Improvement of dissolution properties of albendazole fromdifferent methods of solid dispersion

Poor aqueous solubility of drugs results in poor absorption and bioavailability. The objective of solid dispersion technology is to increase the dissolution properties of highly lipophilic drugs, by using different hydrophilic carriers thereby improving their bioavailability. This technology is useful for enhancing the dissolution, absorption and therapeutic efficacy of drugs in dosage forms. Albendazole is a broad-spectrum antihelmintic agent used for the treatment of a variety of parasitic worm infestations. It is practically insoluble in water but slightly soluble in solvents like chloroform, methanol, ethyl acetate, and acetonitrile. The aim of our study was to improve the dissolution profile of albendazole using HPMC K 100 LV, Kollidon VA64 and Mannitol as carriers by solid dispersion techniques. From the prepared solid dispersion, formulation code CSF5 showed better result where carrier was HMPC K 100 LV at 1:10 ratio in solvent evaporation method. The HPMC K 100 LV showed better result for both kneading and solvent evaporation methods. Moreover, among the method employed, solvent evaporation method showed better solubility of drug at 60 min also at 1:10 ratio which was 78.86%. Results indicated that current formulation of solid dispersion is a promising approach for enhancing drug solubility and dissolution

Bio-analytical method development of generic formulations manufactured at IIUM Pharmaceutical manufacturing plant

Generic drug is a pharmaceutical product, usually intended to be interchangeable with the innovator product, marketed after the expiry of patent or another exclusivity right. After the Hatch Waxman act 1984 expansion of the manufacturing of generic formulations has increased manifold all over the world especially in developing countries. It is required to perform bio-equivalence study for all generic solid dosage forms to ensure the quality, safety and efficacy of the drug. At IIUM pharmaceutical manufacturing plant several generic formulation project has been undertaken to be registered and marketed for local and international usage. Current study focus on the bio-analytical method development of antidiabetic and antihypertensive generic formulations manufactured at IIUM pharmaceutical manufacturing plant in order to support the bio-equivalency of the product. Amlodipine, Gliclazide and Perindopril are the generic drugs being investigated for plasma level detection in human and animal plasma. Challenge of bio-analytical method development greatly lies on cleaner sample preparation and subsequent detection at a low level to capture the drug excretion trend after administration to determine the pharmacokinetic parameters. LC MSMS and UV-Vis detection of the drugs were reported. Liquid-liquid extraction and protein precipitation technique was evaluated for the sample preparation. The recovery of gliclazide and internal standard was found between 75.31% and 104.84% respectively. Interday and intraday precision accuracy was evaluated based on the three different QC concentration namely low (L), medium (M) and high (H). The intraday precision was between 2.06 – 12.90 % and inter day precision was in the ranges of 7.27 – 10.63 % respectively for gliclazide and internal standard. It was found that the recovery of developed method varied between 88.78% - 107.04 % for perindopril and 73.93 – 79.24 % for amlodipine. It demonstrated high accuracy and precision for amlodipine and perindopril the intraday and inter day precision of perindopril were 3.14% - 12.37% and 4.4% - 9.2% respectively, while it was between 3% - 9.05% and 5.78% - 13.17% for amlodipine respectively. Methods were validated following the CDER (FDA) guideline and all the parameters were found within the acceptable range of the prescribed guideline

Development and validation of bioanalytical method for amlodipine in human plasma with optimised extraction method using Design of Experiment (DOE)

Amlodipine is antihypertensive drug belonging to calcium antagonist group. This study aims to apply experimental design for the optimization of extraction method of amlodipine from human plasma for higher and constant recovery. A chromatographic method involving HPLC (High Performance Liquid Chromatography) with DAD (Diode Array Detector) was developed and validated for the determination of Amlodipine in human plasma with cetirizine as internal standard. Sample preparation for the extraction of Amlodipine and Cetirizine (Internal Standard) from plasma was optimised using DOE (Design of Experiment). Three different parameters namely solvent type, solvent volume and pH were monitored at different level for the optimisation of sample preparation that would produce best recovery of the analytes. For this purpose, three level full factorial design, which involves 27 experiments, was conducted. The recovery of amlodipine was determined using the developed and pre validated HPLC-DAD method with an Agilent 1100 HPLC system. Chromatographic separation of the analytes was obtained using phenomenix (150X4.5 mm, 5 um) C18 column. The mobile phase consists of 35:65 v/v of ACN: 0.3% triethylamine with pH adjusted at 3 using phosphoric acid. Detection of analyte was conducted using a diod array detector at 237 nm wavelength. Design Expert 8.0 software was used to interpret all data obtained from the optimisation study. For the parameters solvent and solvent volume “acetonitrile” and “1 ml” was found to be the optimum values required to extract amlodipine and internal standard while pH had no effect on the optimum recovery. The recovery of amlodipine and internal standard was 80-88% and 85-99% respectively

Weeds as alternative useful medicinal source: Mimosa pudica Linn. on diabetes mellitus and its complications

