In situ forming polymeric formulations are drug delivery systems that are in sol form before administration in the body, but once administered, undergo gelation in situ, to form a gel. The formation of gels depends on factors like temperature modulation, pH change, presence of ions and ultra violet irradiation, from which the drug gets released in a sustained and controlled manner. Various polymers that are used for the formulation of in situ gels include gellan gum, alginic acid, xyloglucan, pectin, chitosan, poly(DL-lactic acid), poly(DL-lactide-co-glycolide) and poly-caprolactone. The choice of solvents like water, dimethylsulphoxide, N-methyl pyrrolidone, triacetin and 2-pyrrolidone for these formulations depends on the solubility of polymer used. Mainly in situ gels are administered by oral, ocular, rectal, vaginal, injectable and intraperitoneal routes. The in situ gel forming polymeric formulations offer several advantages like sustained and prolonged action in comparison to conventional drug delivery systems. The article presents a detailed review of these types of polymeric systems, their evaluation, advancements and their commercial formulations. From a manufacturing point of view, the production of such devices is less complex and thus lowers the investment and manufacturing cost.

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A simple, accurate, economical and reproducible HPLC method has been developed for quantitative estimation of metformin hydrochloride from tablet dosage form and formulated microspheres. The developed HPLC method is a reverse phase chromatographic method using phenomenex C ₁₈ column and acetonitrile:phosphate buffer (65:35) pH adjusted to 5.75 with o-phosphoric acid as mobile phase and glipizide as internal standard. The linearity was observed in concentration range of 0-25 μg/ml for metformin hydrochloride. Results of analysis were validated statistically and by recovery studies.

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Natural resources in general and plant materials in particular are receiving more attention due to their safety as pharmaceutical excipients. Present work assessed the potential of a natural polysaccharide, pectin to mask the bitter taste of ambroxol hydrochloride, by microencapsulation technique, and its possibility to formulate as a fast disintegrating dosage form. Taste masking is an important developmental challenge in fast dissolving drug delivery system since it dissolves or disintegrates in the patient's mouth in close proximity to the taste buds. The prepared microspheres by emulsion solvent evaporation technique possessed good sphericity, smooth surface morphology, uniform and narrow size distribution (10-90 μm), when analyzed by scanning electron microscopy, laser diffraction and optical microscopy. Method of preparation has influenced the particle size and drug loading efficiency. Drug-polymer compatibility was confirmed by Fourier transform infrared spectroscopy and thin layer chromatography. DSC and X-ray diffraction studies revealed that the drug was dispersed inside the microspheres in the form of an insoluble matrix. The formation of microspheres was affected by glass transition temperature of the polymer, surfactant, type of plasticizers, volume of internal phase, stirrer speed etc. Fast dissolving tablets were prepared by the modification of melt granulation technique. The resulting granules were found to melt fast at body temperature, have smooth mouth feel and good physical stability. This study demonstrated that pectin could be a right choice in developing patient favored formulations for bitter drugs and can be utilized in fast disintegrating dosage forms as well.

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The aim of the present study was the determination of formulation factors and the in vitro evaluation of an extended release dosage form of a freely soluble weakly basic drug (alfuzosin hydrochloride). Binary mixer of one hydrophilic polymer (hydroxypropylmethylcellulose) and one directly compressible Eudragit (RS PO) was used in tablets prepared by direct compression. The amounts of both polymers were taken as independent variables for the 3 ² Factorial design. The percent drug releases at 1, 6, 12 and 20 h were selected as responses. The main effect and interaction terms were quantitatively evaluated using mathematical model. Dissolution data were fitted to zero order, first order, and Higuchi's release kinetics to evaluate kinetic data. Both the diffusion and erosion mechanisms were responsible for drug release as shown by the power law. The release of Alfuzosin was prolonged for 20 h by binary mixer indicating the usefulness of the formulations for once daily dosage forms.

