Displaying publications 21 - 40 of 48 in total

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  1. Ionic-Liquid-Based Paclitaxel Preparation: A New Potential Formulation for Cancer Treatment
    Chowdhury MR, Moshikur RM, Wakabayashi R, Tahara Y, Kamiya N, Moniruzzaman M, et al.
    Mol Pharm, 2018 06 04;15(6):2484-2488.
    PMID: 29762034 DOI: 10.1021/acs.molpharmaceut.8b00305
    Paclitaxel (PTX) injection (i.e., Taxol) has been used as an effective chemotherapeutic treatment for various cancers. However, the current Taxol formulation contains Cremophor EL, which causes hypersensitivity reactions during intravenous administration and precipitation by aqueous dilution. This communication reports the preliminary results on the ionic liquid (IL)-based PTX formulations developed to address the aforementioned issues. The formulations were composed of PTX/cholinium amino acid ILs/ethanol/Tween-80/water. A significant enhancement in the solubility of PTX was observed with considerable correlation with the density and viscosity of the ILs, and with the side chain of the amino acids used as anions in the ILs. Moreover, the formulations were stable for up to 3 months. The driving force for the stability of the formulation was hypothesized to be the involvement of different types of interactions between the IL and PTX. In vitro cytotoxicity and antitumor activity of the IL-based formulations were evaluated on HeLa cells. The IL vehicles without PTX were found to be less cytotoxic than Taxol, while both the IL-based PTX formulation and Taxol exhibited similar antitumor activity. Finally, in vitro hypersensitivity reactions were evaluated on THP-1 cells and found to be significantly lower with the IL-based formulation than Taxol. This study demonstrated that specially designed ILs could provide a potentially safer alternative to Cremophor EL as an effective PTX formulation for cancer treatment giving fewer hypersensitivity reactions.
    Matched MeSH terms: Drug Compounding/methods
  2. Investigation on the effect of polymer and starch on the tablet properties of lyophilized orally disintegrating tablet
    Liew KB, Peh KK
    Arch Pharm Res, 2021 Aug;44(8):1-10.
    PMID: 25579848 DOI: 10.1007/s12272-014-0542-y
    Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.
    Matched MeSH terms: Drug Compounding/methods
  3. Influence of beta-cyclodextrin and chitosan in the formulation of a colon-specific drug delivery system
    Rehman K, Amin MC, Muda S
    Drug Res (Stuttg), 2013 Dec;63(12):657-62.
    PMID: 23842943 DOI: 10.1055/s-0033-1349129
    The increase in diseases of the colon underscores the need to develop cost-effective site-directed therapies. We formulated a polysaccharide-based matrix system that could release ibuprofen under conditions simulating those in the colon by employing a wet granulation method. Tablets were prepared in a series of formulations containing a polysaccharide (beta-cyclodextrin and chitosan) matrix system along with ethylcellulose. We characterized physicochemical properties and performed an in vitro drug release assay in the absence and presence of digestive enzymes to assess the ability of the polysaccharides to function as a protective barrier against the upper gastrointestinal environment. Fourier transform infrared spectroscopy studies revealed no chemical interaction between ibuprofen and polysaccharides; however, spectrum analysis suggested the formation of an inclusion complex of beta-cyclodextrin with ibuprofen. The formulations contained 50% ethylcellulose and 50% beta-cyclodextrins (1:1) were proven to be the better formulation that slowly released the drug until 24 h (101.04 ± 0.65% maximum drug release in which 83.08 ± 0.89% drug was released in colonic medium) showed better drug release profiles than the formulations containing chitosan. We conclude that a beta-cyclodextrin drug carrier system may represent an effective approach for treatment of diseases of the colon.
    Matched MeSH terms: Drug Compounding/methods
  4. Formulation variables affecting drug release from xanthan gum matrices at laboratory scale and pilot scale
    Billa N, Yuen KH
    AAPS PharmSciTech, 2000;1(4):E30.
