scholarly journals Evaluating the Flow and Release Profiles of Ibuprofen Formulations by Increasing the Binder Concentration

2021 ◽  
Vol 16 (2) ◽  
pp. 111-117
Author(s):  
B.B. Mohammed ◽  
E.J. John ◽  
G.T. Abdulsalam ◽  
K.P. Bahago

Background: Tablets must be able to release the active drug in the gastrointestinal tract for absorption. The release profile of solid pharmaceutical dosage formulations can be quantified by assessing the disintegration and dissolution times tests. Binders are adhesives either from sugar or polymeric material that are added to tablet formulations to provide the cohesiveness required for the bonding together of the granules under compaction to form tablets.Objective: The objective of the study was to formulate and assess ibuprofen tablets using different concentrations of binders (Acacia and Gelatin).Methods: The granules were prepared using wet granulation method and analysed for flow properties based on USP/NF protocols. After granule compression, the tablets release profiles were thereafter assessed via the tablet dissolution and disintegration tests.Results: Weight variation, thickness and diameter were within the acceptable values for all batches indicative of a uniform flow. Batches with binder concentrations of 10 % and 20 % failed disintegration test due to a disintegration time above 15 min while the release rate for batches 1 and 4 was about 88 % in 60 min as against the other batches whose release rate was less than 50 % in 60 min as a result of increasing their binder concentrations.Conclusion: The study concluded that increasing the concentration of acacia and gelatin above 5% led to a decrease in percentage of drug released and an increase in disintegration time above 30 mins because 5% batches gave the best release profiles.

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Kidan Haily Desta ◽  
Ebisa Tadese ◽  
Fantahun Molla

This study is aimed at evaluating the binding effect of Acacia etbaica gum in granule and tablet formulations using paracetamol as a model drug. Some physicochemical properties of the purified gum such as pH, the presence of tannin and dextrin, solubility, viscosity, loss on drying, total ash value, water solubility index, swelling power, moisture sorption, and powder flow properties were investigated. Paracetamol granules were prepared using wet granulation method at 2%, 4%, 6%, and 8% w / w of the Acacia etbaica gum and compared with granules prepared with reference binders (PVP K-30 and Acacia BP) in similar concentrations. The granules were characterized for bulk and tapped densities, compressibility index and Hausner ratio, angle of repose, flow rate, and friability. Finally, the prepared granules were compressed into tablets and evaluated for different tablet characteristics: weight uniformity, thickness, diameter, crushing strength, tensile strength, friability, disintegration time, and in vitro release profile. The physicochemical characterization revealed that tannins and dextrin are absent in the gum, and the gum has acidic pH. Both the moisture content and total ash values were within the official limits. Furthermore, the gum was found to be soluble in cold and hot water but insoluble in organic solvent and exhibited a shear thickening viscosity profile and excellent flow properties with excellent compressibility. The granules prepared with the gum of Acacia etbaica and reference binders showed good particle size distribution and excellent flow and compressibility properties. All the prepared tablets passed pharmacopeial specifications with respect to their uniformity of weight, thickness, and disintegration time. Tablets formulated with Acacia etbaica gum and acacia BP meet the compendial specification for friability at binder concentrations more than 2%. Drug release properties of all the batches formulated with Acacia etbaica, PVP, and acacia BP complied with the pharmacopeial specification. It can be concluded that the gum of Acacia etbaica could be explored as an alternative excipient for its binder effect in granule and tablet formulations.


Author(s):  
Singh K. ◽  
Pandit K. ◽  
Mishra N.

The matrix tablets of cinnarizine and nimodipine were prepared with varying ratio of Carbopol- 971P and co-excipients of varying hydrophilicity (i.e. dicalcium phosphate and spray dried lactose) by direct compression and wet granulation using alcoholic mucilage. The prepared tablets were evaluated for weight variation, hardness and friability. The influence of concentration of the matrix forming material and co-excipients on the release rate of the drug was studied. The release rate of Cinnarizine (more soluble drug) from tablets followed diffusion controlled mechanism whereas for nimodipine (less soluble drug), the drug release followed case-II or super case- II transport mechanism based on Korsmeyer- Peppas equation. The results indicated that the drug release from matrix tablets was increases with increase in hydrophilicity of drug and co-excipients. The release of drug also increased with thermal treatment and decreasing polymer concentration.


