Development and evaluation of herbal formulation AKIGTU01 and AKIGCL03 against acne producing microbes.

Acne vulgaris is a common global skin disease affecting teenagers and adults and exerting serious psychological impacts which includes everlasting scarring, reduced self-image, depression and anxiety. One of the suspected causative agent of acne is Propionibacterium acnes; a Gram positive anaerobic organism which lives in skin hair follicle and openings. Treatments currently available for acne include use of oral antibiotics, hormones, isotretinoin and also physical treatments like lesion removal and photo-therapy. All these are associated with risks and none is completely satisfactory.Therefore, natural alternatives are gaining greater research support but lacks sufficient studies. In our study we have isolated Propionibacterium acnes from infected individuals and tested the effect of certain chemicals and herbs/ vegetable extracts against it. There anti-acne property was studied and compared with commercially used antibiotics including Clinagel (Clindamycin phosphate), Vibramycin (Doxycycline), Erythromycin, Novidat (Ciprofloxacin) and Amoxil (Amoxicillin). Results indicate that some of the selected herbs and chemicals showed good activity against Propionibacterium acnes synergistic to the antibiotics when used alone or in combination. Findings of this research can play an important role in natural product based drug discovery for the treatment of Acne vulgaris.

Synthesis, characterization and biological activity of a series of carboxamide derivatives of ofloxacin.

The present study was designed to help develop new agents with better antimicrobial profiles. Specifically, we focused on modification of the basic structure of ofloxacin by introducing new functionality at its C3 position. For this purpose, the carboxylic group at the C3 position of ofloxacin was replaced by an amide group through an ester aminolysis reaction. The structure of these derivatives was established by various analytical techniques i.e., IR, (1)H-NMR, (13)C-NMR CHNS elemental analysis and mass spectrometry. The antibacterial activity of ofloxacin and its derivatives against ten different Gram-positive and Gram-negative microorganisms was studied using a disk susceptibility method. These compounds were further tested for their activity against various fungi and compared to ofloxacin. The synthesized compounds showed diverse antimicrobial profiles. Among them, a few compounds possessed a comparable or better activity in comparison to the reference drug.

Simultaneous determination of piracetam and its four impurities by RP-HPLC with UV detection.

A simple and rapid high-performance liquid chromatographic method for the separation and determination of piracetam and its four impurities, 2-oxopyrrolidin-1-yl)acetic acid, pyrrolidin-2-one, methyl (2-oxopyrrolidin-1-yl)acetate, and ethyl (2-oxopyrrolidin-1-yl)acetate, was developed. The separation was achieved on a reversed-phase C(18) Nucleosil column (25 cm x 0.46 cm, 10 microm). The mobile phase is composed of an aqueous solution containing 0.2 g/L of triethyl amine-acetonitrile (85:15, v/v). The pH of the mobile phase was adjusted to 6.5 with phosphoric acid at a flow rate of 1 mL/min at ambient temperature and UV detection at 205 nm. The developed method was found to give good separation between the pure drug and its four related substance. The polynomial regression data for the calibration plots showed good linear relationship in the concentration range of 50-10,000 ng/mL, 25-10,000 ng/mL, 45-10,000 ng/mL, 34-10,000 ng/mL, and 55-10,000 ng/mL, respectively, with r(2) = 0.9999. The method was validated for precision, accuracy, ruggedness, and recovery. The minimum quantifiable amounts were found to be 50 ng/mL of piracetam, 25 ng/mL of 2-oxopyrrolidin-1-yl)acetic acid, 45 ng/mL of pyrrolidin-2-one, 34 ng/mL of methyl (2-oxopyrrolidin-1-yl)acetate, and 55 ng/mL of ethyl (2-oxopyrrolidin-1-yl)acetate. Statistical analysis proves that the method is reproducible and selective for the estimation of piracetam as well as its related substance. As the method could effectively separate the drug from the related substances, it can be employed as a stability-indicating one. The proposed method shows high efficiency, allowing the separation of the main component piracetam from other impurities.

Simultaneous determination of metformin, cimetidine, famotidine, and ranitidine in human serum and dosage formulations using HPLC with UV detection.

A new, simple, and reliable reversed-phase high-performance liquid chromatographic method has been developed and validated for the simultaneous determination of metformin (Metf), cimetidine (Cimt), famotidine (Famt), and ranitidine (Rant) in their synthetic mixtures and tablet formulations. These drugs were separated on a Purospher Star RP18 endcapped (250 mm × 4.6 mm i.d.) column packed with 5-µm particles. The mobile phase, optimized through an experimental design, consisted of methanol-water-triethylamine (20:80:0.05), whose pH was adjusted to 3.0 with phosphoric acid (85%) pumped at a flow rate of 1.0 mL/min. UV detection was performed at 229 nm. The method was validated in the sample concentration range of 5-25 µg/mL for all the drugs, where it demonstrated good linearity with r = 0.9998, 0.9979, 0.9997, and 0.9987 (n = 6), respectively. For independent 100% level samples, the intra-day and inter-day precision was in the range i.e. < 2.0 for all the drugs. The method demonstrated robustness, resisting to small deliberate changes in pH, flow rate, and composition (organic:aqueous ratio) of the mobile phase. The limit of detection values were 0.071, 0.116, 0.134, and 0.110 µg/mL, while the limit of quantitation were 0.217, 0.352, 0.405, and 0.368 µg/mL for Metf, Cimt, Famt, and Rant, respectively. The applicability of the method was demonstrated by determining the drug content in pharmaceutical formulations, where it exhibited good performance.

