Muhammad N. Aamir

Development and in vitro–in vivo relationship of controlled-release microparticles loaded with tramadol hydrochloride

In conclusion, the controlled-release microparticles of TmH can be developed via phase separation method. The development and optimization of controlled-release microparticles of tramadol hydrochloride (TmH) for the oral delivery and their in vitro and in vivo correlation was prime objective of the present study. Four formulations of controlled-released microparticles were developed and optimized in terms of encapsulation efficiency, dissolution study and release kinetics. Among all formulated microparticles F-3 (ratio of TmH:EC 1:2) and F-4 (ratio of TmH:EC 1:3) presented the better characteristics in reference to entrapment efficiency, release kinetics and dissolution profile compared to other formulations (F-1, F-2). For in vivo analysis a new HPLC analytical method was developed and validated. The optimized formulations were subjected to in vivo studies to calculate various pharmacokinetic parameters, i.e., C(max), t(max), AUC(0-∞) and MRT. The in vitro dissolution and in vivo absorption data was correlated with the help of Wagner-Nelson method. F-3 showed a good in vitro-in vivo correlation with a correlation determination of 0.9957. Moreover, lower T(max), t(1/2) and MRT, and higher values of C(max) and K(e) were observed for F-3. The control formulation (immediate-release) presented lowest values of t(1/2), MRT and T(max) but the highest values of C(max) and K(e). The controlled-release microparticles (F-3 and F-4) could sustain the drug release within therapeutic level up to 24 h and good IVIVC is expected from them.

Production and Stability Evaluation of Modified-Release Microparticles for the Delivery of Drug Combinations

Production and evaluation of novel formulations of tizanidine and tramadol microparticles was the chief purpose of this project. Microparticles of both drugs were prepared separately via temperature change method. To extend the release of formulations, ethyl cellulose was employed. Higuchi, zero-order, first-order, and Korsmeyer–Peppas kinetic models were applied to appraise the mechanism and mode of drugs release. Higuichi model was found to be best for all release profiles. Stability of microparticles at 40°C/75% RH over a 3-month duration was determined by Fourier transform infrared (FTIR), X-ray diffractometry (XRD), and drugs assay. Microparticles were compatible and stable as no significant differences were observed when subjected to drug assay, FTIR, and XRD during accelerated stability studies.

Development of a sebum control cream from a local desert plant Capparis decidua

The aim of this study was to develop a stable cream from a local desert plant capable of producing Antisebum effects. Two creams (emulsions) were prepared, both of which were of w/o type. One was the formulation in which 5% extract obtained from the plant Capparis decidua was added during the preparation of the cream and the other was the base or control in which the extract was not added while other ingredients were the same as that of the formulation. Thirteen healthy male volunteers were selected and their initial sebum readings of both the cheeks were noted with the help of Sebumeter. The volunteers were given both the creams and asked to apply the creams on the face daily two times, the base on the right side and the formulation on the left side. The readings were taken every fifteen days for a period of three months. At the end of the study period, it was found that the formulation significantly decreased the sebum values on the left side. On the other hand, an increase in the sebum values was observed on the right side where the base was applied, although the increase was not significant statistically. The results showed that the cream prepared from the local desert plant C. decidua had the ability to produce Antisebum effects in the human volunteers.

Bioequivalence assessment of two formulations of celecoxib: Open label, single dose and two-way cross over study in healthy human male volunteers

The purpose of this study was to assess bioequivalence of two marketed formulations of celecoxib capsules in healthy human male volunteers. The study was conducted according to a single dose, randomized sequence, open label, two-period and crossover design. Both test and reference formulations comprised labeled dose of 200 mg celecoxib and were administered to each subject after an overnight fasting on two treatment days separated by one week of washout period. After drug administration, blood samples were collected at predetermined time points for a period of 48 h. Plasma separated from blood was analyzed for celecoxib concentrations using validated reverse phase-high performance liquid chromatographic (RP-HPLC) method. Various pharmacokinetic parameters including C