Author(s):  
Sarika Pundir ◽  
Ashutosh Badola

In the present study we have formulated (F1 to F6) matrix tablets of atenolol and indapamide for the management of hypertension. As in simultaneous estimation of these drugs it was found that a confined release can be formulated. In the formulation of SR matrix tablet by using different concentration of delayed release agent DCP and pregelatinized starch as disintegrant we prepared tablets by wet granulation method. For sustained release action HPMC polymers were used for film coating. Preformulation studies were performed prior to compression. The compressed SR matrix tablets were evaluated for weight variation, hardness, friability, drug content, disintegration time and in vitro drug release using USP dissolution apparatus type 2 (paddle). It was found that the optimized formulation showed 49.33%, 48.90%, 48.52%, 47.65%, 46.84% and 46.51% release for atenolol in 12 hours respectively. However, indapamide released 49.62%, 49.39%, 48.72%, 48.27%, 47.59% and 47.36% at the end of 12 hr. The IR spectrum study revealed that there is no disturbance in the principal peaks of pure drugs atenolol and indapamide. This confirms the integrity of pure drugs and no incompatibility of them with excipients. The stability studies were carried out for the optimized batch for one months and it showed satisfactory results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanism of drug and release follows Zero-order, Super case II transport.


2018 ◽  
Vol 10 (6) ◽  
pp. 187
Author(s):  
Sri Agung Fitri Kusuma ◽  
Soraya Ratnawulan Mita ◽  
Ratna Fitria Ermawati

Objective: The objective of this study was to determine the best ratio of maltodextrin and extract concentration on performance of anti-dysentery granule containing Klutuk banana fruit extract (Musa balbisiana Colla) as an effective antimicrobial to treat dysentery caused by Shigella dysenteriae and combined with its pseudostem extract to supply potassium needed for supporting dehydration impact caused by dysentery.Methods: The dried fruit and pseudostem of the Klutuk banana plant were each extracted by maceration method. Each granule formula was optimized in different ratio of extract and maltodextrin concentration (1:2 (F1); 1:3 (F2); and 1:4 (F3) respectively. Then, the anti-shigellosis granule were formulated using the wet granulation method and evaluated for 30 d. The appearance of the granule, weight variation, loss on drying value, flowability, granule solubility, disintegration time, pH, and anti-dysentery activity of each formula was observed. The potassium content determination of each granule formula was done using an atomic absorption spectrophotometer method. Results: All formulated granules showed good flow properties and antidysentery activity. Concerning to the solubility, maltodextrin addition showed the increasing solubility of all formulated granule. The F3 achieved the best-improved granule characteristic and had good anti-dysentery effectivity, but had the lowest potassium content (0.362 g/l) among all formulas. The potassium content of F1 and F2 were 0.625 g/l and 0.444 g/l, respectively. Conclusion: Maltodextrin can improve the usefulness of granule that containing the Klutuk banana fruit and its pseudostem extracts in dysentery treatment and the dehydration impact.


2020 ◽  
Vol 13 (1) ◽  
Author(s):  
Muhammad M. Hammami ◽  
Rajaa F. Hussein ◽  
Reem AlSwayeh ◽  
Syed N. Alvi

Abstract Objective To evaluate in vitro quality of enteric-coated 50 mg diclofenac sodium tablet formulations on Saudi market. Results A reference and seven generic (G1-7) formulations were commercially available in December 2019/January 2020 and were assessed within 25–75% of manufacture-expiration period. Weight variation (range as% difference from mean, n = 20), active substance content (ASC, mean (SD) as% difference from label, n = 20), hardness (mean (SD), n = 10), and friability (% weight loss, n = 20) were 97–103%, 102.0% (3.4%), 15.4 (1.1) kg, and 0.24%, respectively, for the reference. For G2-7, they were ≤ ±5%, 98.6% (4.0%) to 109.9% (1.8%), 11.9 (0.9) to 18.3 (0.8) kg, and ≤ 0.00 to 0.75%, respectively. G1 ASC, hardness, and friability were 111.3% (1.7%), 20.1 (1.7) kg, and 1.10%, respectively. Disintegration time (n = 6) and dissolution profile (n = 8) were also determined. No formulation disintegrated or released ˃ 0.1% of label ASC in 0.1 N HCl for 2 h. The reference disintegrated in 15:00 min:seconds and released a mean (range) of 100% (99–103%) of label ASC by 45 min in phosphate buffer (pH = 6.8). G1-7 disintegrated in 8:53 to 20:37 min:seconds and released 81% (69–90%) (G1) to 109%. Except for borderline performance of G1, all formulations passed in vitro quality tests according to United States Pharmacopoeia.


