optimal but the distribution is constrained because of its liquid form. For this reason, microencapsulation of liquid probiotics is carried out to protect from the external environment and maintain the viability of probiotic cells in the encapsulated matrix. The purpose of this study was to determine the physical properties of probiotic effervescent tablets using tapioca coating with different concentration variants (10 and 20%) with four effervescent tablet formulas. The results showed that the pH of the probiotic effervescent tablet Formula 3 with a coating concentration of 10% tapioca had a neutral pH compared to all existing formulas. However, the pH for probiotic effervescent tablets produced by all formulas can still be applied to shrimp ponds. Formula 4 with 10% tapioca coating has a mean weight and hardness that is close to the standard as well as a disintegration time that meets the specified standard of tablet physical properties. Meanwhile, the tablet friability value was met by Formula 3 with a concentration of 10% tapioca coating. It can be concluded that the best formula that meets the standard physical properties of tablets is Formula 4 with 10% tapioca coating. The probiotic effervescent tablet with tapioca coating has a weakness in the hardness value which causes the average weight to be not uniform. These results indicate that tapioca coating is not suitable for use as a coating for probiotic effervescent tablets.

The Possible Antidiabetic Effect of Ficus carica L. Tablet on lloxan-Induced Diabetes Model in Rats

BACKGROUND: Fig leaves are reported to have an effect on reducing blood glucose levels. However, the use of fresh leaves makes the effects obtained is not measurable and efficient. AIM: The purpose of this research was to determine the antidiabetic potential of ethanol extract of fig leaves and to optimize tablet dosage formulations. METHODS: Four tablet formulas were made using the wet granulation method. Formula I (FI), Formula I (FII), and Formula III (FIII) groups to give a tablet of ethanol extract of fig leaves with a dose of 40 mg, 60 mg, and 80 mg and placebo treatment group. There were eight groups of male rats strain Wistar treated as follows: Normal control, negative control, positive control (metformin tablets), basis group, placebo treatment group, F1, F2, and F3 groups. The antidiabetic activity was evaluated from a decrease in rat blood glucose levels. Previously, rats were induced first using alloxan 150 mg/kg intraperitoneally to damage β-pancreatic cells so that the rats could experience increased blood glucose levels. After giving treatment to each group for 14 days, a rat blood sample was then taken on days 9 and 14, which were then analyzed by the GOD PAP method with readings carried out using a spectrophotometer with a wavelength of 500 nm. RESULTS: The average weight (mg) of FI tablets (617.8 ± 3.21%), FII (629.35 ± 8.16%), and FIII (643.6 ± 6.21%), and placebo tablet (666.45 ± 4.36%). As for the uniformity of size, all formulas have a diameter of 0.9 ± 0.0 (cm). For the hardness values of FI (5.7 kg), FII (1.31 kg), and FIII (3.09 kg), placebo tablet (2.98%). The value of friability FI (1.42%), FII (11.8%), and FIII (0.84%), placebo tablet (1.16%). While the disintegration time of FI (11.02 min), FII (10.10 min), and FIII (17.00 min), placebo tablet (12.23%). As for the uniformity of size, all formulas have a diameter of 0.9 ± 0.0 (cm). Whereas the dissolution rate (DE45) of each formulation decreased with increasing dose of extract, FI (73.73%), FII (74.80%), and FIII (69.80%). The treatment group of the ethanol extract of fig leaves at a dose of 40 mg, ethanol extract of fig leaves at a dose of 60 mg, and ethanol extract of fig leaves at a dose of 80 mg could reduce rats’ blood glucose levels with statistically significant results (p &lt; 0.05) compared to negative group. When it was compared to the positive group, it had significant results with a statistical value (p &lt; 0.05). CONCLUSION: Ethanol extract of fig leaf tablets had a significant effect on lowering rats’ blood glucose levels.

FAST DISSOLVING ORAL DISINTEGRATING FILMS OF VALSARTAN

- Valsartan orodispersible tablets have been developed at 40-mg dose, with the intention of facilitating administration to patients experiencing problems with swallowing and hopefully, improving its poor oral bioavailability. Work started with selecting drug compatible excipients depending on differential scanning calorimetric analysis. A 33 full factorial design was adopted for the optimization of the tablets prepared by freeze-drying technique. The effects of the filler type, the binder type, and the binder concentration were studied. The different tablet formulas were characterized for their physical properties, weight variation, disintegration time, surface properties, wetting properties, and in vitro dissolution. Amongst the prepared 27 tablet formulas, formula number 6 (consisting of 4:6 valsartan:mannitol and 2% pectin) was selected to be tested in vivo. Oral bioavailability of two 40 mg valsartan orodispersible tablets was compared to the conventional commercial tablets after administration of a single dose to four healthy volunteers. Valsartan was monitored in plasma by high-performance liquid chromatography. The apparent rate of absorption of valsartan from the prepared tablets (Cmax = 2.879 μg/ml, tmax = 1.08 h) was significantly higher than that of the conventional tablets (Cmax = 1.471 μg/ml, tmax = 2.17 h), P ≤ 0.05. The relative bioavailability calculated as the ratio of mean total area under the plasma concentration–time curve for the orodispersible tablets relative to the conventional ones was 135%. The results of the in vivo study revealed that valsartan orodispersible tablets would be advantageous with regards to improved patient compliance, rapid onset of action, and increase in bioavailability.

Effect of Formulation Parameter on Dissolution Rate of Flurbiprofen Using Liquisolid Compact

Attempts were made to improve solubility and the liquisolid technology dissolving of medication flurbiprofen. Liquisolid pill was developed utilizing transcutol-HP, polyethylene glycol 400, Avecil PH 102 carrier material and Aerosil 200 layer coating material. Suitable excipient amounts were determined to produce liquisolid powder using a mathematical model. On the other hand, flurbiprofen tablet with the identical composition, directly compressed, was manufactured for comparison without the addition of any unvolatile solvent. Both powder combination characterizations and after-compression tablets were evaluated. The pure drug and physical combination, and chosen liquisolid tablets were studied in order to exclude interacting with the differentional scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR).&#x0D; The results showed that transcutol is the ideal solvent with a solubility of 260±3.9 mg/ml in flurbiprofen. All formula developed were determined to be flowable within the specified limitations. The transcutol-like liquidsolid tablet formula of 35 percent w/w flurbiprofen and carrier to coating ratio of 10 was the most acceptable for the disintegration time, the tablet weight and other approved tablet characteristics.&#x0D; DSC thermographs demonstrated the development of a solid flurbiprofen amorphic solid solution for both the physical blend of the chosen liquisolid system and its tablets. The lack of chemicals interaction in medication and other components of the formula was demonstrated by the retention of all flurbiprofen characteristic peaks in all FTIR spectra. As an option to enhance solubility and dissolve flurbiprofen, which has a poor water solubility, liquisolid tablet has been evaluated.