    PMID: 14727895
    The purpose of this research was to study processing variables at the laboratory and pilot scales that can affect hydration rates of xanthan gum matrices containing diclofenac sodium and the rate of drug release. Tablets from the laboratory scale and pilot scale proceedings were made by wet granulation. Swelling indices of xanthan gum formulations prepared with different amounts of water were measured in water under a magnifying lens. Granules were thermally treated in an oven at 60 degrees C, 70 degrees C, and 80 degrees C to study the effects of elevated temperatures on drug release from xanthan gum matrices. Granules from the pilot scale formulations were bulkier compared to their laboratory scale counterparts, resulting in more porous, softer tablets. Drug release was linear from xanthan gum matrices prepared at the laboratory scale and pilot scales; however, release was faster from the pilot scales. Thermal treatment of the granules did not affect the swelling index and rate of drug release from tablets in both the pilot and laboratory scale proceedings. On the other hand, the release from both proceedings was affected by the amount of water used for granulation and the speed of the impeller during granulation. The data suggest that processing variables that affect the degree of wetness during granulation, such as increase in impeller speed and increase in amount of water used for granulation, also may affect the swelling index of xanthan gum matrices and therefore the rate of drug release.
    Matched MeSH terms: Drug Compounding/methods
  5. Formulation strategy of nitrofurantoin: co-crystal or solid dispersion?
    Teoh XY, Bt Mahyuddin FN, Ahmad W, Chan SY
    Pharm Dev Technol, 2020 Feb;25(2):245-251.
    PMID: 31690150 DOI: 10.1080/10837450.2019.1689401
    Poor solubility and bioavailability of drugs are often affected by its microscopic structural properties. Nitrofurantoin (NF), a Biopharmaceutics Classification System class II item, has a low water solubility with low plasma concentrations. To improve its therapeutic efficacy, formulation strategy of solid dispersion (SD) and co-crystallization are compared herein. The co-crystal is prepared with citric acid in 1:1 stoichiometric ratio while SD consists of 30% w/w nitrofurantoin and 70% w/w hydroxypropyl methylcellulose (HPMC) as the carrier system. As a control, the physical mixture of NF and HPMC was prepared. All the preparations were characterized with differential scanning calorimetry (DSC), attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), microscopy analysis, solubility, and dissolution studies. The formation of co-crystal, solvent evaporated, and spray-dried SD are confirmed by the ATR-FTIR where peaks shifting of several functional groups indicate the formation of the hydrogen bond. Dissolution studies showed a greater initial dissolution rate in co-crystal than SD despite the possible presence of amorphous content in the SD system. Overall, co-crystal is concluded to be a better approach than SD for an effective dissolution.
    Matched MeSH terms: Drug Compounding/methods
  6. Fulltext Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
    Lim WM, Rajinikanth PS, Mallikarjun C, Kang YB
    Int J Nanomedicine, 2014;9:2117-26.
    PMID: 24833900 DOI: 10.2147/IJN.S57565
    The objectives of this study were to develop and characterize itraconazole (ITZ)-loaded nanostructured lipid carriers (NLCs) and to study their potential for drug delivery into the brain. Precirol(®) ATO 5 and Transcutol(®) HP were selected as the lipid phase, and Tween(®) 80 and Solutol(®) HS15 as surfactants. The ITZ-NLCs were prepared by a hot and high-pressure homogenization method. The entrapment efficiency for the best formulation batch was analyzed using high-performance liquid chromatography and was found to be 70.5%±0.6%. The average size, zeta potential, and polydispersity index for the ITZ-NLCs used for animal studies were found to be 313.7±15.3 nm, -18.7±0.30 mV, and 0.562±0.070, respectively. Transmission electron microscopy confirmed that ITZ-NLCs were spherical in shape, with a size of less than 200 nm. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ was encapsulated in the lipid matrix and present in the amorphous form. The in vitro release study showed that ITZ-NLCs achieved a sustained release, with cumulative release of 80.6%±5.3% up to 24 hours. An in vivo study showed that ITZ-NLCs could increase the ITZ concentration in the brain by almost twofold. These results suggest that ITZ-NLCs can be exploited as nanocarriers to achieve sustained release and brain-targeted delivery.
