Posted by admin on Dec 31, 2019 in |
Solid dispersions (SDs) of Erlotinib hydrochloride (ETN) were prepared to enhance the solubility by solvent evaporation (SE) and Melting (MM) method using poloxamer 188 (PL 188) in the ratio of 1:1, 1:3 and 1:5 (w:w). The solubility of the drug was increased in a concentration-dependent manner of polymer and follow linearity order. The solid dispersion was characterized by Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). The FTIR spectra revealed the drug was found compatible and did not show any interaction with polymer, PXRD spectra, and DSC thermographs showed a clear transformation of crystalline to an amorphous form of drug particles. In-vitro dissolution study was performed in dissolution medium i.e. 0.1N HCl (pH 1.2). Cumulative percent drug release from SDs prepared by the SE method was faster than from the pure drug, physical mixture (PM), and SDs prepared by the MM method. The maximum percent drug release (90.07 ± 0.78) was found with PL 188 in the ratio of 1:5 (w/w). Among the...
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Posted by admin on Dec 31, 2019 in |
Ethylacetate leaf extract of Aganosma cymosa was screened for antimalarial activities in-vivo in rats inoculated with red blood cells parasitized with Plasmodium falcipuram using 4-day Suppressive test and Rane’s test. The result of mean parasitemia by 4-day Suppressive test for the Group AC600, AC400 & AC200 was 4.62 ± 3.63, 13.34 ± 2.42, 19.29 ± 3.23 and percentage suppression were 80.1%, 42.54% and 16.9% respectively. However, standard drug chloroquine (15 mg/kg) was found to exert a considerable lower percentage parasitemia of 2.73 ± 1.6 and higher percentage suppression of 88.24%. From the results of the Ranes test, the parasitemia levels on day 7 for AC200, AC400, AC600 were 16 ± 0.4, 12 ± 0.4 and 2 ± 0.6 and the percentage inhibition was found to be 23.80, 45.45 and 65 respectively. While the chloroquine treated group had a mean parasitemia 6 ± 0.2 and percentage inhibition of 70%.The plant extracts showed significant dose-dependent antiplasmodial activity with the decrease in parasitemia, rectal temperature, body weight and increase in suppression, packed cell volume in all treated...
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Posted by admin on Dec 31, 2019 in |
The main objectives of the present study were to design, optimization and evaluation of buccal drug delivery system of propranolol for hypertension treatment. Propranolol is non-selective β-adrenergic blockers. It shows first-pass metabolism so its bioavailability is decreased and its absolute bioavailability is only about 26%. The buccal tablets of propranolol formulated, by using different mucoadhesive polymers such as sodium crosscarmilose sodium, PVP K30, and HPMC K15M. F8 was containing 18.18% PVPK30, 10.90% HPMC K15M showed desired drug release within 6 h to above batches. The dissolution profile of formulated batch F1 to F8 at the end of 6 h was found in the range of 83.03 to 94.69% in phosphate buffer pH 6.8. From the results, it was found that formulation F8 was shown most similar dissolution profile because the similarity value was found to be above 90%. The swelling index was found higher in formulation F9 80.15% swelling observed because of higher concentration of PVP K30 and HPMC K15M. The results indicate that out of two bioadhesive polymers...
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Posted by admin on Dec 31, 2019 in |
Cymbopogon olivieri (Poaceae) is a native plant to the south of Iran and is used for the treatment of some inflammative based disorders and as a pain killer. Regarding the presence of volatile terpenoids in the aerial parts, we were prompted to investigate the analgesic and anti-inflammatory activities of the essential oil from C. olivieri in animal models. The oil was also analyzed by GC and GC–MS to identify the potentially responsible compounds for observed properties. The analgesic activity of the oil was assessed by acetic acid-induced writhing test and hot plate method while the acute anti-inflammatory effect was investigated by induced-inflammatory paw edema in the rat. The studied oil could decrease the number of acetic acid-induced writhes in mice compared with animals that received vehicle only. In hot-plate tests, the studied doses of C. olivieri were not effective. The oil moderately reduced carrageenan-induced paw edema in rats. The major component of the oil was characterized as Piperitone (66.0%), which might be responsible for these observed activities. The results...
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Posted by admin on Dec 31, 2019 in |
The vast investigations on the derivatives of 1, 2, 3-benzotriazole explore wide applicability for tagging and delivering a number of other heterocyclic nuclei with benzotriazole. In the present work, several derivatives of 1-(substituted)-5- [(N-benzotriazolo-methyl)-1, 3, 4-thiadiazolyl]- imidazole-2-thione have been synthesized and are evaluated for their anticonvulsant activity. The anticonvulsant activities of the synthesized derivatives were assessed by the maximal electroshock (MES) method. Electric shock (50 mA for 0.2 sec) was delivered with the help of a corneal electrode to induce hind limb tonic extension. The synthesized derivatives X2, X3 and X6 exhibited significant anticonvulsant effect against MES-induced seizure model as an indication for compounds which are effective in grand mal...
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