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A sensitive and accurate UV spectrophotometric method with multivariate calibration technique for the determination of metformin hydrochloride in bulk drug and different pharmaceutical formulations has been described. This technique is based on the use of the linear regression equations by using relationship between concentration and absorbance at five different wavelength. The results were treated statistically and were found highly accurate, precise and reproducible. The method is accurate, precise (% recovery 102.50΁0.063, CV≤0.56, r =0.997) and linear within the range 1-10 mg/ml. There was no interference from the excipients i.e Povidone K 30, magnesium stearate, lactose and hydroxypropylmethylcellulose. This statistical approach gives optimum results for the eliminating fluctuations coming from instrumental or experimental conditions.

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The present study was aimed to develop once daily extended release matrix tablets of minocycline hydrochloride, using hydroxypropylmethylcellulose either alone or in combination with ethyl cellulose as the matrix material in different proportions. The formulated tablets were also compared with a marketed product. The results of the dissolution study indicate that formulations FC-IV, FC-V and FC-VI showed maximum drug release upto 24 h, whereas the marketed product was found to extend the release only up to 14 h. Incase of formulations containing combination of hydroxypropylmethylcellulose and ethyl cellulose (FC-I to FC-IX), the release of the drug was found to be dependent on the relative proportions of hydroxypropylmethylcellulose and ethyl cellulose used in the tablet matrix. Mathematical treatment of the in vitro drug release data suggests that, all the formulations best fitted into first order release kinetics. Drug release from the matrix occurred by combination of two mechanisms, diffusion of drug from tablet matrix and erosion of tablet surface, which was reflected from Higuchi's model and Erosion plot.

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The purpose of the present work was to prepare buccal adhesive tablets of miconazole nitrate. The simplex centroid experimental design was used to arrive at optimum ratio of carbopol 934P, hydroxypropylmethylcellulose K4M and polyvinylpyrollidone, which will provide desired drug release and mucoadhesion. Swelling index, mucoadhesive strength and in vitro drug release of the prepared tablet was determined. The drug release and bioadhesion was dependent on type and relative amounts of the polymers. The optimized combination was subjected to in vitro antifungal activity, transmucosal permeation, drug deposition in mucosa, residence time and bioadhesion studies. IR spectroscopy was used to investigate any interaction between drug and excipients. Dissolution of miconazole from tablets was sustained for 6 h. based on the results obtained, it can be concluded that the prepared slow release buccoadhesive tablets of miconazole would markedly prolong the duration of antifungal activity. Comparison of in vitro antifungal activity of tablet with marketed gel showed that drug concentrations above the minimum inhibitory concentration were achieved immediately from both formulations but release from tablet was sustained up to 6 h, while the gel showed initially fast drug release, which did not sustain later. Drug permeation across buccal mucosa was minimum from the tablet as well as marketed gel; the deposition of drug in mucosa was higher in case of tablet. In vitro residence time and bioadhesive strength of tablet was higher than gel. Thus the buccoadhesive tablet of miconazole nitrate may offer better control of antifungal activity as compared to the gel formulation.

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The terahertz gap has a frequency ranges from ~0.3 THz to ~10 THz in the electromagnetic spectrum which is in between microwave and infrared. The terahertz radiations are invisible to naked eye. In comparison with x-ray they are intrinsically safe, non-destructive and non-invasive. Terahertz spectroscopy enables 3D imaging of structures and materials, and the measurement of the unique spectral fingerprints of chemical and physical forms. Terahertz radiations are produced by a dendrimer based high power terahertz source and spectroscopy technologies. It resolves many of the questions left unanswered by complementary techniques, such as optical imaging, Raman and infrared spectra. In the pharmaceutical industries it enables nondestructive, internal, chemical analysis of tablets, capsules, and other dosage forms. Tablet coatings are a major factor in drug bioavailability. Therefore tablet coatings integrity and uniformity are of crucial importance to quality. Terahertz imaging gives an unparalleled certainty about the integrity of tablet coatings and the matrix performance of tablet cores. This article demonstrates the potential of terahertz pulse imaging for the analysis of tablet coating thickness by illustrating the technique on tablets.

