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Quarterly published in print and online "Inventi Impact: Novel Excipients" publishes high quality unpublished as well as high impact pre-published research and reviews catering to the needs of researchers and professionals. It focuses on new pharmaceutical excipients from natural and synthetic origin. Articles pertaining to excipients for conventional dosage forms as well as novel drug delivery systems and nano-medicines are welcome.
The profound use of synthetic and semi-synthetic polymers now-a-days has resulted in overlooking of natural substances that are readily available, economic, and has least adverse effects. In this research work Metroxylon sagu Rottb. and Vigna mungo Hepper are evaluated for their sustain release property by varying concentration in formulation of Diclofenac sodium. The release patterns of formulated tablets were found to be in equivalence with marketed formulation. The results of this research concluded that Metroxylon sagu Rottb. and Vigna mungo Hepper., could be better alternative for synthetic polymers....
A principle aim of this study was to establish the correlation between real time and accelerated in-vitro degradation of biodegradable polymer film composed of poly-L-lactic acid (PLLA) polymer. The effort of establishment of this correlation was to determine feasibility of carrying out accelerated in-vitro degradation study as a substitute of real time degradation study which was proven to be more time consuming. A degradation behavior of biodegradable PLLA polymer was evaluated on each stage of total degradation period up to six month and 15 days for real time and accelerated respectively during in-vitro degradation under simulated environment condition. Various series of samples were employed for study and degradation progress was investigated based on the change in mass loss, molecular weight, crystallinity and visual observation at each interval during degradation period by comparing with initial results. Reasonable evidence of results for degradation progress suggests the implementation of accelerated in-vitro degradation study as a fast quality control tool of PLLA properties evaluation....
Tacrolimus is an immunosuppressive agent for acute rejection after allotransplantation.\nHowever, the low aqueous solubility of tacrolimus poses difficulties in formulating an injection\ndosage. Polypeptide thermosensitive hydrogels can maintain a sustained release depot to deliver\ntacrolimus. The copolymers, which consist of poloxamer and poly(l-alanine) with l-lysine segments\nat both ends (P-Lys-Ala-PLX), are able to carry tacrolimus in an in situ gelled form with acceptable\nbiocompatibility, biodegradability, and low gelling concentrations from 3 to 7 wt %. By adding\nPluronic F-127 to formulate a mixed hydrogel system, the drug release rate can be adjusted to maintain\nsuitable drug levels in animals with transplants. Under this formulation, the in vitro release of\ntacrolimus was stable for more than 100 days, while in vivo release of tacrolimus in mouse model\nshowed that rejection from skin allotransplantation was prevented for at least three weeks with one\nsingle administration. Using these mixed hydrogel systems for sustaining delivery of tacrolimus\ndemonstrates advancement in immunosuppressive therapy....
The present study explores the pharmaceutical potential of a natural organic matter (fulvic acid) for sustained\r\nrelease, acid buffering capacity and mucoadhesion in vaginal drug delivery. The antifungal drug, Itraconazole,\r\nwas first converted into inclusion complexes with fulvic acid (1:1 & 1:2 molar ratio) and then characterized by\r\nDifferential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), Fourier Transform Infrared\r\nSpectroscopy (FT IR) and Mass Spectroscopy. Results were also authenticated by conformational analysis.\r\nSolubility analysis of complexes yielded different thermodynamic parameters and explained the driving force\r\nfor solubilisation when the pH was varied in an acidic range. MTT assays were also performed to assess the\r\npotential in vitro cell toxicity of the complexes in comparison to the neat drug. The complexes were then\r\nformulated into tablets and optimized for hardness, mucoadhesion and release profiles. The optimized tablets\r\npresented with satisfactory mucoadhesion, acid buffering and spreading ability. Moreover, the antifungal\r\nactivity of the formulation was also increased due to improved aqueous solubility of the drug despite the\r\nlarger size of the complex. The study also indicated the potential use of fulvic acid as a functional excipient in\r\nthe preparation of a vaginal drug delivery system (VDDS)....
The current aim of our research work is to isolate the biomaterial from fruit pulp of Annona squamosa and evaluate its binding ability. The fruit pulp was subjected for isolating the biomaterial in a simplified and economic process. Using this biomaterial, granules were prepared taking diclofenac as a model drug. The granules were evaluated through various parameters like flowability, compressibility index, dispersibility, particle size, particle shape, hausner index, disintegration test, friability, angle of repose, bulk density and breaking strength. The research results revealed that the formulated granules using biomaterial show free flowing property with optimum breaking strength, significant dispersibility, and sufficient compressibility comparable to standard granules prepared using starch. Hence it can serve as novel potential biobinder for formulating tablets....
