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• To formulate and evaluate hydrogel of
  moxifloxain & ketorolac in view of
  increasing precorneal residence time &
  bioavailability of drugs
• Ion sensitive (sodium alginate), temperature
  sensitive ( poloxamer)
• HPMC as viscosity enhancing agent.
1)Literature survey
2)Collection of drugs, polymers & other
  exicipents.
3)Standardization of drugs
4)Formulation development
A. Preformulation studies
Identification
1) Determination of melting point
2) Solubility – water ,ethanol, acetone,2-propanol
3) IR spectroscopy- comparison of sample with
   standard
4) Compatibility study
B.Selection of vehicle
C.Formulation optimization by factorial design
D.Methods for in situ hydrogel preparation
•   Moxifloxacin
•   Ketorolac                        •   Electronic balance
•   Sodium alginate                  •   Magentic stirrer
•   Poloxamer                        •   Digital pH meter
•   HPMC                             •   Brookfield viscometer
•   Sodium hydroxide                 •   UV-visible spectrophotometer
•   Hydrochloric acid                •   Autoclave
•   Potassium dihydrogen phosphate   •   Incubator
•   Disodium hydrogen phosphate      •   Open end tube
•   Glacial acetic acid              •   FI-IR spectrometer
•   Ammonium acetate
•   Citric acid monohydrate
Optimization by factorial design
Gelling     Sl no   Formulation   Variable    level   Actual
agent               code          in coded   form     units
                                     X1        X2       X1     X2(%w/v)
                                                      (%w/v)
Sodium        1           F1          -1       +1         1       1.0
alginate
              2           F2         +1        -1        3        0.5
              3           F3          -1       -1        1        0.5
              4           F4         +1        +1        3        1.0
poloxamer     5           F5          -1       +1        15       1.0
              6           F6         +1        -1        25       0.5
              7           F7          -1       -1        15       0.5
              8           F8         +1        +1        25       1.0
D. Evaluation parameters

   Appearance
   pH
   Invitro gelation studies
   Rheological studies
   Drug content
   In vitro release studies
   Sterility
   Ocular irritation studies
   Stability studies
1.Robertson SM, Curtis MA, Schlech BA, Rusinko A, Owen GR, Dembinska O et
al. Ocular pharmacokinetics of moxifloxacin after topical treatment of animals
and humans. Surv Ophthalmol 2005;50:S32–S45.
2. Mcgee DH, Holt WF, Kastner PR, Rice RL. Safety of moxifloxacin as shown in
animal and in vitro studies. Surv ophthol 2005;50(6):S46-S53.
3. Mason BL, Alfonso EC, Miller D. In-use study of potential bacterial
contamination of ophthalmic moxifloxacin. J Cataract Refract Surg
2005;31:1773–6.
4. Silver LH, Woodside AM, Montgomery DB. Clinical safety of moxifloxacin
ophthalmic solution 0.5% (vigamox) in pediatric and nonpediatric patients with
bacterial conjunctivitis. Surv Ophthalmol 2005;50:S55–S63.
5. Kowalski RP, Dhaliwal DK, Karenchak LM, Romanowsk EG, Mah FS,
Ritterband DC. Gatifloxacin and moxifloxacin: an in vitro susceptibility
comparison to levofloxacin, ciprofloxacin, and ofloxacin using bacterial keratitis
isolates. Am J Ophthalmol 2003;136:500–5.
6. Burka JM, Bower KS, vanroeke CR, Stutzman RD, Kuzmowych CP, Howard RS.
The effect of fourth-generation fluoroquinolones gatifloxacin and moxifloxacin on
epithelial healing following photorefractive keratectomy. Am J Ophthalmol
2005;140:83–7.
7. Solomon R, Donnenfeld ED, Perry HD, Snyder RW, Nedrud C, Stein J.
Penetration of topically applied gatifloxacin 0.3%, moxifloxacin 0.5%, and
ciprofloxacin 0.3% into the aqueous humor. Ophthalmology 2005;112:466-9.
8. Patel UL, Chotai NP, Nagda CD, Patel MP, Patel KN. Formulation and in vitro
evaluation of moxifloxacin hydrochloride ophthalmic inserts. Int J Pharm Res
2009;1(1):23-30.
9. Edsman K, Carlfors J, Petersson R . Rheological evaluation of poloxamer as an in
situ gel for ophthalmic use. Eur J Pharm Sci 1998;6:105–12.
10. Gil HJ, Hyun I, Chi SC. Release of flurbiprofen from poloxamer 407 gel. Arch
Pharm Res 1994;17(4):240-43.
Thank you

