Related Experiment Video
Updated: Mar 20, 2026
05:45
Author Spotlight: Process Development for the Spray-Drying of Probiotic Bacteria and Evaluation of the Product Quality
Published on: April 7, 2023
4.5K
Formulation Development, Process Optimization, and In Vitro Characterization of Spray-Dried Lansoprazole Enteric
Chintan Vora1, Riddhish Patadia1, Karan Mittal1
1Pharmacy Department, Faculty of Technology and Engineering, The M.S. University of Baroda, Kalabhavan, Vadodara-390001, Gujarat State, India.
Scientia Pharmaceutica
|May 26, 2016
Summary
Spray drying efficiently creates enteric microparticles of lansoprazole (LPZ). Eudragit S 100 provided superior gastric resistance, while plasticizers negatively impacted stability.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Developing enteric-coated drug delivery systems is crucial for protecting acid-labile drugs and ensuring targeted release in the intestine.
- Lansoprazole (LPZ) is a proton pump inhibitor susceptible to degradation in the stomach.
Purpose of the Study:
- To develop single-step enteric microparticles of lansoprazole using spray drying.
- To investigate the impact of formulation and process variables on entrapment efficiency and in vitro gastric resistance.
Main Methods:
- Spray drying technique was employed for microparticle fabrication.
- Various Eudragit polymers (S 100, L 100-55, L 100), plasticizers (triethyl citrate), and polymer combinations (sodium alginate, glyceryl behenate) were evaluated.
- Process parameters including inlet temperature, atomizing air pressure, feed concentration, feed rate, and aspirator volume were optimized.
- Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD) were used for characterization.
- Stability studies were conducted according to ICH Q1A(R2) guidelines.
Main Results:
- Eudragit S 100 demonstrated superior gastric resistance compared to other Eudragit polymers due to its higher pH threshold.
- Incorporation of plasticizers significantly reduced gastric resistance.
- Polymer combinations with sodium alginate improved gastric resistance, while glyceryl behenate did not show significant impact.
- Optimized process parameters yielded spherical microparticles with smooth morphology.
- Drug analysis confirmed an amorphous state within the microparticles.
- The developed microparticles exhibited good stability under accelerated and long-term conditions.
Conclusions:
- Spray drying is a viable single-step method for producing stable, enteric-coated lansoprazole microparticles.
- Eudragit S 100 is the preferred polymer for achieving high gastric resistance.
- Optimized formulation and process parameters are critical for enhancing entrapment efficiency and drug stability.
Related Concept Videos
01:18Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules
400
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...
400
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
740
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...
740
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
1.9K
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
1.9K
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
213
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,...
213
01:16Bioavailability Enhancement: Drug Solubility Enhancement
419
Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
419
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
300
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...
300