Author(s):  
Nkemakolam Nwachukwu ◽  
Kenneth Chinedu Ugoeze ◽  
Azuka Ijoma Alumona

Aim: The binding properties of a polymer obtained from modification of Triticum aestivum (TA) starch in metronidazole tablets formulation were evaluated. Study Design: Experimental design. Place and Duration of Study: Department of Pharmaceutics and Pharmaceutical Technology, University of Port Harcourt, Choba, Rivers State, Nigeria from January to July, 2018. Methods: TA seeds were steeped for 72 h, wet milled and the native Triticum aestivum starch (NTS) extracted. NTS (1kg) was oxidized by slurring in 4 L of 3.50% w/v sodium hypochlorite, washed to neutral pH with 95% v/v ethanol (MTS). MTS was dried at 60°C for 3 h, milled and classified (250 μm). The starches were characterized using standard methods and applied as binders at 1, 2 and 3% w/w in formulating metronidazole tablets using wet granulation. Methylcellulose and gelatin at similar concentrations were used as standards. Results: The granules and tablets were evaluated using standard methods. NTS and MTS had similar properties with starch. The modification improved the densities, hydration capacity and flow properties of MTS. The granules flowed and compressed well. The tablets had minimal weight variation, hardness (≥ 4 kgF), friability (<1%) and disintegration (<15 min). Metronidazole release (≥ 85%) within 60 min existed in all the batches except batches containing 1% methylcellulose and 3% gelatine. Conclusion: The results met with United States Pharmacopoeia specifications for oral uncoated metronidazole tablets. MTS performed better than NTS and compared well with methylcellulose and gelatin as binder in metronidazole tablet formulation.


2021 ◽  
Vol 6 (3) ◽  
pp. 131-136
Author(s):  
Fitrya Fitrya ◽  
Najma Annuria Fithri ◽  
Budi Untari ◽  
Aprililianti

Helminthostachys zeylanica extract has pharmacological activities such as antioxidant, antiinflamatory, and antihyerucemia. This extract is nontoxic substance from the acute and subchronic toxicity tests. This extract has a potency to be formulated into tablet dosage forms. This study aims to optimize a tablet formula from Helminthostachys zeylanica extract. Disintegrant and binder concentrations were independent variables, while physical properties and dissolution time of the tablets were dependent variables. The tablet was prepared by a wet granulation method. Formula was optimized by Simplex Lattice Design. Physicochemical propertiesof granule, physical properties and dissolution of tablet were then analyzed with One Way ANOVA (p = 0.05). Based on granule analysis, specification of physicochemical parameters, such as hausner’s ratio, compressibility index, flowability, repose angle, and water content, met standard British Pharmacopeia. In addition, the starch and PVA concentrations influenced thickness, weight variation, hardness, friability, disintegration time and dissolution of the tablets (p <0.05), except for friability (p> 0.05). Based on this study, the starch and PVA concentrations for the optimum tablet formula were 19.5% and 1.05%, respectively.