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insitu hydrogel

  • 2.
  • 3. • To formulate and evaluate hydrogel of moxifloxain & ketorolac in view of increasing precorneal residence time & bioavailability of drugs • Ion sensitive (sodium alginate), temperature sensitive ( poloxamer) • HPMC as viscosity enhancing agent.
  • 4. 1)Literature survey 2)Collection of drugs, polymers & other exicipents. 3)Standardization of drugs 4)Formulation development
  • 5. A. Preformulation studies Identification 1) Determination of melting point 2) Solubility – water ,ethanol, acetone,2-propanol 3) IR spectroscopy- comparison of sample with standard 4) Compatibility study B.Selection of vehicle C.Formulation optimization by factorial design D.Methods for in situ hydrogel preparation
  • 6. Moxifloxacin • Ketorolac • Electronic balance • Sodium alginate • Magentic stirrer • Poloxamer • Digital pH meter • HPMC • Brookfield viscometer • Sodium hydroxide • UV-visible spectrophotometer • Hydrochloric acid • Autoclave • Potassium dihydrogen phosphate • Incubator • Disodium hydrogen phosphate • Open end tube • Glacial acetic acid • FI-IR spectrometer • Ammonium acetate • Citric acid monohydrate
  • 7. Optimization by factorial design Gelling Sl no Formulation Variable level Actual agent code in coded form units X1 X2 X1 X2(%w/v) (%w/v) Sodium 1 F1 -1 +1 1 1.0 alginate 2 F2 +1 -1 3 0.5 3 F3 -1 -1 1 0.5 4 F4 +1 +1 3 1.0 poloxamer 5 F5 -1 +1 15 1.0 6 F6 +1 -1 25 0.5 7 F7 -1 -1 15 0.5 8 F8 +1 +1 25 1.0
  • 8. D. Evaluation parameters  Appearance  pH  Invitro gelation studies  Rheological studies  Drug content  In vitro release studies  Sterility  Ocular irritation studies  Stability studies
  • 9. 1.Robertson SM, Curtis MA, Schlech BA, Rusinko A, Owen GR, Dembinska O et al. Ocular pharmacokinetics of moxifloxacin after topical treatment of animals and humans. Surv Ophthalmol 2005;50:S32–S45. 2. Mcgee DH, Holt WF, Kastner PR, Rice RL. Safety of moxifloxacin as shown in animal and in vitro studies. Surv ophthol 2005;50(6):S46-S53. 3. Mason BL, Alfonso EC, Miller D. In-use study of potential bacterial contamination of ophthalmic moxifloxacin. J Cataract Refract Surg 2005;31:1773–6. 4. Silver LH, Woodside AM, Montgomery DB. Clinical safety of moxifloxacin ophthalmic solution 0.5% (vigamox) in pediatric and nonpediatric patients with bacterial conjunctivitis. Surv Ophthalmol 2005;50:S55–S63. 5. Kowalski RP, Dhaliwal DK, Karenchak LM, Romanowsk EG, Mah FS, Ritterband DC. Gatifloxacin and moxifloxacin: an in vitro susceptibility comparison to levofloxacin, ciprofloxacin, and ofloxacin using bacterial keratitis isolates. Am J Ophthalmol 2003;136:500–5.
  • 10. 6. Burka JM, Bower KS, vanroeke CR, Stutzman RD, Kuzmowych CP, Howard RS. The effect of fourth-generation fluoroquinolones gatifloxacin and moxifloxacin on epithelial healing following photorefractive keratectomy. Am J Ophthalmol 2005;140:83–7. 7. Solomon R, Donnenfeld ED, Perry HD, Snyder RW, Nedrud C, Stein J. Penetration of topically applied gatifloxacin 0.3%, moxifloxacin 0.5%, and ciprofloxacin 0.3% into the aqueous humor. Ophthalmology 2005;112:466-9. 8. Patel UL, Chotai NP, Nagda CD, Patel MP, Patel KN. Formulation and in vitro evaluation of moxifloxacin hydrochloride ophthalmic inserts. Int J Pharm Res 2009;1(1):23-30. 9. Edsman K, Carlfors J, Petersson R . Rheological evaluation of poloxamer as an in situ gel for ophthalmic use. Eur J Pharm Sci 1998;6:105–12. 10. Gil HJ, Hyun I, Chi SC. Release of flurbiprofen from poloxamer 407 gel. Arch Pharm Res 1994;17(4):240-43.