DEVELOPMENT AND EVALUATION OF BILAYER MUCOAHESIVE GASTRORETENTIVE TABLET OF DILTIAZEM HYDROCHLORIDE

Objective: The objective of present study was to formulate an oral mcoadhesive tablet of diltiazem hydrochloride. Methods: Investigate the effect of amount of HPMC K4M and sodium alginate on the sustained release and gastric residence time of dosage form. The mucoadhesive tablet prepared by direct compression method was used varying concentrations of HPMC K4M and Sodium alginate and (1:1, 1:1.5, 1:2) Drug and Polymer ratio. Results: The formulations were evaluated and results revealed that FTIR studies showed no evidence of interactions between drug and excipients used. The mucoadhesive strength, residence time and drug content of formulation F3 was found to be 26.35 ± 1.15 mg, >7.5hrs, and 98.75 ± 0.05 % respectively. The formulation F3 exhibited sustained drug release i.e. 75.71% in 12 h. The In Vitro release kinetics studies reveal that formulations fit well with zero order kinetics and mechanism of drug release is Super case II transport. Conclusion: The study was concluded that formulation of mucoadhesive tablets from the cumulative % drug release study reveals that increase in the concentration of adhesive polymers cause slow the drug release. Sustained release tablet of DTZ can be beneficial in treatment of hypertension

PHARMA SCIENCE MONITOR AN INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES APPLICATIONS OF LIPOSOMES IN MEDICINE-A REVIEW

ABSTRACT Liposomes are structurally and functionally some of the most versatile supramolecular assemblies in existence. Since the beginning of active research on lipid vesicles in 1965, the field has progressed enormously and applications are well established in several areas, such as drug and gene delivery. The medical application of liposomes loaded with small molecular weight drugs is discussed and the use of sterically stabilized liposomes containing doxorubicin in cancer therapy is presented. The review also shows that liposomes have a lot of biomedical applications and uses. They have been used in drug targeting, oral delivery of vaccines, insulins, peptides and some compounds, which are usually degraded in the gastrointestinal tract. It has also found application in topical therapy especially in the eye and lungs. Other areas of application are in cancer chemotherapy and treatment of human immunovirus (HIV) infection. The control of the stability of liposomes is an essential prerequisite for effective use as drug carriers. Liposome immunoassays, for example, benefit greatly from the amplification provided by encapsulated markers, and nanotube-interconnected liposome networks have emerged as ultra small-scale analytical devices. This review provides information about new developments in some of the most actively researched liposome-related topics

Novel N‑Linked Aminopiperidine-Based Gyrase Inhibitors with Improved hERG and in Vivo Efficacy against Mycobacterium tuberculosis

DNA gyrase is a clinically validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clinical value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase activity. The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown by their ability to inhibit the growth of fluoroquinolone-resistant Mtb. Biochemical studies demonstrated this class to exert its action via single-strand cleavage rather than double-strand cleavage, as seen with fluoroquinolones. The compounds are highly bactericidal against extracellular as well as intracellular Mtb. Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability. Compounds from this series are efficacious in various murine models of tuberculosis