Understanding impact of pre-dissolved polymers on dissolution behavior of soluble carbamazepine cocrystal.

Cocrystallization is a novel approach for tackling the lower solubility concerns when they can yield solution concentration a lot better than their corresponding parent drug in crystalline form. To get the actual solubility and dissolution gains offered by the cocrystals, phase changes in solution (dissolution) has to be interrupted. In current study, we selected commonly used polymers in order to study their effects on the super saturation of carbamezepine-succinic acid (CBZ-SUC) cocrystal during dissolution studies. To observe solid phase changes during dissolution in situ Raman spectroscopy was used. At the completion of each test the solid phase was analyzed by Fourier-transform infrared spectroscopy (FTIR) and powder X-Ray diffractometry. In polymers absence, no dissolution improvement was achieved by the cocrystal owing to its quick transformation to the stable carbamazepine dihydrate (CBZDH). Pre-dissolved PVP at 2% w/v concentration did not inhibit CBZ crystallization as a dihydrate, whereas at 0.025% w/v pre-dissolved hydroxypropyl methyl cellulose acetate succinate (HPMCAS) did stabilize the cocrystal in buffer solution (pH 6.8) for the course of time studied. This cocrystal stabilization resulted in enhanced CBZ solubility ( Ì´ 4fold) caused by cocrystal super saturation state. Seeding of this stable supersaturated state with 1% w/v CBZDH resulted in CBZ crystallization as dihydrate with ultimate loss of solubility advantage.

Evaluation of different Pakistani medicinal plants for inhibitory potential against Echis carinatus induced Phospholipase A2 toxicity.

Medicinal plants of Pakistan are known for their curative properties against snake bite as rural people have been using natural herbs for such injuries for hundreds to thousands of years. People of rural areas of Pakistan are prone to snakebite, and on the whole death due to snakebite has been increasing worldwide. The objective of this study was to test the neutralizing potential of 17 Pakistani medicinal plant extracts against phospholipase A2 activity in Echis carinatus venom. Plant material was extracted by simple maceration and fractionation of active plant extracts. Venom was collected by manual massage of the venom glands. The PLA2 enzymatic assay was performed to map out the venomous activity of Echis carinatus envenomation. Snake venom released fatty acids at different concentrations (0.1-5 mg/ml) of venom in a dose-dependent manner. Reduction of pH by 01 correlated with 133 µmol of fatty acids released at 5mg/ml of venom. All plants extract inhibited PLA2 activity, however, Curcuma longa, Citrullus colocynthis and Rubia cordifolia inhibited maximum of PLA2 activity (⁓78%) comparable to the standard antidote (p>0.5). Medicinal plants possess secondary metabolites and many active compounds that may have neutralizing or inhibiting properties against the PLA2 activity of Echis venom. Further studies such as compound analysis could provide an alternative against snakebites injuries resulting from Echis carinatus venom.

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.

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.