Evaluation of Antidiabetic Potential of Ipomoea turpethum R.Br. and Ipomoea batata L. (Convolvulaceae) in Alloxan Induced Diabetes in Rats: A Comparative Study

ABSTRACT In order to explore the intra-genera variation for biological activity, the antidiabetic activity of Ipomoea turpethum and Ipomoea batata was carried out in alloxan induced diabetes in rats. Dried powdered material of both plants was defatted with petroleum ether 60-80 °C and cold macerated with hydro-ethanol for seven days. These extracts were screened for antidiabetic activity using alloxan induced diabetes in rats. Diabetes was induced by intra-peritoneal administration of alloxan monohydrate (120 mg/kg) on days 1 and 12 and blood glucose levels were estimated on 15 th day. Hydro-ethanol extracts of both the plants at the dose of 500 mg/kg, oral, significantly lowered the blood glucose levels in diabetic rats treated for 7 days. The antidiabetic activity of these plants was insignificantly different from each other. This suggests that, different species from same genera may have similar chemical constituents and pharmacological activity

Influence of the Component Excipients on the Quality and Functionality of a Transdermal Film Formulation

The influence of formulation variables, i.e., a hydrophilic polymer (Methocel® E15) and a film-forming polymer (Eudragit® RL 100 and Eudragit® RS 100), on the physicochemical and functional properties of a transdermal film formulation was assessed. Several terpenes were initially evaluated for their drug permeation enhancement effects on the transdermal film formulations. d-Limonene was found to be the most efficient permeation enhancer among the tested terpenes. Transdermal film formulations containing granisetron (GRN) as a model drug, d-limonene as a permeation enhancer, and different ratios of a hydrophilic polymer (Methocel® E15) and a film-forming polymer (Eudragit® RL 100 or Eudragit® RS 100) were prepared. The prepared films were evaluated for their physicochemical properties such as weight variation, thickness, tensile strength, folding endurance, elongation (%), flatness, moisture content, moisture uptake, and the drug content uniformity. The films were also evaluated for the in vitro drug release and ex vivo drug permeation. The increasing ratios of Methocel®:Eudragit® polymers in the formulation linearly and significantly increased the moisture content, moisture uptake, water vapor transmission rate (WVTR), and the transdermal flux of GRN from the film formulations. Increasing levels of Methocel® in the formulations also increased the rate and extent of the GRN release and the GRN permeation from the prepared films

Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir

The influence of the ratio of Eudragit® L100-55 or Kolliphor® P188 on the solubility, dissolution, and permeability of ritonavir was studied with a goal of preparing solid dispersions (SDs) of ritonavir. SDs were formulated using solvent evaporation or lyophilization techniques, and evaluated for their physical-chemical properties. The dissolution and permeability assessments of the functionality of the SDs were carried out. The preliminary functional stability of these formulations was assessed at accelerated storage conditions for a period of six months. Ritonavir: Eudragit® L100-55 (RE, 1:3) SD showed a 36-fold higher ritonavir solubility compared to pure ritonavir. Similarly, ritonavir: Kolliphor® P188 (RP, 1:2) SD exhibited a 49-fold higher ritonavir solubility compared to pure ritonavir. Ritonavir dissolution from RE formulations increased with increasing ratios of Eudragit® L100-55, up to a ritonavir: carrier ratio of 1:3. The ritonavir dissolution from RP formulations was highest at ritonavir: Kolliphor® P188 ratio of 1:2. Dissolution efficiencies of these formulations were found to be in line with, and supported the dissolution results. The permeability of ritonavir across the biological membrane from the optimized formulations RE (1:3) and RP (1:2) were ~76 % and ~97 %, respectively; and were significantly higher compared to that of pure ritonavir (~20 %). A preliminary (six-month) stability study demonstrated the functional stability of prepared solid dispersions. The present study demonstrates that ritonavir solubility, dissolution, and permeability improvement can be achieved with a careful choice of the carrier polymer, and optimizing the amount of polymer in a SD formulation

Antidiabetic Potential of Fractions of Hydro-Ethanol Extract of Cyperus rotundus L. (Cyperaceae)

ABSTRACT Traditional systems of medicine reported the use of Cyperus rotundus in the treatment of diabetes. To substantiate this claim, investigations were carried out using hydro-ethanol extract and the same has been reported (Raut and Gaikwad, 2006). Present study evaluated the antidiabetic activity of fractions of hydro-ethanol extract of C. rotundus. Dried powdered material of C. rotundus was defatted with petroleum ether 60-80 °C, cold macerated with hydro-ethanol for seven days and then fractionated successively in Soxhlet apparatus with chloroform, ethyl acetate, acetone and methanol. These fractions were screened for antidiabetic activity using alloxan induced diabetes in rats. Diabetes was induced by intra-peritoneal administration of alloxan monohydrate (120 mg/kg) on days 1 and 12 and blood glucose levels were estimated on 15 th day. Various oral doses were tried and significant antidiabetic activity (p<0.001) was found at a dose of 300 mg/kg in acetone fraction and residue left after successive fractionation. The activities of active extracts were comparable to metformin (450 mg/kg, per oral). The results suggested that, fractions possess antidiabetic activity attributed to the presence of polyphenols and flavonoids

