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FORMULATION OF A FAST-FORMULATION OF A FAST-DISSOLVING KETOPROFEN DISSOLVING KETOPROFEN

LYOPHILIZED TABLETLYOPHILIZED TABLET

I.S. Ahmed a,*, M.M. Nafadi a, F.A. I.S. Ahmed a,*, M.M. Nafadi a, F.A. Fatahalla bFatahalla b

a Department of Pharmaceutics and Industrial a Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Pharmacy, Faculty of Pharmacy, Cairo University,

Egypt.Egypt.b National Organization for Drug Control and b National Organization for Drug Control and

Research, Cairo, Egypt.Research, Cairo, Egypt.

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AIM OF WORKAIM OF WORK The objective of the current The objective of the current work was the improvement of work was the improvement of the solubility and dissolution the solubility and dissolution rate of poorly water-soluble rate of poorly water-soluble ketoprofen by formulating a ketoprofen by formulating a fast-dissolving tablet of fast-dissolving tablet of ketoprofen using highly water ketoprofen using highly water soluble materials and a soluble materials and a freeze-drying technique.freeze-drying technique.

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METHOD OF METHOD OF PREPARATIONPREPARATION

The tablet was prepared by mixing The tablet was prepared by mixing ketoprofen with highly soluble ketoprofen with highly soluble carrier materials namely gelatin, carrier materials namely gelatin, glycine and sorbitol. The suspension glycine and sorbitol. The suspension was poured in blisters packs and was poured in blisters packs and freeze dried in a Novalyphe- NL 500 freeze dried in a Novalyphe- NL 500 Freeze Dryer.Freeze Dryer.

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CONCLUSIONCONCLUSION•We demonstrated that a lyophilized We demonstrated that a lyophilized

ketoprofen tablet made of widely used, ketoprofen tablet made of widely used, safe, water-soluble excipients showed much safe, water-soluble excipients showed much better solubility and much faster dissolution better solubility and much faster dissolution when compared to the plain drug or the PM. when compared to the plain drug or the PM. These results were attributed to the These results were attributed to the formation of an amorphous state of the formation of an amorphous state of the drug in the porous lyophilized matrix. Such drug in the porous lyophilized matrix. Such dosage form could be very beneficial for dosage form could be very beneficial for use in pediatric and geriatric patients and use in pediatric and geriatric patients and those patients who find it difficult to those patients who find it difficult to swallow tablets and capsulesswallow tablets and capsules..

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RESULTS AND DISCUSSIONRESULTS AND DISCUSSIONSolubility StudiesSolubility Studies

Table 1 Solubility of ketoprofen as a plain drug, in LT, and PM in distilled water at 25ºC

Ketoprofen w/v (%) Form of drug Solubility (% SD) 0.1 LT 0.058% 0.018 0.1 PM 0.031% 0.012 0.1 plain drug 0.021% 0.006

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RESULTS AND DISCUSSIONRESULTS AND DISCUSSIONDissolution StudiesDissolution Studies

Dissolution profiles of LT, PM, and ketoprofen powder in distilled water at 37ºC. N = 3 with SD.

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RESULTS AND DISCUSSIONRESULTS AND DISCUSSIONDSC StudiesDSC Studies

(1)

(2)

(3)

DSC thermograms of LT (1), PM (2), and ketoprofen (3).

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RESULTS AND DISCUSSIONRESULTS AND DISCUSSION

XRDXRD(1)

(2)

(3)

Powder X-ray diffraction spectra of LT (1), PM (2), and ketoprofen (3).

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RESULTS AND DISCUSSIONRESULTS AND DISCUSSION

SEMSEM

Figure 4. SEM micrographs of ketoprofen (1), PM (2), and LT (3).

(1) (2) (3)

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•Drug Development and Industrial Pharmacy Publisher:  Taylor & Francis Issue:  Volume 32, Number 4 / 2006 Pages:  437 - 442