stability

Teneligliptin hydrobromide hydrate is a new FDA approved drug for treatment of Diabetes Mellitus. Very few methods have been reported for its identified degradation products and their effects on human. A simple, rapid, precise and accurate stability indicating RP-HPLC method was developed and validated for identification of Teneligliptin hydrobromide hydrate and its degradants on Kromacil C18 column using pH 5.5 phosphate buffer and methanol (75:25v/v) as a mobile phase in isocratic mode of elution at a flow rate 1.2 ml/min. The column effluents were monitored by a variable wavelength UV detector at 270 nm. The method was validated as per ICH guidelines. Forced degradation studies of Teneligliptin hydrobromide hydrate were carried out under acidic, basic, neutral, peroxide, photo and thermal conditions. Degradation was observed in basic and neutral stress samples, but not in acid, peroxide, photo and thermal stress samples.

Monoammonium glycyrrhizinate was determined it has anti-viral activity in case of hepatitis A, B, C, D. We have developed matrix tablet contained monoammonium glycyrrhizinate by previous study. The objective of the study was to evaluate drug release of matrix tablet in vivo  and determinate its stability. In the present study was evaluated in vivo drug release of the matrix tablet. Stability testing was determinated by long term and accelerated method by such criteria’s: appearance, weight variation, biological active compound, hardness, friability, dissolution and microbiological contamination. The Cmax (µg/ml), Tmax (h), AUC0-t (µg h/ml) of Glycyron tablet and Licozinat matrix tablet were determined in vivo. Stability of the matrix tablet was determined. Licozinat matrix tablet was released drug by prolonged time by in vitro. In vivo pharmacokinetic study in rabbits confirmed the prolonged release by showing increase in bioavailability for matrix tablet compared to Glycyron tablet. Licozinat matrix tablet was stable for 12 months. Stability testing of matrix tablet is continuing by long term method.

A stable, simple, accurate, precise, robust and highly selective Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) method was developed and validated using ritonavir. Chromatographic separation was achieved using cyber labs, LC 100 separation module, Agilent C18 column at temperature 30°C. Flow rate selected was 1ml/min. Both drugs are identified with UV detector at 256nm. Mobile phase employed was Methanol: Water (50:50), which resulted best   sensitivity. Developed method was validated in terms of linearity, range (25-150µg/ml), precession (correlation coefficient is less than 0.999), robustness, accuracy(recovery was 101.96%) and  under stress conditions drug degradation was less than 10%.The validation of proposed stability indicating method was verified by recovery studies and can be applicable in routine pharmaceutical analysis.

Lyophilization is promising approach to increase the shelf life of liposome. The major limitation in the widespread use of liposome is its instability. The aim of this study was to investigate the effect of lyophilization either in the presence or in the absence of lyoprotectant on liposome properties Lyophilization is used to ensure an increased shelf life of liposomes by preserving them in dry state more stable than the aqueous dispersion. When stored as aqueous system the encapsulated drugs are released & the liposome might aggregate or fuse. The process of lyophilization without cryoprotectant resulted in particle size increased & significant content leakage. This review work suggests that the investigation of stability of lyophilized liposomes containing PC (Phosphatidyl Choline) & cholesterol. Liposomes sphere-shaped vesicles consisting of one or more phospholipids bilayer in which both hydrophilic & hydrophobic drug entity can be incorporated. Due to their size & hydrophobic & hydrophilic character liposomes are promising for drug delivery. This structure turns liposomes into ideal drug carriers, since hydrophilic drugs tend to entrapped in the core; while hydrophobic ones will be entrapped within the lipid bilayers. Liposome is one of the most successful drug delivery system applying nanotechnology to potentiate the therapeutic efficacy & reduce toxicities of conventional medicines. The encapsulation efficiency partially depends upon the logP of drug. Lyophilization is a strategy often employed to improve liposomal formulation stability, due to reactivity being far less pronounced in the solid versus aqueous state.

A simple reverse phase specific and selective high performance liquid chromatographic method for determination of Exemestane in Exemestane tablets has been developed and validated with Isocratic elution and UV detection. Chromatographic separation was achieved by using Hypersil, C-18, 150 X 4.6mm, 5µ column with a mixture of Acetonitrile and Purified water in the ratio of 35:65, filter and degas the mobile phase same is used as diluent. Detection was at 249 nm. By this method all known and unknown Impurity & Degradation products are well separated from Exemestane main peak.  Peak purity factor for Exemestane peak is not less than 99.0%. Both the Precision (System Precision, Method Precision, Intermediate Precision) and Linearity were within acceptable range. Response was a linear function between concentration and area of peak over the   range from 50% to 150% of assay concentration for Exemestane. It can be concluded that the Exemestane Peak is found to be degraded more in acid, alkali and peroxide stress condition. Exemestane Peak purity factor was more than 99.0% and all degradation product formed were well separated from Exemestane Peak. By this it was found that this method is robust and system suitability test was established and related parameters are recorded. This method is validated hence this method can be used for routine analysis of stability sample.