DEVELOPMENT OF ULTRAVIOLET-SPECTROPHOTOMETRIC METHOD FOR ANALYSIS OF AMOXAPINE IN PHARMACEUTICAL DOSAGE FORM

 Objective: Knowing the exact amount of active pharmaceutical ingredient (API) in pharmaceutical dosage form is of utmost importance to meet regulatory requirements and to ensure patient safety. Spectrophotometric analysis provides a simple, efficient, and economic approach for estimation of API in the pharmaceutical dosage form. In the present work, we have developed simple, sensitive, and highly economic ultraviolet (UV) spectrophotometric method for the estimation of amoxapine in a pharmaceutical formulation.Methods: Amoxapine shows maximum absorbance of light at wavelength 297 nm in water. The linearity study revealed that it obeys Beer-Lambert's law over the range of 2–20 μg/mL. Absorptivity value of amoxapine was found to be 206.6±1.341.Result: The tablet formulation was successfully analyzed by developed UV spectrophotometric method. The developed method was validated as per International Conference on Harmonization guidelines with respect to accuracy, precision, specificity robustness . The limit of detection and limit of quantitation was found to be 19.8 and 60.50 ng/mL, respectively.Conclusion: The developed method is simple, precise, accurate, and cost-effective and can be used for routine analysis of amoxapine

Excipient Variability and Its Impact on Dosage Form Functionality

Pharmaceutical excipients are essential components of most modern dosage forms. Although defined as pharmacologically inert, excipients can be thought of as the true enablers of drug product performance. Unintentional variability in the properties of the excipients may be unavoidable, albeit minimizable. The variability may originate from the source, the excipient-manufacturing process, or during the manufacturing of dosage forms. Excipient variability may have a range of influences on their functionality and performance in the dosage form. A better understanding of these influences on the critical quality attributes of the final product is of prime importance. Modern analytical tools provide a significant assistance in characterizing excipient variability to achieve this understanding. The principles and concepts of Quality-by-Design, process analytical technology, and design space, provide a holistic risk-based approach toward manufacture and application of excipients in pharmaceutical formulations. The International Pharmaceutical Excipients Council (IPEC) has developed guidelines for proper selection, use, and evaluation of excipients in pharmaceutical products. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association

Influence of carrier (polymer) type and drug-carrier ratio in the development of amorphous dispersions for solubility and permeability enhancement of ritonavir.

The influence of the ratio of Eudragit® L100-55 or Kolliphor® P188 on the solubility, dissolution, and permeability of ritonavir was studied with a goal of preparing solid dispersions (SDs) of ritonavir. SDs were formulated using solvent evaporation or lyophilization techniques, and evaluated for their physical-chemical properties. The dissolution and permeability assessments of the functionality of the SDs were carried out. The preliminary functional stability of these formulations was assessed at accelerated storage conditions for a period of six months. Ritonavir: Eudragit® L100-55 (RE, 1:3) SD showed a 36-fold higher solubility of compared with pure ritonavir. Similarly, ritonavir:Kolliphor® P188 (RP, 1:2) SD exhibited a 49-fold higher solubility of ritonavir compared to pure ritonavir. Ritonavir dissolution from RE formulations increased with increasing ratios of Eudragit® L100-55, upto a ritonavir:carrier ratio of 1:3. The ritonavir dissolution from RP formulations was highest at a ritonavir:Kolliphor® P188 ratio of 1:2. Dissolution efficiencies of these formulations were found to be in line with, and supporting the dissolution results. The permeability of ritonavir across the biological membrane from the optimized formulations RE (1:3) and RP (1:2) were ~76 % and ~97 %, respectively; and were significantly higher compared to that of pure ritonavir (~20 %). A preliminary (six-month) stability study demonstrated the functional stability of prepared solid dispersions. The present study demonstrates that a good solubility, dissolution, and permeability improvement of ritonavir can be achieved with a careful choice of the carrier polymer, and by optimizing the amount of the chosen polymer in an SD formulation

Influence of carrier (polymer) type and drug-carrier ratio in the development of amorphous dispersions for solubility and permeability enhancement of ritonavir.

The influence of the ratio of Eudragit® L100-55 or Kolliphor® P188 on the solubility, dissolution, and permeability of ritonavir was studied with a goal of preparing solid dispersions (SDs) of ritonavir. SDs were formulated using solvent evaporation or lyophilization techniques, and evaluated for their physical-chemical properties. The dissolution and permeability assessments of the functionality of the SDs were carried out. The preliminary functional stability of these formulations was assessed at accelerated storage conditions for a period of six months. Ritonavir: Eudragit® L100-55 (RE, 1:3) SD showed a 36-fold higher solubility of compared with pure ritonavir. Similarly, ritonavir:Kolliphor® P188 (RP, 1:2) SD exhibited a 49-fold higher solubility of ritonavir compared to pure ritonavir. Ritonavir dissolution from RE formulations increased with increasing ratios of Eudragit® L100-55, upto a ritonavir:carrier ratio of 1:3. The ritonavir dissolution from RP formulations was highest at a ritonavir:Kolliphor® P188 ratio of 1:2. Dissolution efficiencies of these formulations were found to be in line with, and supporting the dissolution results. The permeability of ritonavir across the biological membrane from the optimized formulations RE (1:3) and RP (1:2) were ~76 % and ~97 %, respectively; and were significantly higher compared to that of pure ritonavir (~20 %). A preliminary (six-month) stability study demonstrated the functional stability of prepared solid dispersions. The present study demonstrates that a good solubility, dissolution, and permeability improvement of ritonavir can be achieved with a careful choice of the carrier polymer, and by optimizing the amount of the chosen polymer in an SD formulation