(T1330-03-17) Developing Biosustane SAIB NF as a Novel Excipient for Oral Dosage Forms

Purpose: Biosustane SAIB NF is a highly hydrophobic, nonpolymeric, and novel excipient. The FDA has already approved it for parenteral administration. It is a colorless, odorless, highly viscous liquid prepared by the controlled esterification of natural sugar (sucrose) with acetic and isobutyric anhydrides. FDA already approved bupivacaine (POSIMIR ) as an injectable for extended release, which used SAIB. The high viscosity of SAIB poses challenges in handling and formulating oral dosage forms, which is an attractive, noninvasive alternative to other routes of administration. Hence, this study showed the preparation and characterization of granules using Biosustane SAIB NF and manufacturing oral dosage forms of tablets and capsules. Later, the dissolution profile was optimized for both tablets and capsules.

Methods: Biosustane SAIB NF handling and formulation are optimized by trials and errors considering granules' properties. Granules were prepared using two solvents (Ethanol & DCM), which helped dissolve the Biosustane SAIB NF following two distinct formulation strategies. Finally, the solvent evaporated from the granules using temperature in the oven. Optimized formulation granules were evaluated for flowability (Carr Index, Hausner ratio, angle of repose) and characterized by DSC, XRD, TGA, and NMR. Formulated Tablets and Capsule dissolution were checked and optimized using a super disintegrant of sodium starch glycolate (SSG) following the pH gradient dissolution methods.

Results: Based on the flowability characterization of the granules (Fig. 1A), F2 (with Biosustane) & F3 (without Biosustane) from process 1, F5 (without Biosustane) & F6 (with Biosustane) from process 2, had been selected for the DSC, XRD, TGA & NMR analysis. The peak of the Carbamazepine (CBZ) shifted due to the formulation & process, but it did not significantly change for the Biosustane SAIB NF excipients (Fig. 1B-E). Prepared tablets (100 mg CBZ) and capsules (50 mg CBZ) dissolution were checked, and it found that the capsules dissolution was more sustained than the tablet (Fig. 2A-B) due to the Biosustane SAIB NF, then dissolution was optimized by using super disintegrant (SSG) (Fig. 2C-F). Finally, the higher dissolution-optimized batches were selected for both processes and initiated stability. There are no significant changes for stability samples up to 1 month into accelerated conditions. (40 °C/75% RH) (Fig. 3A-D).

Conclusion: Current research revealed the successful development of oral dosage forms for carbamazepine as a model drug using Biosustane SAIB NF as a novel excipient.


Figure 1: Granules Characterized by A. Flow ability of granules, B.DSC, C.XRD, D.TGA & E. NMR


Figure 2: Dissolution of the A. F2,F3,F5,F6 Tablets, B. F2,F3,F5,F6 Capsules & Optimization the dissolution profile by using SSG (C-F)


Figure 3: Stability 1M Samples evaluation by using DSC (A-B) & dissolution profile comparison (C-D)