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The present study was conducted to assess the attitudes and behaviors of practicing community pharmacists towards patient counselling and use of patient information leaflets in the state of Karnataka. Convenient sampling method was adopted to collect the responses with the help of self-completion questionnaires. A total of 258 practicing community pharmacists in the age group of 22-60 y of both gender with practicing experience of 2-30 y participated in the study. Majority of respondents (80%) agreed that, patient counselling is their professional obligation. About 17% of the respondents mentioned that, they try to give basic information regarding drug usage to the patient. The reasons stated by the pharmacists to provide patient counselling were, professional satisfaction (43%), patients go with satisfaction (32%), observed increase in sales (8%), and also improved patient compliance (7.5%). The major barriers for offering patient counselling were mentioned as pharmacists' inadequate knowledge and confidence (78%), doctor dispensing (72%), no professional fee (56%), poor response from patients (82%), inadequate continuous professional development programs (75%). Many respondents agreed that, patient information leaflets certainly help in counselling but available information leaflets are company generated and prescriber focused. Many respondents found the present continuing professional development module was useful and are interested in weekend workshops to update their professional knowledge (83%). Restrictions on doctor dispensing, legalization of patient counselling, regular continuing professional development programs are the factors observed to motivate the pharmacists to offer patient counselling.

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The aim of the present study was to monitor adverse drug reactions associated with antihypertensive drugs. The study was conducted in medicine out patient department of 150-bed Majeedia Hospital at Hamdard University Campus in New Delhi. The study was conducted by way of one to one patient interview by a registered pharmacist using a questionnaire-based Adverse Drug Reaction Monitoring Form drafted according to the World Health Organisation Monitoring Guidelines. A total of 34 adverse drug reactions were observed in 250 hypertensive patients during the four month study. A high percentage of adverse drug reactions occurred in middle aged and female patients. Of the 34 adverse drug reactions, 18 (52.9%) were mild, 14 (41.2%) moderate and only 2 (5.8%) were classified as severe. Combination therapy was associated with significantly high occurrence (P < 0.05) of adverse drug reactions, with a total of 21 (61.8%) as compared to monotherapy (n=13, 38.2%). Cardiovascular adverse drug reactions constituted a major component, followed by gastrointestinal and respiratory complaints. Beta-blockers were the drug category associated with majority of adverse drug reactions, followed by angiotensin-converting enzyme inhibitors and calcium channel blockers. The above pharmacovigilance study presents the adverse drug reaction profile of antihypertensive medicines prescribed in our University Teaching Hospital. It was concluded that calcium channel blockers were the most frequently prescribed drug category but beta blockers were associated with higher frequency of adverse drug reactions.

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A gelatin and sodium alginate complex coacervation system was studied and an effect of pH and colloid mixing ratios on coacervation was investigated. A colloid mixing ratio at which optimum coacervation occurred varied with the coacervation pH. Viscometric, turbidity and coacervate dry yield investigations were used to investigate optimum conditions for complex coacervation. Optimum coacervation occurred at pH 3.5 at a gelatin sodium alginate ratio 4:1. Coacervate and equilibrium fluid was analyzed for gelatin and sodium alginate contents and yields calculated on the basis of chemical analysis showed that optimum coacervation occurred at 25% sodium alginate fraction at pH 3.5.

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The free radical scavenging potential of the plant Alocasia indica (Linn.) was studied by using different antioxidant models of screening like scavenging of 1,1-diphenyl-2-picryl hydrazyl radical, nitric oxide radical, superoxide anion radical, hydroxyl radical, iron chelating activity, total antioxidant capacity, non-enzymatic glycosylation of haemoglobin, rapid screening for antioxidant compounds by thin layer chromatography. The hydroalcoholic extract at 1000 ΅g/ml showed maximum scavenging of superoxide radical (87.17) by riboflavin-NBT-system, followed by scavenging of stable radical 1,1-diphenyl-2-picryl hydrazyl radical (83.48%), nitric oxide radical (74.09%) hydroxyl radical (60.96%) at the same concentration. However the extract showed only moderate activity by iron chelation (68.26%). That could be due to higher phenolic content in the extract. This finding suggests that hydro alcoholic extract of A. indica possess potent in vitro antioxidant activity as compared to the standard ascorbic acid. The results justify the therapeutic applications of the plant in the indigenous system of medicine, augmenting its therapeutic value.

