Evaluation and Characterization of Tamarind Gum Polysaccharide: The Biopolymer.

Polymers from natural sources are widely used as excipients in the formulation of pharmaceutical dosage forms. The objective of this study was to extract and further characterize the tamarind gum polysaccharide (TGP) obtained from Tamarindus indica as an excipient for biomedical applications. Double distilled water was used as a solvent for the extraction of gum while Ethyl alcohol was used as an antisolvent for the precipitation. The results of the Hausner ratio, Carr's index and angle of repose were found to be 0.94, 6.25, and 0.14, respectively, which revealed that the powder is free-flowing with good flowability. The gum was investigated for purity by carrying out chemical tests for different phytochemical constituents and only carbohydrates were found to be present. The swelling index was found to be 87 ± 1%, which shows that TGP has good water intake capacity. The pH of the 1% gum solution was found to be neutral, approximately 6.70 ± 0.01. The ash values such as total ash, sulphated ash, acid insoluble ash, and water-soluble ash were found to be 14.00 ± 1.00%, 13.00 ± 0.05%, 14.04 ± 0.57% and 7.29 ± 0.06%, respectively. The IR spectra confirmed the presence of alcohol, amines, ketones, anhydrides groups. The contact angle was <90°, indicating favorable wetting and good spreading of liquid over the surface The scanning electron micrograph (SEM) revealed that the particle is spherical in shape and irregular. DSC analysis shows a sharp exothermic peak at 350 °C that shows its crystalline nature. The results of the evaluated properties showed that TGP has acceptable properties and can be used as a excipient to formulate dosage forms for biomedical applications.

Cardioprotective Efficacy of Silymarin Liquisolid in Isoproterenol Prompted Myocardial Infarction in Rats.

Myocardial infarction (MI) is the principal cause of death in many countries. Silymarin (SM) is a herbal antioxidant and can be efficiently used in preventing cardiovascular diseases (CVDs). The study is aimed to enhance the absorption rate and biological activity of SM by using liquisolids besides investigating the cardioprotective activity of SM and its selected liquisolid formula against isoproterenol prompted cardiotoxicity in rats. Eight formulae were prepared according to (23) full-factorial design. The effect of viscosity increasing agent type and concentration, as well as the carrier/coat ratio on the dissolution rate and angle of repose were studied. All formulae were tested for content uniformity, micromeritic properties, dissolution performance besides the evaluation of its physicochemical properties, and scanning electron microscopy (SEM). Based on the factorial design outcomes, the highest desirability was obtained from F3 with excipient ratio value (R) of 20%, dissolution rate at Q5 min of 26.9%, and angle of repose of 19. Oral administration of F3 liquisolid and SM revealed a significant protective efficacy against the modification of cardiac plasma markers, brain natriuretic peptide (BNP), interleukin-10 (IL-10), vascular endothelial growth factor (VEGF), and transforming growth factor (TGF)-ß1 besides cardiac superoxide dismutase (SOD), malondialdehyde (MDA), and total protein kinase-1 (Akt-1) levels. Additionally, they minimized cardiac inducible nitric oxide synthase (iNOS), microRNA-34a (miR-34a), and p38 mitogen-activated protein kinase (p38-MAPK) levels. In conclusion, F3 liquisolid compact possessed an overall pronounced results over pure SM reckoned to its enhanced solubility and efficacy.

A mixed solvent system for preparation of spherically agglomerated crystals of ascorbic acid.

The objective of this research was to develop a novel solvent system to prepare spherically agglomerated crystals (SAC) of ascorbic acid with improved flowability for direct compression. A spherical agglomeration method was developed by selecting the mixed solvents (n-butyl and ethyl acetate) as a poor solvent and the process was further optimized by using triangular phase diagram and particle vision measurement. Physiochemical properties of SAC were characterized and compared with original drug crystals. It showed that amount of poor solvent, ratio of solvent mixture, and drug concentration are critical for preparation of SAC with desirable properties. The solid state of SAC was same as original crystals according to DSC, XRD, and FT-IR results. There was no significant difference in solubility and dissolution rate of drug between SAC and original crystals. The flowability and packability of SAC as well as the tensile strength and elastic recovery of tablets made from SAC were all significantly improved when compared with original crystals and tablets from crystals. It is concluded that the present method was suitable to prepare SAC of ascorbic acid for direct compression.

A contemporary approach on design, development, and evaluation of Ayurvedic formulation - Triphala Guggulu.

