scholarly journals CHARACTERIZATION AND CONCENTRATION OPTIMIZATION OF HIBISCUS ROSA-SINENSIS L. MUCILAGE POWDER AS SUPERDISINTEGRANT

Author(s):  
IMAM PRABOWO ◽  
ISKANDARSYAH ◽  
RINA ADRIANY

Objective: The main purpose of this study is to characterize Hibiscus rosa-sinensis L. mucilage (MHR) powder as superdisintegrant and to decide the optimum concentration of Hibiscus rosa-sinensis L. Methods: Characterization was conducted in many tests such as organoleptic, swelling ratio, solubility, polysaccharide, viscosity, particle size distribution, flowability and compressibility index. Next, MHR powder was included in fast disintegrating tablet (FDT) domperidone formulation in several concentrations and compared with FDT domperidone formulation that using sodium starch glycolate as superdisintegrant. Results: The result of characterization of MHR powder were brownish powder, specific smell like traditional medicines, swelling ratio of 24, solubility of 0.426±0.034 mg/ml, positive polysaccharide, the viscosity of 491.33±119.44 cps (2% w/v), 4520.00±1224.42 cps (4% w/v), Dv(10) of 26.2 µm, Dv(50) of 157 µm, Dv(90) of 260 µm, Dv(100) of 380 µm, flowless, and average compressibility index of 26.75±1.79%. The optimum MHR powder concentration was 1% because the average disintegration time was 39.67±4.73 seconds and the average wetting time was 66.33±14.29 seconds. Those times were faster than domperidone FDT that used this superdisintegrant in other concentrations or sodium starch glycolate in the same concentration. Conclusion: Hibiscus rosa-sinensis L. mucilage powder can be used as superdisintegrant in FDT formulation with an optimum concentration of 1%.

2020 ◽  
Vol 35 (2) ◽  
pp. 119-134
Author(s):  
Yohannes Mengesha ◽  
Anteneh Belete ◽  
Tsige Gebre-Mariam

Starch and modified starches have been commonly employed as excipient in pharmaceutical industry. The use of non-modified or “native” starch,  However, is mostly confined due to limitation in several physicochemical properties. Cross-linked sodium carboxymethyl starch which is also known as sodium starch glycolate is extensively used in fast dissolving tablets to disperse the drugs within short span of time. In this study, enset starch was carboxymethylated and subsequently cross-linked. Carboxymethyl enset starch (CMES) was obtained by reacting enset starch and monochloroacetic acid (MCA) in the presence of sodium hydroxide. CMESs having different degree of substitution (DS) were cross-linked at variousconcentrations (2.5, 5 and 10% w/w) of sodium hexametaphosphate (SHMP) to provide sodium starch glycolate of enset starch (SSG-E). The fourier transform infrared (FTIR) spectra confirmed the presence of carboxymethylated group in the modified starch granules with new band at 1608.52 cm-1. This dually modified enset starch (SSG-E) was evaluated as a potential disintegrant in paracetamol tablets in comparison with commercially available sodium starch glycolate, Disegel. Carboxymethylation was significantly influenced by reaction medium, reaction temperature and reaction time (p < 0.05). CMES with higher DS (0.437 ± 0.03) exhibited higher peak viscosity than CMES with lower DS (0.224 ± 0.01). Despite exhibiting greater swelling power, CMES showed significantly lower pasting viscosity compared to the native starch (p < 0.05). At 2.5% SHMP, the dually modified starch (SSG-E) exhibited significant increase in swelling but its rate of water-uptake was lower than that of Disegel. As the SHMP concentration wasincreased from 2.5 to 5%, the swelling power decreased significantly (p < 0.05). When the concentration was increased to 10% the swelling power increased significantly (p < 0.05). At 2.5% SHMP concentration SSG-E showed a viscosity comparable to that of CMES. As the concentration of SHMP increased to 5 and to 10% w/w, significant decrease in viscosity (p < 0.05) was observed. Compared to the native enset starch (NES), the solubility of SSG-E was more than 4-fold, but its viscosity was much lower than that of CMESs. The SSG-E exhibited lower moisture sorption than CMES but higher sorption than NES. SSG-E showed good flowability, superior swelling power and solubility than NES. The disintegration time (DT) of paracetamol tablets containing SSG-E as a disintegrant was comparable to those tablets with similar concentration of Disegel. At 4% SSG-E, paracetamol tablets exhibited DT less than 1 min. Keywords: carboxymethylation, degree of cross-linking, enset starch, paracetamol tablets, sodium starch glycolate 


2018 ◽  
Vol 8 (5-s) ◽  
pp. 372-377
Author(s):  
Druv Dev ◽  
Diksha Kumari Rehal ◽  
DN Prasad