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Three simple, accurate and economical methods have been developed for the estimation of norfloxacin and ornidazole in tablet dosage form. First method is based on the simultaneous equations, wavelengths selected for analysis were 273.0 nm (λ_max of norfloxacin) and 318.5 nm (λ_max of ornidazole), respectively, in 0.1N NaOH. Second method is Q-analysis method, based on absorbance ratio at two selected wavelengths 297.0 nm (iso-absorptive point) and 318.5 nm (λ_max of ornidazole). Third method is first order derivative spectroscopy using 297.5 nm (zero cross for norfloxacin) and 264.0 nm (zero cross for ornidazole). The linearity was obtained in the concentration range of 4-20 μg/ml and 5-25 μg/ml for norfloxacin and ornidazole, respectively. The results of the analysis have been validated statistically and by recovery studies.

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Ethanol extract of roots of Sida cordifolia was evaluated for antistress, adaptogenic activity using cold restraint stress and swim endurance in mice. Mice pretreated with extract of Sida cordifolia showed significant improvement in the swim duration and reduced the elevated WBC, blood glucose and plasma cortisone.

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In Iranian folk medicine, Perovskia abrotanoides is used for treatment of leishmaniasis. These patients may develop secondary infections with opportunistic microorganisms. Therefore, the antimicrobial activity of essential oil from aerial part of P. abrotanoides and its main components was evaluated against different microorganisms. Disc diffusion and broth micro dilution assays were used for in vitro antimicrobial screening. The antibacterial activity of this oil and main components on viability of S. aureus was determined. The oil showed antimicrobial activity against Candida albicans and Gram positive bacteria especially Staphylococcus aureus with zone inhibitions and minimal inhibitory concentration values in the range of 7.6 to 29 mm and 2 to 8 μl/ml respectively, whereas the least susceptible were Aspergillus niger and Gram negative bacteria. In viability test, the results showed that the antimicrobial activity of 1,8-cineole was more than that of α-pinene and camphor but after 60 min this effect gradually decreased only for 1,8-cineole and ultimately the antibacterial activity of camphor was more than that of α-pinene. 1,8-cineole had weak antimicrobial activity against all of the tested microorganisms. Hence the use of P. abrotanoides oil could be useful in fighting secondary infections in leishmaniasis especially against S. aureus.

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The naturally occurring xanthone glycoside mangiferin has been isolated by column chromatography from the ethanol extract of stem bark of Mangifera indica. Mangiferin was further converted to 5-(N-phenylaminomethyleno)mangiferin, 5-(N-p-chlorophenylaminomethyleno) mangiferin, 5-(N-2-methylphenylaminomethyleno) mangiferin, 5-(N-p-methoxyphenylaminomethyleno) mangiferin, 5-(N,N-diphenylaminomethyleno) mangiferin, 5-(N--napthylaminomethyleno) mangiferin and 5-(N-4-methylphenylaminomethyleno) mangiferin. Mangiferin and its analogues were characterized by melting point and R _f value determination and through spectral technique like UV, IR, and NMR spectral analysis. The synthesized compounds were screened for antimicrobial activity.

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In the present investigation 0.5 M ibuprofen sodium solution has been used as hydrotropic solubilizing agent for naproxen, a poorly water-soluble drug and in it there was more than 350 fold enhancement in the solubility of naproxen as compared to the solubility in distilled water. Therefore, this hydrotropic solution was employed to extract out the drug from its tablet dosage form for quantitative estimation by titrimetry. The naproxen has been successfully analyzed in tablets. The results of analysis obtained by proposed method compared well with those by corresponding British pharmacopoeial method involving the use of methanol. The proposed method was also validated by recovery studies. Presence of ibuprofen sodium and common excipients did not interfere in analysis. Proposed method is new, simple, economic, safe, rapid, accurate, reproducible and environment-friendly.