A stability indicating RP-HPLC method was developed for the simultaneous determination of Spironolactone (SRL) and Hydroflumethiazide (HFM) in pharmaceutical dosage form. Inertsil ODS - C18 (250 mm x 4.6 mm, 5 µm) column and mobile phase of methanol: acetonitrile : phosphate buffer in the ratio of 55:40:05 v/v at a flow rate of 1.0 mL/min was used for separation of the components. The components were detected at a wavelength of 221nm using UV detector. The Spironolactone and Hydroflumethiazide were separated at retention time 4.67 and 6.74 min respectively. The developed method was validated in terms of precision, accuracy, linearity, specificity, limit of detection, limit of quantitation. The range of linearity was found to be 5-30 µg/mL for Hydroflumethiazide and 5-30 µg/mL for Spironolactone. The proposed method was applied to study the stability of the drugs under different degradation conditions such as acid, alkali, peroxide, thermal and photo light. The developed method was found to be simple, sensitive and rapid and hence, It can be adopted in any laboratory for quality control analysis.

The poor aqueous solubility and dissolution rate of API is one of the main challenge in pharmaceutical development. The improvement of solubility and dissolution profiles of these lipophilic drug molecules without altering the molecular structure is a particular challenge for the successful development of pharmaceutical products. Pharmaceutical cocrystals are molecular complexes of an API and one or more cocrystal formers, which are solids at room temperature, interacting through hydrogen bonding, π-stacking or van der Waals forces. A crystalline form of the API is strongly preferred because of their relative ease of isolation, and the physico-chemical stability that the crystalline solid state affords. The vast majority of APIs occur as solids; these include, salts, polymorphs, cocrystals and hydrates/solvates. Cocrystallization as a method of obtaining new forms of Active Pharmaceutical Ingredients (APIs) with improved physicochemical properties like solubility, stability, and melting point has gained much attention in recent years and is a promising alternative to so far employed preparation of salts, hydrates, solvates and other forms. Cocrystallization improves physicochemical properties of drug without affecting their pharmacological properties. There are various methods for preparation of cocrystals like solvent evaporation, solution crystallization, antisolvent addition, kneading etc. The characterization methods includes FTIR, DSC, PXRD, NMR, Raman spectroscopy etc.

The natural product curcumin is a polyphenolic compound extracted from the rhizome of Curcuma longa L. Curcumin is the principle curcuminoid present in turmeric, responsible for its bright yellow color. Curcumin is a nature’s gift to mankind which has broad range of therapeutic, diagnostic and prophylactic potential. In addition to its use as a spice, flavoring and coloring agent in food, turmeric has been used in India for medicinal values for centuries. In Ayurveda, use of curcumin is well documented for the treatment of various ailments. But the applications of curcumin are curtailed by its low solubility, stability, bioavailability, rapid metabolism and short half life. This weapon can be sharpened and re explored as new age one key answer to many ailments and disorders by using it in the form of liposomal, nanoparticulate, microparticulate drug delivery and also by complexing it with metal ions, polymers, cyclodextrine and other carriers. Curcumin has ability to bind with various transition and earth metal ions to form stable complex. Complexation of curcumin with transition metals is one of the useful ways to overcome the problem related to solubility, stability and bioavailability. From several recent studies, it was observed that curcumin metallocomplexes shows greater therapeutic effects than curcumin alone.

Metronidazole 2-(2-methyl-5-nitro-1H-imidazole-1-yl) ethanol is a synthetic nitroimidazole derivative of antibacterial and antiprotozoal activity. It has different dosage forms. The stability of the Metronidazole intravenous of three different brands was studied in order to investigate the kinetics of photodegradation of this drug using a UV/ Vis spectroscopy. The degradation was carried out by the use of short (254 nm) and long UV (352 nm) lamps. The kinetics parameters of reaction order and the rate constants of the degradation were determined for the three brands products.  The degradation process was found to follow first-order kinetics. The present study also reveals that the drug is light-sensitive. Thus, appropriate light protection is recommended during the storage and handling of metronidazole products. The study highlighted the fact that there is a correlation between the radiation intensity and degradation of metronidazole (photodegradation), i.e. as the radiation energy becomes stronger, the degradation rates increases. Furthermore, the rate of degradation was found to follow pseudo-first order reaction. It was also found that as the exposure time of these drugs to radiation increased the degradation was amplified. For all three brands were used in the investigation, the average rate of degradation when using long UV irradiation, and short UV radiation as stress factors were found to be,-0.0061 day-1 and -0.026 day-1 respectively. The obtained results show that UV/vis spectroscopy is satisfactory technique at the determination of metronidazole degradation kinetics in e intravenous products.

The aim of present study was to design and development of a proniosomal transdermal drug delivery system of lornoxicam for the treatment of rheumatoid arthritis and enhanced skin targeting effect, sustained & prolonged drug release, enhanced skin bioavailability by using different type of non ionic surfactant & cholesterol. Proniosomes of Lornoxicam were prepared by coacervation-phase separation method. The formulation systems were characterized in vitro for size, vesicle count, drug entrapment, drug release profile and vesicular stability. The method used for preparing proniosome resulted in an encapsulation yield of 67.71-87.64%. Proniosomes were characterized by transmission electron microscopy. In vitro studies showed prolonged release of entrapped lornoxicam. A successful attempt was made to develop proniosomal gel for transdermal delivery of lornoxicam using different grades of nonionic surfactant.