The aim of present study was to preparation and evaluation of modified Tamarind seed as natural superdisintegrant. The extracted gum from the Tamarind seed was modified chemically by carboxymethylation of extracted gum was done to improve the hydrophilic nature of the gum. Futher, carboxymethylated gum was complexed by using calcium chloride to enhances  the wetting capacity of the gum. The modification in functional group of extracted gum, carboxymethyled gum, Calcium complexed gum was studied by FT-IR spectrophotometer. The DSC studies shows that the changes in melting point of the carboxymethyled gum and the calcium complexed gum as compared to the extracted gum without undergoing chemical modification. The modified gum was then subjected to different studies like color, pH of gum solution, swelling indexetc. The dummy tablet prepared with calcium complexed modified Tamarind seed gum to check its disintegration effect of the tablet. The various pre-compression parameters of the tablet blend was determined like bulk density, tapped density, Carr's index, angle of repose and Hausner's ratio. The disintegration time of these dummy tablet carry the calcium complexed tamarind seed gum was compared to formulate tablet with marketed superdisintegrant i.e. sodium starch glycolate . The disintegration time of calcium complexed Tamarind seed gum was observed to be 1 min. approx. 32.5 sec. -35.2 sec. showing good disintegrating property. It can be concluded that Fast disintegrating tablet using modified Tamarind seed gum as natural superdisintegrant improves the disintegration time of the tablet. Keywords: FDT tablet, Tamarind seed gum, Sodium starch glycolate, Swelling time. 


Author(s):  
Ganesh kumar Gudas ◽  
Manasa B ◽  
Senthil Kumaran K ◽  
Rajesham V V ◽  
Kiran Kumar S ◽  
...  

Promethazine.HCl is a potent anti-emetic. The central antimuscarinic actions of antihistamines are probably responsible for their anti-emetic effects. Promethazine is also believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine -induced vomiting. Fast dissolving tablets of Promethazine.HCl were prepared using five superdisintegrants viz; sodium starch glycolate, crospovidone, croscarmellose, L-HPC and pregelatinised starch. The precompression blend was tested for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The tablets were evaluated for weight variation, hardness, friability, disintegration time (1 min), dissolution rate, content uniformity, and were found to be within standard limit. It was concluded that the fast dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants. Among the different formulations of Promethazine.HCl was prepared and studied and the formulation S2 containing crospovidone, mannitol and microcrystalline cellulose combination was found to be the fast dissolving formulation. In the present study an attempt has been made to prepare fast dissolving tablets of Promethazine.HCl, by using different superdisintegrants with enhanced disintegration and dissolution rate. 


2020 ◽  
Vol 17 (3) ◽  
pp. 241-254
Author(s):  
Yaqiong Zhang ◽  
Zhiping Jia ◽  
Yunyang Liu ◽  
Xinwen Zhou ◽  
Yi Kong

Background: Deinagkistrodon acutus (D. acutus) and Bungarus multicinctus (B. multicinctus) as traditional medicines have been used for hundreds of years in China. The venoms of these two species have strong toxicity on the victims. Objective: The objective of this study is to reveal the profile of venom proteins and peptides of D. acutus and B. multicinctus. Method: Ultrafiltration, SDS-PAGE coupled with in-gel tryptic digestion and Liquid Chromatography- Electrospray Ionization-Tandem Mass Spectrometry (LC-ESI-MS/MS) were used to characterize proteins and peptides of venoms of D. acutus and B. multicinctus. Results: In the D. acutus venom, 67 proteins (16 protein families) were identified, and snake venom metalloproteinases (SVMPs, 38.0%) and snake venom C-type lectins (snaclecs, 36.7%) were dominated proteins. In the B. multicinctus venom, 47 proteins (15 protein families) were identified, and three-finger toxins (3FTxs, 36.3%) and Kunitz-type Serine Protease Inhibitors (KSPIs, 32.8%) were major components. In addition, both venoms contained small amounts of other proteins, such as Snake Venom Serine Proteinases (SVSPs), Phospholipases A2 (PLA2s), Cysteine-Rich Secreted Proteins (CRISPs), 5'nucleotidases (5'NUCs), Phospholipases B (PLBs), Phosphodiesterases (PDEs), Phospholipase A2 Inhibitors (PLIs), Dipeptidyl Peptidases IV (DPP IVs), L-amino Acid Oxidases (LAAOs) and Angiotensin-Converting Enzymes (ACEs). Each venom also had its unique proteins, Nerve Growth Factors (NGFs) and Hyaluronidases (HYs) in D. acutus, and Cobra Venom Factors (CVFs) in B. multicinctus. In the peptidomics, 1543 and 250 peptides were identified in the venoms of D. acutus and B. multicinctus, respectively. Some peptides showed high similarity with neuropeptides, ACE inhibitory peptides, Bradykinin- Potentiating Peptides (BPPs), LAAOs and movement related peptides. Conclusion: Characterization of venom proteins and peptides of D. acutus and B. multicinctus will be helpful for the treatment of envenomation and drug discovery.


INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (01) ◽  
pp. 37-43
Author(s):  
Ashwin A. Patil ◽  
Ketan B. Patil ◽  
Laxmikant R. Zawar

Present work focused on thiolation for enhancing the mucoadhesive potential of Gum kondagogu (GK). Thiolation of GK was done by esterification process with 80 % thioglycolic acid in presence of 7N HCl. Thiolated Gum kondagogu (ThioGK) was determined to possess 1.59 ±0.04 mmol of thiol groups/g of the polymer by Ellman’s method. ThioGK was characterized by FTIR, NMR, DSC, XRD, and FE-SEM. The tablets were prepared by direct compression using 75 mg of ThioGK and GK. Tablets containing ThioGK (F1) and GK (F2) were subjected to evaluation of weight variation, hardness and friability and show enhanced disintegration time, swelling behavior, drug release and mucoadhesion. In vitro drug release of batch F1 exhibits complete release of drug in 24 hr with zero order release kinetics. Comparative mucoadhesive strength was studied using chicken ileum by texture analyzer and revealed higher mucoadhesion of tablet containing ThioGK. From the above study, ThioGK was suitability exploited as mucoadhesive sustained release matrix tablet.


2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant. 


2020 ◽  
Vol 5 (1-2) ◽  
pp. 16-19
Author(s):  
Ahmed Abdalla Bakheit Abdelgader ◽  
Daud Baraka Abdallah ◽  
Elnazeer I. Hamedelniel ◽  
Hiba Atif Mutwakil Gafar ◽  
Mohammed Abdelrahman Mohammed

Starch is found almost in all organs of plants as a carbohydrate reserve. It is considered one of the most commonly used pharmaceutical additives, mainly in tablet dosage forms; it used as a tablet binder when incorporated through the wet granulation process or as a disintegrant. Cajanus cajan has a high level of carbohydrate, which makes it another potential choice as a source for starch. This study aims to investigate and optimize the effect of Cajanus cajan starch concentrations as well as wet massing granulation time on physicochemical properties of metronidazole tablets. The hardness, friability percentage, and disintegration time of prepared tablets were determined, and the central composite design was employed in the optimization process. Then the tablets of optimized batch were compared against those tablets in which maize starch and sodium starch glycolate were used instead of Cajanus cajan starch. The results indicated that metronidazole tablets containing the upper level of starch paste (Cajanus cajan and/or maize starch paste) exhibited better percentage friability, hardness, and disintegration time than those formulated with lower levels and those without starch paste. The study showed that experimental design is a useful technique for optimizing Cajanus cajan starch-based tablets, which enabled a better understanding of how different variables could affect the responses. In addition, the study demonstrated that incorporation of Cajanus cajan starch in tablets formulation led to improvement of its physical properties compared to the formulations of maize starch and sodium starch glycolate respectively.


2021 ◽  
Vol 32 (4) ◽  
pp. 555-560
Author(s):  
Samirah ◽  
Aniek Setiya Budiatin ◽  
Ferdiansyah Mahyudin ◽  
Junaidi Khotib

Abstract Objectives Alendronate are widely used in the treatment of bone disorders characterized by inhibit osteoclast-mediated bone resorption such as Paget’s disease, fibrous dysplasia, myeloma, bone metastases and osteoporosis. In recent studies alendronate improves proliferation and differentiation of osteoblasts, thereby facilitating for bone regeneration. The disadvantages of this class are their poor bioavailability and side effects on oral and intravenous application such as stomach irritation and osteonecrosis in jaw. Thus, local treatment of alendronate is needed in order to achieve high concentration of drug. Bovine hydroxyapatite-gelatin scaffold with alendronate was studied. Glutaraldehyde was used as cross-linking agent, increase the characteristics of this scaffold. The objectives of this study were to manufacture and characterize alendronate scaffold using bovine hydroxyapatite-gelatin and crosslinked by glutaraldehyde. Methods Preparation of cross-linked bovine hydroxyapatite-gelatin and alendronate scaffold with different concentration of glutaraldehyde (0.00, 0.50, 0.75, and 1.00%). The scaffolds were characterized for compressive strength, porosity, density, swelling ratio, in vitro degradation, and cytotoxicity (the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay, shorted as MTT assay). Results Bovine hydroxyapatite-gelatin-alendronate scaffold cross-linked with glutaraldehyde showed lower density than without glutaraldehyde. As glutaraldehyde concentration increased, porosity also increased. Eventually, it reduced compressive strength. Swelling ratio and in vitro degradation was negatively dependent on glutaraldehyde concentration. In addition, the scaffold has a good safety by MTT assay. Conclusions Bovine hydroxyapatite-gelatin-alendronate scaffold was fabricated with various concentrations of glutaraldehyde. The presence of glutaraldehyde on bovine hydroxyapatite-gelatin-alendronate is safe and suitable candidate scaffold for bone regeneration.


2021 ◽  
pp. 151-164
Author(s):  
Smriti Mall ◽  
Vineeta Pandey ◽  
Aarshi Srivastava ◽  
Rajarshi Kumar Gaur

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