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Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

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Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules01:18

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Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...
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Biopharmaceutical Factors Influencing Drug Product Design: Overview01:22

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Rational drug product design integrates knowledge of the drug’s physicochemical properties, formulation components, manufacturing techniques, and intended route of administration. Each factor influences the drug’s performance, including how it is released, absorbed, and eliminated in the body.The physicochemical properties of a drug—such as solubility, stability, and particle size—affect its compatibility with excipients and the choice of dosage form. Excipients, though...
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Oral Drug Delivery Systems: Introduction01:23

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Oral drug delivery is the most common route of administration due to its convenience, cost-effectiveness, and high patient compliance. It enables precise formulation to ensure proper drug dosage and bioavailability. The development of oral dosage forms considers drug properties such as solubility, stability, and absorption to optimize therapeutic efficacy.Tablets, capsules, liquids, and chewable formulations enhance drug stability, mask undesirable tastes, and improve patient experience.
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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation.

Burak Çelik1

  • 1Department of Pharmaceutical Technology, Faculty of Pharmacy, Bezmialem Vakıf University, Fatih, Istanbul, Turkey.

Drug Design, Development and Therapy
|December 12, 2017
PubMed
Summary
This summary is machine-generated.

This study optimized risperidone (RIS) buccal tablets for systemic delivery. The developed mucoadhesive tablets offer a promising alternative route for schizophrenia treatment with sustained drug release.

Keywords:
Carbopolbuccal tabletscontrolled releasedrug deliverymucoadhesionquality by designrisperidonesodium alginate

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Materials Science

Background:

  • Systemic delivery of risperidone (RIS) via buccal tablets offers an alternative route.
  • Mucoadhesive buccal tablets require careful optimization of polymers and formulation for effective drug delivery.

Purpose of the Study:

  • To design and optimize mucoadhesive buccal tablets of risperidone for systemic delivery.
  • To evaluate the physicochemical properties, in vitro release, and ex vivo residence time of the optimized buccal tablets.

Main Methods:

  • Direct compression method used for tablet preparation.
  • Response surface methodology applied for optimization using Carbopol (CP) and sodium alginate (SA).
  • Evaluation of tablet hardness, ex vivo residence time, detachment force, physicochemical compatibility (FT-IR, DSC), in vitro drug release, swelling, and erosion.

Main Results:

  • Optimized formulation (16.4% CP, 20.3% SA) showed favorable ex vivo residence time (7.67±0.29 hr), hardness (45.52±4.85 N), and detachment force (2.12±0.17 N).
  • FT-IR and DSC confirmed no chemical interactions between RIS and excipients.
  • >90% RIS release achieved in 8 hours, following zero-order kinetics with anomalous (non-Fickian) release (n=0.77).

Conclusions:

  • Optimized risperidone buccal tablets are a viable alternative drug delivery system.
  • The mucoadhesive system demonstrates sustained drug release suitable for schizophrenia treatment.
  • Combined swelling and erosion mechanisms govern the drug release profile.