Combined eutexia and amorphization for simultaneous enhancement of dissolution rate of triamterene and hydrochlorothiazide : preparation of orodispersible tablets
BACKGROUND: Triamterene is an oral antihypertensive drug with dissolution-limited poor bioavailability. It can be used as monotherapy or in fixed dose combination with hydrochlorothiazide which also suffers from poor dissolution. Moreover, co-processing of drugs in fixed dose combination can alter their properties. Accordingly, pre-formulation studies should investigate the effect of co-processing and optimize the dissolution of drugs before and after fixed dose combination. This is expected to avoid deleterious interaction (if any) and to hasten the biopharmaceutical properties.
OBJECTIVE: Accordingly, the aim of this work was to optimize the dissolution rate of triamterene alone and after fixed dose combination with hydrochlorothiazide.
METHODOLOGY: Triamterene was subjected to dry co-grinding with xylitol, HPMC-E5 or their combination. The effect of co-grinding with hydrochlorothiazide was also tested in absence and presence of xylitol and HPMC-E5. The products were assessed using Fourier-transform infrared (FTIR), differential scanning calorimetry, X-ray powder diffraction (XRPD), in addition to dissolution studies. Optimum formulations were fabricated as oral disintegrating tablets (ODT).Results: Co-processing of triamterene with xylitol formed eutectic system which hastened dissolution rate. HPMC-E5 resulted in partial amorphization and improved triamterene dissolution. Co-grinding with both materials combined their effects. Co-processing of triamterene with hydrochlorothiazide resulted in eutexia but the product was slowly dissolving due to aggregation. This problem was vanished in presence of HPMC-E5 and xylitol. Compression of the optimum formulation into ODT underwent fast disintegration and liberated acceptable amounts of both drugs.
CONCLUSION: The study introduced simple co-processing with traditional excipients for development of ODT of triamterene and hydrochlorothiazide.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:50 |
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| Enthalten in: |
Drug development and industrial pharmacy - 50(2024), 4 vom: 17. Apr., Seite 306-319 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Awad, Hend A [VerfasserIn] |
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| Links: |
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| Themen: |
0J48LPH2TH |
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| Anmerkungen: |
Date Completed 22.04.2024 Date Revised 22.04.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1080/03639045.2024.2323996 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM36890816X |
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| 100 | 1 | |a Awad, Hend A |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Combined eutexia and amorphization for simultaneous enhancement of dissolution rate of triamterene and hydrochlorothiazide |b preparation of orodispersible tablets |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a BACKGROUND: Triamterene is an oral antihypertensive drug with dissolution-limited poor bioavailability. It can be used as monotherapy or in fixed dose combination with hydrochlorothiazide which also suffers from poor dissolution. Moreover, co-processing of drugs in fixed dose combination can alter their properties. Accordingly, pre-formulation studies should investigate the effect of co-processing and optimize the dissolution of drugs before and after fixed dose combination. This is expected to avoid deleterious interaction (if any) and to hasten the biopharmaceutical properties | ||
| 520 | |a OBJECTIVE: Accordingly, the aim of this work was to optimize the dissolution rate of triamterene alone and after fixed dose combination with hydrochlorothiazide | ||
| 520 | |a METHODOLOGY: Triamterene was subjected to dry co-grinding with xylitol, HPMC-E5 or their combination. The effect of co-grinding with hydrochlorothiazide was also tested in absence and presence of xylitol and HPMC-E5. The products were assessed using Fourier-transform infrared (FTIR), differential scanning calorimetry, X-ray powder diffraction (XRPD), in addition to dissolution studies. Optimum formulations were fabricated as oral disintegrating tablets (ODT).Results: Co-processing of triamterene with xylitol formed eutectic system which hastened dissolution rate. HPMC-E5 resulted in partial amorphization and improved triamterene dissolution. Co-grinding with both materials combined their effects. Co-processing of triamterene with hydrochlorothiazide resulted in eutexia but the product was slowly dissolving due to aggregation. This problem was vanished in presence of HPMC-E5 and xylitol. Compression of the optimum formulation into ODT underwent fast disintegration and liberated acceptable amounts of both drugs | ||
| 520 | |a CONCLUSION: The study introduced simple co-processing with traditional excipients for development of ODT of triamterene and hydrochlorothiazide | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Triamterene | |
| 650 | 4 | |a amorphization | |
| 650 | 4 | |a eutexia | |
| 650 | 4 | |a hydrochlorothiazide | |
| 650 | 4 | |a orodisintegrating | |
| 650 | 7 | |a Hydrochlorothiazide |2 NLM | |
| 650 | 7 | |a 0J48LPH2TH |2 NLM | |
| 650 | 7 | |a Triamterene |2 NLM | |
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| 650 | 7 | |a Xylitol |2 NLM | |
| 650 | 7 | |a VCQ006KQ1E |2 NLM | |
| 650 | 7 | |a Antihypertensive Agents |2 NLM | |
| 650 | 7 | |a Tablets |2 NLM | |
| 700 | 1 | |a Fetouh, Mohamed I |e verfasserin |4 aut | |
| 700 | 1 | |a Sultan, Amal A |e verfasserin |4 aut | |
| 700 | 1 | |a El Maghraby, Gamal M |e verfasserin |4 aut | |
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