    Matched MeSH terms: Drug Compounding/methods
  7. Extraction and microencapsulation of khat: effects on sexual motivation and estradiol level in female rats
    Aziz HA, Peh KK, Tan YT
    J Sex Med, 2009 Mar;6(3):682-95.
    PMID: 19143913 DOI: 10.1111/j.1743-6109.2008.01157.x
    Khat (Catha edulis) is an evergreen tree/shrub that is thought to affect sexual motivation or libido. Its positive effect on sexual desire is more frequently observed in females than in males and occurs when khat is chewed. Thus, khat's effects on sexual behavior may depend on the release mode of its active constituent.
    Matched MeSH terms: Drug Compounding/methods*
  8. Encapsulation of caffeine into starch matrices: Bitterness evaluation and suppression mechanism
    Shao M, Li S, Tan CP, Kraithong S, Gao Q, Fu X, et al.
    Int J Biol Macromol, 2021 Mar 15;173:118-127.
    PMID: 33444656 DOI: 10.1016/j.ijbiomac.2021.01.043
    In this study, caffeine (CA) was encapsulated into food-grade starch matrices, including swelled starch (SS), porous starch (PS), and V-type starch (VS). The bitterness of the microcapsules and suppression mechanisms were investigated using an electronic tongue, molecular dynamics (MD) simulation and the in vitro release kinetics of CA. All the CA-loaded microcapsules showed a lower bitterness intensity than the control. The MD results proved that the weak interactions between starch and CA resulted in a moderate CA release rate for SS-CA microcapsules. The PS-CA microcapsule presented the longest CA release, up to 40 min, whereas the VS-CA microcapsule completely released CA in 9 min. The CA release rate was found to be related to the microcapsule structure and rehydration properties. A low CA bitterness intensity could be attributed to a delay in the CA release rate and resistance to erosion of the microcapsules. The results of this work are valuable for improving starch-based microcapsules (oral-targeted drug-delivery systems) by suppressing the bitterness of alkaloid compounds.
    Matched MeSH terms: Drug Compounding/methods*
  9. Fulltext Empty nano and micro-structured lipid carriers of virgin coconut oil for skin moisturisation
    Noor NM, Khan AA, Hasham R, Talib A, Sarmidi MR, Aziz R, et al.
    IET Nanobiotechnol, 2016 Aug;10(4):195-9.
    PMID: 27463789 DOI: 10.1049/iet-nbt.2015.0041
    Virgin coconut oil (VCO) is the finest grade of coconut oil, rich in phenolic content, antioxidant activity and contains medium chain triglycerides (MCTs). In this work formulation, characterisation and penetration of VCO-solid lipid particles (VCO-SLP) have been studied. VCO-SLP were prepared using ultrasonication of molten stearic acid and VCO in an aqueous solution. The electron microscopy imaging revealed that VCO-SLP were solid and spherical in shape. Ultrasonication was performed at several power intensities which resulted in particle sizes of VCO-SLP ranged from 0.608 ± 0.002 µm to 44.265 ± 1.870 µm. The particle size was directly proportional to the applied power intensity of ultrasonication. The zeta potential values of the particles were from -43.2 ± 0.28 mV to -47.5 ± 0.42 mV showing good stability. The cumulative permeation for the smallest sized VCO-SLP (0.608 µm) was 3.83 ± 0.01 µg/cm(2) whereas for larger carriers it was reduced (3.59 ± 0.02 µg/cm(2)). It is concluded that SLP have the potential to be exploited as a micro/nano scale cosmeceutical carrying vehicle for improved dermal delivery of VCO.
    Matched MeSH terms: Drug Compounding/methods
  10. Fulltext Electrodeposition of Ginseng/Polyaniline Encapsulated Poly(lactic-co-glycolic Acid) Microcapsule Coating on Stainless Steel 316L at Different Deposition Parameters
    Lukman SK, Al-Ashwal RH, Sultana N, Saidin S
    Chem Pharm Bull (Tokyo), 2019;67(5):445-451.
