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Pharmaceutical Drug Regulatory Affairs Journal Research Article 1 min read

Piperine: An Effective Bioenhancer for Drug Absorption

Singh S*
* Corresponding author
ISSN: 2642-6315  10.23880/pdraj-16000126  Received: November 22, 2021  Published: November 26, 2021
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 13 references
 1 figure
 1 table
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Figures

Figure 1: Structure of piperine.
Click to enlarge
Figure 1: Structure of piperine.

Tables

Mechanism of Action
Piperine and RifampicinPiperine augments transcription inhibitory activity of rifampicin by several folds against Mycobacterium smegmatis. Combining piperine with rifampicin decreased the dose of rifampicin from 450 to 200 mg.
Piperine and ResveratrolEffect of piperine on oral bioavailability of resveratrol was studied in mice and the study demonstrated that piperine significantly improves the in-vivo bioavailability of resveratrol
Piperine with Propranolol and TheophyllineThe effects of piperine on the bioavailability an pharmacokinetics of propranolol and theophylline were studied. An earlier tmax and a higher Cmax and AUC were observed in the subjects who received piperine and propranolol. It produced a higher Cmax, longer t1/2, and a higher AUC with theophylline.
Piperine and Coenzyme Q10In a double-blind study, it is postulated that the bioenhancing mechanism of piperine to increase plasma levels of supplemental coenzyme Q10 is nonspecific and possibly based on its description in the literature as a thermonutrient
Piperine and β-CaroteneThe effectiveness of piperine was evaluated for its ability to improve serum response of β-carotene during oral supplementation using a double-blind, crossover study design. Study suggested that the serum response during oral β-carotene supplementation is improved through the nonspecific, thermogenic property of piperine
Piperine and CurcuminInfluence of piperine on the pharmacokinetics of curcumin in animals and human volunteers was studied. Piperine, a known inhibitor of hepatic and intestinal glucuronidation, enhanced the serum concentration, extent of absorption, and bioavailability of curcumin in both rats and humans with no adverse effects.
Piperine and Aflatoxin B1Piperine enhances bioavailability of aflatoxin B1 in rat tissues. A 10 mg dose of piperine causes a marked increase in serum gonadotropins and a decrease in intratesticular testosterone concentration, despite normal serum testosterone titres in adult male albino rats.
Piperine and PentobarbitoneEffect of piperine on pentobarbitone-induced hypnosis in rats was studied. Piperine treatment in rats, treated chronically with phenobarbitone, significantly potentiated pentobarbitone sleeping time, as compared to the controls There was no alteration in barbital sodium sleeping time. It is possible that piperine inhibits liver microsomal enzyme system and thereby potentiates the pentobarbitone sleeping time.
Piperine and PhenytoinEffect of piperine on pharmacokinetics of phenytoin was studied in healthy volunteers. The results of a crossover study, showed that a single daily dose of piperine for 7 days decreased the t1/2α (P<0.05), prolonged the t1/2 (P<0.01), and produced a higher AUC (P<0.05) in comparison to phenytoin alone.

Table 1: Some examples of bioavailability enhancement of various drugs by piperine.

References

  1. Patil UK, Singh A, Chakraborty AK (2011) Role of piperine as a bioavailability enhancer. Int J Recent Adv Pharm Res 4: 16-23.
  2. (1991) Ministry of Health and Family Welfare (CSIR), Government of India, 5th (edn), Indian Pharmacopoeia Volume I, Delhi, pp: 10-14.
  3. Annamalai AR, Manavalan R (1990) Effect of Trikatu and its Individual Components and piperine on gastrointestinal tracts: Trikatu- a bioavailability enhancer. Indian Drugs 27(12): 595- 604.
  4. Atal CK, Dhar KL, Singh J (1975) The Chemistry of Indian Piper Species. Lyodia 38(3): 256-259.
  5. Raj KPS, Nagarsheth HK (1992) Pepper. Indian Drugs 16(1): 199-203.
  6. Peterson B, Weyers M , Steenekamp JH, Steyn JD, Gouws C, et al. (2019) Drug Bioavailability Enhancing Agents of Natural Origin (Bioenhancers) that Modulate Drug Membrane Permeation and Pre-Systemic Metabolism. Pharmaceutics 11(1): 33.
  7. Alexander A, Qureshi A, Kumari L, Vaishnav P, Sharma M, et al. (2014) Role of herbal bioactives as a potential bioavailability enhancer for active pharmaceutical ingredients. Fitoter 97: 1-14.
  8. Bhardwaj RK, Glaeser H, Becquemont L, Klotz U, Gupta SK, et al. (2002) Piperine, a major constituent of black pepper, inhibits human p-glycoprotein and cyp3a4. J Pharmacol Exp Ther 302(2): 645-650.
  9. Ahmad N, Fazal H, Abbasi BH, Farooq S, Ali M, et al. (2012) Biological role of piper nigrum l.(black pepper): A review. Asian Pac J Trop Biomed 2(3): S1945–S1953.
  10. Singh A, Amardeep (2011) Piperine: A Bioenhancer. Int J Pharmacy Res Technol 1(1): 01-05.
  11. Mhaske DB, Sreedharan S, Mahadik KR (2018) Role of Piperine as an Effective Bioenhancer in Drug Absorption 9: 7.
  12. Javed S, Ahsan W, Kohli K (2016) The concept of bioenhancers in bioavailability enhancement of drugs – a patent review. J Sci let 1(3): 143-165.
  13. Majeed M, Badmaev V, Rajendran R (1998) Use of piperine as a bioavailability enhancer US5744161, pp: 1-17.
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@article{singh2021,
  title   = {Piperine: An Effective Bioenhancer for Drug Absorption},
  author  = {Singh S},
  journal = {Pharmaceutical Drug Regulatory Affairs Journal},
  year    = {2021},
  volume  = {4},
  number  = {1},
  doi     = {10.23880/pdraj-16000126}
}
Singh S (2021). Piperine: An Effective Bioenhancer for Drug Absorption. Pharmaceutical Drug Regulatory Affairs Journal, 4(1). https://doi.org/10.23880/pdraj-16000126
TY  - JOUR
TI  - Piperine: An Effective Bioenhancer for Drug Absorption
AU  - Singh S
JO  - Pharmaceutical Drug Regulatory Affairs Journal
PY  - 2021
VL  - 4
IS  - 1
DO  - 10.23880/pdraj-16000126
ER  -