INTRODUCTION: Ayurvedic texts describe many formulations for different ailments. Triphala Guggulu (TG) is reputed for treating inflammatory conditions. These formulations have been considered complementary medicine or alternative to conventional medicines across the globe. These complex polyherbal formulations need science-based approach toward manufacturing process and chemical standardization. AIM: To evaluate TG tablets to meet modern pharmaceutical approaches and also standardization processes. MATERIALS AND METHODS: Shodhana of Guggulu was performed using Triphala Kwatha (decoction) as mentioned in ayurvedic texts. This processed material was dried using spray drying technique, blended with other herbal powders as per formula and using suitable excipients was incorporated for compressing into tablets. Excipients and their concentrations were evaluated for various micromeritic properties and the formula that met the requirements was compressed. RESULTS: The angle of repose was considered fair with a range of 25-30, Carr's index at a range between 17 and 30, and Hausner ratio of 1.21:1.44, which was well within the limits as per the United States Pharmacopeia (USP) and among the three blends tested, blend Triphala Guggulu formulation-3 was found most suitable for tablets compression. Physical properties were well within the limits as per the USP and disintegration time was within 30 min. CONCLUSION: Modern pharmaceutical processing can very well be adapted for Guggulu preparations.

Influence of ultrafine grinding on micromeritic properties of Zhengfupian / 中草药

Objective: To study the effect of ultrafine grinding on the micromeritic properties of Zhengfupian (steamed pieces of Aconiti Lateralis Radix Praeparata) and provide the basis for its preparation and quality control. Methods: Three kinds of Zhengfupian powders were prepared by ultrafine grinding mill. Their micromeritic properties, including size distribution, surface area and porosity, flowability, scanning electronic microscope, infrared spectrum, moisture absorption and dissolution rate were detected. Then the effects were comprehensively analyzed. Results: With the increasing of grinding time, the powder's particle size decreased, morphology and structure tended to be uniform, the specific surface area and porosity increased, the particles assembled easily, the compressibility and the angle of repose increased, the dissolution rate increased dramatically, and there were no significant changes in the infrared spectrum and moisture absorption. Conclusion: As the micromeritic properties and dissolution rate of Zhengfupian are considered, Zhengfupian's ultrafine grinding time should be controlled at about 25 min, particle size d0.9 should be around 100.46 μm.

Multivariate analysis on micromeritic properties of Sarcandrae Herba Granule and its correlation with tablet compactibility / 中草药

Objective: To investigate the correlations between micromeritic primary properties and compactibility of granules produced by wet granulation of Sarcandrae Herba with soluble starch and microcrystalline cellulose (MCC). Methods: Micromeritic primary properties and compactibility of granules produced by wet granulation which was obtained by different prescriptions and processes were determined. Particle size (D90), specific surface area (SSA), pore volume (PV), moisture content (MC), bulk density (BD), tap density (TD), tap index (TI), angle of repose (AOR), and Kawakita equation parameters a and b were used as evaluation indexs to study the micromeritic primary properties of granulation. The tensile strengths of granules at 5, 10, 15, 20, 25, and 30 kN pressure were used as the indexs to evaluate the compactibility of granules produced. Multivariate analysis was applied to evaluating the correlations between micromeritic primary properties and compactibility of granules produced. Results: The micromeritic primary properties of granules could be extracted as two principal components, morphology parameter and compressibility parameter. The significant effects on the tablet compactibility are the compressibility, moisture, and surface morphology of granules produced. Conclusion: Multivariate data analysis could make the quick and easy classification of Sarcandrae Herba Granule. The correlation between granules micromeritic primary properties and tablet compactibility is given. By controlling compressibility, moisture, and surface morphology of granules produced, the tablets with good compactibility can be obtained.

Formulation and design of sustained release matrix tablets of metformin hydrochloride: Influence of hypromellose and polyacrylate polymers.

AIM: The current paper was an attempt to design a sustained release dosage form using various grades of hydrophilic polymers, Hypromellose (hydroxyl-propyl methylcellulose [HPMC] K15M, HPMC K100M and HPMC K200M) and Polyacrylate polymers, Eudragit RL100 and Eudragit RS100 with or without incorporating ethyl cellulose on a matrix-controlled drug delivery system of Metformin hydrochloride. MATERIALS AND METHODS: Laboratory scale batches of nine tablet formulations were prepared by wet granulation technique (Low shear). Micromeritic properties of the granules were evaluated prior to compression. Tablets were characterized as crushing strength, friability, weight variation, thickness, drug content or assay and evaluated for in-vitro release pattern for 12 h using Phosphate buffer of pH 6.8 at 37 ± 0.5°C. The in-vitro release mechanism was evaluated by kinetic modeling. RESULTS AND DISCUSSION: The results obtained revealed that HPMC K200M at a concentration of 26% in formulation (F6) was able to sustain the drug release for 12 h and followed the Higuchi pattern quasi-Fickian diffusion. With that, combined effect of HPMC K15M as an extragranular section and Eudragit RS100 displayed a significant role in drug release. Dissolution data were compared with innovator for similarity factor (f2), and exhibited an acceptable value of ≥50 Three production validation scale batches were designed based on lab scale best batch and charged for stability testing, parameters were within the limit of acceptance. There was no chemical interaction found between the drug and excipients during Fourier Transform Infrared Spectroscopy (FTIR) and Differential scanning calorimetry study. CONCLUSION: Hence, combinely HPMC K200M and Eudragit RS100 at a suitable concentration can effectively be used to sustain drug release.

