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AAPS PharmSciTech

, 8:229 | Cite as

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

  • Mohd Aftab Alam
  • Farhan Jalees Ahmad
  • Zeenat Iqbal Khan
  • Roop Krishen Khar
  • Mushir Ali
Article

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 withLactobacillus 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).

Keywords

Bioadhesion Bioadhesive polymers Vaginal infections Acid-buffering bioadhesive tablet Mixed vaginal infections 

References

  1. 1.
    ACOG. ACOG technical bulletin:Vaginitis.Int J Gynecol & Obstet. 1996;53:271–280.CrossRefGoogle Scholar
  2. 2.
    Sherrard J. European guidelines for the management of vaginal discharge.Int J STD AIDS. 2001;12:73–77.PubMedCrossRefGoogle Scholar
  3. 3.
    Kukner S, Ergin T, Cicek N, Ugur M, Yesilyurt H, Gokmen O. Treatment of vaginitis.Int J Gynecol & Obstet. 1996;52:43–47.CrossRefGoogle Scholar
  4. 4.
    Yu K, Chien YW. Vaginal delivery and absorption of drugs. In: Swarbrick J, Boylan JC, eds.Encyclopedia of Pharmaceutical Technology. vol. 16. New York, NY: Marcel Dekker Inc.; 1997:153–185.Google Scholar
  5. 5.
    Deshpande AA, Rhodes CT, Danish M. Intravaginal drug delivery.Drug Dev Ind Pharm. 1992;18:1225–1279.CrossRefGoogle Scholar
  6. 6.
    Ceschel GC, Maffei P, Borgia SL, Ronchi C, Rossi S. Development of a mucoadhesive dosage form for vaginal administration.Drug Dev Ind Pharm. 2001;27:541–547.PubMedCrossRefGoogle Scholar
  7. 7.
    Vermani K, Garg S. The scope and potential of vaginal drug delivery.Pharm Sci Tech Today. 2000;3:359–364.CrossRefGoogle Scholar
  8. 8.
    Levinson RS, Thompson DJ. VagiSite bioadhesive technology. In: Rathbone MJ, Hadgraft J, Roberts MS, eds.Modified-release Drug Delivery Technology. New York, NY: Marcel Dekker; 2003:801–806.Google Scholar
  9. 9.
    Maggi L, Mastromarino P, Macchia S, et al. Technological and biological evaluation of tablets containing different strains of lactobacilli for vaginal administration.Eur J Pharm Biopharm. 2000;50:389–395.PubMedCrossRefGoogle Scholar
  10. 10.
    Owen DH, Katz DF. A vaginal fluid stimulant.Contraception. 1999;59:91–95.PubMedCrossRefGoogle Scholar
  11. 11.
    Singh S, Garg S. Understanding analytical method validation.Pharm Times. 1999;8:15–20.Google Scholar
  12. 12.
    Setnikar I, Fantelli S. Liquefication time of rectal suppositories.J Pharm Sci. 1962;51:566–571.PubMedCrossRefGoogle Scholar
  13. 13.
    De Paula IC, Ortega GG, Bassani VL, Petrovick PR. Development of ointment formulations prepared with Achyrocline satureioides spray dried extracts.Drug Dev Ind Pharm. 1998;24:235–241.PubMedCrossRefGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  • Mohd Aftab Alam
    • 1
  • Farhan Jalees Ahmad
    • 1
  • Zeenat Iqbal Khan
    • 1
  • Roop Krishen Khar
    • 1
  • Mushir Ali
    • 1
  1. 1.Department of Pharmaceutics, Faculty of PharmacyHamdard UniversityNew DelhiIndia

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