Spectrophotometric determination of gabapentin in pharmaceutical formulations using ninhydrin and pi-acceptors.

Simple, rapid and sensitive spectrophotometric procedures are developed for the analysis of gabapentin in pure form as well as in their pharmaceutical formulations. The methods are based on the reaction of gabapentin as n-electron donor with ninhydrin and pi-acceptors namely, 2,3,5,6-tetrachloro-1,4-benzoquinone, chloranilic acid, 2,3-dichloro-5,6-dicyano-1,4-benzoquinone, tetracyanoethylene and 7,7,8,8-tetracyanoquinodimethane. The obtained complexes were measured at 568, 230, 314, 304, 335 and 439 nm for ninhydrin, chloranil, Chloranilic acid, DDQ, TCNE and TCNQ respectively. The proposed procedures could be successfully applied to the determination of gabepentin with good recovery; percent ranged from 99.3 to 100.7 The association constants and free energy changes using Benesi-Hildebrand plots are also studied.

In vitro hypoglycemic activity of methanolic extract of some indigenous plants.

Pakistan is rich in medicinally important plants and has ancient herbal treatment methods. Present work is based on the study of six indigenous plants Eugenia jambolana, Lawsonia inermis, Momordica charantia, Morus alba, Nigella sativa and Trigonella foenum graecum which show the inhibitory effect of glucose utilization, and are in use as hypoglycemic agents of varying degree in traditional system of medicine. The glucose uptake activity of (methanolic extracts) of these plants was tested in vitro and glucose was estimated by glucose oxidase method. The results in three different media revealed that, hypoglycemic activity is more prominent in neutral and basic media as compared to acidic medium.

Spectrophotometric methods for the simultaneous analysis of meclezine hydrochloride and pyridoxine hydrochloride in bulk drug and pharmaceutical formulations.

Three new spectrophotometric procedures for the simultaneous determination of pyridoxine hydrochloride and meclezine hydrochloride are described. The first method depends on the application of simultaneous equation to resolve the interference due to spectral overlapping. The analytical signals were measured at 231 and 220 nm. Calibration graphs were established for 1 to 20 microGmL(-1) for pyridoxine hydrochloride and 0.5 to 10 microGmL(-1) for meclezine hydrochloride in binary mixture. In the second method, the determination of pyridoxine hydrochloride and meclezine hydrochloride was performed by measuring the absorbances at 290 and 235 nm in the simple absorbance spectra of their mixture. In third method a yellowish orange complex of pyridoxine hydrochloride was formed with ferric chloride, which absorbs in the visible region with lambda(max) at 445 nm. Calibration curve of complex formation range was conducted in between 20 to 250 microGmL(-1). These methods were validated with respect to accuracy, precision, linearity, limit of detection and quantification. Regression analysis of Beer's plot showed good correlation in a general concentration range of 1 to 20 microGml(-1) with correlation coefficient (r = 0.9999 and 0.9999; CV < 0.858) for pyridoxine hydrochloride, whereas meclezine hydrochloride concentration range 0.5 to 10 microGmL(-1) with correlation coefficient (r = 0.9998 and 0.9998; CV < 0.826). These methods can be readily applied, without any interference from the excipients. The suggested procedures were successfully applied to the determination of these compounds in synthetic mixtures and in pharmaceutical preparations, with high percentage of recovery, good accuracy and precision.

Development and validation of RP-HPLC method for the analysis of metformin.

The reversed-phase high-performance liquid chromatographic (RP-HPLC) method has been developed to quantify metformin hydrochloride (MfCl) in raw material and pharmaceutical formulations using C(18) analytical reverse-phase column. Diazepam was used as an internal standard. Mobile phase consisted of methanol-water (30:70 v/v), pumped at a flow rate of 0.5 ml/min at ambient temperature and the retention time was about 4.4 min with symmetrical peaks. (MfCl) was detected by ultraviolet absorbance at 233 nm with no interference of commonly used excipients. The method was linear over the concentration range 0.312-5 mug/mL (R2 = 0.9995). The limit of detection of metformin was 0.1 mug/mL and the limit of quantitation was 0.3 mug/mL. The results obtained showed a good agreement with the declared contents in case of pharmaceutical formulations. The proposed method is rapid, accurate, economical and selective and it may be used for the quantitative analysis of metformin in Neodipar tablets because of its sensitivity and reproducibility.