Background Increasing hydrophilicity of poorly water-soluble drugs is a major challenge in drug discovery and development. Cocrystallization is one of the techniques to enhance the hydrophilicity of such drugs. Carvedilol (CAR), a nonselective beta/alpha1 blocker, used in the treatment of mild to moderate congestive heart failure and hypertension, is classified under BCS class II with poor aqueous solubility and high permeability. Present work is an attempt to improve the solubility of CAR by preparing cocrystals using hydrochlorothiazide (HCT), a diuretic drug, as coformer. CAR-HCT (2:0.5) cocrystals were prepared by slurry conversion method and were characterized by DSC, PXRD, FTIR, Raman, and SEM analysis. The solubility, stability, and dissolution (in vitro) studies were conducted for the cocrystals. Results The formation of CAR-HCT cocrystals was confirmed based on melting point, DSC thermograms, PXRD data, FTIR and Raman spectra, and finally by SEM micrographs. The solubility of the prepared cocrystals was significantly enhanced (7.3 times), and the dissolution (in vitro) was improved by 2.7 times as compared to pure drug CAR. Further, these cocrystals were also found to be stable for 3 months (90 days). Conclusion It may be inferred that the drug–drug (CAR-HCT) cocrystallization enhances the solubility and dissolution rate of carvedilol significantly. Further, by combining HCT as coformer could well be beneficial pharmacologically too.

Background Cocrystallization is one of the crystal engineering strategies used to alter the physicochemical properties of drugs that are poorly water-soluble. Gliclazide (GLZ), an antidiabetic drug, belongs to Biopharmaceutical Classification System class-II (low solubility and high permeability) and has low bioavailability, resulting in poor therapeutic effects in patients. Therefore, to impart better solubility and bioavailability of GLZ, the study was carried out by preparing GLZ cocrystals using liquid-assisted grinding method with three coformers [3,5-dinitrosalicylic acid (DNS), 2,6-pyridine dicarboxylic acid (PDA), and L-proline (LPN)], and these were characterized using Differential Scanning Colorimetry (DSC), Powder X-ray diffraction (PXRD), Fourier Transform Infra-red spectroscopy (FTIR), and Raman spectral studies. Further, Scanning electron microscopy (SEM) analysis, accelerated stability, solubility, in vitro dissolution studies, and in vivo pharmacokinetic studies were performed in male Wistar rats. Results DSC and PXRD analysis confirmed the formation of the GLZ cocrystals. Hydrogen bonding between pure GLZ and its coformers was demonstrated based on FTIR and Raman analysis. SEM data showed morphological images for GLZ cocrystals differed from those of pure GLZ. In comparison with pure GLZ, these GLZ cocrystals have greatly improved solubility, in vitro dissolution, and in vivo profiles. Among the three, GLZ–DNS cocrystals outperformed the pure drug in terms of solubility (6.3 times), degradation (1.5 times), and relative bioavailability (1.8 times). Conclusion Hence, cocrystallization of GLZ leads to improved physicochemical properties of poorly soluble drug gliclazide.

OBJECTIVES:Cardiovascular disease (CVD) is the primary cause of death globally despite the advanced health-care facilities. Extensive disparity exists in pharmacotherapy pattern among CVD patients where rational drug use plays a pivotal role in promoting safety and efficacy. The study focused to evaluate drug utilization using the World Health Organization (WHO) prescribing indicators and defined daily dose (DDD) in patients admitted to a teaching/referral hospital in Northern Telangana.MATERIALS AND METHODS:A total of 1120 medical records were analyzed for drug utilization for a period of 7 months. Prescription pattern was assessed using the WHO prescribing indicators and DDD to measure individual drug utilization categorized under anatomical–therapeutic–chemical classification.RESULTS:Of the total admissions, 58.57% (55.19 ± 15.19 years) were male and 41.43% (56.64 ± 15.28 years) were female where coronary artery disease was the most common cause of admission followed by cardiomyopathy. Among prescribing indicators, percentage of drugs with generic names was least accounted with 26.86% and 18.95% during hospitalization and discharge, respectively. A mean of 11.55 (hospitalization) and 6.55 (discharge) drugs were prescribed per prescription. Antiplatelet (72.86%) and statin (80.62%) use was predominate during complete therapy. The DDD of furosemide (109.33) was found to be high, followed by atorvastatin (64.6), enalapril (58.44), aspirin (58.14) and clopidogrel (53.2).CONCLUSION:Polypharmacy and least use of generic name were observed in the study which may affect the rationality. The use of antiplatelets, statins, and angiotensin-converting enzyme-inhibitors was appropriate, but furosemide overuse is of major concern. Therefore, appropriate prescription writing improvises treatment compliance in the patients, which results in rationality.