Author(s):  
Shikha Thakur ◽  
Brisha Bhardwaj ◽  
Shouvik Kumar Nandy

Tablets are used as formulation and are prepared by using plant extracts i.e., Carica papaya and Embelica officinalis. These tablets were prepared by using wet granulation method. In this article the extract of leaves of Carica papaya and fruits of Embelica officinalis were used for making herbal tablets. Extracts of leaves of Carica papaya was obtained by cold extraction and through maceration method and the extract of fruits of Embelica officinalis was obtained by maceration process. Both extracts were dried and mixed. These extracts were then impregnated with the excipients like diluents, binding agents, super disintegrating agent, lubricants, etc. to make granules. These granules were then evaluated by using various parameters like Angle of repose, tapped density, bulk density, Carr’s Index, Hausner’s Ratio and void volume. These granules were then used for the making of tablets of desired size and shape by punching in the machine. After preparation of the tablets their evaluation parameters were studied like physical appearance, weight variation, friability, disintegration time, hardness test and thickness. Also the parameters for the acceptance of the tablets is also done like flavor and sweetness. Recent studies have shown that herbal extract of leaves of papaya has beneficial effect as an anti-inflammatory agent, for its wound healing properties, anti-tumor as well as Immunomodulatory effects and as an antioxidant. Amla fruit is a rich natural source of vitamin C (Ascorbic acid) and contains 600-750 mg/100 g of the fresh pulp. Also it is rich in minerals matters like phosphorus, iron and calcium. Amla is used as an Immunomodulatory agent and hence enhance the immunity of the patient. Aim of the study is to design develop and optimize the dosage form to cure dengue and is based on the use of natural plant ingredients to intermingle with chemical as well as synthetic ingredients to develop an effective unit dosage forms for better patient compliance. KEYWORDS: Papaya, Amla, Extracts, Herbal tablet, Dengue, Immunomodulatory, Platelets.


Author(s):  
Hitesh P. Dalvadi ◽  
Pritesh J. Patel ◽  
Nirmal Vashi ◽  
Arindam Paul

The current research work was to develop bilayer tablet of venlafaxine hydrochloride to increase drug efficacy for efficient treatment of depression. The satisfactory result of treatment can be achieved upon the maintenance of drug concentration within an effective level in the body, so a uniform and constant drug supply are desirable. An immediate layer of venlafaxine HCl was formulated using super disintegrants, i.e., croscarmellose sodium (CCS) and sodium starch glycolate (SSG); tablet compact by direct compression. HPMC K100M and ethylcellulose (EC) were utilized as release retarding polymers in sustained release layer by wet granulation technique with the help of PVP K30 in IPA solution (10%) as a granulating agent. Full 32 factorial designs were used to find out the optimum quantity of release retardant polymers. Bilayer tablet was evaluated for various parameters, i.e. hardness, friability, weight variation, % drug content, disintegration time (IR layer), and % drug release study. Statically, an analysis was carried out using factor X1 (HPMC K100M) and X2 (EC) for dependent variable % drug release at 8, 12, and 20 hours. A formulation was optimized and a formulation containing 305.36 mg of HPMC K100M and 54.03 mg of ethyl cellulose. Optimized formulation show 47.12 ± 2.1, 59.89 ± 2.2, and 89.06 ± 2.3 drug release at 8, 12, and 20 hours, respectively, which is almost similar to theoretical dose calculation with similarity factor f2 97, 99, and 98%, respectively. Bilayer tablet formulation was observed to be stable and fulfilled all compendia specifications.


2021 ◽  
Author(s):  
Zilhadia Zilhadia ◽  
Shoffiya Amaliya ◽  
Yuni Anggraeni ◽  
Vivi Anggia ◽  
Yahdiana Harahap

Abstract Halal gelatin extracted from goatskin could be used as a new excipient in pharmaceutical dosage forms. This study was to determine the potency of gelatin extracted from goatskin as a binder on paracetamol tablets using wet granulation process with 2, 3 and 4% concentration ranges. As a comparison, tablets were formulated using bovine gelatin at the same concentration level. The results showed that weight variation, thickness uniformity and hardness value have met the requirements. Here, the paracetamol tablets using goatskin gelatin as a binder had better friability value, faster disintegration time and easier dissolution than the comparison (p < 0.05). Comparative test result showed increasing the concentration of gelatine caused the hardness value to go up, the disintegration time to take longer, and the tablet friability value to decrease (p < 0.05). The best tablets were produced with the 3% concentration of goatskin gelatine with the following evaluation results: the hardness value of 15.07 ± 0.67 Kp, the disintegration time of 3.71 ± 1.00 minutes and the friability value of 0.62% ± 0.89 respectively. The concentration of paracetamol in the 30th-minute dissolution test was equal to 99.78 ± 0.94%. The goatskin gelatin was very promising as a good binder using the wet granulation process.


Sign in / Sign up

Export Citation Format

Share Document