Aim The aim of the present study was to prepare tablets which can rapidlydisintegrate in saliva, containing active ingredient in high dose (37.5% W/W). Methods Rapidlydisintegrating tablets containing rotundine were p...Aim The aim of the present study was to prepare tablets which can rapidlydisintegrate in saliva, containing active ingredient in high dose (37.5% W/W). Methods Rapidlydisintegrating tablets containing rotundine were prepared by direct compression, wet granulation andmoulding, respectively . Different disintegrants and excipients were decided by single factor test.The typical disintegration time measurement and a new method of wetting time measuring wereintroduced for assessing rapidly disintegrating tablets. Results The tablets (80 mg) prepared bydirect compression have the crushing strength of 4.0 kg ?mm^(-2) and rapidly disintegratewithin 15 s in the saliva of healthy volunteers; the tablets prepared by wet granulation also havesufficient strength, a little longer but acceptable disintegration time (within 25 s in saliva) ;and the tablets obtained by moulding show disintegration within 40 s in saliva but low strength (2kg·mm^(-2)) . Disintegration time profiles of tablets are similar to those of wetting time, and thedisintegration and wetting times in vitro are similar to the disintegration time in vivo, thelatter having higher correlation with that in oral cavity. Conclusion The rapidly disintegratingtablets can be prepared by using these three techniques and excipients. Both in vitro disintegrationtime and wetting time are necessary indexes for judgment of in vitro disintegration profile.展开更多
Hydroxypropyl starch(HPS)is widely used in various applications due to its unique functional properties,but optimizing its molecular characteristics for specific applications remains a challenge.This study aimed to op...Hydroxypropyl starch(HPS)is widely used in various applications due to its unique functional properties,but optimizing its molecular characteristics for specific applications remains a challenge.This study aimed to optimize the process parameters for producing HPS capsules with desirable molecular and performance properties.The mass fraction of the etherification reagent,reaction pH,reaction temperature,and reaction duration were controlled to create HPS with varying degrees of substitution(DS).Acid solution degradation was used to prepare HPS of varying molecular weights(MW),and cold-gelation was employed to prepare hollow HPS capsules.A rigorous evaluation of performance indicators was conducted,and response surface methodology(RSM)was used to examine the effects of solid content,MW,and dipping temperature on capsule performance.Experimental results showed that these factors influenced performance in the following order:solid content>molecular weight>dipping temperature.Optimal parameters were identified as a solid content of 18%,an MW of 77 kDa,and a dipping temperature of 57℃,yielding capsules with a wall thickness of 0.086 mm,a disintegration time of 328 s,and moisture absorption of 8.594%.These findings provide valuable insights for the tailored design of HPS capsules,which could enhance their utility in industrial applications.展开更多
文摘Aim The aim of the present study was to prepare tablets which can rapidlydisintegrate in saliva, containing active ingredient in high dose (37.5% W/W). Methods Rapidlydisintegrating tablets containing rotundine were prepared by direct compression, wet granulation andmoulding, respectively . Different disintegrants and excipients were decided by single factor test.The typical disintegration time measurement and a new method of wetting time measuring wereintroduced for assessing rapidly disintegrating tablets. Results The tablets (80 mg) prepared bydirect compression have the crushing strength of 4.0 kg ?mm^(-2) and rapidly disintegratewithin 15 s in the saliva of healthy volunteers; the tablets prepared by wet granulation also havesufficient strength, a little longer but acceptable disintegration time (within 25 s in saliva) ;and the tablets obtained by moulding show disintegration within 40 s in saliva but low strength (2kg·mm^(-2)) . Disintegration time profiles of tablets are similar to those of wetting time, and thedisintegration and wetting times in vitro are similar to the disintegration time in vivo, thelatter having higher correlation with that in oral cavity. Conclusion The rapidly disintegratingtablets can be prepared by using these three techniques and excipients. Both in vitro disintegrationtime and wetting time are necessary indexes for judgment of in vitro disintegration profile.
文摘Hydroxypropyl starch(HPS)is widely used in various applications due to its unique functional properties,but optimizing its molecular characteristics for specific applications remains a challenge.This study aimed to optimize the process parameters for producing HPS capsules with desirable molecular and performance properties.The mass fraction of the etherification reagent,reaction pH,reaction temperature,and reaction duration were controlled to create HPS with varying degrees of substitution(DS).Acid solution degradation was used to prepare HPS of varying molecular weights(MW),and cold-gelation was employed to prepare hollow HPS capsules.A rigorous evaluation of performance indicators was conducted,and response surface methodology(RSM)was used to examine the effects of solid content,MW,and dipping temperature on capsule performance.Experimental results showed that these factors influenced performance in the following order:solid content>molecular weight>dipping temperature.Optimal parameters were identified as a solid content of 18%,an MW of 77 kDa,and a dipping temperature of 57℃,yielding capsules with a wall thickness of 0.086 mm,a disintegration time of 328 s,and moisture absorption of 8.594%.These findings provide valuable insights for the tailored design of HPS capsules,which could enhance their utility in industrial applications.
