Studies on in-vitro transcutaneous delivery of losartan potassium, influence of penetration enhancers and barrier membrane

Formulation and in vitro evaluation of losartan potassium (LP) loaded transdermal delivery system (TDS) was investigated for controlled release and improved therapeutic efficacy. TDS (patches) were prepared by varying the composition of Eudragit RL 100 and Eudragit RS 100 (5:0, 4:1, 3:2, 2.5:2.5, 2:3, 1:4 and 0:5). Patches were evaluated for thickness, content uniformity, mechanical properties, moisture uptake and in vitro drug release. Technological parameters for all the formulations were found to be within the limit. In vitro studies showed relatively high permeation of LP (F1- 42.17 ± 1.13 %) from the formulation comprising 4:1 ratio of polymer. Inclusion of capsaicin (55.70 ± 1.55 %) and pluronic F-68 (70.88 ± 1.20 %) to formulation F1 resulted increased permeation of LP across human skin. In conclusion, this study demonstrated the potential of simple transdermal adhesive patch incorporating LP to deliver therapeutically useful dose in-vivo for the treatment of hypertension.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development and characterization of ternary solid dispersion systems of olmesartan medoxomil

The ternary solid dispersion systems of poorly water soluble olmesartan medoxomil (OLM) were prepared by conventional kneading method in order to improve its physicochemical performance. A 32 full factorial design approach was employed to optimize influence of concentration of polyvinylpyrrolidone K30 (PVP) and poloxamer 407 (PLX) on physicochemical characteristics of these dispersions. All formulations were characterized by XRPD, DSC and dissolution studies. Physical studies revealed complete loss of crystallinity and formation of uniform molecular dispersion of OLM in its ternary systems. All dispersion systems showed significant improvement in dissolution profile in comparison to pure drug alone (p 2 : 68.43 ± 2.8 %) of OLM suggesting optimum ratio of carrier system. The kinetic study of dissolution displayed to follow the Korsmeyer-Peppas model (r2 = 0.9835).Colegio de Farmacéuticos de la Provincia de Buenos Aire

Adhesion as an interplay between particle size and surface roughness

Abstract Surface roughness plays an important role in the adhesion of small particles. In this paper we have investigated adhesion as a geometrical effect taking into account both the particle size and the size of the surface features. Adhesion is studied using blunt model particles on surfaces up to 10 nm root-mean-square (RMS) roughness. Measurements with particles both smaller and larger than surface features are presented. Results indicate different behavior in these areas. Adhesion of particles smaller than or similar in size to the asperities depend mainly on the size and shape of the asperities and only weakly on the size of the particle. For large particles also the particle size has a significant effect on the adhesion. A new model, which takes the relative size of particles and asperities into account, is also derived and compared to the experimental data. The proposed model predicts adhesion well over a wide range of particle/asperity length scales

Study of prescribing practices of injections in outpatients of a rural tertiary care teaching hospital

Background: Injections are probably the most common of all medical procedures. The combination of injection overuse and unsafe practices creates a major route of transmission of blood borne pathogenic infections. Unnecessary use of injections can also lead to unnecessary burden on the institution in terms of efficiency, infrastructure, staff requirement and poor utilization of resources. Monitoring and analysis of prescribing practices can help to achieve rational use of injections. The present study was carried out to study the injection prescription patterns in outpatients of a rural tertiary care teaching hospital, Ambajogai, Maharashtra, India. Methods: A cross sectional descriptive study was conducted for duration of two months and 744 prescriptions were randomly collected and analyzed.Results: The total number of injections prescribed in 744 prescriptions was 205. Most (71.70%) of the patients receiving them were above 35 years of age. The most common complaint for which the injections were prescribed was musculoskeletal pain (45.36%) followed by fever. About 155 (75.60%) prescriptions contained injection diclofenac which was the most commonly used drug followed by injection paracetamol (11.21%). There was a high tendency of using brand names in prescriptions (89.30%). Conclusion: The study revealed high proportion of use of injectable drugs. There was overuse of analgesic injections like diclofenac, most of which were unnecessary and irrational. This leads to unnecessary burden on the institution in terms of efficiency, infrastructure, staff requirement and poor utilization of resources. There is a need to develop local guidelines for injection usage along with educational sessions for prescribing doctors

Use of anti-snake venom and clinical outcomes in snake envenomation: a prospective observational study