The objective of the present research is to evaluate directly compressible chitosan-based
tableting materials for the formulation of mucoadhesive matrix tablets intended for targeted drug
release to distal segments of the GIT. The influence of sodium alginate, hypromellose, and silicified
microcrystalline cellulose (P90) on compressibility, compactability and lubricant sensitivity ratio was
tested. Furthermore, the rheological properties of the hydrated surface layer of the matrix tablets
and the mucoadhesion to a mucin substrate were analysed. Compressibility was evaluated using
the energy profile of the compression process, compactability by means of the tensile strength of
tablets, and lubricant sensitivity ratio was calculated to assess the sensitivity to lubricant. Addition
of P90 to chitosan improved compressibility, which is demonstrated by the increase in the energy of
plastic deformation and the higher tensile strength of tablets. P90 also significantly reduced the high
lubricant sensitivity of chitosan. Presence of retarding components led to a decrease in Emax. All
tested matrix tablets revealed a good mucoadhesion without a negative effect of P90 content. The
viscosity of a gel layer on the surface of matrix tablets containing hypromellose was higher compared
to those with sodium alginate. This was not reflected in the adhesive strength of the tablets. The
formulated tableting materials combining chitosan and P90 are a suitable matrix for incorporation of
an active ingredient, whose delayed release in the intestine can be achieved by the functionality of
the chitosan-sodium alginate complex....
Lornoxicam tablets were prepared by conventional wet granulation method using various binding agents. Lornoxicam, a widely prescribed non steroidal anti-inflammatory drug with analgesic properties, belonging to the oxicam class. The objective of the present work was to study the effect of various binding agents on qualities and dissolution rate of lornoxicam tablets. Compressed tablets each containing 8 mg of lornoxicam were prepared using various binders namely acacia, tragacanth, gelatin, xantham gum, HPMC K4M, PVP K30, PVA and MCC. The effects of binding agents on the physical characteristics of lornoxicam granules were studied. The granules were evaluated for angle of repose, bulk density, compressibility index and the tablets were evaluated for content of active ingredient, hardness, friability, disintegration time, dissolution rate. The binder used has significant influence on the tablet and rate of lornoxicam release from the tablets....
Taro Boloso-I (TB1), a newly improved Colocasia esculenta variety, is a potential source of starch with high yield. However, to\nimprove some limitations of the native starches (NS), such as flowability and compactibility, different physical and chemical starch\nmodifications have been employed. Acetylation is one of the chemical modifications which improves the flow and compaction of the\nNS, which are prerequisite during direct compression (DC) of tablets. Hence, in this study, TB1 starch was acetylated using acetic\nanhydride and evaluated as an ideal excipient for direct compression. Starch acetates (SA) with a degree of substitution (DS) of 0.072\n(SA1) and 0.695 (SA2) were produced and evaluated. FTIR spectra of the SAs were used to verify the acetylation of the NS. Powder\nflow evaluation parameters showed significant improvement in the flow properties of the NS following acetylation. In addition, the\nswelling power, solubility, and compactibility were also improved. Tensile strength (TS) of the tablets comprising SAs only, SA1\n(41.40) and SA2 (63.43 Kg/cm2), was significantly higher than tablets made of the NS (31.96) and Starch 1500Â® (15.12 Kg/cm2). The SAs\nalso showed lower sensitivity towards lubrication than the NS and Starch 1500Â® as lower lubricant sensitivity ratios were recorded. In\naddition, tablets comprising the SAs satisfactorily accommodated at least up to 50% w/w paracetamol-compared to 30 %w/w by Starch\n1500Â®-upon DC processing. The paracetamol tablets comprising SAs also complied with the United States Pharmacopeia specifications\nfor disintegration and dissolution studies. Therefore, taking all the facts into consideration, the SAs could be potential DC excipients in\ntablet formulations....
Research in natural polymeric materials has witnessed growing interest and attention. This is attributable to a number of factors which include their relative abundance, low cost, and biodegrable and eco-firendly profiles. This article reviews the current applications of natural polymeric materials in pharmaceutical formulations. The pharmaceutical applications of some of the traditional and commercially available natural polymers were discussed. Emerging potential pharmaceutical excipients of natural origins were also discussed. The increasing research interests in this group of materials are indications of their increasing importance. It is believed that as technology and testing techniques advance, more understanding of their physicochemical nature would be gained that can enable them to be tailored for wider Pharmaceutical applications than their synthetic counterparts....
The aim of this study is to evaluate the adhesion ability of okra gum, which is gaining\npopularity as a tablet binder. For this purpose, gum was extracted from okra pods, and the binding\nstrength of different concentrations (1%, 3%, and 5%) was determined quantitatively. Additionally,\nnaproxen sodium tablets were prepared by using okra gum as a binder and were evaluated for\ntheir properties including hardness, friability, disintegration time, and dissolution rate. The binding\nstrength values were compared with that of pre-gelatinized starch, a commonly used tablet binder.\nThe results from universal testing machine indicate that the binding strengths of all dispersions of okra\nincrease as the concentration increases from 1% to 5% and ranges from 2.5 to 4.5 N, which are almost\ntwice a high as those of pre-gelatinized starch. The tablets prepared with okra gum have shown good\nmechanical strength with hardness values of 7Ã¢â?¬â??8.5 kg/cm2 and a friability <1%, comparable to tablets\nprepared with starch. The disintegration time was longer (7.50 min with okra gum and 5.05 min with\nstarch paste), and the drug release from these tablets was slower than the formulations with starch.\nThe higher binding ability of okra gum probably linked with its chemical composition as it mainly\ncontains galactose, rhamnose, and galacturonic acid. This study concludes that okra gum is a better\nbinder than pre-gelatinized starch, it might be explored in future for introduction as a cost-effective\nbinder in the pharmaceutical industry....
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