Development of Co-Amorphous Loratadine–Citric Acid Orodispersible Drug Formulations

Round 1

Reviewer 1 Report

This manuscript by Sipos and coworkers discloses a coamorphous system of laratadine-citric acid which shows improved solubility and faster dissolution, leading to an improved dosage form.

Overall, the manuscript is well written and tells a compelling story of process development.  The experiments are presented in appropriate detail and the conclusions are reasonable.

The manuscript should be ready for publication once the comments below are addressed:

1) Is there a known co-crystal of loratidine-citric acid?  Was this species ever detected by PXRD or DSC?  It's hard to say you don't have the material present if you haven't characterized it first.

2) Figure 1 shows a hydrogen bond from citric acid to the amide of loratadine.  How was this structure established?  Is there a crystal structure of crystalline form of this or computations?  Should the hydrogen bond be to the more basic pyridine functionality instead?

3) The FTIR data is of low quality and is very difficult to interpret.  Also, it's not clear how the complex of citric acid and loratadine would cause a an IR shift of both COOH groups (1751 cm-1).

4) pg 6, line 222:  the Amide moiety of loratadine is incorrectly described as an ester

5) There are quite a few minor grammatical errors and this could use another round of editing by a fluent English speaker.  Also, the authors need to run spell check.

 

 

 

 

Author Response

Please see the attachment

Author Response File: Author Response.docx

Reviewer 2 Report

This is an interesting study regarding the preparation and characterization of some disintregating dosage forms containing loratadine. But, some minor changes are urged to be performed.

line 2: co-amorphous is the correct word

line 53: please explain how humidity needs selective packaging (a reference would be thoughtfull)

line 77: the correct word i think it is Pharmaburst 500

lines 120-128 (2.2.3 Dissolution test): was medium was used? You mentioned first distilled water and then fresh water. I do understand something different with fresh water. Also, there is only o parenthesis at the end of the paragraph.

lines 146-147: please check the English manner of writing (the phrase has no meaning)

lines 151-153: please check the English manner of writing (the phrase has no meaning)

line 188: what version of Excel was used?

line 217: Figure 3 (without point after)

line 224: There result? Where there?

 

 

Author Response

Please see the attachment.

Author Response File: Author Response.docx