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The unique anatomical arrangement of blood vessels and sinuses in the human skull and the brain, the prevalence of a high density of skin appendages in the scalp, extracranial vessels of the scalp communicating with the brain via emissary veins and most importantly, the way that the scalp is used in Ayurvedic medical system in treating diseases associated with the brain show that a drug could be transcranially delivered and targeted to the brain through the scalp. The present study was to investigate by measuring the antinociceptive effect on rats whether the opioid analgesic methadone could be delivered and targeted to the brain by transcranial delivery route. A non aqueous solution of methadone base in sesame oil was used for the application on the scalp. Animal studies were carried out using six groups of male rats consisting of group 1, the oral control treated with distilled water 1 ml; group 2, the oral positive control treated with methadone hydrochloride solution 316.5 μg/ml; group 3, the negative control treated transcranially with the blank sesame oil 0.2 ml and three test groups 4, 5 and 6 treated with three different dose levels of the transcranial oil formulation of methadone base, 41.6 μg/0.2 ml, 104 μg/0.2 ml and 208 μg/0.2 ml, respectively. The antinociceptive effects were examined by subjecting the rats to the hot plate and tail flick tests. The two higher concentrations of the three transcranial methadone formulations yielded response vs time curves showing nearly equal maximum antinociceptive effects similar to that of the oral positive control. Maximum analgesic effect after transcranial administration was observed between 1st and 2nd h and declined up to 6th hour. The results indicate that the transcranial brain targeted delivery of methadone base in the form of an oil based non aqueous solution results in statistically significant antinociceptive effects under experimental conditions. Therefore, it is possible to deliver central nervous system drugs through the proposed transcranial route when suitably formulated.

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Ethanol extract of Passiflora edulis Sims was analyzed for its antioxidant (1,1-diphenyl-2-picryl hydrazyl radical reducing power methods) and phytochemical analysis. The extract was found effective against the antioxidant test models exhibiting an IC ₅₀ value of 875΁87.83 ΅g/ml and showed strong potential antioxidant activity in both assays.

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A simple, precise and rapid HPLC method has been developed and validated for the estimation of quinapril and hydrochlorothiazide simultaneously in combined dosage form. The mobile phase used was a mixture of 0.1% v/v triethylamine (pH 3.5), containing 1 mM of hexane sulphonic acid: acetonitrile (30:70% v/v). The detection of quinapril and hydrochlorothiazide was carried out on photo diode array detector at 220 nm. Results of the analysis were validated statistically and by recovery studies. The proposed method can be successfully used to determine the drug contents of marketed formulation.

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Based on principles of pharmacophore delineation and drug designing, compounds containing diketofunctionallity namely 1,2-bis[5-thiazolyl]ethane-1,2-diones were designed and synthesized as antiinflammatory agents. The compounds were evaluated in carrageenan-induced rat-paw edema method. G-3, G-6, G-17, G-20, G-23, G-22, L-708 and 906 showed good antiinflammatory activity. In addition as diketo functionality containing compounds are reported to have HIV-1 integrase inhibitory property, and these compounds contains diketo functionality, so these compounds were screened in assay for HIV-1 integrase inhibition. Few compounds showed weak HIV-1 integrase Inhibitory activity.

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The in vitro anticandidal activity of Asparagus racemosus roots and tubers extract was investigated against Candida albicans, Candida tropicalis, Candida krusei, Candida guillermondii, Candida parapsilosis and Candida stellatoida, which are isolated from vaginal thrush patients. The extract of Asparagus racemosus showed high degree of activity against all the Candida strains. The inhibitory effect of the extract against all the Candida tested was found comparable with that of standard antibiotics used.

