Formulation of sumatriptan succinate orodispersible tablets using chitosan and sodium starch glycolate for immediate migraine relief.

Migraine is one of the common neurological disease affecting around 23% of the Pakistani population. Prompt treatment is required to regain the functional ability of patients. The present study was designed to develop sumatriptan succinate orodispersible tablets that would quickly overcome acute migraine episodes using 22 full-factorial design. The chitosan and sodium starch glycolate were taken as independent variables; friability, disintegration, dispersion time and water absorption ratio as response variables. Eight trial formulations were generated by Design Expert® software. The main effect plots were used to check the interaction of formulations with response variables. All trial formulations showed good micromeritic properties in terms of angle of repose (19.59o-24.57°), Carr's index (17.08-24.90%) and Hausner's ratio (1.20-1.33). The tablets wetted quickly (17.1- 39 sec) in dispersion medium, showed higher water absorption ratio (188-341 sec) and disintegrated quickly (13-20 sec) with an excellent dissolution rate (94-99%). The main effect plots show interactions between the independent variables against most of the study responses. A 22 full-factorial model was found to be effective in studying the influence of formulation variables on response parameters. Both chitosan and sodium starch glycolate can be used in combination to fabricate an effective orodispersible formulation of sumatriptan succinate.

Formulation optimization, in vitro characterization and stability studies of sustain release tablets of Ketoprofen.

The aim of the current study was to formulate sustain release (SR) tablets of ketoprofen. Five batches (batch I -V) of matrix based ketoprofen tablet were prepared by dry granulation method using hydroxyl propyl methyl cellulose (15000cps). Compatibility of formulation excipients with drug was explored through FT-IR technique. Various physical and chemical parameters of all tablet batches were evaluated with multi-point dissolution profile (for 24hrs) for formulation optimization. Release kinetics of trials was estimated by model dependent and independent methods. Formulations having excellent quality attributes were then compared with marketed ketoprofen SR tablets. Accelerated stability study was also conducted to compute the shelf life of the optimized formulation. FT-IR scans illustrated the compatibility of ketoprofen with all tablet excipients. On the basis of testing results and controlled release pattern batch II was set to be an optimized trial having shelf life of 37 months. All trial batches (batch I-V) and the marketed brand exhibited highest linearity towards zero order and Korsmeyer-Peppas model with non-fickian anomalous transport (n=0.541-0.655).

Development of quality standard and phytochemical analysis of Carica papaya Linn leaves.

Carica papaya Linn is the member of Caricaceae family of Kingdom Plantae. The study was executed for the development of qualitative standards of male and female leaves of the plant. The study included evaluation of macroscopial, physico-chemical and preliminary phytochemical parameters to authorize the purity and authenticity of leaf of Carica papaya Linn based on guidelines provided by WHO. Qualitative phytochemical screening of extracts revealed the existence of alkaloids, flavonoids, tannins, phenolic compounds, glycosides including cardiac glycosides, proteins and carbohydrate in different extracts of Carica papaya Linn which are majorly rich in female leaves as compared to male. Mean ash values, acid insoluble ash, water soluble ash, foaming index, swelling index and moisture contents were also evaluated which are more or less similar. FTIR profile of the samples were also generated that confirmed distinct peak values with respective functional groups exhibited by Carica papaya male and female plant. The current research reflected that female and male plant showed variations in phyto-constituents. This data will be utilized for additional Pharmacological and Instrumental evaluation of the plant which can not only be beneficial in discriminating and refining the type as well as nature of various phytochemicals present in Carica papaya male and female leaves but also establish the quality standards for future researches.

Development and validation of HPLC method for the determination of pioglitazone in human plasma.

Pioglitazone is widely used for the management of type-II diabetes mellitus. The objective of the present study was to develop a simple and cost-effective HPLC method for the quantification of pioglitazone in human plasma. The mobile phase comprises of Acetonitrile, 0.1 M ammonium acetate and glacial acetic acid (25:25:1 v/v/v) at a flow rate of 1.2 mL/min., using Macherey-Nagel Column C18, (dimensions: 5 µm; 250 × 4.6mm) with a guard column. The UV detector was set at 269nm. The method was validated according to FDA guidelines. The present method showed good linearity (R2=0.9998) from 0.1 to 2.0µg/ml standards, with a limit of detection 0.1 µg/ml. Intra-day accuracy and precision in terms of %CV (range: 93.33% to 100.4% and 3.8% to 9.2%) and interday accuracy and precision (range: 94.1% to 102.7% and 4.8% to 9.6%) were in agreement with FDA guidelines. Freeze thaw stability showed that the plasma samples could be stored for one month at -20oC without any appreciable degradation. The present method was successfully applied to the blood samples obtained from one volunteer after oral administration of 30 mg pioglitazone tablet. Some preliminary pharmacokinetic parameters were calculated. It is concluded that the present method could be conveniently used for the routine analysis of pioglitazone blood samples obtained in pharmacokinetics studies.

Effects of various excipients on tizanidine hydrochloride tablets prepared by direct compression.

This study was conducted to assess the effects of various excipients in 10 different Tizanidine hydrochloride tablet dosage forms that were prepared by direct compression method (DC). Various excipients are available for DC method; we selected those excipients that are used commonly in tablet manufacturing. The excipients used included lactose anhydrous, di-basic calcium phosphate anhydrous, starch, talc, sodium carboxy methyl cellulose, polyvinyl pyrrolidone (PVP), silicon dioxide (Aerosil), stearic acid, magnesium stearate and microcrystalline cellulose (Avicel). These tablets were then evaluated by performing different pharmacopoeial and non-pharmacopoeial tests (i.e. diameter, hardness, thickness, weight variation, disintegration and assay). It was observed that Formulations B, D and H of Tizanidine hydrochloride gave best results within USP specified limits for the tests employed among all the formulations whereas Formulations F and G showed poor friability, disintegration and dissolution profiles rendering starch in combination of talc and sodium carboxy-methyl cellulose unsuitable for Tizanidine hydrochloride tablet formulations. With the present approach, more studies can be designed using other active ingredients and excipients to get an optimal and cost effective product.

Evaluation and comparison of different brands of domperidone tablets available in Karachi, Pakistan.

Domperidone is an anti-dopaminergic drug used for the treatment of nausea, vomiting and dyspepsia. It has also been used in Parkinson's disease. In this study, five different brands of Domeperidone tablets were selected from the local market for evaluation of their quality as the local market is occupied of many competitors for a single generic. The evaluation of Domperidone tablets was done using various pharmacopoeial and non-pharmacopoeial tests. All the test results fell within BP specified limits for all the selected brands i.e. the results for Brands A to E for weight variation, thickness and diameter were satisfactory and within limits. For Brands A to E, the results for hardness and friability were also satisfactory i.e. 4-10kg/cm2and 0.1-0.6% respectively. The results for Brands A to E for disintegration were 2-6 minutes; for dissolution and assay, the results were 89-92% and 95-99% respectively. The results of similarity factor (f2) also showed that all brands of Domperidone have comparative dissolution profiles.