Verapamil was encapsulated with ethylcellulose (EC) and cellulose acetate (CA) in various ratios of drug and polymer by the hot melt technique and the prepared microcapsules were evaluated for size range, drug content, drug release profiles, and kinetics of drug release. The microcapsules were compressed into tablets to study the variation of drug release between the 2 types of formulations (ie, microcapsules and tablets). The size analysis of prepared microcapsules was done by a standard sieving method and in vitro dissolution studies were carried out in USP XXI dissolution test apparatus in 0.1 N HCl as dissolution media to study the drug release profiles of the microcapsules. Scanning electron microscopy studies were carried out to investigate the surface characteristics of the microcapsules prepared from both type of polymers. Drug release profiles from the compressed non-disintegrating matrix tablets prepared from the microcapsules were also investigated. All the microcapsules were discrete, free flowing, and reproducible with respect to size distribution and drug content. Maximum percentage of the microcapsules belonged to the size range of 35/50. Drug release durations of VERCA1 (drug: CA 3:1), VERCA2 (drug: CA 2:1), and VERCA3 (drug: CA 1:1) microcapsules were extended up to 3, 5, and 6 hours, respectively, and those of VEREC1 (drug: EC 3:1), VEREC2 (drug: EC 2:1), and VEREC3 (drug: EC 1:1) microcapsules were extended up to 4, 5, and 7 hours, respectively. The microcapsules of both types having a drug:polymer ratio of 1:1 had the slowest release rate in their respective categories. The microcapsules were compressed into nondisintegrating matrix tablets. The hardness of the tablets was tested using the Monsanto Hardness Tester and was found to be 6-7 kg/cm. All the tablets contained the drug verapamil within 100% +/- 5%. The drug release data of both the microcapsules and tablets prepared were examined kinetically, and the ideal kinetic model was determined for the drug release. The tablets prepared by compressing the microcapsule formulations were more satisfactory in releasing the drug at a controlled and uniform rate following Higuchian kinetics and the formulations VCACRT3 and VECCRT3 were able to control release of drug up to 12 hours. Thus, it is possible to formulate a single-unit, controlled-release dosage form of verapamil for oral administration at least once every 12 hours using the polymers CA and EC.
SUMMERYThe present study was carried out to elucidate the potential of, chloroform extract of Pandanus (P.) fascicularis Lamk (Family-Pandanaceae) leaves on antinociceptive, behavioral study and antiinflammatory effects using various animal models The dried, powdered leaves of, P. fascicularis were extracted successively with petroleum ether (60 -80°C) and chloroform in soxhlet apparatus. The chloroform extract (yield 21.6% w/w with respected to dry powdered plant material) was selected for all experimental procedure. Two models were employed to investigate the effects on nociception, the tail immersion and hot plate method in Swiss albino mice and anti inflammatory effect were investigated by employing the carrageenan induced rat paw edema test in. adult Wister albino rats. Behavioral study was investigated by elevated plus maze method in Swiss albino mice. Results were revealed that the PFCE was found significant antinociceptive effect (P < 0.001) at the dose levels of 100, 200 and 400 mg/kg, orally in mice and produced remarkable antiinflammatory effect (P < 0.001) at the same dose levels used in the rats. Behavioral study of the PFCE has no significant anxiolysis effect when used orally. It concludes that, PFCE possessed remarkable antinociceptive effect and anti-inflammatory effect but no anxiolytic effect on animal models.
Topical application of cream prepared from the chloroform extract of Croton sparsiflorus Morong were formulated and evaluated for its efficacy and safety. Creams were prepared at different concentrations i.e. 5%, 7.5% and 10% (w/w) by fusion method using different excipients. These topical formulations were tested for pH, viscosity, spreadability and drug contents uniformity. The stability study was carried out at 4, 25 and 37 0 C. The drug content uniformity of creams was found within the range of 98.09 to 98.21%. All the formulations were evaluated for its acute skin irritancy, wound healing activity in Swiss Albino rats. These formulations did not produce any skin irritation for about a week when applied over the skin. Comparative studies showed that the viscosity of the formulations increases, spreadability decreases and vice versa. From the stability studies, creams showed no changes in properties after keeping at different temperatures for 90 days. All the formulations and the normal chloroform extracts of C. sparsiflorus Morong showed significant (P<0.001) wound healing activity by excision wound model and comparable with that of the reference standards and control bases. The measurement of the wound areas were taken on 3rd, 6th, 9th, 12th, 15th and 18th days and the percentages of wound closures were calculated.
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