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The aim of the present study was to establish antihistamines drug prescribing pattern in order to improve the rational prescribing of antihistamines by physicians at Panjab University Health Centre. The study was performed in between the months of November 2005 to April 2006. Five hundred out patients were monitored and data was collected on WHO-based prescription-auditing performa. Demographic analysis of this prospective study revealed that out of the 500 patients, 293 (58.6 %) were male and 207 (41.4 %) were female and maximum patients were in the age group of 21-40 (34.8 %). Chlorpheniramine maleate (235 prescriptions) was the highest prescribed among antihistamine prescriptions (36.89 %) followed by diphenhydramine hydrochloride (186 prescriptions, 29.19%), cetirizine (175 prescriptions, 27.47 %) and promethazine (41 prescriptions, 6.4%). In comparison to generic drugs (169 prescriptions, 26.54%), branded were more prescribed at PUHC. Majority of antihistamines were in form of tablets (414 prescriptions, 64.99%) followed by liquid formulations (195 prescriptions, 30.61%) and injections (28 prescriptions, 4.40%). The average cost of different antihistamine drugs prescribed was as follows: diphenhydramine hydrochloride Rs. 34.74 followed by promethzine Rs. 22.46, chlorpheniramine maleate Rs. 15.30, and cetirizine Rs. 13.50. Average numbers of drugs prescribed per prescription were 1.27. The average consulting and dispensing time was 4.82 and 3.56 min, respectively. Out of the 500 university patients, 258 (51.6%) had the knowledge regarding the medication prescribed and 242 (48.4%) were unaware of the medication prescribed.

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The present study was designed to investigate the effect of folic acid on homocysteine, lipid profile and hematological changes in methionine-induced hyperhomocysteinemic rats. Hyperhomocysteinemia was induced by methionine (1 g/kg, p.o.) administration for 30 days. Biochemical and hematological observations were further substantiated with histopathological examination. The increase in homocysteine, total cholesterol, low density lipoprotein-cholesterol, very low density lipoprotein-cholesterol and triglycerides levels with reduction in the levels of high density lipoprotein in serum were the salient features observed in methionine treated toxicologic control rats (i.e. group II). Hematological observations of the peripheral blood smears of toxicologic rats also showed crenation of red blood cells membrane and significant (P<0.01) increase in total leukocyte count, differential leukocyte count and platelet counts with significant (P<0.01) decrease in the mean hemoglobin levels, as compared to vehicle control rats. Administration of folic acid (100 mg/kg, p.o.) for 30 days to methionine- induced hyperhomocysteinemic rats produced a significant (P<0.01) decrease in the levels of homocysteine, total cholesterol, low density lipoprotein-cholesterol, very low density lipoprotein-cholesterol and triglycerides with significant (P<0.01) increase in high density lipoprotein-cholesterol levels in serum when compared with toxicologic control rats. The present study, for the first time, investigates the effect of folic acid treatment on hematological changes in rats with methionine-induced hyperhomocysteinemia.

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Ayurvedic powders are widely used as therapeutic agents but most of them have unpleasant taste and large doses. One of the possible approach to overcome these drawbacks is to represent them in unit dosage form i.e. tablet dosage form. The purpose of this study is to elucidate and quantify the compressibility and compactibility of herbal granules prepared by using hydrogel isolated from whole seeds of Ocimum basilicum as a novel binder. The compressibility is the ability of the powder to deform under pressure and the compactibility is the ability of a powder to form coherent compacts. To test the functionality of novel excipients, Sonnergaard proved a simple linear model to confirm compactability, which is an uncomplicated tool for quantification. The tablets were compressed at increasing compression pressures and were evaluated for various mechanical properties. The linear relationship between specific crushing strength and compression pressure revealed the compactibility of the herbal granules and the linear relationship between porosity and logarithm of compression pressure revealed the compressible nature of the herbal granules according to the model developed by Sonnergaard. Thus the hydrogel isolated from whole seeds of Ocimum basillicum had potential as a granulating and binding agent.

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