    PMID: 31061369 DOI: 10.1248/cpb.c18-00847
    Electrodeposition is commonly used to deposit ceramic or metal coating on metallic implants. Its utilization in depositing polymer microcapsule coating is currently being explored. However, there is no encapsulation of drug within polymer microcapsules that will enhance its chemical and biological properties. Therefore, in this study, ginseng which is known for its multiple therapeutic effects was encapsulated inside biodegradable poly(lactic-co-glycolic acid) (PLGA) microcapsules to be coated on pre-treated medical grade stainless steel 316L (SS316L) using an electrodeposition technique. Polyaniline (PANI) was incorporated within the microcapsules to drive the formation of microcapsule coating. The electrodeposition was performed at different current densities (1-3 mA) and different deposition times (20-60 s). The chemical composition, morphology and wettability of the microcapsule coatings were characterized through attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM) and contact angle analyses. The changes of electrolyte colors, before and after the electrodeposition were also observed. The addition of PANI has formed low wettability and uniform microcapsule coatings at 2 mA current density and 40 s deposition time. Reduction in the current density or deposition time caused less attachment of microcapsule coatings with high wettability records. While prolonging either one parameter has led to debris formation and melted microcapsules with non-uniform wettability measurements. The color of electrolytes was also changed from milky white to dark yellow when the current density and deposition time increased. The application of tolerable current density and deposition time is crucial to obtain a uniform microcapsule coating, projecting a controlled release of encapsulated drug.
    Matched MeSH terms: Drug Compounding/methods
  11. Fulltext Effect of supercritical fluid density on nanoencapsulated drug particle size using the supercritical antisolvent method
    Kalani M, Yunus R
    Int J Nanomedicine, 2012;7:2165-72.
    PMID: 22619552 DOI: 10.2147/IJN.S29805
    The reported work demonstrates and discusses the effect of supercritical fluid density (pressure and temperature of supercritical fluid carbon dioxide) on particle size and distribution using the supercritical antisolvent (SAS) method in the purpose of drug encapsulation. In this study, paracetamol was encapsulated inside L-polylactic acid, a semicrystalline polymer, with different process parameters, including pressure and temperature, using the SAS process. The morphology and particle size of the prepared nanoparticles were determined by scanning electron microscopy and transmission electron microscopy. The results revealed that increasing temperature enhanced mean particle size due to the plasticizing effect. Furthermore, increasing pressure enhanced molecular interaction and solubility; thus, particle size was reduced. Transmission electron microscopy images defined the internal structure of nanoparticles. Thermal characteristics of nanoparticles were also investigated via differential scanning calorimetry. Furthermore, X-ray diffraction pattern revealed the changes in crystallinity structure during the SAS process. In vitro drug release analysis determined the sustained release of paracetamol in over 4 weeks.
    Matched MeSH terms: Drug Compounding/methods
  12. Effect of Gum Arabic, β-Cyclodextrin, and Sodium Caseinate as Encapsulating Agent on the Oxidative Stability and Bioactive Compounds of Spray-Dried Kenaf Seed Oil
    Chew SC, Tan CP, Nyam KL
    J Food Sci, 2018 Sep;83(9):2288-2294.
    PMID: 30074623 DOI: 10.1111/1750-3841.14291
    Kenaf seed oil is prone to undergo oxidation due to its high content of unsaturated fatty acids, thus microencapsulation stands as an alternative to protect kenaf seed oil from the adverse environment. This study primarily aimed to evaluate the oxidative stability of microencapsulated refined kenaf seed oil (MRKSO) by the use of gum arabic, β-cyclodextrin, and sodium caseinate as the wall materials by spray drying. Bulk refined kenaf seed oil (BRKSO) and MRKSO were kept at 65 °C for 24 days to evaluate its oxidative stability, changes of tocopherol and tocotrienol contents, phytosterol content, and fatty acid profile. The results showed that the peroxide value, p-Anisidine value, and total oxidation value of BRKSO were significantly higher than the MRKSO at day 24. The total tocopherol and tocotrienol contents were reduced 66.1% and 56.8% in BRKSO and MRKSO, respectively, upon the storage. There was a reduction of 71.7% and 23.5% of phytosterol content in BRKSO and MRKSO, respectively, upon the storage. The degradation rate of polyunsaturated fatty acids in BRKSO was higher than that of MRKSO. This study showed that the current microencapsulation technique is a feasible way to retard the oxidation of kenaf seed oil.