Diabetes mellitus is one of the major reasons for mortality worldwide and numerous scientific studies are going on to find plausible solutions to overcome and manage diabetes and its related infirmities. Traditional medicines use medicinal plants as anti-diabetic agents and despite being a disturbing weed to farming land Mimosa pudica Linn. has a high traditional usage for various purposes including anti-diabetic complications. The objective of this article is to accumulate and organise literatures based on traditional claims and correlate those with current findings on the use of M. pudica in the management of diabetes mellitus. M. pudica is a creeping perennial shrub which is a common weed widely distributed in Southeast Asia specially in India, Bangladesh, Malaysia, China, Philippine etc. This plant has various species of which M. pudica is a well recognised plant of medicinal origin which has been traditionally used as folk medicine in India, Bangladesh and Philippine, Chinese, herbal and siddha medicines. It has wound healing, antidiabetic, anti-diarrhoeal, antimicrobial, anti-cancer, anti-infections, anti-worm, anti-proliferative, anti-snake venom, anti-depressant and anxiolytic etc. activities. The objective of this article is to provide up-to-date information on the traditional and scientific studies based on this plant on the frontier of diabetes mellitus. The methodology followed was to methodically collect, organise and chart the recent advances in the use of M. pudica in diabetes and its related complications like vascular complications, diabetic wound, hyperlipidemia etc. Various scientific studies and traditional literatures clearly support the use of M. pudica as an anti-diabetic agent among other uses. So far, the anti-diabetic compounds have not been isolated from this plant and this can be a good scientific study for the future anti-diabetic implications

Development and validation of bioanalytical method for the detection of gliclazide in human plasma

A robust High Performance Liquid Chromatography Diod Array Detection (HPLC- DAD) method was developed for the detection of gliclazide in human plasma. Liquid liquid extraction method was used as a sample preparation for HPLC analysis. The separation was carried out on Agilent Zorbax Reversed Phase C-18 column (150 x 4.6 mm, 5µ m) with PDA detection at 236 nm. with an isocratic elution (1 mL/min) at 30°C column temperature. The mobile phases used consisted of acetonitrile: 0.3% triethylamine buffer (pH=3.0 adjusted with H3PO4 85%) 57:43 v/v. Then, 10 µL aliquot samples were injected onto chromatographic system. The results showed that the retention time for the gliclazide and the internal standard, glibenclamide were 3.8 and 4.8 respectively. The method was linear over the range of 10 – 5000 ppb with R2 of 0.9971. The recoveries of the developed methods for gliclazide were found to be between 84.9% and 104.0%, while for the glibenclamide were found to be between 100.0% and 112.0%. The stability analysis showed that gliclazide is stable for at least 3 months but glibenclamide is degraded for about 2 months when stored at -20 ?. For conclusion, the develop method is suitable and reliable for the detection of gliclazide in human plasma

Starvation time and successive collection effects on leeches saliva collection quantity and proteins quality and quantity in wet season (Kesan masa kebuluran dan kejayaan pengumpulan kuantiti air liur lintah serta kualiti dan kuantiti protein dalam musim hujan)

The salivary gland secretion of the haematophagous animals, leeches, has attracted the attention of therapists since the extreme old ages due to its wide range of medical properties. Thus, many researches have been done to develop and optimize new methods to collect leech saliva with high quality and quantity. In the present study, we aimed to evaluate the effects of starvation period and repeated collection on the quality and quantity of leech saliva extract LSE and its contents of proteins during the rainy season. Protein recovery in the LSE was also studied after first collection. It was found that leeches are able to produce protein-containing saliva whenever fed during the whole study period of 18 weeks with varied protein concentrations. The results showed that the highest protein concentrations (105-91 μ g/mL ) were produced after 12-15 weeks of starvation. The results of successive collection showed that leeches are able to produce proteins and peptides whenever they suck the solution after first collection with some varies in the concentrations. The concentrations varied between 0 and 72% of the initial concentration. Gel electrophoresis results showed absence for some bands when the concentrations are too low. Also the results showed that leeches are able to recover about 42% of their initial proteins concentration within four weeks of starvation after first feeding. The gel electrophoresis results showed the closeness between the first and second collections. To conclude, all test factors (starvation period, successive collection and recovery test) were shown to have an important impact on protein concentration of leech saliva and therefore its medicinal affectivity. The mentioned results are reported for the first time and they open the gate for further studies

Current analytical methods for amlodipine and its formulations: A review

The use of amlodipine is very common due to the effects of amlodipine on hypertension and coronary artery disease (CAD) like chronic stable angina, vasospastic angina (Prinzmetal’s or variant angina), and angiographically documented CAD. Amlodipine is involved in several combinations with other antihypertensive drugs. The analysis of amlodipine and its co-drugs is reported using several analytical methods such as spectrophotometric, capillary electrophoresis and chromatographic methods. To our knowledge, there is no comprehensive reports which address all analytical methods for the analysis of amlodipine and combination, therefore we tried to gather as much as reports in one review paper to help researchers and industrial experts to easily access the information related to amlodipine analysis