Development and evaluation of acid-buffering bioadhesive vaginal tablet for mixed vaginal infections.

Abstract

An acid-buffering bioadhesive vaginal tablet was developed for the treatment of genitourinary tract infections. From the bioadhesion experiment and release studies it was found that polycarbophil and sodium carboxymethylcellulose is a good combination for an acid-buffering bioadhesive vaginal tablet. Sodium monocitrate was used as a buffering agent to provide acidic pH (4.4), which is an attribute of a healthy vagina. The effervescent mixture (citric acid and sodium bicarbonate) along with a superdisintegrant (Ac-Di-sol) was used to enhance the swellability of the bioadhesive tablet. The drugs clotrimazole (antifungal) and metronidazole (antiprotozoal as well as an antibacterial) were used in the formulation along with Lactobacillus acidophilus spores to treat mixed vaginal infections. From the ex vivo retention study it was found that the bioadhesive polymers hold the tablet for more than 24 hours inside the vaginal tube. The hardness of the acid-buffering bioadhesive vaginal tablet was optimized, at 4 to 5 kg hardness the swelling was found to be good and the cumulative release profile of the developed tablet was matched with a marketed conventional tablet (Infa-V). The in vitro spreadability of the swelled tablet was comparable to the marketed gel. In the in vitro antimicrobial study it was found that the acid-buffering bioadhesive tablet produces better antimicrobial action than marketed intravaginal drug delivery systems (Infa-V, Candid-V and Canesten 1).

• Authors: Mohd Aftab Alam, Farhan Jalees Ahmad, Zeenat Iqbal Khan, Roop Krishen Khar, Mushir Ali
• Journal: AAPS PharmSciTech (AAPS PharmSciTech) Vol. 8 Issue 4 Pg. E109 (Dec 14 2007) ISSN: 1530-9932 [Electronic] United States
• PMID: 18181530 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Acrylic Resins
• Antifungal Agents
• Antiprotozoal Agents
• Buffers
• Citrates
• Drug Combinations
• Excipients
• Membranes, Artificial
• Tablets
• Metronidazole
• Sodium Citrate
• calcium polycarbophil
• Clotrimazole
• Carboxymethylcellulose Sodium

Topics

• Acrylic Resins (chemistry)
• Adhesiveness
• Animals
• Antifungal Agents (chemistry, pharmacology, therapeutic use)
• Antiprotozoal Agents (chemistry, pharmacology, therapeutic use)
• Buffers
• Candida albicans (drug effects, growth & development)
• Carboxymethylcellulose Sodium (chemistry)
• Chemistry, Pharmaceutical
• Citrates (chemistry)
• Clotrimazole (chemistry)
• Drug Combinations
• Drug Compounding
• Excipients (chemistry)
• Female
• Humans
• Hydrogen-Ion Concentration
• Kinetics
• Lactobacillus acidophilus
• Membranes, Artificial
• Metronidazole (chemistry, pharmacology, therapeutic use)
• Mucous Membrane (chemistry)
• Probiotics
• Reproducibility of Results
• Sodium Citrate
• Solubility
• Tablets
• Technology, Pharmaceutical (methods)
• Vaginitis (drug therapy, microbiology, parasitology)