Background: The only effective measure to prevent or reverse most of the manifestations of venomous snake-bite is timely administration of antisnake venom (ASV) with or without adjunctive treatment as necessary in each case. But recently several concerns have been raised with regard to use of polyvalent ASV. Hence the present study was conducted to assess use of ASV, early adverse reactions to ASV, adjunctive treatment and clinical outcomes in snake-bite patients, which would help to identify areas of problem and provide basis for planning strategies to increase rational use of drugs.Methods: It was a prospective observational study approved by Institutional Ethics Committee. All indoor patients with systemic manifestations of snake envenomation were included in the study. All participants gave written informed consent. Data was obtained prospectively using a structured case record form. Descriptive statistics was used to express the results.Results: Among 52 patients, snake-bite predominantly affected males (59.62%) than females (40.38%). The most common site of snake-bite was lower limb (65.38%). The main indication for ASV administration was vasculotoxic snake-bite (59.62%). Mean dose of ASV use was 18.21±15.51 vials. Mortality was seen in one patient. Majority of patients (28/52, 53.85%) received ASV in the range of 1-10 vials for the management of snake-bite.Conclusions: The use and dose of ASV was appropriate in vasculotoxic snake-bite while few neurotoxic snake-bite patients needed higher than recommended dose.

Physicochemical characterization and improved in vitro dissolution performance of diacerein solid dispersions with PVP K30

Solid dispersions (SDs) of poorly water soluble diacerein were prepared with polyvinylpyrrolidone K30 at drug to polymer ratios of 1:1, 1:3 and 1:5 w/w utilizing kneading technique. Physical mixture (PM) was prepared at drug to polymer ratio of 1:5 w/w for comparison. All formulations were further characterized by TLC, DSC, XRPD, SEM and dissolution studies. TLC indicated an absence of chemical interaction between drug and polymer. A prominent decrease in the crystallinity was accounted for diacerein in binary systems from XRPD data. DSC thermograms revealed a uniform molecular dispersion and generation of amorphous entities of drug accompanied by loss of crystalline and irregular shape with distinct changes in surface morphological features of diacerein detected in SEM photomicrographs. The drug dissolution properties of SDs were significantly improved (DP2: 95.87-100%) in comparison to crystalline diacerein and PM suggesting suitability of kneading method for improving the release rate properties of diacerein.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Physicochemical characterization and improved in vitro dissolution performance of diacerein solid dispersions with PVP K30

Solid dispersions (SDs) of poorly water soluble diacerein were prepared with polyvinylpyrrolidone K30 at drug to polymer ratios of 1:1, 1:3 and 1:5 w/w utilizing kneading technique. Physical mixture (PM) was prepared at drug to polymer ratio of 1:5 w/w for comparison. All formulations were further characterized by TLC, DSC, XRPD, SEM and dissolution studies. TLC indicated an absence of chemical interaction between drug and polymer. A prominent decrease in the crystallinity was accounted for diacerein in binary systems from XRPD data. DSC thermograms revealed a uniform molecular dispersion and generation of amorphous entities of drug accompanied by loss of crystalline and irregular shape with distinct changes in surface morphological features of diacerein detected in SEM photomicrographs. The drug dissolution properties of SDs were significantly improved (DP2: 95.87-100%) in comparison to crystalline diacerein and PM suggesting suitability of kneading method for improving the release rate properties of diacerein.Colegio de Farmacéuticos de la Provincia de Buenos Aire

A study of adverse drug reactions in patients receiving treatment for multi-drug resistant tuberculosis

Background: A high frequency of adverse drug reactions (ADRs) is one of the major challenges in the treatment of Multi-drug resistant tuberculosis (MDR-TB). Patients may refuse to continue treatment if ADRs are not properly addressed, drugs may be stopped unnecessarily and treatment may be terminated prematurely by inexperienced health workers, resulting in a high proportion of failure.Methods: Patients diagnosed for MDR-TB and registered in Drug Resistant TB centre (DR-TB) of tertiary care hospital during period of July 2014 to June 2015 were enrolled in the study. Data of patients hospitalized for the complaints of ADR in DR-TB centre during study period was collected.Results: Out of 468 patients, 60 (12.82%) patients developed at least one adverse reaction and were hospitalised for the same. Among 109 reported ADRs, Gastrointestinal upset was the most common ADR reported (5.98%) followed by psychosis (4.91%) and ototoxicity (2.99%).Conclusions: The health providers, the patients and their relatives should be sensitised about these ADRs for early detection and treatment. It can also be suggested that the setup of DR-TB centre should be integrated with psychiatry and ENT specialities, with all the provisions of early detection of ADR and treatment