    PRACTICAL APPLICATION: There is increasing research on the functional properties of crude kenaf seed oil, but the crude kenaf seed oil is not edible. This study offered in developing of microencapsulated refined kenaf seed oil by spray drying, which is suitable for food application. The microencapsulation of refined kenaf seed oil with healthier wall materials is beneficial in developing a diversity of functional food products and supplements.

    Matched MeSH terms: Drug Compounding/methods*
  13. Fulltext Eco-friendly synthesis of silver nanoparticles and its larvicidal property against fourth instar larvae of Aedes aegypti
    Ali ZA, Roslan MA, Yahya R, Wan Sulaiman WY, Puteh R
    IET Nanobiotechnol, 2017 Mar;11(2):152-156.
    PMID: 28476997 DOI: 10.1049/iet-nbt.2015.0123
    In this study, larvicidal activity of silver nanoparticles (AgNPs) synthesised using apple extract against fourth instar larvae of Aedes aegypti was determined. As a result, the AgNPs showed moderate larvicidal effects against Ae. aegypti larvae (LC50 = 15.76 ppm and LC90 = 27.7 ppm). In addition, comparison of larvicidal activity performance of AgNPs at high concentration prepared using two different methods showed that Ae. aegypti larvae was fully eliminated within the duration of 2.5 h. From X-ray diffraction, the AgNP crystallites were found to exhibit face centred cubic structure. The average size of these AgNPs as estimated by particle size distribution was in the range of 50-120 nm. The absorption maxima of the synthesised Ag showed characteristic Ag surface plasmon resonance peak. This green synthesis provides an economic, eco-friendly and clean synthesis route to Ag.
    Matched MeSH terms: Drug Compounding/methods
  14. Development of a novel direct compressible co-processed excipient and its application for formulation of Mirtazapine orally disintegrating tablets
    Loke YH, Chew YL, Janakiraman AK, Lee SK, Uddin ABMH, Goh CF, et al.
    Drug Dev Ind Pharm, 2024 Jan;50(1):36-44.
    PMID: 38149637 DOI: 10.1080/03639045.2023.2294095
    INTRODUCTION: Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited.

    OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs.

    METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation.

    RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min.

    CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.

    Matched MeSH terms: Drug Compounding/methods
  15. Development and evaluation of omeprazole pellets fabricated by sieving-spheronization and extrusion - spheronization process
    Karim S, Baie SH, Hay YK, Bukhari NI
    Pak J Pharm Sci, 2014 May;27(3):425-38.
    PMID: 24811797
    Pelletized dosage forms can be prepared by different methods which, in general, are time consuming and labor intensive. The current study was carried out to investigate the feasibility of preparing the spherical pellets of omeprazole by sieving-spheronization. An optimized formulation was also prepared by extrusion-spheronization process to compare the physical parameters between these two methods. The omeprazole pellets were consisted of microcrystalline cellulose, polyvinylpyrrolidone K 30, sodium lauryl sulphate and polyethylene glycol 6000. The omeprazole delay release system was developed by coating the prepared pellets with aqueous dispersion of Kollicoat 30 DP. The moisture content, spheronization speed and residence time found to influence the final properties of omeprazole pellets prepared by extrusion-spheronization and sieving-spheronization. The Mann-Whitney test revealed that both methods produced closely similar characteristics of the pellets in terms of, friability (p=0.553), flowability (p=0.677), hardness (p=0.103) and density (bulk, p=0.514, tapped, p=0.149) except particle size distribution (p=0.004). The percent drug release from the coated formulation prepared by sieving-spheronization and extrusion spheronization was observed to be 84.12 ± 1.10% and 82.67 ± 0.96%, respectively. Dissolution profiles of both formulations were similar as indicated by values of f1 and f2, 1.52 and 89.38, respectively. The coated formulation prepared by sieving-spheronization and commercial reference product, Zimore ® also showed similar dissolution profiles (f1=1.22, f2=91.52). The pellets could be prepared using sieving-spheronization. The process is simple, easy, less time- and labor-consuming and economical as compared to extrusion-spheronization process.
