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Formulation and Delivery - Chemical

(M1030-10-58) A Comparative Study of Hypromellose Acetate Succinate and HPMCP by Spray Drying Method and Top Spray Method for Solubility Enhancement

Monday, October 21, 2024
10:30 AM – 11:30 AM MT

    Presenting Author(s)

  • SS

    Sonam Ajay Singh, M.S.

    Assistant Lab Manger
    Shin-Etsu Chemical Tylose India Pvt., Ltd.
    Mumbai, Maharashtra, India

    • Main Author(s)

  • SS

    Sonam Ajay Singh, M.S.

    Assistant Lab Manger
    Shin-Etsu Chemical Tylose India Pvt., Ltd.
    Mumbai, Maharashtra, India

    • Co-Author(s)

  • NB

    Nitin B. Bhusane, B.Sc. MBA

    Director
    Shin-Etsu Chemical Tylose India Pvt., Ltd.
    Mumbai, Maharashtra, India

  • SN

    Shrikanth Nair

    Research Intern
    Shin-Etsu Chemical Tylose India Pvt., Ltd.
    Mumbai, Maharashtra, India

Purpose: Most of the new drugs are approved for solid dispersion by spray drying using HPMCAS. But to overcome the patent issues and machine availability, different strategies need to be evaluated to prepare the solid dispersion by using different technologies like spray drying or by top spray method.

Methods: This study was divided in two strategies; first strategy to generate comparative data of different grades of Hypromellose Acetate Succinate by Spray drying and Top spray method and second strategy to generate comparative data between Hypromellose Acetate Succinate by Spray drying and HPCMP by Top spray method. In this development, Itraconazole was used as a model API with a dose of 65mg. The solvent system selected for the preparation of API and Polymer solution was Dichloromethane and Methanol in 1:1 ratio and it was kept constant for the Spray drying method and Top Spray granulation method. For the Top spray granulation process Lactose was selected as the carrier. The prepared spray dried powder and the top spray granules were further evaluated for In-vitro dissolution studies, XRD and DSC studies. When Hypromellose Acetate succinate was evaluated with all the grades by Spray Drying method it was observed that at 1:3 ratio (Drug: Polymer) resulted in a better In-vitro dissolution release and even when the spray dried granules were characterized for the DSC and XRD studies complete conversion of crystalline nature of drug to amorphous form was observed.

Results: Dissolution studies of the Spray dried powder and the Top spray granules were carried out as per the reference product where the dissolution media mentioned was Water +0.5% sodium lauryl sulphate for 2hr. Fig no.0 1represents the comparative profile within the Hypromellose Acetate Succinate grades by spray drying method. Fig no.02 represents Comparative profile of Hypromellose Acetate Succinate by spray drying and HPMCP by spray drying method. Fig no.03 represents Comparative profile of Hypromellose Acetate Succinate by spray drying and HPMCP by Top spray method

Conclusion: When Hypromellose Acetate Succinate grades were compared within the two methods i.e. Spray drying method and Top Spray method, the Spray drying method was much better. This may be mainly because the spray drying process doesn’t involve any carrier and there is interaction of the Drug and polymer at a molecular level and even the particle size achieved is much smaller which later helps in improving the solubility whereas with Top spray method carrier is required and here particle achieved are porous in nature which helps in enhancing the solubility, comparable release profile can be achieved when the ratio of Drug to Polymer is increased. The other challenge with the Top spray method will be the filled weight when the ASD needs to be converted to capsule dosage form. Whereas when the two polymer types were evaluated by i.e. Hypromellose Acetate Succinate and HPMCP by spray drying method HP-50 led to much better release profile. Spray drying of Hypromellose Acetate Succinate and Top spray of HPMCP was compared it was observed that with HP-50 the release profile was appreciable when compared to Hypromellose Acetate Succinate spray drying. Though, there is no exact replacement either for the Hypromellose Acetate Succinate or for the Spray drying technology, the Top spray method can be explored at higher concentration to get a similar release profile like Hypromellose Acetate Succinate formulation. The other positive outcome from the study was solid dispersion prepared either by the Spray drying method or by the Top spray method using Hypromellose Acetate Succinate or HPMCP led to conversion of crystalline nature of the API to the amorphous form.

Fig no.01 Comparative profile of Hypromellose Acetate Succinate by Spray drying Method and Top spray Method

Fig no.02 Comparative profile of Hypromellose Acetate Succinate by spray drying and HPMCP by spray drying method.

Fig no.03 Comparative profile of Hypromellose Acetate Succinate by spray drying and HPMCP by Top spray method