Research Article
Employing Co-grinding Technique for Improving Cefpodoxime Proxetil Dissolution Characteristics
Nouran Abdel Kader*
Issue:
Volume 9, Issue 2, December 2025
Pages:
37-52
Received:
21 May 2025
Accepted:
16 June 2025
Published:
21 July 2025
Abstract: Cefpodoxime Proxetil (CP) is an oral prodrug. Its extremely poor solubility in the biological fluids, is what causes its poor bioavailability. And since dissolution is rate-limiting stage in attaining the required bioavailability, co-grinding technique was exploited, it comprises grinding the medicine with excipients (one or more excipients) to create nanoparticles. Formulations were prepared by dry co-grinding technique, for different durations 5, 10 and 20 minutes either alone or with the selected carrier using mortar and pestle. Different premixes of CP as binary or ternary mixtures using fixed concentration of the API (260mg of CP equivalent to 200mg Cefpodoxime base) along with various ratios of other additives. Carriers used were Aerosil 200, Glycine, polyvinylpyrrolidone (PVP) K25 and HPMC E6. The prepared formulations were characterized through dissolution testing, FTIR and DSC techniques. Dissolution parameters such as dissolution efficiency (DE%), amount released after 5 minutes (Q5) and 60 minutes (Q60) were calculated. Statistical evaluation covering student’s T-test, f1, dissimilarity factor and f2, similarity factor was calculated. The findings from the binary mixtures of CP with Aerosil 200 has shown to be very promising, and hence, ternary mixtures of the CP/Aerosil 200 and one of the three carriers -namely, glycine, PVP K25 and HPMC E6- at the ratio of 1:1:1, were separately co-grounded to give mixtures where Q5 ranged from 60% – 68%, Q60 ranged from 80 to 100% and DE% ranged from 67-82%. These results are suggested augmenting effect of the large surface area of Aerosil 200 and the hydrophilic nature of the other carriers. Upon decreasing the weight ratios of Aerosil 200 and other carriers to 1:0.25:0.5, PVP K25 was the most effective tested polymer in terms of improving drug dissolution rate at the lowest weight ratio.
Abstract: Cefpodoxime Proxetil (CP) is an oral prodrug. Its extremely poor solubility in the biological fluids, is what causes its poor bioavailability. And since dissolution is rate-limiting stage in attaining the required bioavailability, co-grinding technique was exploited, it comprises grinding the medicine with excipients (one or more excipients) to cre...
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Research Article
Development of a Capsule Formulation Containing Dry Bark Extract of Annickia Polycarpa: Laboratory to Pilot Scale-up
Issue:
Volume 9, Issue 2, December 2025
Pages:
53-63
Received:
9 August 2025
Accepted:
20 August 2025
Published:
11 September 2025
DOI:
10.11648/j.pst.20250902.12
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Abstract: This study focuses on the development and scale-up of a capsule formulation based on the dry extract of Annickia polycarpa bark, a West African medicinal plant known for its antimalarial, antibacterial, and antioxidant properties. The objective was to adapt the process, initially optimized at laboratory scale, to a pilot scale for pharmaceutical valorization. Hot maceration followed by drying yielded a higher extraction rate at pilot scale (24%) compared to laboratory scale (18.46%). Powder characterization revealed very fine particles (Dx50 < 125 µm), residual moisture within pharmacopeial limits (4%), and good solubility (100-200 g/L). However, the powders exhibited poor flowability, requiring wet granulation with pregelatinized starch or carboxymethylcellulose as binders. This step significantly improved flow properties and particle cohesion. Capsules produced from the granules met uniformity of mass requirements according to the European Pharmacopeia and displayed a rapid disintegration time (< 7 minutes), ensuring efficient release of active compounds. The human equivalent dose (HED), extrapolated from animal studies, was estimated at 3,402 mg/day for a 70 kg adult, allowing the definition of capsule size 2 with 247-296 mg of extract per unit. Overall, these findings demonstrate the technical feasibility and robustness of the encapsulation process for Annickia polycarpa, providing promising perspectives for industrial development and the production of standardized phytomedicines. However, further studies on long-term stability, bioavailability, and clinical efficacy are required to ensure the quality, safety, and therapeutic effectiveness of the final product.
Abstract: This study focuses on the development and scale-up of a capsule formulation based on the dry extract of Annickia polycarpa bark, a West African medicinal plant known for its antimalarial, antibacterial, and antioxidant properties. The objective was to adapt the process, initially optimized at laboratory scale, to a pilot scale for pharmaceutical va...
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