    Matched MeSH terms: Drug Compounding/methods*
  16. Fulltext Development and evaluation of a novel modified-release pellet-based tablet system for the delivery of loratadine and pseudoephedrine hydrochloride as model drugs
    Zeeshan F, Bukhari NI
    AAPS PharmSciTech, 2010 Jun;11(2):910-6.
    PMID: 20496016 DOI: 10.1208/s12249-010-9456-2
    Modified-release multiple-unit tablets of loratadine and pseudoephedrine hydrochloride with different release profiles were prepared from the immediate-release pellets comprising the above two drugs and prolonged-release pellets containing only pseudoephedrine hydrochloride. The immediate-release pellets containing pseudoephedrine hydrochloride alone or in combination with loratadine were prepared using extrusion-spheronization method. The pellets of pseudoephedrine hydrochloride were coated to prolong the drug release up to 12 h. Both immediate- and prolonged-release pellets were filled into hard gelatin capsule and also compressed into tablets using inert tabletting granules of microcrystalline cellulose Ceolus KG-801. The in vitro drug dissolution study conducted using high-performance liquid chromatography method showed that both multiple-unit capsules and multiple-unit tablets released loratadine completely within a time period of 2 h, whereas the immediate-release portion of pseudoephedrine hydrochloride was liberated completely within the first 10 min of dissolution study. On the other hand, the release of pseudoephedrine hydrochloride from the prolonged release coated pellets was prolonged up to 12 hr and followed zero-order release kinetic. The drug dissolution profiles of multiple-unit tablets and multiple-unit capsules were found to be closely similar, indicating that the integrity of pellets remained unaffected during the compression process. Moreover, the friability, hardness, and disintegration time of multiple-unit tablets were found to be within BP specifications. In conclusion, modified-release pellet-based tablet system for the delivery of loratadine and pseudoephedrine hydrochloride was successfully developed and evaluated.
    Matched MeSH terms: Drug Compounding/methods
  17. Development and Standardization of Moringa oleifera Leaves as a Natural Dietary Supplement
    Ali MA, Yusof YA, Chin NL, Ibrahim MN, Muneer S
    J Diet Suppl, 2019;16(1):66-85.
    PMID: 29469600 DOI: 10.1080/19390211.2018.1429517
    Moringa oleifera leaves were selected as a model due to their hundreds of health benefits. On the other hand, the powder of these leaves has exhibited poor flowability, low tensile strength, bitter taste, poor dissolution rate, and lack of information regarding dosage. These are the common hurdles and limitations in the adaptation of herbal-based medications. Therefore, a comprehensive study was planned to introduce herbal-based medicines into mainstream medicines by standardization according to the U.S. Food and Drug Administration (FDA) and international pharmaceutical standards. A Simplex Lattice Design (SLD) of Design Expert 8.0 software was used to formulate different concentrations of superdisintegrant, binder/diluent, and sweeteners. An Instron Universal Testing machine coupled with a 13 mm stainless cylindrical die was used to manufacture tablets by means of direct compression method at 20 kN applied force. Therefore, selection of excipients was made on the basis of their tensile strength, flowability, and taste-masking properties. Optimum formulation was tested on rabbits for toxicity and growth rate. All formulated tablets were evaluated on standard parameters for orally disintegrating tablets described by the Food and Drug Authority (U.S.). The optimum formulation fulfills all standard parameters such as hardness, disintegration time, friability, and dissolution rate. The present formulation showed no toxicity when tested on rabbits. The present study provides a fundamental understanding of the tableting characteristics of natural medicines. The present study provides information that will help to overcome the challenges.