Propriedades micromeríticas e análise físico-química de matérias-primas de alopurinol / Micromeritic properties and physicochemical analysisof allopurinol raw materials

O controle de qualidade de matérias-primas é imprescindível, pois visa assegurar a qualidade do produto acabado. O objetivo do trabalho foi avaliar a qualidade físico-química e farmacotécnica de matérias-primas de alopurinol, fármaco utilizado para a prevenção e o tratamento de crises de gota, amplamente prescrito e produzido por indústrias e farmácias magistrais. As amostras (A, B, C e D) de alopurinol oriundas de diferentes fornecedores foram submetidas a ensaios farmacopeicos (características organolépticas; solubilidade; ensaios de identificação: teste de precipitação e varredura no UV; ensaios de pureza: limpidez de solução, perda por dessecação, cinzas sulfatadas; doseamento), análise térmica (DSC, TG), análise granulométrica e determinação das propriedades de fluxo (ângulo de repouso, densidade bruta e de compactação, fator de Hausner, índice de compressibilidade e compactabilidade). As amostras foram aprovadas em todos os ensaios farmacopeicos. Nas curvas de DSC, o ponto de fusão foi de cerca de 380 °C para todas as amostras e, após a fusão houve a degradação, confirmada pelas curvas TG, com uma perda de massa de aproximadamente 100 %. A partir da distribuição granulométrica as amostras A e B foram classificadas como pós finos e as C e D como finíssimos. Os valores de ângulo de repouso caracterizaram as amostras A, B, C e D como de fluxo fraco e, o fator de Hausner e índice de compressibilidade caracterizaram as amostras como amostras de fluxo bastante deficiente. Os ensaios demonstraram-se úteis para avaliar a qualidade das amostras. A adição de adjuvantes apropriados durante o preparo das formulações de alopurinol é essencial para melhoramento do fluxo.

The quality control of raw materials is intended to ensure the quality of the finished product. The objective of this study was to carry out physicochemical and pharmacotechnical assessments of allopurinol raw materials. This drug is widely prescribed for the prevention and treatment of gout and is produced both by drug manufacturers and compounding pharmacies. Samples (A, B, C and D) from 4 different suppliers were subjected to pharmacopoeial testing (organoleptic characteristics; solubility; identification tests: precipitation and scanning UV; purity tests: clarity of solution, loss on drying, sulphated ash; assay), thermal analysis (DSC, TG), particle size analysis and flow property tests (angle of repose, bulk density and tapped density, Hausner ratio, compressibility and compactibility). The samples were approved in all the pharmacopoeial tests. In the DSC curves, the melting point was about 380 °C for all samples and after fusion there was degradation, confirmed by TG, with a weight loss of approximately 100%. From the particle size distributions, samples A and B were classified as fine powders and C and D as very fine powders. The angles of repose characterized the samples A, B, C and D as having weak flow, while the Hausner ratio and compressibility index indicated that they had very, very poor flow. The tests proved useful for assessing the quality of the samples and showed that appropriate adjuvants need to be added to the allopurinol formulations to improve the flow.

Formula and process optimization of Danggui Buxue Pellets prepared by extrusion-spheronization / 中成药

AIM: To prepare traditional Chinese medicine formula Danggui Buxue Pellets by extrusion-spheronization and to study the optimal process and formulation. METHODS: Danggui Buxue Pellets were prepared by a new style extrusion-spheronization equipment;The optimal process and formulation were obtained on the studies of influenitial factors and L_9(3~4) orthogonal design,The micromeritic properties and reception percentage of pellets were determined. RESULTS: The prepared Danggui Buxue Pellets by extrusion-spheronization were all spheral with smooth surface;The percent of reception was not less than 85%. CONCLUSIONS: Extrusion-spheronization is suitable to produce herbal medicine pellets.The preparation process is simple and feasible;The quality of the prepared pellets is excellent and the percent of reception is high.