    Matched MeSH terms: Drug Compounding/methods*
  18. Detrimental consequences of the paracetamol tablet elastic relaxation during ejection
    Anuar MS, Briscoe BJ
    Drug Dev Ind Pharm, 2010 Aug;36(8):972-9.
    PMID: 20515396 DOI: 10.3109/03639041003610807
    It is generally accepted that the tablet elastic relaxation during compaction plays a vital role in undermining the final tablet mechanical integrity. One of the least investigated stages of the compaction process is the ejection stage.
    Matched MeSH terms: Drug Compounding/methods
  19. Comparison of Disintegrant-addition Methods on the Compounding of Orodispersible Tablets
    Mahesparan VA, Bin Abd Razak FS, Ming LC, Uddin AH, Sarker MZI, Bin LK
    Int J Pharm Compd, 2020 3 21;24(2):148-155.
    PMID: 32196477
    Orodispersible tablets disintegrate rapidly (within 3 minutes) in the oral cavity and release the medicament before swallowing. The mode of disintegrant addition might affect the properties of orodispersible tablets. The objective of this study was to formulate and evaluate orodispersible tablets by studying different modes of disintegration addition with varying concentrations of disintegrants. The wet granulation method was used to produce the orodispersible tablets. Two methods of disintegration addition were compared (i.e., intragranular, extragranular). Three disintegrants (i.e., cornstarch, sodium starch glycolate, crospovidone) were used at three levels (5%, 10%, and 15%) in the study. The formulations were tested for the powder flowability (angle of repose) and characterized physically (hardness, weight, thickness, friability, disintegration time). The mangosteen pericarp extract was used as a model active pharmaceutical ingredient to be incorporated into the optimum formulation. It was observed that the extragranular method produced granules with better flowability compared to that of the intragranular method. Crospovidone was found as the most efficient disintegrant among the three. The optimum formulation selected was one with the highest concentration of crospovidone (15%), which showed the fastest disintegration time. The mode of disintegrant addition into the orodispersible tablets formulation was found to show a marked difference in the disintegration, as well as other physical characteristics of the orodispersible tablets where the extragranular mode of addition showed better property, which caused the orodispersible tablets to disintegrate the fastest.
    Matched MeSH terms: Drug Compounding/methods*
  20. Fulltext Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum)
    Meka VS, Nali SR, Songa AS, Kolapalli VR
    AAPS PharmSciTech, 2012 Dec;13(4):1451-64.
    PMID: 23090110 DOI: 10.1208/s12249-012-9873-5
    The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosage form is exposed to gastrointestinal fluids in the gastric environment. As BG was being explored for the first time for its pharmaceutical application, physicochemical, microbiological, rheological, and stability studies were carried out on this gum. In the present investigation, the physicochemical properties, such as micromeritic, rheological, melting point, moisture content, pH, swelling index, water absorption, and volatile acidity, were evaluated. The gum was characterized by scanning electron microscopy, differential scanning calorimetry (DSC), powder X-ray diffraction studies (PXRD), and Fourier transform infrared spectroscopy (FTIR). Gastroretentive floating tablets of BG were prepared with the model drug propranolol HCl by direct compression methods. The prepared tablets were evaluated for all their physicochemical properties, in vitro buoyancy, in vitro drug release, and rate order kinetics. PBG 04 was selected as an optimized formulation based on its 12-h drug release and good buoyancy characteristics. The optimized formulation was characterized with FTIR, DSC, and PXRD studies, and no interaction between the drug and BG was found. Thus, the study confirmed that BG might be used in the gastroretentive drug delivery system as a release-retarding polymer.
    Matched MeSH terms: Drug Compounding/methods
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